PYRAZOLOPYRIMIDINE DERIVATIVES AS A KINASE INHIBITOR Russian patent published in 2020 - IPC C07D487/04 C07D403/12 C07D403/14 C07D401/14 A61K31/519 A61K31/496 A61P35/00 A61P37/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to pyrazolopyrimidine derivative of general formula I or its pharmaceutically acceptable salt possessing activity with respect to JAK3 and BTK, as well as to pharmaceutical compositions based on them. In general formula I R₁ is benzothiazolyl, isothiazolyl, isoxazolyl, phenyl or pyrazolyl; where R₁ is unsubstituted or substituted with a substituent selected from a group consisting of piperazinyl, unsubstituted or substituted C_1-4 alkyl; benzyl substituted with C_1-4 alkoxy; one or two C_1-4 alkyl groups, unsubstituted or substituted morpholino, -N(C_1-4 alkyl)₂, C_1-4 alkoxy, cyano or -CONH(C_1-4 alkyl) group; C_1-4 haloalkyl; C_3-6 cycloalkyl; morpholino; -CO-(morpholino); morpholino and halogen; -N(C_1-4 alkyl)₂; -NHCO(C_2-4 alkenyl); -NHCO(pyrrolidinyl); C_1-4 alkoxy, unsubstituted or substituted with -N(C_1-4 alkyl)₂ group; phenoxy; pyrazolyl unsubstituted or substituted with one or two C_1-4 alkyl groups; pyrrolidinyl; and tetrahydropyranyl; R₂ is hydrogen, C_1-4 alkyl or halogen; R₃ is C_1-4 alkyl, unsubstituted or substituted with cyano or halogen; C_2-6 alkenyl unsubstituted or substituted with one or two substitutes independently selected from a group consisting of cyano, C_3-6 cycloalkyl and -N(C_1-4 alkyl)₂; or C_2-4 alkynyl, unsubstituted or substituted C_3-6 cycloalkyl, X_l is CR₄ or N, where R₄ is hydrogen, X₂ is CR₅, where R₅ is hydrogen, C_1-4 alkyl, halogen, cyano or C_1-4 alkylthio, X₃ is NR₆, O or S, where R₆ is hydrogen or C_1-4 alkyl, X₄ is CH or N, and X₅ is a bond or NH.

EFFECT: disclosed are pyrazolopyrimidine derivatives as a kinase inhibitor.

13 cl, 5 tbl, 194 ex