Imidazo-pyrazine derivatives as ligands for gaba receptors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/415 (2006.01) A61K 31/495 (2006.01) A61P 25/28 (2006.01) C07D 235/00 (2006.01) C07D 241/00 (2006.01)

Patent

CA 2417121

A class of imidazo[1,2-.alpha.]pyrazine analogues substituted in the 3- position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the .alpha.2 and/or .alpha.3 subunit than with the .alpha.1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.

L'invention concerne une classe d'analogues imidazo[1,2-.alpha.]pyrazine substitués en position 3 par un cycle phénylique substitué, étant des ligands sélectifs destinés à des récepteurs GABA¿A? qui interagissent plus favorablement avec la sous-unité .alpha.2 et/ou .alpha.3 qu'avec la sous-unité .alpha.1, qui, selon l'invention, présentent un intérêt dans le traitement et/ou la prévention d'une variété de troubles du système nerveux central, notamment l'anxiété et les convulsions, avec une propension réduite à provoquer la sédation.

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