ATE139783T1 - Azasteroide zur behandlung prostatischer hypertrophie, ihre herstellung und verwendung - Google Patents

Azasteroide zur behandlung prostatischer hypertrophie, ihre herstellung und verwendung

Info

Publication number
ATE139783T1
ATE139783T1 AT91309967T AT91309967T ATE139783T1 AT E139783 T1 ATE139783 T1 AT E139783T1 AT 91309967 T AT91309967 T AT 91309967T AT 91309967 T AT91309967 T AT 91309967T AT E139783 T1 ATE139783 T1 AT E139783T1
Authority
AT
Austria
Prior art keywords
alkyl group
substituted alkyl
carbon
aryl
preparation
Prior art date
Application number
AT91309967T
Other languages
English (en)
Inventor
Koichi Kojima
Hitoshi Kurata
Hiroyoshi Horikoshi
Takakazu Hamada
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
Application granted granted Critical
Publication of ATE139783T1 publication Critical patent/ATE139783T1/de

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
    • 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
    • A61K31/56—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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (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)
AT91309967T 1990-10-29 1991-10-29 Azasteroide zur behandlung prostatischer hypertrophie, ihre herstellung und verwendung ATE139783T1 (de)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ATE139783T1 true ATE139783T1 (de) 1996-07-15

Family

ID=17768420

Family Applications (1)

Application Number Title Priority Date Filing Date
AT91309967T ATE139783T1 (de) 1990-10-29 1991-10-29 Azasteroide zur behandlung prostatischer hypertrophie, ihre herstellung und verwendung

Country Status (19)

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

Families Citing this family (39)

* 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 (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
US5543406A (en) * 1991-12-20 1996-08-06 Glaxo Wellcome, Inc. Inhibitors of 5-α-testosterone reductase
US5698720A (en) * 1992-04-20 1997-12-16 Sankyo Company, Limited Steroid derivatives
DK0567271T3 (da) * 1992-04-20 1998-02-16 Sankyo Co Steroidderivater til behandling af prostatahypertrofi, fremgangsmåde til fremstilling heraf og anvendelser heraf
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
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.
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-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
AU5323694A (en) * 1992-10-06 1994-04-26 Merck & Co., Inc. 17beta -carboxanilides of 4-aza-5alpha-androstan-3-ones as 5alpha-reductase inhibitors
WO1994022900A1 (en) * 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
DE69417925T2 (de) * 1993-11-04 1999-11-25 Merck & Co., Inc. 7-substituierte-4-aza-steroid-derivate als 5-alpha-reductase-hemmer
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
AU707324B2 (en) * 1995-09-15 1999-07-08 Merck & Co., Inc. 4-azasteroids for treatment of hyperandrogenic conditions
CN1215339A (zh) * 1996-02-05 1999-04-28 三共株式会社 5α－还原酶抑制剂的口服制剂及其制备方法和应用
US6093722A (en) 1997-02-26 2000-07-25 Sankyo Company, Limited Method for treating prostate cancer
EP0963998B1 (de) * 1997-02-26 2004-05-06 Sankyo Company Limited Azasteroidverbindung zur behandlung oder vorbeugung von prostatakrebs
ES2218840T3 (es) * 1997-07-29 2004-11-16 Sankyo Company Limited Composicion azasteroide para ael tratamiento de la alopecia, el hirsutismo femenino y la seborrea.
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
IL163825A0 (en) * 2002-03-13 2005-12-18 Merck & Co Inc Fluorinated 4-azasteroid derivatives 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
AU2004256075B2 (en) * 2003-06-30 2008-12-04 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
JP2007521292A (ja) * 2003-06-30 2007-08-02 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モジュレータとしての１７−アセトアミド−４−アザステロイド誘導体
AU2004259664B2 (en) * 2003-06-30 2009-05-28 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP1734963A4 (de) * 2004-04-02 2008-06-18 Merck & Co Inc Verfahren zur behandlung von menschen mit metabolischen und anthropometrischen störungen
AU2006229840B2 (en) * 2005-03-25 2010-12-23 Merck Sharp & Dohme Corp. Method of treating men with testosterone supplement and 5alpha-reductase inhibitor

Family Cites Families (8)

* 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
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
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
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
DE69120500D1 (de) 1996-08-01
AU640279B2 (en) 1993-08-19
CN1062145A (zh) 1992-06-24
HUT59417A (en) 1992-05-28
CN1209319A (zh) 1999-03-03
HU913396D0 (en) 1992-01-28
PT99371B (pt) 1999-04-30
EP0484094A3 (en) 1993-07-14
KR920008063A (ko) 1992-05-27
PT99371A (pt) 1992-09-30
EP0484094B1 (de) 1996-06-26
HK1017274A1 (en) 1999-11-19
HK1005456A1 (en) 1999-01-08
CA2054368C (en) 2001-10-02
IL99889A0 (en) 1992-08-18
CN1072935C (zh) 2001-10-17
CZ279312B6 (cs) 1995-04-12
IE913747A1 (en) 1992-05-22
CS326991A3 (en) 1992-05-13
ES2091299T3 (es) 1996-11-01
AU8682191A (en) 1992-04-30
DK0484094T3 (da) 1996-10-28
HU218667B (hu) 2000-10-28
ZA918570B (en) 1992-08-26
US5302621A (en) 1994-04-12
KR0134570B1 (ko) 1998-04-14
EP0484094A2 (de) 1992-05-06
IL99889A (en) 1995-06-29
RU2070204C1 (ru) 1996-12-10
HU211642A9 (en) 1995-12-28
GR3020483T3 (en) 1996-10-31
CN1053672C (zh) 2000-06-21
DE69120500T2 (de) 1997-02-27
JPH0532693A (ja) 1993-02-09
CA2054368A1 (en) 1992-04-30
IE76452B1 (en) 1997-10-22
JPH0819151B2 (ja) 1996-02-28

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