BENZOXAZEPINE PI3K INHIBITORS AND METHODS OF USE Russian patent published in 2016 - IPC C07D498/04 C07D498/14 C07D519/00 A61K31/4162 A61K31/4188 A61K31/4196 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to benzoxazepin compounds of formula I exhibiting PI3 kinase inhibitory activity, pharmaceutical composition based thereon, use thereof and to a kit for treatment. In general formula I Z¹ denotes CR¹ or N, Z² denotes CR² or N, Z³ denotes CR³ or N, Z⁴ denotes CR⁴ or N, B denotes pyrazoline or imidazoline cycle substituted with A and condensed with benzoxepine cycle, R¹, R², R³ and R⁴ are independently selected from H, F, Cl, Br, -CN, -CO₂R¹⁰, -C(=O)N(R¹⁰)OR¹¹, -C(=O)NR¹⁰R¹¹, -NR¹⁰R¹¹, -NR¹²C(=O)NR¹⁰R¹¹, -NR¹²(C₁-C₁₂alkylene)NR¹⁰R¹¹, -NR¹²(C₁-C₁₂alkylene)OR¹⁰, -NR¹²(C₁-C₁₂alkylene)C(=O)NR¹⁰R¹¹, -OR¹⁰, C₁-C₁₂alkyl, C₃-C₆carbocyclyl, 4-8-membered heterocyclyl with 1-2 heteroatoms selected from N and O, phenyl, 5-6-member heteroaryl with 1-2 nitrogen and oxygen atoms, -(4-6-member heterocyclic ring with 1-2 nitrogen atoms)-(C₁-C₁₂alkyl), -phenyl (C₁-C₁₂alkyl), -(5-member heteroaryl with 1-2 nitrogen atoms)-(C₁-C₁₂alkyl), -(C₁-C₁₂alkylene)-(5-6-member heterocyclic ring with 1-2 nitrogen atoms), -(C₁-C₁₂alkylene)-(6-member heterocyclyl with 2 nitrogen atoms)-(C₁-C₁₂alkyl), -(C₁-C₁₂alkylene)C(=O)OR¹⁰, -(C₁-C₁₂alkylene)-NR¹⁰R¹¹.

EFFECT: compounds may be used in treatment of PI3K-mediated cancer.

16 cl, 4 tbl