Non-nucleoside reverse transcriptase inhibitors

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

C - Chemistry, Metallurgy

07

D

C07D 471/14 (2006.01) A61K 31/55 (2006.01) A61P 31/18 (2006.01) C07D 221/00 (2006.01) C07D 243/00 (2006.01)

Patent

CA 2495721

Compounds represented by formula (I): wherein R1 is H, halogen, (C1-4) alkyl, O(C1-4) alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4) alkyl; R4 is (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.

L'invention concerne des composés représentés par la formule (I), dans laquelle R?1¿ représente H, halogène, alkyle(C¿1-4?), alkyle O(C¿1-4?) et haloalkyle, R?2¿ représente H ou alkyle(C¿1-4?), R?3¿ représente H ou alkyle(C¿1-4?), R?4¿ représente alkyle(C¿1-4?), alkyle(C¿1-4?)cycloalkyle(C¿3-7?) ou cycloalkyle(C¿3-7?), et Q représente un hétérocycle fondu saturé à 5 ou 6 chaînons phényle possédant un ou deux hétéroatomes choisis parmi O et N, Q étant éventuellement substitué avec hydroxy ou alkyle(C¿1-4?) qui peut à son tour être éventuellement substitué avec pyridinyl-N-oxyde ou C(O)OR, R représentant H ou alkyle(C¿1-4?), ou un sel de ces composés. Ces composés présentent une action inhibitrice contre le type sauvage ainsi que les souches mutantes simple et double du VIH.

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