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    • 8. 发明授权
    • Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia
    • 单独或与STI571组合使用c-Src抑制剂治疗白血病
    • US08268837B2
    • 2012-09-18
    • US11285664
    • 2005-11-22
    • Nicholas J DonatoDoriano FabbroPaul W ManleyJurgen MestanMarkus WarmuthMichael HallekMoshe TalpazJi Wu
    • Nicholas J DonatoDoriano FabbroPaul W ManleyJurgen MestanMarkus WarmuthMichael HallekMoshe TalpazJi Wu
    • A61K31/519
    • A61K35/02A61K31/506A61K31/519
    • The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
    • 本发明涉及一种组合,其包含(a)至少一种降低c-Src活性的化合物和(b)N- {5- [4-(4-甲基 - 哌嗪基 - 甲基) - 苯甲酰氨基] -2-甲基苯基} -4-(3-吡啶基)-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病,特别是慢性骨髓性白血病的温血动物的方法,包括向所述动物施用至少一种抑制Src激酶家族成员,Btk激酶家族,Tec激酶家族的活性的化合物或 Raf激酶抑制剂,特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性,单独或与Bcr-Abl抑制剂组合,特别是N - {5- [4-(4-甲基 - 哌嗪子基 - 甲基) - 苯甲酰氨基] -2-甲基苯基} -4-(3-吡啶基)-2-嘧啶胺。