HETEROARYL COMPOUNDS, THEIR COMPOSITIONS AND USE THEREOF AS PROTEIN KINASE INHIBITORS Russian patent published in 2013 - IPC C07D473/00 C07D475/00 A61K31/52 A61K31/522 A61K31/519 A61P35/00 A61P29/00 A61P37/00 

FIELD: medicine.

SUBSTANCE: invention refers to new heteroaryl compounds of general formula (I) and their pharmaceutically acceptable salts possessing the properties of protein kinase inhibitor, such as mTOR, IKK-2, Tyk2, Syk-kinase. In formula (I) R¹ represents substituted or unsubstituted C_1-8alkyl, substituted or unsubstituted aryl, specified in phenyl, substituted or unsubstituted 5-6-member heteroaryl with 1-3 nitrogen atoms in a cycle specified in pyridine, pyrazole, indole, indazole, triazole, benzimidazole, 2-(1H-imidazo-[4,5-b]pyridine, substituted or unsubstituted 5-7- member cycloalkyl or substituted or unsubstituted heterocycloalkyl specified in pyrrolidinyl; -X-A-B-Y- taken together form -N(R²)CH₂C(O)NH-, -N(R²)C(O)CH₂NH-, -N(R²)C(O)NH-, -N(R²)C=N- or -C(R²)=CHNH-; L represents a direct bond, NH or O; R² represents substituted or unsubstituted C_1-8alkyl, substituted or unsubstituted aryl specified in phenyl, tetrahydronaphthalene, unsubstituted 5-7- member mono- or 8- member bicycloalkyl; and R³ and R⁴ independently represent H or C_1-8alkyl. The substitutes in the substituted groups are specified in one or more halogen, C_1-8alkyl, hydroxyl, amino, nitro, thiol, C_1-4alkyl thioether, cyano, carboxyl, C_1-4alkyl ester, halogen alkyl, C₆cycloalkyl or heteroaryl specified in pyridyl, triazole, O-lower alkyl, aryl specified in phenyl, phenyl-lower alkyl, CO₂CH₃, CONH₂, OCHF₂, CF₃ or OCF₃ groups wherein CONH₂ group may be substituted by cyclohexyl.

EFFECT: compounds can find application for treating or preventing cancer, inflammatory pathological conditions, metabolic pathological conditions.

24 cl, 8 dwg, 2 tbl, 169 ex