C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/75 (2006.01) A61K 31/44 (2006.01) A61P 31/18 (2006.01) C07D 213/85 (2006.01)
Patent
CA 2458093
Compounds of the formula (I): where R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1- C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CR8R9)n-, R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are =0, n is 1, 2 or 3, and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
L'invention concerne des composés correspondant à la formule (I), des promédicaments et des sels pharmaceutiquement acceptables de ceux-ci, lesquels peuvent être utilisés comme inhibiteurs de la transcriptase inverse du VIH-1, en particulier de mutants échappant à l'action des médicaments. Dans ladite formule (I): R¿1? représente O, S; R¿2? représente un hétérocycle éventuellement substitué contenant de l'azote, l'azote étant située en position 2 par rapport à la liaison (thio)urée; R¿3? représente H, alkyle C¿1?-C¿3?; R¿4?-R¿7? sont, indépendamment l'un de l'autre, choisis parmi H, alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alkynyle C¿2?-C¿6?, halo-alkyle C¿1?-C¿6?, alcanoyle C¿1?-C¿6?, halo-alcanoyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, halo-alcoxy C¿1?-C¿6?, alkyloxy C¿1?-C¿6?-alkyle C¿1?-C¿6?, halo-alkyloxy C¿1?-C¿6?-alkyle C¿1?-C¿6?, hydroxyalkyle C¿1?-C¿6?, aminoalkyle C¿1?-C¿6?, carboxyalkyle C¿1?-C¿6?, cyanoalkyle C¿1?-C¿6?, amino, carboxy, carbamoyle, cyano, halo, hydroxy ou un groupe céto; X représente -(CR¿8?R¿9?)¿n?-; et R¿8? et R¿9? représentent, indépendamment l'un de l'autre, H, alkyle C¿1?-C¿3?, OH, ou bien R¿8? et R¿9? représentent ensemble =O, n valant 1, 2 ou 3.
Antonov Dmitry
Noreen Rolf
Sahlberg Christer
Wallberg Hans
Gowling Lafleur Henderson Llp
Medivir Ab
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