Dipyridodiazepinones as reverse transcriptase inhibitors

Details Dipyridodiazepinones as reverse transcriptase inhibitors Dipyridodiazepinones as 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 2479216

Disclosed are compounds of formula I:whereinR2 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, NH(C1-4alkyl) or N(C1-4alkyl)2;R4 is H or CH3;R5 is H or CH3;R12 is H, halogen, (C1-4)alkyl, CF3, or NO2; R13 is H, (C1-4)alkyl, halogen, OH, or NH2, with the proviso that R12 and R13 are not both H; andR14 is COOR14a wherein R14a is H or (C1-6)alkyl; or R14 is (C2-4)alkenyl-COOR14a wherein R14a is as defined herein; or R14 is (C1-4)alkyl-COOR14a wherein R14a is as defined above;or a salt or a prodrug thereof, useful as inhibitors of HIV reverse transcriptase.

Cette invention concerne des composés représentés par la formule (I) ou bien un sel ou un promédicament de ces composés, qui sont utiles en tant qu'inhibiteurs de la transcriptase inverse. Dans cette formule, R?2¿ est H, halogène, (C¿1-4?)alkyle, O(C¿1-4?)alkyle, NH(C¿1-4?alkyle) ou N(C¿1-4?alkyle)¿2?; R?4¿ est H ou CH¿3?; R?5¿ est H ou CH¿3?; R?12¿ est H, halogène, (C¿1-4?)alkyle, CF¿3?, ou NO¿2?; R?13¿ est H, (C¿1-4?)alkyle, halogène, OH, ou NH¿2?, à condition que R?12¿ et R?13¿ ne soient pas tous deux H; et R?14¿ est COOR?14a¿ dans lequel R?14a¿ est H ou (C¿1-6?)alkyle; ou R?14¿ est (C¿2-4?)alcényl-COOR?14a¿ dans lequel R?14a¿ est comme défini dans le descriptif; ou R?14¿ est (C¿1-4?)alkyl-COOR?14a¿ dans lequel R?14a¿ est comme défini ci-dessus.

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