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 31/551 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2450868

Provided are compounds represented by formula (I):wherein R2 is H, halogen, NHNH2, (C1-4)alkyl, O(C1-6)alkyl, and haloalkyl; R4 is H or Me; R5 is H or (C1- 4)alkyl; R11 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is naphthyl, fused phenyl(C4-7)cycloalkyl and fused phenyl-5, 6, or 7- membered saturated heterocycle having one to two heteroatom selected from O, N, or S, said Q being substituted with from 1 to 4 R12 substituents selected from: R13, (C1-6)alkyl, (C3-7)cycloalkyl, or (C2-6)alkenyl, said alkyl, cycloalkyl, or alkenyl being optionally substituted with R13; or a salt thereof. Compounds represented by formula I have inhibitory activity against Wild Type, single and double mutant strains of HIV.

L'invention se rapporte à des composés représentés par la formule I dans laquelle R?2¿ est H, halogène, NHNH¿2?, (C¿1-4?)alkyl, O(C¿1-6?)alkyl, et haloalkyl ; R?4¿ est H ou Me ; R?5¿ est H ou (C¿1-4?)alkyl, R?11¿ est (C¿1-4?)alkyl, (C¿1-4?)alkyl(C¿3-7?)cycloalkyl, ou (C¿3-7?)cycloalkyl; et Q est naphthyl, phényle fusionné(C¿4-7?)cycloalkyl et un hétérocycle saturé à 5, 6 ou 7 membres de phényle fusionné présentant un ou deux hétéroatomes choisis parmi O, N ou S, Q étant substitué par des substituants R?12¿ compris entre 1 et 4 et choisis parmi : R?13¿, (C¿1-6?)alkyl, (C¿3-7?)cycloalkyl, ou (C¿2-6?)alkényl, alkyle, cycloalkyle ou alkényle étant facultativement substitués par R?13¿, ou un sel de ce dernier. Les composés représentés par la formule I présentent une activité inhibitrice contre les souches mutantes simples et doubles de type sauvage du virus VIH.

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