Pyrazolo-pyridine derivatives as ligands for gaba receptors

Details Pyrazolo-pyridine derivatives as ligands for gaba receptors Pyrazolo-pyridine derivatives as ligands for gaba receptors

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/47 (2006.01) A61P 25/18 (2006.01) A61P 25/22 (2006.01)

Patent

CA 2392944

A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the .beta.2 and/or .beta.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.

L'invention concerne une classe de dérivés substitués et/ou annelés de pyrazolo[3,4-b]pyridine, comprenant un substituant cycloalkyle, phényle ou hétéroaryle éventuellement substitué sur l'atome d'azote de pyrazole adjacent au noyau de pyridine, et un substituant cycloalkyle-alkoxy, aryle-alkoxy ou hétéroaryle-alkoxy éventuellement substitué sur l'atome de carbone adjacent à l'atome d'azote du noyau de pyridine. Ces dérivés sont des ligands sélectifs des récepteurs de GABA¿A?, possédant en particulier une grande affinité avec la sous-unité .alpha.2 et/ou .alpha.3 de celui-ci, et étant par conséquent très utiles dans le traitement et/ou la prévention de troubles neurologiques indésirables, y compris l'anxiété et les convulsions.

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