4-Substituted piperazine-2-carboxylic acids process and pharmaceutical compositions.

摘要

Compounds of the general formula <CHEM> wherein X is C1-C6, straight chain saturated or unsaturated hydrocarbyl group, the group R<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<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<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<4>-X-Y represents a carboxylic acyl group; R<1> is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl; R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group; R<2>, R<3> and R<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<2> and R<3> together with the carbon atoms to which they are attached form a ring system or R<3> and R<4> together and/or R<3> and X together form one or more than one ring system, and physiologically acceptable salts thereof have activity in the central nervous system.