KR910004651A - 5α-환원효소 억제제로서의 17β-아실-4-아자-5α-안드로스트-1-엔-3-온 - Google Patents

5α-환원효소 억제제로서의 17β-아실-4-아자-5α-안드로스트-1-엔-3-온 Download PDF

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KR910004651A
KR910004651A KR1019900012779A KR900012779A KR910004651A KR 910004651 A KR910004651 A KR 910004651A KR 1019900012779 A KR1019900012779 A KR 1019900012779A KR 900012779 A KR900012779 A KR 900012779A KR 910004651 A KR910004651 A KR 910004651A
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South Korea
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androst
aza
methyl
compound
tolylcarbonyl
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KR1019900012779A
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에이치.라스무슨 게리
에프.레이놀즈 글렌
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제임스 에프.너턴
머크 앤드 캄파니, 인코포레이티드
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Publication of KR910004651A publication Critical patent/KR910004651A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/30—Unsaturated compounds
    • C07C62/38—Unsaturated compounds containing keto groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음.

Description

5α-환원효소 억제제로서의 17β-아실-4-아자-5α-안드로스트-1-엔-3-온
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 일반식(I)의 화합물
    상기식에서, R은 수소, 메틸 및 에틸 중에서 선택되며, R2는 하나 또는 그 이상의 탄소수 1 내지 2인 저급 알킬 치환체 및/또는 하나 또는 그 이상의 할로(C1, F 또는 Br) 치환체를 임의로 함유하는 모노사이클릭 아릴이고; R′, R″ 및 R″′ 는 각각 수소 및 메틸 중에서 선택된다.
  2. 제1항에 있어서, 하기 일반식(II)의 화합물.
    상기식에서, R은 수소, 메틸 및 에틸 이고, R3는 페닐, 1 또는 2개의 탄소수 1 내지 2인 저급 알킬 치환체에 의해 치환된 페닐 1 또는 2개의 할로(Cl, F 또는 Br) 치환체에 의해 치환된 페닐이다.
  3. 제2항에 있어서, R3가 페닐, 2-, 3- 또는 4-톨릴, 크실릴, 2-브로모 또는 24-클로로페닐, 2,6-디클로로 또는 2,6-디브로모페닐인 화합물.
  4. 제3항에 있어서, 17β-(페닐카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(2-톨릴카로닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(3-톨릴카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(4-톨릴카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(2-브로모페닐카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(2-클로로페닐카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(2,6-디클로로페닐카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(2,6-디브로모페닐카보닐)-4-아자-4-메틸-5α-안드로스트-1-엔-3-온; 17β-(크실릴카보닐)-4-아자-4-메틸-5-안드로스트-1-엔-3-온인 화합물.
  5. 제3항에 있어서, 17β-(페닐카보닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(2-톨릴카보닐)-4-아자5α-안드로스트-1-엔-3-온; 17β-(3-톨릴카보닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(4-톨릴카로닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(2-브로모페닐카로닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(2-클로로페닐카보닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(2,6-디클로로페닐카보닐)-4-아자-5α-안드로스트-1-엔-3-온; 17β-(2,6-디브로모페닐카보닐)-4-아자-4-5α-안드로스트-1-엔-3-온인 화합물.
  6. 제5항에 있어서, 17β-(페닐카보닐)-4-아자-5α-안드로스트-1-엔-3-온인 화합물.
  7. 치료학적 유효량의 제1항의 화합물을 좌창 심상, 지루, 여성조모증, 아드로겐성, 탈모증, 전립선 종양 및 양성 건립선 비대의 과안드로겐 상태의 치료를 필요로 하는 환자에 투여함을 특징으로 하여, 상기의 과안드로겐 상태를 치료하는 방법.
  8. 치료학적 유효량의 제1항의 화합물을 테스토스테론 5α-환원효소 억제치료를 필요로 하는 환자에 투여함을 특징으로 하여 상기의 테스토스테론 5α-환원효소 억제시키는 방법.
  9. 약제학적으로 허용되는 담체 및 유효량의 제1항의 화합물을 함유함을 특징으로 하는 테스토스테론 5α-환원 효소를 억제시키기 위한 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900012779A 1989-08-21 1990-08-20 5α-환원효소 억제제로서의 17β-아실-4-아자-5α-안드로스트-1-엔-3-온 KR910004651A (ko)

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Application Number Priority Date Filing Date Title
US07/396,184 US5049562A (en) 1984-02-27 1989-08-21 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
US07396.184 1989-08-21

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KR910004651A true KR910004651A (ko) 1991-03-29

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US (1) US5049562A (ko)
EP (1) EP0414491A3 (ko)
JP (1) JPH03163093A (ko)
KR (1) KR910004651A (ko)
AU (1) AU6116990A (ko)
CA (1) CA2023158A1 (ko)
FI (1) FI904101A0 (ko)
IE (1) IE903004A1 (ko)
IL (1) IL95351A0 (ko)
NO (1) NO903656L (ko)
NZ (1) NZ234874A (ko)
PT (1) PT95046A (ko)
ZA (1) ZA906579B (ko)

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ZA906579B (en) 1992-11-25
CA2023158A1 (en) 1991-02-22
NZ234874A (en) 1993-03-26
US5049562A (en) 1991-09-17
JPH03163093A (ja) 1991-07-15
AU6116990A (en) 1991-02-21
EP0414491A2 (en) 1991-02-27
NO903656D0 (no) 1990-08-20
FI904101A0 (fi) 1990-08-20
EP0414491A3 (en) 1992-08-26
IE903004A1 (en) 1991-02-27
PT95046A (pt) 1991-04-18
NO903656L (no) 1991-02-22
IL95351A0 (en) 1991-06-30

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