| abstract |
"HIV SULPHONAMIDE PROTEASE INHIBITORS CONTAINING HIGH-SPECIFIC HETEROCYCLIC REPLACED PHENYL". The present invention relates to compounds having formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and their metabolites, wherein Harila is aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 14 ring members containing 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 C 1-6 alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC 1-6-, alkyl, carboxy, C 3-7 cycloalkyl, optionally mono or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, (R 7) a ~) nM- 7b-, Het ^ 1 ^ and Het ^ 2 ^; whereby optional substituents on any amino function are independently selected from R 5 and -A-R 6; and on (II) a nitrogen atom if present by hydroxy or -A-R6. This further relates to their use as broad spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and kits comprising them. It also refers to their combinations with another antiretroviral agent, and to their use in assays as reference compounds or as reagents. |