USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA
    14.
    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。

    Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome
    15.
    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
    17.
    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 PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS MEDIATED BY THE LEUCINE ZIPPER-AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK)
    18.
    发明申请
    USE OF PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS MEDIATED BY THE LEUCINE ZIPPER-AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK) 审中-公开
    用于治疗由拉皮钳和非甾体类ALPHA含运动激素(ZAK)介导的疾病的吡嗪酰胺苯甲酰胺衍生物的使用

    公开(公告)号:US20120015968A1

    公开(公告)日:2012-01-19

    申请号:US13254261

    申请日:2010-03-05

    IPC分类号: A61K31/506 A61P9/00 A61P35/00

    摘要: The invention relates to the use of a pyrimidylaminobenzamide derivative of formula I wherein the radicals have the meanings as defined herein, or of a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for use in the treatment of disorders mediated by ZAK, to the use of a pyrimidylaminobenzamide derivatives of formula I or pharmaceutically acceptable salt thereof in the treatment of disorders mediated by ZAK, and to a method of treating warm-blooded animals including humans suffering from disorders mediated by ZAK by administering to said warm-blooded animal in need of such treatment an effective dose of a pyrimidylaminobenzamide of formula I or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及式I的嘧啶基氨基苯甲酰胺衍生物的用途,其中基团具有本文定义的含义或其药学上可接受的盐在制备用于治疗由ZAK介导的病症的药物组合物中的用途 式I的嘧啶基氨基苯甲酰胺衍生物或其药学上可接受的盐在治疗由ZAK介导的病症中的应用,以及一种治疗温血动物(包括患有由ZAK介导的病症的人)的方法,该方法包括向所需的所述温血动物施用 这种治疗有效剂量的式I的嘧啶基氨基苯甲酰胺或其药学上可接受的盐。

    Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia
    20.
    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。