首页> 外国专利> 2-PHENYL BENZIMIDAZOLES AND IMIDAZO-4,5-PYRIDINES AS CDSI/CHK2-INHIBITORS AND ADJUVANTS TO CHEMOTHERAPY OR RADIATION THERAPY IN THE TREATMENT OF CANCER

2-PHENYL BENZIMIDAZOLES AND IMIDAZO-4,5-PYRIDINES AS CDSI/CHK2-INHIBITORS AND ADJUVANTS TO CHEMOTHERAPY OR RADIATION THERAPY IN THE TREATMENT OF CANCER

机译:作为CDSI / CHK2抑制剂和化学疗法或放射疗法辅助剂的2-苯基苯并咪唑和咪唑并[[4,5]-吡咯酮]

摘要

2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines of formula (I) a re 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, -SCF 3, 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 o r C1-4alkyl; AR1 is an aromatic group as defined in the claims.
机译:式(I)的2-芳基取代的苯并咪唑和咪唑并[4,5]吡啶被公开为Cds1的抑制剂,并且在癌症的治疗中用作化学疗法或放射疗法的佐剂。其中W是COOH,-(CO)NHR 1或-(SO 2)NHR 1 R 1是H或C 1-4烷基; Q是N或CH; Ra和Rb是H或卤素; Y,Y1和Y2独立地选自N和C-Rc,条件是Y,Y1和Y2的0、1或2为N且Rc中的至少2个必须为氢; R c独立地选自-H,-OH,-C 1-6烷基,-SCF 3,卤素,-CF 3和-OCF 3; Z选自O,S,SO,SO 2,SO 2 NR 2,NR 2 SO 2,NH,CONR 2,哌嗪二基或共价键; R 2为H 1 -C 1-4烷基; AR1是如权利要求中所定义的芳族基团。

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