HIV INTEGRASE INHIBITORS

摘要

The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het<2> ; R<1> is hydrogen, halo, nitro, cyano, sultam, sulltim, C3-7cycloalkyl, C(=O)-R<5>, S(=O)y-R<6>, OR <7>, NR<8>R<9>, C(=NR<8>)-R<5>, optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R< 2> is hydrogen, C3-7cycloalkyl, aryl, Het<1>, Het<2>, C(=O)-R<5>, S(=O)Y-R<6> OR<7>, NR<8>R<9>, C=NR<8>)-R<5>, or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, and to their use in assays as reference compounds or as reagents.