BG99177A - Нови 7 бета-заместени-4-аза-5 алфа-холестанони като инхибитори на 5 алфа-редуктаза - Google Patents

Нови 7 бета-заместени-4-аза-5 алфа-холестанони като инхибитори на 5 алфа-редуктаза

Info

Publication number
BG99177A
BG99177A BG99177A BG9917794A BG99177A BG 99177 A BG99177 A BG 99177A BG 99177 A BG99177 A BG 99177A BG 9917794 A BG9917794 A BG 9917794A BG 99177 A BG99177 A BG 99177A
Authority
BG
Bulgaria
Prior art keywords
alpha
aza
substituted
cholestanone
beta
Prior art date
Application number
BG99177A
Other languages
English (en)
Inventor
Raman Bakshi
Gary Rasmusson
Richard Tolman
Gool 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 BG99177A publication Critical patent/BG99177A/bg

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic 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
    • C07D221/20—Spiro-condensed ring systems
    • 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
    • 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
    • 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
    • C07J9/00—Normal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52—Stabilizers
    • A61K2800/522—Antioxidants; 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)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Изобретението се отнася до нови 7 -заместени-4-аза-5 -холестан-3-они и сродни съединения, които сеизползват като инхибитори на 5 -редуктаза.
BG99177A 1992-05-20 1994-11-11 Нови 7 бета-заместени-4-аза-5 алфа-холестанони като инхибитори на 5 алфа-редуктаза BG99177A (bg)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88602392A 1992-05-20 1992-05-20
PCT/US1993/004615 WO1993023419A1 (en) 1992-05-20 1993-05-14 NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS

Publications (1)

Publication Number Publication Date
BG99177A true BG99177A (bg) 1995-07-28

Family

ID=25388214

Family Applications (1)

Application Number Title Priority Date Filing Date
BG99177A BG99177A (bg) 1992-05-20 1994-11-11 Нови 7 бета-заместени-4-аза-5 алфа-холестанони като инхибитори на 5 алфа-редуктаза

Country Status (21)

Country Link
US (1) US5527807A (bg)
EP (1) EP0572165B1 (bg)
JP (2) JPH07119232B2 (bg)
CN (1) CN1085562A (bg)
AT (1) ATE158300T1 (bg)
AU (1) AU658296B2 (bg)
BG (1) BG99177A (bg)
CA (1) CA2096576A1 (bg)
CZ (1) CZ283894A3 (bg)
DE (1) DE69313921T2 (bg)
FI (1) FI945442A7 (bg)
HU (1) HUT71484A (bg)
IL (1) IL105717A0 (bg)
MX (1) MX9302931A (bg)
NO (1) NO944406L (bg)
RU (1) RU94046044A (bg)
SI (1) SI9300270A (bg)
SK (1) SK137994A3 (bg)
WO (1) WO1993023419A1 (bg)
YU (1) YU34393A (bg)
ZA (1) ZA933496B (bg)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522540A (en) * 1982-04-09 1985-06-11 Nippon Kokan Kabushiki Kaisha Method and apparatus for removing cutting burr sticking to lower surface of slab
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
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
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
UA44257C2 (uk) * 1993-10-21 2002-02-15 Мерк Енд Ко, Інк 16-ЗАМІЩЕНІ ПОХІДНІ 4-АЗААНДРОСТАНУ, ЯК ІНГІБІТОРИ ІЗОФЕРМЕНТУ 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, СПОСІБ ІНГІБУВАННЯ 5-<font face="Symbol">a</font>-РЕДУКТАЗИ ТА ЇЇ ІЗОФЕРМЕНТУ, СПОСІБ ЛІКУВАННЯ, СПОСІБ ПРИПИНЕННЯ ТА ОБЕРНЕННЯ АНДРОГЕННОЇ АЛОПЕЦІЇ ТА СТИМУЛЮВАННЯ РОСТУ ВОЛОССЯ У ССАВЦІВ, СПОСІБ ІНГІБУВАННЯ БІОСИНТЕТИЧНОЇ КОНВЕРСІЇ ТЕСТОСТЕРОНУ В ДИГІДРОТЕСТОСТЕРОН У ССАВЦІВ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ
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
WO1998025622A1 (en) * 1996-12-09 1998-06-18 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
EP0983295A2 (en) * 1997-05-07 2000-03-08 Novopharm Ltd. 4-aza-steroids substituted in one or more of positions 7, 11 and 15 or with an unsaturated 14(15)-double bond as inhibitors of testosterone-5-alpha-reductase
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

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2227876A (en) * 1937-10-16 1941-01-07 Firm Of N V Organon Steroid derivatives with nuclear substituted nitrogen
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
US3264301A (en) * 1963-08-22 1966-08-02 Norman J Doorenbos Substituted-4-azasteroids
FR1465544A (fr) * 1965-11-29 1967-01-13 Roussel Uclaf Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation
CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
US4596812A (en) * 1976-05-24 1986-06-24 The Upjohn Company Methods and solutions for treating male pattern alopecia
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
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
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-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
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
EP0314199B1 (en) * 1984-02-27 1991-09-18 Merck & Co. Inc. 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
CA1331457C (en) * 1988-05-25 1994-08-16 Dennis Alan Holt Aromatic steroid 5-–-reductase inhibitors
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4970205A (en) * 1988-12-23 1990-11-13 Smithkline Beecham Corporation Sulfonic 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
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
GB9006023D0 (en) * 1990-03-16 1990-05-09 Smithkline Beecham Corp Synergistic compositions
EP0555309A1 (en) * 1990-10-31 1993-08-18 BEECHAM GROUP plc Topical composition with retinoid penetration enhancer
IL101245A0 (en) * 1991-03-20 1992-11-15 Merck & Co Inc Pharmaceutical compositions for the treatment of prostatic cancer
US5175155A (en) * 1991-10-07 1992-12-29 Sterling Winthrop Inc. Win 49596-finasteride method of use and compositions
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
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
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids

Also Published As

Publication number Publication date
AU658296B2 (en) 1995-04-06
RU94046044A (ru) 1996-10-10
HU9403311D0 (en) 1995-02-28
IL105717A0 (en) 1993-09-22
JPH07206759A (ja) 1995-08-08
SI9300270A (sl) 1993-12-31
FI945442A0 (fi) 1994-11-18
EP0572165A1 (en) 1993-12-01
HUT71484A (en) 1995-11-28
EP0572165B1 (en) 1997-09-17
CA2096576A1 (en) 1993-11-21
YU34393A (sh) 1996-10-09
SK137994A3 (en) 1995-04-12
FI945442L (fi) 1994-11-18
NO944406D0 (no) 1994-11-17
WO1993023419A1 (en) 1993-11-25
ZA933496B (en) 1993-12-22
CZ283894A3 (en) 1995-09-13
CN1085562A (zh) 1994-04-20
JPH07119232B2 (ja) 1995-12-20
MX9302931A (es) 1994-02-28
DE69313921T2 (de) 1998-04-09
FI945442A7 (fi) 1994-11-18
US5527807A (en) 1996-06-18
DE69313921D1 (de) 1997-10-23
JPH0656881A (ja) 1994-03-01
ATE158300T1 (de) 1997-10-15
NO944406L (no) 1995-01-19
AU3869793A (en) 1993-11-25

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