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WO2011031745A1 - Analogues de fluoroquinolone antibactériens - Google Patents

Analogues de fluoroquinolone antibactériens Download PDF

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Publication number
WO2011031745A1
WO2011031745A1 PCT/US2010/048110 US2010048110W WO2011031745A1 WO 2011031745 A1 WO2011031745 A1 WO 2011031745A1 US 2010048110 W US2010048110 W US 2010048110W WO 2011031745 A1 WO2011031745 A1 WO 2011031745A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
optionally substituted
hydrogen
alkyl
cycloalkyl
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/US2010/048110
Other languages
English (en)
Inventor
Allan Scott Wagman
Heinz Ernst Moser
Glenn A. Mcenroe
James Bradley Aggen
Martin Sheringham Linsell
Adam Aaron Goldblum
John H. Griffin
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.)
Achaogen Inc
Original Assignee
Achaogen 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 Achaogen Inc filed Critical Achaogen Inc
Publication of WO2011031745A1 publication Critical patent/WO2011031745A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Definitions

  • each R 8b is, independently, hydrogen, halogen, C C 6 alkyl, C 3 -C 6 cycloalkyl, Q-Q haloalkyl or C -Ce cycloalkylalkyl; each Rg c is, independently, hydrogen or Ci-C 6 alkyl;
  • Niro refers to the -N0 2 radical.
  • Aralkyl refers to a radical of the formula -Rb-Rc where R b is an alkylene chain as defined above and R c is one or more aryl radicals as defined above, for example, benzyl, diphenylmethyl and the like. Unless stated otherwise specifically in the specification, an aralkyl group may be optionally substituted.
  • Heterocyclyl or “heterocyclic ring” refers to a stable 3- to 18-membered non-aromatic ring radical which consists of two to twelve carbon atoms and from one to six heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur.
  • the heterocyclyl radical may be a monocyclic, bicyclic, tricyclic or tetracyclic ring system, which may include fused or bridged ring systems; and the nitrogen, carbon or sulfur atoms in the heterocyclyl radical may be optionally oxidized; the nitrogen atom may be optionally quaternized; and the heterocyclyl radical may be partially or fully saturated.
  • R g and R h are the same or different and independently hydrogen, alkyl, alkoxy, alkylamino, thioalkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, heterocyclyl, N-heterocyclyl, heterocyclylalkyl, heteroaryl, N-heteroaryl and/or heteroarylalkyl.
  • substitution with heavier isotopes such as deuterium, i.e. H may afford certain therapeutic advantages resulting from greater metabolic stability, for example, increased in vivo half-life or reduced dosage requirements, and hence may be preferred in some circumstances.
  • the invention disclosed herein is also meant to encompass the in vivo metabolic products of the disclosed compounds. Such products may result from, for example, the oxidation, reduction, hydrolysis, amidation, esterification, and the like of the administered compound, primarily due to enzymatic processes. Accordingly, the invention includes compounds produced by a process comprising administering a compound of this invention to a mammal for a period of time sufficient to yield a metabolic product thereof. Such products are typically identified by administering a radiolabelled compound of the invention in a detectable dose to an animal, such as rat, mouse, guinea pig, monkey, or to human, allowing sufficient time for metabolism to occur, and isolating its conversion products from the urine, blood or other biological samples. "Stable compound” and “stable structure” are meant to indicate a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.
  • Optional or “optionally” means that the subsequently described event of circumstances may or may not occur, and that the description includes instances where said event or circumstance occurs and instances in which it does not.
  • optionally substituted aryl means that the aryl radical may or may not be substituted and that the description includes both substituted aryl radicals and aryl radicals having no substitution.
  • solvate refers to an aggregate that comprises one or more molecules of a compound of the invention with one or more molecules of solvent.
  • the solvent may be water, in which case the solvate may be a hydrate.
  • the solvent may be an organic solvent.
  • the compounds of the present invention may exist as a hydrate, including a monohydrate, dihydrate, hemihydrate, sesquihydrate, trihydrate, tetrahydrate and the like, as well as the corresponding solvated forms.
  • the compound of the invention may be true solvates, while in other cases, the compound of the invention may merely retain adventitious water or be a mixture of water plus some adventitious solvent.
  • each Rio is hydroxyl or amino
  • the pharmaceutical composition of the invention may be intended for rectal administration, in the form, for example, of a suppository, which will melt in the rectum and release the drug.
  • the composition for rectal administration may contain an oleaginous base as a suitable nonirritating excipient.
  • bases include, without limitation, lanolin, cocoa butter and polyethylene glycol.
  • Suitable protecting groups for hydroxy include, for example, trialkylsilyl or diarylalkylsilyl (for example, triethylsilyl (TES), triisopropylsilyl (TIPS), t-butyldimethylsilyl (TBS), t-butyldiphenylsilyl (TBDPS) or trimethylsilyl (TMS)), tert-butoxycarbonyl (Boc), allyloxycarbonyl (Alloc), carboxybenzyl (Cbz), fluorenylmethoxycarbonyl (Fmoc), trichloroethoxycarbonyl (Troc), trityl (Trt), benzyl, methoxybenzyl, dimethoxybenzyl, chlorobenz
  • reaction mixture was cooled, diluted with 50 mL ethyl acetate and washed with two 50 mL portions of H 2 0 and 50 mL brine.
  • the organic phase was dried over Na 2 S0 4 , filtered and concentrated to a brown, sticky foam.
  • the material was purified by flash chromatography (40 g flash silica gel; 2-6% MeOH/CH 2 Cl 2 ) to yield compound (3).
  • Bacteria are suspended in sterile saline and added to each assay plate to obtain a final concentration of 5xl0 5 CFU/mL. The plates are incubated at 35 °C for 20 hours in ambient air. The MIC is determined to be the lowest concentration of the test compound that results in no visible bacterial growth as compared to untreated control.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des composés présentant une activité antibactérienne, représentés par les structures (I) à (X) suivantes, ainsi que certains de leurs stéréoisomères, de leurs sels pharmaceutiquement admis, et de leurs promédicaments. Dans ces structures, les A, B, D, E, G, R1, R2, R3, R4, R5, R6, R7, R9 et R10 sont tels que définis dans la description. L'invention concerne également, d'une part des procédés associés à l'élaboration et à l'utilisation de tels composés, et d'autre part des compositions pharmaceutiques comprenant de tels composés.
PCT/US2010/048110 2009-09-09 2010-09-08 Analogues de fluoroquinolone antibactériens Ceased WO2011031745A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24092809P 2009-09-09 2009-09-09
US61/240,928 2009-09-09

Publications (1)

Publication Number Publication Date
WO2011031745A1 true WO2011031745A1 (fr) 2011-03-17

Family

ID=43063430

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/048110 Ceased WO2011031745A1 (fr) 2009-09-09 2010-09-08 Analogues de fluoroquinolone antibactériens

Country Status (1)

Country Link
WO (1) WO2011031745A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019186387A3 (fr) * 2018-03-26 2020-04-09 University Of Sharjah Nouveaux systèmes hétérocycliques et leurs applications pharmaceutiques

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* Cited by examiner, † Cited by third party
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