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    Certain substituted ureas, as modulators of kinase activity
    1.
    发明授权
    Certain substituted ureas, as modulators of kinase activity 有权
    某些取代的脲，作为激酶活性的调节剂

    公开(公告)号：US08222421B2

    公开(公告)日：2012-07-17

    申请号：US12840246

    申请日：2010-07-20

    申请人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    发明人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  David R. Brittelli ,  Pavel Zhichkin ,  Matthew E. Voss

    IPC分类号： C07D215/38

    CPC分类号： C07D471/04 ,  C07D401/06

    摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    摘要翻译： 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物及其前体药物。 还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。

    Certain substituted diphenyl ureas, as modulators of kinase activity
    6.
    发明授权
    Certain substituted diphenyl ureas, as modulators of kinase activity 有权
    某些取代的二苯脲，作为激酶活性的调节剂

    公开(公告)号：US07625931B2

    公开(公告)日：2009-12-01

    申请号：US11331347

    申请日：2006-01-13

    申请人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  Robert W. DeSimone ,  Douglas A. I. Pippin

    发明人： Scott A. Mitchell ,  Mihaela Diana Danca ,  Peter A. Blomgren ,  Robert W. DeSimone ,  Douglas A. I. Pippin

    IPC分类号： A61K31/4439 ,  C07D403/02

    CPC分类号： C07D401/04 ,  C07D401/06

    摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

    摘要翻译： 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。 本文还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物，其选自载体，佐剂和赋形剂。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。