Non-nucleoside reverse transcriptase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 413/14 (2006.01) A61K 31/44 (2006.01) A61K 31/4433 (2006.01) A61K 31/4436 (2006.01) A61K 31/5377 (2006.01) A61P 31/18 (2006.01) C07D 213/65 (2006.01) C07D 213/73 (2006.01) C07D 307/93 (2006.01) C07D 311/94 (2006.01) C07D 333/78 (2006.01) C07D 335/06 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2501924

A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, Cl-C3 alkyl; X is -(CR8R8')n-D-(CR8R8')m-; D is a bond, - NR9-, -O-, -S-, -S(=O)- or -S(=O)2-; n and m are independently 0, 1 or 2, R8 and R8' are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8' together with their adjacent C atom is -C(=O)-; R9 is independently H, C1- C3 alkyl; E is CH2-, -CHOH-, -C(=O)-, -NR9-, -O-, -S-, -S(=O)2-; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q <= 2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted Cl-C3alkyl, hydroxy; have utility as HIV antivirals.

La présente invention a trait à un composé de formule (Y), dans laquelle : R¿1? est O, S ; R¿2? est un hétérocycle azoté ; R¿3? est H, alkyle en C¿1?-C¿3 ?; X est -(CR¿8?R¿8'?)¿n?-D-(CR¿8?R¿8'?)¿m?-; D est une liaison, -NR¿9?-, -O-, -S-, -S(=O)- ou -S(=O)¿2?-;¿?R¿8? et R¿8'? avec leur atome de carbone adjacent est -C(=O) ; R¿9? est indépendamment H, alkyle en C¿1?-C¿3?; E est -CH¿2?-, -CHOH-, -C(=O)-, -NR¿9?-, -O-, -S-, -S(=O)¿2?-; n et m sont indépendamment 0,1 ou 2 ; p et q sont indépendamment 0,1 ou 2, où p+q <= 2 ; R¿10? est un système carbocyclique ou hétérocyclique éventuellement substitué ; R¿11? est indépendamment H, alkyle en C¿1?-C¿3? alkyle en C¿1?-C¿3? substitué par halo, hydroxy. Ledit composé est utile en tant qu'agent antiviral du VIH.

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