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    Use of a kinase inhibitor for the treatment of particular resistant tumors
    1.
    发明授权
    Use of a kinase inhibitor for the treatment of particular resistant tumors 失效
    使用激酶抑制剂治疗特定抗性肿瘤

    公开(公告)号：US07803829B2

    公开(公告)日：2010-09-28

    申请号：US12295447

    申请日：2007-03-29

    申请人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Jurgen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    发明人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Jurgen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    IPC分类号： A61K31/415

    CPC分类号： A61K31/4162 ,  A61K31/44

    摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

    摘要翻译： 本发明提供了低分子量化合物，即1H-噻吩并[2,3-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。 本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

    USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS
    2.
    发明申请
    USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS 失效
    使用激酶抑制剂治疗特异性抗肿瘤药物

    公开(公告)号：US20100022532A1

    公开(公告)日：2010-01-28

    申请号：US12295447

    申请日：2007-03-29

    申请人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Jurgen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    发明人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Jurgen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    IPC分类号： A61K31/4162 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/496

    CPC分类号： A61K31/4162 ,  A61K31/44

    摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

    摘要翻译： 本发明提供了低分子量化合物，即1H-噻吩并[2,3-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。 本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

    Use of a kinase inhibitor for the treatment of particular resistant tumors
    3.
    发明授权
    Use of a kinase inhibitor for the treatment of particular resistant tumors 有权
    使用激酶抑制剂治疗特定抗性肿瘤

    公开(公告)号：US08084455B2

    公开(公告)日：2011-12-27

    申请号：US12293985

    申请日：2007-03-29

    申请人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Juergen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    发明人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Juergen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    IPC分类号： A61K31/497

    CPC分类号： A61K31/4162 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

    摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

    摘要翻译： 本发明提供了低分子量化合物，即四氢吡咯并[3,4-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。 本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。

    Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors
    4.
    发明申请
    Use of a Kinase Inhibitor for the Treatment of Particular Resistant Tumors 有权
    使用激酶抑制剂治疗特异抗性肿瘤

    公开(公告)号：US20100035876A1

    公开(公告)日：2010-02-11

    申请号：US12293985

    申请日：2007-03-29

    申请人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Juergen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    发明人： Daniele Fancelli ,  Antonella Isacchi ,  Michele Modugno ,  Juergen Moll ,  Luisa Rusconi ,  Chiara Soncini ,  Rosita Lupi

    IPC分类号： A61K31/5377 ,  C12N5/00 ,  A61K31/496 ,  A61K31/454 ,  G01N33/53

    CPC分类号： A61K31/4162 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

    摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.

    摘要翻译： 本发明提供了低分子量化合物，即四氢吡咯并[3,4-c]吡唑，显示出对ABL酪氨酸激酶的ATP口袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，也显示出显着的抑制效力，特别是对抗BCR-ABL抑制剂抗性的T315I ABL突变体。 本发明的化合物可用于治疗BCR-ABL抑制剂抗性ABL介导的疾病，例如伊马替尼耐药性慢性骨髓性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP口袋，特别是T315I突变体ABL激酶的化合物的筛选方法。