申请人:British Technology Group Limited
公开号:US05399693A1
公开(公告)日:1995-03-21
Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen; R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms; Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group; R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl; R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group; R.sup.2 R.sup.3 and R.sup.5 which may be the same or different is each hydrogen or an alkyl, hydroxy, alkoxy, carboxy, alkyloxycarbonyl, halo, aryl, haloaryl or aryloxycarbonyl group; or R.sup.2 and R.sup.3 together with the carbon atoms to which they are attached form a ring system or R.sup.3 and R.sup.4 together and/or R.sup.3 and X together form one or more than one ring systems, or a physiologically acceptable salt thereof have activity in the central nervous system.
通式为##STR1##的化合物,其中X是C.sub.1-C.sub.6直链饱和或不饱和的烃基,基团R.sup.4和基团Y位于该链的任何位置,并且X中至少有一个氢原子可以是氘同位素;R.sup.4是氢或烷基、烷氧基、羟基、芳基、芳氧基、芳基烷基、芳基烷氧基、芳基烷基氨基或吗啉基团,其中上述任一群的烷基或芳基部分可能被一个或多个卤素基团取代;或者R.sup.4与基团X中的至少一个碳原子形成5到6个环原子的碳环或杂环;Y是一个酸性或相关的基团,在该基团中引起一个或多个电负性位点;或R.sup.4--X--Y代表一个羧酰基团;R是氢或烷基、卤代烷基、芳基、卤代芳基、芳基烷基或卤代芳基烷基;R.sup.1是氢或烷基、卤代烷基、芳基、卤代芳基、芳基烷基或卤代芳基烷基基团;R.sup.2、R.sup.3和R.sup.5,它们可以相同也可以不同,每个是氢或烷基、羟基、烷氧基、羧基、烷氧羰基、卤素、芳基、卤代芳基或芳氧羰基基团;或R.sup.2和R.sup.3与它们附着的碳原子一起形成一个环系统,或R.sup.3和R.sup.4一起和/或R.sup.3和X一起形成一个或多个环系统,或其生理上可接受的盐在中枢神经系统中具有活性。