ES2149208T3 - Inhibidores 4-azaesteroides de 5-alfa-reductasa. - Google Patents

Inhibidores 4-azaesteroides de 5-alfa-reductasa.

Info

Publication number
ES2149208T3
ES2149208T3 ES93911333T ES93911333T ES2149208T3 ES 2149208 T3 ES2149208 T3 ES 2149208T3 ES 93911333 T ES93911333 T ES 93911333T ES 93911333 T ES93911333 T ES 93911333T ES 2149208 T3 ES2149208 T3 ES 2149208T3
Authority
ES
Spain
Prior art keywords
pct
alpha
image
reductase inhibitors
sec
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.)
Expired - Lifetime
Application number
ES93911333T
Other languages
English (en)
Inventor
Bruce E Witzel
Richard L Tolman
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.)
Merck and Co Inc
Original Assignee
Merck and 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 and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of ES2149208T3 publication Critical patent/ES2149208T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Cosmetics (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

NUEVOS INHIBIDORES DE 4-AZAESTEROIDES 5-ALFA-REDUCTASA SUSTITUIDOS DE FORMULA (I) EN LA QUE A ES (A), (B) O (C) SON SOLICITADOS, ASI COMO SALES FARMACEUTICAMENTE ACEPTABLES Y FORMULACIONES DE ESTOS. ESTOS COMPUESTOS SON INHIBIDORES EFECTIVOS DE TESTOSTERONA 5ALFAREDUCTASA(S), SON ASI UTILES EN EL TRATAMIENTO DE UN NUMERO DE CONDICIONES HIPERANDROGENICAS QUE COMPRENDEN HIPERTROFIA PROSTATICA BENIGNA, ACNE, SEBORREA, HIRSUTISMO FEMENINO, Y CALVICIE MASCULINA Y FEMENINA (ALOPECIA).
ES93911333T 1992-05-20 1993-05-17 Inhibidores 4-azaesteroides de 5-alfa-reductasa. Expired - Lifetime ES2149208T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88664592A 1992-05-20 1992-05-20

Publications (1)

Publication Number Publication Date
ES2149208T3 true ES2149208T3 (es) 2000-11-01

Family

ID=25389449

Family Applications (1)

Application Number Title Priority Date Filing Date
ES93911333T Expired - Lifetime ES2149208T3 (es) 1992-05-20 1993-05-17 Inhibidores 4-azaesteroides de 5-alfa-reductasa.

Country Status (9)

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

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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
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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
CA2530047A1 (en) * 2003-06-30 2005-02-03 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530182A1 (en) * 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US7696217B2 (en) * 2003-06-30 2010-04-13 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP1707188B1 (en) * 2005-04-02 2007-08-01 Wella Aktiengesellschaft Reductive colouring system for keratin fibres
EP1707187B1 (en) * 2005-04-02 2007-08-01 Wella Aktiengesellschaft Reductive colorant for keratin fibres
US20100048913A1 (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
CN102686600A (zh) 2009-02-05 2012-09-19 托凯药业股份有限公司 甾体cyp17抑制剂/抗雄激素物质的新型药物前体
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
RU2015137617A (ru) 2013-03-14 2017-04-18 Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер Агенты, подавляющие андрогенные рецепторы, и их применение
CN105636594A (zh) 2013-08-12 2016-06-01 托凯药业股份有限公司 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物
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
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
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
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
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.
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
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
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
US5110939A (en) * 1987-01-28 1992-05-05 Smithkline Beecham Corporation Intermediates in the preparation of steriod 5-alpha-reductase inhibitors
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 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
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
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4970205A (en) * 1988-12-23 1990-11-13 Smithkline Beecham Corporation Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-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
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
UA35589C2 (uk) * 1992-05-21 2001-04-16 Андорешерш Інк. ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ

Also Published As

Publication number Publication date
AU4250793A (en) 1993-12-13
ATE195129T1 (de) 2000-08-15
EP0641208A1 (en) 1995-03-08
AU672978B2 (en) 1996-10-24
JPH07508035A (ja) 1995-09-07
DE69329149T2 (de) 2001-03-29
US5620986A (en) 1997-04-15
EP0641208A4 (en) 1995-08-30
DE69329149D1 (de) 2000-09-07
WO1993023048A1 (en) 1993-11-25
EP0641208B1 (en) 2000-08-02
CA2135055A1 (en) 1993-11-25

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