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

Small-molecule inhibitors of the androgen receptor Download PDF

Info

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
Other languages
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
Original Assignee
University of California Berkeley
University of California, San Diego
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 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

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • 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
    • C07D401/06—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 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 (enExample)
EP (1) EP2276345A4 (enExample)
JP (1) JP5599385B2 (enExample)
KR (1) KR101640512B1 (enExample)
AU (1) AU2009240417B2 (enExample)
CA (1) CA2722340A1 (enExample)
NZ (1) NZ589299A (enExample)
WO (1) WO2009132307A1 (enExample)

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
EP2959013A2 (en) * 2013-02-25 2015-12-30 Novartis AG Novel androgen receptor mutation
GB2513615A (en) 2013-05-01 2014-11-05 Cancer Rec Tech Ltd Medical use
EP3350167A4 (en) 2015-09-04 2019-04-03 City of Hope Androgen receptor Antagonist
WO2019126739A1 (en) 2017-12-21 2019-06-27 Shepherd Therapeutics, Inc. Pyrvinium pamoate anti-cancer therapies
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
AU7558900A (en) * 1999-10-14 2001-04-23 Kaken Pharmaceutical Co., Ltd. Tetrahydroquinoline derivatives
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
CA2576988A1 (en) * 2004-08-25 2006-03-09 Merck & Co., Inc. Androgen receptor modulators
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
JP5599385B2 (ja) 2014-10-01
KR20110002872A (ko) 2011-01-10
WO2009132307A1 (en) 2009-10-29
KR101640512B1 (ko) 2016-07-18
EP2276345A1 (en) 2011-01-26
JP2011518843A (ja) 2011-06-30
US20130096095A1 (en) 2013-04-18
CA2722340A1 (en) 2009-10-29
NZ589299A (en) 2013-01-25
US20110224253A1 (en) 2011-09-15
US8580773B2 (en) 2013-11-12
AU2009240417A1 (en) 2009-10-29
EP2276345A4 (en) 2012-06-06
US8354538B2 (en) 2013-01-15

Similar Documents

Publication Publication Date Title
US7696227B2 (en) Small-molecule inhibitors of the androgen receptor
US8580773B2 (en) Small-molecule inhibitors of the androgen receptor
DK2656842T3 (en) Androgen receptor MODULATOR FOR THE TREATMENT OF PROSTATE CANCER AND androgen receptor-ASSOCIATED DISEASES
JP2017031224A (ja) ジアリールチオヒダントイン化合物
CA3138197A1 (en) Anti-cancer nuclear hormone receptor-targeting compounds
WO2016109470A1 (en) Small molecule stimulators of steroid receptor coactivator proteins and their use in the treatment of cancer
US9745261B2 (en) Inhibitors of the MITF molecular pathway
EP3844166B1 (en) Substituted macrocycles useful as kinase inhibitors
JP2022031509A (ja) アンドロゲン依存性又は非依存性前立腺癌細胞の抑制用の組成物及びそれを含有する前立腺癌の医薬製剤
JP2022519080A (ja) 過剰増殖性疾患を治療するための１，２，４－トリアジン－３（２ｈ）－オン化合物
CA2983249C (en) Oxadiazole propanamide compounds for treating rac-gtpase mediated disorder
Lou et al. Enzalutamide (Xtandi): An Androgen Receptor Antagonist for Late‐Stage Prostate Cancer
JP2025539347A (ja) Ｋｒａｓ阻害剤とｓｈｐ２阻害剤とを含む併用療法
WO2019236966A2 (en) Methods of treatment of cancer with substituted pyrrole and pyrazole compounds and diagnosis of cancers susceptible to treatment with substituted pyrrole and pyrazole compounds
HK1231375B (en) Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases
HK1163495B (en) Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired