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2,3-BENZODIAZEPIN-2-ONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF PROTEIN TYROSINE KINASES

机译:2,3-苯并二氮杂-2-酮衍生物,其制备及其作为蛋白酪氨酸激酶抑制剂的用途

摘要

Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. A compound represented by structural formula (I), where R1, R2 and R3 are independently described as Y bonded to W, where Y is a 0-6 atom straight or branched saturated or unsaturated chain group comprising C, N, O or S as shown in Table 1, and W is hydrogen or any three membered, four membered, five membered, six membered or fused bicyclic ring system comprising C, N, O or S as shown in Tables 4-9; X is separately and independently selected from Table 2; and salts of said compound. Methods are provided for inhibition of specific protein tyrosine kinases, for example pp60c-src. Methods are further provided for the use of these inhibitors in situations where the inhibition of a protein tyrosine kinase is indicated, for example, in the treatment of certain diseases in mammals, including humans.
机译:本文公开了蛋白质酪氨酸激酶的小分子非肽基抑制剂及其使用方法。本发明的抑制剂基于1,4-苯并二氮杂-2--2-核。由结构式(I)表示的化合物,其中R1,R2和R3独立地描述为与W键合的Y,其中Y为0-6个原子的直链或支链的饱和或不饱和链基,包括C,N,O或S,如表4所示,W为氢或包含C,N,O或S的任何三元,四元,五元,六元或稠合双环系统; X独立地选自表2;和所述化合物的盐。提供了抑制特定蛋白质酪氨酸激酶,例如pp60 c-src的方法。还提供了用于这些抑制剂在需要抑制蛋白酪氨酸激酶的情况下的用途,例如在哺乳动物包括人的某些疾病的治疗中的用途。

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