Substituted imidazole derivatives and their preparation and use

C - Chemistry – Metallurgy – 07 – D

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C07D 233/64 (2006.01) A61K 31/415 (2006.01) C07D 233/54 (2006.01)

Patent

CA 2117305

This invention provides novel compounds of formula (I) wherein Y is -CH2- or - CO-; R1 is F, C1 or OH; R2 is H, F or C1; and R3 is H, CH3 or CH2CH3, excluding 4-(5-chloro-2,3-dihydro-1H-inden-2- yl)-1H-imidazole and 4-(4-chloro-2,3-di- hydro-1H-inden-2-yl)-1H-imidazole and their non-toxic acid addition salts and mixtures thereof. Processes for the prepara- tion of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds or their salts. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are highly selective and long acting antagonists at a2-adrenoceptors. Their peroral bioavailability is good. The compounds are especially useful in the treatment of cognitive disorders.

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