ZA918570B - Azasteroid compounds for the treatment of prostatic hypertrophy,their preparation and use - Google Patents

Azasteroid compounds for the treatment of prostatic hypertrophy,their preparation and use

Info

Publication number
ZA918570B
ZA918570B ZA918570A ZA918570A ZA918570B ZA 918570 B ZA918570 B ZA 918570B ZA 918570 A ZA918570 A ZA 918570A ZA 918570 A ZA918570 A ZA 918570A ZA 918570 B ZA918570 B ZA 918570B
Authority
ZA
South Africa
Prior art keywords
alkyl group
substituted alkyl
carbon
preparation
treatment
Prior art date
Application number
ZA918570A
Other languages
English (en)
Inventor
Koichi Kojima
Kojima Koichi
Hitoshi Kurata
Kurata Hitoshi
Hiroyoshi Horikoshi
Horikoshi Hiroyoshi
Takakazu Hamada
Hamada Takakazu
Original Assignee
Sankyo Co
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 Sankyo Co filed Critical Sankyo Co
Publication of ZA918570B publication Critical patent/ZA918570B/xx

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
    • 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
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ZA918570A 1990-10-29 1991-10-28 Azasteroid compounds for the treatment of prostatic hypertrophy,their preparation and use ZA918570B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP29140190 1990-10-29

Publications (1)

Publication Number Publication Date
ZA918570B true ZA918570B (en) 1992-08-26

Family

ID=17768420

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA918570A ZA918570B (en) 1990-10-29 1991-10-28 Azasteroid compounds for the treatment of prostatic hypertrophy,their preparation and use

Country Status (19)

Country Link
US (1) US5302621A (fr)
EP (1) EP0484094B1 (fr)
JP (1) JPH0819151B2 (fr)
KR (1) KR0134570B1 (fr)
CN (2) CN1053672C (fr)
AT (1) ATE139783T1 (fr)
AU (1) AU640279B2 (fr)
CA (1) CA2054368C (fr)
CZ (1) CZ279312B6 (fr)
DE (1) DE69120500T2 (fr)
DK (1) DK0484094T3 (fr)
ES (1) ES2091299T3 (fr)
GR (1) GR3020483T3 (fr)
HU (2) HU218667B (fr)
IE (1) IE76452B1 (fr)
IL (1) IL99889A (fr)
PT (1) PT99371B (fr)
RU (1) RU2070204C1 (fr)
ZA (1) ZA918570B (fr)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
CA2084799C (fr) 1991-12-17 2003-01-28 Glenn J. Gormley Methode de prevention du carcinome prostatique a l'aide de 17 beta-n-monosubstitue-carbamyl-4-aza-5 alpha-androst-1 -en-3-ones
ATE165368T1 (de) * 1991-12-20 1998-05-15 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha reductase.
US5698720A (en) * 1992-04-20 1997-12-16 Sankyo Company, Limited Steroid derivatives
EP0725074A3 (fr) * 1992-04-20 1996-11-20 Sankyo Co Composés intermédiaires pour la préparation des dérivés androst-3,5-diène-3-carboxy
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
AU674145B2 (en) * 1992-05-20 1996-12-12 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
EP0663924B1 (fr) * 1992-10-06 2001-02-14 Merck & Co. Inc. 17-beta-carboxanilides de 4-aza-5-alpha-androstan-3-ones utilises comme inhibiteurs de 5-alpha-reductase
WO1994022900A1 (fr) * 1993-04-02 1994-10-13 Ciba-Geigy Ag AZA-ANDROSTANE-17β-CARBOXAMIDES
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
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5578724A (en) * 1994-09-20 1996-11-26 Eli Lilly And Company Process for preparation of benzo[f]quinolinones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
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
IT1271325B (it) * 1994-12-23 1997-05-27 Poli Ind Chimica Spa Composti diastereomericamente puri derivati da 3-oxo e 3-tioxo-4-azaandrostani e loro uso come antiandrogeni
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
CN1072679C (zh) * 1995-07-30 2001-10-10 重庆医科大学 一种氮杂甾体化合物、制备及其用途
US6001844A (en) * 1995-09-15 1999-12-14 Merck & Co., Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
EP0859761A4 (fr) * 1995-09-15 2000-01-26 Merck & Co Inc 4-azasteroides utilises pour le traitement d'etats hyperandrogeniques
PT923942E (pt) * 1996-02-05 2002-03-28 Sankyo Co Preparacao inibidora de 5alfa-reductase para administracao oral um processo para producao da mesma e sua utilizacao
PT963998E (pt) * 1997-02-26 2004-07-30 Sankyo Co Composicoes para tratar ou prevenir cancro prostatico
US6093722A (en) 1997-02-26 2000-07-25 Sankyo Company, Limited Method for treating prostate cancer
IL134199A0 (en) 1997-07-29 2001-04-30 Sankyo Co MEDICAMENTS CONTAINING 5α-ANDROST-1-ENE-17β-CARBOXAMIDE DERIVATIVES
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
HRP20040822A2 (en) * 2002-03-13 2005-06-30 Merck & Co. Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
CA2524409C (fr) * 2003-05-07 2011-12-20 Merck & Co., Inc. Modulateurs du recepteur d'androgenes et leur methode d'utilisation
AU2004255749B2 (en) * 2003-06-30 2008-12-18 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US7329750B2 (en) * 2003-06-30 2008-02-12 Merck & Co., Inc. 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530025A1 (fr) * 2003-06-30 2005-01-20 William P. Dankulich Derives de 17-acetamido-4-azasteroide en tant que modulateurs du recepteur d'androgene
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
CN101146535A (zh) * 2005-03-25 2008-03-19 默克公司 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法
CN116621913B (zh) * 2022-08-12 2026-03-27 湖南科益新生物医药有限公司 一种4-氮杂甾体化合物及其制备方法、用途及药物组合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4179453A (en) 1978-04-13 1979-12-18 Merck & Co., Inc. Process for preparing 17β-carboxy-5-androsten-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
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
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids

Also Published As

Publication number Publication date
HUT59417A (en) 1992-05-28
HU913396D0 (en) 1992-01-28
US5302621A (en) 1994-04-12
GR3020483T3 (en) 1996-10-31
HU218667B (hu) 2000-10-28
AU8682191A (en) 1992-04-30
DE69120500T2 (de) 1997-02-27
DE69120500D1 (de) 1996-08-01
IE913747A1 (en) 1992-05-22
HK1005456A1 (en) 1999-01-08
JPH0819151B2 (ja) 1996-02-28
DK0484094T3 (da) 1996-10-28
AU640279B2 (en) 1993-08-19
EP0484094B1 (fr) 1996-06-26
RU2070204C1 (ru) 1996-12-10
PT99371B (pt) 1999-04-30
CA2054368C (fr) 2001-10-02
IE76452B1 (en) 1997-10-22
HU211642A9 (en) 1995-12-28
CZ279312B6 (cs) 1995-04-12
IL99889A (en) 1995-06-29
ES2091299T3 (es) 1996-11-01
CN1053672C (zh) 2000-06-21
KR920008063A (ko) 1992-05-27
CA2054368A1 (fr) 1992-04-30
CN1062145A (zh) 1992-06-24
ATE139783T1 (de) 1996-07-15
CN1072935C (zh) 2001-10-17
CN1209319A (zh) 1999-03-03
PT99371A (pt) 1992-09-30
EP0484094A2 (fr) 1992-05-06
IL99889A0 (en) 1992-08-18
HK1017274A1 (en) 1999-11-19
CS326991A3 (en) 1992-05-13
JPH0532693A (ja) 1993-02-09
KR0134570B1 (ko) 1998-04-14
EP0484094A3 (en) 1993-07-14

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