2-amino-5,6-dichlorobenzimidazole derivatives having...

C - Chemistry – Metallurgy – 07 – D

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C07D 235/30 (2006.01) A61K 31/415 (2006.01) A61K 31/675 (2006.01) C07D 235/24 (2006.01) C07D 403/04 (2006.01) C07F 9/6506 (2006.01)

Patent

CA 2241893

The present invention relates to benzimidazole derivatives of formula (I) wherein: R1 represents H, C1-4 alkyl, C3-5 cycloalkyl; R2 represents H, C1-4 alkyl; or R1 and R2 together form with the nitrogen a 4 or 5 membered heterocyclic ring; R3 represents BR4 or R4 wherein B represents a bridging group -C(O)NH-, -C(O)NC1-4alkyl-, or -C(O)O- and R4 represents H, C1-4alkyl, C2-6alkenyl or halo (preferably fluoro); and each n is an integer independently selected from 0, 1, or 2 (preferably 0 or 1); and geometric isomers or mixtures thereof; and physiologically functional derivatives thereof, and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to their preparation and pharmaceutical formulations containing them.

L'invention concerne des dérivés benzimidazole de la formule (I). Dans cette formule, R?1¿ représente H, C¿1-4? alkyle, C¿3-5? cycloalkyle; R?2¿ représente H, C¿1-4? alkyle; ou R?1¿ et R?2¿ forment ensemble avec l'azote un noyau hétérocyclique à 4 ou 5 éléments; R?3¿ représente BR?4¿ ou R?4¿, où B représente un pont -C(O)NH-, -C(O)NC¿1-4?alkyl-, ou -C(O)O- et R?4¿ représente H, C¿1-4? alkyle, C¿2-6? alcényle ou halo (de préférence fluoro); et chaque n est un nombre entier choisi d'une manière indépendante entre 0,1 ou 2 (de préférence 0 ou 1). L'invention concerne aussi les isomères géométriques ou leurs mélanges, et leurs dérivés actifs du point de vue plan physiologique. L'invention concerne également l'utilisation thérapeutique de ces dérivés, en particulier pour la prévention ou le traitement d'infections virales telles que celles provoquées par des virus de l'herpès, ainsi que la préparation de ces dérivés et celle de formulations pharmaceutiques les contenant.

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