BROADSPECTRUM HETEROCYCLIC SUBSTITUTED PHENYL CONTAINING SULFONAMIDE HIV PROTEASE INHIBITORS

摘要

The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by Calkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloCalkyl, carboxyl, Ccycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, -(R)-M-R, Hetand Het; whereby the optional substituents on any amino function are independently selected from Rand -A-R; and on (ii) a nitrogen atom if present by hydroxy or -A-R. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.