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    1,2,4-benzotriazine-1,4-dioxides
    2.
    发明授权
    1,2,4-benzotriazine-1,4-dioxides 有权
    1,2,4-苯并三嗪-1,4-二氧化物

    公开(公告)号：US07816521B2

    公开(公告)日：2010-10-19

    申请号：US10590796

    申请日：2005-03-01

    申请人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    发明人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    IPC分类号： C07D253/10 ,  C07D413/12 ,  A61K31/53 ,  A61P35/00

    CPC分类号： C07D253/10 ,  C07D253/08 ,  C07D401/12

    摘要： The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.

    摘要翻译： 化合物3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物及其药理学上可接受的盐。 还描述了在受试者中治疗癌症的方法，其中给予3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药理学上可接受的盐 到缺氧环境中的肿瘤细胞。 还描述了通过向受试者施用含有3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-恶二唑的药物组合物，在缺氧条件下的实体瘤的受试肿瘤细胞中放射增敏的方法， 苯并三嗪1,4-二氧化物或其药理学上可接受的盐，其量足以在肿瘤细胞中产生放射敏感性，并对肿瘤细胞进行辐射。 另外提供含有治疗有效量的3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药学上可接受的盐和药学上可接受的盐的药物组合物 可接受的赋形剂，佐剂，载体，缓冲液或稳定剂。