HIV INTEGRASE INHIBITORS

WIPO Patent Application WO2001096283

A9

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).

PCT/US2001/019476

October 17, 2002

June 18, 2001

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BRISTOL MYERS SQUIBB CO (US)
WALKER MICHAEL A (US)
JOHNSON TIMOTHY D (US)
MEANWELL NICHOLAS A (US)
BANVILLE JACQUE

A61K31/18; A61K31/192; A61K31/195; A61K31/341; A61K31/357; A61K31/36; A61K31/381; A61K31/4406; A61K45/00; A61P31/00; A61P31/18; A61P43/00; C07C27/02; C07C51/09; C07C59/215; C07C59/90; C07C235/28; C07C235/74; C07C237/42; C07C311/51; C07D213/30; C07D213/38; C07D213/40; C07D307/52; C07D317/34; C07D317/40; C07D317/46; C07D317/58; C07D333/20; C07D333/58; C07D405/12; C07D407/12; (IPC1-7): C07C235/28; A61K31/16; A61P31/00; C07C237/42; C07C235/74; C07D213/40; C07D307/52; C07D317/34; C07D317/46; C07D317/58; C07D333/20; C07D405/12; C07D407/12

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