ATE255125T1 - Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren von 5-alpha-reduktase - Google Patents

Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren von 5-alpha-reduktase

Info

Publication number
ATE255125T1
ATE255125T1 AT96202933T AT96202933T ATE255125T1 AT E255125 T1 ATE255125 T1 AT E255125T1 AT 96202933 T AT96202933 T AT 96202933T AT 96202933 T AT96202933 T AT 96202933T AT E255125 T1 ATE255125 T1 AT E255125T1
Authority
AT
Austria
Prior art keywords
alpha
androstan
aza
beta
substituted
Prior art date
Application number
AT96202933T
Other languages
English (en)
Inventor
Raman K Bakshi
Gary H Rasmusson
Richard L Tolman
Gool F Patel
Georgianna Harris
Donald W Graham
Bruce E Witzel
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 ATE255125T1 publication Critical patent/ATE255125T1/de

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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (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)
AT96202933T 1992-05-20 1993-05-19 Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren von 5-alpha-reduktase ATE255125T1 (de)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ATE255125T1 true ATE255125T1 (de) 2003-12-15

Family

ID=25389283

Family Applications (2)

Application Number Title Priority Date Filing Date
AT93303882T ATE156838T1 (de) 1992-05-20 1993-05-19 Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren 5-alpha-reduktases
AT96202933T ATE255125T1 (de) 1992-05-20 1993-05-19 Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren von 5-alpha-reduktase

Family Applications Before (1)

Application Number Title Priority Date Filing Date
AT93303882T ATE156838T1 (de) 1992-05-20 1993-05-19 Neue 7-beta-substituierte-4-aza-5-alpha-androstan-3- nen als inhibitoren 5-alpha-reduktases

Country Status (14)

Country Link
US (1) US5710275A (de)
EP (2) EP0572166B1 (de)
JP (1) JPH06100587A (de)
CN (1) CN1087092A (de)
AT (2) ATE156838T1 (de)
CA (1) CA2096616A1 (de)
DE (2) DE69313018T2 (de)
DK (1) DK0572166T3 (de)
ES (2) ES2210336T3 (de)
GR (1) GR3024884T3 (de)
IL (1) IL105715A (de)
MX (1) MX9302932A (de)
WO (1) WO1993023420A1 (de)
ZA (1) ZA933497B (de)

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US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
AU672978B2 (en) * 1992-05-20 1996-10-24 Merck & Co., Inc. 4-azasteroid 5-alpha-reductase inhibitors
US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
EP0641209A4 (de) * 1992-05-20 1995-08-23 Merck & Co Inc Neue 17-ester-, amid- und ketonderivate von 3-oxo-4-azasteroiden als 5-alpha-reduktaseinhibitoren.
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
WO1994007861A1 (en) * 1992-10-06 1994-04-14 Merck & Co., Inc. 17β-CARBOXANILIDES OF 4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
PT674521E (pt) * 1992-12-18 2001-10-31 Merck & Co Inc Metedo para o tratamento da prostatite cronica com 17beta-n-carbamoil monossubstituido-4-aza-5alfa-androst-1-en-3-onas
AU679769B2 (en) * 1993-06-28 1997-07-10 Merck & Co., Inc. 4-AZA-pregnane 5alpha-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
DE69417925T2 (de) * 1993-11-04 1999-11-25 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
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
EP0862556B1 (de) * 1995-10-23 2001-09-05 Merck & Co., Inc. 17-alkyl-7-substituierte-4-aza-steroidderivate
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
WO1998050419A2 (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
AU2003219656B2 (en) 2002-01-15 2007-05-17 Merck Sharp & Dohme Corp. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
JP4832303B2 (ja) * 2003-05-07 2011-12-07 メルク・シャープ・エンド・ドーム・コーポレイション アンドロゲン受容体モジュレータおよびこれらの使用
AU2004259664B2 (en) * 2003-06-30 2009-05-28 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP1641535A4 (de) * 2003-06-30 2008-05-14 Merck & Co Inc 17-acetamido-4-azasteroidderivate als androgenrezeptormodulatoren
WO2005005606A2 (en) * 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530048A1 (en) * 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CN1849120A (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－氮杂甾类衍生物
AU2004272004B2 (en) 2003-09-10 2009-01-22 Merck Sharp & Dohme Corp. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
WO2005099707A1 (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
WO2022261774A1 (en) * 2021-06-16 2022-12-22 UNIVERSITé LAVAL Novel inhibitors of 17b-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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US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
EP0641209A4 (de) * 1992-05-20 1995-08-23 Merck & Co Inc Neue 17-ester-, amid- und ketonderivate von 3-oxo-4-azasteroiden als 5-alpha-reduktaseinhibitoren.
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
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
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Also Published As

Publication number Publication date
JPH06100587A (ja) 1994-04-12
DE69313018T2 (de) 1998-02-19
EP0778284A3 (de) 1997-08-13
ES2106965T3 (es) 1997-11-16
ZA933497B (en) 1993-12-14
EP0778284B1 (de) 2003-11-26
GR3024884T3 (en) 1998-01-30
CN1087092A (zh) 1994-05-25
WO1993023420A1 (en) 1993-11-25
EP0778284A2 (de) 1997-06-11
MX9302932A (es) 1995-01-31
AU3869893A (en) 1993-11-25
AU662224B2 (en) 1995-08-24
EP0572166A1 (de) 1993-12-01
ES2210336T3 (es) 2004-07-01
IL105715A (en) 1997-07-13
DE69333317D1 (de) 2004-01-08
DE69313018D1 (de) 1997-09-18
DE69333317T2 (de) 2004-08-19
ATE156838T1 (de) 1997-08-15
IL105715A0 (en) 1993-09-22
CA2096616A1 (en) 1993-11-21
EP0572166B1 (de) 1997-08-13
DK0572166T3 (da) 1997-09-01
US5710275A (en) 1998-01-20

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