Triazolo-pyrimidines as ligands for gaba receptors

Details Triazolo-pyrimidines as ligands for gaba receptors Triazolo-pyrimidines as ligands for gaba receptors

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01) C07D 239/00 (2006.01) C07D 249/00 (2006.01)

Patent

CA 2334817

A class of substituted or 6,7-ring fused 1,2,3-triazolo[1,5-a]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety 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 de pyrimidine 1,2,3-triazolo [1,5-a] substitués ou réunis par fusion au noyau 6,7, possédant un substituant cycloalkyle, phényle ou hétéroaryle éventuellement substitué à la position 3 et une fraction alcoxy substituée à la position 5, ces dérivés constituant des ligands sélectifs de récepteurs de GABA¿A?; ils présentent notamment une grande affinité pour leurs sous-unités .alpha.2 et/ou .alpha.3 et sont par conséquent utiles dans le traitement et/ou la prévention de troubles du système nerveux central, y compris l'anxiété et les convulsions.

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