Imidazo-pyrimidine derivatives as ligands for gaba receptors

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 31/519 (2006.01) A61P 25/00 (2006.01) C07D 235/00 (2006.01) C07D 239/00 (2006.01)

Patent

CA 2441455

A class of imidazo[1,2-.alpha.]pyrimidine derivatives, substituted at the 3- position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the .alpha.2 and/or .alpha.3 and/or .alpha.5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

L'invention concerne une classe de dérivés d'imidazo[1,2-.alpha.]pyrimidine, substitués à la position 3 par un anneau hétéroaromatique à cinq ou six éléments éventuellement substitué. Ces dérivés, qui constituent des ligands sélectifs pour les récepteurs GABA¿A?, présentent en particulier une bonne affinité pour la sous-unité .alpha.2 et/ou .alpha.3 et/ou .alpha.5 desdits récepteurs et, par conséquent, s'avèrent utiles dans le traitement et/ou la prévention de troubles du système nerveux central, notamment l'anxiété, les convulsions et les troubles cognitifs.

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