AU2004288196B2 - 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators - Google Patents

21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators Download PDF

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Publication number
AU2004288196B2
AU2004288196B2 AU2004288196A AU2004288196A AU2004288196B2 AU 2004288196 B2 AU2004288196 B2 AU 2004288196B2 AU 2004288196 A AU2004288196 A AU 2004288196A AU 2004288196 A AU2004288196 A AU 2004288196A AU 2004288196 B2 AU2004288196 B2 AU 2004288196B2
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Australia
Prior art keywords
alkyl
methyl
aza
androst
cycloalkyl
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Ceased
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AU2004288196A
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AU2004288196A1 (en
Inventor
William P. Dankulich
Helen J. Mitchell
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Alteration of Name(s) of Applicant(s) under S113 Assignors: MERCK & CO., INC.
Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
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    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Vascular Medicine (AREA)
  • Nutrition Science (AREA)
AU2004288196A 2003-10-31 2004-10-27 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators Ceased AU2004288196B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US51642503P 2003-10-31 2003-10-31
US60/516,425 2003-10-31
PCT/US2004/035838 WO2005044988A2 (en) 2003-10-31 2004-10-27 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators

Publications (2)

Publication Number Publication Date
AU2004288196A1 AU2004288196A1 (en) 2005-05-19
AU2004288196B2 true AU2004288196B2 (en) 2009-11-26

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AU2004288196A Ceased AU2004288196B2 (en) 2003-10-31 2004-10-27 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators

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Country Link
US (1) US7312229B2 (enExample)
EP (1) EP1696925A4 (enExample)
JP (1) JP2007509962A (enExample)
CN (1) CN1871005B (enExample)
AU (1) AU2004288196B2 (enExample)
CA (1) CA2543956A1 (enExample)
WO (1) WO2005044988A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006110683A1 (en) 2005-04-11 2006-10-19 Abbott Laboratories 2-substituted-1h-benzimidazole-4-carboxamides are parp inhibitors
RU2329035C1 (ru) * 2006-11-28 2008-07-20 ГУ Научно-исследовательский институт фармакологии Томского научного центра Сибирского отделения Российской академии медицинских наук Лекарственные средства для профилактики и лечения анемии при невротических воздействиях
US20160331729A9 (en) 2007-04-11 2016-11-17 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
US11241420B2 (en) 2007-04-11 2022-02-08 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
ES2830073T3 (es) * 2007-04-11 2021-06-02 Omeros Corp Composiciones y métodos para la profilaxis y el tratamiento de adicciones
MX2012014431A (es) 2010-06-10 2013-02-26 Aragon Pharmaceuticals Inc Modulares del receptor de estrogenos y usos de los mismos.
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
CN105820206B (zh) * 2016-04-18 2017-08-01 广西师范学院 22‑降‑豆甾苯并咪唑化合物及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
US5629318A (en) * 1992-12-18 1997-05-13 Merck & Co., Inc. Method of treatment of chronic prostatitis with 17β-N-monosubstituted-carbamoyl-4-aza-5α-androst-1-en-3-ones

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
CA2478186C (en) * 2002-03-13 2011-08-23 Merck & Co., Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
JP2007505118A (ja) 2003-09-10 2007-03-08 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調節剤としての１７−複素環−４−アザステロイド誘導体

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
US5629318A (en) * 1992-12-18 1997-05-13 Merck & Co., Inc. Method of treatment of chronic prostatitis with 17β-N-monosubstituted-carbamoyl-4-aza-5α-androst-1-en-3-ones

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Publication number Publication date
EP1696925A2 (en) 2006-09-06
JP2007509962A (ja) 2007-04-19
WO2005044988A2 (en) 2005-05-19
US20070088047A1 (en) 2007-04-19
CN1871005A (zh) 2006-11-29
CN1871005B (zh) 2010-10-27
CA2543956A1 (en) 2005-05-19
US7312229B2 (en) 2007-12-25
AU2004288196A1 (en) 2005-05-19
EP1696925A4 (en) 2009-11-18
WO2005044988A3 (en) 2005-10-27

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