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Substituted benzimidazoles and Methods for use as inhibitors of kinases associated with tumorigenesis

机译:取代的苯并咪唑和用作与肿瘤发生有关的激酶抑制剂的方法

摘要

In some embodiments, the compounds and compositions are effective to inhibit the activity of at least a serine / Threonine Kinase and tyrosine kinase receptors.The compounds and compositions may be used alone or in combination with at least one additional agent for treating a disorder mediated by a serine / Threonine Kinase and tyrosine kinase Receptors, such as cancer.Claim 1: wherein is a compound of formula (1), wherein each R1 is selected independently between Hydroxy alkyl, Halo, C1 - 6, 6 - (alkyl alkoxy C1, C1 - 6) sulfanilo (C1 - sulfonyl alkyl, cycloalkyl, 6) heterocicloalquilo phenyl heteroaryl, and R2 is alqui; The C1 - 6 or Halo (alkyl C1 - 6); R3 are each independently selected from alkyl, Halo, C1 - 6Alkoxy and C1 - 6; each R4 is selected independently between Hydroxy alkyl, alkoxy C1 C1 - 6 - 6, Halo (alkoxy, carboxyl, carbonyl, aminocarbonilo C1 - 6), alquilaminocarbonilo C1 - 6, carbonitrilo, cycloalkyl, heterocicloalquilo, heterocicloalquilcarbonilo, phenyl, and heteroaryl; where R1, r 2 R3And R4 may be optionally substituted with one or more substituents selected independently between Hydroxy alkyl, Halo, Halo (C1 - 6, 6 - alkoxy alkyl C1, C1) and Halo (- 6, 6 - alkoxy C1); a is 1, 2, 3, 4, or 5; b is 0, 1, 2, or 3; and C is 1 or 2; or a stereoisomer, polymorphic, and tautomero, Ster, metabolite, or a Salt or prodrug thereof acceptable for pharmaceutical use of the compoundTautomero, stereoisomer, polymorphic, metabolite, Ester or prodrug.
机译:在一些实施方案中,所述化合物和组合物可有效抑制至少丝氨酸/苏氨酸激酶和酪氨酸激酶受体的活性。所述化合物和组合物可单独使用或与至少一种其他试剂组合使用以治疗介导的疾病。权利要求1:其中为式(1)的化合物,其中每个R 1独立地选自羟基烷基,卤代,C 1-6,6-(烷基烷氧基);或通过酪氨酸激酶和酪氨酸激酶受体,例如癌症。 C 1,C 1-6)磺酰苯胺基(C 1-6磺酰基烷基,环烷基,6)杂环基喹啉基苯基杂芳基,R 2为氢。 C1-6或卤代(烷基C1-6); R3各自独立地选自烷基,卤素,C1-6烷氧基和C1-6;每个R 4独立地选自羟基烷基,烷氧基C 1 -C 6-6,卤代(烷氧基,羧基,羰基,氨基羰基C 1-6),烷氨基羰基C 1-6,羰基三氯,环烷基,杂环氯基,杂环氯基羰基,苯基和杂芳基;其中R1,r 2,R3和R4可以任选地被一个或多个独立地选自羟基烷基,卤代基,卤代基(C1-6、6-烷氧基烷基C1,C1)和卤代基(-6、6-烷氧基C1)中的取代基取代; a为1、2、3、4或5; b为0、1、2或3; C为1或2;或其可药用的化合物互变异构体,立体异构体,多晶型,代谢物,酯或前药的立体异构体,多晶型和互变异构体,Ster,代谢物或其盐或前药。

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