Non-nucleoside reverse transcriptase inhibitors

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

2007-09-25

2007-09-25

Coleman, Brenda (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S555000

Reexamination Certificate

active

10662606

ABSTRACT:
Compounds represented by formula 1:wherein R1is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2is H or methyl; R3is H or (C1-4)alkyl; R4is H or (C1-4)alkyl; R5is (C1-4)alkyl, (C1-4)alkyl(C3-7)cyclo-alkyl or (C3-7)cycloalkyl; and W is a fused phenyl-5 or 6-membered heterocycle having one or two heteroatoms selected from N or S; or W is phenyl, 1,1′-biphenyl, 2,3-dihydro-1H-indene, 1,2,3,4-tetrahydronaphthyl, or naphthyl; said W being optionally substituted with (C1-4)alkyl, which in turn can be optionally substituted with a carboxy or (C1-4)alkoxycarbonyl, or a salt or ester thereof. The compounds have inhibitory activity against Wild Type, single and double mutant strains of HIV.

REFERENCES:
patent: 0767172 (1997-04-01), None
patent: 0791594 (1997-08-01), None
patent: WO 02/076982 (2002-10-01), None
patent: WO 03/011862 (2003-02-01), None
Nicholas K. Terrett et al; Imidazo[2′,3′:6,5]Dipyrido[3,2-b:2′,3′-e]—1,4-Diazepines: Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors with Greater Enzyme Affinity than Nevlrapine; Bioorganic & Medicinal Chemistry Letters vol. 2 No. 12 pp. 1745-1750 (1992); Pergamon Press.
International Search Report Reference #PCT/CA 03/01410, 2004.

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