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    Combination for treatment of proliferative diseases
    1.
    发明授权
    Combination for treatment of proliferative diseases 失效
    用于治疗增殖性疾病的组合

    公开(公告)号：US5744460A

    公开(公告)日：1998-04-28

    申请号：US612775

    申请日：1996-03-07

    申请人： Marcel Muller ,  Thomas Geiger ,  Karl-Heinz Altmann ,  Doriano Fabbro ,  Nicholas M. Dean ,  Brett Monia ,  Clarence Frank Bennett

    发明人： Marcel Muller ,  Thomas Geiger ,  Karl-Heinz Altmann ,  Doriano Fabbro ,  Nicholas M. Dean ,  Brett Monia ,  Clarence Frank Bennett

    IPC分类号： A61K45/06 ,  A61K31/44 ,  A61K31/445 ,  A61K31/505 ,  A61K31/53 ,  A61K31/70 ,  A61K48/00 ,  C07H21/04

    CPC分类号： A61K31/70 ,  A61K45/06

    摘要： The invention relates to combinations of PKC-targeted (especially PKC-.alpha.-targeted) deoxyribo- and ribo-oligonucleotides and derivatives thereof with other chemotherapeutic compounds, as well as to pharmaceutical preparations and/or therapies, in relation to disease states which respond to such oligonucleotides or oligonucleotide derivatives, especially to to modulation of the activity of a regulatory protein. In particular, the invention relates to products or combinations comprising antisense oligonucleotides or oligonucleotide derivatives targeted to nucleic acids encoding human PKC and other (preferably standard) chemotherapeutics, either in fixed combination or for chronologically staggered or simultaneous administration, and the combined use of both classes of compounds, either in fixed combination or for chronologically staggered or simultaneous administration, for the treatment of proliferative diseases, especially tumor diseases, that can be treated by inhibition of PKC activity, that is, where the antisense oligonucleotides or oligonucleotide derivatives are targeted to nucleic acids encoding the regulatory protein PKC or active mutated derivatives thereof.

    摘要翻译： 本发明涉及PKC靶向（特别是PKC-α靶向的）脱氧核糖核苷酸和核糖寡核苷酸及其衍生物与其它化学治疗化合物的组合，以及关于响应于所述药物的疾病状态的药物制剂和/或治疗 这样的寡核苷酸或寡核苷酸衍生物，特别是调节调节蛋白的活性。 特别地，本发明涉及包含针对编码人PKC的核酸的反义寡核苷酸或寡核苷酸衍生物或其它（优选标准的）化学治疗剂的产品或组合，其以固定组合或按时间顺序交错或同时施用，以及两类的组合使用 的化合物，以固定组合或按时间顺序交错或同时给药，用于治疗可通过抑制PKC活性治疗的增殖性疾病，特别是肿瘤疾病，即反义寡核苷酸或寡核苷酸衍生物靶向核酸 编码调节蛋白PKC的酸或其活性突变衍生物。

    Use of c-Src inhibitors alone or in combinaton with STI571 for the treatment of leukaemia
    3.
    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

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

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

    IPC分类号： A61K31/519

    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)-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
    7.
    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

    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。

    Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome
    8.
    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

    申请人： Paul W. Manley ,  Jurgen Mestan ,  Doriano Fabbro

    发明人： Paul W. Manley ,  Jurgen Mestan ,  Doriano Fabbro

    IPC分类号： A61K31/506 ,  A61P35/04 ,  A61P35/00

    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。