KR880007478A - 약제학적 활성 화합물 - Google Patents

약제학적 활성 화합물 Download PDF

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KR880007478A
KR880007478A KR870014005A KR870014005A KR880007478A KR 880007478 A KR880007478 A KR 880007478A KR 870014005 A KR870014005 A KR 870014005A KR 870014005 A KR870014005 A KR 870014005A KR 880007478 A KR880007478 A KR 880007478A
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compound
formula
lower alkyl
substituted
group
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KR870014005A
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무필 지리야발라반 비요르
쿠마르 간굴리 애쉬트
안토니 핀토 패트릭
윌리암 베르사체 리챠드
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스테이너 브리.캔스타드
쉐링 코포레이션
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Publication of KR880007478A publication Critical patent/KR880007478A/ko

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Abstract

내용 없음.

Description

약제학적 활성 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(I) 및 (II)의 화합물, 및 이들의 약제학적으로 허용되는 산부가염, 염기부가염 및 4급 아민염, 및 이들의 약제학적으로 허용되는 용매화물.
    상기식에서 각각의 Z는 독립적으로 3급 부틸, 페닐, 나프틸 또는 아다만틸이거나, 치환된 페닐(여기에서, 치환체는 할로겐, 저급 알콕시, 페녹시, 니트릴, 니트로, 페닐설포닐, 저급알킬설포닐, 옥사졸-2-일, 저급 알카노일, 벤조일, 저급 알콕시카보닐, 저급 알킬, 저급 알킬티오, 페닐, 페닐아미노티오카보닐, 및 저급 알킬아미노티오카보닐 중의 하나 이상의 그룹이다)이거나, 또는 적어도 하나의 질소원자를 함유하며 환의 나머지 구성원으로서 적어도 하나의 탄소원자, 및 임의로 황 또는 산소를 함유하는 비치환되거나 치환된 4내지 6원 헤테로사이클릭 환(여기에서 치환체는 카복실, 하이드록시메틸, 저급 알킬, 저급 알킬카보닐 및 아릴저급알킬중의 하나이상의 그룹이다)이며, X 및 Y는 각각 독립적으로 결합을 나타내거나, 또는또는를 나타내고, 각각의 Q는 독립적으로 2가의 치환되거나 비치환된 직쇄 또는 측쇄 저급 알칸디일, 저급 알칸디일-사이클로 알칸디일-저급알칸디일, 저급 알켄디일, 저급 알킨디일, 페닐렌, 디하이드로푸란디일, 테트라하이드로푸란디일, 테트라하이드로피란디일 또는, 저급 알칸디일-테트라하드로 푸란디일-저급 알칸디일(여기에서 치환체는 하이드록시, 에폭시, 불소, 염소, 아지드 및 아미노중의 하나이상의 그룹이다)이고, W는 1가의 치환되거나 비치환된 아릴 그룹 또는 4 내지 10개의 환 원자를 함유하는 헤테로사이클릭 단일 또는 융합 환(환중의 적어도 하나의 헤테로 원자는 질소원자이고 나머지 환 원자는 적어도 하나의 탄소원자 및 임의로 황 또는 산소원자이다)[여기에서 치환체는 하이드록시, 옥소, 아미노, 카바모일, 카복실, 니트릴, 니트로, 저급알콕시카보닐, 할로겐, 설파밀, 저급 알킬, 저급 알킬티오, 저급 알콕시, 하이드록시저급 알킬, 저급 알콕시카보닐저급알킬, 아미노저급알킬, 카복시-저급알킬구아니디노, 티오우레이도, 저급 알킬설포닐아미노, 아미노카보닐저급알킬, 알릴옥시카보닐메틸 및 카바모일 옥시저급알킬중의 하나이상의 그룹이다]이나, 단 W는 치환되거나 비치환된 이속사졸릴일 수는 없으며, W′는 2가의 W이다.
  2. 제1항에 있어서, 하기 일반식(III)의 화합물 및 이의 약제학적으로 허용되는 산부가염.
    상기식에서 Q1은 탄소수 5,6 또는 7의 저급 알칸디일, 탄소수 6,7, 또는 8의 저급 알킨디일, 또는 메틸사이클로헥실메틸이며, , W1은 비치환되거나 치환된 이미다졸-1-일, 퓨린-9-일 또는 이미다졸-2-일(여기에서 치환체는 저급 알킬, 하이드록시저급알킬, 니트로, 저급 알콕시카보닐, 카복시메틸 및 아미노카보닐메틸중의 하나 이상의 그룹이다)이고, X1은 -O-,, 또는이며,
  3. 제1항에 있어서, 하기 일반식(IV)의 화합물 및 이의 약제학적을 허용되는 산부가염.
    상기식에서 R1, R2및 R3은 각각 독립적으로 수소, 하이드록시저급알킬 또는 저급 알킬이나, R2및 R3중의 하나가 저급알킬인 경우 다른 하나는 수소이다.
  4. 제1항에 있어서, 하기 일반식(V)의 화합물 및 이의 약제학적으로 허용되는 산부가염 또는 4급 아민염.
    상기식에서 각각의 Z2는 치환된 페닐(여기에서, 치환체는 할로겐, 저급 알킬티오, 저급 알킬 설포닐, 저급 알콕시, 옥사졸-2-일 및 페녹시중에서 독립적으로 선택된 하나이상의 그룹이다), 이미다조-1-일, 저급 알킬 치환된 이미다조-1-일, 또는 3급-부틸이고, X2는 결합을 나타내거나, 또는또는 -SO2-를 나타내며, Q2는 -OH에 의해 치환된 탄소수 6 또는 7의 저급 알칸디일, 탄소수 6 내지 8의 저급 알킨디일 또는 메틸사이클로헥실메틸이고, Y2는 결합을 나타내거나, 또는 -S- 또는 -SO2를 나타내며, W2는 이미다졸-1-일, 치환된 이미다졸-1-일(여기에서, 치환체는 저급 알킬 하이드록시 저급 알킬, 아미노저급알킬 및 저급알콕시카보닐중에서 독립적으로 선택된 하나이상의 그룹이다), 이미다졸-2-일, 이미다졸-4-일, 이미다졸-5-일, 치환된 이미다졸-2-일, -4-일 또는 -5-일(여기에서 치환체는 저급 알킬 및 알릴옥시카보닐메틸 중에서 독립적으로 선택된 하나이상의 그룹이다), 피롤리딘-1-일, 벤즈이미다졸-1-일, 1,4-디하이드로-4-옥소-7-메틸-1,8-3카복실-나프티리딘-1-일, 퓨린-9-일, 피리딘-2-일, 피라졸-1-일, 또는 벤즈이미다졸-2-일이다.
  5. 제1항에 있어서, 하기 일반식(VI)의 화합물 및 이의 약제학적으로 허용되는 산부가염 또는 4급 아민염.
    상기식에서
    R4는 수소, 저급 알킬 또는 하이드록시 저급 알킬이고, R5는 저급 알킬이며, R5및 R7은 독립적으로 하나이상의 수소, 저급알킬 아미노저급알킬 또는 니트로이며,
    X3은또는이고, Q3은 -OH에 의해 임의로 치환된 탄소수, 5,6 또는 7의 저급 알칸디일이다.
  6. 제1항에 있어서, 하기의 화합물들로 이루어진 그룹중에서 선택되는 화합물.
  7. 바이러스성감염 또는 염증을 치료하거나 또는 혈소판 활성인자를 억제하는데 유용한 약제학적 조성물을 제조하기 위한, 제1 내지 6항중 어느 한 항에서 정의된 일반식(I) 또는 (II)의 화합물을 용도.
  8. 제1 내지 6항중 어느 한 항에서 정의된 일반식(I) 또는 (II)의 화합물의 유효량을 투여함을 특징으로 하는 바이러스성 감염 또는 염증을 치료하거나 혈소판 활성 인자를 억제하는 방법.
  9. 제1 내지 6항중 어느 한 항에서 정의된 일반식(I) 또는 (II)의 구조를 가짐을 특징으로 하는 치료목적을 위한 화학적 화합물.
  10. 일반식(VII)의 화합물과 일반식(VIII)의 화합물을 반응시켜 일반식(I)의 화합물을 생성시키거나, 적어도 하나의 일반식(VII)의 화합물을 일반식(IX)의 화합물과 반응시켜 일반식(II)의 화합물 및 가능하게는 일반식(I)의 화합물을 생성시키거나, 또는 일반식(VII)의 화합물을 일반식(X)의 화합물과 반응시켜 Z와 W가 동일하고 X와 Y가 동일한 일반식(I)의 화합물로 생성시키고(상기 방법들에서, 반응성 그룹은 필요한 경우 보호시킨다), 이어서 필요한 경우, 보호 그룹을 제거하거나, 이렇게 하여 생성된 화합물을 일반식(I) 또는 (II)의 다른 화합물로 전환시키거나, 일반식(I) 또는 (II)의 화합물이 하나 이상 생성된 경우, 생성된 화합물을 분리시키거나, 또는 이렇게 하여 생성된 화합물을 이의 산부가염, 염기부가염 또는 4급 아민염 또는 약제학적으로 허용되는 용매화물로 전환시킴을 특징으로 하여, 제1항에서 정의된 일반식(I) 또는 (II)의 화합물을 제조하는 방법.
    상기식에서 Z 및 X는 제1항에서 정의된 바와 같고, Q′는 제1항에서 정의된 Q와 동일하거나, 또는 일반식(I)에서의 Q가 적어도 하나의 그룹(여기에서 각 R은 독립적으로 수소 또는 저급 알킬이다)을 함유해야하는 Q′는 제1항에서 정의된 것보다 그룹 -CH-이 적어도 하나 적은 Q와 동일할 수 있으며, L1, L2, L3, L5및 L6은 각각 이탈 그룹이고, W″는 제1항에서 W에 대해 정의된 것과 동일하거나 이의 토오토머이고, Y′는 제1항에서 정의된 Y와 동일하거나, 또는 일반식(I)에서의 Q가 적어도 하나의 그룹(여기에서 각 R은 독립적으로 수소 또는 저급 알킬이다)을 함유해야 하는 경우 Y′는 제1항에서 정의된 것보다 그룹이 적어도 하나 많은 Y와 동일할 수 있으며, W″′는 상기 정의된 바와 같은 2가의 W′이고, Q″는 상기 정의된 바와 같은 Q′이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870014005A 1986-12-10 1987-12-09 약제학적 활성 화합물 KR880007478A (ko)

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DE3751820D1 (de) 1996-06-27
DK645487A (da) 1988-06-11
EP0274867B1 (en) 1994-04-13
DE3789615D1 (de) 1994-05-19
IE873340L (en) 1988-06-10
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ATE138370T1 (de) 1996-06-15
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DE3751820T2 (de) 1996-09-26
AU620535B2 (en) 1992-02-20
DK645487D0 (da) 1987-12-09
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ZA879267B (en) 1988-08-31
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AU647222B2 (en) 1994-03-17
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