ATE115587T1 - 11-keto- oder hydroxy-3,5-diensteroiden als inhibitoren der steroid-5-alpha-reduktase. - Google Patents

11-keto- oder hydroxy-3,5-diensteroiden als inhibitoren der steroid-5-alpha-reduktase.

Info

Publication number
ATE115587T1
ATE115587T1 AT90311807T AT90311807T ATE115587T1 AT E115587 T1 ATE115587 T1 AT E115587T1 AT 90311807 T AT90311807 T AT 90311807T AT 90311807 T AT90311807 T AT 90311807T AT E115587 T1 ATE115587 T1 AT E115587T1
Authority
AT
Austria
Prior art keywords
alpha
keto
steroids
steroid
hydroxy
Prior art date
Application number
AT90311807T
Other languages
English (en)
Inventor
Dennis Alan Holt
Brian Walter Metcalf
Mark Alan Levy
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
Application granted granted Critical
Publication of ATE115587T1 publication Critical patent/ATE115587T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0011Androstane derivatives substituted in position 17 by a keto group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J61/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/002Expansion of ring A by one atom, e.g. A homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0095Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 carbon in position 21 is part of carboxylic group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Toxicology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AT90311807T 1989-11-01 1990-10-29 11-keto- oder hydroxy-3,5-diensteroiden als inhibitoren der steroid-5-alpha-reduktase. ATE115587T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/430,152 US5041433A (en) 1987-04-29 1989-11-01 11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-α-reductase

Publications (1)

Publication Number Publication Date
ATE115587T1 true ATE115587T1 (de) 1994-12-15

Family

ID=23706275

Family Applications (1)

Application Number Title Priority Date Filing Date
AT90311807T ATE115587T1 (de) 1989-11-01 1990-10-29 11-keto- oder hydroxy-3,5-diensteroiden als inhibitoren der steroid-5-alpha-reduktase.

Country Status (15)

Country Link
US (1) US5041433A (de)
EP (1) EP0427434B1 (de)
JP (1) JPH03169890A (de)
KR (1) KR100187945B1 (de)
AT (1) ATE115587T1 (de)
AU (1) AU641701B2 (de)
CA (1) CA2028622A1 (de)
DE (1) DE69015129T2 (de)
DK (1) DK0427434T3 (de)
ES (1) ES2064661T3 (de)
GR (1) GR3015372T3 (de)
IE (1) IE65562B1 (de)
NZ (1) NZ235871A (de)
PT (1) PT95750A (de)
ZA (1) ZA908730B (de)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5516768A (en) * 1990-03-16 1996-05-14 Smithkline Beecham Corporation Uncompetitive inhibition of steroid and 5α-reductose
US5300294A (en) * 1990-06-27 1994-04-05 Smithkline Beecham Corporation Method of treating prostatic adenocarcinoma
IT1259419B (it) * 1991-05-24 1996-03-18 Erba Carlo Spa Steroidi 3-carbossi 17b - sostituiti insaturi utili come inibitori della testosterone 5 a reduttasi
NZ245504A (en) * 1991-12-20 1995-08-28 Hoechst Ag Bile acid derivatives containing an ethylenically unsaturated grouping
US5215894A (en) * 1992-02-25 1993-06-01 Merck & Co., Inc. Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors
HUT71514A (en) * 1992-05-21 1995-12-28 Endorecherche Inc Inhibitors of testosterone 5 alfa-reductase activity and pharmaceutical compositions containing the same
US5641765A (en) * 1992-11-18 1997-06-24 Smithkline Beecham Corporation 17-αand 17-βsubstituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-α-reductase
US5683995A (en) * 1992-11-18 1997-11-04 Smithkline Beecham Corporation 17 substituted acyl-3-carboxy 3,5-diene steroidals as α-reductase inhibitors
AP9300589A0 (en) * 1992-11-18 1994-01-31 Smithkline Beecham Corp Novel 17a and 17b substituted acyl-3-carboxy 3,5-diene steroidal compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-a-reductase.
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5637310A (en) * 1993-12-20 1997-06-10 Smithkline Beecham Corporation Method of treating prostatic adenocarcinoma
WO1995028413A1 (en) * 1994-04-15 1995-10-26 Smithkline Beecham Corporation 17β-SUBSTITUTED 3-CARBOXY STEROIDS THAT INHIBIT 5-α-REDUCTASE
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
CA2330611A1 (en) 1998-05-22 1999-12-02 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
US20060148725A1 (en) * 2001-12-21 2006-07-06 The Miriam Hospital Selective 11beta HSD inhibitors and methods of use thereof
WO2003059267A2 (en) * 2001-12-21 2003-07-24 Rhode Island Hospital SELECTIVE 11β-HSD INHIBITORS AND METHODS FOR USE THEREOF
US20050020550A1 (en) * 2003-04-29 2005-01-27 Morris David J. Selective testicular 11beta-HSD inhibitors and methods of use thereof
SI1889198T1 (sl) 2005-04-28 2015-02-27 Proteus Digital Health, Inc. Farma-informacijski sistem
WO2007035716A2 (en) 2005-09-16 2007-03-29 Raptor Pharmaceutical Inc. Compositions comprising receptor-associated protein (rap) variants specific for cr-containing proteins and uses thereof
DK2398500T3 (da) 2009-02-20 2019-05-13 2 Bbb Medicines B V Glutathion-baseret lægemiddelafgivelsessystem
SG175896A1 (en) 2009-05-06 2011-12-29 Lab Skin Care Inc Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same
CN116606340A (zh) * 2022-10-14 2023-08-18 上海醇健实业发展有限公司 一种甾体化合物及其制备方法、其用途和其药物组合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-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
US4814324A (en) * 1987-03-06 1989-03-21 Merck & Co., Inc. Sterol inhibitors of testosterone 5α-reductase
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors

Also Published As

Publication number Publication date
KR100187945B1 (ko) 1999-06-01
KR910009725A (ko) 1991-06-28
NZ235871A (en) 1991-12-23
DK0427434T3 (da) 1995-05-08
US5041433A (en) 1991-08-20
JPH03169890A (ja) 1991-07-23
AU6551190A (en) 1991-07-18
DE69015129D1 (de) 1995-01-26
IE65562B1 (en) 1995-11-01
EP0427434B1 (de) 1994-12-14
EP0427434A2 (de) 1991-05-15
AU641701B2 (en) 1993-09-30
ES2064661T3 (es) 1995-02-01
PT95750A (pt) 1991-09-13
EP0427434A3 (en) 1992-03-04
CA2028622A1 (en) 1991-05-02
ZA908730B (en) 1991-11-27
GR3015372T3 (en) 1995-06-30
DE69015129T2 (de) 1995-05-04
IE903920A1 (en) 1991-05-08

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Legal Events

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UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee