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Bicyclic pyrimidine PI3K inhibitor compounds selective for p110δ and methods of use

机译:对p110δ具有选择性的双环嘧啶PI3K抑制剂化合物及其使用方法

摘要

Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
机译:式I(Ia和Ib)的化合物,其中(i)X1为N,X2为S,(ii)X1为CR7,X2为S,(iii)X1为N,X2为NR2,或(iv)X1为CR7, X 2是O,包括立体异构体,互变异构体,代谢产物及其药学上可接受的盐,可用于抑制PI3K的δ同工型,并用于治疗由脂质激酶介导的疾病,例如炎症,免疫学和癌症。公开了将式I化合物用于哺乳动物细胞中此类疾病或相关病理状况的体外,原位和体内诊断,预防或治疗的方法。

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