SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TROPOMYOSIN-RELATED KINASE INHIBITORS Russian patent published in 2014 - IPC C07D471/04 C07D487/04 C07D413/14 A61K31/519 A61K31/5377 A61P25/28 A61P35/00 A61P31/00 A61P25/04 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in formula R¹ is H or (1-6C alkyl); R² represents NR^bR^c, (1-4C)alkyl, (1-4C)fluoroalkyl, CF₃, (1-4C)hydroxyalkyl, -(1-4Calkyl)hetAr¹, -(1-4Calkyl)NH₂, -(1-4C alkyl)NH(1-4Calkyl), -(1-4Calkyl)N(1-4Calkyl)₂, hetAr², hetCyc¹, hetCyc², phenyl substituted where applicable by NHSO₂(1-4Calkyl) or (3-6C)cycloalkyl, substituted where applicable by (1-4C alkyl), CN, OH, OMe, NH₂, NHMe, N(CH₃)₂, F, CF₃, CO₂(1-4C alkyl), CO₂H; C(=O)NR^eR^f or C(=O)OR^g; R^b is H or (1-6C alkyl); R^c represents H, (1-4C)alkyl, (1-4C)hydroxyalkyl, hetAr³ or phenyl, wherein the above phenyl is substituted where applicable by one or more substitutes independently from halogen, CN, CF₃ and -O(1-4C alkyl); R^e represents H or (1-4C)alkyl; R^f represents H, (1-4C)alkyl or (3-6C)cycloalkyl; R^g represents H or (1-6C)alkyl; X is absent or represents -CH₂-, -CH₂CH₂-, -CH₂O- or -CH₂NR^d; R^d represents H or (1-4C alkyl); R³ represents H or (1-4C alkyl); and n is equal to 0-6. The radical values NR^bR^c, Y, hetAr¹, hetAr², hetAr³, hetCyc¹, hetCyc², NR^eR^f, R⁴ are specified in the patent claim. The invention also refers to a pharmaceutical composition containing the above compounds, to a method of treating Trk kinase mediated diseases and conditions, such as pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection, osteolytic disease, and to a method of preparing the above compounds.

EFFECT: invention refers to new derivatives of pyrazolo[1,5-a]pyrimidines possessing an inhibitory activity on tropomyosin-related kinases (Trk).

42 cl, 1 tbl, 105 ex