| abstract |
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 R1 is C1-C4 alkyl, carbocyclic radical, heterocyclic radical, aryl-C1-C2 alkylene, aryloxy-C1-C2 alkylene, alkoxy-CC(O)-, wherein R1 is optionally substituted from 1-3 times with halo, C¿1?-C2 alkyl or C1-C2 alkoxy, or R?1¿ is H; R2 is H or C¿1?-C4 alkyl; R?3¿ is H, C¿1?-C4 alkyl or phenyl-C0-C2 alkylene which is optionally substituted with 1-3 R?5; R4a¿ is carbocylic radical, heterocyclic radical, aryloxy, aryl-C¿1?-C4 alkylene, aryl-cyclopropylene, aryl-NHC(O)-, wherein R?4a¿ is optionally substituted with 1-3 R5; and wherein each R5 is independently selected from H, halo, C¿1?-C4 alkyl, C1-C4 alkenyl, C1-C4 haloalkyl, C1-C4 alkoxy, R?6¿-phenyl, R6-phenoxy, R6-benzyl, R6-benzyloxy, NH¿2?C(O)-, alkyl-NHC(O)-, wherein R?6¿ is H, halo; Z is a bond or a substituted or unsubstituted C¿1?-C4 alkylene group; and B?2¿ is formula (a), (b), or (c). |