KR910004653A - 스테로이드 5-α-환원효소의 억제제로서의 7-케토 또는 히드록시 3,5-디엔 스테로이드 - Google Patents

스테로이드 5-α-환원효소의 억제제로서의 7-케토 또는 히드록시 3,5-디엔 스테로이드 Download PDF

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KR910004653A
KR910004653A KR1019900013108A KR900013108A KR910004653A KR 910004653 A KR910004653 A KR 910004653A KR 1019900013108 A KR1019900013108 A KR 1019900013108A KR 900013108 A KR900013108 A KR 900013108A KR 910004653 A KR910004653 A KR 910004653A
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compound
salt
alkyl
diene
androstar
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KR1019900013108A
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월터 메트칼프 브리안
알란 홀트 데니스
알란 레비 마크
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원본미기재
스미스클라인 비참 코포레이션
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    • 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
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • 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
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

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  • Organic Chemistry (AREA)
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  • Reproductive Health (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Abstract

내용 없음.

Description

스테로이드 5-α-환원요소의 억제제로서의 7-케토 또는 히드록시 3,5-디엔 스테로이드
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 하기 식(I)로 표시되는 화합물 또는 약학적으로 허용되는 그의 염 :
  3. 상기식중, D고리는 점선으로 나타낸 바와같이 임의의 이중결합을 가지며, 단 R2가 2개의 치환체이거나 또는 2가 치환체인 경우에는 D고리는 C16-C17이중결합을 갖지않고; X는 (1) 케토, 또는 (2) 수소원자 및 히드록실기 이며; R1는 H 또는 C1-8알킬이고; 및 R2는 (1) α-수소, α-히드록실, 또는 α-아세톡시 및/또는로서, 식중 W는 단일결합 또는 C1-12알킬이고, 및 R3는 (I) C1-8알킬 (II) C1-8알콕시, (III) N(R4)2로서, 각각의 R4는 수소, C1-8알킬, C3-6시클로알킬, 페닐로부터 독립적으로 선택되거나; 또는 2개의 R4는 자신들이 결합되어 있는 질소와 함께 산소 및 질소로부터 선택된 1개 이하의 다른 헤테로원자를 포함하는 5-6원 포화고리를 나타내거나; (2) =CH-W-CO-R3또는 =CH-W-OR5로서, 식중 W 및 R3는 앞서 정의한 바와같고, 및 R5는 (I) 페닐 C1-6알킬카르보닐, (II) C5-10시클로알킬카르보닐, (III) 벤조일 (IV) C1-8알콕시카르보닐, (V) 아미노카르보닐, 또는 C1-8알킬치환된 아미노카르보닐, (VI) C1-8알킬, 또는 (VII) C1-20알킬카르보닐이거나; (3) α-수소 및 β-NHCOR6(식중, R6는 C1-C12알킬임) 또는 β-N(R4)2(식중, R4는 앞서 정의한 바와 같음)이거나; 또는 (4) 케토이다.
  4. 제1항에 있어서, R2가 α-수소 및, β-CON(R4)2(식중, 각각의 R4는 수소 및 C1-8알킬로부터 독립적으로 선택됨)인 화합물 또는 약학적으로 허용되는 그의 염.
  5. 제1항 또는 제2항에 있어서, 17β-(N-t-부틸 카르복스아미드)-7-옥소-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염인 화합물.
  6. 제1항 또는 제2항에 있어서, 17β-(N,N-디이소프로필카르복스아미드)-7β-히드록시-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염인 화합물.
  7. 제1항 또는 제2항에 있어서, 17β-(N,N-디이소프로필카르복스아미드)-7-옥소-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염인 화합물.
  8. 약제로서 사용하기 위한 제1항 내지 제5항중 어느 한 항에서 정의한 화합물.
  9. 제1항에서 정의한 화합물 및 적당한 약학적 담체를 함유하는 약학조성물.
  10. 제7항에 있어서, 화합물이 17β-(N,N-디이소프로필카르복스아미드)-7-옥소-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염, 17β-(N,N-디이소프로필카르복스아미드)-7,β-히드록시-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염, 또는 17β-(N-t-부틸카르복스아미드)-7-옥소-안드로스타-3,5-디엔-3-카르복실산 또는 그의 염인 조성물.
  11. 제1항에서 정의한 식(I)의 화합물 또는 약학적으로 허용되는 그의 염을 전립선 크기를 감소 또는 유지시키기 위한 약제의 제조에 사용하는것.
  12. 제1항에서 정의한 식(I)의 화합물 또는 약학적으로 허용되는 그의 염을 대머리 치료용 약제의 제조에 사용하는 것.
  13. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900013108A 1989-08-24 1990-08-24 스테로이드 5-α-환원효소의 억제제로서의 7-케토 또는 히드록시 3,5-디엔 스테로이드 KR910004653A (ko)

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US398,192 1989-08-24
US07/398,192 US5032586A (en) 1989-08-24 1989-08-24 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase

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US (1) US5032586A (ko)
EP (1) EP0414529B1 (ko)
JP (1) JPH03118326A (ko)
KR (1) KR910004653A (ko)
AT (1) ATE116657T1 (ko)
AU (1) AU640396B2 (ko)
CA (1) CA2023609A1 (ko)
DE (1) DE69015736T2 (ko)
DK (1) DK0414529T3 (ko)
ES (1) ES2066140T3 (ko)
GR (1) GR3015461T3 (ko)
IE (1) IE903070A1 (ko)
NZ (1) NZ235000A (ko)
PT (1) PT95090A (ko)
ZA (1) ZA906710B (ko)

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PT95090A (pt) 1991-04-18
NZ235000A (en) 1992-03-26
IE903070A1 (en) 1991-02-27
DE69015736T2 (de) 1995-05-11
CA2023609A1 (en) 1991-02-25
DK0414529T3 (da) 1995-05-22
EP0414529A2 (en) 1991-02-27
ES2066140T3 (es) 1995-03-01
ATE116657T1 (de) 1995-01-15
AU6115290A (en) 1991-02-28
EP0414529B1 (en) 1995-01-04
DE69015736D1 (de) 1995-02-16
US5032586A (en) 1991-07-16
ZA906710B (en) 1991-09-25
AU640396B2 (en) 1993-08-26
EP0414529A3 (en) 1991-07-24
JPH03118326A (ja) 1991-05-20
GR3015461T3 (en) 1995-06-30

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