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

    • 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)
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
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
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
CN101880277A (zh) 2003-04-24 2010-11-10 因塞特公司 作为金属蛋白酶抑制剂的氮杂螺烷衍生物
NZ545864A (en) 2003-09-22 2009-12-24 S Bio Pte Ltd Benzimidazole derivates: preparation and pharmaceutical applications
AU2004296764B2 (en) * 2003-12-02 2011-04-28 The Ohio State University Research Foundation Zn2+ -chelating motif-tethered short -chain fatty acids as a novel class of histone deacetylase 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
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
EA011010B1 (ru) 2004-02-27 2008-12-30 Эмджен, Инк. Соединения, модулирующие рецептор gpr40, фармацевтическая композиция, способ лечения заболеваний, чувствительных к модулированию рецептора gpr40 (варианты), способ модулирования функции gpr40 (варианты) и способ модулирования циркулирующей концентрации инсулина
MX341797B (es) * 2004-06-24 2016-09-02 Vertex Pharmaceuticals Incorporated * Moduladores de transportadores con casete de union con atp.
US8354427B2 (en) * 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated 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
WO2007033002A1 (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
EA200801108A1 (ru) * 2005-10-31 2008-10-30 Биолипокс Аб Триазолы, пригодные для лечения воспалений
JP2009513692A (ja) * 2005-11-01 2009-04-02 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
EP1957483A1 (de) 2005-12-01 2008-08-20 F.Hoffmann-La Roche Ag Neue vinyloge säurederivate
EP1979367A2 (de) * 2005-12-24 2008-10-15 Vertex Pharmaceuticals Incorporated Chinolin-4-on-derivate als modulatoren von abc-transportern
LT1993360T (lt) * 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma
NZ570014A (en) 2006-02-03 2011-04-29 Bionomics Ltd 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
WO2008030618A1 (en) 2006-09-07 2008-03-13 Amgen Inc. Benzo-fused compounds for use in treating metabolic disorders
CA2662305C (en) 2006-09-07 2012-04-17 Amgen Inc. Heterocyclic gpr40 modulators
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.
EP2099444A4 (de) 2006-12-14 2012-11-07 Nps Pharma Inc Verwendung von d-serin-derivaten zur behandlung von angststörungen
US7572934B2 (en) 2007-04-16 2009-08-11 Amgen Inc. Substituted biphenyl GPR40 modulators
CN101821266B (zh) 2007-09-14 2014-03-12 沃泰克斯药物股份有限公司 囊性纤维化跨膜通道调节因子的调节剂
BRPI0818253A2 (pt) 2007-10-10 2015-04-07 Amgen Inc Moduladores de gpr40 bifenil substituídos
WO2009111056A1 (en) 2008-03-06 2009-09-11 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
JP5551707B2 (ja) 2008-10-15 2014-07-16 アムジエン・インコーポレーテツド スピロ環ｇｐｒ４０調節因子
WO2010083084A1 (en) * 2009-01-14 2010-07-22 The Trustees Of The University Of Pennsylvania Receptor activator of the rank receptor complex inhibitor
MX384179B (es) 2009-03-20 2025-03-14 Vertex Pharma Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quística.
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
JP2015511583A (ja) 2012-02-27 2015-04-20 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ 薬学的組成物およびその投与
EP3204358B1 (de) 2014-10-07 2018-09-19 Vertex Pharmaceuticals Incorporated Cokristalle von modulatoren des transmembrankonduktanzregulators bei zystischer fibrose
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
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
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
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
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
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
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
WO1993023041A1 (en) 1993-11-25
JPH07508039A (ja) 1995-09-07
EP0649306B1 (de) 2001-01-10
AU668181B2 (en) 1996-04-26
US5610162A (en) 1997-03-11
AU4252593A (en) 1993-12-13
EP0649306A1 (de) 1995-04-26
EP0649306A4 (de) 1995-08-23
DE69329856D1 (de) 2001-02-15
CA2135173A1 (en) 1993-11-25

Similar Documents

Publication Publication Date Title
ATE198601T1 (de) Ester derivate von 4-aza-steroiden
DE69329240D1 (de) 17-ether und thioether von 4-aza-steroiden
TR200002784T2 (tr) Tip 5 ve tip 3 17beta-Hidroksisteroid dehidrojenaz inhibitörleri ve bunların kullanımı için metodlar
DE59409312D1 (de) Imidazopyridine und ihre anwendung zur behandlung von magen-darm krankheiten
NZ332762A (en) Isobutylgaba and its derivatives for the treatment of pain
DE69625691D1 (de) Verabreichung von peptidylheterocyclen zur behandlung von thrombin in zusammenhang stehenden krankheiten
DE10199023I1 (de) Benzoenaphthalinderivate Verfahren zu deren Herstellung und ihre Verwendung in Pharmazie und Kosmetik
NO913923D0 (no) 17beta-substituerte-4-aza-5alfa-androstan-3-on-derivater ogfremgangsmaate ved fremstilling av disse
DE69735442D1 (de) Antidiabetische mittel
CA2264750A1 (en) Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of alzheimer's disease and dementias
ES2149208T3 (es) Inhibidores 4-azaesteroides de 5-alfa-reductasa.
ATE212351T1 (de) Androsten-derivate
DE69534908D1 (de) Verwendung von statin zur behandlung von hauterkrankungen
BG100510A (bg) Метод за лечение на андрогенна алопеция с инхибитори на 5-алфа редуктаза
EP1098642A4 (de) Verfahren zur behandlung von zustanden moduliert durch lactosylceramiden
DE69631478D1 (de) Verwendung von vitamin d4-derivaten zur behandlung von hauterkrankungen
NO166939C (no) Analogifremgangsmaate for fremstilling av terapeutisk aktive carboxylsyrederivater.
KR950031085A (ko) 표피증식 질환 치료용 의약 조성물
DE69519728D1 (de) 17 beta-aryl-4-aza-steroidderivate
DE59902666D1 (de) Edelfosin zur behandlung von hirntumoren
DE69822153D1 (de) Verwendung von stickstoffhaltigen aromatischen heterozyklusderivaten zur topischen behandlung von epithelerkrankungen
RU95110751A (ru) Новые 17бета -замещенные производные 4-азандростана, фармацевтические составы, содержащие их, и способ их получения
ATE75399T1 (de) Therapeutikum zur behandlung von magengeschwueren.
DK0632717T3 (da) Middel til anvendelse som et anti-irritationsmiddel
NO910033L (no) Fremgangsmaate for fremstilling av terapeutisk aktive 2-hydroksy-3-fenoksypropylaminoforbindelser.

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties