Human Adam-10 Inhibitors
    1.
    发明申请
    Human Adam-10 Inhibitors 审中-公开
    人类Adam-10抑制剂

    公开(公告)号:US20140206865A1

    公开(公告)日:2014-07-24

    申请号:US14221937

    申请日:2014-03-21

    IPC分类号: C07D241/04 C07D401/12

    摘要: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.

    摘要翻译: 本发明提供了用于抑制ADAM-10蛋白质的化合物,具有选择性对MMP-1。 这些化合物可用于体外研究ADAM-10(及其抑制)在生物过程中的作用。 本发明还包括药物组合物,其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症,关节炎和与血管发生相关的疾病。 相应地,本发明还包括治疗癌症,关节炎和与血管生成有关的疾病形式的方法,其中ADAM-10起关键作用。

    Receptor-Type Kinase Modulators and Methods of Use
    2.
    发明申请
    Receptor-Type Kinase Modulators and Methods of Use 有权
    受体型激酶调节剂和使用方法

    公开(公告)号:US20140155418A1

    公开(公告)日:2014-06-05

    申请号:US14060123

    申请日:2013-10-22

    IPC分类号: C07D403/12

    摘要: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

    摘要翻译: 本发明提供用于调节受体激酶活性的化合物,特别是ephrin和EGFR,以及利用其化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。 由受体激酶活性介导的疾病包括但不限于由细胞增殖异常水平(即肿瘤生长),程序性细胞死亡(细胞凋亡),细胞迁移和与肿瘤生长相关的血管生成的特征的疾病。 本发明的化合物包括“光谱选择性”激酶调节剂,抑制,调节和/或调节受体型酪氨酸激酶(包括ephrin和EGFR)亚家族的信号转导的化合物。

    Methods of Treating Aneurysmal Dilatation, Blood Vessel Wall Weakness and Specifically Abdominal Aortic and Thoracic Aneurysm Using Matrix Metalloprotease-2 Inhibitors
    3.
    发明申请
    Methods of Treating Aneurysmal Dilatation, Blood Vessel Wall Weakness and Specifically Abdominal Aortic and Thoracic Aneurysm Using Matrix Metalloprotease-2 Inhibitors 审中-公开
    使用基质金属蛋白酶-2抑制剂治疗动脉瘤扩张,血管壁弱点和具体的腹主动脉和胸腔动脉瘤的方法

    公开(公告)号:US20120270884A1

    公开(公告)日:2012-10-25

    申请号:US13497726

    申请日:2010-09-30

    IPC分类号: A61K31/495 A61P9/00

    摘要: The present invention provides methods of treating aneurysmal dilatation, blood vessel wall weakness, and specifically abdominal aortic aneurysm and thoracic aneurysm by inhibiting MMPs and ADAM-IO. Such compounds are useful in the in vitro study of the role of MMPs and ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more MMPs or ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm. The invention also comprises methods of treating aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm utilizing the compounds of the invention in conjunction with inhibitors of angiotensin II, including angiotensin II receptor blockers and angiotensin converting enzyme inhibitors, and cyclophillin inhibitors.

    摘要翻译: 本发明提供了通过抑制MMP和ADAM-10来治疗动脉瘤扩张,血管壁虚弱,特别是腹主动脉瘤和胸动脉瘤的方法。 这些化合物可用于体外研究MMPs和ADAM-10(及其抑制)在生物过程中的作用。 本发明还包括药物组合物,其包含根据本发明的一种或多种MMP或ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗动脉瘤扩张或血管壁无力,例如腹主动脉瘤和胸动脉瘤。 本发明还包括利用本发明化合物与血管紧张素II抑制剂(包括血管紧张素II受体阻断剂和血管紧张素转换酶抑制剂)和环磷酰胺转移酶抑制剂联合治疗动脉瘤扩张或血管壁虚弱的方法,例如腹主动脉瘤和胸动脉瘤 抑制剂。

    Human ADAM-10 inhibitors
    7.
    发明授权
    Human ADAM-10 inhibitors 有权
    人ADAM-10抑制剂

    公开(公告)号:US08426415B2

    公开(公告)日:2013-04-23

    申请号:US12682874

    申请日:2008-10-15

    CPC分类号: C07D241/04 C07D401/12

    摘要: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.

    摘要翻译: 提供了可用于抑制ADAM-10蛋白的化合物的镁盐/络合物及其制备和纯化方法。 还提供了包含化合物的镁盐/复合物与药学上可接受的载体组合的组合物。 与包含它们的组合物一样,这些化合物可用于治疗癌症,关节炎,与血管生成有关的疾病,例如肾脏疾病,心脏病如心力衰竭,动脉粥样硬化和中风,炎症,溃疡,不育症,硬皮病,子宫内膜异位症 ,间皮瘤和糖尿病。 另外,还提供了治疗ADAM-10起关键作用的癌症,关节炎和血管生成相关疾病形式的方法。