申请人:ICI Pharma
公开号:US05196422A1
公开(公告)日:1993-03-23
The invention concerns a thiazole of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted aryl of up to 10 carbon atoms; A is a direct link to X, or is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene; X is oxy, thio, sulphinyl, sulphonyl or imino; Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms; R.sup.1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; R.sup.2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, substituted (1-4C)alkyl or (2-6C)alkanoyl; Q is optionally substituted thiazolyl; or a pharmaceutically-acceptable salt thereof. The invention also concerns processes for the manufacture of a thiazole of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said thiazole.
本发明涉及一种公式I的噻唑化合物,其中Ar1是最多含有10个碳原子的可选取代芳基; A是直接连接到X的链或(1-6C)烷基、(3-6C)烯基、(3-6C)炔基或环(3-6C)烷基; X是氧、硫、亚磺酰、磺酰或亚氨基; Ar2是可选取代苯基或含有最多三个氮原子的6元杂环基; R1是氢、(1-6C)烷基、(2-6C)烯基、(2-6C)炔基或取代的(1-4C)烷基; R2是氢、(1-6C)烷基、(3-6C)烯基、(3-6C)炔基、取代的(1-4C)烷基或(2-6C)酰基; Q是可选取代的噻唑基; 或其药学上可接受的盐。本发明还涉及制备公式I的噻唑化合物或其药学上可接受的盐的方法,以及含有该噻唑化合物的制药组合物。