[EN] BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE<br/>[FR] COMPOSÉS PYRIMIDINES BICYCLIQUES INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA, ET PROCÉDÉS D'UTILISATION
申请人:GENENTECH INC
公开号:WO2010138589A1
公开(公告)日:2010-12-02
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.
公式(I)((Ia)和(Ib))化合物,其中(i)X1为N且X2为S,(ii)X1为CR7且X2为S,(iii)X1为N且X2为NR2,或(iv)X1为CR7且X2为O,包括其立体异构体,互变异构体,代谢物和药用可接受盐,用于抑制PI3K的δ异构体,并用于治疗由脂质激酶介导的疾病,如炎症,免疫和癌症。公开了使用公式(I)化合物进行体外,体内和体内诊断,预防或治疗哺乳动物细胞中的这类疾病或相关病理状况的方法。