Benzimidazole and pyridylimidazole derivatives as ligands...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/4184 (2006.01) A61K 31/437 (2006.01) A61P 25/00 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/14 (2006.01) C07D 473/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2431592

This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

L'invention concerne des benzimidazoles, des pyridylimidazoles et des composés hétéroaryles bicycliques associés de formule (I). Plus particulièrement, l'invention concerne des composés se liant avec une sélectivité et une affinité élevées au site benzodiazépinique des récepteurs GABA¿A?. L'invention se rapporte en outre à des compositions pharmaceutiques comprenant ces composés, ainsi qu'à l'utilisation desdits composés dans le traitement de certaines maladies du système nerveux central (SNC). Elle concerne également des procédés de préparation des composés de formule (I), ainsi que l'utilisation de benzimidazoles, de pyridylimidazoles et de composés hétéroaryles bicycliques associés de formule (I) en combinaison avec un ou plusieurs agents du SNC en vue de renforcer les effets d'autres agents du SNC. Par ailleurs, cette invention porte sur l'utilisation desdits composés comme sondes pour la localisation des récepteurs GABA¿A? dans certaines parties du tissu.

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