ATE198601T1 - Ester derivate von 4-aza-steroiden - Google Patents

Ester derivate von 4-aza-steroiden

Info

Publication number
ATE198601T1
ATE198601T1 AT93911362T AT93911362T ATE198601T1 AT E198601 T1 ATE198601 T1 AT E198601T1 AT 93911362 T AT93911362 T AT 93911362T AT 93911362 T AT93911362 T AT 93911362T AT E198601 T1 ATE198601 T1 AT E198601T1
Authority
AT
Austria
Prior art keywords
pct
ester derivatives
date nov
sec
aza steroids
Prior art date
Application number
AT93911362T
Other languages
English (en)
Inventor
Bruce E Witzel
Gary H Rasmusson
Richard L Tolman
Shu Shu Yang
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 ATE198601T1 publication Critical patent/ATE198601T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001Steroids 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
    • C07J73/005Steroids 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)
AT93911362T 1992-05-20 1993-05-19 Ester derivate von 4-aza-steroiden ATE198601T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88602292A 1992-05-20 1992-05-20
PCT/US1993/004771 WO1993023041A1 (en) 1992-05-20 1993-05-19 Ester derivatives of 4-aza-steroids

Publications (1)

Publication Number Publication Date
ATE198601T1 true ATE198601T1 (de) 2001-01-15

Family

ID=25388211

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93911362T ATE198601T1 (de) 1992-05-20 1993-05-19 Ester derivate von 4-aza-steroiden

Country Status (8)

Country Link
US (1) US5610162A (de)
EP (1) EP0649306B1 (de)
JP (1) JPH07508039A (de)
AT (1) ATE198601T1 (de)
AU (1) AU668181B2 (de)
CA (1) CA2135173A1 (de)
DE (1) DE69329856D1 (de)
WO (1) WO1993023041A1 (de)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4311987A1 (de) * 1993-04-07 1994-10-13 Schering Ag Neue Glucocorticoide
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
US5547957A (en) 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
TW382595B (en) * 1993-10-15 2000-02-21 Merck & Co Inc Pharmaceutical composition for use in arresting and reversing androgenic alopecia
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
US5770620A (en) * 1995-06-19 1998-06-23 Ontogen Corporation Aryl acrylic acid derivatives useful as protein tyrosine phosphatase inhibitors
US6388076B1 (en) 1995-06-19 2002-05-14 Ontogen Corporation Protein tyrosine phosphatase-inhibiting compounds
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US6534037B1 (en) 1998-01-21 2003-03-18 Neorx Corporation Non-steroidal compounds for steroid receptors and uses relating thereto
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
US6797820B2 (en) * 1999-12-17 2004-09-28 Vicuron Pharmaceuticals Inc. Succinate compounds, compositions and methods of use and preparation
US6477900B2 (en) 2001-01-08 2002-11-12 Jet Sensor Ltd. Fluidic gas metering system
JP5082033B2 (ja) 2001-12-21 2012-11-28 エグゼリクシス パテント カンパニー エルエルシー Lxrのモジュレーター
US7482366B2 (en) 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
DE10256187A1 (de) * 2002-12-02 2004-06-09 Bayer Ag 2-Oxyamino-1-cyclopenten-1-nitrile als Materialschutzmittel
GEP20084393B (en) 2003-04-24 2008-06-10 Incyte Corp Aza spiro alkane derivatives as inhibitors of metalloproteases
US7781595B2 (en) 2003-09-22 2010-08-24 S*Bio Pte Ltd. Benzimidazole derivatives: preparation and pharmaceutical applications
CA2552279C (en) * 2003-12-02 2014-07-15 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
KR20070004769A (ko) 2004-02-27 2007-01-09 암젠 인코포레이션 대사 장애의 치료에 사용되는 화합물, 약제학적 조성물 및그 사용방법
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
HUE032540T2 (en) * 2004-06-24 2017-09-28 Vertex Pharma Modulators of ATP-binding cassette transporters
EP1794130A1 (de) * 2004-09-20 2007-06-13 Biolipox AB Pyrazolverbindungen die in der behandlung von entzündungen nützlich sind
JP2008513426A (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
EP1924546A1 (de) 2005-09-14 2008-05-28 Amgen, Inc Konformationseingeschränkte 3- (4-hydroxy-phenyl) substitutierte propansäuren zur behandlung von stoffwechselstörungen
TW200800911A (en) * 2005-10-20 2008-01-01 Biolipox Ab Pyrazoles useful in the treatment of inflammation
EP1943234A1 (de) * 2005-10-31 2008-07-16 Biolipox AB Triazolverbindungen als lipoxygenaseinhibitoren
TW200732320A (en) * 2005-10-31 2007-09-01 Biolipox Ab Pyrazoles useful in the treatment of inflammation
WO2007052000A1 (en) * 2005-11-01 2007-05-10 Biolipox Ab Pyrazoles useful in the treatment of inflammation
BRPI0619096A2 (pt) 2005-12-01 2011-09-13 Hoffmann La Roche derivados de ácidos vinìlogos
US20090105272A1 (en) * 2005-12-24 2009-04-23 Grootenhuis Peter D J Prodrugs of modulators of ABC transporters
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
ES2386299T3 (es) 2006-02-03 2012-08-16 Bionomics Limited Benzofuranos, benzotiofenos, benzoselenofenos e indoles sustituidos y su uso como inhibidores de la polimerización de tubulina
WO2007143600A2 (en) * 2006-06-05 2007-12-13 Incyte Corporation Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases
EP2061760A1 (de) 2006-09-07 2009-05-27 Amgen, Inc Benzokondensierte verbindungen zur verwendung bei der behandlung von stoffwechselerkrankungen
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
AU2007332754A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
CA2672494A1 (en) 2006-12-14 2008-06-19 Nps Pharmaceuticals, Inc. Use of d-serine derivatives for the treatment of anxiety disorders
CA2683751C (en) 2007-04-16 2013-01-08 Amgen Inc. Substituted biphenyl phenoxy-, thiophenyl- and aminophenylpropanoic acid gpr40 modulators
AU2008298545B2 (en) 2007-09-14 2013-12-12 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2010003876A (es) 2007-10-10 2010-12-02 Amgen Inc Moduladores de gpr40 bifenilo- sustituidos.
EP2260017A1 (de) 2008-03-06 2010-12-15 Amgen, Inc Konformationseingeschränkte carbonsäurederivate, die sich für die behandlung von stoffwechselerkrankungen eignen
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
AU2009303475B2 (en) 2008-10-15 2012-09-13 Amgen Inc. Spirocyclic GPR40 modulators
US20120108559A1 (en) * 2009-01-14 2012-05-03 The Trustees Of The University Of Pennsylvania Receptor activator of the rank receptor complex inhibitor
EP2821400B1 (de) 2009-03-20 2017-09-27 Vertex Pharmaceuticals Incorporated Verfahren zur Herstellung von CFTR-Regulatoren
US9012594B2 (en) * 2010-04-22 2015-04-21 Northwestern University Catalyst and byproduct-free native chemical ligation using cyclic thioester precursors
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
RU2692779C2 (ru) 2012-02-27 2019-06-27 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтическая композиция и ее введения
RU2749213C2 (ru) 2014-10-07 2021-06-07 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе
AR108257A1 (es) 2016-05-02 2018-08-01 Mei Pharma Inc Formas polimórficas de 3-[2-butil-1-(2-dietilamino-etil)-1h-bencimidazol-5-il]-n-hidroxi-acrilamida y usos de las mismas
US12425371B2 (en) * 2022-09-16 2025-09-23 Cisco Technology, Inc. System and method for providing SCHC-based edge firewalling

Family Cites Families (30)

* Cited by examiner, † Cited by third party
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
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
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
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
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
JPH0737199B2 (ja) * 1985-04-02 1995-04-26 株式会社ジェイエスイー 表面の付着物除去方法
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
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
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
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

Also Published As

Publication number Publication date
AU668181B2 (en) 1996-04-26
EP0649306A4 (de) 1995-08-23
AU4252593A (en) 1993-12-13
US5610162A (en) 1997-03-11
DE69329856D1 (de) 2001-02-15
EP0649306A1 (de) 1995-04-26
EP0649306B1 (de) 2001-01-10
JPH07508039A (ja) 1995-09-07
WO1993023041A1 (en) 1993-11-25
CA2135173A1 (en) 1993-11-25

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