Heterocyclic carboxylic acids

US5198451A · kind A · utility

Assignee

• Novo Nordisk A/S · DK

Inventors

• Knud Erik Andersen
• Lars J. Stray Knudsen · Hørsholm, DK
• Ursula Sonnewald · Rang Taché Est, DK
• Per Ole Sorensen · Copenhagen, DK

Key dates

• Filing date: Nov 20, 1990
• Grant date: Mar 30, 1993
• Expiry date: Nov 20, 2010

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 the general formula I ##STR1## wherein Y is ##STR2## wherein R.sup.1 and R.sup.2 independently are C.sub.3-8 cycloalkyl phenyl or thienyl all of which may be optionally substituted with halogen, trifluoromethyl, C.sub.1-16 alkyl or C.sub.1-6 alkoxy; PA0 s is 1, 2 or 3; PA0 x is --CH.sub.2 --, --O-- or ##STR3## -wherein R.sup.3 is hydrogen or C.sub.1-6 -alkyl; r is 2, 3 or 4; R.sup.4 and R.sup.5 each represents hydrogen or may together represent a bond and R.sup.6 is OH or C.sub.1-8 -alkoxy; and pharmaceutically acceptable acid addition salts are potent inhibitors of GABA uptake from the synaptic cleft.