ATE195129T1 - 4-azasteroide als 5-alpha-reduktase - Google Patents

4-azasteroide als 5-alpha-reduktase

Info

Publication number
ATE195129T1
ATE195129T1 AT93911333T AT93911333T ATE195129T1 AT E195129 T1 ATE195129 T1 AT E195129T1 AT 93911333 T AT93911333 T AT 93911333T AT 93911333 T AT93911333 T AT 93911333T AT E195129 T1 ATE195129 T1 AT E195129T1
Authority
AT
Austria
Prior art keywords
pct
alpha
reductase
image
sec
Prior art date
Application number
AT93911333T
Other languages
English (en)
Inventor
Bruce E Witzel
Richard L Tolman
Original Assignee
Merck & Co 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 Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE195129T1 publication Critical patent/ATE195129T1/de

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AT93911333T 1992-05-20 1993-05-17 4-azasteroide als 5-alpha-reduktase ATE195129T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88664592A 1992-05-20 1992-05-20
PCT/US1993/004634 WO1993023048A1 (en) 1992-05-20 1993-05-17 4-azasteroid 5-alpha-reductase inhibitors

Publications (1)

Publication Number Publication Date
ATE195129T1 true ATE195129T1 (de) 2000-08-15

Family

ID=25389449

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93911333T ATE195129T1 (de) 1992-05-20 1993-05-17 4-azasteroide als 5-alpha-reduktase

Country Status (9)

Country Link
US (1) US5620986A (de)
EP (1) EP0641208B1 (de)
JP (1) JPH07508035A (de)
AT (1) ATE195129T1 (de)
AU (1) AU672978B2 (de)
CA (1) CA2135055A1 (de)
DE (1) DE69329149T2 (de)
ES (1) ES2149208T3 (de)
WO (1) WO1993023048A1 (de)

Families Citing this family (25)

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ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5994334A (en) * 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
US5994335A (en) 1997-10-17 1999-11-30 The University Of Maryland, Baltimore 17-azolyl steroids useful as androgen synthesis inhibitors
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
CA2524409C (en) * 2003-05-07 2011-12-20 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
AU2004255749B2 (en) * 2003-06-30 2008-12-18 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530025A1 (en) * 2003-06-30 2005-01-20 William P. Dankulich 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US7329750B2 (en) * 2003-06-30 2008-02-12 Merck & Co., Inc. 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators
ES2290806T3 (es) * 2005-04-02 2008-02-16 Wella Aktiengesellschaft Sistema colorante reductor para fibras de queratina.
DE602005001847T2 (de) * 2005-04-02 2008-04-17 Wella Ag System zum reduktiven Färben von Keratinfasern
US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
WO2010091306A1 (en) 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
KR20150127720A (ko) 2013-03-14 2015-11-17 유니버시티 오브 매릴랜드, 발티모어 안드로겐 수용체 하향 조절제 및 그의 용도
CA2920317A1 (en) 2013-08-12 2015-02-19 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
WO2023101256A1 (ko) * 2021-12-03 2023-06-08 주식회사 팜어스바이오사이언스 5-알파-환원효소 억제제, 그의 약학적으로 허용 가능한 염 및 그 용도
KR102829242B1 (ko) * 2021-12-03 2025-07-07 주식회사 팜어스바이오사이언스 5-알파-환원효소 억제제, 그의 약학적으로 허용 가능한 염 및 그 용도

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US2227876A (en) * 1937-10-16 1941-01-07 Firm Of N V Organon Steroid derivatives with nuclear substituted nitrogen
US3285918A (en) * 1962-04-18 1966-11-15 Norman J Doorenbos 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
US3239417A (en) * 1962-12-07 1966-03-08 Smith Kline French Lab Methods and compositions for inhibiting sterol biosynthesis
US3264301A (en) * 1963-08-22 1966-08-02 Norman J Doorenbos Substituted-4-azasteroids
FR1465544A (fr) * 1965-11-29 1967-01-13 Roussel Uclaf Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation
CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
US4596812A (en) * 1976-05-24 1986-06-24 The Upjohn Company Methods and solutions for treating male pattern alopecia
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
ATE67503T1 (de) * 1984-02-27 1991-10-15 Merck & Co Inc 17-beta-substituierte-4-aza-5-alpha-androstenon und ihre anwendung als 5-alpha-reduktaseinhibitoren.
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US5110939A (en) * 1987-01-28 1992-05-05 Smithkline Beecham Corporation Intermediates in the preparation of steriod 5-alpha-reductase inhibitors
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
AU627466B2 (en) * 1988-05-25 1992-08-27 Smithkline Beckman Corporation Aromatic steroid 5-alpha-reductase inhibitors
US4970205A (en) * 1988-12-23 1990-11-13 Smithkline Beecham Corporation Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
DE69326008T2 (de) * 1992-05-20 2000-03-02 Merck & Co., Inc. 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤

Also Published As

Publication number Publication date
ES2149208T3 (es) 2000-11-01
JPH07508035A (ja) 1995-09-07
AU4250793A (en) 1993-12-13
DE69329149D1 (de) 2000-09-07
AU672978B2 (en) 1996-10-24
US5620986A (en) 1997-04-15
EP0641208A4 (de) 1995-08-30
EP0641208B1 (de) 2000-08-02
CA2135055A1 (en) 1993-11-25
EP0641208A1 (de) 1995-03-08
DE69329149T2 (de) 2001-03-29
WO1993023048A1 (en) 1993-11-25

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Legal Events

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RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties