申请人:John Wyeth & Brother Limited
公开号:US04734510A1
公开(公告)日:1988-03-29
Novel quinazoline and cinnoline derivatives having the formula ##STR1## (wherein one of A and B is CH and the other one of A and B is N; X.sub.1 is halogen or CF.sub.3 and X.sub.3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are independently lower alkyl or R.sub.2 and R.sub.3 are a divalent radical such that HNR.sub.2 R.sub.3 is a secondary cyclic amine with 5 to 7 ring atoms; R.sub.4 is lower alkyl; n is 0 or 1; the rings shown in formulae III and IV are piperidine or pyrrolidine optionally substituted by lower alkyl; and the ring shown in formula V is piperazine optionally substituted by lower alkyl) and their pharmaceutically acceptable salts are useful as pharmaceuticals particularly as anti-hypertensives. Novel intermediates are also described including the corresponding sulphonic acids of formula I (where A, B and X.sub.1 are defined above and X.sub.3 is OH).
具有以下式子的新型喹嗪和咪唑啉衍生物##STR1##(其中A和B中的一个是CH,另一个是N;X.sub.1是卤素或CF.sub.3,X.sub.3是II,III,IV或V组之一##STR2##其中Q是低碳链;R.sub.1是氢或低碳基;R.sub.2和R.sub.3独立地是低碳基或R.sub.2和R.sub.3是二价基团,使得HNR.sub.2 R.sub.3是具有5到7个环原子的次级环状胺;R.sub.4是低碳基;n为0或1;在式III和IV中显示的环是哌啶或吡咯啉,可以选择地被低碳基取代;在式V中显示的环是哌嗪,可以选择地被低碳基取代),以及它们的药物可接受盐,可用作药物,特别是作为抗高血压药物。还描述了新的中间体,包括式I的相应磺酸(其中A,B和X.sub.1如上定义,X.sub.3为OH)。