1-arylphthalazine antagonists of excitatory amino acid...

C - Chemistry – Metallurgy – 07 – D

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C07D 237/30 (2006.01) A61K 31/50 (2006.01) A61K 31/502 (2006.01) C07D 491/04 (2006.01) C07D 491/056 (2006.01)

Patent

CA 2242775

Substituted 1-arylphthalazine compositions such as formula (1) are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtypes of the ionotropic EAA receptors. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compositions may be provided in combination with a suitable pharmaceutical carrier for therapeutic administration for the treatment of a variety of disorders associated with non-NMDA EAA receptor function. The compositions may be used, for example, as sedatives or for the treatment of neuropsychopharmacological disorders such as stroke, ischemia, epilepsy and mood disorders.

L'invention porte sur des préparations de 1-arylphthalazine de formule (1) actifs comme antagonistes de récepteurs ionotropes (du sous-type non NMDA) d'acides aminés excitateurs. Ces préparations peuvent servir pour le traitement des troubles associés à une activation excessives desdits récepteurs, ou comme agents d'essai pour l'identification et la caractérisation d'autres composés utilisés pour le traitement desdits troubles. Elles peuvent être combinées à des excipients pharmaceutiques appropriés pour être administrées en vue du traitement de différents troubles liés à la fonction du susdit récepteur, et peuvent en outre servir par exemple de sédatifs ou pour le traitement de troubles neuropsychopharmacologiques tels que les accidents cérébrovasculaires, l'ischémie, l'épilepsi et les troubles de l'humeur.

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