2-phenyl benzimidazoles and imidazo-[4,5]-pyridines as...

Details 2-phenyl benzimidazoles and imidazo-[4,5]-pyridines as... 2-phenyl benzimidazoles and imidazo-[4,5]-pyridines as...

C - Chemistry, Metallurgy

07

D

C07D 235/18 (2006.01) A61K 31/4184 (2006.01) A61K 31/437 (2006.01) A61K 31/4439 (2006.01) A61K 31/496 (2006.01) C07D 401/04 (2006.01) C07D 401/10 (2006.01) C07D 403/10 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2464000

2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines of formula (I) are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer. wherein W is COOH, -(CO)NHR1, or -(SO2)NHR1 R1 is H or C1-4alkyl; Q is N or CH; Ra and Rb are H or halogen; Y, Y1 and Y2 are independently selected from N and C-Rc with the proviso that 0, 1 or 2 of Y, Y1 and Y2 are N and at least 2 of Rc must be hydrogen; Rc are independently selected from the group consiting of -H, -OH, -C1-6alkyl, -SCF3, halo, -CF3 and -OCF3; Z is selected from the group consisting of O, S, SO, SO2, SO2NR2, NR2SO2, NH, CONR2, piperazin-diyl or a covalent bond; R2 is H or C1-4alkyl; AR1 is an aromatic group as defined in the claims.

L'invention concerne des benzimidazoles substitués par 2-aryl et des imidazo[4,5]pyridines selon la formule (I) utilisés comme inhibiteurs de Cds1 et utiles comme adjuvants en chimiothérapie et radiothérapie dans le traitement du cancer. Dans cette formule, W représente COOH, -(CO)NHR?1¿, ou -(SO=¿2?)NHR?1¿ R?1¿ est H ou C¿1-4?alkyle; Q est N ou CH; R¿a? et R¿b? représentent H ou halogène; Y, Y¿1? et Y¿2? sont indépendamment sélectionnés parmi N et C-R¿c? à condition que 0, 1 ou 2 parmi Y, Y¿1? et Y¿2? représentent N et au moins 2 de R¿c? doit être hydrogène; R¿c? sont indépendamment sélectionnés dans le groupe se composant de -H, -OH, -C¿1-6?alkyle, -SCF¿3?, halo, -CF¿3? et -OCF¿3?; Z est choisi dans le groupe se composant de O, S, SO, SO¿2?, SO¿2?NR?2¿, NR?2¿SO¿2?, NH, CONR?2¿, pipérazine-diyle ou une liaison covalente; R?2¿ est H ou C¿1-4?alkyle; AR¿1? est un groupe aromatique tel que défini dans les revendications.

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