Non-nucleoside reverse transcriptase inhibitors

Details Non-nucleoside reverse transcriptase inhibitors Non-nucleoside reverse transcriptase inhibitors

2006-09-12

2006-09-12

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S495000

Reexamination Certificate

active

07105510

ABSTRACT:
Compounds represented by formula I:wherein R1is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2is H or (C1-4)alkyl; R3is H or (C1-4)alkyl; R4is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.

REFERENCES:
patent: 5705499 (1998-01-01), Cywin et al.
patent: 2003/0069226 (2003-04-01), Ogilvie et al.
patent: 2003/0171363 (2003-09-01), Ogilvie et al.
Janice M. Klunder et al; Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 7. 8-Arylethyldipyridodiazepinones as Potent Broad-Spectrum Inhibitors of Wild-Type and Mutant Enzymes; J. Med. Chem 1998 vol. 41 pp. 2960-2971; American Chemical Society.
Charles L. Cywin et al; Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones; J. Med. Chem 1998 vol. 41 pp. 2972-2984; American Chemical Society.

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