COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS Russian patent published in 2010 - IPC C07D403/04 A61K31/506 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I), specifically compounds of formula (Ia) which have inhibiting activity during activity of kinase selected from Abl, BCR-AbI, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2a2, MKK4, c-RAF, MKK6, SAPK2a and SAPK2P and pharmaceutical compositions containing such compounds. In the compound of formula I, Ia, m and n are equal to 0; R₁ denotes XNR₅R₆, where X denotes a bond; R₅ is selected from hydrogen, C_1-6alkyl, phenyl, C_5-10heteroaryl-C_0-4alkyl, C_3-6cycloalkyl and C_3-10heterocycloalkyl-C_0-4alkyl, where the heteroaryl and heterocycloalkyl contain 1-2 heteroatoms selected from nitrogen and oxygen; and R₆ is selected from hydrogen and C_1-6alkyl; or R₅ and R₆ together with the nitrogen atom with which both are bonded form a heteroaryl or heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl and heterocycloalkyl, R₅ or a combination of R₅ and R₆ can be optionally substituted with 1-3 radicals independently selected from a halogen group, C_1-6alkyl, C_1-6alkoxy group, halogen-substituted alkyl, -XNR₇R₈, -XOR₇, -XR₈, -XC(O)NR₇R₈, -XC(O)NR₇XNR₇R₈, -XNR₇C(O)R₈, -XR₉; where X denotes a bond or C_1-4alkylene; R₇ and R₈ are independently selected from a group consisting of hydrogen and C_1-4alkyl;and R₈ is selected form C_5-6heterocycloalkyl and C_5-6heteroaryl; where said heterocycloalkyl or heteroaryl contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R₈ is optionally substituted with a radical selected from a group consisting of C_1-4alkyl and XOR₇; R₃ denotes -NR₁₀R₁₁; where R₁₀ denotes hydrogen; R₁₁ denotes phenyl; where phenyl in R₁₁ is optionally substituted with 1-3 radicals selected from a halogen group, C_1-6alkyl, C_1-6alkoxy group, halogen-substituted alkyl, halogen-substituted alkoxy group, -NR₁₂C(O)R₁₃, -NR₁₂C(O)NR₁₂R₁₃ and -NR₁₂S(O)_0-2R₁₃; where R₁₂ denotes hydrogen; R₁₃ is selected from phenyl, C_5-6heteroaryl and C_5-6heterocycloalkyl; where any of phenyl, heteroaryl, cycloalkyl or heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R₁₃ is substituted with 1-3 radicals independently selected from a halogen group, C_1-6alkyl, halogen-substituted C_1-6alkyl, C_1-6alkoxy group, halogen-substituted C_1-6alkoxy group, -XNR₇R₈, phenyl-C_0-4alkyl, C_5-6heteroaryl-C_0-4alkyl, C_5-6heterocycloalkyl-C_0-4alkoxy group and C_5-6heterocycloalkyl-C_0-4alkyl; where X, R₇ and R₈ are described above, and where any of the phenyl, heteroaryl or heterocycloalkyl fragments contain 1-2 heteroatoms selected from nitrogen and oxygen, and said heterocycloalkyl or heteroaryl in R₁₃ optionally further substituted with 1-3 radicals independently selected from a halogen group, C_1-6alkyl, halogen-substituted C_1-6alkyl, hydroxy-substituted C_1-6alkyl, C_1-6alkoxy group; R₁₅ and R₁₆ are selected from phenyl substitutes given in values of R₁₁ and R₁₂ for formula I compounds.

EFFECT: compounds can be used to treat or prevent such diseases as proliferative disorders, and diseases resulting from anomalous activation of the immune and nervous systems.

8 cl, 1 tbl, 1 dwg, 1 ex