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
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)
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).
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) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE69329149T2 (de) * | 1992-05-20 | 2001-03-29 | Merck & Co Inc | 4-azasteroide als 5-alpha-reduktase |
TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
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 |
EP1622567B1 (en) * | 2003-05-07 | 2013-07-24 | Merck Sharp & Dohme Corp. | Androgen receptor modulators and methods of use thereof |
US7482357B2 (en) * | 2003-06-30 | 2009-01-27 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
JP2007521293A (ja) * | 2003-06-30 | 2007-08-02 | 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としての17−アセトアミド−4−アザステロイド誘導体 |
CN100528168C (zh) * | 2003-06-30 | 2009-08-19 | 麦克公司 | 作为雄激素受体调节剂的17-乙酰氨基-4-氮杂甾类衍生物 |
EP1707187B1 (en) * | 2005-04-02 | 2007-08-01 | Wella Aktiengesellschaft | Reductive colorant for keratin fibres |
DE602005001848T2 (de) * | 2005-04-02 | 2008-04-17 | Wella Ag | System zum reduktiven Färben von Keratinfasern |
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 |
EP2393827B1 (en) | 2009-02-05 | 2015-10-07 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
GB201102913D0 (en) | 2011-02-18 | 2011-04-06 | Univ Birmingham | Novel therapeutic |
US9884067B2 (en) | 2013-03-14 | 2018-02-06 | University Of Maryland, Baltimore | Androgen receptor down-regulating agents and uses thereof |
US9808472B2 (en) | 2013-08-12 | 2017-11-07 | 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 |
Family Cites Families (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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. |
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 |
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 |
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 |
WO1989011282A1 (en) * | 1988-05-25 | 1989-11-30 | Smithkline Beckman Corporation | AROMATIC STEROID 5-alpha-REDUCTASE INHIBITORS |
US4937237A (en) * | 1988-12-23 | 1990-06-26 | Smithkline Beckman Corporation | Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase |
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 |
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 |
WO1993023038A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS |
WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
DE69329149T2 (de) * | 1992-05-20 | 2001-03-29 | Merck & Co Inc | 4-azasteroide als 5-alpha-reduktase |
KR950701527A (ko) * | 1992-05-21 | 1995-04-28 | 라브리 페르낭 | 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY) |
-
1993
- 1993-05-17 DE DE69329149T patent/DE69329149T2/de not_active Expired - Fee Related
- 1993-05-17 ES ES93911333T patent/ES2149208T3/es not_active Expired - Lifetime
- 1993-05-17 EP EP93911333A patent/EP0641208B1/en not_active Expired - Lifetime
- 1993-05-17 AT AT93911333T patent/ATE195129T1/de not_active IP Right Cessation
- 1993-05-17 WO PCT/US1993/004634 patent/WO1993023048A1/en active IP Right Grant
- 1993-05-17 JP JP6503781A patent/JPH07508035A/ja active Pending
- 1993-05-17 CA CA002135055A patent/CA2135055A1/en not_active Abandoned
- 1993-05-17 US US08/338,574 patent/US5620986A/en not_active Expired - Fee Related
- 1993-05-17 AU AU42507/93A patent/AU672978B2/en not_active Ceased
Also Published As
Publication number | Publication date |
---|---|
ATE195129T1 (de) | 2000-08-15 |
EP0641208B1 (en) | 2000-08-02 |
US5620986A (en) | 1997-04-15 |
EP0641208A1 (en) | 1995-03-08 |
AU672978B2 (en) | 1996-10-24 |
DE69329149T2 (de) | 2001-03-29 |
EP0641208A4 (en) | 1995-08-30 |
AU4250793A (en) | 1993-12-13 |
WO1993023048A1 (en) | 1993-11-25 |
CA2135055A1 (en) | 1993-11-25 |
DE69329149D1 (de) | 2000-09-07 |
JPH07508035A (ja) | 1995-09-07 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG2A | Definitive protection |
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