N-SUBSTITUTED AZAHETEROCYCLIC CARBOXYLIC ACIDS AND A PHARMACEUTICAL COMPOSITION

摘要

(see fig. I) (I) (see fig. II) (d) Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent, the compounds thus having general formula (I) wherein Y is (a), (b) or (c) wherein R1 and R2 independently are C3-8 cycloalkyl phenyl or thienyl all of which may be optionally substituted with halogen, trifluoromethyl, C1-6 alkyl or C1-6 alkoxy; s is 1, 2 or 3; X is -CH2-, -O- or (d) wherein R3 is hydrogen or C1-6-alkyl; r is 2, 3 or 4; R4 and R5 each represents hydrogen or may together represent a bond and R6 is OH or C1-8-alkoxy; and pharmaceutically acceptable acid addition salts are potent inhibitors of GABA uptake from the synaptic cleft.