Publication number: 20050043370
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 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, C1-C2 alkyl or C1-C2 alkoxy, or R1 is H; R2 is H or C1-C4 alkyl; R3 is H, C1-C4 alkyl or phenyl-C0-C2 alkylene which is optionally substituted with 1-3 R5; R4a is carbocylic radical, heterocyclic radical, aryloxy, aryl-C1-C4 alkylene, aryl-cyclopropylene, aryl-NHC(O)—, wherein R4a is optionally substituted with 1-3 R5; and wherein each R5 is independently selected from H, halo, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 haloalkyl, C1-C4 alkoxy, R6-phenyl, R6-phenoxy, R6-benzyl, R6-benzyloxy, NH2C (O)-, alkyl-NHC(O)—, wherein R6 is H, halo; Z is a bond or a substituted or unsubstituted C1-C4 alkylene group; and B2 is
Type:
Application
Filed:
August 17, 2004
Publication date:
February 24, 2005
Inventors:
Michael Walker, Timothy Johnson, Nicholas Meanwell, Jacques Banville
