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1. 发明公开

KR1020010012205A 도파민 Ｄ3 수용체 조절체로서의 테트라히드로이소퀴놀린유도체 无效
标题翻译：四氢异喹啉衍生物作为多巴胺D 3 受体的调节剂
公开(公告)号：KR1020010012205A
公开(公告)日：2001-02-15
申请号：KR1019997010154
申请日：1998-04-27
申请人： 스미스크라인 비참 리미티드
发明人： 브랜치,클라이브,레슬리 , 존슨,크리스토퍼,노버트 , 스템프,지오프리
IPC分类号： C07D217/04
摘要： R represents a substituent selected from: a hydrogen or a substituent as defined in the claims; R 2 represents a hydrogen atom or a C 1-4 alkyl group; q is 1 or 2; A represents a group of formula (a), (b) or (c) wherein: Ar represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; or an optionally substituted bicyclic ring system; Ar 1 and Ar 2 each independently represent an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and Y represents a bond, -NHCO-, -CONH-, -CH 2 -, or -(CH 2) m Y 1 (CH 2) n -, wherein Y 1 represents O, S, SO 2, or CO and m and n each represent zero or 1 such that the sum of m+n is zero or 1; providing that when A represents a group of formula (a), any substituent present in Ar ortho to the carboxamide moiety is necessarily a hydrogen or a methoxy group; and salts thereof. Compounds of formula (I) and their salts have affinity for dopamine receptors, in particular the D 3 receptor, and thus potential in the treatment of conditions wherein modulation of the D 3 receptor is beneficial, e.g. as antipsychotic agents.
摘要翻译： R表示选自以下的取代基：权利要求中定义的氢或取代基; R 2表示氢原子或C 1-4烷基; q为1或2; A表示式（a），（b）或（c）的基团，其中：Ar表示任选取代的苯环或任选取代的5或6元芳族杂环; 或任选取代的双环体系; Ar 1和Ar 2各自独立地表示任选取代的苯环或任选取代的5或6元芳族杂环; 并且Y表示键，-NHCO-，-CONH - ， - CH 2 - 或 - （CH 2）m Y 1（CH 2）n - ，其中Y 1表示O，S，SO 2或CO和m 并且n分别表示0或1，使得m + n的和为零或1; 条件是当A表示式（a）的基团时，存在于羧酰胺部分的Ar中的任何取代基必须是氢或甲氧基; 及其盐。式（I）化合物及其盐对多巴胺受体，特别是D 3受体具有亲和性，因此在治疗D 3受体调节有利的条件下具有潜力，例如，作为抗精神病药。

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