N-substituted azaheterocyclic carboxylic acids

C - Chemistry – Metallurgy – 07 – D

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C07D 211/60 (2006.01) A61K 31/445 (2006.01) C07D 211/78 (2006.01) C07D 409/00 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2005919

Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which an ether group forms part of the N-substituent, the compounds thus having the general for- mula I Image (I) wherein R1 and R2 are the same or different and each re- presents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl or 3-pyrrolyl, substituted with one or more substituents se- lected among the following atoms or groups: hydrogen, ha- logen, C1-6-alkyl, C1-6-alkoxy or cyano; R3 and R4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m i8 1 and n is 0 when m is 2; R5 and R6 each represents hydrogen or may - when m is 2 - together represent a bond, and R7 is OH or C1-8-alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R is H and C1-4-alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.

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