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Novo Nordisk A/s

Lars Jacob Knudsen

Knud Erik Andersen

Anker S Jorgensen

Ursula Sonnewald

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 formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl- or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1-8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1-4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.

N-substituted azaheterocyclic carboxylic acids

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 formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1 -C.sub.8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1 -C.sub.4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.

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Lars Jacob Knudsen