KR950003276A - 당단백질 IIb/IIIa 길항물질 - Google Patents

당단백질 IIb/IIIa 길항물질 Download PDF

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KR950003276A
KR950003276A KR1019940017557A KR19940017557A KR950003276A KR 950003276 A KR950003276 A KR 950003276A KR 1019940017557 A KR1019940017557 A KR 1019940017557A KR 19940017557 A KR19940017557 A KR 19940017557A KR 950003276 A KR950003276 A KR 950003276A
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carbon
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nitrogen
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조셉 피셔 매튜
마리 해프 앤
앤토니 자쿠보브스키 조셉
딘 키닉 마이클
데일 클라인 알렌
Ii세 존 마이클 모린
존 살 다니엘
앨런 스켈톤 마샬
테오도르 바실레프 로버트
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피터 지.스트링거
일라이 릴리 앤드 캄파니
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Abstract

본 발명은 염기성 작용기 및 산성 작용기 모두로 치환된 2개으 융합된 6원 고리로 형성된 핵, 예를들어 이소퀴놀린, 이소퀴놀론, 테트라하이드로나프탈렌, 디하이드로나프탈렌 또는 테트랄론을 갖는 몇몇 이환 화합물에 관한 것이며, 이는 혈소판 응집의 억제에 유용하다.

Description

당단백질 IIb/IIIa 길항물질
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 2개의 융합된 6원 고리 A 및 B로 형성된 핵을 갖는 하기 일반식(Ⅰ)의 이환 화합물, 및 그의 약학적으로 허용가능한 염, 용매화물 및 전구약물 유도체;
    상기식에서, B1, B2, B3및 B4는 독립적으로 탄소, 산소, 황 및 질소중에서 선택되나, 단, B1, B2, B3및 B4중 적어도 2개는 탄소이고; R3는 산성 그룹이고; n은 2 내지 6이고; R0는 동일하거나 상이하며, 독립적으로 수소, 알킬, 할로 치환된 알킬, 알케닐, 알키닐, 사이클로알킬, 아릴, 아릴알킬, 하이드록시, 알콕시, 아릴알콕시, 아미노, 치환된 아미노, 카바밀, 카복시, 아실, 시아노, 할로, 니트로, 설포, =O 및 =S중에서 선택되나; 단, R0가 =0 또는 =S인 경우, B1, B2, B3및 B4중의 하나만이 질소일 수 있고; A1, A2, A3및 A4는 독립적으로 탄소, 산소, 황 및 질소중에서 선택되나, 단,A1, A2, A3및 A4중 적어도 2개는 탄소이고; m은 2 내지 6이고; R10는 동일하거나 상이하며, 독립적으로 수소, 알킬, 할로치환된 알킬, 알케닐, 알키닐, 사이클로알킬, 아릴, 아릴알킬, 하이드록시, 알콕시, 아릴알콕시, 카복시, 아실, 시아노, 할로, 니트로, 설포, =O 및 =S중에서 선택되나; 단, 하나의 R10만이 =O 또는 =S일 수 있고; 연결 그룹 -(L)-은 결합, 또는 탄소, 질소, 황 및 산소로 이루어진 그룹중에서 선택된 하나 내지 10개의 원자를 갖는 2가의 치환되거나 비치환된 쇄이고; Q는 염기성 라디칼을 포함하는 유기 그룹이다.
  2. 제1항에 있어서, (A) 상기 고리 A 및 B의 이환 핵이 하기 구조식(a) 내지 (r)로 이루어진 그룹중에서 선택되고;
    (B) R3가 하기 구조식으로 이루어진 그룹중에서 선택되고;
    (C) Q가 아미노, 이미노, 아미디노, 아미노메틸렌아미노, 이미노메틸아미노, 구아니디노, 아미노구아니디노, 알킬아미노, 디알킬아미노, 트리알킬아미노, 알킬리덴아미노, 피라닐, 피롤릴, 이미다졸릴, 피라졸릴, 피리딜, 피라지닐, 피리미디닐, 피리다지닐, 인돌리지닐, 이소인돌릴, 3H-인돌릴, 인돌릴, 1H-인다졸릴, 퓨리닐, 4H-퀴놀리지닐, 이소퀴놀릴, 퀴놀릴, 프탈라지닐, 나프티리디닐, 퀴녹살리닐, 퀴나졸리닐, 신놀리닐, 프테리디닐, 4aH-카보졸릴, 카보졸릴, 베타-카볼리닐, 페난트리디닐, 아크리디닐, 피리미디닐, 페난트롤리닐, 페나지닐, 페나르스아지닐, 페노티아지닐, 피롤리닐, 이미다졸리디닐, 이미다졸리닐, 피라졸리디닐, 피라졸리닐, 피레리딜, 피페라지닐, 인돌리닐, 이소인돌리닐, 퀴누클리디닐, 모르폴리닐, 및 아미노, 이미노, 아미디노, 아미노메틸렌아미노, 이미노메틸아미노, 구아니디노, 알킬아미노, 디알킬아미노, 트리알킬아미노 또는 알킬리덴아미노 그룹으로 치환된 선행그룹들중 임의의 그룹으로 이루어진 그룹중에서 선택된 염기성 라디칼을 함유하고; (D) 연결 그룹 -(L)-이 하기 구조식으로 나타낸 그룹;
    -C≡C-, -CH=CH-, -CH2-CH2-,, -C-O-, 중에서 선택되는 화합물.
  3. 2개의 융합된 6원 고리 A 및 B로 형성된 핵을 갖는 하기 일반식(Ⅱ)의 이환 화합물, 및 그의 약학적으로 허용가능한 염, 용매화물 및 전구약물 유도체;
    상기식에서, B1, B2, B3및 B4는 독립적으로 탄소, 산소, 황 및 질소중에서 선택되나, 단, B1, B2, B3및 B4중 적어도 2개는 탄소이고; R3는 산성 그룹이고; n은 2 내지 6이고; R0는 동일하거나 상이하며, 독립적으로 수소, 알킬, 할로 치환된 알킬, 알케닐, 알키닐, 사이클로알킬, 아릴, 아릴알킬, 하이드록시, 알콕시, 아릴알콕시, 아미노, 치환된 아미노, 카바밀, 카복시, 아실, 시아노, 할로, 니트로, 설포, =O 및 =S중에서 선택되나; 단, R0가 =0 또는 =S인 경우, B1, B2, B3및 B4중의 하나만이 질소일 수 있고; A1, A2, A3및 A4는 독립적으로 탄소, 산소, 황 및 질소중에서 선택되나, 단,A1, A2, A3및 A4중 적어도 2개는 탄소이고; m은 2 내지 6이고; R10는 동일하거나 상이하며, 독립적으로 수소, 알킬, 할로치환된 알킬, 알케닐, 알키닐, 사이클로알킬, 아릴, 아릴알킬, 하이드록시, 알콕시, 아릴알콕시, 카복시, 아실, 시아노, 할로, 니트로, 설포, =O 및 =S중에서 선택되나; 단, 하나의 R10만이 =O 또는 =S일 수 있고; 연결 그룹 -(L)-은 결합, 또는 탄소, 질소, 황 및 산소로 이루어진 그룹중에서 선택된 하나 내지 10개의 원자를 갖는 2가의 치환되거나 비치환된 쇄이고; D는 D1, D2, D3, D4, D5및 D6원자가 독립적으로 탄소, 질소, 산소 및 황중에서 선택되나; 단, D1, D2, D3, D4, D5및 D6중의 적어도 2개는 탄소인 6원 고리이고; Q1는 염기성 그룹이고; w는 1 내지 3의 정수이고; R20은 동일하거나 상이하며, 독립적으로 수소, 알킬, 할로치환된 알킬, 알케닐, 알키닐, 사이클로알킬, 아릴, 아릴알킬, 하이드록시, 알콕시, 아릴알콕시, 아미노, 치환된 아미노, 카바밀, 카복시, 아실, 시아노, 할로, 니트로 및 설포중에서 선택되고 p는 0 내지 8의 정수이다.
  4. 활성 성분으로서 제1,2 또는 3항에 청구된 일반식(Ⅰ) 또는 (Ⅱ)의 화합물 또는 그의 약학적으로 허용 가능한 염, 용매화물 또는 전구약물 유도체와 함께, 하나이상의 이들의 약학적으로 허용가능한 담체를 포함하는 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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