首页> 外国专利> N-(1-(1-BENZYL-4-PHENYL-1H-IMIDAZOL-2-YL)-2,2-DIMETHYLPROPYL)BENZAMIDE DERIVATIVE AND RELATED COMPOUND AS KINESIN SPINDLE PROTEIN (KSP) INHIBITOR FOR TREATMENT OF CANCER

N-(1-(1-BENZYL-4-PHENYL-1H-IMIDAZOL-2-YL)-2,2-DIMETHYLPROPYL)BENZAMIDE DERIVATIVE AND RELATED COMPOUND AS KINESIN SPINDLE PROTEIN (KSP) INHIBITOR FOR TREATMENT OF CANCER

机译:N-(1-(1-苄基-4-苯基-1H-咪唑-2-基)-2,2-二甲基丙基)苯甲酰胺衍生物及相关化合物作为驱动蛋白的梭状蛋白(KSP)抑制剂治疗癌症

摘要

PROBLEM TO BE SOLVED: To provide KSP inhibitors that are effective in vivo inhibitors of KSP and KSP-related proteins.SOLUTION: There are disclosed substituted imidazole compounds which modulate the activity of KSP and are useful for the treatment of cancer and are represented by the formula (I), wherein: Ris selected from the group consisting of aminoacyl, acylamino, carboxyl, carboxyl ester, aryl, and alkyl optionally substituted with hydroxy or halo; Ris selected from the group consisting of hydrogen, alkyl, and aryl; Ris selected from the group consisting of hydrogen and-X-A, wherein X is selected from the group consisting of-C(O)-, -C(S)-, -S(O)-, -S(O)-, and-S(O)-N(R)-, where R is hydrogen or alkyl.
机译:解决的问题:提供有效的KSP和KSP相关蛋白的体内抑制剂的KSP抑制剂。解决方案:公开了调节KSP活性的取代的咪唑化合物,其可用于治疗癌症,并以式(I),其中:Ris选自氨基酰基,酰基氨基,羧基,羧基酯,芳基和任选地被羟基或卤素取代的烷基; Ris选自氢,烷基和芳基; Ris选自氢和-XA,其中X选自-C(O)-,-C(S)-,-S(O)-,-S(O)-和-S(O)-N(R)-,其中R为氢或烷基。

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