BG100516A - 16-заместени-4-аза-андростани като инхибитори наизозима 5 алфа-редуктаза 1 - Google Patents

16-заместени-4-аза-андростани като инхибитори наизозима 5 алфа-редуктаза 1

Info

Publication number
BG100516A
BG100516A BG100516A BG10051696A BG100516A BG 100516 A BG100516 A BG 100516A BG 100516 A BG100516 A BG 100516A BG 10051696 A BG10051696 A BG 10051696A BG 100516 A BG100516 A BG 100516A
Authority
BG
Bulgaria
Prior art keywords
reductase
inhibitors
androstanes
aza
initiative
Prior art date
Application number
BG100516A
Other languages
English (en)
Other versions
BG61978B1 (bg
Inventor
Philippe Durette
William Hagmann
Jun. Thomas Lanza
Soumya Sahoo
Gary Rasmusson
Richard Tolman
Langen Derek Von
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/bg
Publication of BG61978B1 publication Critical patent/BG61978B1/bg

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)
  • 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)

Abstract

Изобретението се отнася до съединения с формула, които са инхибитори на изозима 5 -редуктаза 1. Самостоятелно или в комбинация с инхибитор на 5 -редуктаза 2 те са полезни за лечение на андрогенни чувствителни заболявания като акне вулгарис, себорея, женски хирзутизъм, мъжки тип плешивост и доброкачествена хиперплазия на простатата.
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 (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Publications (2)

Publication Number Publication Date
BG100516A true BG100516A (bg) 1996-11-29
BG61978B1 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 (28)

Country Link
US (4) US5739137A (bg)
EP (1) EP0724592B1 (bg)
JP (1) JP2862376B2 (bg)
KR (1) KR100363994B1 (bg)
CN (1) CN1058499C (bg)
AT (1) ATE175420T1 (bg)
BG (1) BG61978B1 (bg)
BR (2) BR9407866A (bg)
CA (1) CA2173863C (bg)
CY (1) CY2136B1 (bg)
CZ (1) CZ292614B6 (bg)
DE (1) DE69415824T2 (bg)
DK (1) DK0724592T3 (bg)
ES (1) ES2125495T3 (bg)
FI (1) FI961697A7 (bg)
HU (1) HUT74613A (bg)
IL (1) IL111357A (bg)
LV (2) LV11622B (bg)
NO (1) NO308037B1 (bg)
NZ (1) NZ275293A (bg)
PL (1) PL179611B1 (bg)
RO (1) RO116197B1 (bg)
RU (1) RU2142956C1 (bg)
SK (1) SK281645B6 (bg)
TW (1) TW413682B (bg)
UA (1) UA44257C2 (bg)
WO (1) WO1995011254A1 (bg)
ZA (1) ZA948285B (bg)

Families Citing this family (29)

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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
HUT74613A (en) 1993-10-21 1997-01-28 Merck & Co Inc 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same
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
JPH10508586A (ja) * 1994-10-21 1998-08-25 メルク エンド カンパニー インコーポレーテッド 組み合わせ式アクネ治療方法
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
CA2283098A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
WO1999021563A1 (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
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
US6048869A (en) * 1998-07-29 2000-04-11 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
WO2002054996A2 (en) * 2000-10-23 2002-07-18 Euro Celtique Sa Terazosin transdermal device and methods
UA80094C2 (en) * 2001-05-15 2007-08-27 Taisho Pharmaceutical Co Ltd Minoxidil-containing liquid composition and use of arginine for preventing from suffering the thermal coloration
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
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
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
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
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
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]
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
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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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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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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
HUT74613A (en) * 1993-10-21 1997-01-28 Merck & Co Inc 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same
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
CY2136B1 (en) 2002-06-21
LV12316A (lv) 1999-07-20
BR1100217A (pt) 1999-11-09
CN1136318A (zh) 1996-11-20
FI961697A0 (fi) 1996-04-18
CZ292614B6 (cs) 2003-11-12
SK49696A3 (en) 1996-10-02
PL314039A1 (en) 1996-08-05
US6204273B1 (en) 2001-03-20
LV12316B (en) 1999-11-20
LV11622A (lv) 1996-12-20
US5739137A (en) 1998-04-14
LV11622B (en) 1997-06-20
US5719158A (en) 1998-02-17
NO308037B1 (no) 2000-07-10
EP0724592A1 (en) 1996-08-07
DE69415824T2 (de) 1999-08-05
FI961697L (fi) 1996-04-18
AU680063B2 (en) 1997-07-17
CN1058499C (zh) 2000-11-15
CZ122896A3 (en) 1997-01-15
FI961697A7 (fi) 1996-04-18
HK1009047A1 (en) 1999-05-21
ZA948285B (en) 1995-06-19
JP2862376B2 (ja) 1999-03-03
JPH09511213A (ja) 1997-11-11
KR100363994B1 (ko) 2003-04-10
US5910497A (en) 1999-06-08
CA2173863A1 (en) 1995-04-27
BG61978B1 (bg) 1998-11-30
SK281645B6 (sk) 2001-06-11
DE69415824D1 (de) 1999-02-18
IL111357A (en) 2001-01-28
HUT74613A (en) 1997-01-28
NZ275293A (en) 1998-02-26
EP0724592B1 (en) 1999-01-07
UA44257C2 (uk) 2002-02-15
ES2125495T3 (es) 1999-03-01
RO116197B1 (ro) 2000-11-30
CA2173863C (en) 2003-05-13
HU9601037D0 (en) 1996-06-28
PL179611B1 (pl) 2000-10-31
DK0724592T3 (da) 1999-08-30
TW413682B (en) 2000-12-01
NO961575L (no) 1996-04-19
RU2142956C1 (ru) 1999-12-20
NO961575D0 (no) 1996-04-19
ATE175420T1 (de) 1999-01-15
AU8086194A (en) 1995-05-08
BR9407866A (pt) 1996-10-29
IL111357A0 (en) 1994-12-29
WO1995011254A1 (en) 1995-04-27
KR960705839A (ko) 1996-11-08

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