PYRIMIDINE-SUBSTITUTED PURINE DERIVATIVES, PHARMACEUTICAL COMPOSITION BASED THEREON, METHOD OF PROTEIN KINASE INHIBITION, METHOD OF TREATING OR PREVENTING DISEASES SENSITIVE TO PROTEIN KINASE INHIBITION AND METHOD OF TREATING PROLIFERATIVE DISEASES Russian patent published in 2014 - IPC C07D473/32 A61K31/52 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to purine compounds of the formula (I):

,

wherein R¹ is specified in a group containing H, halogen and C₁-C₆alkyl, R² is specified in a group containing H, CN, an optionally substituted C₁-C₁₂alkyl, an optionally substituted C₃-C₁₂cycloalkyl, an optionally substituted C₂-C₁₂heterocycloalkyl, an optionally substituted C₆-C₁₈aryl, an optionally substituted C₁-C₁₂alkyloxy, COR⁸, COOH, COOR⁸, CONR⁸R⁹ and acyl; if R² represents the optionally substituted C₆-C₁₈aryl, the above optional substitute is specified in F and CH₃; if R² represents the optionally substituted C₁-C₁₂alkyl, the above optional substitute is specified in CH₃, OCH₃ and O-C(CH₃)₃; if R² represents the optionally substituted C₃-C₁₂cycloalkyl, the above optional substitute represents CH₃; if R² represents the optionally substituted C₂-C₁₂heterocycloalkyl, the above optional substitute is specified in a group consisting of COOC(CH₃)₃, CO(CH₂)₂CH₃, COPh and CO(5-methylthiophen-2-yl), each R³ and R⁴ is independently specified in a group containing H, C₁-C₆alkyl and OR⁸, R⁶ is specified in a group containing H, OH, OR⁸, CH₂OH, NH₂ and NR⁸R⁹, or R⁸ and R⁹ if taken together with atoms attached thereto form a cyclic group, each R⁸ and R⁹ is independently specified in a group containing H and C₁-C₁₂alkyl; each R² independently represents C₁-C₆alkyl, q represents an integer specified in a group containing 0 and 1, X represents a group of formula (CR¹⁰ ₂)_m, each R¹⁰ is independently specified in a group containing H and C₁-C₆ alkyl, m represents an integer specified in a group containing 0, 1, 2 and 3, C₂-C₁₂heterocycloalkyl contains at least one heteroatom specified in a group containing O, N and S, in at least one ring; each ring is 3- to 10-merous, or their pharmaceutically acceptable salts or N-oxides.

EFFECT: compounds may be effective as agents for a number of proliferative diseases or disorders, including tumours and malignant growth, as well as other PI3K and/or mTOR kinase related disorders or diseases.

31 cl, 3 tbl, 5 ex