HK1009047A1 - 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors - Google Patents

16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Info

Publication number
HK1009047A1
HK1009047A1 HK98109814A HK98109814A HK1009047A1 HK 1009047 A1 HK1009047 A1 HK 1009047A1 HK 98109814 A HK98109814 A HK 98109814A HK 98109814 A HK98109814 A HK 98109814A HK 1009047 A1 HK1009047 A1 HK 1009047A1
Authority
HK
Hong Kong
Prior art keywords
inhibitors
androstane
aza
reductase
alpha
Prior art date
Application number
HK98109814A
Other languages
English (en)
Inventor
Philippe L Durette
William K Hagmann
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 HK1009047A1 publication Critical patent/HK1009047A1/xx

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)
  • Veterinary Medicine (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)
HK98109814A 1993-10-21 1998-08-11 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors HK1009047A1 (en)

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 (1)

Publication Number Publication Date
HK1009047A1 true HK1009047A1 (en) 1999-05-21

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
HK98109814A HK1009047A1 (en) 1993-10-21 1998-08-11 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Country Status (29)

Country Link
US (4) US5739137A (ru)
EP (1) EP0724592B1 (ru)
JP (1) JP2862376B2 (ru)
KR (1) KR100363994B1 (ru)
CN (1) CN1058499C (ru)
AT (1) ATE175420T1 (ru)
BG (1) BG61978B1 (ru)
BR (2) BR9407866A (ru)
CA (1) CA2173863C (ru)
CY (1) CY2136B1 (ru)
CZ (1) CZ292614B6 (ru)
DE (1) DE69415824T2 (ru)
DK (1) DK0724592T3 (ru)
ES (1) ES2125495T3 (ru)
FI (1) FI961697A (ru)
HK (1) HK1009047A1 (ru)
HU (1) HUT74613A (ru)
IL (1) IL111357A (ru)
LV (2) LV11622B (ru)
NO (1) NO308037B1 (ru)
NZ (1) NZ275293A (ru)
PL (1) PL179611B1 (ru)
RO (1) RO116197B1 (ru)
RU (1) RU2142956C1 (ru)
SK (1) SK281645B6 (ru)
TW (1) TW413682B (ru)
UA (1) UA44257C2 (ru)
WO (1) WO1995011254A1 (ru)
ZA (1) ZA948285B (ru)

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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
WO1995011254A1 (en) * 1993-10-21 1995-04-27 Merck & Co., Inc. 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
AU694576B2 (en) * 1994-10-21 1998-07-23 Merck & Co., Inc. Combination method for acne treatment
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
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
JPH11513684A (ja) * 1995-10-19 1999-11-24 メルク エンド カンパニー インコーポレーテッド １６−置換−６−アザ−ステロイド５α−レダクターゼ阻害剤
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
EP1009740A1 (en) * 1997-03-17 2000-06-21 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
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
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.
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production 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
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
JP2008534505A (ja) 2005-03-25 2008-08-28 メルク エンド カムパニー インコーポレーテッド テストステロンサプリメントおよび５アルファ−レダクターゼインヒビターによる男性の治療方法
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
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI593411B (zh) 2013-04-30 2017-08-01 徐懷山 組合物於製備抑制雄性素受體有關之功能及治療雄性素 受體相關之疾病的藥物之用途

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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
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
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
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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.
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.
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
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EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY
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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
WO1995011254A1 (en) * 1993-10-21 1995-04-27 Merck & Co., Inc. 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
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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
PL179611B1 (pl) 2000-10-31
BG100516A (en) 1996-11-29
HUT74613A (en) 1997-01-28
FI961697A0 (fi) 1996-04-18
SK281645B6 (sk) 2001-06-11
US6204273B1 (en) 2001-03-20
IL111357A0 (en) 1994-12-29
LV12316B (en) 1999-11-20
EP0724592B1 (en) 1999-01-07
AU8086194A (en) 1995-05-08
DK0724592T3 (da) 1999-08-30
CN1058499C (zh) 2000-11-15
HU9601037D0 (en) 1996-06-28
LV11622A (lv) 1996-12-20
FI961697A (fi) 1996-04-18
ZA948285B (en) 1995-06-19
CA2173863C (en) 2003-05-13
CY2136B1 (en) 2002-06-21
ATE175420T1 (de) 1999-01-15
UA44257C2 (uk) 2002-02-15
NO961575L (no) 1996-04-19
US5910497A (en) 1999-06-08
KR960705839A (ko) 1996-11-08
PL314039A1 (en) 1996-08-05
NO308037B1 (no) 2000-07-10
CZ292614B6 (cs) 2003-11-12
ES2125495T3 (es) 1999-03-01
BR1100217A (pt) 1999-11-09
BR9407866A (pt) 1996-10-29
JP2862376B2 (ja) 1999-03-03
DE69415824T2 (de) 1999-08-05
NO961575D0 (no) 1996-04-19
EP0724592A1 (en) 1996-08-07
WO1995011254A1 (en) 1995-04-27
IL111357A (en) 2001-01-28
NZ275293A (en) 1998-02-26
SK49696A3 (en) 1996-10-02
TW413682B (en) 2000-12-01
AU680063B2 (en) 1997-07-17
JPH09511213A (ja) 1997-11-11
CN1136318A (zh) 1996-11-20
CA2173863A1 (en) 1995-04-27
KR100363994B1 (ko) 2003-04-10
LV11622B (en) 1997-06-20
RU2142956C1 (ru) 1999-12-20
RO116197B1 (ro) 2000-11-30
US5739137A (en) 1998-04-14
CZ122896A3 (en) 1997-01-15
US5719158A (en) 1998-02-17
DE69415824D1 (de) 1999-02-18
LV12316A (lv) 1999-07-20
BG61978B1 (bg) 1998-11-30

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Legal Events

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