5'-substituted-ribofuranosyl benzimidazoles as antiviral agents

Details 5'-substituted-ribofuranosyl benzimidazoles as antiviral agents 5'-substituted-ribofuranosyl benzimidazoles as antiviral agents

C - Chemistry, Metallurgy

07

H

C07H 19/052 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2223814

The present invention relates to polysubstituted benzimidazoles, having formula (I), wherein Q is substituted benzimidazole group attached at the benzimidazole 1-position; R is a halogen or atomic number 9 to 53, inclusive (i.e., -F, -Cl, -Br, or -I); azido (i.e., -N3); or -X-R1, wherein X is a chalcogen of atomic number 8 to 16, inclusive (i.e., -O- or -S-), and R1 may be straight or branched chain alkyl of 1 to 8 carbon atoms; and R2 and R3 may be the same or different and are separately -O-C(=O)CH3 (i.e., -OAc) or hydroxy (i.e., -OH); and pharmaceutically acceptable salts and operative combinations thereof. Also provided by this invention are compositions comprising a polysubstituted benzimidazoles as defined above and methods of use thereof.

On décrit des benzimidazoles polysubstitués de formule (I) où Q représente un groupe benzimidazole substitué rattaché à la position 1 de benzimidazole; R représente un halogène de numéro atomique 9 à 53 inclus (c'est-à-dire -F, -Cl, -Br, ou -I); azido (c'est-à-dire -N¿3?); ou -X-R¿1?, où X représente un chalcogène de numéro atomique 8 à 16 inclus (c'est-à-dire -O- ou -S-), et R¿1? peut représenter un alkyle à chaîne droite ou ramifiée de 1 à 8 atomes de carbone; et R¿2? et R¿3?, identiques ou non, représentent chacun -O-C(=O)CH¿3? (c'est-à-dire -OAc) ou hydroxy (c'est-à-dire -OH). On décrit aussi leurs sels de combinaison actives pharmacologiquement acceptables, de même que des compositions comprenant un benzimidazole polysubstitué tel que défini ci-dessus, et leurs procédés d'utilisation.

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