公开(公告)号：US20090227608A1

公开(公告)日：2009-09-10

申请号：US12466186

申请日：2009-05-14

申请人： Nicholas J. Donato ,  Doriano Fabbro ,  Paul William Manley ,  Jurgen Mestan ,  Markus Warmuth ,  Michael Hallek ,  Moshe Talpaz ,  Ji Wu

发明人： Nicholas J. Donato ,  Doriano Fabbro ,  Paul William Manley ,  Jurgen Mestan ,  Markus Warmuth ,  Michael Hallek ,  Moshe Talpaz ,  Ji Wu

IPC分类号： A61K31/519 ,  A61P35/00

CPC分类号： A61K35/02 ,  A61K31/506 ,  A61K31/519

摘要： 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.

摘要翻译： 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。