AU2009240417B2 - Small-molecule inhibitors of the androgen receptor - Google Patents

Small-molecule inhibitors of the androgen receptor Download PDF

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Publication number
AU2009240417B2
AU2009240417B2 AU2009240417A AU2009240417A AU2009240417B2 AU 2009240417 B2 AU2009240417 B2 AU 2009240417B2 AU 2009240417 A AU2009240417 A AU 2009240417A AU 2009240417 A AU2009240417 A AU 2009240417A AU 2009240417 B2 AU2009240417 B2 AU 2009240417B2
Authority
AU
Australia
Prior art keywords
compound
compounds
group
alkyl
androgen
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
AU2009240417A
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English (en)
Other versions
AU2009240417A1 (en
Inventor
Marc Diamond
Jeremy Jones
Adam Renslo
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.)
University of California San Diego UCSD
Original Assignee
University of California Berkeley
University of California San Diego UCSD
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 University of California Berkeley, University of California San Diego UCSD filed Critical University of California Berkeley
Publication of AU2009240417A1 publication Critical patent/AU2009240417A1/en
Application granted granted Critical
Publication of AU2009240417B2 publication Critical patent/AU2009240417B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2009240417A 2008-04-24 2009-04-24 Small-molecule inhibitors of the androgen receptor Ceased AU2009240417B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4755908P 2008-04-24 2008-04-24
US61/047,559 2008-04-24
PCT/US2009/041715 WO2009132307A1 (en) 2008-04-24 2009-04-24 Small-molecule inhibitors of the androgen receptor

Publications (2)

Publication Number Publication Date
AU2009240417A1 AU2009240417A1 (en) 2009-10-29
AU2009240417B2 true AU2009240417B2 (en) 2014-06-26

Family

ID=41217163

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009240417A Ceased AU2009240417B2 (en) 2008-04-24 2009-04-24 Small-molecule inhibitors of the androgen receptor

Country Status (8)

Country Link
US (2) US8354538B2 (https=)
EP (1) EP2276345A4 (https=)
JP (1) JP5599385B2 (https=)
KR (1) KR101640512B1 (https=)
AU (1) AU2009240417B2 (https=)
CA (1) CA2722340A1 (https=)
NZ (1) NZ589299A (https=)
WO (1) WO2009132307A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2496135B (en) * 2011-11-01 2015-03-18 Valirx Plc Inhibitors of the interaction between a Src family kinase and an androgen receptor or estradiol receptor for treatment of endometriosis
CN105143463A (zh) * 2013-02-25 2015-12-09 诺华股份有限公司 新的雄激素受体突变
GB2513615A (en) 2013-05-01 2014-11-05 Cancer Rec Tech Ltd Medical use
CN108349900A (zh) 2015-09-04 2018-07-31 希望之城 雄激素受体拮抗剂
US10933061B2 (en) 2017-12-21 2021-03-02 Shepherd Therapeutics, Inc. Pyrvinium pamoate therapies and methods of use
WO2019152731A1 (en) * 2018-01-31 2019-08-08 Alpine Androsciences, Inc. Androgen receptor antagonists

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3821228A (en) * 1967-06-10 1974-06-28 Pfizer Ltd 2-aminoalkyl tetrahydroquinolines
DE2421382A1 (de) * 1974-05-03 1975-11-20 Council Scient Ind Res 1-substituierte 4-(beta-2-chinolylaethyl)- piperazine und deren 1,2,3,4-tetrahydrochinolinanaloge
WO2003031436A1 (en) * 2001-10-05 2003-04-17 Recordati S.A. Heterocyclic compounds for use in the treatment of disorders of the urinary tract
EP1325914A1 (en) * 2000-09-14 2003-07-09 Kaken Pharmaceutical Co., Ltd. Tetrahydroquinoline compounds
WO2006078754A1 (en) * 2005-01-18 2006-07-27 Immusol Incorporated Novel quinolinium salts and derivatives

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3983121A (en) * 1974-07-01 1976-09-28 Council Of Scientific And Industrial Research 1-Substituted 4-(β-2-quinolylethyl)piperazines and 1,2,3,4-tetrahydroquinolyl-ethyl analogues thereof
US5840500A (en) * 1996-07-11 1998-11-24 Trega Biosciences, Inc. Quinoline derivatives and quinoline combinatorial libraries
KR100826485B1 (ko) * 1999-10-14 2008-05-02 가켄 세야쿠 가부시키가이샤 테트라히드로퀴놀린 유도체
CN1506359A (zh) 2002-12-05 2004-06-23 �й�ҽѧ��ѧԺҩ���о��� 新的香豆素酰胺衍生物及其制法和其药物组合物与用途
US8519158B2 (en) * 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
JP2008510811A (ja) * 2004-08-25 2008-04-10 メルク エンド カムパニー インコーポレーテッド アンドロゲン受容体モジュレーター
WO2007117466A2 (en) 2006-03-31 2007-10-18 Massachusetts Institute Of Technology Celastrol, gedunin, and derivatives thereof as hsp90 inhibitors
WO2008128100A1 (en) 2007-04-13 2008-10-23 The Regents Of The University Of California Small-molecule inhibitors of the androgen receptor

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3821228A (en) * 1967-06-10 1974-06-28 Pfizer Ltd 2-aminoalkyl tetrahydroquinolines
DE2421382A1 (de) * 1974-05-03 1975-11-20 Council Scient Ind Res 1-substituierte 4-(beta-2-chinolylaethyl)- piperazine und deren 1,2,3,4-tetrahydrochinolinanaloge
EP1325914A1 (en) * 2000-09-14 2003-07-09 Kaken Pharmaceutical Co., Ltd. Tetrahydroquinoline compounds
WO2003031436A1 (en) * 2001-10-05 2003-04-17 Recordati S.A. Heterocyclic compounds for use in the treatment of disorders of the urinary tract
US20030162777A1 (en) * 2001-10-05 2003-08-28 Recordati S.A. Novel N-acylated heterocycles
WO2006078754A1 (en) * 2005-01-18 2006-07-27 Immusol Incorporated Novel quinolinium salts and derivatives

Also Published As

Publication number Publication date
WO2009132307A1 (en) 2009-10-29
KR20110002872A (ko) 2011-01-10
US20130096095A1 (en) 2013-04-18
US8580773B2 (en) 2013-11-12
CA2722340A1 (en) 2009-10-29
JP2011518843A (ja) 2011-06-30
KR101640512B1 (ko) 2016-07-18
US8354538B2 (en) 2013-01-15
AU2009240417A1 (en) 2009-10-29
JP5599385B2 (ja) 2014-10-01
EP2276345A1 (en) 2011-01-26
NZ589299A (en) 2013-01-25
EP2276345A4 (en) 2012-06-06
US20110224253A1 (en) 2011-09-15

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