ATE171188T1 - In 15-stellung substituierte 4-azasteroide - Google Patents

In 15-stellung substituierte 4-azasteroide

Info

Publication number
ATE171188T1
ATE171188T1 AT94911577T AT94911577T ATE171188T1 AT E171188 T1 ATE171188 T1 AT E171188T1 AT 94911577 T AT94911577 T AT 94911577T AT 94911577 T AT94911577 T AT 94911577T AT E171188 T1 ATE171188 T1 AT E171188T1
Authority
AT
Austria
Prior art keywords
group
alkyl
hydrogen
azasteroids
substituted
Prior art date
Application number
AT94911577T
Other languages
English (en)
Inventor
Philippe L Durette
Craig K Esser
William Hagmann
Ihor E Kopka
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 ATE171188T1 publication Critical patent/ATE171188T1/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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/001—Lactones
    • C07J21/003—Lactones at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Saccharide Compounds (AREA)
AT94911577T 1993-03-12 1994-03-11 In 15-stellung substituierte 4-azasteroide ATE171188T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/030,508 US5359071A (en) 1993-03-12 1993-03-12 15-substituted 4-azasteroids

Publications (1)

Publication Number Publication Date
ATE171188T1 true ATE171188T1 (de) 1998-10-15

Family

ID=21854519

Family Applications (1)

Application Number Title Priority Date Filing Date
AT94911577T ATE171188T1 (de) 1993-03-12 1994-03-11 In 15-stellung substituierte 4-azasteroide

Country Status (9)

Country Link
US (1) US5359071A (de)
EP (1) EP0700291B1 (de)
JP (1) JP3337689B2 (de)
AT (1) ATE171188T1 (de)
AU (1) AU674222B2 (de)
CA (1) CA2157363A1 (de)
DE (1) DE69413393T2 (de)
ES (1) ES2122258T3 (de)
WO (1) WO1994020104A1 (de)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
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WO1993023419A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
EP0705273B1 (de) * 1993-06-24 2002-03-27 Richter Gedeon Vegyeszeti Gyar R.T. 17-halogen-4-azaandrosten-derivate und verfahren zu ihrer herstellung
CN1058499C (zh) * 1993-10-21 2000-11-15 麦克公司 １６－取代－４－氮杂－雄甾烷－５α－还原酶同工酶１抑制剂
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
AU694576B2 (en) * 1994-10-21 1998-07-23 Merck & Co., Inc. Combination method for acne treatment
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
US5811510A (en) * 1995-04-14 1998-09-22 General Hospital Corporation Biodegradable polyacetal polymers and methods for their formation and use
EP0859617A1 (de) * 1995-09-27 1998-08-26 Merck & Co., Inc. Verfahren zur verhinderung des androgenes haarausfalls mittels 5-alpha reduktaseinhibitoren
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
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
CA2283098A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
EP1321146A3 (de) * 1998-03-11 2004-06-02 Endorecherche Inc. Typ 5 und Typ 3 17 Beta-Hydroxisteroid-Dehydrogenasehemmer und Verfahren zu ihrer Anwendung
KR100872722B1 (ko) * 2002-06-28 2008-12-05 주식회사 중외제약 피나스테라이드의 제조방법
US7519874B2 (en) * 2002-09-30 2009-04-14 Lecroy Corporation Method and apparatus for bit error rate analysis
WO2004100874A2 (en) * 2003-05-07 2004-11-25 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
CA2724130C (en) * 2008-06-06 2016-04-26 Harbor Biosciences, Inc. Methods for preparing 17-alkynyl-7-hydroxy steroids and related compounds

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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
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
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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
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
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
EP0285382B1 (de) * 1987-04-03 1994-04-13 Merck & Co. Inc. Behandlung von androgener Alopecia mit 17-bêta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
JP2675418B2 (ja) * 1988-05-25 1997-11-12 スミスクライン・ベックマン・コーポレイション 芳香族ステロイド５‐α‐レダクターゼ抑制剤
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
US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
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
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors

Also Published As

Publication number Publication date
DE69413393T2 (de) 1999-05-12
JP3337689B2 (ja) 2002-10-21
US5359071A (en) 1994-10-25
DE69413393D1 (de) 1998-10-22
AU674222B2 (en) 1996-12-12
WO1994020104A1 (en) 1994-09-15
CA2157363A1 (en) 1994-09-15
EP0700291B1 (de) 1998-09-16
ES2122258T3 (es) 1998-12-16
EP0700291A1 (de) 1996-03-13
JPH08507535A (ja) 1996-08-13
AU6406594A (en) 1994-09-26
EP0700291A4 (de) 1996-07-03

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