PURINE COMPOUNDS INHIBITING PI3K, AND APPLICATION METHODS Russian patent published in 2014 - IPC C07D473/32 A61K31/52 A61P35/00 

FIELD: biotechnologies.

SUBSTANCE: invention refers to new purine compounds of formula I and their pharmaceutically acceptable salts that have properties of an inhibitor of lipidic kinases including p110 alpha and other isoforms of PI3K. In formula I , R¹ is chosen from H, C₁-C₁₂alkyl and -(C₁-C₁₂alkene)-(C₅-C₆ heterocyclyl), where heterocyclyl can contain 1-2 heteroatoms in a cycle, which are chosen from nitrogen, and in which alkyl and heterocyclyl are optionally replaced with one or more groups independently chosen from -NHCOCH₃, -NHS(O)₂CH₃, -OH, -S(O)₂N(CH₃)₂ and -S(O)₂CH₃; R² is chosen from C₁-C₁₂alkyl, -(C₁-C₆alkene)-(C₅-C₆heterocyclyl) or -(C₁-C₆alkene)-C(=O)-(C₅-C₆heterocyclyl), in each of which heterocyclyl contains 1-2 heteroatoms chosen from nitrogen and oxygen, -(C₁-C₆alkene)-(C₆aryl), where aryl is chosen from phenyl, and -(C₁-C₆alkene)-(C₅-C₆heteroaryl), where heteroaryl contains 1 atom of nitrogen, in which alkyl, heterocyclyl, aryl and heteroaryl are optionally replaced with one or more groups independently chosen from F, Cl, Br, I, CH₃, -CF₃, -CO₂H, -COCH₃, -CO₂CH₃, -CONHCH₃, -NHCOCH₃, -NH(SO)₂CH₃, -OH, -OCH₃, -S(O)₂N(CH₃)₂ and -S(O)₂CH₃; and R³ represents monocyclic heteroaryl chosen from derivatives of pyridine and pyrimidine, which are specified in Claim 1 of the invention formula.

EFFECT: applicability of a compound for treatment of proliferative diseases, such as cancer.

7 cl, 2 dwg 1 tbl, 59 ex