COMPOUNDS AND COMPOSITIONS AS PROTEIN TYROSINE KINASE INHIBITORS Russian patent published in 2010 - IPC C07D403/14 C07D403/04 C07D401/14 C07D409/14 C07D413/14 A61K31/496 A61K31/505 A61K31/5377 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula Ia: and its pharmaceutically acceptable salt, where: p equals 0 or 1; n assumes values from 1 to 3, q equals 1; R₅ is selected from hydrogen, -XNR₇R₈, pyrimidine-C_0-4alkyl, pyridine-C_0-4alkyl, phenyl, C_3-10cycloalkyl-C_0-4alkyl and C_3-6heterocycloalkyl-C_0-4alkyl, where C_3-6heterocycloalkyl is a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R is hydrogen or C_1-4alkyl; R₇ and R₈ represent C_1-4alkyl; R₆ denotes hydrogen; or R₅ and R₆ together with a nitrogen atom to which they are both bonded form morpholine or piperidine; where any piperdine-C_0-4alkyl, piperidine-C_0-4alkyl or C_3-10cycloalkyl-C_0-4alkyl of substitute R₅ or a combination of radicals R₅ and R₆ can be optionally substituted with 1-2 radicals which are independently selected from -XNR₇R₈ and -XOR₇, the said phenyl of substitute R₅ is substituted with a -XR₉ group, the said C_3-6heterocycloalkyl-C_0-4alkyl of substitute R₅ is optionally substituted with a -XOR₇ group, where X is a single bond or C_1-4alkylene; R₇ and R₈ are independently selected from hydrogen and C_1-4alkyl; R₉ is selected from C_3-10heterocycloalkyl which is a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R is as given above; R₁₀ denotes hydrogen; R₁₅ is selected from halogen, C_1-6alkyl and C_1-6alkoxy; and R₁₆ is selected from halogen, methoxy, nitro, -NR₁₂C(O)R₁₃, -C(O)NR₁₂R₁₂, -NR₁₂R₁₂, -C(O)OR₁₂ and -C(O)NR₁₂R₁₃; each R₁₂ is selected from hydrogen and C_1-6alkyl; R₁₃ is selected from phenyl, thienyl, pyrazolyl, pyridinyl or isoxazolyl, where any phenyl, thienyl, pyrazolyl, pyridinyl or isoxazolyl of substitute R₁₃ can be optionally substituted with 1-2 radicals which are independently selected from halogen, C_1-6alkyl, halogen-substituted C_1-6alkyl, imidazole-C_0-4alkyl, C_3-10cycloalkyl, C_3-10heterocycloalkyl-C_0-4alkoxy and C_3-10heterocycloalkyl-C_0-4alkyl; where the said C_3-10heterocycloalkyl-C_0-4alkoxy and C_3-10heterocycloalkyl-C_0-4alkyl each represent a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R assumes values given above; and the said C_3-10heterocycloalkyl-C_0-4alkoxy and C_3-10heterocycloalkyl-C_0-4alkyl can each be optionally substituted with 1 radical independently selected from C_1-6alkyl, hydroxyl-substituted C_1-6alkyl and NR₇R₈, where R₇ and R₈ assume values given above. The invention also relates to pharmaceutical compositions containing the said compounds.

EFFECT: obtaining novel compounds and compositions based on the said compounds which can be used in medicine for treating and preventing diseases or disorders associated with abnormal or uncontrolled kinase activity, particularly diseases or disorders associated with abnormal activity of kinase c-Src, FGFR3, KDR and/or Lck.

12 cl, 1 tbl, 2 ex