ANTIVIRAL NUCLEOSIDE ANALOGUES CONTAINING A SUBSTITUTED BENZIMIDAZOLE BASE ATTACHED TO A CARBOCYCLIC RING, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM

摘要

Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. In formulae (I) and (I-1), R1 is H, CH3 or CH2OH; R2 is H or OH; R3 is H or OH; or R2 and R3 together form a bond; R4 is amino, cyclopropylamino, cyclobutylamino, isopropylamino, tert-butylamino or -NR8R9 where R8 and R9 together with the nitrogen atom to which they are attached form a 4, 5 or 6-membered heterocyclic ring; R5 is H and R6 and R7 are Cl, excluding the compound (+/-)-(1R*, 2S*, 3S*, 5S*)-5-[5,6-Dichloro-2-(cyclopropylamino)-1uH/u-benzimidazol-1-yl]-3-(hydroxymethyl)-1,2-cyclopentanediol and provided that at least one of R1, R2 and R3 is or contains OH. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.