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WO2024138128A3 - Cereblon degrader conjugates, and uses thereof - Google Patents

Cereblon degrader conjugates, and uses thereof Download PDF

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Publication number
WO2024138128A3
WO2024138128A3 PCT/US2023/085698 US2023085698W WO2024138128A3 WO 2024138128 A3 WO2024138128 A3 WO 2024138128A3 US 2023085698 W US2023085698 W US 2023085698W WO 2024138128 A3 WO2024138128 A3 WO 2024138128A3
Authority
WO
WIPO (PCT)
Prior art keywords
cereblon
degrader
conjugates
antibody
cdacs
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2023/085698
Other languages
French (fr)
Other versions
WO2024138128A2 (en
Inventor
Thomas Harden Pillow
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Original Assignee
Genentech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Genentech Inc filed Critical Genentech Inc
Priority to EP23848435.6A priority Critical patent/EP4637833A2/en
Priority to CN202380088484.7A priority patent/CN120417934A/en
Publication of WO2024138128A2 publication Critical patent/WO2024138128A2/en
Publication of WO2024138128A3 publication Critical patent/WO2024138128A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Provided here are cereblon degrader antibody conjugates (cDACs) comprising a cereblon degrader moiety covalently attached to an antibody. The cDAC targets proteins for intracellular degradation and may be useful to treat diseases and disorders.
PCT/US2023/085698 2022-12-23 2023-12-22 Cereblon degrader conjugates, and uses thereof Ceased WO2024138128A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP23848435.6A EP4637833A2 (en) 2022-12-23 2023-12-22 Cereblon degrader conjugates, and uses thereof
CN202380088484.7A CN120417934A (en) 2022-12-23 2023-12-22 CEREBLON degrader conjugates and uses thereof

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202263435142P 2022-12-23 2022-12-23
US63/435,142 2022-12-23
US202363525282P 2023-07-06 2023-07-06
US63/525,282 2023-07-06

Publications (2)

Publication Number Publication Date
WO2024138128A2 WO2024138128A2 (en) 2024-06-27
WO2024138128A3 true WO2024138128A3 (en) 2024-07-25

Family

ID=89843299

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2023/085698 Ceased WO2024138128A2 (en) 2022-12-23 2023-12-22 Cereblon degrader conjugates, and uses thereof

Country Status (4)

Country Link
EP (1) EP4637833A2 (en)
CN (1) CN120417934A (en)
TW (1) TW202432187A (en)
WO (1) WO2024138128A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202500195A (en) * 2023-05-18 2025-01-01 美商飛爾富來生物公司 Isoindolinone-glutarimide antibody conjugates, and uses thereof
WO2025054181A1 (en) * 2023-09-05 2025-03-13 Seagen Inc. Targeted degrader molecules and ligand drug conjugates thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017201449A1 (en) * 2016-05-20 2017-11-23 Genentech, Inc. Protac antibody conjugates and methods of use
WO2018227018A1 (en) * 2017-06-07 2018-12-13 Silverback Therapeutics, Inc. Antibody conjugates of immune-modulatory compounds and uses thereof
EP3865152A1 (en) * 2018-10-09 2021-08-18 Eubulus Biotherapeutics Inc. Targeted protease degradation platform

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