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WO2025019599A2 - Composés bifonctionnels de liaison à la kinase et leurs utilisations - Google Patents

Composés bifonctionnels de liaison à la kinase et leurs utilisations Download PDF

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Publication number
WO2025019599A2
WO2025019599A2 PCT/US2024/038400 US2024038400W WO2025019599A2 WO 2025019599 A2 WO2025019599 A2 WO 2025019599A2 US 2024038400 W US2024038400 W US 2024038400W WO 2025019599 A2 WO2025019599 A2 WO 2025019599A2
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substituted
unsubstituted
formula
certain embodiments
compound
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WO2025019599A3 (fr
Inventor
Florence Fevrier WAGNER
Alexander W. HIRD
Moses Moustakim
Julia N. DOOLEY
Angela M. ZAINO
Alexandria P. TAYLOR
Jae Young Ahn
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Photys Therapeutics Inc
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Photys Therapeutics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Definitions

  • Kinase dysfunction is also associated with a variety of human diseases including, but not limited to, cancer, inflammatory conditions, autoimmune disorders, and cardiovascular diseases.
  • Agents that block protein phosphorylation via kinase inhibition have had a transformative impact in basic science and medicine.
  • agents that can both engage a kinase and one or more other target substrates of interest (e.g., proteins) to be phosphorylated may also be useful as a means of evoking desired attributes or responses from those target substrates.
  • AMPK 5'-AMP-activated protein kinase
  • the net effect of AMPK activation includes stimulation of hepatic fatty acid oxidation, ketogenesis, stimulation of skeletal muscle fatty acid oxidation and glucose uptake, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipogenesis, inhibition of adipocyte lipolysis, and modulation of insulin secretion by pancreatic ⁇ -cells.
  • PHICS phosphorylation-inducing chimeric small molecules
  • One of the small molecule moieties is designed to bind to a target protein while the other small molecule moiety binds to a protein kinase.
  • the PHICS selectively binds to the target substrate of interest and simultaneously binds to and recruits a specific kinase to phosphorylate the target substrate. The PHICS may then dissociate from the target substrate and initiate another catalytic cycle.
  • Phosphorylation (native or neo) of any given target substrate e.g., a protein
  • PHICS compounds which enable a kinase (e.g., AMPK) to phosphorylate target substrates, including substrates that may not normally be substrates for the kinase, thus providing new modes to induce substrate alterations via strategic phosphorylation in a variety of settings.
  • bifunctional compounds that comprise a first functional moiety that engages AMPK and a second functional moiety that comprises a detectable moiety (e.g., a chromophore, dye, fluorophore, luminophore or luminescent material, or radioactive material) joined together by a linker.
  • a detectable moiety e.g., a chromophore, dye, fluorophore, luminophore or luminescent material, or radioactive material
  • the present disclosure provides new compounds, compositions, kits, uses, and methods for modulating a target substrate (e.g., protein) via proximity-induced engagement between AMPK and a target substrate.
  • a target substrate e.g., protein
  • a target substrate e.g., protein
  • a target substrate e.g., protein
  • V 1 is CR 2 or N
  • each of R 2 , R 3 , and R 4 is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -CN, -N(R A ) 2
  • V 1 is N or CR 2 ; each of R 2 , R 3 , and R 4 is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -N(R A ) 2 , -OR A , or -SR A ; R 5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted acyl, or a nitrogen protecting group; R 6
  • a target substrate e.g., protein
  • the method comprising administering a compound of the disclosure, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, or a pharmaceutical composition comprising a compound of the disclosure, to a mixture that comprises AMPK and the target substrate.
  • a target substrate e.g., protein
  • AMPK phosphorylation of a target substrate
  • the method comprising contacting the target substrate with a compound of the disclosure, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, or a pharmaceutical composition comprising a compound of the disclosure.
  • a protein kinase in another aspect, provided are methods of modulating a protein kinase, the method comprising contacting the protein kinase with a compound of the disclosure, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, or a pharmaceutical composition comprising a compound of the disclosure.
  • the protein kinase is AMPK.
  • kits comprising a compound of the disclosure, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, or a pharmaceutical composition comprising a compound of the disclosure.
  • the kit further comprises instructions for administration and/or use.
  • Compounds described herein can comprise one or more asymmetric centers, and thus can exist in various stereoisomeric forms, e.g., enantiomers and/or diastereomers.
  • the compounds described herein can be in the form of an individual enantiomer, diastereomer or geometric isomer, or can be in the form of a mixture of stereoisomers, including racemic mixtures and mixtures enriched in one or more stereoisomer.
  • Isomers can be isolated from mixtures by methods known to those skilled in the art, including chiral high pressure liquid chromatography (HPLC) and the formation and crystallization of chiral salts; or preferred isomers can be prepared by asymmetric syntheses.
  • HPLC high pressure liquid chromatography
  • C1-6 alkyl is intended to encompass C1, C2, C3, C4, C5, C6, C1-6, C 1-5 , C 1-4 , C 1-3 , C 1-2 , C 2-6 , C 2-5 , C 2-4 , C 2-3 , C 3-6 , C 3-5 , C 3-4 , C 4-6 , C 4-5 , and C 5-6 alkyl.
  • aliphatic refers to alkyl, alkenyl, alkynyl, and carbocyclic groups.
  • heteroaliphatic refers to heteroalkyl, heteroalkenyl, heteroalkynyl, and heterocyclic groups.
  • alkyl refers to a radical of a straight-chain or branched saturated hydrocarbon group having from 1 to 10 carbon atoms (“C 1-10 alkyl”). In some embodiments, an alkyl group has 1 to 9 carbon atoms (“C1-9 alkyl”). In some embodiments, an alkyl group has 1 to 8 carbon atoms (“C 1-8 alkyl”). In some embodiments, an alkyl group has 1 to 7 carbon atoms (“C 1-7 alkyl”). In some embodiments, an alkyl group has 1 to 6 carbon atoms (“C 1-6 alkyl”). In some embodiments, an alkyl group has 1 to 5 carbon atoms (“C 1-5 alkyl”).
  • an alkyl group has 1 to 4 carbon atoms (“C 1-4 alkyl”). In some embodiments, an alkyl group has 1 to 3 carbon atoms (“C 1-3 alkyl”). In some embodiments, an alkyl group has 1 to 2 carbon atoms (“C 1-2 alkyl”). In some embodiments, an alkyl group has 1 carbon atom (“C1 alkyl”). In some embodiments, an alkyl group has 2 to 6 carbon atoms (“C 2-6 alkyl”).
  • C 1-6 alkyl groups include methyl (C 1 ), ethyl (C 2 ), propyl (C 3 ) (e.g., n-propyl, isopropyl), butyl (C 4 ) (e.g., n- butyl, tert-butyl, sec-butyl, iso-butyl), pentyl (C5) (e.g., n-pentyl, 3-pentanyl, amyl, neopentyl, 3- methyl-2-butanyl, tertiary amyl), and hexyl (C6) (e.g., n-hexyl).
  • alkyl groups include n-heptyl (C 7 ), n-octyl (C 8 ), and the like. Unless otherwise specified, each instance of an alkyl group is independently unsubstituted (an “unsubstituted alkyl”) or substituted (a “substituted alkyl”) with one or more substituents (e.g., halogen, such as F).
  • substituents e.g., halogen, such as F
  • the alkyl group is an unsubstituted C1-10 alkyl (such as unsubstituted C1-6 alkyl, e.g., ⁇ CH3 (Me), unsubstituted ethyl (Et), unsubstituted propyl (Pr, e.g., unsubstituted n-propyl (n-Pr), unsubstituted isopropyl (i-Pr)), unsubstituted butyl (Bu, e.g., unsubstituted n-butyl (n-Bu), unsubstituted tert-butyl (tert-Bu or t-Bu), unsubstituted sec-butyl (sec-Bu), unsubstituted isobutyl (i-Bu)).
  • unsubstituted C1-6 alkyl e.g., ⁇ CH3 (Me), unsubstituted ethyl (Et), unsub
  • the alkyl group is a substituted C1-10 alkyl (such as substituted C 1-6 alkyl, e.g., ⁇ CF 3 , Bn).
  • haloalkyl is a substituted alkyl group, wherein one or more of the hydrogen atoms are independently replaced by a halogen, e.g., fluoro, bromo, chloro, or iodo.
  • the haloalkyl moiety has 1 to 8 carbon atoms some embodiments, the haloalkyl moiety has 1 to 6 carbon atoms some embodiments, the haloalkyl moiety has 1 to 4 carbon atoms some embodiments, the haloalkyl moiety has 1 to 3 carbon atoms some embodiments, the haloalkyl moiety has 1 to 2 carbon atoms (“C 1-2 haloalkyl”).
  • Examples of haloalkyl groups include –CHF2, ⁇ CH2F, ⁇ CF3, ⁇ CH2CF3, ⁇ CF2CF3, ⁇ CF2CF2CF3, ⁇ CCl3, ⁇ CFCl2, ⁇ CF2Cl, and the like.
  • heteroalkyl refers to an alkyl group, which further includes at least one heteroatom (e.g., 1, 2, 3, or 4 heteroatoms) selected from oxygen, nitrogen, or sulfur within (i.e., inserted between adjacent carbon atoms of) and/or placed at one or more terminal position(s) of the parent chain.
  • a heteroalkyl group refers to a saturated group having from 1 to 20 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC 1-20 alkyl”).
  • a heteroalkyl group is a saturated group having 1 to 18 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1-18 alkyl”).
  • a heteroalkyl group is a saturated group having 1 to 16 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1-16 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 14 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC 1-14 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 12 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1-12 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 10 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC 1-10 alkyl”).
  • a heteroalkyl group is a saturated group having 1 to 8 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1-8 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 6 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1-6 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 4 carbon atoms and 1 or 2 heteroatoms within the parent chain (“heteroC 1-4 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 3 carbon atoms and 1 heteroatom within the parent chain (“heteroC1-3 alkyl”).
  • a heteroalkyl group is a saturated group having 1 to 2 carbon atoms and 1 heteroatom within the parent chain (“heteroC 1-2 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 carbon atom and 1 heteroatom (“heteroC1 alkyl”). In some embodiments, the heteroalkyl group defined herein is a partially unsaturated group having 1 or more heteroatoms within the parent chain and at least one unsaturated carbon, such as a carbonyl group. For example, a heteroalkyl group may comprise an amide or ester functionality in its parent chain such that one or more carbon atoms are unsaturated carbonyl groups.
  • each instance of a heteroalkyl group is independently unsubstituted (an “unsubstituted heteroalkyl”) or substituted (a “substituted heteroalkyl”) with one or more substituents.
  • the heteroalkyl group is an unsubstituted heteroC1-20 alkyl.
  • the heteroalkyl group is an unsubstituted heteroC 1-10 alkyl.
  • the heteroalkyl group is a substituted heteroC1-20 alkyl.
  • the heteroalkyl group is an unsubstituted heteroC1-10 alkyl.
  • alkenyl refers to a radical of a straight-chain or branched hydrocarbon group having from 2 to 10 carbon atoms and one or more carbon-carbon double bonds (e.g., 1, 2, 3, or 4 double bonds).
  • an alkenyl group has 2 to 9 carbon atoms (“C2-9 alkenyl”).
  • an alkenyl group has 2 to 8 carbon atoms (“C2-8 alkenyl”).
  • an alkenyl group has 2 to 7 carbon atoms (“C 2-7 alkenyl”).
  • an alkenyl group has 2 to 6 carbon atoms (“C2-6 alkenyl”).
  • an alkenyl group has 2 to 5 carbon atoms (“C2-5 alkenyl”). In some embodiments, an alkenyl group has 2 to 4 carbon atoms (“C 2-4 alkenyl”). In some embodiments, an alkenyl group has 2 to 3 carbon atoms (“C2-3 alkenyl”). In some embodiments, an alkenyl group has 2 carbon atoms (“C2 alkenyl”).
  • the one or more carbon-carbon double bonds can be internal (such as in 2-butenyl) or terminal (such as in 1-butenyl).
  • Examples of C 2-4 alkenyl groups include ethenyl (C 2 ), 1-propenyl (C 3 ), 2- propenyl (C3), 1-butenyl (C4), 2-butenyl (C4), butadienyl (C4), and the like.
  • Examples of C2-6 alkenyl groups include the aforementioned C 2-4 alkenyl groups as well as pentenyl (C5), pentadienyl (C 5 ), hexenyl (C 6 ), and the like.
  • Additional examples of alkenyl include heptenyl (C7), octenyl (C8), octatrienyl (C8), and the like.
  • each instance of an alkenyl group is independently unsubstituted (an “unsubstituted alkenyl”) or substituted (a “substituted alkenyl”) with one or more substituents.
  • the alkenyl group is an unsubstituted C2-10 alkenyl.
  • the alkenyl group is a substituted C2-10 alkenyl.
  • a C C double bond for which the stereochemistry is not specified ( )-double bond.
  • heteroalkenyl refers to an alkenyl group, which further includes at least one heteroatom (e.g., 1, 2, 3, or 4 heteroatoms) selected from oxygen, nitrogen, or sulfur within (i.e., inserted between adjacent carbon atoms of) and/or placed at one or more terminal position(s) of the parent chain.
  • a heteroalkenyl group refers to a group having from 2 to 10 carbon atoms, at least one double bond, and 1 or more heteroatoms within the parent chain (“heteroC2-10 alkenyl”).
  • a heteroalkenyl group has 2 to 9 carbon atoms at least one double bond, and 1 or more heteroatoms within the parent chain (“heteroC 2-9 alkenyl”). In some embodiments, a heteroalkenyl group has 2 to 8 carbon atoms, at least one double bond, and 1 or more heteroatoms within the parent chain (“heteroC2-8 alkenyl”). In some embodiments, a heteroalkenyl group has 2 to 7 carbon atoms, at least one double bond, and 1 or more heteroatoms within the parent chain (“heteroC2-7 alkenyl”).
  • a heteroalkenyl group has 2 to 6 carbon atoms, at least one double bond, and 1 or more heteroatoms within the parent chain (“heteroC 2-6 alkenyl”). In some embodiments, a heteroalkenyl group has 2 to 5 carbon atoms, at least one double bond, and 1 or 2 heteroatoms within the parent chain (“heteroC2-5 alkenyl”). In some embodiments, a heteroalkenyl group has 2 to 4 carbon atoms, at least one double bond, and 1 or 2 heteroatoms within the parent chain (“heteroC 2-4 alkenyl”).
  • a heteroalkenyl group has 2 to 3 carbon atoms, at least one double bond, and 1 heteroatom within the parent chain (“heteroC 2-3 alkenyl”). In some embodiments, a heteroalkenyl group has 2 to 6 carbon atoms, at least one double bond, and 1 or 2 heteroatoms within the parent chain (“heteroC2-6 alkenyl”). Unless otherwise specified, each instance of a heteroalkenyl group is independently unsubstituted (an “unsubstituted heteroalkenyl”) or substituted (a “substituted heteroalkenyl”) with one or more substituents. In certain embodiments, the heteroalkenyl group is an unsubstituted heteroC2-10 alkenyl.
  • the heteroalkenyl group is a substituted heteroC 2-10 alkenyl.
  • alkynyl refers to a radical of a straight-chain or branched hydrocarbon group having from 2 to 10 carbon atoms and one or more carbon-carbon triple bonds (e.g., 1, 2, 3, or 4 triple bonds) (“C2-10 alkynyl”).
  • an alkynyl group has 2 to 9 carbon atoms (“C 2-9 alkynyl”).
  • an alkynyl group has 2 to 8 carbon atoms (“C 2-8 alkynyl”).
  • an alkynyl group has 2 to 7 carbon atoms (“C 2-7 alkynyl”).
  • an alkynyl group has 2 to 6 carbon atoms (“C2-6 alkynyl”). In some embodiments, an alkynyl group has 2 to 5 carbon atoms (“C 2-5 alkynyl”). In some embodiments, an alkynyl group has 2 to 4 carbon atoms (“C 2-4 alkynyl”). In some embodiments, an alkynyl group has 2 to 3 carbon atoms (“C2-3 alkynyl”). In some embodiments, an alkynyl group has 2 carbon atoms (“C2 alkynyl”). The one or more carbon-carbon triple bonds can be internal (such as in 2-butynyl) or terminal (such as in 1-butynyl).
  • Examples of C 2-4 alkynyl groups include, without limitation, ethynyl (C2), 1-propynyl (C3), 2-propynyl (C3), 1-butynyl (C4), 2-butynyl (C4), and the like.
  • Examples of C2-6 alkenyl groups include the aforementioned C 2-4 alkynyl groups as well as pentynyl (C 5 ), hexynyl (C 6 ), and the like. Additional examples of alkynyl include heptynyl (C 7 ), octynyl (C8), and the like.
  • each instance of an alkynyl group is independently unsubstituted (an “unsubstituted alkynyl”) or substituted (a “substituted alkynyl”) with one or more substituents.
  • the alkynyl group is an unsubstituted C 2-10 alkynyl.
  • the alkynyl group is a substituted C2-10 alkynyl.
  • heteroalkynyl refers to an alkynyl group, which further includes at least one heteroatom (e.g., 1, 2, 3, or 4 heteroatoms) selected from oxygen, nitrogen, or sulfur within (i.e., inserted between adjacent carbon atoms of) and/or placed at one or more terminal position(s) of the parent chain.
  • a heteroalkynyl group refers to a group having from 2 to 10 carbon atoms, at least one triple bond, and 1 or more heteroatoms within the parent chain (“heteroC 2-10 alkynyl”).
  • a heteroalkynyl group has 2 to 9 carbon atoms, at least one triple bond, and 1 or more heteroatoms within the parent chain (“heteroC2-9 alkynyl”). In some embodiments, a heteroalkynyl group has 2 to 8 carbon atoms, at least one triple bond, and 1 or more heteroatoms within the parent chain (“heteroC 2-8 alkynyl”). In some embodiments, a heteroalkynyl group has 2 to 7 carbon atoms, at least one triple bond, and 1 or more heteroatoms within the parent chain (“heteroC2-7 alkynyl”).
  • a heteroalkynyl group has 2 to 6 carbon atoms, at least one triple bond, and 1 or more heteroatoms within the parent chain (“heteroC2-6 alkynyl”). In some embodiments, a heteroalkynyl group has 2 to 5 carbon atoms, at least one triple bond, and 1 or 2 heteroatoms within the parent chain (“heteroC2-5 alkynyl”). In some embodiments, a heteroalkynyl group has 2 to 4 carbon atoms, at least one triple bond, and 1 or 2 heteroatoms within the parent chain (“heteroC 2-4 alkynyl”).
  • a heteroalkynyl group has 2 to 3 carbon atoms, at least one triple bond, and 1 heteroatom within the parent chain (“heteroC 2-3 alkynyl”). In some embodiments, a heteroalkynyl group has 2 to 6 carbon atoms, at least one triple bond, and 1 or 2 heteroatoms within the parent chain (“heteroC2-6 alkynyl”). Unless otherwise specified, each instance of a heteroalkynyl group is independently unsubstituted (an “unsubstituted heteroalkynyl”) or substituted (a “substituted heteroalkynyl”) with one or more substituents.
  • the heteroalkynyl group is an unsubstituted heteroC2-10 alkynyl. In certain embodiments, the heteroalkynyl group is a substituted heteroC 2-10 alkynyl.
  • the term “carbocyclyl” or “carbocyclic” refers to a radical of a non-aromatic cyclic hydrocarbon group having from 3 to 14 ring carbon atoms (“C3-14 carbocyclyl”) and zero heteroatoms in the non-aromatic ring system. In some embodiments, a carbocyclyl group has 3 to 10 ring carbon atoms (“C 3-10 carbocyclyl”).
  • a carbocyclyl group has 3 to 8 ring carbon atoms (“C3-8 carbocyclyl”). In some embodiments, a carbocyclyl group has 3 to 7 ring carbon atoms (“C3-7 carbocyclyl”). In some embodiments, a carbocyclyl group has 3 to 6 ring carbon atoms (“C 3-6 carbocyclyl”). In some embodiments, a carbocyclyl group has 4 to 6 ring carbon atoms (“C4-6 carbocyclyl”). In some embodiments, a carbocyclyl group has 5 to 6 ring carbon atoms (“C5-6 carbocyclyl”).
  • a carbocyclyl group has 5 to 10 ring carbon atoms (“C 5-10 carbocyclyl”).
  • Exemplary C 3-6 carbocyclyl groups include, without limitation, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), and the like.
  • Exemplary C 3-8 carbocyclyl groups include, without limitation, the aforementioned C 3-6 carbocyclyl groups as well as cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), bicyclo[2.2.1]heptanyl (C7), bicyclo[2.2.2]octanyl (C 8 ), and the like.
  • Exemplary C 3-10 carbocyclyl groups include, without limitation, the aforementioned C3-8 carbocyclyl groups as well as cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro-1H-indenyl (C9), decahydronaphthalenyl (C 10 ), spiro[4.5]decanyl (C 10 ), and the like.
  • the carbocyclyl group is either monocyclic (“monocyclic carbocyclyl”) or polycyclic (e.g., containing a fused, bridged or spiro ring system such as a bicyclic system (“bicyclic carbocyclyl”) or tricyclic system (“tricyclic carbocyclyl”)) and can be saturated or can contain one or more carbon-carbon double or triple bonds.
  • Carbocyclyl also includes ring systems wherein the carbocyclyl ring, as defined above, is fused with one or more aryl or heteroaryl groups wherein the point of attachment is on the carbocyclyl ring, and in such instances, the number of carbons continue to designate the number of carbons in the carbocyclic ring system.
  • each instance of a carbocyclyl group is independently unsubstituted (an “unsubstituted carbocyclyl”) or substituted (a “substituted carbocyclyl”) with one or more substituents.
  • the carbocyclyl group is an unsubstituted C3-14 carbocyclyl.
  • the carbocyclyl group is a substituted C3-14 carbocyclyl.
  • “carbocyclyl” is a monocyclic, saturated carbocyclyl group having from 3 to 14 ring carbon atoms (“C 3-14 cycloalkyl”).
  • a cycloalkyl group has 3 to 10 ring carbon atoms (“C3-10 cycloalkyl”).
  • a cycloalkyl group has 3 to 8 ring carbon atoms (“C3-8 cycloalkyl”).
  • a cycloalkyl group has 3 to 6 ring carbon atoms (“C 3-6 cycloalkyl”).
  • a cycloalkyl group has 4 to 6 ring carbon atoms (“C4-6 cycloalkyl”). In some embodiments, a cycloalkyl group has 5 to 6 ring carbon atoms (“C5-6 cycloalkyl”). In some embodiments, a cycloalkyl group has 5 to 10 ring carbon atoms (“C5-10 cycloalkyl”). Examples of C5-6 cycloalkyl groups include cyclopentyl (C5) and cyclohexyl (C 5 ). Examples of C 3-6 cycloalkyl groups include the aforementioned C 5-6 cycloalkyl groups as well as cyclopropyl (C3) and cyclobutyl (C4).
  • C3-8 cycloalkyl groups include the aforementioned C3-6 cycloalkyl groups as well as cycloheptyl (C7) and cyclooctyl (C 8 ).
  • each instance of a cycloalkyl group is independently unsubstituted (an “unsubstituted cycloalkyl”) or substituted (a “substituted cycloalkyl”) with one or more substituents.
  • the cycloalkyl group is an unsubstituted C3-14 cycloalkyl.
  • the cycloalkyl group is a substituted C 3-14 cycloalkyl.
  • heterocyclyl refers to a radical of a 3- to 14-membered non-aromatic ring system having ring carbon atoms and 1 to 4 ring heteroatoms, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“3-14 membered heterocyclyl”).
  • heterocyclyl groups that contain one or more nitrogen atoms, the point of attachment can be a carbon or nitrogen atom, as valency permits.
  • a heterocyclyl group can either be monocyclic (“monocyclic heterocyclyl”) or polycyclic (e.g., a fused, bridged or spiro ring system such as a bicyclic system (“bicyclic heterocyclyl”) or tricyclic system (“tricyclic heterocyclyl”)), and can be saturated or can contain one or more carbon-carbon double or triple bonds.
  • Heterocyclyl polycyclic ring systems can include one or more heteroatoms in one or both rings.
  • Heterocyclyl also includes ring systems wherein the heterocyclyl ring, as defined above, is fused with one or more carbocyclyl groups wherein the point of attachment is either on the carbocyclyl or heterocyclyl ring, or ring systems wherein the heterocyclyl ring, as defined above, is fused with one or more aryl or heteroaryl groups, wherein the point of attachment is on the heterocyclyl ring, and in such instances, the number of ring members continue to designate the number of ring members in the heterocyclyl ring system.
  • each instance of heterocyclyl is independently unsubstituted (an “unsubstituted heterocyclyl”) or substituted (a “substituted heterocyclyl”) with one or more substituents.
  • the heterocyclyl group is an unsubstituted 3-14 membered heterocyclyl.
  • the heterocyclyl group is a substituted 3-14 membered heterocyclyl.
  • a heterocyclyl group is a 5-10 membered non-aromatic ring system having ring carbon atoms and 1-4 ring heteroatoms, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-10 membered heterocyclyl”).
  • a heterocyclyl group is a 5-8 membered non-aromatic ring system having ring carbon atoms and 1-4 ring heteroatoms, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-8 membered heterocyclyl”).
  • a heterocyclyl group is a 5-6 membered non-aromatic ring system having ring carbon atoms and 1- 4 ring heteroatoms, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-6 membered heterocyclyl”).
  • the 5-6 membered heterocyclyl has 1-3 ring heteroatoms selected from nitrogen, oxygen, and sulfur.
  • the 5-6 membered heterocyclyl has 1-2 ring heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the 5-6 membered heterocyclyl has 1 ring heteroatom selected from nitrogen, oxygen, and sulfur.
  • Exemplary 3-membered heterocyclyl groups containing 1 heteroatom include, without limitation, azirdinyl, oxiranyl, and thiiranyl.
  • Exemplary 4-membered heterocyclyl groups containing 1 heteroatom include, without limitation, azetidinyl, oxetanyl, and thietanyl.
  • Exemplary 5-membered heterocyclyl groups containing 1 heteroatom include, without limitation, tetrahydrofuranyl, dihydrofuranyl, tetrahydrothiophenyl, dihydrothiophenyl, pyrrolidinyl, dihydropyrrolyl, and pyrrolyl-2,5-dione.
  • Exemplary 5-membered heterocyclyl groups containing 2 heteroatoms include, without limitation, dioxolanyl, oxathiolanyl and dithiolanyl.
  • Exemplary 5- membered heterocyclyl groups containing 3 heteroatoms include, without limitation, triazolinyl, oxadiazolinyl, and thiadiazolinyl.
  • Exemplary 6-membered heterocyclyl groups containing 1 heteroatom include, without limitation, piperidinyl, tetrahydropyranyl, dihydropyridinyl, and thianyl.
  • Exemplary 6-membered heterocyclyl groups containing 2 heteroatoms include, without limitation, piperazinyl, morpholinyl, dithianyl, and dioxanyl.
  • Exemplary 6-membered heterocyclyl groups containing 3 heteroatoms include, without limitation, triazinyl.
  • Exemplary 7- membered heterocyclyl groups containing 1 heteroatom include, without limitation, azepanyl, oxepanyl, and thiepanyl.
  • Exemplary 8-membered heterocyclyl groups containing 1 heteroatom include, without limitation, azocanyl, oxecanyl, and thiocanyl.
  • Exemplary bicyclic heterocyclyl groups include, without limitation, indolinyl, isoindolinyl, dihydrobenzofuranyl, dihydrobenzothienyl, tetrahydrobenzothienyl, tetrahydrobenzofuranyl, tetrahydroindolyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl, decahydroisoquinolinyl, octahydrochromenyl, octahydroisochromenyl, decahydronaphthyridinyl, decahydro-1,8- naphthyridinyl, octahydropyrrolo[3,2-b]pyrrole
  • aryl refers to a radical of a monocyclic or polycyclic (e.g., bicyclic or tricyclic) 4n+2 aromatic ring system (e.g., having 6, 10, or 14 electrons shared in a cyclic array) having 6-14 ring carbon atoms and zero heteroatoms provided in the aromatic ring system (“C6-14 aryl”).
  • an aryl group has 6 ring carbon atoms (“C6 aryl”; e.g., phenyl).
  • an aryl group has 10 ring carbon atoms (“C10 aryl”; e.g., naphthyl such as 1-naphthyl and 2-naphthyl).
  • an aryl group has 14 ring carbon atoms (“C14 aryl”; e.g., anthracyl).
  • Aryl also includes ring systems wherein the aryl ring, as defined above, is fused with one or more carbocyclyl or heterocyclyl groups wherein the radical or point of attachment is on the aryl ring, and in such instances, the number of carbon atoms continue to designate the number of carbon atoms in the aryl ring system.
  • each instance of an aryl group is independently unsubstituted (an “unsubstituted aryl”) or substituted (a “substituted aryl”) with one or more substituents.
  • the aryl group is an unsubstituted C6-14 aryl.
  • the aryl group is a substituted C6-14 aryl.
  • “Aralkyl” is a subset of “alkyl” and refers to an alkyl group substituted by an aryl group, wherein the point of attachment is on the alkyl moiety.
  • heteroaryl refers to a radical of a 5-14 membered monocyclic or polycyclic (e.g., bicyclic, tricyclic) 4n+2 aromatic ring system (e.g., having 6, 10, or 14 electrons shared in a cyclic array) having ring carbon atoms and 1-4 ring heteroatoms provided in the aromatic ring system, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-14 membered heteroaryl”).
  • the point of attachment can be a carbon or nitrogen atom, as valency permits.
  • Heteroaryl polycyclic ring systems can include one or more heteroatoms in one or both rings.
  • Heteroaryl includes ring systems wherein the heteroaryl ring, as defined above, is fused with one or more carbocyclyl or heterocyclyl groups wherein the point of attachment is on the heteroaryl ring, and in such instances, the number of ring members continue to designate the number of ring members in the heteroaryl ring system. “Heteroaryl” also includes ring systems wherein the heteroaryl ring, as defined above, is fused with one or more aryl groups wherein the point of attachment is either on the aryl or heteroaryl ring, and in such instances, the number of ring members designates the number of ring members in the fused polycyclic (aryl/heteroaryl) ring system.
  • a heteroaryl group is a 5-10 membered aromatic ring system having ring carbon atoms and 1-4 ring heteroatoms provided in the aromatic ring system, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-10 membered heteroaryl”).
  • a heteroaryl group is a 5-8 membered aromatic ring system having ring carbon atoms and 1-4 ring heteroatoms provided in the aromatic ring system, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-8 membered heteroaryl”).
  • a heteroaryl group is a 5-6 membered aromatic ring system having ring carbon atoms and 1-4 ring heteroatoms provided in the aromatic ring system, wherein each heteroatom is independently selected from nitrogen, oxygen, and sulfur (“5-6 membered heteroaryl”).
  • the 5-6 membered heteroaryl has 1-3 ring heteroatoms selected from nitrogen, oxygen, and sulfur.
  • the 5-6 membered heteroaryl has 1-2 ring heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the 5-6 membered heteroaryl has 1 ring heteroatom selected from nitrogen, oxygen, and sulfur. Unless otherwise specified, each instance of a heteroaryl group is independently unsubstituted (an “unsubstituted heteroaryl”) or substituted (a “substituted heteroaryl”) with one or more substituents. In certain embodiments, the heteroaryl group is an unsubstituted 5-14 membered heteroaryl. In certain embodiments, the heteroaryl group is a substituted 5-14 membered heteroaryl.
  • Exemplary 5-membered heteroaryl groups containing 1 heteroatom include, without limitation, pyrrolyl, furanyl, and thiophenyl.
  • Exemplary 5-membered heteroaryl groups containing 2 heteroatoms include, without limitation, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, and isothiazolyl.
  • Exemplary 5-membered heteroaryl groups containing 3 heteroatoms include, without limitation, triazolyl, oxadiazolyl, and thiadiazolyl.
  • Exemplary 5-membered heteroaryl groups containing 4 heteroatoms include, without limitation, tetrazolyl.
  • Exemplary 6- membered heteroaryl groups containing 1 heteroatom include, without limitation, pyridinyl.
  • Exemplary 6-membered heteroaryl groups containing 2 heteroatoms include, without limitation, pyridazinyl, pyrimidinyl, and pyrazinyl.
  • Exemplary 6-membered heteroaryl groups containing 3 or 4 heteroatoms include, without limitation, triazinyl and tetrazinyl, respectively.
  • Exemplary 7- membered heteroaryl groups containing 1 heteroatom include, without limitation, azepinyl, oxepinyl, and thiepinyl.
  • Exemplary 5,6-bicyclic heteroaryl groups include, without limitation, indolyl, isoindolyl, indazolyl, benzotriazolyl, benzothiophenyl, isobenzothiophenyl, benzofuranyl, benzoisofuranyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazolyl, benzthiazolyl, benzisothiazolyl, benzthiadiazolyl, indolizinyl, and purinyl.
  • Exemplary 6,6- bicyclic heteroaryl groups include, without limitation, naphthyridinyl, pteridinyl, quinolinyl, isoquinolinyl, cinnolinyl, quinoxalinyl, phthalazinyl, and quinazolinyl.
  • Exemplary tricyclic heteroaryl groups include, without limitation, phenanthridinyl, dibenzofuranyl, carbazolyl, acridinyl, phenothiazinyl, phenoxazinyl, and phenazinyl.
  • Heteroaralkyl is a subset of “alkyl” and refers to an alkyl group substituted by a heteroaryl group, wherein the point of attachment is on the alkyl moiety.
  • the term “unsaturated bond” refers to a double or triple bond.
  • the term “unsaturated” or “partially unsaturated” refers to a moiety that includes at least one double or triple bond.
  • the term “saturated” refers to a moiety that does not contain a double or triple bond, i.e., the moiety only contains single bonds.
  • alkylene is the divalent moiety of alkyl
  • alkenylene is the divalent moiety of alkenyl
  • alkynylene is the divalent moiety of alkynyl
  • heteroalkylene is the divalent moiety of heteroalkyl
  • heteroalkenylene is the divalent moiety of heteroalkenyl
  • heteroalkynylene is the divalent moiety of heteroalkynyl
  • carbocyclylene is the divalent moiety of carbocyclyl
  • heterocyclylene is the divalent moiety of heterocyclyl
  • arylene is the divalent moiety of aryl
  • heteroarylene is the divalent moiety of heteroaryl.
  • a group is optionally substituted unless expressly provided otherwise.
  • the term “optionally substituted” refers to being substituted or unsubstituted.
  • acyl, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl groups are optionally substituted.
  • Optionally substituted refers to a group which may be substituted or unsubstituted (e.g., “substituted” or “unsubstituted” acyl, “substituted” or “unsubstituted” alkyl, “substituted” or “unsubstituted” alkenyl, “substituted” or “unsubstituted” alkynyl, “substituted” or “unsubstituted” heteroalkyl, “substituted” or “unsubstituted” heteroalkenyl, “substituted” or “unsubstituted” heteroalkynyl, “substituted” or “unsubstituted” carbocyclyl, “substituted” or “unsubstituted” heterocyclyl, “substituted” or “unsubstituted” aryl, or “substituted” or “unsub
  • substituted means that at least one hydrogen present on a group is replaced with a permissible substituent, e.g., a substituent which upon substitution results in a stable compound, e.g., a compound which does not spontaneously undergo transformation such as by rearrangement, cyclization, elimination, or other reaction.
  • a “substituted” group has a substituent at one or more substitutable positions of the group, and when more than one position in any given structure is substituted, the substituent is either the same or different at each position.
  • substituted is contemplated to include substitution with all permissible substituents of organic compounds, and includes any of the substituents described herein that results in the formation of a stable compound.
  • the present invention contemplates any and all such combinations in order to arrive at a stable compound.
  • heteroatoms such as nitrogen may have hydrogen substituents and/or any suitable substituent as described herein which satisfy the valencies of the heteroatoms and results in the formation of a stable moiety.
  • the invention is not intended to be limited in any manner by the exemplary substituents described herein.
  • halo or halogen refers to fluorine (fluoro, ⁇ F), chlorine (chloro, ⁇ Cl), bromine (bromo, ⁇ Br), or iodine (iodo, ⁇ I).
  • hydroxyl or “hydroxy” refers to the group ⁇ OH.
  • amino refers to the group ⁇ NH 2 .
  • substituted amino by extension, refers to a monosubstituted amino, a disubstituted amino, or a trisubstituted amino. In certain embodiments, the “substituted amino” is a monosubstituted amino or a disubstituted amino group.
  • trisubstituted amino refers to an amino group wherein the nitrogen atom directly attached to the parent molecule is substituted with three groups, and includes groups selected from ⁇ N(R bb ) 3 and ⁇ N(R bb ) 3 + X ⁇ , wherein R bb and X ⁇ are as defined herein.
  • acyl groups include aldehydes ( ⁇ CHO), carboxylic acids ( ⁇ CO2H), ketones, acyl halides, esters, amides, imines, carbonates, carbamates, and ureas.
  • Acyl substituents include, but are not limited to, any of the substituents described herein, that result in the formation of a stable moiety (e.g., aliphatic, alkyl, alkenyl, alkynyl, heteroaliphatic, heterocyclic, aryl, heteroaryl, acyl, oxo, imino, thiooxo, cyano, isocyano, amino, azido, nitro, hydroxyl, thiol, halo, aliphaticamino, heteroaliphaticamino, alkylamino, heteroalkylamino, arylamino, heteroarylamino, alkylaryl, arylalkyl, aliphaticoxy, heteroaliphaticoxy, alkyl
  • sil refers to the group –Si(R aa ) 3 , wherein R aa is as defined herein.
  • Nitrogen atoms can be substituted or unsubstituted as valency permits, and include primary, secondary, tertiary, and quaternary nitrogen atoms.
  • the substituent present on the nitrogen atom is an nitrogen protecting group (also referred to herein as an “amino protecting group”).
  • Nitrogen protecting groups are well known in the art and include those described in detail in Protecting Groups in Organic Synthesis, T. W. Greene and P. G. M. Wuts, 3 rd edition, John Wiley & Sons, 1999, incorporated herein by reference.
  • Nitrogen protecting groups such as carbamate groups include, but are not limited to, methyl carbamate, ethyl carbamate, 9-fluorenylmethyl carbamate (Fmoc), 9-(2- sulfo)fluorenylmethyl carbamate, 9-(2,7-dibromo)fluoroenylmethyl carbamate, 2,7-di-t-butyl-[9- (10,10-dioxo-10,10,10,10-tetrahydrothioxanthyl)]methyl carbamate (DBD-Tmoc), 4- methoxyphenacyl carbamate (Phenoc), 2,2,2-trichloroethyl carbamate (Troc), 2- trimethylsilylethyl carbamate (Teoc), 2-phenylethyl carbamate (hZ), 1-(1-adamantyl)-1- methyle
  • Nitrogen protecting groups such as sulfonamide groups include, but are not limited to, p-toluenesulfonamide (Ts), benzenesulfonamide, 2,3,6-trimethyl-4- methoxybenzenesulfonamide (Mtr), 2,4,6-trimethoxybenzenesulfonamide (Mtb), 2,6-dimethyl-4- methoxybenzenesulfonamide (Pme), 2,3,5,6-tetramethyl-4-methoxybenzenesulfonamide (Mte), 4-methoxybenzenesulfonamide (Mbs), 2,4,6-trimethylbenzenesulfonamide (Mts), 2,6-dimethoxy- 4-methylbenzenesulfonamide (iMds), 2,2,5,7,8-pentamethylchroman-6-sulfonamide (Pmc), methane
  • Ts p-toluenesulfonamide
  • Mtr 2,
  • nitrogen protecting groups include, but are not limited to, phenothiazinyl-(10)- acyl derivative, N ⁇ -p-toluenesulfonylaminoacyl derivative, N ⁇ -phenylaminothioacyl derivative, N- benzoylphenylalanyl derivative, N-acetylmethionine derivative, 4,5-diphenyl-3-oxazolin-2-one, N-phthalimide, N-dithiasuccinimide (Dts), N-2,3-diphenylmaleimide, N-2,5-dimethylpyrrole, N- 1,1,4,4-tetramethyldisilylazacyclopentane adduct (STABASE), 5-substituted 1,3-dimethyl-1,3,5- triazacyclohexan-2-one, 5-substituted 1,3-dibenzyl-1,3,5-triazacyclohexan-2-one, 1-substituted 3,5, pheno
  • a nitrogen protecting group is benzyl (Bn), tert-butyloxycarbonyl (BOC), carbobenzyloxy (Cbz), 9-flurenylmethyloxycarbonyl (Fmoc), trifluoroacetyl, triphenylmethyl, acetyl (Ac), benzoyl (Bz), p-methoxybenzyl (PMB), 3,4- dimethoxybenzyl (DMPM), p-methoxyphenyl (PMP), 2,2,2-trichloroethyloxycarbonyl (Troc), triphenylmethyl (Tr), tosyl (Ts), brosyl (Bs), nosyl (Ns), mesyl (Ms), triflyl (Tf), or dansyl (Ds).
  • Bn benzyl
  • BOC tert-butyloxycarbonyl
  • Cbz carbobenzyloxy
  • Fmoc 9-flurenylmethyloxycarbony
  • the substituent present on an oxygen atom is an oxygen protecting group (also referred to herein as an “hydroxyl protecting group”).
  • Oxygen protecting groups are well known in the art and include those described in detail in Protecting Groups in Organic Synthesis, T. W. Greene and P. G. M. Wuts, 3 rd edition, John Wiley & Sons, 1999, incorporated herein by reference.
  • oxygen protecting groups include, but are not limited to, methyl, methoxylmethyl (MOM), methylthiomethyl (MTM), t-butylthiomethyl, (phenyldimethylsilyl)methoxymethyl (SMOM), benzyloxymethyl (BOM), p- methoxybenzyloxymethyl (PMBM), (4-methoxyphenoxy)methyl (p-AOM), guaiacolmethyl (GUM), t-butoxymethyl, 4-pentenyloxymethyl (POM), siloxymethyl, 2-methoxyethoxymethyl (MEM), 2,2,2-trichloroethoxymethyl, bis(2-chloroethoxy)methyl, 2-(trimethylsilyl)ethoxymethyl (SEMOR), tetrahydropyranyl (THP), 3-bromotetrahydropyranyl, tetrahydrothiopyranyl, 1- methoxycyclohexyl, 4-methoxytetrahydropyranyl (MT), methyl,
  • an oxygen protecting group is silyl.
  • an oxygen protecting group is t-butyldiphenylsilyl (TBDPS), t-butyldimethylsilyl (TBDMS), triisoproylsilyl (TIPS), triphenylsilyl (TPS), triethylsilyl (TES), trimethylsilyl (TMS), triisopropylsiloxymethyl (TOM), acetyl (Ac), benzoyl (Bz), allyl carbonate, 2,2,2-trichloroethyl carbonate (Troc), 2-trimethylsilylethyl carbonate, methoxymethyl (MOM), 1-ethoxyethyl (EE), 2-methyoxy-2-propyl (MOP), 2,2,2-trichloroethoxyethyl, 2-methoxyethoxymethyl (MEM), 2- trimethylsilylethoxymethyl (SEM), methylthiomethyl (MTM), tetra
  • the substituent present on a sulfur atom is a sulfur protecting group (also referred to as a “thiol protecting group”).
  • a sulfur protecting group is acetamidomethyl, t-Bu, 3-nitro-2-pyridine sulfenyl, 2-pyridine- sulfenyl, or triphenylmethyl.
  • a “counterion” or “anionic counterion” is a negatively charged group associated with a positively charged group in order to maintain electronic neutrality.
  • An anionic counterion may be monovalent (i.e., including one formal negative charge).
  • An anionic counterion may also be multivalent (i.e., including more than one formal negative charge), such as divalent or trivalent.
  • exemplary counterions include halide ions (e.g., F – , Cl – , Br – , I – ), NO3 – , ClO4 – , OH – , H2PO4 – , HCO ⁇ 3 , HSO4 – , sulfonate ions (e.g., methansulfonate, trifluoromethanesulfonate, p– toluenesulfonate, benzenesulfonate, 10–camphor sulfonate, naphthalene–2–sulfonate, naphthalene–1–sulfonic acid–5–sulfonate, ethan–1–sulfonic acid–2–sulfonate, and the like), carboxylate ions (e.g.,
  • Exemplary counterions which may be multivalent include CO3 2 ⁇ , HPO4 2 ⁇ , PO 3 ⁇ 4 , B4O7 2 ⁇ , SO4 2 ⁇ , S2O3 2 ⁇ , carboxylate anions (e.g., tartrate, citrate, fumarate, maleate, malate, malonate, gluconate, succinate, glutarate, adipate, pimelate, suberate, azelate, sebacate, salicylate, phthalates, aspartate, glutamate, and the like), and carboranes.
  • carboxylate anions e.g., tartrate, citrate, fumarate, maleate, malate, malonate, gluconate, succinate, glutarate, adipate, pimelate, suberate, azelate, sebacate, salicylate, phthalates, aspartate, glutamate, and the like
  • carboxylate anions e.g., tartrate, citrate, fumarate, maleate,
  • suitable leaving groups include, but are not limited to, halogen (such as F, Cl, Br, or I (iodine)), alkoxycarbonyloxy, aryloxycarbonyloxy, alkanesulfonyloxy, arenesulfonyloxy, alkyl- carbonyloxy (e.g., acetoxy), arylcarbonyloxy, aryloxy, methoxy, N,O-dimethylhydroxylamino, pixyl, and haloformates.
  • halogen such as F, Cl, Br, or I (iodine
  • the leaving group is a brosylate, such as p-bromobenzenesulfonyloxy.
  • the leaving group is a nosylate, such as 2- nitrobenzenesulfonyloxy.
  • the leaving group may also be a phosphineoxide (e.g., formed during a Mitsunobu reaction) or an internal leaving group such as an epoxide or cyclic sulfate.
  • phosphineoxide e.g., formed during a Mitsunobu reaction
  • an internal leaving group such as an epoxide or cyclic sulfate.
  • Other non- limiting examples of leaving groups are water, ammonia, alcohols, ether moieties, thioether moieties, zinc halides, magnesium moieties, diazonium salts, and copper moieties.
  • non-hydrogen group refers to any group that is defined for a particular variable that is not hydrogen.
  • salt refers to any and all salts, and encompasses pharmaceutically acceptable salts.
  • pharmaceutically acceptable salt refers to those salts which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of humans and lower animals without undue toxicity, irritation, allergic response, and the like, and are commensurate with a reasonable benefit/risk ratio.
  • Pharmaceutically acceptable salts are well known in the art. For example, Berge et al. describe pharmaceutically acceptable salts in detail in J. Pharmaceutical Sciences, 1977, 66, 1-19, incorporated herein by reference.
  • Pharmaceutically acceptable salts of the compounds of this invention include those derived from suitable inorganic and organic acids and bases.
  • Examples of pharmaceutically acceptable, nontoxic acid addition salts are salts of an amino group formed with inorganic acids, such as hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, and perchloric acid or with organic acids, such as acetic acid, oxalic acid, maleic acid, tartaric acid, citric acid, succinic acid, or malonic acid or by using other methods known in the art such as ion exchange.
  • inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, and perchloric acid
  • organic acids such as acetic acid, oxalic acid, maleic acid, tartaric acid, citric acid, succinic acid, or malonic acid or by using other methods known in the art such as ion exchange.
  • salts include adipate, alginate, ascorbate, aspartate, benzenesulfonate, benzoate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, citrate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, formate, fumarate, glucoheptonate, glycerophosphate, gluconate, hemisulfate, heptanoate, hexanoate, hydroiodide, 2-hydroxy-ethanesulfonate, lactobionate, lactate, laurate, lauryl sulfate, malate, maleate, malonate, methanesulfonate, 2- naphthalenesulfonate, nicotinate, nitrate, oleate, oxalate, palmitate, pamoate, pectinate
  • Salts derived from appropriate bases include alkali metal, alkaline earth metal, ammonium, and N + (C 1-4 alkyl) 4 ⁇ salts.
  • Representative alkali or alkaline earth metal salts include sodium, lithium, potassium, calcium, magnesium, and the like.
  • Further pharmaceutically acceptable salts include, when appropriate, nontoxic ammonium, quaternary ammonium, and amine cations formed using counterions, such as halide, hydroxide, carboxylate, sulfate, phosphate, nitrate, lower alkyl sulfonate, and aryl sulfonate.
  • solvate refers to forms of the compound, or a salt thereof, that are associated with a solvent, usually by a solvolysis reaction. This physical association may include hydrogen bonding.
  • solvents include water, methanol, ethanol, acetic acid, DMSO, THF, diethyl ether, and the like.
  • the compounds described herein may be prepared, e.g., in crystalline form, and may be solvated. Suitable solvates include pharmaceutically acceptable solvates and further include both stoichiometric solvates and non-stoichiometric solvates.
  • the solvate will be capable of isolation, for example, when one or more solvent molecules are incorporated in the crystal lattice of a crystalline solid.
  • “Solvate” encompasses both solution- phase and isolatable solvates.
  • Representative solvates include hydrates, ethanolates, and methanolates.
  • the term “hydrate” refers to a compound that is associated with water. Typically, the number of the water molecules contained in a hydrate of a compound is in a definite ratio to the number of the compound molecules in the hydrate. Therefore, a hydrate of a compound may be represented, for example, by the general formula R ⁇ x H2O, wherein R is the compound, and x is a number greater than 0.
  • a given compound may form more than one type of hydrate, including, e.g., monohydrates (x is 1), lower hydrates (x is a number greater than 0 and smaller than 1, e.g., hemihydrates (R ⁇ 0.5 H2O)), and polyhydrates (x is a number greater than 1, e.g., dihydrates (R ⁇ 2 H2O) and hexahydrates (R ⁇ 6 H2O)).
  • monohydrates x is 1
  • lower hydrates x is a number greater than 0 and smaller than 1, e.g., hemihydrates (R ⁇ 0.5 H2O)
  • polyhydrates x is a number greater than 1, e.g., dihydrates (R ⁇ 2 H2O) and hexahydrates (R ⁇ 6 H2O)
  • tautomers or “tautomeric” refers to two or more interconvertible compounds resulting from at least one formal migration of a hydrogen atom and at least one change in valency (e.g., a single bond to a double bond, a triple bond to a single bond, or vice versa).
  • the exact ratio of the tautomers depends on several factors, including temperature, solvent, and pH. Tautomerizations (i.e., the reaction providing a tautomeric pair) may catalyzed by acid or base.
  • Exemplary tautomerizations include keto-to-enol, amide-to-imide, lactam-to-lactim, enamine-to- imine, and enamine-to-(a different enamine) tautomerizations.
  • isomers compounds that have the same molecular formula but differ in the nature or sequence of bonding of their atoms or the arrangement of their atoms in space are termed “isomers”. Isomers that differ in the arrangement of their atoms in space are termed “stereoisomers”.
  • stereoisomers that are not mirror images of one another are termed “diastereomers” and those that are non-superimposable mirror images of each other are termed “enantiomers”.
  • enantiomers When a compound has an asymmetric center, for example, it is bonded to four different groups, a pair of enantiomers is possible.
  • An enantiomer can be characterized by the absolute configuration of its asymmetric center and is described by the R- and S-sequencing rules of Cahn and Prelog, or by the manner in which the molecule rotates the plane of polarized light and designated as dextrorotatory or levorotatory (i.e., as (+) or ( ⁇ )-isomers respectively).
  • a chiral compound can exist as either individual enantiomer or as a mixture thereof.
  • a mixture containing equal proportions of the enantiomers is called a “racemic mixture”.
  • the term “polymorph” refers to a crystalline form of a compound (or a salt, hydrate, or solvate thereof). All polymorphs have the same elemental composition. Different crystalline forms usually have different X-ray diffraction patterns, infrared spectra, melting points, density, hardness, crystal shape, optical and electrical properties, stability, and solubility. Recrystallization solvent, rate of crystallization, storage temperature, and other factors may cause one crystal form to dominate.
  • Various polymorphs of a compound can be prepared by crystallization under different conditions.
  • prodrugs refers to compounds that have cleavable groups and become by solvolysis or under physiological conditions the compounds described herein, which are pharmaceutically active in vivo. Such examples include, but are not limited to, choline ester derivatives and the like, N-alkylmorpholine esters and the like. Other derivatives of the compounds described herein have activity in both their acid and acid derivative forms, but in the acid sensitive form often offer advantages of solubility, tissue compatibility, or delayed release in the mammalian organism (see, Bundgard, H., Design of Prodrugs, pp.7-9, 21-24, Elsevier, Amsterdam 1985).
  • Prodrugs include acid derivatives well known to practitioners of the art, such as, for example, esters prepared by reaction of the parent acid with a suitable alcohol, or amides prepared by reaction of the parent acid compound with a substituted or unsubstituted amine, or acid anhydrides, or mixed anhydrides. Simple aliphatic or aromatic esters, amides, and anhydrides derived from acidic groups pendant on the compounds described herein are particular prodrugs. In some cases it is desirable to prepare double ester type prodrugs such as (acyloxy)alkyl esters or ((alkoxycarbonyl)oxy)alkylesters.
  • a “subject” to which administration is contemplated refers to a human (i.e., male or female of any age group, e.g., pediatric subject (e.g., infant, child, or adolescent) or adult subject (e.g., young adult, middle-aged adult, or senior adult)) or non-human animal.
  • a human i.e., male or female of any age group, e.g., pediatric subject (e.g., infant, child, or adolescent) or adult subject (e.g., young adult, middle-aged adult, or senior adult)) or non-human animal.
  • the non-human animal is a mammal (e.g., primate (e.g., cynomolgus monkey or rhesus monkey), commercially relevant mammal (e.g., cattle, pig, horse, sheep, goat, cat, or dog), or bird (e.g., commercially relevant bird, such as chicken, duck, goose, or turkey)).
  • the non-human animal is a fish, reptile, or amphibian.
  • the non-human animal may be a male or female at any stage of development.
  • the non-human animal may be a transgenic animal or genetically engineered animal.
  • the subject may also be a plant. In certain embodiments, the plant is a land plant.
  • the plant is a non-vascular land plant. In certain embodiments, the plant is a vascular land plant. In certain embodiments, the plant is a seed plant. In certain embodiments, the plant is a cultivated plant. In certain embodiments, the plant is a dicot. In certain embodiments, the plant is a monocot. In certain embodiments, the plant is a flowering plant. In some embodiments, the plant is a cereal plant, e.g., maize, corn, wheat, rice, oat, barley, rye, or millet. In some embodiments, the plant is a legume, e.g., a bean plant, e.g., soybean plant. In some embodiments, the plant is a tree or shrub.
  • tissue sample refers to any sample including tissue samples (such as tissue sections and needle biopsies of a tissue); cell samples (e.g., cytological smears (such as Pap or blood smears) or samples of cells obtained by microdissection); samples of whole organisms (such as samples of yeasts or bacteria); or cell fractions, fragments or organelles (such as obtained by lysing cells and separating the components thereof by centrifugation or otherwise).
  • tissue samples such as tissue sections and needle biopsies of a tissue
  • cell samples e.g., cytological smears (such as Pap or blood smears) or samples of cells obtained by microdissection) or samples of cells obtained by microdissection
  • samples of whole organisms such as samples of yeasts or bacteria
  • cell fractions, fragments or organelles such as obtained by lysing cells and separating the components thereof by centrifugation or otherwise.
  • tissue refers to any biological tissue of a subject (including a group of cells, a body part, or an organ) or a part thereof, including blood and/or lymph vessels, which is the object to which a compound and/or composition of the disclosure is delivered.
  • a tissue may be an abnormal or unhealthy tissue.
  • a tissue may also be a normal or healthy tissue that is under a higher than normal risk of becoming abnormal or unhealthy.
  • the term “administer,” “administering,” or “administration” refers to implanting, absorbing, ingesting, injecting, inhaling, or otherwise introducing a compound described herein, or a composition thereof, into a biological system.
  • An “effective amount” of a compound described herein refers to an amount sufficient to elicit a desired outcome (e.g., induce phosphorylation of a target substrate).
  • An effective amount of a compound described herein may vary depending on such factors as the desired biological endpoint (e.g., extent of phosphorylation) and the nature of the biological sample.
  • small molecule refers to molecules, whether naturally occurring or artificially created (e.g., via chemical synthesis) that have a relatively low molecular weight.
  • a small molecule is an organic compound (i.e., it contains carbon).
  • the small molecule may contain multiple carbon-carbon bonds, stereocenters, and other functional groups (e.g., amines, hydroxyl, carbonyls, and heterocyclic rings, etc.).
  • the molecular weight of a small molecule is not more than about 1,000 g/mol, not more than about 900 g/mol, not more than about 800 g/mol, not more than about 700 g/mol, not more than about 600 g/mol, not more than about 500 g/mol, not more than about 400 g/mol, not more than about 300 g/mol, not more than about 200 g/mol, or not more than about 100 g/mol.
  • the molecular weight of a small molecule is at least about 100 g/mol, at least about 200 g/mol, at least about 300 g/mol, at least about 400 g/mol, at least about 500 g/mol, at least about 600 g/mol, at least about 700 g/mol, at least about 800 g/mol, or at least about 900 g/mol, or at least about 1,000 g/mol. Combinations of the above ranges (e.g., at least about 200 g/mol and not more than about 500 g/mol) are also possible.
  • the small molecule is a therapeutically active agent such as a drug (e.g., a molecule approved by the U.S.
  • the small molecule may also be complexed with one or more metal atoms and/or metal ions.
  • the small molecule is also referred to as a “small organometallic molecule.”
  • Preferred small molecules are biologically active in that they produce a biological effect in animals, preferably mammals, more preferably humans. Small molecules include, but are not limited to, radionuclides and imaging agents.
  • the small molecule is a drug.
  • the drug is one that has already been deemed safe and effective for use in humans or animals by the appropriate governmental agency or regulatory body. For example, drugs approved for human use are listed by the FDA under 21 C.F.R.
  • targeting moiety refers to any chemical entity that serves to bind or otherwise direct the compound to a particular location or association.
  • bioactive moiety refers to an agent or moiety that can influence (i.e., effect a change in) a biological system, such as in an organism, tissue, or cell. In some embodiments, the bioactive moiety is a small molecule.
  • the bioactive moiety is a peptide or protein.
  • nucleophilic group refers to a chemical entity having a nucleophile, a moiety that forms bonds by donating an electron pair. All molecules and ions with a free pair of electrons or at least one pi bond can act as nucleophiles. Nucleophiles may take part in nucleophilic substitution, whereby a nucleophile becomes attracted to a full or partial positive charge, and nucleophilic addition.
  • electrophilic group refers to a chemical entity having an electrophile, a moiety that forms bonds with nucleophiles by accepting an electron pair.
  • Electrophiles are positively charged, have an atom that carries a partial positive charge, or have an atom that does not have an octet of electrons. Electrophiles mainly interact with nucleophiles through addition and substitution reactions.
  • the term “orienting moiety” refers to a chemical entity that acts as a spacing group in a molecule to spatially orient or establish the position and direction from which it joins one or more other moieties.
  • FIG.1 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 105.
  • FIG.2 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 106.
  • FIG.3 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 107.
  • FIG.4 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 109.
  • FIG.5 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 111.
  • FIG.6 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 112.
  • FIG.7 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 122.
  • FIG.8 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 124.
  • FIG.9 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 126.
  • FIG.10 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 128.
  • FIG.11 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 129.
  • FIG.12 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 130.
  • FIG.13 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 131.
  • FIG.14 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 132.
  • FIG.15 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 133.
  • FIG.16 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 134.
  • FIG.17 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 135.
  • FIG.18 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 136.
  • FIG.19 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 137.
  • FIG.20 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 138.
  • FIG.21 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 139.
  • FIG.22 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 140.
  • FIG.23 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 141.
  • FIG.24 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 142.
  • FIG.25 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 144.
  • FIG.26 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 145.
  • FIG.27 shows a plot of compound-mediated phosphorylation of KRAS by AMPK with exemplary compound 146.
  • FIG.28 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 147.
  • FIG.29 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 148.
  • FIG.30 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 47.
  • FIG.31 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 149.
  • FIG.32 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 150.
  • FIG.33 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 151.
  • FIG.34 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 152.
  • FIG.35 shows a plot of compound-mediated phosphorylation of BRD4 by AMPK with exemplary compound 153.
  • bifunctional compounds that bind a target substrate (e.g., protein) and recruit a kinase (e.g., AMPK) to promote the phosphorylation of the target substrate (e.g., protein).
  • a target substrate e.g., protein
  • compounds that act as chemical probes having a detectable moiety e.g., luminescent materials, such as dyes
  • compounds useful in the production and manufacture of the bifunctional compounds and probes described herein are also provided.
  • the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof.
  • V 1 is CR 2 or N
  • each of R 2 , R 3 , and R 4 is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -CN, -N(R A ) 2 , -OR A , or -SR A ;
  • R 5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted acyl, or a nitrogen protecting group;
  • R 6 is
  • the compound of Formula (I) is not of formula:
  • the compound of Formula (I) is not of formula: ;
  • the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, and stereoisomers, and pharmaceutical compositions thereof. In some embodiments, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, and stereoisomers, and pharmaceutical compositions thereof. In some embodiments, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, tautomers, and stereoisomers, and pharmaceutical compositions thereof. In some embodiments, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, and tautomers, and pharmaceutical compositions thereof.
  • the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof.
  • the disclosure provides compounds that may be useful as intermediates in the preparation of the compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof.
  • the compound of Formula (II) is not of formula: [00133]
  • the disclosure provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, and stereoisomers, and pharmaceutical compositions thereof.
  • the disclosure provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, and stereoisomers, and pharmaceutical compositions thereof.
  • the disclosure provides compounds of Formula (II), and pharmaceutically acceptable salts, tautomers, and stereoisomers, and pharmaceutical compositions thereof.
  • the disclosure provides compounds of Formula (II), and pharmaceutically acceptable salts, and tautomers, and pharmaceutical compositions thereof. In some embodiments, the disclosure provides compounds of Formula (II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof.
  • V 1 [00134] As described herein, V 1 is CR 2 or N. In certain embodiments, V 1 is CR 2 . In certain embodiments, V 1 is N.
  • R 2 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -CN, -N(R A ) 2 , -OR A , or -SR A .
  • R 2 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroalkyl.
  • R 2 is hydrogen, halogen, or substituted or unsubstituted alkyl.
  • R 2 is hydrogen, halogen, or unsubstituted alkyl.
  • R 2 is halogen.
  • R 2 is fluoro.
  • R 2 is hydrogen.
  • R 3 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -CN, -N(R A ) 2 , -OR A , or -SR A .
  • R 3 is hydrogen, -CN, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroalkyl.
  • R 3 is hydrogen, -CN, halogen, or substituted or unsubstituted alkyl.
  • R 3 is substituted or unsubstituted alkyl.
  • R 3 is -CH 3 or -CF 3 .
  • R 3 is -CH 3 . In certain embodiments, R 3 is -CF3. In certain embodiments, R 3 is hydrogen. In certain embodiments, R 3 is halogen. In certain embodiments, R 3 is fluoro. In certain embodiments, R 3 is bromo. In certain embodiments, R 3 is chloro. In certain embodiments, R 3 is -CN.
  • R 4 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroalkyl, -CN -N(R A ) 2 , -OR A , or -SR A .
  • R 4 is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heteroalkyl.
  • R 4 is hydrogen, halogen, or substituted or unsubstituted alkyl.
  • R 4 is hydrogen, halogen, or unsubstituted alkyl.
  • R 4 is halogen.
  • R 4 is fluoro.
  • R 4 is hydrogen.
  • R 2 , R 3 , and R 4 are each independently hydrogen, -CN, halogen, or substituted or unsubstituted alkyl. In certain embodiments, R 2 , R 3 , and R 4 are each independently hydrogen, halogen, or substituted or unsubstituted alkyl. [00142] In certain embodiments, R 2 and R 4 are each independently hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is halogen. In certain embodiments, R 2 and R 4 are each hydrogen; and R 3 is halogen.
  • R 4 is hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is halogen. In certain embodiments, R 4 is hydrogen; and R 3 is halogen. [00143] In certain embodiments, R 2 and R 4 are each independently hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is chloro. In certain embodiments, R 2 and R 4 are each independently hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is -CN. In certain embodiments, R 2 and R 4 are each hydrogen; and R 3 is chloro. In certain embodiments, R 2 and R 4 are each hydrogen; and R 3 is -CN.
  • R 4 is hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is chloro. In certain embodiments, R 4 is hydrogen, halogen, or substituted or unsubstituted alkyl; and R 3 is -CN. In certain embodiments, R 4 is hydrogen; and R 3 is chloro. In certain embodiments, R 4 is hydrogen; and R 3 is -CN.
  • R 5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted acyl, or a nitrogen protecting group. In certain embodiments, R 5 is hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted alkyl.
  • R 5 is hydrogen or substituted or unsubstituted alkyl. In certain embodiments, R 5 is hydrogen or unsubstituted alkyl. In certain embodiments, R 5 is hydrogen. In certain embodiments, R 5 is a nitrogen protecting group. In certain embodiments, R 5 is 2-(trimethylsilyl)ethoxymethyl (SEM).
  • R 6 [00145] As described herein, R 6 is -OR C , -N(R B ) 2 , or substituted or unsubstituted alkyl. In certain embodiments, R 6 is -OR C or substituted or unsubstituted alkyl. [00146] In certain embodiments, R 6 is substituted or unsubstituted alkyl.
  • R 6 is unsubstituted alkyl. In certain embodiments, R 6 is unsubstituted C 1-4 alkyl. [00147] In certain embodiments, R 6 is -N(R B ) 2 . In certain embodiments, R 6 is -N(R B ) 2 , wherein each occurrence of R B is, independently, substituted or unsubstituted alkyl, or two R B groups are attached to the same atom to form a substituted or unsubstituted heterocyclic ring. In certain embodiments, R 6 is -N(CH3) 2 or . [00148] In certain embodiments, R 6 is -OR C .
  • R 6 is -OR C , wherein R C is substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted aryl.
  • R 6 is - OR C , wherein R C is substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocyclyl.
  • R 6 is -OR C , wherein R C is substituted or unsubstituted C 3-6 cycloalkyl, or substituted or unsubstituted 4-10 membered heterocyclyl.
  • R 6 is -OR C , wherein R C is substituted or unsubstituted C 3-6 cycloalkyl. In certain embodiments, , [00150] In certain embodiments, R 6 is -OR C , wherein R C is substituted or unsubstituted 4-10 membered heterocyclyl . In certain embodiments, R 6 is -OR C , wherein R C is substituted or unsubstituted 4-6 membered heterocyclyl or a sugar moiety. In certain embodiments, R 6 is , [00151] In certain embodiments, R 6 is -OR C , wherein R C is substituted or unsubstituted aryl.
  • R 6 is -OR C , wherein R C is substituted or unsubstituted phenyl. In . [00152] In certain embodiments, R 6 is -OR C , wherein R C is substituted or unsubstituted alkyl. In certain embodiments, R 6 is -OR C , wherein R C is substituted alkyl. In certain embodiments, R 6 is -OR C , wherein R C is substituted C 1-4 alkyl. In certain embodiments, R 6 is . [00153] In certain embodiments, R 6 is methyl, ethyl, isopropyl, ,
  • R 6 is methyl. In certain embodiments, R 6 is ethyl. In certain embodiments, R 6 is isopropyl. In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, certain embodiments, certain embodiments, R 6 is . In certain embodiments, certain embodiments, certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments
  • R 6 is . In certain embodiments, certain embodiments, certain embodiments, . In certain embodiments, R 6 is In certain embodiments, R 6 is In certain embodiments, R 6 is . In certain embodiments, R 6 is . In certain embodiments, certain embodiments, certain embodiments, certain embodiments, embodiments, certain embodiments, certain embodiments, R 6 is embodiments, certain embodiments, . In certain embodiments, embodiments, certain embodiments, R 6 is . In certain embodiments, R 6 is -N(CH 3 ) 2 . In certain embodiments, . [00156] In certain embodiments, R 6 is not certain embodiments, R 6 is not certain embodiments, R 6 is not .
  • A is a bond or an orienting moiety.
  • An orienting moiety is a group that acts as a spacer between the bicyclic kinase-binding moiety (e.g., AMPK-binding moiety) and L, the linker of the disclosed compounds.
  • the orienting moiety spatially orients or establishes the position and direction from which the linker attaches to the AMPK-binding moiety (i.e., the orientation in space into which the linker extends), thus having an impact on the overall geometry of the compound.
  • A is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted carbocyclylene, substituted or unsubstituted heterocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene; and Y is a bond, -NR A -, -O-, -S-, -S(O) 2 -, -S(O)-, -C ⁇ C-, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted C1-2 alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted heterocyclylene, or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted carbocyclylene, substituted or unsubstituted heterocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene; and Y is a bond, substituted or unsubstituted heteroalkylene, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted heterocyclylene, substituted or unsubstituted carbocyclylene, or substituted or unsubstituted arylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is a bond, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted carbocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is a bond, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted carbocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heterocyclylene.
  • A is of formula: , ,
  • A is of formula: certain embodiments, A is of formula: certain embodiments, A is of formula: .
  • A is of formula: .
  • A is of formula: -X-Y-, wherein: X is a bond, -NR A -, -O-, -S-, -S(O) 2 -, -S(O)-, -C ⁇ C-, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted C1-2 alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted heterocyclylene, or substituted or unsubstituted carbocyclylene; and Y is substituted or unsubstituted carbocyclylene, substituted or unsubstituted heterocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene.
  • A is of formula: -X-Y-, wherein: X is -C ⁇ C-; and Y is substituted or unsubstituted arylene. In certain embodiments, A is of formula . [00168] In certain embodiments, A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is substituted or unsubstituted heteroarylene. In certain [00169] In certain embodiments, A is not of formula: .
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene; and Y is a bond, substituted or unsubstituted methylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted heterocyclylene, or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is a bond, substituted or unsubstituted methylene, or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is a bond, substituted or unsubstituted methylene, or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is a bond.
  • A is of formula: .
  • A is of formula: .
  • a i is of formula:
  • A is of formula: .
  • A is of formula: .
  • A is of formula: .
  • A is of formula: .
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is substituted or unsubstituted methylene or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is substituted or unsubstituted methylene or substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is substituted or unsubstituted methylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted arylene; and Y is substituted or unsubstituted carbocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is substituted or unsubstituted methylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted phenylene; and Y is substituted or unsubstituted carbocyclylene.
  • A is of formula: wherein n is 0 or 1; m is 0 or 1; R y1 is hydrogen, C 1-6 alkyl, or halogen; and R y2 is hydrogen, C 1-6 alkyl, or halogen.
  • A is of formula: ; wherein n is 0 or 1; m is 0 or 1.
  • A is of formula: hydrogen, C 1-6 alkyl, or halogen; and R y2 is hydrogen, C 1-6 alkyl, or halogen.
  • A is of formula: wherein n is 0 or 1; m is 0 or 1; R y1 is C1-6 alkyl or halogen; and R y2 is C 1-6 alkyl or halogen.
  • A is of formula: wherein n is 0 or 1; m is 0 or 1.
  • A is of formula: ; wherein R y1 is C1-6 alkyl or halogen; and R y2 is C1-6 alkyl or halogen.
  • A is of formula: ; wherein n is 0 or 1; m is 0 or 1; R y1 is C 1-6 alkyl; and R y2 is C 1-6 alkyl.
  • A is of formula: i i wherein n is 0 or 1; m is 0 or 1; R y1 is C1-3 alkyl; and R y2 is C1-3 alkyl.
  • A is of formula: ; wherein n is 0 or 1; m is 0 or 1. In certain embodiments, A is
  • A is of formula: certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: certain embodiments, A is of formula: . [00177] In certain embodiments, A is of formula -X-Y-, wherein: X is substituted or unsubstituted carbocyclylene; and Y is a bond. In certain embodiments, A is of formula: certain embodiments, A is of formula: . In certain embodiments, A is of formula: certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: .
  • A is of formula -X O -X-Y-, wherein X O is a bond, -NR A -, -O-, -S-, -S(O) 2 -, or -S(O)-; X is substituted or unsubstituted carbocyclylene, substituted or unsubstituted heterocyclylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene; and Y is a bond, -NR A -, -O-, -S-, -S(O) 2 -, -S(O)-, -C ⁇ C-, substituted or unsubstituted -C ⁇ C-heterocyclylene, substituted or unsubstituted C 1-2 alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted heterocyclylene, or substituted or unsubstituted
  • A is of formula -X O -X-Y-, wherein X O is - NR A -, -O-, -S-, -S(O) 2 -, or -S(O)-; X is substituted or unsubstituted carbocyclylene; and Y is a bond.
  • A is of formula: .
  • A is of formula: -X-Y-; X is substituted or unsubstituted heterocyclylene; and Y is a bond or substituted or unsubstituted arylene.
  • A is of formula: .
  • A is of formula: embodiments, A is of formula: certain embodiments, A is of formula: certain embodiments, A is of formula: certain embodiments, A is of formula: . In certain embodiments, A is of formula: . In certain embodiments, A is of formula: . [00180] In certain embodiments, A is of formula: -X-Y-, wherein: X is substituted or unsubstituted heteroarylene; and Y is a bond or substituted or unsubstituted heterocyclylene. In certain embodiments, A is of formula: -X-Y-, wherein: X is substituted or unsubstituted 6- membered heteroarylene; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, substituted or unsubstituted pyrimidine, or substituted or unsubstituted pyrazine; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is a bond or substituted or unsubstituted heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, substituted or unsubstituted pyrimidine, or substituted or unsubstituted pyrazine, substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, substituted or unsubstituted pyrimidine, or substituted or unsubstituted pyrazine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is a bond or substituted or unsubstituted 6-7 membered heterocyclylene.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, substituted or unsubstituted pyrimidine, or substituted or unsubstituted pyrazine; and Y is a bond, substituted or unsubstituted piperidine, substituted or unsubstituted piperazine, or substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is a bond, substituted or unsubstituted piperidine, substituted or unsubstituted piperazine, or substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted piperidine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted piperazine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine, or substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is a bond, substituted or unsubstituted piperidine, substituted or unsubstituted piperazine, or substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is substituted or unsubstituted piperidine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is substituted or unsubstituted piperazine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyridine; and Y is substituted or unsubstituted 2,6- diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is a bond, substituted or unsubstituted piperidine, substituted or unsubstituted piperazine, or substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted piperidine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted piperazine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrimidine; and Y is substituted or unsubstituted 2,6- diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is a bond, substituted or unsubstituted piperidine, substituted or unsubstituted piperazine, or substituted or unsubstituted 2,6-diazaspiro[3.3]heptane.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is a bond.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is substituted or unsubstituted piperidine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is substituted or unsubstituted piperazine.
  • A is of formula: -X-Y-, wherein: X is substituted or unsubstituted pyrazine; and Y is substituted or unsubstituted 2,6- diazaspiro[3.3]heptane.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl.
  • A is of formula: , wherein R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • R x is -OR A .
  • R x is -OR A , wherein R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R x is -OR A , wherein R A is unsubstituted C 1-4 alkyl. [00197] In certain embodiments, A is of formula:
  • A is of formula: .
  • L is a bond or a linker. In certain embodiments, L is a bond. In certain embodiments, L is a linker. In certain embodiments, L is a chain of at least 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or 15 contiguous atoms. In certain embodiments, L is a chain of at least 1 atom. In certain embodiments, L is a chain of at least 2 contiguous atoms. In certain embodiments, L is a chain of at least 3 contiguous atoms. In certain embodiments, L is a chain of at least 4 contiguous atoms.
  • L is a chain of at least 5 contiguous atoms. In certain embodiments, L is a chain of at least 6 contiguous atoms. In certain embodiments, L is a chain of at least 7 contiguous atoms. In certain embodiments, L is a chain of at least 8 contiguous atoms. In certain embodiments, L is a chain of at least 9 contiguous atoms. In certain embodiments, L is a chain of at least 10 contiguous atoms. In certain embodiments, L is a chain of at least 11 contiguous atoms. In certain embodiments, L is a chain of at least 12 contiguous atoms. In certain embodiments, L is a chain of at least 13 contiguous atoms.
  • L is a chain of at least 14 contiguous atoms. In certain embodiments, L is a chain of at least 15 contiguous atoms. In certain embodiments, L is a chain of any range of from 1 to 15 contiguous atoms. [00203] In certain embodiments of L disclosed herein where L is depicted as a chemical structure, the lefthand attachment point is to A and the righthand attachment point is to B when B is present; or the lefthand attachment point is to A and the righthand attachment point is to T when T is present.
  • the lefthand attachment point is to B and the righthand attachment point is to A when B is present; or the lefthand attachment point is to T and the righthand attachment point is to A when T is present.
  • t is 0-20; and
  • u is 0-6; provided that L comprises at least one atom.
  • L is of formula: t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: , wherein: t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: , wherein: t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: Z 3 is a bond or -N(R A )-; t is 0-20; and u is 0-6; provided that L comprises at least one atom. [00223] In certain embodiments, L is of formula: , wherein:
  • Z 3 is a bond or -N(R A )-; t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: , wherein: t is 0-20; and u is 0-6; provided that L comprises at least one atom.
  • L is of formula: , wherein: t is 0-20; and u is 0-6; provided that L comprises at least one atom. [00227] In certain embodiments, L is of formula: , wherein: t is 0-20; and u is 0-6; provided that L comprises at least one atom. [00228] In certain embodiments, L is of formula:
  • L is of formula: [00230] In certain embodiments, L is of formula: . [00231] In certain embodiments, L is of formula: . [00232] In certain embodiments, L is of formula: . [00233] In certain embodiments, L is of formula: . [00234] In certain embodiments, L is of formula: . [00235] In certain embodiments, L is of formula: . [00236] In certain embodiments, L is of formula: . [00237] In certain embodiments, L is of formula: . [00238] In certain embodiments, L is of formula: . [00239] In certain embodiments, L is of formula: .
  • L is of formula: . [00241] In certain embodiments, L is of formula: . [00242] In certain embodiments, L is of formula: . [00243] In certain embodiments, L is of formula: . [00244] In certain embodiments, L is of formula: . [00245] In certain embodiments, L is of formula: . [00246] In certain embodiments, L is of formula: . [00247] In certain embodiments, L is of formula: . [00248] In some embodiments, L is of formula: , , , or . [00249] In certain embodiments, L is selected from any one of L1-L73:
  • L is of formula L2, L4, L10, L12, L13, L16, L17, L18, L20, L21, L23, L27, L28, L29, L30, L32, L37, L40, L46, L47, L51, L52, L53, L54, L55, L56, L57, L58, L59, L60, L68, L69, L70, L71, L72, or L73.
  • L is of formula L2, L4, L12, L16, L17, L18, L20, L23, L27, L28, L29, L32, L37, L40, L46, L47, L51, L52, L53, L54, L68, L69, L70, L71, L72, or L73.
  • L is of formula L2.
  • L is of formula L4.
  • L is of formula L10.
  • L is of formula L12.
  • L is of formula L13.
  • L is of formula L16.
  • L is of formula L17.
  • L is of formula L18.
  • L is of formula L20.
  • L is of formula L21. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55.
  • L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59.. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. [00251] In certain embodiments, L is of formula:
  • L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: mula: . In some embodiments, L is of formula: .
  • L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: mula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of f . n some em o ments, s o ormua: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of
  • L is of formula: .
  • t is 1-20, 1-10, 1-8, 1-6, 1-5, 1-4, 1-3, or 1-2. In certain embodiments, t is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20.
  • u is 1-6, 1-5, 1-4, 1-3, or 1-2. In certain embodiments, u is 1, 2, 3, 4, 5, or 6.
  • L is selected from any one of L74-L232:
  • L is selected from any one of L1-L232.
  • L is of formula L75, L76, L79, L80, L82, L83, L84, L87, L88, L89, L90, L92, L93, L94, L95, L96, L97, L99, L101, L102, L103, L105, L106, L107, L108, L109, L110, L111, L112, L113, L115, L116, L117, L118, L119, L120, L137, L138, L139, L140, L141, L149, L153, L182, L187, L189, L191, L192, L193, L194, L195, L196, L197, L198, L199, L200, L201, L202, L203, L214, L215, L216, L217, L218, L222, L223, L224, L225, L226, L227, L228, L2
  • L is of formula L75, L76, L79, L80, L87, L88, L93, L94, L95, L96, L97, L99, L101, L102, L103, L105, L106, L107, L108, L109, L110, L111, L112, L113, L137, L138, L139, L140, L141, L149, L153, L182, L187, L189, L191, L192, L193, L194, L195, L196, L197, L198, L200, L201, L202, L203, L223, L224, L225, L226, L227, L228, L229, L230, L231, or L232.
  • L is of formula L75, L76, L79, L80, L87, L88, L93, L94, L95, L96, L97, L99, L101, L102, L103, L105, L106, L107, L108, L109, L110, L111, L112, L113, L137, L138, L139, L140, L141, L149, L153, L182, L187, L189, L191, L192, L193, L194, L195, L196, L197, L198, L200, L201, L202, L203, L223, L224, L225, L226, L227, L228, L229, L230, or L231.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95.
  • L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L115.
  • L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232. [00262] In certain embodiments, L is of formula:
  • L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: mbodiments, L is of formula: . In some embodiments, L is o ormu a: . In some embodiments, L is of formula: some embodiments, L is of formula: .
  • L is of some embodiments, L is of formula: . In some embodiments, L is of . , . In some embodiments, L is of formula: . In some embodiments, L is of formula: bodiments, L is of formula: . In some embodiments, L is . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments,
  • L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: In some embodiments, L is of formula: In some embodiments, L is of formula: . In some embodiments, L is of formula: In some embodiments, L is of formula: some embodiments, L is of formula: some embodiments, L is of formula: ormula: . In some embodiments, L is of formula: . me embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: .
  • L is of formula: embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of formula: . In some embodiments, L is of . [00264] In certain embodiments, L is of formula:
  • L is not: .
  • L is not: .
  • L is not one or more of the following:
  • L is not . In certain embodiments, L i
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, a sulfur protecting group when attached to a sulfur atom, an oxygen protecting group when attached to an oxygen atom, or a nitrogen protecting group when attached to a nitrogen atom, or two R A groups are attached to the same atom to form a substituted or unsubstituted heterocyclic or substituted or unsubstituted heteroaryl ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, a sulfur protecting group when attached to a sulfur atom, an oxygen protecting group when attached to an oxygen atom, or a nitrogen protecting group when attached to a nitrogen atom, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring or a substituted or unsubstituted heteroaryl ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, a nitrogen protecting group when attached to a nitrogen atom, an oxygen protecting group when attached to an oxygen atom, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted 5-6 membered heterocyclyl, substituted or unsubstituted phenyl, substituted or unsubstituted 5-6 membered heteroaryl, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C1-30 heteroalkyl, substituted or unsubstituted 5-6 membered heterocyclyl, substituted or unsubstituted phenyl, substituted or unsubstituted 5-6 membered heteroaryl, or two R A groups are joined to form a substituted or unsubstituted heterocyclic ring.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C1-30 heteroalkyl.
  • each occurrence of R A is, independently, hydrogen, substituted or unsubstituted C 1-6 alkyl, or substituted or unsubstituted C 1-20 heteroalkyl.
  • each occurrence of R A is, independently, hydrogen, or substituted or unsubstituted C 1-6 alkyl. In certain embodiments, R A is hydrogen or substituted or unsubstituted alkyl. In certain embodiments, R A is substituted or unsubstituted alkyl. In certain embodiments, R A is substituted or unsubstituted C 1-4 alkyl. In certain embodiments, R A is unsubstituted C 1-4 alkyl.
  • R A is t-butyl. In certain embodiments, R A is methyl. In certain embodiments, R A is t-butyl, n-butyl, n-propyl, iso-propyl, ethyl, methyl, or hydrogen In certain embodiments, R A is methyl. In certain embodiments, R A is t-butyl, methyl, or hydrogen. In certain embodiments, R A is t-butyl or hydrogen. In certain embodiments, R A is hydrogen.
  • B is a targeting moiety or detectable moiety (e.g., a chromophore, dye, fluorophore, luminophore or luminescent material, or radioactive material).
  • B is a detectable moiety (e.g., a chromophore, dye, fluorophore, luminophore or luminescent material, or radioactive material).
  • B is a dye.
  • B is a targeting moiety.
  • the targeting moiety is a bioactive moiety.
  • the targeting moiety is a protein-binding moiety.
  • the targeting moiety binds an enzyme.
  • the luminescent material is a phosphorescent agent.
  • the targeting moiety provides a means for recruiting, binding, modulating, modifying, inhibiting, and/or associating the compound with a target substrate.
  • the target substrate is a biomolecule.
  • the target substrate is a polypeptide, a polynucleotide, or a polysaccharide.
  • the target substrate is a protein.
  • B is a ligand, binder, modulator, modifier, and/or inhibitor of a protein.
  • B is a protein-binding moiety.
  • B is an inhibitor of a protein.
  • B is an inhibitor of an enzyme.
  • the compounds disclosed herein may bind to a kinase, such as AMPK, and to a target substrate associated with the targeting moiety in order to alter the function of the kinase or the target substrate.
  • a compound recruits, binds, modulates, modifies, inhibits, activates, and/or associates with a kinase, such as AMPK, to phosphorylate the target substrate associated with the targeting moiety.
  • the target substrate e.g., protein
  • the target substrate is not a natural substrate of the kinase to which the compound also binds.
  • the compounds disclosed herein include a moiety that binds to a kinase, such as AMPK, and a targeting moiety that binds to a second kinase.
  • the compounds disclosed herein include a moiety that binds to a kinase, such as AMPK, and a targeting moiety that binds to a phosphatase.
  • B is a BTK-binding moiety, bromodomain and extra-terminal domain (BET)-binding moiety, BRD2-binding moiety, BRD3-binding moiety, BRD4-binding moiety, BRDT-binding moiety, a kinase-binding moiety, KRAS-binding moiety, TRIM24- binding moiety, CAII-binding moiety, or a phosphatase-binding moiety.
  • B is a BTK-binding moiety.
  • B is a bromodomain and extra-terminal domain (BET)-binding moiety.
  • B is a BRD2-binding moiety. In some embodiments, B is a BRD3-binding moiety. In some embodiments, B is a BRD4-binding moiety. In some embodiments, B is a BRDT-binding moiety. In some embodiments, B is a kinase-binding moiety. In some embodiments, B is a KRAS-binding moiety. In some embodiments, B is a phosphatase-binding moiety. In some embodiments, B is a TRIM24-binding moiety. In some embodiments, B is a CAII-binding moiety.
  • B is a moiety that recruits, binds, modulates, modifies, inhibits, activates, and/or associates with 5'-AMP-activated protein kinase (AMPK) or isoforms of AMPK, a bromodomain-containing protein (e.g., BRD2, BRD3, BRD4, BRDT); histone acetyltransferase (e.g., CREBBP, GCN5, PCAF, TAFII250); methyltransferase (e.g., ASH1L, MLL); Swi2/Snf2; estrogen receptor; p53; Max; beta-catenin; BTK; BCR-ABL; KRAS (K-Ras protein or Kirsten rat sarcoma virus protein) or KRAS mutant; TRIM24 (Tripartite motif- containing 24); MDM2; EGFR; CDK4; CDK6; C-MET; PSENEN (presen
  • AMPK 5'-AMP
  • CTSB cerebrospinal bovine serum
  • PSEN1 presenilin 1
  • APP amyloid beta (A4) precursor protein
  • APH1B anterior pharynx defective 1 homolog B (C. elegans)
  • PSEN2 presenilin 2
  • BACE1 beta-site APP-cleaving enzyme 1
  • ITM2B integrated membrane protein 2B
  • CTSD cathepsin D
  • NOTCH1 Notch homolog 1, translocation-associated
  • TNF tumor necrosis factor (TNF superfamily, member 2
  • INS INS
  • insulin DYT10 (dystonia 10); ADAM17 (ADAM metallopeptidase domain 17); APOE (apolipoprotein E); ACE (angiotensin I converting enzyme (peptidyl-dipeptidase A) 1); STN (statin); TP53 (tumor protein p53); IL6 (interleukin 6 (interferon, beta
  • B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with KRAS or KRAS mutant, BRD4, CAII, TRIM24, BTK, BET, BRD2, BRD3, or BRDT.
  • B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BRD4 or BTK.
  • B is a ligand, recruiter, binder, modulator, modifier, inhibitor, activator, and/or associator of KRAS or KRAS mutant, BRD4, CAII, TRIM24, or BTK.
  • B is a ligand, recruiter, binder, modulator, modifier, inhibitor, activator, and/or associator of BRD4 or BTK.
  • B is an inhibitor of KRAS or KRAS mutant, BRD4, CAII, TRIM24, or BTK.
  • B is an inhibitor of BRD4 or BTK.
  • B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with KRAS or KRAS mutant.
  • B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BRD4.
  • B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BTK. In certain embodiments, B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BET. In certain embodiments, B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BRD2. In certain embodiments, B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BRD3. In certain embodiments, B recruits, binds, modulates, modifies, inhibits, activates, and/or associates with BRDT. In certain embodiments, B is an inhibitor of KRAS or KRAS mutant.
  • B is an inhibitor of BRD4. In certain embodiments, B is an inhibitor of CAII. In certain embodiments, B is an inhibitor of TRIM24. In certain embodiments, B is an inhibitor of BTK. In certain embodiments, B is an inhibitor of BET. In certain embodiments, B is an inhibitor of BRD2. In certain embodiments, B is an inhibitor of BRD3. In certain embodiments, B is an inhibitor of BRDT. [00290] In certain embodiments, B is a KRAS-binding moiety, a kinase-binding moiety or a phosphatase-binding moiety. [
  • B is of formula:
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is of formula: , or a pharmaceutically acceptable salt thereof.
  • B is a detectable moiety. In certain embodiments, B is a chromophore. In certain embodiments, B is a dye. In certain embodiments, B is a fluorophore. In certain embodiments, B is a luminophore. In certain embodiments, B is a luminescent material. In certain embodiments, B is a radioactive material. [00300] In certain embodiments, B is a dye. In certain embodiments, B is a fluorescent dye. In certain embodiments, B is of formula: [00301] In certain embodiments, B is of formula: or a pharmaceutically acceptable salt thereof. [00302] In certain embodiments, B is of formula: , or a pharmaceutically acceptable salt thereof.
  • the targeting moiety B binds a target substrate (e.g., protein) with a Kd of less than 20,000 nM, less than 10,000 nM, less than 5,000 nM, less than 2,500 nM, less than 1,000 nM, less than 900 nM, less than 800 nM, less than 700 nM, less than 600 nM, less than 500 nM, less than 400 nM, less than 300 nM, less than 200 nM, less than 100 nM, less than 90 nM, less than 80 nM, less than 70 nM, less than 60 nM, less than 50 nM, less than 40 nM, less than 30 nM, less than 20 nM, less than 10 nM, less than 5 nM, less than 4 nM, less than 3 nM, less than 2 nM, or less than 1 nM.
  • a target substrate e.g., protein
  • the targeting moiety B selectively binds a target substrate (e.g., protein) as compared to another substrate (e.g., protein).
  • the selectivity is from about 2-fold to about 5-fold. In certain embodiments, the selectivity is from about 5-fold to about 10-fold. In certain embodiments, the selectivity is from about 10-fold to about 20-fold. In certain embodiments, the selectivity is from about 20-fold to about 50-fold. In certain embodiments, the selectivity is from about 50-fold to about 100-fold. In certain embodiments, the selectivity is from about 100-fold to about 200-fold.
  • the selectivity is from about 200-fold to about 500-fold. In certain embodiments, the selectivity is from about 500-fold to about 1000-fold. In certain embodiments, the selectivity is at least about 1000-fold.
  • T is hydrogen, a protecting group, a nucleophilic group, an electrophilic group, a leaving group, or a click chemistry handle. In certain embodiments, T is hydrogen, a nucleophilic group, an electrophilic group, a leaving group, a nitrogen protecting group, an oxygen protecting group, or a click chemistry handle.
  • T is hydrogen, a nucleophilic group, an electrophilic group, a leaving group, or a click chemistry handle [00306] In certain embodiments, T is a click chemistry handle.
  • Click chemistry refers to a chemical approach to conjugation introduced by Sharpless in 2001 and describes chemistry tailored to generate substances quickly and reliably by joining units together. See, e.g., Kolb, Finn and Sharpless Angewandte Chemie International Edition 200140, 2004–2021; Evans, Australian Journal of Chemistry 200760, 384–395).
  • Exemplary coupling reactions include, but are not limited to, formation of esters, thioesters, amides (e.g., such as peptide coupling) from activated acids or acyl halides; nucleophilic displacement reactions (e.g., such as nucleophilic displacement of a halide or ring opening of strained ring systems); azide–alkyne Huisgen cycloaddition; thiol–yne addition; imine formation; Michael additions (e.g., maleimide addition reactions); and Diels–Alder reactions (e.g., tetrazine [4 + 2] cycloaddition).
  • nucleophilic displacement reactions e.g., such as nucleophilic displacement of a halide or ring opening of strained ring systems
  • azide–alkyne Huisgen cycloaddition thiol–yne addition
  • imine formation Michael additions (e.g., maleimide addition reactions)
  • click chemistry reactions and click-chemistry handles can be found in, e.g., Kolb, H. C.; Finn, M. G. and Sharpless, K. B., Angew. Chem. Int. Ed.2001, 40, 2004-2021. Kolb, H. C. and Sharless, K. B. Drug Disc. Today, 2003, 8, 112-1137; Rostovtsev, V. V.; Green L. G.; Fokin, V. V. and Shrapless, K. B. Angew. Chem. Int. Ed.2002, 41, 2596-2599; Tomoe, C. W.; Christensen, C. and Meldal, M. J. Org. Chem.2002, 67, 3057- 3064.
  • click chemistry handles are used that can react to form covalent bonds in the absence of a metal catalyst.
  • click chemistry handles are known to those of skill in the art and include the click chemistry handles described in Becer, Hoogenboom, and Schubert, Click Chemistry beyond Metal-Catalyzed Cycloaddition, Angewandte Chemie International Edition (2009) 48: 4900 – 4908.
  • the click-chemistry handle comprises an alkenylene group or alkynylene group.
  • the click-chemistry handle comprises an internal alkenylene group or alkynylene group.
  • the click-chemistry handle comprises a terminal alkenylene group or alkynylene group.
  • the click- chemistry handle is –CoCH, substituted or unsubstituted cyclooctynyl optionally fused independently with one or more instances of substituted or unsubstituted phenyl, substituted or unsubstituted cyclopropenyl, substituted or unsubstituted cyclobutenyl, substituted or unsubstituted trans-cyclooctenyl optionally fused independently with one or more instances of substituted or unsubstituted phenyl, or substituted or unsubstituted .
  • the click chemistry handle is an azide, tetrazine, tetrazole, dithioester, anthracene, amine, or thiol.
  • T is hydrogen, a nucleophilic group, an electrophilic group, a leaving group, or a click chemistry handle.
  • T is hydrogen, a nucleophilic group, a leaving group, a nitrogen protecting group, or an oxygen protecting group.
  • T is hydrogen, a nucleophilic group, a leaving group, or a nitrogen protecting group.
  • T is hydrogen, -OR A , -N 3 , -COOR A , -C ⁇ CH, halogen, or a nitrogen protecting group.
  • T is hydrogen, an amine, a carboxylic acid, an aldehyde, an alkyne, an alkene, an azide, an alcohol, a halogen, or a nitrogen protecting group.
  • T is hydrogen, halogen, -OH, -OMe, -OtBu, -OMs (mesylate), -OTs (tosylate), or -C ⁇ CH. In certain embodiments, T is -C ⁇ CH. In certain embodiments, T is hydrogen or a halogen (e.g., -Br). In certain embodiment, T is halogen. In certain embodiments, T is -Cl or -Br. In certain embodiments, T is -Br.
  • T is hydrogen, -OH, -OMe, -OtBu, -OMs (mesylate), -OTs (tosylate), -C ⁇ CH, -Br, or a nitrogen protecting group (e.g., Boc). In certain embodiments, T is a nitrogen protecting group (e.g., Boc). In certain embodiments, T is hydrogen, -OH, -OMe, or -OtBu. In certain embodiments, T is -OH or -OMe. In certain embodiments, T is -OH. In certain embodiments, T is hydrogen. In certain embodiments, T is -NHR A . In certain embodiments, T is -NH2. In certain embodiments, T is -Cl.
  • the compound of Formula (I) is a compound of Formula (I-a): (I-a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, R 3 , R 4 , R 5 , and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 1): (I-a-1), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, R 3 , and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-1), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 2): (I-a-2), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-2), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 3): (I-a-3), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-3), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 4): (I-a-4), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-4), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232..
  • the compound of Formula (I) is a compound of Formula (I-a- 5): (I-a-5), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-5), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 5a): (I-a-5a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-5a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 6): (I-a-6), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-6), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 6a): (I-a-6a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-6a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 7): (I-a-7), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-7), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 7a): (I-a-7a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-7a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 7b): (I-a-7b), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-7b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 8): (I-a-8), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-8), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 9): (I-a-9), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-9), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 9a): (I-a-9a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-9a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 10): (I-a-10), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-10), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 10a): (I-a-10a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-10a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 11): (I-a-11), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-11), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 12): (I-a-12), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-12), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 13): (I-a-13), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-13), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 14): (I-a-14), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-14), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 15): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-15), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 16): (I-a-16), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-16), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 17): (I-a-17), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-17), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 18): (I-a-18), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-18), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 19): (I-a-19), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-19), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 20): (I-a-20), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-20), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 21): (I-a-21), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-21), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 22): (I-a-22), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-22), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 23): (I-a-23), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-23), wherein L is any one of L1-L120, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 24): (I-a-24), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-24), wherein L is any one of L1-L120, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 25): (I-a-25), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-25), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 26): (I-a-26), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-26), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 27): (I-a-27), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-27), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 28): (I-a-28), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-28), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 29): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-a-29), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2.
  • L is of formula L3.
  • L is of formula L4.
  • L is of formula L5.
  • L is of formula L6.
  • L is of formula L7.
  • L is of formula L8.
  • L is of formula L9.
  • L is of formula L10.
  • L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26.
  • L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42.
  • L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58.
  • L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74.
  • L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90.
  • L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106.
  • L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122.
  • L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137.
  • L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153.
  • L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169.
  • L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185.
  • L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201.
  • L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216.
  • L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231.
  • L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 30): (I-a-30), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-30), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1. In certain embodiments, L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16.
  • L is of formula L17. In certain embodiments, L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32.
  • L is of formula L33. In certain embodiments, L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48.
  • L is of formula L49. In certain embodiments, L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64.
  • L is of formula L65. In certain embodiments, L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80.
  • L is of formula L81. In certain embodiments, L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96.
  • L is of formula L97. In certain embodiments, L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112.
  • L is of formula L113. In certain embodiments, L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127.
  • L is of formula L128. In certain embodiments, L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142.
  • L is of formula L143. In certain embodiments, L is of formula L144. In certain embodiments, L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158.
  • L is of formula L159. In certain embodiments, L is of formula L160. In certain embodiments, L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173.
  • L is of formula L174. In certain embodiments, L is of formula L175. In certain embodiments, L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189.
  • L is of formula L190. In certain embodiments, L is of formula L191. In certain embodiments, L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205.
  • L is of formula L206. In certain embodiments, L is of formula L207. In certain embodiments, L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220.
  • L is of formula L221. In certain embodiments, L is of formula L222. In certain embodiments, L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I-a- 31): (I-a-31), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-a-31), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • L is of formula L1.
  • L is of formula L2. In certain embodiments, L is of formula L3. In certain embodiments, L is of formula L4. In certain embodiments, L is of formula L5. In certain embodiments, L is of formula L6. In certain embodiments, L is of formula L7. In certain embodiments, L is of formula L8. In certain embodiments, L is of formula L9. In certain embodiments, L is of formula L10. In certain embodiments, L is of formula L11. In certain embodiments, L is of formula L12. In certain embodiments, L is of formula L13. In certain embodiments, L is of formula L14. In certain embodiments, L is of formula L15. In certain embodiments, L is of formula L16. In certain embodiments, L is of formula L17.
  • L is of formula L18. In certain embodiments, L is of formula L19. In certain embodiments, L is of formula L20. In certain embodiments, L is of formula L21. In certain embodiments, L is of formula L22. In certain embodiments, L is of formula L23. In certain embodiments, L is of formula L24. In certain embodiments, L is of formula L25. In certain embodiments, L is of formula L26. In certain embodiments, L is of formula L27. In certain embodiments, L is of formula L28. In certain embodiments, L is of formula L29. In certain embodiments, L is of formula L30. In certain embodiments, L is of formula L31. In certain embodiments, L is of formula L32. In certain embodiments, L is of formula L33.
  • L is of formula L34. In certain embodiments, L is of formula L35. In certain embodiments, L is of formula L36. In certain embodiments, L is of formula L37. In certain embodiments, L is of formula L38. In certain embodiments, L is of formula L39. In certain embodiments, L is of formula L40. In certain embodiments, L is of formula L41. In certain embodiments, L is of formula L42. In certain embodiments, L is of formula L43. In certain embodiments, L is of formula L44. In certain embodiments, L is of formula L45. In certain embodiments, L is of formula L46. In certain embodiments, L is of formula L47. In certain embodiments, L is of formula L48. In certain embodiments, L is of formula L49.
  • L is of formula L50. In certain embodiments, L is of formula L51. In certain embodiments, L is of formula L52. In certain embodiments, L is of formula L53. In certain embodiments, L is of formula L54. In certain embodiments, L is of formula L55. In certain embodiments, L is of formula L56. In certain embodiments, L is of formula L57. In certain embodiments, L is of formula L58. In certain embodiments, L is of formula L59. In certain embodiments, L is of formula L60. In certain embodiments, L is of formula L61. In certain embodiments, L is of formula L62. In certain embodiments, L is of formula L63. In certain embodiments, L is of formula L64. In certain embodiments, L is of formula L65.
  • L is of formula L66. In certain embodiments, L is of formula L67. In certain embodiments, L is of formula L68. In certain embodiments, L is of formula L69. In certain embodiments, L is of formula L70. In certain embodiments, L is of formula L71. In certain embodiments, L is of formula L72. In certain embodiments, L is of formula L73. In certain embodiments, L is of formula L74. In certain embodiments, L is of formula L75. In certain embodiments, L is of formula L76. In certain embodiments, L is of formula L77. In certain embodiments, L is of formula L78. In certain embodiments, L is of formula L79. In certain embodiments, L is of formula L80. In certain embodiments, L is of formula L81.
  • L is of formula L82. In certain embodiments, L is of formula L83. In certain embodiments, L is of formula L84. In certain embodiments, L is of formula L85. In certain embodiments, L is of formula L86. In certain embodiments, L is of formula L87. In certain embodiments, L is of formula L88. In certain embodiments, L is of formula L89. In certain embodiments, L is of formula L90. In certain embodiments, L is of formula L91. In certain embodiments, L is of formula L92. In certain embodiments, L is of formula L93. In certain embodiments, L is of formula L94. In certain embodiments, L is of formula L95. In certain embodiments, L is of formula L96. In certain embodiments, L is of formula L97.
  • L is of formula L98. In certain embodiments, L is of formula L99. In certain embodiments, L is of formula L100. In certain embodiments, L is of formula L101. In certain embodiments, L is of formula L102. In certain embodiments, L is of formula L103. In certain embodiments, L is of formula L104. In certain embodiments, L is of formula L105. In certain embodiments, L is of formula L106. In certain embodiments, L is of formula L107. In certain embodiments, L is of formula L108. In certain embodiments, L is of formula L109. In certain embodiments, L is of formula L110. In certain embodiments, L is of formula L111. In certain embodiments, L is of formula L112. In certain embodiments, L is of formula L113.
  • L is of formula L114. In certain embodiments, L is of formula L115. In certain embodiments, L is of formula L116. In certain embodiments, L is of formula L117. In certain embodiments, L is of formula L118. In certain embodiments, L is of formula L119. In certain embodiments, L is of formula L120. In certain embodiments, L is of formula L121. In certain embodiments, L is of formula L122. In certain embodiments, L is of formula L123. In certain embodiments, L is of formula L124. In certain embodiments, L is of formula L125. In certain embodiments, L is of formula L126. In certain embodiments, L is of formula L127. In certain embodiments, L is of formula L128.
  • L is of formula L129. In certain embodiments, L is of formula L130. In certain embodiments, L is of formula L131. In certain embodiments, L is of formula L132. In certain embodiments, L is of formula L133. In certain embodiments, L is of formula L134. In certain embodiments, L is of formula L135. In certain embodiments, L is of formula L136. In certain embodiments, L is of formula L137. In certain embodiments, L is of formula L138. In certain embodiments, L is of formula L139. In certain embodiments, L is of formula L140. In certain embodiments, L is of formula L141. In certain embodiments, L is of formula L142. In certain embodiments, L is of formula L143. In certain embodiments, L is of formula L144.
  • L is of formula L145. In certain embodiments, L is of formula L146. In certain embodiments, L is of formula L147. In certain embodiments, L is of formula L148. In certain embodiments, L is of formula L149. In certain embodiments, L is of formula L150. In certain embodiments, L is of formula L151. In certain embodiments, L is of formula L152. In certain embodiments, L is of formula L153. In certain embodiments, L is of formula L154. In certain embodiments, L is of formula L155. In certain embodiments, L is of formula L156. In certain embodiments, L is of formula L157. In certain embodiments, L is of formula L158. In certain embodiments, L is of formula L159. In certain embodiments, L is of formula L160.
  • L is of formula L161. In certain embodiments, L is of formula L162. In certain embodiments, L is of formula L163. In certain embodiments, L is of formula L164. In certain embodiments, L is of formula L165. In certain embodiments, L is of formula L166. In certain embodiments, L is of formula L167. In certain embodiments, L is of formula L168. In certain embodiments, L is of formula L169. In certain embodiments, L is of formula L170. In certain embodiments, L is of formula L171. In certain embodiments, L is of formula L172. In certain embodiments, L is of formula L173. In certain embodiments, L is of formula L174. In certain embodiments, L is of formula L175.
  • L is of formula L176. In certain embodiments, L is of formula L177. In certain embodiments, L is of formula L178. In certain embodiments, L is of formula L179. In certain embodiments, L is of formula L180. In certain embodiments, L is of formula 181. In certain embodiments, L is of formula L182. In certain embodiments, L is of formula L183. In certain embodiments, L is of formula L184. In certain embodiments, L is of formula L185. In certain embodiments, L is of formula L186. In certain embodiments, L is of formula L187. In certain embodiments, L is of formula L188. In certain embodiments, L is of formula L189. In certain embodiments, L is of formula L190. In certain embodiments, L is of formula L191.
  • L is of formula L192. In certain embodiments, L is of formula L193. In certain embodiments, L is of formula L194. In certain embodiments, L is of formula L195. In certain embodiments, L is of formula L196. In certain embodiments, L is of formula L197. In certain embodiments, L is of formula L198. In certain embodiments, L is of formula L199. In certain embodiments, L is of formula L200. In certain embodiments, L is of formula L201. In certain embodiments, L is of formula L202. In certain embodiments, L is of formula L203. In certain embodiments, L is of formula L204. In certain embodiments, L is of formula L205. In certain embodiments, L is of formula L206. In certain embodiments, L is of formula L207.
  • L is of formula L208. In certain embodiments, L is of formula L209. In certain embodiments, L is of formula L210. In certain embodiments, L is of formula L211. In certain embodiments, L is of formula L212. In certain embodiments, L is of formula L213. In certain embodiments, L is of formula L214. In certain embodiments, L is of formula L215. In certain embodiments, L is of formula L216. In certain embodiments, L is of formula L217. In certain embodiments, L is of formula L218. In certain embodiments, L is of formula L219. In certain embodiments, L is of formula L220. In certain embodiments, L is of formula L221. In certain embodiments, L is of formula L222.
  • L is of formula L223. In certain embodiments, L is of formula L224. In certain embodiments, L is of formula L225. In certain embodiments, L is of formula L226. In certain embodiments, L is of formula L227. In certain embodiments, L is of formula L228. In certain embodiments, L is of formula L229. In certain embodiments, L is of formula L230. In certain embodiments, L is of formula L231. In certain embodiments, L is of formula L232.
  • the compound of Formula (I) is a compound of Formula (I- b): (I-b), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 1): (I-b-1), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, R 3 , and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-1), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 2): (I-b-2), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R 6 are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-2), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 3): (I-b-3), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-3), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 4): (I-b-4), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, B, and R C as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-4), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b-5): (I-b-5), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-5), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b-5a): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-5a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 6): (I-b-6), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-6), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 6a): (I-b-6a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-6a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 7): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-7), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 7a): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-7a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 7b): (I-b-7b), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b- 7b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 8): (I-b-8), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-8), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 9): (I-b-9), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-9), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 9a): (I-b-9a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-9a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 10): (I-b-10), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-10), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 10a): (I-b-10a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and B are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b- 10a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 11): (I-b-11), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-11), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 12): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-12), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 13): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-13), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 14): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-14), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 15): (I-b-15), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-15), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 16): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-16), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 1 or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-17), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 18): (I-b-18), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-18), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 19): (I-b-19), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-19), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 20): (I-b-20), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-20), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I- b-21): (I-b-21), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-21), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 22): (I-b-22), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-22), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 23): (I-b-23), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-23), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 24): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-24), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 25): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-25), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 26): (I-b-26), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-26), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 27): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-27), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 28): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-28), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 29): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (I) is a compound of Formula (I-b-29), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 30): (I-b-30), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-30), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (I) is a compound of Formula (I-b- 31): (I-b-31), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, B, and R C are as defined herein.
  • the compound of Formula (I) is a compound of Formula (I-b-31), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof. [00424] In certain embodiments, the compound of Formula (I) is of formula:
  • the compound of Formula (I) is of formula:
  • the compound of Formula (II) is a compound of Formula (II- a): (II-a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, R 3 , R 4 , R 5 , and R 6 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-1): (II-a-1), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, R 6 , and R 3 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-1), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-2): (II-a-2), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, and R 6 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-2), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-3): (II-a-3), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, R B , and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-3), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-4): (II-a-4), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-4), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-5): (II-a-5), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-5), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-5a): (II-a-5a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a- 5a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-6): (II-a-6), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-6), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-6a): (II-a-6a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a- 6a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-7): (II-a-7), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-7), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-7a): (II-a-7a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-7a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-7b): (II-a-7b), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a- 7b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-8): (II-a-8), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (II) is a compound of Formula (II-a-8), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II-a- 9): (II-a-9), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-9), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II-a- 9a): (II-a-9a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-9a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-10): (II-a-10), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-10), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-10a): (II-a-10a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a- 10a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-11): (II-a-11), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or un
  • the compound of Formula (II) is a compound of Formula (II-a-11), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-12): (II-a-12), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-12), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-13): (II-a-13), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-13), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-14): (II-a-14), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubsti
  • the compound of Formula (II) is a compound of Formula (II-a-14), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-15): (II-a-15), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-15), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-16): (II-a-16), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-16), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-17): (II-a-17), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (II) is a compound of Formula (II-a-17), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-18): (II-a-18), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-18), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-19), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (II) is a compound of Formula (II-a-20), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II-a-21): (II-a-21), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-21), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-22): (II-a-22), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-22), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- (II-a-23), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted
  • the compound of Formula (II) is a compound of Formula (II-a-23), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-24): (II-a-24), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-24), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-25): (II-a-25), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-25), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-26): (II-a-26), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or un
  • the compound of Formula (II) is a compound of Formula (II-a-26), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-27): (II-a-27), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-27), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-28), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-29): (II-a-29), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (II) is a compound of Formula (II-a-29), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-30): (II-a-30), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-30), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- a-31): (II-a-31), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-a-31), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, R 3 , R 4 , R 5 , and R 6 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-1): (II-b-1), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, R 6 , and R 3 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-1), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-2): (II-b-2), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, and R 6 are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-2), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-3): (II-b-3), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, R B , and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-3), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-4): (II-b-4), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein A, L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-4), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-5): (II-b-5), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-5), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-5a): (II-b-5a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b- 5a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-6): (II-b-6), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-6), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-6a): (II-b-6a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b- 6a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-7): or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-7), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-7a): (II-b-7a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b- 7a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-7b): (II-b-7b), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b- 7b), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-8): (II-b-8), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein;
  • R x is hydrogen, halogen, substituted or unsubstituted C 1-4 alkyl, substituted or unsubstituted C 2-4 alkenyl, substituted or unsubstituted C 2-4 alkynyl, -N(R A ) 2 , -OR A , or -SR A ; and each occurrence of R A is, independently, hydrogen, substituted or unsubstituted acyl, or substituted or unsubstituted C 1-4 alkyl.
  • the compound of Formula (II) is a compound of Formula (II-b-8), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II-b- 9): (II-b-9), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-9), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-9a): (II-b-9a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b- 9a), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-10): (II-b-10), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L, T, and R C are as defined herein.
  • the compound of Formula (II) is a compound of Formula (II-b-10), wherein L is any one of L1-L232, or a pharmaceutically acceptable salt thereof.
  • the compound of Formula (II) is a compound of Formula (II- b-10a): (II-b-10a), or a pharmaceutically acceptable salt, co-crystal, tautomer, stereoisomer, solvate, hydrate, polymorph, isotopically enriched derivative, or prodrug thereof, wherein L and T are as defined herein.

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Abstract

La présente invention concerne des composés bifonctionnels qui se lient à la protéine kinase activée par 5'-AMP (AMPK) et/ou favorisent la phosphorylation ciblée d'un substrat. La phosphorylation induite du substrat cible peut modifier la structure et la fonction du substrat, fournissant ainsi des composés qui permettent la phosphorylation de substrats cibles, notamment ceux qui peuvent ne pas être autrement des substrats pour l'AMPK, et fournissant de nouveaux modes destinés à induire une phosphorylation stratégique. La présente invention concerne également des compositions pharmaceutiques comprenant les composés bifonctionnels et des procédés de promotion de la phosphorylation de substrats cibles dans un échantillon biologique par administration d'un composé ou d'une composition décrits dans la présente invention.
PCT/US2024/038400 2023-07-17 2024-07-17 Composés bifonctionnels de liaison à la kinase et leurs utilisations Pending WO2025019599A2 (fr)

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