NO961575L - 16-substituerte-4-aza-androstan 5-reduktase-isoenzym 1-inhibitorer - Google Patents

16-substituerte-4-aza-androstan 5-reduktase-isoenzym 1-inhibitorer

Info

Publication number
NO961575L
NO961575L NO961575A NO961575A NO961575L NO 961575 L NO961575 L NO 961575L NO 961575 A NO961575 A NO 961575A NO 961575 A NO961575 A NO 961575A NO 961575 L NO961575 L NO 961575L
Authority
NO
Norway
Prior art keywords
inhibitors
reductase
androstan
aza
substituted
Prior art date
Application number
NO961575A
Other languages
English (en)
Other versions
NO308037B1 (no
NO961575D0 (no
Inventor
Philippe L Durette
William K Hagmann
Jr Thomas J Lanza
Soumya P Sahoo
Gary H Rasmusson
Richard L Tolman
Derek Von Langen
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 NO961575L publication Critical patent/NO961575L/no
Publication of NO961575D0 publication Critical patent/NO961575D0/no
Publication of NO308037B1 publication Critical patent/NO308037B1/no

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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • A61P5/28—Antiandrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
NO961575A 1993-10-21 1996-04-19 16-substituerte-4-aza-androstan 5<alfa>-reduktase-isoenzym 1- inhibitorer og farmasøytisk preparat NO308037B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21
PCT/US1994/012071 WO1995011254A1 (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Publications (3)

Publication Number Publication Date
NO961575L true NO961575L (no) 1996-04-19
NO961575D0 NO961575D0 (no) 1996-04-19
NO308037B1 NO308037B1 (no) 2000-07-10

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
NO961575A NO308037B1 (no) 1993-10-21 1996-04-19 16-substituerte-4-aza-androstan 5<alfa>-reduktase-isoenzym 1- inhibitorer og farmasøytisk preparat

Country Status (28)

Country Link
US (4) US5739137A (no)
EP (1) EP0724592B1 (no)
JP (1) JP2862376B2 (no)
KR (1) KR100363994B1 (no)
CN (1) CN1058499C (no)
AT (1) ATE175420T1 (no)
BG (1) BG61978B1 (no)
BR (2) BR9407866A (no)
CA (1) CA2173863C (no)
CY (1) CY2136B1 (no)
CZ (1) CZ292614B6 (no)
DE (1) DE69415824T2 (no)
DK (1) DK0724592T3 (no)
ES (1) ES2125495T3 (no)
FI (1) FI961697A0 (no)
HU (1) HUT74613A (no)
IL (1) IL111357A (no)
LV (2) LV11622B (no)
NO (1) NO308037B1 (no)
NZ (1) NZ275293A (no)
PL (1) PL179611B1 (no)
RO (1) RO116197B1 (no)
RU (1) RU2142956C1 (no)
SK (1) SK281645B6 (no)
TW (1) TW413682B (no)
UA (1) UA44257C2 (no)
WO (1) WO1995011254A1 (no)
ZA (1) ZA948285B (no)

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US5547957A (en) 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
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
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
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
EP0786999A4 (en) * 1994-10-21 1999-01-20 Merck & Co Inc Combination method for acne treatment
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
WO1997014418A1 (en) * 1995-10-19 1997-04-24 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
WO1998041509A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
CA2308070A1 (en) * 1997-10-28 1999-05-06 Merck & Co., Inc. Prevention of precipitated acute urinary retention
US6187925B1 (en) 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
WO1999058550A1 (en) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7beta-methyl-16beta-((4-methylsulfonyl)-phenoxy)-4-aza-5alpha-androst-1-en-3-one as a 5-alpha-reductase isozyme 1 inhibitor
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
AU754604B2 (en) * 1998-07-29 2002-11-21 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
JP4189223B2 (ja) * 2001-05-15 2008-12-03 大正製薬株式会社 ミノキシジル配合液剤組成物
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
AU2006229840B2 (en) * 2005-03-25 2010-12-23 Merck Sharp & Dohme Corp. Method of treating men with testosterone supplement and 5alpha-reductase inhibitor
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (fr) * 2006-12-13 2009-01-30 Sanofi Aventis Sa Nouveau procede pour l'obtention diastereoselective d'une amine primaire chirale sur un steroide
RU2364402C1 (ru) * 2008-04-28 2009-08-20 Государственное образовательное учреждение высшего профессионального образования Московская медицинская академия им. И.М. Сеченова Федерального агентства по здравоохранению и социальному развитию (ГОУВПО ММА им. И.М. Сеченова Росздрава) Способ лечения больных хроническим простатитом
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI522102B (zh) 2013-04-30 2016-02-21 長庚醫療財團法人 組合物於製備治療或預防性治療痤瘡的藥物之用途

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US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
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
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 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
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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
DE3888994T2 (de) * 1987-04-03 1994-11-03 Merck & Co Inc Behandlung von androgener Alopecia mit 17-beta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen.
DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
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CA2135167A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-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
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
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
US5380728A (en) * 1993-02-10 1995-01-10 Merck & Co., Inc. Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a
US5407944A (en) * 1993-02-19 1995-04-18 Goldman; Boris E. Compositions and methods for promoting hair growth
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
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
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
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
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

Also Published As

Publication number Publication date
WO1995011254A1 (en) 1995-04-27
RO116197B1 (ro) 2000-11-30
CN1058499C (zh) 2000-11-15
CZ292614B6 (cs) 2003-11-12
CA2173863A1 (en) 1995-04-27
LV11622A (lv) 1996-12-20
BG100516A (bg) 1996-11-29
DK0724592T3 (da) 1999-08-30
UA44257C2 (uk) 2002-02-15
FI961697L (fi) 1996-04-18
NO308037B1 (no) 2000-07-10
ZA948285B (en) 1995-06-19
KR960705839A (ko) 1996-11-08
ES2125495T3 (es) 1999-03-01
US5910497A (en) 1999-06-08
US5719158A (en) 1998-02-17
HK1009047A1 (en) 1999-05-21
EP0724592B1 (en) 1999-01-07
LV12316A (lv) 1999-07-20
TW413682B (en) 2000-12-01
RU2142956C1 (ru) 1999-12-20
HU9601037D0 (en) 1996-06-28
SK281645B6 (sk) 2001-06-11
AU680063B2 (en) 1997-07-17
SK49696A3 (en) 1996-10-02
FI961697A7 (fi) 1996-04-18
CA2173863C (en) 2003-05-13
CZ122896A3 (en) 1997-01-15
CN1136318A (zh) 1996-11-20
US5739137A (en) 1998-04-14
US6204273B1 (en) 2001-03-20
BR1100217A (pt) 1999-11-09
JPH09511213A (ja) 1997-11-11
KR100363994B1 (ko) 2003-04-10
EP0724592A1 (en) 1996-08-07
DE69415824D1 (de) 1999-02-18
IL111357A (en) 2001-01-28
HUT74613A (en) 1997-01-28
LV12316B (en) 1999-11-20
DE69415824T2 (de) 1999-08-05
PL314039A1 (en) 1996-08-05
ATE175420T1 (de) 1999-01-15
IL111357A0 (en) 1994-12-29
LV11622B (en) 1997-06-20
JP2862376B2 (ja) 1999-03-03
NZ275293A (en) 1998-02-26
PL179611B1 (pl) 2000-10-31
AU8086194A (en) 1995-05-08
NO961575D0 (no) 1996-04-19
FI961697A0 (fi) 1996-04-18
CY2136B1 (en) 2002-06-21
BG61978B1 (bg) 1998-11-30
BR9407866A (pt) 1996-10-29

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