Pyrazolo-triazine derivatives as ligands for gaba receptors

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

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/53 (2006.01) C07D 231/00 (2006.01) C07D 253/00 (2006.01)

Patent

CA 2346289

A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position and a substituted alkoxy moiety at the 2-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 se rapporte à une classe de dérivés pyrazolo[1,5-d][1,2,4]triazine, qui possèdent en position 7 un substituant hétéroaryle, phényle ou cycloalkyle éventuellement substitué et une fraction alcoxy substituée en position 2. Ces dérivés sont des ligands sélectifs des récepteurs GABA¿A?. Ils présentent en particulier une grande affinité pour la sous-unité .alpha.2 et/ou .alpha.3 de ces récepteurs. Ils s'avèrent de ce fait intéressants pour le traitement et/ou la prévention des troubles du système nerveux central, et notamment de l'anxiété et des convulsions.

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