Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome
    5.
    发明申请
    Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome 有权
    嗜酸性粒细胞综合征的嘧啶基氨基苯甲酰胺衍生物

    公开(公告)号:US20080227800A1

    公开(公告)日:2008-09-18

    申请号:US11911562

    申请日:2006-05-02

    CPC分类号: A61K31/506

    摘要: The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of FIP1L1-PDGFRα-induced or TEL-PDGFRβ-induced myeloproliferative diseases, especially for the curative and/or prophylactic treatment of hypereosinophilic syndrome and hypereosinophilic syndrome with resistance to imatinib, and to a method of treating hypereosinophilic syndrome, chronic eosinophilic leukemia and hypereosinophilic syndrome with resistance to imatinib, or other diseases associated with FIP1L1-PDGFRα, TEL-PDGFRβ or similar mutations that activate PDGFR.

    摘要翻译: 本发明涉及嘧啶氨基苯甲酰胺衍生物用于制备用于治疗FIP1L1-PDGFRα诱导或TEL-PDGFRβ诱导的骨髓增生性疾病的药物的用途,特别是用于治疗和/或预防性治疗嗜酸性粒细胞增多综合征和嗜酸细胞过多综合征, 对伊马替尼的耐药性,以及治疗嗜酸性粒细胞综合征,慢性嗜酸细胞性白血病和对伊马替尼具有抗性的嗜酸性粒细胞综合征或与FIP1L1-PDGFRα,TEL-PDGFRβ或与激活PDGFR的类似突变相关的其它疾病的方法。

    Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia
    6.
    发明授权
    Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
    单独或与STI571组合使用c-Src抑制剂治疗白血病

    公开(公告)号:US08268837B2

    公开(公告)日:2012-09-18

    申请号:US11285664

    申请日:2005-11-22

    IPC分类号: 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。

    Use of c-Src inhibitors alone or in combinaton with STI571 for the treatment of leukaemia
    7.
    发明申请
    Use of c-Src inhibitors alone or in combinaton with STI571 for the treatment of leukaemia 审中-公开
    单独使用c-Src抑制剂或与STI571组合用于治疗白血病

    公开(公告)号:US20070027167A1

    公开(公告)日:2007-02-01

    申请号:US11515981

    申请日:2006-09-05

    IPC分类号: 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)-benzoylamdio]-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 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,Tec激酶家族或Raf激酶抑制剂的活性的化合物, 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。

    USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA
    8.
    发明申请
    USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA 审中-公开
    使用C-SRC抑制剂或与STI571组合用于治疗白血病

    公开(公告)号:US20070149539A1

    公开(公告)日:2007-06-28

    申请号:US11679901

    申请日:2007-02-28

    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)-benzoylamdio]-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 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,包括向动物施用至少一种抑制Src激酶家族成员,Tec激酶家族或Raf激酶抑制剂的活性的化合物, 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。

    USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA
    9.
    发明申请
    USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA 失效
    使用C-SRC抑制剂或与STI571组合用于治疗白血病

    公开(公告)号:US20090227608A1

    公开(公告)日:2009-09-10

    申请号:US12466186

    申请日:2009-05-14

    IPC分类号: A61K31/519 A61P35/00

    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。

    Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia
    10.
    发明申请
    Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
    单独或与STI571组合使用c-Src抑制剂治疗白血病

    公开(公告)号:US20060074094A1

    公开(公告)日:2006-04-06

    申请号:US11285664

    申请日:2005-11-22

    IPC分类号: 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。