1- [2' , 3' -DIDEOXY-3' C- (HYDROXYMETHYL) - BETA-D-ERYTHRO-PENTOFURANOSYL] CYTOSINE DERIVATIVES AS HIV INHIBITORS

摘要

Compounds of the formula (I) wherein: R¹ is independently H₁ -OR³, -NHR⁴; C₁-C₄ alkyl; or, when n is 2, adjacent R¹ together define an olefin ic bond; R² is H; or when the gem R¹ is C₁-C₄ alkyl, that R² may also be C₁-C₄ alkyl; or when the gem R¹ is -OR³, that R² may also be -C(=O)OH or a pharmaceutically acceptable ester thereof; R³ is independently H, or a pharmaceutically acceptable ester thereof; R⁴ is independently H or a pharmaceutically acceptable amide thereof; R⁵ and R6 are H or an amine prodrug moiety n is 1 , 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.