ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS

摘要

3-phosphoindole compounds substantially in the form of a single enantiome r useful for the treatment of Flaviviridae virus infections, and particularl y for HLV infections are provided. Also provided are pharmaceutical composit ions comprising the 3-phosphoindole compounds alone or in combination with o ne or more other antiviral agents, processes for their preparation, and meth ods of manufacturing a medicament incorporating these compounds. The 3-phosp hoindole compounds are of the formula (A) or (B) and the pharmaceutically ac ceptable salts, solvates, hydrates, or esters thereof. In the formulae X is hydrogen; aryl or heterocyclyl; C2-6 alkenyl, C2-6 alkynyl or alkyl; Y is hy drogen, -R, -O-R, -NH-R, or -NRR; Z is -OR, -NHR, -NRR, carboxamido, arnido, carboxyl, carbonyl, or an amino acid residue; R1 is hydrogen, acyl, -S(O)n- R, carboxyl, carbonyl, or an amino acid residue; each R4', R5', R6' and R7' is independently hydrogen, C2-6 alkenyl, C2-6 alkynyl, aryl, heterocyclyl, h alogen, -CN, -CF3, -OR, -NHR, -NRR, or -NO2; n is 0, 1, or 2; and each R is independently hydrogen, alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heterocy clyl.