HIV INTEGRASE INHIBITORS

摘要

The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula (Ia) wherein R<1> is C1-C4 alkyl, carbocyclic radical, heterocyclic radical, aryl-C1-C2 alkylene, aryloxy-C1-C2 alkylene, alkoxy-CC(O)-, wherein R<1> is optionally substituted from 1-3 times with halo, C1-C2 alkyl or C1-C2 alkoxy, or R<1> is H; R<2> is H or C1-C4 alkyl; R<3> is H, C1-C4 alkyl or phenyl-C0-C2 alkylene which is optionally substituted with 1-3 R<5>; R<4a> is carbocylic radical, heterocyclic radical, aryloxy, aryl-C1-C4 alkylene, aryl-cyclopropylene, aryl-NHC(O)-, wherein R<4a> is optionally substituted with 1-3 R<5>; and wherein each R<5> is independently selected from H, halo, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 haloalkyl, C1-C4 alkoxy, R<6>-phenyl, R<6>-phenoxy, R<6>-benzyl, R<6>-benzyloxy, NH2C(O)-, alkyl-NHC(O)-, wherein R<6> is H, halo; Z is a bond or a substituted or unsubstituted C1-C4 alkylene group; and B<2> is formula (a), (b), or (c).