ES2148229T3 - Eteres y tioeteres en la posicion 17 de 4-aza-esteroides. - Google Patents
Eteres y tioeteres en la posicion 17 de 4-aza-esteroides.Info
- Publication number
- ES2148229T3 ES2148229T3 ES93911358T ES93911358T ES2148229T3 ES 2148229 T3 ES2148229 T3 ES 2148229T3 ES 93911358 T ES93911358 T ES 93911358T ES 93911358 T ES93911358 T ES 93911358T ES 2148229 T3 ES2148229 T3 ES 2148229T3
- Authority
- ES
- Spain
- Prior art keywords
- thioeteres
- ateres
- aza
- steroids
- compounds
- 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)
- Cosmetics (AREA)
Abstract
LOS COMPUESTOS DE FORMULA (I), DONDE Z CONTIENE UNA UNIDAD DE ETER O TIOETER, SON INHIBIDORES DE LA ENZIMA 5ALFA REDUCTASA Y SUS ISOMEROS. LOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO DE CONDICIONES DE ENFERMEDAD HIPERANDROGENICA Y ENFERMEDADES DE LA PIEL Y EL CUERO CABELLUDO.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88603192A | 1992-05-20 | 1992-05-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2148229T3 true ES2148229T3 (es) | 2000-10-16 |
Family
ID=25388234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES93911358T Expired - Lifetime ES2148229T3 (es) | 1992-05-20 | 1993-05-19 | Eteres y tioeteres en la posicion 17 de 4-aza-esteroides. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US5536727A (es) |
| EP (1) | EP0641204B1 (es) |
| JP (1) | JPH07508038A (es) |
| AT (1) | ATE195530T1 (es) |
| AU (1) | AU668180B2 (es) |
| CA (1) | CA2135174A1 (es) |
| DE (1) | DE69329240D1 (es) |
| ES (1) | ES2148229T3 (es) |
| WO (1) | WO1993023040A1 (es) |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
| DE4311987A1 (de) * | 1993-04-07 | 1994-10-13 | Schering Ag | Neue Glucocorticoide |
| 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 |
| US5583239A (en) * | 1995-05-30 | 1996-12-10 | Lehigh University | Antimicrobial sterol conjugates |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| US6147106A (en) | 1997-08-20 | 2000-11-14 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| US6365597B1 (en) | 1996-02-14 | 2002-04-02 | Aventis Pharmaceuticals Inc. | 4-aza steroids |
| US5872126A (en) * | 1996-09-06 | 1999-02-16 | Merck & Co., Inc. | Methods and compositions for treating preterm labor |
| US6486185B1 (en) | 1997-05-07 | 2002-11-26 | Sugen, Inc. | 3-heteroarylidene-2-indolinone protein kinase inhibitors |
| US6316429B1 (en) | 1997-05-07 | 2001-11-13 | Sugen, Inc. | Bicyclic protein kinase inhibitors |
| US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
| CO5031249A1 (es) | 1998-05-29 | 2001-04-27 | Sugen Inc | Pirrol substituido-2-indolinonas inhibidoras de proteinci-nasas |
| US6689806B1 (en) | 1999-03-24 | 2004-02-10 | Sugen, Inc. | Indolinone compounds as kinase inhibitors |
| US6878733B1 (en) | 1999-11-24 | 2005-04-12 | Sugen, Inc. | Formulations for pharmaceutical agents ionizable as free acids or free bases |
| US6797820B2 (en) * | 1999-12-17 | 2004-09-28 | Vicuron Pharmaceuticals Inc. | Succinate compounds, compositions and methods of use and preparation |
| ATE369359T1 (de) | 2000-02-15 | 2007-08-15 | Sugen Inc | Pyrrol substituierte indolin-2-on protein kinase inhibitoren |
| CA2377629A1 (en) * | 2000-04-25 | 2001-11-08 | Hae-Young Bae | Biphenyl butyric acid derivative as a matrix metalloproteinase inhibitor |
| AR042586A1 (es) | 2001-02-15 | 2005-06-29 | Sugen Inc | 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa |
| AU2002351412B2 (en) | 2001-12-21 | 2010-05-20 | Exelixis Patent Company Llc | Modulators of LXR |
| US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| EA200701782A3 (ru) | 2003-04-24 | 2008-04-28 | Инсайт Корпорейшн | Производные азаспироалканов в качестве ингибиторов металлопротеаз |
| US7534894B2 (en) | 2003-09-25 | 2009-05-19 | Wyeth | Biphenyloxy-acids |
| WO2005055928A2 (en) * | 2003-12-02 | 2005-06-23 | The Ohio State University Research Foundation | Zn2+ -chelating motif-tethered short -chain fatty acids as a novel class of histone deacetylase inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| BRPI0508098A (pt) | 2004-02-27 | 2007-07-17 | Amgen Inc | compostos, composições farmacêuticas e métodos para uso no tratamento de distúrbios metabólicos |
| US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
| NZ587549A (en) * | 2004-06-24 | 2012-10-26 | Vertex Pharma | 6-Amino-indole derivatives and processes for their preparation |
| US20080090836A1 (en) * | 2004-09-20 | 2008-04-17 | Peter Nilsson | Pyrazole Compounds Useful In The Treatment Of Inflammation |
| US20070225318A1 (en) * | 2004-09-20 | 2007-09-27 | Biolipox Ab | Pyrazole Compounds Useful In The Treatment Of Inflammation |
| US7465804B2 (en) | 2005-05-20 | 2008-12-16 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders |
| EP1760076A1 (en) * | 2005-09-02 | 2007-03-07 | Ferring B.V. | FAP Inhibitors |
| EP1924546A1 (en) | 2005-09-14 | 2008-05-28 | Amgen, Inc | Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders |
| TW200800911A (en) * | 2005-10-20 | 2008-01-01 | Biolipox Ab | Pyrazoles useful in the treatment of inflammation |
| TW200732320A (en) * | 2005-10-31 | 2007-09-01 | Biolipox Ab | Pyrazoles useful in the treatment of inflammation |
| KR20080067364A (ko) * | 2005-10-31 | 2008-07-18 | 바이올리폭스 에이비 | 리폭시게나제 억제제로서의 트리아졸 화합물 |
| EP1943225A1 (en) * | 2005-11-01 | 2008-07-16 | Biolipox AB | Pyrazoles useful in the treatment of inflammation |
| EP1957483A1 (en) | 2005-12-01 | 2008-08-20 | F.Hoffmann-La Roche Ag | Novel vinylogous acids derivatives |
| JP2009521468A (ja) * | 2005-12-24 | 2009-06-04 | バーテックス ファーマシューティカルズ インコーポレイテッド | Abc輸送体の調節因子としてのキノリン−4−オン誘導体 |
| CA2635581C (en) | 2005-12-28 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| EP2460793A1 (en) | 2006-02-03 | 2012-06-06 | Bionomics Limited | Substituted Benzofurans, Benzothiophenes, Benzoselenophenes and Indoles And Their Use as Tubulin Polymerisation Inhibitors |
| US7910108B2 (en) * | 2006-06-05 | 2011-03-22 | Incyte Corporation | Sheddase inhibitors combined with CD30-binding immunotherapeutics for the treatment of CD30 positive diseases |
| WO2008030520A1 (en) | 2006-09-07 | 2008-03-13 | Amgen Inc. | Heterocyclic gpr40 modulators |
| EP2061760A1 (en) | 2006-09-07 | 2009-05-27 | Amgen, Inc | Benzo-fused compounds for use in treating metabolic disorders |
| US7705034B2 (en) | 2006-10-13 | 2010-04-27 | Hoffmann-La Roche Inc. | Vinylogous acid derivatives |
| MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
| JP2010524932A (ja) | 2007-04-16 | 2010-07-22 | アムジエン・インコーポレーテツド | 置換ビフェニルフェノキシ−、チオフェニル−及びアミノフェニルプロパン酸gpr40調節物質 |
| JP5461405B2 (ja) | 2007-09-14 | 2014-04-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | 嚢胞性線維症膜コンダクタンス制御因子の調節因子 |
| KR20100090249A (ko) | 2007-10-10 | 2010-08-13 | 암젠 인크 | 치환된 비페닐 grp40 조절제 |
| US8450522B2 (en) | 2008-03-06 | 2013-05-28 | Amgen Inc. | Conformationally constrained carboxylic acid derivatives useful for treating metabolic disorders |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| ES2450567T3 (es) | 2008-10-15 | 2014-03-25 | Amgen, Inc | Moduladores de GPR40 espirocíclicos |
| PL2408750T3 (pl) | 2009-03-20 | 2016-02-29 | Vertex Pharma | Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy |
| US8802700B2 (en) | 2010-12-10 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| AU2013226076B2 (en) | 2012-02-27 | 2017-11-16 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administration thereof |
| KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
Family Cites Families (31)
| 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 |
| US4139619A (en) * | 1976-05-24 | 1979-02-13 | The Upjohn Company | 6-Amino-4-(substituted amino)-1,2-dihydro-1-hydroxy-2-iminopyrimidine, topical compositions and process for hair growth |
| 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 |
| 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 |
| 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 |
| 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. |
| US5120742A (en) * | 1984-02-27 | 1992-06-09 | Merck & Co., Inc. | 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-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 |
| 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 |
| 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 |
| 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 |
| US5175155A (en) * | 1991-10-07 | 1992-12-29 | Sterling Winthrop Inc. | Win 49596-finasteride method of use and compositions |
-
1993
- 1993-05-19 EP EP93911358A patent/EP0641204B1/en not_active Expired - Lifetime
- 1993-05-19 US US08/338,572 patent/US5536727A/en not_active Expired - Fee Related
- 1993-05-19 CA CA002135174A patent/CA2135174A1/en not_active Abandoned
- 1993-05-19 AU AU42521/93A patent/AU668180B2/en not_active Ceased
- 1993-05-19 AT AT93911358T patent/ATE195530T1/de not_active IP Right Cessation
- 1993-05-19 ES ES93911358T patent/ES2148229T3/es not_active Expired - Lifetime
- 1993-05-19 WO PCT/US1993/004746 patent/WO1993023040A1/en not_active Ceased
- 1993-05-19 DE DE69329240T patent/DE69329240D1/de not_active Expired - Lifetime
- 1993-05-19 JP JP6503831A patent/JPH07508038A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA2135174A1 (en) | 1993-11-25 |
| AU668180B2 (en) | 1996-04-26 |
| US5536727A (en) | 1996-07-16 |
| WO1993023040A1 (en) | 1993-11-25 |
| JPH07508038A (ja) | 1995-09-07 |
| AU4252193A (en) | 1993-12-13 |
| DE69329240D1 (de) | 2000-09-21 |
| EP0641204A4 (en) | 1995-08-23 |
| ATE195530T1 (de) | 2000-09-15 |
| EP0641204A1 (en) | 1995-03-08 |
| EP0641204B1 (en) | 2000-08-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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