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DUAL INHIBITORS OF ALK5 AND P38A MAP KINASE

机译:ALK5和P38A MAP激酶的双重抑制剂

摘要

The present disclosure generally relates to the compounds that exhibits protein kinase inhibitory activity. Specifically, the present disclosure provides compounds of formula (I) that exhibits dual inhibitory activity against ALK5 and P38A MAP kinase. The present disclosure also provides process(es) for preparation of such compounds, pharmaceutical compositions containing one or a combination of these compounds, and methods of treatment of conditions associated with excessive activity of any or a combination of transforming growth factor-beta (TGFβ) and p38 mitogen-activated protein kinase (MAPK) utilizing these compounds. An aspect of the present disclosure provides compounds of Formula (I):; embedded image ;and pharmaceutically acceptable salt, polymorph, solvate or stereoisomer thereof that exhibit dual inhibitory activity against ALK5 and P38 alpha.
机译:本公开总体上涉及表现出蛋白激酶抑制活性的化合物。具体地,本公开提供了对ALK5和P38A MAP激酶表现出双重抑制活性的式(I)化合物。本公开还提供了制备此类化合物的方法,包含一种或这些化合物的组合的药物组合物,以及与转化生长因子-β(TGFβ)的任何或组合的过度活性相关的病症的治疗方法。以及利用这些化合物的p38丝裂原活化蛋白激酶(MAPK)。本公开的一个方面提供了式(I)的化合物: “嵌入式图像” ;以及对ALK5和P38α具有双重抑制活性的可药用盐,多晶型物,溶剂化物或立体异构体。

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