ES2106965T3 - Nuevas 4-aza-5alfa-androstan-3-onas 7beta-sustituidas como inhibidores de 5alfa-reductasa. - Google Patents

Nuevas 4-aza-5alfa-androstan-3-onas 7beta-sustituidas como inhibidores de 5alfa-reductasa.

Info

Publication number
ES2106965T3
ES2106965T3 ES93303882T ES93303882T ES2106965T3 ES 2106965 T3 ES2106965 T3 ES 2106965T3 ES 93303882 T ES93303882 T ES 93303882T ES 93303882 T ES93303882 T ES 93303882T ES 2106965 T3 ES2106965 T3 ES 2106965T3
Authority
ES
Spain
Prior art keywords
5alfa
reductasa
new
7beta
onas
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
Application number
ES93303882T
Other languages
English (en)
Inventor
Raman K Bakshi
Gary H Rasmusson
Richard L Tolman
Gool F Patel
Georgianna Harris
Donald W Graham
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and 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 and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of ES2106965T3 publication Critical patent/ES2106965T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/76—Unsaturated compounds containing keto groups
    • C07C59/80—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings
    • C07C59/82—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/76—Unsaturated compounds containing keto groups
    • C07C59/90—Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE DESCRIBEN NUEVAS 4 DE 5 ALFA - REDUCTASA.
ES93303882T 1992-05-20 1993-05-19 Nuevas 4-aza-5alfa-androstan-3-onas 7beta-sustituidas como inhibidores de 5alfa-reductasa. Expired - Lifetime ES2106965T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88657292A 1992-05-20 1992-05-20

Publications (1)

Publication Number Publication Date
ES2106965T3 true ES2106965T3 (es) 1997-11-16

Family

ID=25389283

Family Applications (2)

Application Number Title Priority Date Filing Date
ES96202933T Expired - Lifetime ES2210336T3 (es) 1992-05-20 1993-05-19 Nuevas 7-beta-sustituido-4-aza-5-alfa-androstan-3-onas como inhibidores de 5-alfa-reductasa.
ES93303882T Expired - Lifetime ES2106965T3 (es) 1992-05-20 1993-05-19 Nuevas 4-aza-5alfa-androstan-3-onas 7beta-sustituidas como inhibidores de 5alfa-reductasa.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES96202933T Expired - Lifetime ES2210336T3 (es) 1992-05-20 1993-05-19 Nuevas 7-beta-sustituido-4-aza-5-alfa-androstan-3-onas como inhibidores de 5-alfa-reductasa.

Country Status (14)

Country Link
US (1) US5710275A (es)
EP (2) EP0778284B1 (es)
JP (1) JPH06100587A (es)
CN (1) CN1087092A (es)
AT (2) ATE156838T1 (es)
CA (1) CA2096616A1 (es)
DE (2) DE69333317T2 (es)
DK (1) DK0572166T3 (es)
ES (2) ES2210336T3 (es)
GR (1) GR3024884T3 (es)
IL (1) IL105715A (es)
MX (1) MX9302932A (es)
WO (1) WO1993023420A1 (es)
ZA (1) ZA933497B (es)

Families Citing this family (41)

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AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
CA2135057A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel 17-amino substituted 4-azasteroid 5a-reductase inhibitors
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
CA2135167A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors
DE69313114T2 (de) * 1992-05-20 1998-03-19 Merck & Co Inc NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE
WO1993023048A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 4-azasteroid 5-alpha-reductase inhibitors
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
EP0663924B1 (en) * 1992-10-06 2001-02-14 Merck & Co. Inc. 17-beta-carboxanilides of 4-aza-5-alpha-androstan-3-ones as 5-alpha-reductase inhibitors
ES2158887T3 (es) * 1992-12-18 2001-09-16 Merck & Co Inc Procedimiento para tratar la prostatitis cronica con 17 beta-n-terc-butilcarbamoil-4-aza-5 alfa-androst-1-en-ona.
CA2165077A1 (en) * 1993-06-28 1995-01-05 Philippe L. Durette 4-aza-pregnane 5.alpha.-reductase isozyme 1 inhibitors
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
ATE178795T1 (de) * 1993-11-04 1999-04-15 Merck & Co Inc 7-substituierte-4-aza-steroid-derivate als 5- alpha-reductase-hemmer
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
GB9415178D0 (en) * 1994-07-28 1994-09-21 Erba Carlo Spa 4-azasteroids with side-chain fluoroketones
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
JPH11513711A (ja) * 1995-10-23 1999-11-24 メルク エンド カンパニー インコーポレーテッド １７−アルキル−７−置換−４−アザステロイド誘導体
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
EP0983295A2 (en) * 1997-05-07 2000-03-08 Novopharm Ltd. 4-aza-steroids substituted in one or more of positions 7, 11 and 15 or with an unsaturated 14(15)-double bond as inhibitors of testosterone-5-alpha-reductase
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
AU2003219656B2 (en) * 2002-01-15 2007-05-17 Merck Sharp & Dohme Corp. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
EP1622567B1 (en) * 2003-05-07 2013-07-24 Merck Sharp & Dohme Corp. Androgen receptor modulators and methods of use thereof
EP1641761A4 (en) * 2003-06-30 2008-05-14 Merck & Co Inc 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
WO2005009949A2 (en) * 2003-06-30 2005-02-03 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004255749B2 (en) * 2003-06-30 2008-12-18 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP1641535A4 (en) * 2003-06-30 2008-05-14 Merck & Co Inc 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
EP1670483A4 (en) 2003-09-10 2010-02-17 Merck & Co Inc 17-heterocyclic 4-azasteroid derivatives as androgen receptor modules
EP1663228A4 (en) * 2003-09-10 2010-10-06 Merck Sharp & Dohme 17-heterocyclic 4-azasteroid derivatives as androgen receptor modules
CA2562132A1 (en) * 2004-04-08 2005-10-27 Merck & Co., Inc. 17 beta-acetamide-4-azasteroids as androgen receptor modulators
CN100355772C (zh) * 2005-12-28 2007-12-19 天津大学 具有5α－还原酶抑制活性的甾体化合物及其制备方法
ES2478875T3 (es) * 2010-04-20 2014-07-23 Syngenta Participations Ag Proceso para preparar amidas de ácidos carboxílicos pirazólicos
CN111175410A (zh) * 2020-02-12 2020-05-19 武汉大学 N-甲基苯乙胺及其同位素试剂在羧基化合物检测中的应用
US12662509B2 (en) 2021-06-16 2026-06-23 Shengxiang LIN Inhibitors of 17β-HSD7 and uses thereof
CN121108234B (zh) * 2025-11-13 2026-02-24 安徽益普克医药科技发展有限公司 一种5α-还原酶长效衍生物及其制备方法与用途

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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
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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
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
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
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DE69313114T2 (de) * 1992-05-20 1998-03-19 Merck & Co Inc NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE
SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
CA2135167A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors
WO1993023040A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
US5278159A (en) * 1992-10-06 1994-01-11 Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-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

Also Published As

Publication number Publication date
DE69313018D1 (de) 1997-09-18
DE69313018T2 (de) 1998-02-19
EP0572166A1 (en) 1993-12-01
ATE156838T1 (de) 1997-08-15
AU3869893A (en) 1993-11-25
AU662224B2 (en) 1995-08-24
IL105715A0 (en) 1993-09-22
ES2210336T3 (es) 2004-07-01
IL105715A (en) 1997-07-13
EP0778284A3 (en) 1997-08-13
CA2096616A1 (en) 1993-11-21
WO1993023420A1 (en) 1993-11-25
GR3024884T3 (en) 1998-01-30
MX9302932A (es) 1995-01-31
DE69333317T2 (de) 2004-08-19
EP0778284A2 (en) 1997-06-11
JPH06100587A (ja) 1994-04-12
EP0778284B1 (en) 2003-11-26
DK0572166T3 (da) 1997-09-01
ZA933497B (en) 1993-12-14
CN1087092A (zh) 1994-05-25
US5710275A (en) 1998-01-20
ATE255125T1 (de) 2003-12-15
EP0572166B1 (en) 1997-08-13
DE69333317D1 (de) 2004-01-08

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