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    • 1. 发明申请
    • HUMAN ADAM-10 INHIBITORS
    • 人ADAM-10抑制剂
    • WO2009052200A2
    • 2009-04-23
    • PCT/US2008080021
    • 2008-10-15
    • EXELIXIS INCNAGANATHAN SRIRAMWILSON JOANNDICKMAN DANIEL A
    • NAGANATHAN SRIRAMWILSON JOANNDICKMAN DANIEL A
    • C07D241/04C07D401/12
    • 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.
    • 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。 此外,还提供了治疗形式的癌症,关节炎和与其中ADAM-10起关键作用的血管发生相关的疾病的方法。