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    1,2,4-benzotriazine-1,4-dioxides
    3.
    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。

    Novel 1,2,4-benzotriazine-1,4-dioxides
    4.
    发明申请
    Novel 1,2,4-benzotriazine-1,4-dioxides 有权
    新的1,2,4-苯并三嗪-1,4-二氧化物

    公开(公告)号：US20070197534A1

    公开(公告)日：2007-08-23

    申请号：US10590796

    申请日：2005-03-01

    申请人： William Denny ,  Michael Hay ,  Kevin Hicks ,  Frederik Pruijn ,  William Wilson ,  Karin Pchalek

    发明人： William Denny ,  Michael Hay ,  Kevin Hicks ,  Frederik Pruijn ,  William Wilson ,  Karin Pchalek

    IPC分类号： C07D253/08 ,  A61K31/28 ,  A61K31/53

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

    摘要： The present invention provides a simplified set of characteristics that can be used to select 1,2,4 benzotriazine 1,4 dioxide compounds (TPZ analogues) with therapeutic activity against hypoxic cells in human tumour xenografts, and to further provide a novel class of 1,2,4-benzotriazine-1,4-dioxides (TPZ analogues) with predicted in vivo activity against tumours, to their preparation, and to their use as hypoxia-selective cytotoxic drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.

    摘要翻译： 本发明提供了可用于选择具有对人类肿瘤异种移植物中的缺氧细胞具有治疗活性的1,2,4苯并三嗪二氧化物化合物（TPZ类似物）的简化特征集，并进一步提供新的1类 ，具有预测的针对肿瘤的体内活性的2,4-苯并三嗪-1,4-二氧化物（TPZ类似物），其制备及其作为用于癌症治疗的缺氧选择性细胞毒性药物和放射增敏剂的用途，单独或与 辐射和/或其他抗癌药物。