ZA933496B - New 7betabsubstituted-4-aza-5alpha-cholestan-3-ones as 5alpha-reductase inhibitors - Google Patents

New 7betabsubstituted-4-aza-5alpha-cholestan-3-ones as 5alpha-reductase inhibitors

Info

Publication number
ZA933496B
ZA933496B ZA933496A ZA933496A ZA933496B ZA 933496 B ZA933496 B ZA 933496B ZA 933496 A ZA933496 A ZA 933496A ZA 933496 A ZA933496 A ZA 933496A ZA 933496 B ZA933496 B ZA 933496B
Authority
ZA
South Africa
Prior art keywords
5alpha
cholestan
aza
ones
new
Prior art date
Application number
ZA933496A
Other languages
English (en)
Inventor
Raman K Bakshi
Gary H Rasmusson
Richard L Tolman
Gool F Patel
Georgianna Harris
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of ZA933496B publication Critical patent/ZA933496B/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001Steroids 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
    • C07J73/005Steroids 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52Stabilizers
    • A61K2800/522Antioxidants; Radical scavengers

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ZA933496A 1992-05-20 1993-05-19 New 7betabsubstituted-4-aza-5alpha-cholestan-3-ones as 5alpha-reductase inhibitors ZA933496B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88602392A 1992-05-20 1992-05-20

Publications (1)

Publication Number Publication Date
ZA933496B true ZA933496B (en) 1993-12-22

Family

ID=25388214

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA933496A ZA933496B (en) 1992-05-20 1993-05-19 New 7betabsubstituted-4-aza-5alpha-cholestan-3-ones as 5alpha-reductase inhibitors

Country Status (21)

Country Link
US (1) US5527807A (cs)
EP (1) EP0572165B1 (cs)
JP (2) JPH07119232B2 (cs)
CN (1) CN1085562A (cs)
AT (1) ATE158300T1 (cs)
AU (1) AU658296B2 (cs)
BG (1) BG99177A (cs)
CA (1) CA2096576A1 (cs)
CZ (1) CZ283894A3 (cs)
DE (1) DE69313921T2 (cs)
FI (1) FI945442L (cs)
HU (1) HUT71484A (cs)
IL (1) IL105717A0 (cs)
MX (1) MX9302931A (cs)
NO (1) NO944406L (cs)
RU (1) RU94046044A (cs)
SI (1) SI9300270A (cs)
SK (1) SK137994A3 (cs)
WO (1) WO1993023419A1 (cs)
YU (1) YU34393A (cs)
ZA (1) ZA933496B (cs)

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WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
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SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
BR9407866A (pt) 1993-10-21 1996-10-29 Merck & Co Inc Composto processos para inibiçao de 5 -redufase ou isoenzimas da mesma paratratamento de condiçoes de acne vulgar alopécia androgènica hirsutismo feminino hiperplasia prostática benigna prostatite e para o tratamento e/ou prevençao do cancer da próstata para interrupçao e reversao de alopécia androgènica e promoçao do crescimento de cabelo em um mamifero e para inibiçao de conversao biossintética da testosterona para di-hidro- testosterona em um mamifero e composiçao farmacèutica
IL111467A0 (en) * 1993-11-12 1994-12-29 Merck & Co Inc Pharmaceutical compositions comprising 7 beta -substituted -4-aza 5 alpha -cholestan-3-ones and 5 alpha reductase 1 inhibitors
CN1152316A (zh) * 1994-05-19 1997-06-18 麦克公司 具有烯丙基的甾族化合物的氧化
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
GB9506678D0 (en) * 1995-03-31 1995-05-24 Glaxo Inc Substituted 6-azacholesten-3-ones
US5585383A (en) * 1995-05-03 1996-12-17 Merck & Co., Inc. Process for crystallizing a 4-azasteroid 5alpha-reductase inhibitor
US5763361A (en) * 1995-10-23 1998-06-09 Merck & Co., Inc. 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
AU5791698A (en) * 1996-12-09 1998-07-03 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
WO1998041211A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
JP2001523259A (ja) * 1997-05-07 2001-11-20 ノヴォファーム リミテッド 4−アザ−ステロイド類
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
FR2898272B1 (fr) * 2006-03-09 2008-07-04 Trophos Sa Utilisation de derives du 3,5-seco-4-nor-cholestrane pour l'obtention d'un medicament cytoprotecteur
FR2919181A1 (fr) * 2007-07-25 2009-01-30 Trophos Sa Utilisation du 4-azacholest-4-ene n-oxide ou de ses derives comme antioxydants

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US3285918A (en) * 1962-04-18 1966-11-15 Norman J Doorenbos 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
US3239417A (en) * 1962-12-07 1966-03-08 Smith Kline French Lab Methods and compositions for inhibiting sterol biosynthesis
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FR1465544A (fr) * 1965-11-29 1967-01-13 Roussel Uclaf Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation
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UA35589C2 (uk) * 1992-05-21 2001-04-16 Андорешерш Інк. ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ
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Also Published As

Publication number Publication date
HU9403311D0 (en) 1995-02-28
BG99177A (bg) 1995-07-28
CA2096576A1 (en) 1993-11-21
FI945442A7 (fi) 1994-11-18
EP0572165B1 (en) 1997-09-17
SI9300270A (sl) 1993-12-31
EP0572165A1 (en) 1993-12-01
JPH0656881A (ja) 1994-03-01
HUT71484A (en) 1995-11-28
YU34393A (sh) 1996-10-09
SK137994A3 (en) 1995-04-12
CZ283894A3 (en) 1995-09-13
AU3869793A (en) 1993-11-25
NO944406L (no) 1995-01-19
DE69313921D1 (de) 1997-10-23
RU94046044A (ru) 1996-10-10
NO944406D0 (no) 1994-11-17
FI945442A0 (fi) 1994-11-18
JPH07119232B2 (ja) 1995-12-20
CN1085562A (zh) 1994-04-20
AU658296B2 (en) 1995-04-06
US5527807A (en) 1996-06-18
IL105717A0 (en) 1993-09-22
WO1993023419A1 (en) 1993-11-25
JPH07206759A (ja) 1995-08-08
FI945442L (fi) 1994-11-18
MX9302931A (es) 1994-02-28
ATE158300T1 (de) 1997-10-15
DE69313921T2 (de) 1998-04-09

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