ATE195530T1 - 17-ether und thioether von 4-aza-steroiden - Google Patents
17-ether und thioether von 4-aza-steroidenInfo
- Publication number
- ATE195530T1 ATE195530T1 AT93911358T AT93911358T ATE195530T1 AT E195530 T1 ATE195530 T1 AT E195530T1 AT 93911358 T AT93911358 T AT 93911358T AT 93911358 T AT93911358 T AT 93911358T AT E195530 T1 ATE195530 T1 AT E195530T1
- Authority
- AT
- Austria
- Prior art keywords
- pct
- thioether
- ether
- date nov
- sec
- Prior art date
Links
- 150000003568 thioethers Chemical class 0.000 title abstract 2
- 150000000520 4-azasteroids Chemical class 0.000 title 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 abstract 1
- 108010044467 Isoenzymes Proteins 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 210000004761 scalp Anatomy 0.000 abstract 1
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
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88603192A | 1992-05-20 | 1992-05-20 | |
PCT/US1993/004746 WO1993023040A1 (en) | 1992-05-20 | 1993-05-19 | 17-ethers and thioethers of 4-aza-steroids |
Publications (1)
Publication Number | Publication Date |
---|---|
ATE195530T1 true ATE195530T1 (de) | 2000-09-15 |
Family
ID=25388234
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AT93911358T ATE195530T1 (de) | 1992-05-20 | 1993-05-19 | 17-ether und thioether von 4-aza-steroiden |
Country Status (9)
Country | Link |
---|---|
US (1) | US5536727A (de) |
EP (1) | EP0641204B1 (de) |
JP (1) | JPH07508038A (de) |
AT (1) | ATE195530T1 (de) |
AU (1) | AU668180B2 (de) |
CA (1) | CA2135174A1 (de) |
DE (1) | DE69329240D1 (de) |
ES (1) | ES2148229T3 (de) |
WO (1) | WO1993023040A1 (de) |
Families Citing this family (60)
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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 |
US6316429B1 (en) | 1997-05-07 | 2001-11-13 | Sugen, Inc. | Bicyclic protein kinase inhibitors |
US6486185B1 (en) | 1997-05-07 | 2002-11-26 | Sugen, Inc. | 3-heteroarylidene-2-indolinone protein kinase inhibitors |
US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
US6395734B1 (en) | 1998-05-29 | 2002-05-28 | Sugen, Inc. | Pyrrole substituted 2-indolinone protein kinase inhibitors |
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 |
CA2377629A1 (en) * | 2000-04-25 | 2001-11-08 | Hae-Young Bae | Biphenyl butyric acid derivative as a matrix metalloproteinase inhibitor |
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
CA2469435A1 (en) | 2001-12-21 | 2003-07-24 | X-Ceptor Therapeutics, Inc. | Modulators of lxr |
US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
JP4841429B2 (ja) * | 2003-04-24 | 2011-12-21 | インサイト・コーポレイション | メタロプロテアーゼの阻害剤としてのアザスピロアルカン誘導体 |
US7534894B2 (en) | 2003-09-25 | 2009-05-19 | Wyeth | Biphenyloxy-acids |
HUE028490T2 (en) * | 2003-12-02 | 2016-12-28 | Univ Ohio State Res Found | Short-chain fatty acids fixed to the Zn2-chelating motif as a new class of histone deacetylase inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CA2558585C (en) | 2004-02-27 | 2010-10-12 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders |
US8354427B2 (en) * | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
PL1773816T3 (pl) | 2004-06-24 | 2015-06-30 | Vertex Pharma | Modulatory transporterów posiadających kasetę wiążącą ATP |
WO2006032851A1 (en) * | 2004-09-20 | 2006-03-30 | Biolipox Ab | Pyrazole compounds useful in the treatment of inflammation |
JP2008513427A (ja) * | 2004-09-20 | 2008-05-01 | バイオリポックス エービー | 炎症の治療に有用なピラゾール化合物 |
US7465804B2 (en) | 2005-05-20 | 2008-12-16 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders |
EP1760076A1 (de) * | 2005-09-02 | 2007-03-07 | Ferring B.V. | FAP Inhibitoren |
CA2621949A1 (en) | 2005-09-14 | 2007-03-22 | 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 |
NZ567605A (en) * | 2005-10-31 | 2010-07-30 | Biolipox Ab | Triazole compounds as lipoxygenase inhibitors |
US20090088463A1 (en) * | 2005-11-01 | 2009-04-02 | Benjamin Pelcman | Pyrazoles Useful in the Treatment of Inflammation |
WO2007063010A1 (en) | 2005-12-01 | 2007-06-07 | F. Hoffmann-La Roche Ag | Novel vinylogous acids derivatives |
WO2007075901A2 (en) * | 2005-12-24 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Quinolin- 4 - one derivatives as modulators of abc transporters |
WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
EP1984333B1 (de) | 2006-02-03 | 2012-04-25 | Bionomics Limited | Substituierte benzofurane, benzothiophene, benzoselenophene und indole und ihre verwendung als tubulinpolymerisationsinhibitoren |
WO2007143600A2 (en) * | 2006-06-05 | 2007-12-13 | Incyte Corporation | Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases |
US7687526B2 (en) | 2006-09-07 | 2010-03-30 | Amgen Inc. | Benzo-fused compounds for use in treating metabolic disorders |
US7714008B2 (en) | 2006-09-07 | 2010-05-11 | Amgen Inc. | Heterocyclic GPR40 modulators |
US7705034B2 (en) | 2006-10-13 | 2010-04-27 | Hoffmann-La Roche Inc. | Vinylogous acid derivatives |
EP2064191B1 (de) | 2006-12-12 | 2014-06-25 | Merck Sharp & Dohme Corp. | Aspartylproteasehemmer |
US7572934B2 (en) | 2007-04-16 | 2009-08-11 | Amgen Inc. | Substituted biphenyl GPR40 modulators |
AU2008298545B2 (en) | 2007-09-14 | 2013-12-12 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
JP5591706B2 (ja) | 2007-10-10 | 2014-09-17 | アムジエン・インコーポレーテツド | 置換ビフェニルgpr40調節因子 |
MX2010009654A (es) | 2008-03-06 | 2010-09-28 | Amgen Inc | Derivados de acido carboxilico de conformacion restringida utiles para tratar trastornos metabolicos. |
AU2009303475B2 (en) | 2008-10-15 | 2012-09-13 | Amgen Inc. | Spirocyclic GPR40 modulators |
EP2408750B1 (de) | 2009-03-20 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Verfahren zur herstellung von modulatoren des cystic fibrosis transmembrane conductance-regulators |
US8802700B2 (en) | 2010-12-10 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
CA2865519C (en) | 2012-02-27 | 2018-01-02 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions comprising a solid dispersion of n-[2,4-bis(1,1-dimethylethyl0-5-hydroxyphenyl-1]-1,4-dihydro-4-oxoquinolone-3-carboxamide for treating cystic fibrosis |
MX370450B (es) | 2014-10-07 | 2019-12-13 | Vertex Pharma | Co-cristales de moduladores de regulador de conductancia de transmembrana en fibrosis quistica. |
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 |
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 |
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 |
EP0314199B1 (de) * | 1984-02-27 | 1991-09-18 | Merck & Co. Inc. | 17-Beta-substituierte-4-aza-5-alpha-Androstenone und ihre Anwendung als 5-Alpha-Reduktase-Inhibitoren |
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 |
NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
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 |
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 |
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 |
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 |
US5175155A (en) * | 1991-10-07 | 1992-12-29 | Sterling Winthrop Inc. | Win 49596-finasteride method of use and compositions |
-
1993
- 1993-05-19 JP JP6503831A patent/JPH07508038A/ja active Pending
- 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 DE DE69329240T patent/DE69329240D1/de not_active Expired - Lifetime
- 1993-05-19 AT AT93911358T patent/ATE195530T1/de not_active IP Right Cessation
- 1993-05-19 US US08/338,572 patent/US5536727A/en not_active Expired - Fee Related
- 1993-05-19 WO PCT/US1993/004746 patent/WO1993023040A1/en active IP Right Grant
- 1993-05-19 EP EP93911358A patent/EP0641204B1/de not_active Expired - Lifetime
- 1993-05-19 ES ES93911358T patent/ES2148229T3/es not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
WO1993023040A1 (en) | 1993-11-25 |
EP0641204A1 (de) | 1995-03-08 |
EP0641204A4 (de) | 1995-08-23 |
JPH07508038A (ja) | 1995-09-07 |
EP0641204B1 (de) | 2000-08-16 |
AU668180B2 (en) | 1996-04-26 |
CA2135174A1 (en) | 1993-11-25 |
DE69329240D1 (de) | 2000-09-21 |
ES2148229T3 (es) | 2000-10-16 |
AU4252193A (en) | 1993-12-13 |
US5536727A (en) | 1996-07-16 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |