IMIDAZO[1,2-b]PYRIDAZINE AND PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND USE THEREOF AS PROTEIN KINASE INHIBITOR Russian patent published in 2013 - IPC C07D487/04 A61K31/5025 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives of the following structures (I) and (II) wherein X represents NH or O; R represents H or C_1-6alkyl; R₁ represents a structure specified in wherein R₁' means a substitution in n-, o- or m-positions by one or more substitutes from halogen, -OCF₃, -CF₃ or -OCH₃; R₂ represents -(CH₂)_1;2-piperid-4-yl or substituted -(CH₂)_1,2-piperid-4-yl, substituted by C_1-6alkyl or C(O)cyclopropyl; or R₂ represents -(CH₂)_n-cyclohexyl wherein n means 0 or 1, wherein -(CH₂)_n-cyclohexyl is optionally substituted by one or more substitutes specified in halogen, oxo, cyano, amino, alkylamino, alkyl, alkoxy, hydroxyalkyl, morpholinyl, -NR_eC(=O)R_f, -S(=O)₂NH₂, -NR_eS(=O)₂R_f, wherein R_f and R_e are identical or different and independently represent hydrogen, alkyl or morpholinylalkyl. The invention also refers to a composition possessing activity inhibiting Pim-1 kinase activity.

EFFECT: there are produced new compounds and composition on their basis which can find application in medicine for treating cancer expressing Pim-1 kinase.

13 cl, 5 dwg, 9 tbl, 9 ex