| abstract |
-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:-n wherein:n n is a positive whole integer 2, 3 or 4; m is zero; R 4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R 5 is hydrogen, or hydroxy, or when the dotted line forms a double bond, hydrogen; B isn wherein R, is hydrogen, fluorine, chlorine, methyl or methoxy; Y is -C(A)=C(R 3 )- -CHn -CHR 3 - in which case n is 3 or 4, or -C=C-, wherein R 2 is hydrogen, fluorine, chlorine, methyl or methoxy, R 3 is hydrogen or methyl, and A isn 2-thienyl, 3-thienyl or cyclohexyl; or B-Y is (cyclohexyl) 2 C=C(R 3 )-; or when Y is a -C(A)=C(R 3 )- m may also be one: or a pharmaceutically acceptable acid addition salt thereof, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester. |