| 摘要 |
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 Calkyl; Rrepresents a structure specified inwherein R' means a substitution in n-, o- or m-positions by one or more substitutes from halogen, -OCF, -CFor -OCH; Rrepresents -(CH)-piperid-4-yl or substituted -(CH)-piperid-4-yl, substituted by Calkyl or C(O)cyclopropyl; or Rrepresents -(CH)-cyclohexyl wherein n means 0 or 1, wherein -(CH)-cyclohexyl is optionally substituted by one or more substitutes specified in halogen, oxo, cyano, amino, alkylamino, alkyl, alkoxy, hydroxyalkyl, morpholinyl, -NRC(=O)R, -S(=O)NH, -NRS(=O)R, wherein Rand Rare 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 |
