abstract |
2-aryl-substituted benzimidazoles and imidazo [4,5] pyridines of formula (I) are described as Cds1 inhibitors and as useful adjuvants for chemotherapy or radiation therapy in the treatment of cancer, wherein W is COOH, - (CO) NHR1 or - (SO2 ) NHR1; R 1 is H or C 1-4 alkyl; Ra and Rb are H or halogen; Y, Y1 and Y2 are independently selected from N and C-Rc provided that 0, 1 or 2 0 Y, Y1 and Y2 are N and at least 2 of Rc must be hydrogen; Rc is independently selected from the group consisting of -H, -OH, -C1-6, alkyl, -SCF3, halo, -CF3, and -OCF3; Z is selected from the group consisting of O, S, SO, SO2, SO2NR2, NR2SO2, NH, CONR2, piperazinediyl or a covalent bond; R2 is H or C1-4alkyl; Ar1 is one aromatic group as defined in the claims. [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, piperazine-diyl or a covalent bond; R2 is H or C1-4alkyl; AR1 is an aromatic group as defined in the claims. |