PYRAZOLE DERIVATIVES, USEFUL AS INHIBITORS OF PROTEIN KINASE Russian patent published in 2008 - IPC C07D403/12 C07D403/14 A61K31/517 A61K31/5377 A61P35/00 A61P3/10 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to the new pyrazole derivatives of formula (IIa) or their pharmaceutically acceptable salts, where: R^x and R^y banded with intervening atoms while deriving benzol or cyclohexylene rings, optionally substituted by R³; R¹ represents T-(ring D); ring D represents phenyl, optionally substituted by 1-2 groups R⁵, or naphtyl or imidazolyl or benzymidazolyl, optionally substituted by C₁-C₆alkyl group; T represents the linking; R² represents hydrogen, C₁-C₆alkyl or C₃-C₆cycloalkyl; R^2' represents hydrogen, or R² and R^2' is banded with their intervening atoms while deriving phenyl ring; R³ is selected from C₁-C₆alkyl, hydrogen, halogen, -OH, -NH₂, -NHOH, -NO₂, C₁-C₆alkoxy, optionally substituted -N(R⁴)₂; each R⁴ independently selected from C₁-C₆alkyl, -CO₂C₁-C₆alkyl or two R⁴ at the same nitrogen atom joined with nitrogen atom while deriving morpholine ring; each R⁵ represents one or two substitutes, independently selected from C₁-C₆alkyl, halogen, OH, -NH₂, -CF₃, C₁-C₆alkoxy, -COOH, -CO₂C₁-C₆alkyl, -NHCO-C₁-C₆aliphatic group, NHCO(C₁-C₆alkyl)N(R⁴)₂, -CONHC₁-C₆alkyl, -CONH(C₁-C₆alkyl)N(R⁴)₂, and -NHSO₂C₁-C₆alkyl. The compounds are useful as inhibitors of protein kinase, in particular as inhibitors Aurora-2 and GSK-3 for the treatment of cancer, diabetes and Alzheimer's disease. The subjects matter is also pharmaceutical composition on basis of their compounds and methods of the treatment of diseases mediated by the protein kinase.

EFFECT: production of new pyrazole derivatives - inhibitors of protein kinase.

25 cl, 12 tbl, 292 ex