BG61978B1 - 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 - Google Patents

16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 Download PDF

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Publication number
BG61978B1
BG61978B1 BG100516A BG10051696A BG61978B1 BG 61978 B1 BG61978 B1 BG 61978B1 BG 100516 A BG100516 A BG 100516A BG 10051696 A BG10051696 A BG 10051696A BG 61978 B1 BG61978 B1 BG 61978B1
Authority
BG
Bulgaria
Prior art keywords
aza
oxo
dimethyl
androstane
methyl
Prior art date
Application number
BG100516A
Other languages
Bulgarian (bg)
English (en)
Other versions
BG100516A (en
Inventor
Philippe L. Durette
William K. Hagmann
Thomas J. Lanza Jun.
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 BG100516A publication Critical patent/BG100516A/xx
Publication of BG61978B1 publication Critical patent/BG61978B1/bg

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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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
BG100516A 1993-10-21 1996-04-18 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 BG61978B1 (bg)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21
PCT/US1994/012071 WO1995011254A1 (fr) 1993-10-21 1994-10-21 INHIBITEURS DE L'ISOZYME 5α-REDUCTASE 1 DE 4-AZA-ANDROSTANE-5 A SUBSTITUTION EN POSITION 16

Publications (2)

Publication Number Publication Date
BG100516A BG100516A (en) 1996-11-29
BG61978B1 true BG61978B1 (bg) 1998-11-30

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
BG100516A BG61978B1 (bg) 1993-10-21 1996-04-18 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1

Country Status (29)

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

Families Citing this family (27)

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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
SK281645B6 (sk) * 1993-10-21 2001-06-11 Merck & Co., Inc. 16-substituované-4-azaandrostanové deriváty, farmaceutické prostriedky s ich obsahom a ich použitie
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
WO1996012487A1 (fr) * 1994-10-21 1996-05-02 Merck & Co., Inc. Procede combine de traitement de l'acne
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
EP0862436A1 (fr) * 1995-10-19 1998-09-09 Merck & Co., Inc. Inhibiteurs de 5-alpha-reductase a 6-aza-steroides a substitution en position 16
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 (fr) * 1997-03-17 2000-06-21 Merck & Co., Inc. Methodes et compositions de traitement de la polykystose ovarienne
US5942519A (en) * 1997-10-28 1999-08-24 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 (fr) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7β-METHYL-16β-((4-METHYLSULFONYL)-PHENOXY)-4-AZA-5α-ANDROST-1-EN-3-ONE UTILISEE COMME INHIBITEUR D'ISO-ENZYME 5α-REDUCTASE 1
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
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
CA2338298A1 (fr) * 1998-07-29 2000-02-10 Merck & Co., Inc. Composes tricycliques
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
WO2002054996A2 (fr) * 2000-10-23 2002-07-18 Euro Celtique Sa Dispositif transdermique de la terazosine et procedes associes
WO2005097127A2 (fr) * 2004-04-02 2005-10-20 Merck & Co., Inc. Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
CN101146535A (zh) 2005-03-25 2008-03-19 默克公司 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法
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
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
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
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
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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
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EP0285382B1 (fr) * 1987-04-03 1994-04-13 Merck & Co. Inc. Traitement d'alopécia androgénique avec 17-bêta-n-monosubstitué-carbamoyl-4-aza-5-alpha-androst-1-en-3-ones
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.
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AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
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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
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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
SK281645B6 (sk) * 1993-10-21 2001-06-11 Merck & Co., Inc. 16-substituované-4-azaandrostanové deriváty, farmaceutické prostriedky s ich obsahom a ich použitie
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
RO116197B1 (ro) 2000-11-30
CZ292614B6 (cs) 2003-11-12
KR960705839A (ko) 1996-11-08
US5739137A (en) 1998-04-14
CA2173863C (fr) 2003-05-13
NZ275293A (en) 1998-02-26
IL111357A0 (en) 1994-12-29
WO1995011254A1 (fr) 1995-04-27
NO961575D0 (no) 1996-04-19
BR1100217A (pt) 1999-11-09
AU8086194A (en) 1995-05-08
NO961575L (no) 1996-04-19
AU680063B2 (en) 1997-07-17
HUT74613A (en) 1997-01-28
FI961697A0 (fi) 1996-04-18
US5910497A (en) 1999-06-08
UA44257C2 (uk) 2002-02-15
US5719158A (en) 1998-02-17
HK1009047A1 (en) 1999-05-21
JP2862376B2 (ja) 1999-03-03
EP0724592B1 (fr) 1999-01-07
DE69415824T2 (de) 1999-08-05
LV11622B (en) 1997-06-20
US6204273B1 (en) 2001-03-20
TW413682B (en) 2000-12-01
RU2142956C1 (ru) 1999-12-20
CA2173863A1 (fr) 1995-04-27
HU9601037D0 (en) 1996-06-28
PL314039A1 (en) 1996-08-05
LV12316B (en) 1999-11-20
SK49696A3 (en) 1996-10-02
BG100516A (en) 1996-11-29
LV11622A (lv) 1996-12-20
CY2136B1 (en) 2002-06-21
ZA948285B (en) 1995-06-19
ATE175420T1 (de) 1999-01-15
BR9407866A (pt) 1996-10-29
KR100363994B1 (ko) 2003-04-10
NO308037B1 (no) 2000-07-10
JPH09511213A (ja) 1997-11-11
EP0724592A1 (fr) 1996-08-07
FI961697A (fi) 1996-04-18
DK0724592T3 (da) 1999-08-30
PL179611B1 (pl) 2000-10-31
CZ122896A3 (en) 1997-01-15
SK281645B6 (sk) 2001-06-11
ES2125495T3 (es) 1999-03-01
DE69415824D1 (de) 1999-02-18
CN1058499C (zh) 2000-11-15
IL111357A (en) 2001-01-28
CN1136318A (zh) 1996-11-20
LV12316A (lv) 1999-07-20

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