首页> 外国专利> Benzokondenserte 5-ringheterocykler, fremgangsmåte for fremstilling derav, deres anvendelse som medikament, deres anvendelse som diagnostikum samt medikament inneholdene disse

Benzokondenserte 5-ringheterocykler, fremgangsmåte for fremstilling derav, deres anvendelse som medikament, deres anvendelse som diagnostikum samt medikament inneholdene disse

机译:苯并稠合的5环杂环化合物,其制备方法,用作药物,用作诊断剂和含有它们的药物

摘要

There are described benzo-fused 5-membered ring heterocycles of the formula I IMAGE where X is N or CR(6); Y is oxygen; A and B together are a bond or are both hydrogen if X is simultaneously CR(6) and Y is NR(7), one of these substituents R(1) to R(6) is a -CO-N = C(NH2)2 group; the other substituents R(1) to R(6) in each case are H, Hal, alkyl; up to two of the other substituents R(1) to R(6) are CN, NO2, N3, (C1-C4)-alkoxy, CF3; up to one of the other substituents is R(8)-CnH2n-Z-, phenyl; R(7) is H, alk(en)yl, R(8)-CnH2n-, and their pharmaceutically tolerable salts. There is further described a process for the preparation of the compounds I, which consists in reacting a compound of the formula II IMAGE wherein one of the substituents R(1)' to R(5)' is a -CO-L group and L is a leaving group which can be readily nucleophilically substituted, with guanidine, and in optionally converting the product to the pharmacologically tolerable salts.
机译:描述了式I 的苯并稠合的5元环杂环,其中X是N或CR(6); Y是氧;如果X同时为CR(6)并且Y为NR(7),则A和B共同为键或均为氢,这些取代基R(1)至R(6)之一为-CO-N = C(NH2 )2组;在每种情况下的其他取代基R(1)至R(6)是H,Hal,烷基;最多两个其他取代基R(1)至R(6)是CN,NO 2,N 3,(C 1 -C 4)-烷氧基,CF 3;最多一个其他取代基是R(8)-CnH2n-Z-,苯基; R(7)为H,烷(烯)基,R(8)-CnH2n-及其药学上可接受的盐。进一步描述了化合物I的制备方法,该方法包括使式II化合物反应,其中取代基R(1)'至R(5)'之一是-CO-L基团L为离去基团,其易于被胍亲核取代,并任选地将产物转化为药理学上可耐受的盐。

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