Imidazo-triazine derivatives as ligands for gaba receptors

Details Imidazo-triazine derivatives as ligands for gaba receptors Imidazo-triazine derivatives as ligands for gaba receptors

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/53 (2006.01) A61P 25/22 (2006.01)

Patent

CA 2380452

A class of substituted imidazo[1,2-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position, a range of substituents at the 3-position and an optional alkyl or cycloalkyl substituent at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

L'invention concerne une classe de dérivés d'imidazo[1,2-<i>d</i>][1,2,4]triazine substitués, qui possèdent un substituant cycloalkyle, phényle ou hétéroaryle éventuellement substitué en position 8, une fraction alcoxy substituée en position 2, un choix de substituants en position 3 et un substituant alkyle ou cycloalkyle facultatif en position 5. Ces dérivés sont des ligands sélectifs de récepteurs GABAA, qui présentent en particulier une affinité élevée pour la sous-unité alpha 2 et/ou alpha 3 de ceux-ci, et sont de ce fait utiles pour traiter et/ou prévenir des troubles du système nerveux central, y compris l'anxiété et les convulsions.

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