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    • 7. 发明授权
    • 1,2,4-benzotriazine-1,4-dioxides
    • 1,2,4-苯并三嗪-1,4-二氧化物
    • US07816521B2
    • 2010-10-19
    • US10590796
    • 2005-03-01
    • William Alexander DennyMichael Patrick HayKevin Owen HicksFrederik PruijnWilliam Robert WilsonKarin Pchalek
    • William Alexander DennyMichael Patrick HayKevin Owen HicksFrederik PruijnWilliam Robert WilsonKarin Pchalek
    • C07D253/10C07D413/12A61K31/53A61P35/00
    • C07D253/10C07D253/08C07D401/12
    • 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.
    • 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。