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    • 3. 发明申请
    • Chemical compounds
    • 化合物
    • US20060128745A1
    • 2006-06-15
    • US11336010
    • 2006-01-20
    • Karen LackeyEdgar Wood
    • Karen LackeyEdgar Wood
    • A61K31/4745C07D471/02
    • C07D471/04
    • The present invention is related to aza-oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
    • 本发明涉及氮杂 - 羟基吲哚衍生物,含有它们的组合物及其使用和制造方法。 这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用,特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。 这种疾病状态包括肿瘤生长,再狭窄,动脉粥样硬化,疼痛和血栓形成。 特别地,本发明涉及一系列取代的羟吲哚化合物,其表现出Trk家族蛋白酪氨酸激酶抑制,并且其可用于癌症治疗和慢性疼痛适应症。