KR920701167A - 약제학적 활성 화합물 - Google Patents

약제학적 활성 화합물

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Publication number
KR920701167A
KR920701167A KR1019910700253A KR910700253A KR920701167A KR 920701167 A KR920701167 A KR 920701167A KR 1019910700253 A KR1019910700253 A KR 1019910700253A KR 910700253 A KR910700253 A KR 910700253A KR 920701167 A KR920701167 A KR 920701167A
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KR
South Korea
Prior art keywords
chloro
lower alkyl
alkanediyl
substituted
hydrochloride
Prior art date
Application number
KR1019910700253A
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English (en)
Inventor
엠.기리자발라브한 비요르
케이. 간글리 아쉬트
에이.핀토 패트릭
더블유.버세이스 리챠드
Original Assignee
에릭 에스. 딕커
쉐링 코포레이션
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Application filed by 에릭 에스. 딕커, 쉐링 코포레이션 filed Critical 에릭 에스. 딕커
Publication of KR920701167A publication Critical patent/KR920701167A/ko

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Abstract

내용 없음

Description

약제학적 활성 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 일반식(Ⅰ)및 (Ⅱ)의 화합물 및 이들의 약제학적으로 허용되는 산부가염, 염기 부가염 및 4급 아민염 및 이들의 약제학적으로 허용되는 용매 혼합물.
    상기 식에서, 각각의 Z는 독립적으로 3급 부틸, 페닐, 나프틸, 아다만틸, 치환된 페닐(여기에서, 치환제는 하나 이상의 할로겐, 저급 알콕시, 페녹시, 니트릴, 니트로, 페닐설포닐, 저급알킬설포닐, 옥사졸-2-일, 저급알카노일, 벤조일, 저급 알콕시카보닐, 저급알킬, 저급알칼티오, 페닐, 페닐아미노티오카보닐, 저급 알킬아미노티오카보닐, 하이드록사이미노저급알킬, 하이드록시저급알킬, 또는 카바모일이다), 또는 환에 적어도 하나의 질소를 함유하고 환의 나머지 성분이 적어도 하나의 탄소 및 임의로는 황 또는 산소인 4내지 6원의 비치환된 또는 치환된 헤테로사이클릭 환(여기에서, 치환체는 하나 이상의 카복실, 하이드록시메틸, 저급알킬, 저급알킬카보닐 또는 아릴저급알킬이다)이고, X및 Y는 각각 독립적으로 결합, -O-, -S-, -SO2-, 또는 -CH2-O-이며, 각각의 Q는 독립적으로 이가 치환되거나 비치환된, 직쇄 또는 측쇄 저급 알칸디일, 저급 알칸디일-사이클로알칸디일-저급 알칸디일, 저급 알칸디일, 저급 알칸디일, 페닐렌, 다하이드로푸란디일, 저급 알칸디일,-디하이드로푸란디일-저급 알칸디일, 테트라하이드로푸란디일, 테트라하이드로피란디일, 저급알칸디일-테트라하이드로피란디일-저급알칸디일 또는 저급알킨디일-테트라하이드로푸란디일-저급알칸디일(여기에서, 치환체는 하나 이상의 하이드록시, 케탈화된 인접 하이드록시, 에폭시, 불소, 염소, 아지드 또는 아미노이다)이며, W는 일가치환되거나 비치환된 아릴 그룹(여기에서, 아릴, 그룹상의 치환체는 Z(여기에서, Z는 치환된 페닐이다)에 대하여 정의한 바와 같거나, 환 원자중 적어도 하나의 헤테로원자가 질소원자이고 나머지 환 원자가 적어도 하나의 탄소 및 임의로는 황 또는 산소인 4내지 10개의 환원자를 함유하는 비치환되거나 치환된 헤테로사이클릭 단독 또는 융합된 환(여기에서, 헤테로사이클릭 환상의 치환체는 하나 이상의 하이드록시, 옥소, 아미노, 카바모일, 카복실, 니트릴, 니트로, 저급알킬, 저급알콕시카보닐, 할로겐, 설파밀, 저급알콕시카보닐, 저급알킬, 저급알킬티오, 저급알콕시, 하이드록시 저급알킬, 아미노 저급알킬, 카복시 저급알킬, 구아니디노, 티오우레이도, 저급알킬 설포닐아미노, 아미노카보닐저급알킬, 알릴옥시카보닐메틸 또는 카바모일저급알킬이다)이고 단, W는 치환되거나 비치환된 이속사졸릴일 수 없으며, 추가로 Z가 2-클로로-4-메톡시페닐이고, X가 -O-이며 Q가 C1-C7알칸디일이며 Y가 결합인 경우, W는 2,4및 5 위치에서 수소, 하이드록시저급알킬, 니트로, 저급알콕시카보닐, 저급알킬 및 아미노메틸렌으로 이루어진 그룹 중에서 독립적으로 선택된 1내지 3개의 치환체로 치환된 이미다졸릴이 아니며, W'는 이가 W이다.
  2. 제1항에 있어서, 하기식의 화합물 및 이의 약제학적으로 허용되는 산부가염.
    Z-W-Q-W
    상기 식에서, Q은 탄소수 5,6또는 7의 저급알칸디일, 탄소수 6,7 또는 8의 저급알킨디일, 메틸사이클로헥실메틸, 테트라하이드로푸란디일, 또는 (C1-C2)저급알칸디일-테트라하이드로푸란디일-(C1-C2)-저급알칸디일이며, 테트라하이드로푸란 환은 0내지 2개의 하이드록시 그룹으로 치환되며, W는 비치환되거나 치환된 이미다졸-1-일, 퓨린-9-일 이미다졸-2-일(여기에서, 치환체는 하나 이상의 저급알킬, 하이드록시저급알킬, 니트로, 저급알콕시카보닐, 카복시메틸, 아미노카보닐메틸이다)이며, X는 결합이거나, -S-,또는이며, Z은
    단, Z가 2-클로로-4-메톡시페닐이고 X기 -O-이며 Q가 C5-C7알칸디일이며 Y가 결합인 경우, W는 2,4 및 5위치에서 수소, 하이드록시-저급알킬, 니트로, 저급알콕시 카보닐 및 아미노 메틸렌으로 이루어진 그룹 중에서 독립적으로 선택된 1내지 3개의 치환체로 치환된 이미다졸릴이 아니다.
  3. 제1항에 있어서, 하기식의 화합물 및 이의 약제학적으로 허용되는 산부가염.
    상기 식에서, R1, R2및 R3는 각각 독립적으로 수소 또는 저급알킬이고, 단, R1R2및 R3중 적어도 하나는 저급 알킬이고, R2및 R3중 하나가 급 알킬인 경우, 나머니 하나는 수소이다.
  4. 제1항에 있어서, 하기식의 화합물, 이의 약제학적으로 허용되는 산부가염 또는 4급 아민염.
    Z-X-Q-Y-W
    상기 식에서, Z는 페닐, 치환된 페닐(여기에서, 치환체는 독립적으로 하나 이상의 할로겐, 저급 알킬티오, 저급 알킬설포닐, 저급 알콕시, 옥사졸-2-일, 페녹시이다), 이미다조-1-일, 저급 알킬 치환된 이미다조-1-일, 또는 3급-부틸이며, X는 결합이거나, -S-,또는-NH- 또는 -SO-이며, Qsms -OH에 의해 임의로 치환된 탄소수 5,6 또는 7의 저급 알칸디일, 탄소수 6 내지 8의 저급알킨디일, 메틸사이클로헥실메틸, 테트라하이드로푸란디일, 또는 (C1-C2)저급알칸디일-테트라하이드로푸란디일-(C1-C2)저급알칸디일이며, 테트라하이드로푸란 환은 0내지 2개의 하이드록시 그룹에 의하여 치환되며 Y는 결합이며, W는 이디다졸-1-일, 치환된 이미다졸-1-일(여기에서, 치환체는 독립적으로 하나 이상의 저급알킬, 하이드록시 저급알킬, 아미노저급알킬, 또는 저급알콕시카보닐이다), 이미다졸-2-일, 이미다졸-4-일, 이미다졸-5-일, 치환된 이미다졸-2-일, -4-일 또는 -5-일(여기에서, 치환체는 독립적으로 하나 이상의 저급 알킬 및 아릴옥시카보닐 메틸이다), 피롤리딘-1-일, 벤즈이미다졸-1-일, 1,4-디하이드로-4-옥소-7-메틸-1,8-3-카복실-나프티리딘-1-일, 퓨린-9-일, 피리딘-2-일, 피라졸-1-일, 또는 벤즈이미다졸-2-일 이며 단, Z가 2-클로로-4-메톡시페닐이고 X가 -O-이며 Q가 C5-C7알칼디일이며 Y가 결합인 경우, W는 2,4 및 5위치에서 수소, 하이드록시저급알킬, 니트로, 저급알콕시카보닐 및 아미노 메틸렌으로 이루어진 그룹 중에서 독립적으로 선택된 1내지 3개의 치환체로 치환된 이미다졸릴이 아니다.
  5. 제1항에 있어서, 하기식 화합물 및 이의 약제학적으로 허용되는 산부가염 또는 4급 아민염.
    Z-/X-Q-W
    상기 식에서, W는
    R4는 수소, 저급알킬 또는 하이드록시 저급알킬이고, R5는 저급알킬이며, R5및 R7은 독립적으로 하나 이상의 수소, 저급알킬, 아미노 저급알킬 또는 니트로이며, Z는
    X3는-S-, -O-,또는이며, Q는 -OH에 의하여 임의로 치환된 탄소수 5,6 또는 7의 저급알칸디일, 테트라하이드로푸란디일, 또는(C1-C2)저급알칸디일-테트라하이드로푸란디일-(C1-C2)-저급알칸디일(여기에서, 테트라하이드로푸란 환은 0내지 2개의 하이드록시 그룹으로 치환되며, 단, Z가 2-클로로-4-메톡시페닐이고, X가 -O-이며, Q가 C5-C7알칸디일이며, Y가 결합인 경우, W는 2,4 및 5위치에서 수소, 하이드록시저급알킬, 니트로, 저급알콕시 카보닐 및 아미노 메틸렌으로 이루어진 그룹중에서 독립적으로 선택된 1내지 3개의 치환체로 치환된 이미다졸릴이 아니다.
  6. 제1항에 있어서, 1-[7-(2-클로로4-메톡시페녹시)옥틸]이미다졸 하이드로클로라이드, N-(2-클로로-4-메틸페닐)-6-(1H-1-이미다졸릴)헥산 아미드 하이드로클로라이드, N-(2-클로로-4-메틸페닐)-N-메틸-6-(1-이미다졸릴)-1-헥산 아미드 하이드로클로라이드, N-(2-클로로4-메틸페닐)-N-메틸-6-(1-이미다졸릴)헥산 아미드 하이드로클로라이드, 1-[6-(3,5-디메톡시벤질옥시)헥실]이미아졸 하이드로클로라이드, 2(R)-[2-(2-클로로-4-메톡시페녹시)에틸]-3(R), 4(S)-디하이드록시-5(R)-(1-(1,2,4-트리아졸릴메틸)]-테트라하이드로푸란, 2(S)-[2-(2-클로로-4-메톡시페녹시)에틸]-3(R), 4(S)-디하이드록시-5(R)-(1-이미다졸릴메틸)]-2,5-디하이드루푸란하이드로클로라이드, 2(S)-[2-(2-클로로-4-메톡시페녹시)에틸]-3(R), 4(S)-디하이드록시-5(R)-2,4-디옥소-1,2,3,4-테트라하이드로피리미딘-1-일)메틸 테트라하이드로푸란, 2(S)-(2-클로로-4-메톡시페녹시)메틸]-3(R), 4(S)-디하이드록시-5(R)-[2-(2,4-디옥소-1,2,3,4-테트라하이드로피리미딘-1-일)에틸]테트라하이드로푸란, 5(S)-[2-(1-아미다졸릴)에틸]-3(R), 4(S)-디하이드록시-2(R)-(2-클로로-4-메톡시페녹시)메틸-테트라하이드로푸란 하이드로클로라이드, 2(S)-[2-(2-클로로-4-메톡시페녹시)에틸]-3(R), 4(S)-디하이드록시-5(R)-(2-클로로-4-메톡시페녹시)메틸 테트라하이드로푸란, 2(R)-[2-아데닌-7-일)에틸]-3(R), 4(S)-디하이드록시-5(R)-(2-클로로-4-메톡시페녹시)메틸 테트라하이드로푸란, 5(R)-[2-클로로-4-메톡시페녹시)메틸]-3(R), 4(S)-디하이드록시-2(R)-[2-(N-벤즈이다졸릴)에틸]-테트라하이드로푸란, 5(S)-[2-(1-이미다졸릴)에틸]-3(R), 4(S)-디하이드록시-2(R)-(2-클로로-4-메톡시페녹시)메틸-테트라하이드로푸란 하이드로클로라이드, 2(R)-[2-클로로-4-메톡시페녹시)메틸]-3(R), 4(S)-디하이드록시-5(R)-[2(N-벤즈이미다졸릴)에틸]-테트라하이드로푸란 하이드로클로라이드, (3 및 4)-하이드록시-5(S)-[2-(1-이미다졸릴)에틸]-2)(R)-(2-클로로-4-메톡시페녹시)메틸-테트라하이드로푸란 하이드로클로라이드, 5(S)-[2-(1-이미다졸릴)에틸]-2(R)-(2-클로로-4-메톡시페녹시)메틸-2,5-디하이드로푸란 하이드로클로라이드, 5(S)-[2-(1-이미다조릴)에틸]-2(R)-(2-클로로-4-메톡시페녹시)메틸-테트라하이드로푸란 하이드로클로라이드, 1-[6-(4-아세틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(4-(1-하이드록시에틸)페녹시헥실]이미다졸 하이드로클로라이드, 1-[6-(4-카바밀페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2,4-디클로로페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(4-클로로-3-메틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(4-클로로-5-메틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(4-클로로-4,5-디메틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(3,5-디메틸-4-클로로페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2,4-디플루오로페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2-메틸-4-클로로페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2,6-디메틸-4-클로로페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2-클로로-6-메틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2-브로모-4-메틸페녹시)헥실]이미다졸 하이드로클로라이드, 1-[6-(2,6-디클로로페녹시)헥실]이미다졸 하이드로클로라이드, 및 1-[6-(2-클로로-5-하이드록시페녹시)헥실]이미다졸로 이루어진 그룹 중에서 선택된 화합물.
  7. 횔성 성분으로서 제1항 내지 6항중 어느 한 항에 따른 화합물 및 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.
  8. 바이러스 감염이나 염증의 치료 또는 혈소판 활성화 인자의 억제에 사용하기 위한 약제를 제조하기 위한 제1항 내지 6항중 어느 한 항에 따른 화합물의 용도.
  9. 유효량의 제1항 내지 6항중 어느 한 항에 따른 화합물을 투여함을 특징으로 하여, 바이러스 감염 또는 염증을 치료하거나 혈소판 활성화 인자를 억제시키는 방법.
  10. 바이러스 감염 또는 염증을 치료하거나 혈소판 활성화 인자를 억제시키기 위한, 제1항 내지 6항중 어느 한 항에 따른 화합물의 용도.
  11. (A) 일반식(Ⅰ)의 화합물을 제조하기 위하여, 일반식 Z-X-Q'-L'[여기에서, Z 및 X는 제1항에서 정의한 바와 같고, Q'는 제1항에서 정의한 Q와 동일하거나, 단 일반식(Ⅰ)에서의 Q가 적도 하나의 그룹(여기에서, R은 각각 독립적으로 수소 또는 저급알킬이다)을 함유하는 경우 Q'는 또한 적어도 하나의 그룹이 빠진 제1항에서 정의한 Q와 동일할 수도 있으며, L'은 이탈 그룹이다]의 화합물을 일반식 L2-Y'W″[여기에서, L2는 이탈 그룹이고, W″는 제1항에서 W에 대하여 정의한 바와 같거나 이의 토토머이고, Y'는 제1항에서 정의한 Y와 동일하거나 단, 일반식(Ⅰ)에서의 Q가 적어도 하나의 그룹여기에서 R은 각각 독립적으로 수소 또는 저급알킬이다)를 함유하는 경우, Y'은 또한 적어도 하나의 그룹이 달린 제1항에서 정의한 Y와 동일할 수도 있다]의 화합물과 반응시키거나 (B) 일반식(Ⅱ)의 화합물을 제조하기 위하여, 적어도 하나의 일반식, Z-X-Q'L'(여기에서, Z, X, Q', L'은 전술한 바와 같다)의 화합물을 일반식 L3-Y1-W″′-Y'-L4(여기에서 L3및 L4는 이탈 그룹이고, 각각의 Y'는 독립적으로 전술한 바와 같고 W″′는 전술한 이가 W'이다)의 화합물과 반응시키거나, (C) Z및 W가 동일하고 X및 Y가 동일한, 일반식(Ⅰ)의 화합물을 제조하기 위하여, 일반식 L2-Y'-W″′(여기에서, Y'및 W″은 전술한 바와 같고, L2는 이탈 그룹이다)의 화합물을 일반식 L5-Q-L5(여기에서, L5및 L6는 이탈 그룹이고, Q″는 전술한 이가 Q이다)의 화합물과 반응시키며, 상기의 공정(a),(b)및 (c)에서 필요하다면, 특정의 반응성 그룹을 보호시키며 상기 공정을 수행한 후 필요하다면 (ⅰ) 특정의 보호 그룹을 제거시키거나, (ⅱ) 이와 같은 생성된 화합물을 일반식(Ⅰ)또는 일반식(Ⅱ)의 다른 화합물로 전환시키거나, (ⅲ) 하나 이상의 일반식(Ⅰ)또는 (Ⅱ)의 화합물이 생성될 경우, 생성된 화합물을 분리해 내거나 (ⅳ) 생성된 화합물을 이외 산부가염, 염기 부가염, 또는 4급 아민염 또는 약제학적으로 허용되는 용매화물로 전환시킴을 특징으로 하여, 제1항에 따른 일반식(Ⅰ)또는 (Ⅱ)의 화합물을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910700253A 1989-07-07 1990-07-06 약제학적 활성 화합물 KR920701167A (ko)

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EP0407217A1 (en) 1991-01-09
IE902465A1 (en) 1991-02-13
AU6062590A (en) 1991-02-06
WO1991000858A1 (en) 1991-01-24

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