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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
androstan
aza
new
inhibitors
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)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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
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.
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.

Family Applications After (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) ATE255125T1 (es)
CA (1) CA2096616A1 (es)
DE (2) DE69333317T2 (es)
DK (1) DK0572166T3 (es)
ES (2) ES2106965T3 (es)
GR (1) GR3024884T3 (es)
IL (1) IL105715A (es)
MX (1) MX9302932A (es)
WO (1) WO1993023420A1 (es)
ZA (1) ZA933497B (es)

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JPH07508033A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド ５α−レダクターゼ阻害剤としての３−オキソ−４−アザステロイドの新規１７−エステル，アミド及びケトン誘導体
JPH07508034A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド １７−アミノ置換４−アザステロイド５α−レダクターゼ阻害剤
ES2149208T3 (es) * 1992-05-20 2000-11-01 Merck & Co Inc Inhibidores 4-azaesteroides de 5-alfa-reductasa.
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
AU676478B2 (en) * 1992-05-20 1997-03-13 Merck & Co., Inc. New delta-17 and delta-20 olefinic and saturated 17beta- substituted-4-aza-5alpha-androstan-3-ones as 5alpha- reductase inhibitors
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY
US5693810A (en) * 1992-10-06 1997-12-02 Merck & Co., Inc. 17 β-carboxanilides of 4-aza-5α-androstan-3-ones as 5α-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.
JP3325026B2 (ja) * 1993-06-28 2002-09-17 メルク エンド カンパニー インコーポレーテッド ４−アザ−プレグナン５α−レダクターゼアイソザイム１阻害剤
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
JPH09504553A (ja) * 1993-11-04 1997-05-06 メルク エンド カンパニー インコーポレーテッド ５α−レダクターゼ阻害薬としての７−置換−４−アザ−ステロイド誘導体
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
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
ES2160842T3 (es) * 1995-10-23 2001-11-16 Merck & Co Inc Derivados de esteroides 17-alquil-4-aza-7-sustituidos.
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
CA2287924A1 (en) * 1997-05-07 1998-11-12 Novopharm Limited 4-aza-steroids as inhibitors of testosterone-5-alpha-reductase
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
WO2003059293A2 (en) * 2002-01-15 2003-07-24 Merck & Co., Inc. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
WO2004100874A2 (en) * 2003-05-07 2004-11-25 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
EP1641464A4 (en) * 2003-06-30 2008-05-14 Merck & Co Inc 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR
WO2005005606A2 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004255200A1 (en) * 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004256075B2 (en) * 2003-06-30 2008-12-04 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CN1849126A (zh) 2003-09-10 2006-10-18 默克公司 作为雄激素受体调节剂的17－杂环－4－氮杂甾族衍生物
JP2007505120A (ja) * 2003-09-10 2007-03-08 メルク　エンド　カムパニー　インコーポレーテッド アンドロゲン受容体調節因子としての１７−複素環式−４−アザステロイド誘導体。
EP1734964A4 (en) * 2004-04-08 2009-06-17 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
BR112012026720B1 (pt) * 2010-04-20 2018-01-30 Syngenta Participations Ag Compostos de amidas do ácido pirazol carboxílico e processo para a preparação dos mesmos
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
CA3223165A1 (en) * 2021-06-16 2022-12-22 Universite Laval Novel inhibitors of 17.beta.-hsd7 and uses thereof

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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
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
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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
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
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
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
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US5300294A (en) * 1990-06-27 1994-04-05 Smithkline Beecham Corporation Method of treating prostatic adenocarcinoma
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JPH07508033A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド ５α−レダクターゼ阻害剤としての３−オキソ−４−アザステロイドの新規１７−エステル，アミド及びケトン誘導体
AU676478B2 (en) * 1992-05-20 1997-03-13 Merck & Co., Inc. New delta-17 and delta-20 olefinic and saturated 17beta- substituted-4-aza-5alpha-androstan-3-ones as 5alpha- reductase inhibitors
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-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
MX9302932A (es) 1995-01-31
AU662224B2 (en) 1995-08-24
JPH06100587A (ja) 1994-04-12
ES2210336T3 (es) 2004-07-01
IL105715A (en) 1997-07-13
IL105715A0 (en) 1993-09-22
DE69333317D1 (de) 2004-01-08
CA2096616A1 (en) 1993-11-21
EP0572166A1 (en) 1993-12-01
DE69333317T2 (de) 2004-08-19
DK0572166T3 (da) 1997-09-01
GR3024884T3 (en) 1998-01-30
CN1087092A (zh) 1994-05-25
WO1993023420A1 (en) 1993-11-25
EP0778284A3 (en) 1997-08-13
ATE156838T1 (de) 1997-08-15
AU3869893A (en) 1993-11-25
EP0572166B1 (en) 1997-08-13
EP0778284A2 (en) 1997-06-11
EP0778284B1 (en) 2003-11-26
US5710275A (en) 1998-01-20
ATE255125T1 (de) 2003-12-15
DE69313018D1 (de) 1997-09-18
DE69313018T2 (de) 1998-02-19
ZA933497B (en) 1993-12-14

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