DE68917884T2 - Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren. - Google Patents

Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren.

Info

Publication number
DE68917884T2
DE68917884T2 DE68917884T DE68917884T DE68917884T2 DE 68917884 T2 DE68917884 T2 DE 68917884T2 DE 68917884 T DE68917884 T DE 68917884T DE 68917884 T DE68917884 T DE 68917884T DE 68917884 T2 DE68917884 T2 DE 68917884T2
Authority
DE
Germany
Prior art keywords
steroids
acid derivatives
phosphinic acid
reductase inhibitors
alpha reductase
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 - Fee Related
Application number
DE68917884T
Other languages
English (en)
Other versions
DE68917884D1 (de
Inventor
Dennis Alan Holt
Mark Alan Levy
Brian Walter Metcalf
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of DE68917884D1 publication Critical patent/DE68917884D1/de
Application granted granted Critical
Publication of DE68917884T2 publication Critical patent/DE68917884T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/002—Expansion of ring A by one atom, e.g. A homo steroids
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J61/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
DE68917884T 1988-12-23 1989-12-19 Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren. Expired - Fee Related DE68917884T2 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/290,212 US5026882A (en) 1988-12-23 1988-12-23 Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase

Publications (2)

Publication Number Publication Date
DE68917884D1 DE68917884D1 (de) 1994-10-06
DE68917884T2 true DE68917884T2 (de) 1995-03-23

Family

ID=23114995

Family Applications (1)

Application Number Title Priority Date Filing Date
DE68917884T Expired - Fee Related DE68917884T2 (de) 1988-12-23 1989-12-19 Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren.

Country Status (13)

Country Link
US (1) US5026882A (de)
EP (1) EP0375349B1 (de)
JP (1) JPH02215796A (de)
AT (1) ATE110735T1 (de)
AU (1) AU630139B2 (de)
CA (1) CA2005214A1 (de)
DE (1) DE68917884T2 (de)
DK (1) DK645389A (de)
ES (1) ES2059789T3 (de)
HU (1) HU205137B (de)
IE (1) IE894111L (de)
PT (1) PT92723A (de)
ZA (1) ZA899671B (de)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4970204A (en) * 1989-08-23 1990-11-13 Smithkline Beecham Corporation 3-substituted nitro-steroid derivatives as 5-α-reductase inhibitors
US5516768A (en) * 1990-03-16 1996-05-14 Smithkline Beecham Corporation Uncompetitive inhibition of steroid and 5α-reductose
US5162332A (en) * 1990-06-20 1992-11-10 Merck & Co., Inc. Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
US5061802A (en) * 1990-06-20 1991-10-29 Merck & Co. Inc. 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors
US5151430A (en) * 1990-06-20 1992-09-29 Merck & Co., Inc. Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen agents
US5091380A (en) * 1990-06-28 1992-02-25 Merck & Co., Inc. N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
CH681153A5 (de) * 1991-01-28 1993-01-29 Marigen S.A. Neue sterolester- und sterolphosphorverbindungen.
NZ241979A (en) * 1991-03-20 1996-01-26 Merck & Co Inc Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
HUT71484A (en) * 1992-05-20 1995-11-28 Merck & Co Inc Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them
ATE198601T1 (de) * 1992-05-20 2001-01-15 Merck & Co Inc Ester derivate von 4-aza-steroiden
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
ATE183193T1 (de) * 1992-05-20 1999-08-15 Merck & Co Inc 17-amino-substituierte 4-azasteroide als 5-alpha- reductase inhibitoren
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
DE69329240D1 (de) * 1992-05-20 2000-09-21 Merck & Co Inc 17-ether und thioether von 4-aza-steroiden
DE69329149T2 (de) * 1992-05-20 2001-03-29 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
RU2141967C1 (ru) * 1992-05-21 1999-11-27 Андорешерш Инк. ИНГИБИТОРЫ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ АКТИВНОСТИ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ
US5324734A (en) * 1992-09-15 1994-06-28 Merck & Co., Inc. Oxidization metabolites of 5-α-23-methyl-4-aza-21-nor-chol-1-ene-3, 20-dione
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
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
WO1995000147A1 (en) * 1993-06-28 1995-01-05 Merck & Co., Inc. 4-AZA-PREGNANE 5α-REDUCTASE ISOZYME 1 INHIBITORS
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US6867216B1 (en) 1998-04-09 2005-03-15 Johns Hopkins University School Of Medicine Inhibitors of hedgehog signal pathways, compositions and uses related thereto
US7291626B1 (en) 1998-04-09 2007-11-06 John Hopkins University School Of Medicine Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
IL138645A0 (en) * 1998-04-09 2001-10-31 Univ Johns Hopkins Med Use of steroidal alkaloid derivatives as inhibitors of hedghog signalling pathways
CA2330611A1 (en) 1998-05-22 1999-12-02 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
WO2001027135A2 (en) 1999-10-13 2001-04-19 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
DK1889198T3 (da) 2005-04-28 2015-02-09 Proteus Digital Health Inc Farma-informatiksystem
EP1945240B1 (de) 2005-09-16 2016-12-28 Raptor Pharmaceutical Inc Zusammensetzungen mit rezeptor-assoziierten protein (rap) varianten, die für cr-haltige proteine spezifisch sind und ihre verwendungen
ES2728225T3 (es) 2009-02-20 2019-10-23 2 Bbb Medicines B V Sistema de administración de fármacos a base de glutatión
US8445002B2 (en) 2009-05-06 2013-05-21 Laboratory Skin Care, Inc. Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

Family Cites Families (9)

* 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
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
DK465481A (da) * 1980-11-21 1982-05-22 Hoffmann La Roche Fremgangsmaade til fremstilling af d-homostemoider
CA1252778A (en) * 1983-08-25 1989-04-18 Hoffmann-La Roche Limited/Hoffmann-La Roche Limitee Steroids
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US4946834A (en) * 1988-12-23 1990-08-07 Smithkline Beecham Corporation Phosphonic acid substituted steroids as steroid 5α-reductase inhibitors
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase

Also Published As

Publication number Publication date
DK645389D0 (da) 1989-12-19
EP0375349B1 (de) 1994-08-31
CA2005214A1 (en) 1990-06-23
IE894111L (en) 1990-06-23
EP0375349A1 (de) 1990-06-27
DK645389A (da) 1990-06-24
PT92723A (pt) 1990-06-29
HUT55795A (en) 1991-06-28
ATE110735T1 (de) 1994-09-15
AU4703989A (en) 1990-06-28
ES2059789T3 (es) 1994-11-16
JPH02215796A (ja) 1990-08-28
ZA899671B (en) 1990-11-28
DE68917884D1 (de) 1994-10-06
HU205137B (en) 1992-03-30
US5026882A (en) 1991-06-25
HU895286D0 (en) 1990-01-28
AU630139B2 (en) 1992-10-22

Similar Documents

Publication Publication Date Title
DE68917884T2 (de) Phosphinsäure-Derivate von Steroiden als 5-alpha-Reduktase-Inhibitoren.
ATE118505T1 (de) Phosphinsäure-derivate von aromatischen steroiden als 5-alpha reduktase-inhibitoren.
DE68919660T2 (de) Phosphonsäure-Derivate von aromatischen Steroiden als 5-alpha-Reduktase-Inhibitoren.
ATE77388T1 (de) Steroid-5-alpha-reduktase-inhibitoren.
DE68917885D1 (de) Phosphonsäure-Derivate von Steroiden als Hemmstoffe der 5-alpha-Reduktase.
DE68920128D1 (de) Sulfonsäure-substituierte aromatische Steroide als 5-Alpha-Reduktase-Inhibitoren.
IE881269L (en) Steroids
ES2075180T3 (es) Nuevos derivados de la piridona, su procedimiento de preparacion, los nuevos productos intermedios obtenidos, su aplicacion como medicamentos y las composiciones farmaceuticas que los contienen.
ES2052075T3 (es) Composicion farmaceutica liquida para derivados de piperidinoalcanol.
ES2095542T3 (es) Nuevos ciclopentanperhidrofenantren-17beta-(hidroxi o alcoxi)-17alfa-(aril o heterociclil)-3beta-derivados activos sobre el sistema cardiovascular, procesos para su preparacion y composiciones farmaceuticas que contienen los mismos.
IL86731A0 (en) Pharmaceutical compositions containing estradien-3-one derivatives and androst-2-ene-2-carbonitrile derivatives

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee