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isoquinolin-1 (2h) -one derivatives as parp-i inhibitors

机译:isoquinolin-1(2h)-一种衍生物作为parp-i抑制剂

摘要

There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
机译:提供了取代的异喹啉-1(2H)-一衍生物,其相对于聚(ADP-核糖)聚合酶PARP-2选择性抑制聚(ADP-核糖)聚合酶PARP-1的活性。因此,本发明的化合物可用于治疗疾病,例如癌症,心血管疾病,中枢神经系统损伤和不同形式的炎症。本发明还提供了制备这些化合物的方法,包含这些化合物的药物组合物以及利用包含这些化合物的药物组合物治疗疾病的方法。本发明的进一步目的是用于鉴定能够结合几种PARP蛋白的化合物的筛选方法,以及用于该方法的探针。

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