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

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

机译:2-苯基苯并咪唑和咪唑并-[ 4,5]-吡啶类化合物作为CDSI / CHK2抑制剂和化疗药物或放射治疗的辅助药物

摘要

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)NHR?1¿, or -(SO=¿2?)NHR?1¿ R?1¿ is H or C¿1-4?alkyl; Q is N or CH; R¿a? and R¿b? are H or halogen; Y, Y¿1? and Y¿2? are independently selected from N and C-R¿c? with the proviso that 0, 1 or 2 of Y, Y¿1? and Y¿2? are N and at least 2 of R¿c? must be hydrogen; R¿c? are independently selected from the group consiting of -H, -OH, -C¿1-6?alkyl, -SCF¿3?, halo, -CF¿3? and -OCF¿3?; Z is selected from the group consisting of O, S, SO, SO¿2?, SO¿2?NR?2¿, NR?2¿SO¿2?, NH, CONR?2¿, piperazin-diyl or a covalent bond; R?2¿ is H or C¿1-4?alkyl; AR¿1? is an aromatic group as defined in the claims.
机译:公开了式(I)的2-芳基取代的苯并咪唑和咪唑并[4,5]吡啶作为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 1 R 1′是H或C 1-4烷基; Q是N或CH;啊?和R¿b?是氢或卤素; Y,Y¿1?和Y¿2?是分别从N和C-R?c中选择的?前提是Y,Y¿1是0、1或2?和Y¿2?是N和R?c中的至少2个?必须是氢; R?c?选自-H,-OH,-C 1-6烷基,-SCF 3,卤素,-CF 3的基团。和-OCF¿3?; Z选自O,S,SO,SO 2,SO 2 NR 2,NR 2 2 SO 2,NH,CONR 2,哌嗪二基或共价基团键; R 2是H或C 1-4烷基; AR¿1?是如权利要求中所定义的芳族基团。

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