申请人:SmithKline Beecham PLC
公开号:US05589492A1
公开(公告)日:1996-12-31
A compound of the formula A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; A.sup.2 represents a benzene ring having three optional substituents; A.sup.3 represents a moiety of formula --(CH.sub.2).sub.m --CHR.sup.1 -- wherein R.sup.1 represents a halogen atom or a moiety of formula S(O).sub.p A.sup.4 wherein A.sup.4 represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl, alkylcarbonyl or an aromatic heterocyclyl group and p represents zero or an integer 1 or 2 and m represents zero or an integer in the range of from 1 to 5, or A.sup.3 represents a moiety of formula --CH.dbd.CR.sup.1 -- wherein R.sup.1 is as defined above; R.sup.2 represents OR.sup.3 wherein R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, or R.sup.2 represents --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each independently represent hydrogen or alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a heterocyclic ring; X represents O, S or NR wherein R represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; and n represents an integer in the range of from 2 to 6; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound and composition in medicine.
一种具有以下结构的化合物:A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I)或其互变异构体和/或其药学上可接受的盐,和/或其药学上可接受的溶剂,其中:A.sup.1代表取代或未取代的芳香杂环基团;A.sup.2代表具有三个可选取代基团的苯环;A.sup.3代表具有式--(CH.sub.2).sub.m --CHR.sup.1 --的基团,其中R.sup.1代表卤素原子或式S(O).sub.p A.sup.4的基团,其中A.sup.4代表氢、取代或未取代的烷基、芳基、芳基烷基、烷基羰基或芳香杂环基团,p代表零或整数1或2,m代表零或范围在1到5之间的整数,或A.sup.3代表具有式--CH.dbd.CR.sup.1 --的基团,其中R.sup.1如上定义;R.sup.2代表OR.sup.3,其中R.sup.3代表氢、烷基、芳基或芳基烷基,或R.sup.2代表--NR.sup.4 R.sup.5,其中R.sup.4和R.sup.5各自独立地代表氢或烷基,或R.sup.4和R.sup.5与它们连接的氮原子一起形成杂环环;X代表O、S或NR,其中R代表氢原子、烷基、酰基、芳基烷基,其中芳基可能是取代或未取代的,或取代或未取代的芳基;n代表范围在2到6之间的整数;一种制备这种化合物的方法,包括这种化合物的药物组合物和这种化合物及组合物在医学中的用途。