CA2231041A1 - 4-azasteroides utilises pour le traitement d'etats hyperandrogeniques - Google Patents

4-azasteroides utilises pour le traitement d'etats hyperandrogeniques Download PDF

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Publication number
CA2231041A1
CA2231041A1 CA002231041A CA2231041A CA2231041A1 CA 2231041 A1 CA2231041 A1 CA 2231041A1 CA 002231041 A CA002231041 A CA 002231041A CA 2231041 A CA2231041 A CA 2231041A CA 2231041 A1 CA2231041 A1 CA 2231041A1
Authority
CA
Canada
Prior art keywords
methyl
alpha
oxo
aza
ene
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.)
Abandoned
Application number
CA002231041A
Other languages
English (en)
Inventor
Raman K. Bakshi
Soumya P. Sahoo
Richard L. Tolman
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
Individual
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
Priority claimed from GBGB9603487.1A external-priority patent/GB9603487D0/en
Application filed by Individual filed Critical Individual
Publication of CA2231041A1 publication Critical patent/CA2231041A1/fr
Abandoned legal-status Critical Current

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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

L'invention porte sur des composés représentés par la formule développée (I), et sur leurs sels et leurs esters pharmaceutiquement acceptables, possédant une activité inhibitrice de 5.alpha.-réductase. Ces composés inhibent la 5.alpha.-réductase des types 1 et 2. Les composés de formule développée (I) servent au traitement curatif et préventif systémique - y compris oral, et parentéral - y compris local, d'états hyperandrogéniques, y compris de carcinomes prostatiques, de l'hyperplasie prostatique, de l'acné vulgaire, de la séborrhée, de l'alopécie androgénique (également appelée alopécie androgénétique), qui comprend la calvitie masculine et féminime, l'hirsutisme féminin et la prostatite. Des composés de la présente invention sont également de puissants anti-androgènes. L'invention porte également sur des compositions contenant de tels composés, sur leurs procédés d'utilisation et leurs procédés de fabrication.
CA002231041A 1995-09-15 1996-09-11 4-azasteroides utilises pour le traitement d'etats hyperandrogeniques Abandoned CA2231041A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US382695P 1995-09-15 1995-09-15
US60/003,826 1995-09-15
GBGB9603487.1A GB9603487D0 (en) 1996-02-20 1996-02-20 4-azasteroids for the treatment of hyperandrogenic conditions
GB9603487.1 1996-02-20
PCT/US1996/014564 WO1997010217A1 (fr) 1995-09-15 1996-09-11 4-azasteroides utilises pour le traitement d'etats hyperandrogeniques

Publications (1)

Publication Number Publication Date
CA2231041A1 true CA2231041A1 (fr) 1997-03-20

Family

ID=26308763

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002231041A Abandoned CA2231041A1 (fr) 1995-09-15 1996-09-11 4-azasteroides utilises pour le traitement d'etats hyperandrogeniques

Country Status (5)

Country Link
EP (1) EP0859761A4 (fr)
JP (1) JPH11512434A (fr)
AU (1) AU707324B2 (fr)
CA (1) CA2231041A1 (fr)
WO (1) WO1997010217A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6137399A (en) * 1998-09-09 2000-03-27 Merck & Co., Inc. Method of determining and reducing the risk of bph-related urologic events
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
US7402577B2 (en) * 2001-10-03 2008-07-22 Merck & Co., Inc. Androstane 17-beta-carboxamides as androgen receptor modulators
PL372920A1 (en) * 2002-03-13 2005-08-08 Merck & Co,Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
JP2007500219A (ja) 2003-05-16 2007-01-11 アンビット バイオサイエンシス コーポレーション 複素環化合物およびその使用法
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
JP2008534505A (ja) 2005-03-25 2008-08-28 メルク エンド カムパニー インコーポレーテッド テストステロンサプリメントおよび５アルファ−レダクターゼインヒビターによる男性の治療方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
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
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
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
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
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes

Also Published As

Publication number Publication date
AU6973796A (en) 1997-04-01
AU707324B2 (en) 1999-07-08
EP0859761A1 (fr) 1998-08-26
JPH11512434A (ja) 1999-10-26
EP0859761A4 (fr) 2000-01-26
WO1997010217A1 (fr) 1997-03-20

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead