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    Certain substituted ureas, as modulators of kinase activity
    2.
    发明申请
    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：US20060270702A1

    公开(公告)日：2006-11-30

    申请号：US11415419

    申请日：2006-05-02

    Applicant: Scott Mitchell ,  Mihaela Danca ,  Peter Blomgren ,  David Brittelli ,  Pavel Zhichkin ,  Matthew Voss

    Inventor： Scott Mitchell ,  Mihaela Danca ,  Peter Blomgren ,  David Brittelli ,  Pavel Zhichkin ,  Matthew Voss

    IPC: C07D471/02 ,  C07D403/02 ,  A61K31/4745

    CPC classification number: C07D471/04 ,  C07D401/06

    Abstract: 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.

    Abstract translation: 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 ureas as modulators of kinase activity
    3.
    发明申请
    Certain substituted ureas as modulators of kinase activity 审中-公开
    某些取代的脲类作为激酶活性的调节剂

    公开(公告)号：US20060199846A1

    公开(公告)日：2006-09-07

    申请号：US11331346

    申请日：2006-01-13

    Applicant: Scott Mitchell ,  Mihaela Danca ,  Peter Blomgren ,  Robert DeSimone ,  Douglas Pippin ,  David Brittelli

    Inventor： Scott Mitchell ,  Mihaela Danca ,  Peter Blomgren ,  Robert DeSimone ,  Douglas Pippin ,  David Brittelli

    IPC: A61K31/4439 ,  C07D403/02

    CPC classification number: C07D401/14 ,  C07D401/06

    Abstract: 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.

    Abstract translation: 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。

    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    5.
    发明申请
    Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 审中-公开
    通过取代的联芳基氧代丁酸抑制基质金属蛋白酶

    公开(公告)号：US20050267102A1

    公开(公告)日：2005-12-01

    申请号：US11168664

    申请日：2005-06-27

    Applicant: Michael VanZandt ,  David Brittelli ,  Brian Dixon

    Inventor： Michael VanZandt ,  David Brittelli ,  Brian Dixon

    IPC: A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32 ,  C07D253/08

    CPC classification number: C07D253/08 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4706 ,  A61K31/502 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5513 ,  C07C62/38 ,  C07D237/32

    Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

    Abstract translation: 提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式：其中r为0-2，T选自并且R 40是单或双杂环结构。 这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，溃疡性溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症 反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。

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