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1. 发明授权

US07989451B2 Tricyclic 1,2,4-triazine oxides and compositions for therapeutic use in cancer treatments 有权
标题翻译：三环1,2,4-三嗪氧化物和治疗用于癌症治疗的组合物
公开(公告)号：US07989451B2
公开(公告)日：2011-08-02
申请号：US11887368
申请日：2006-03-31
申请人： Michael Patrick Hay , Adrian Blaser , William Alexander Denny , Kevin Owen Hicks , Ho Huat Lee , Karin Pchalek , Frederik Bastiaan Pruijn , Bronwyn Gae Siim , William Robert Wilson , Shangjin Yang
发明人： Michael Patrick Hay , Adrian Blaser , William Alexander Denny , Kevin Owen Hicks , Ho Huat Lee , Karin Pchalek , Frederik Bastiaan Pruijn , Bronwyn Gae Siim , William Robert Wilson , Shangjin Yang
IPC分类号： A01N43/64 , A01N43/62 , A61K31/53 , A61K31/55 , C07D253/08 , C07D487/00
CPC分类号： C07D253/10 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D491/056
摘要： The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明涉及式I的新型三环1,2,4-三嗪-1-氧化物和新型三环1,2,4-三嗪-1,4-二氧化物及其相关类似物及其制备方法及其用途低氧选择性药物和用于癌症治疗的放射增敏剂，单独或与辐射和/或其它抗癌药物组合。

2. 发明申请

US20090186886A1 Tricyclic 1,2,4-Triazine Oxides and Compositions for Therapeutic Use in Cancer Treatments 有权
标题翻译：用于治疗癌症治疗的三环1,2,4-三嗪氧化物和组合物
公开(公告)号：US20090186886A1
公开(公告)日：2009-07-23
申请号：US11887368
申请日：2006-03-31
申请人： Michael Patrick Hay , Adrian Blaser , William Alexander Denny , Kevin Owen Hicks , Ho Huat Lee , Karin Pchalek , Frederik Bastiaan Pruijn , Bronwyn Gae Siim , William Robert Wilson , Shangjin Yang
发明人： Michael Patrick Hay , Adrian Blaser , William Alexander Denny , Kevin Owen Hicks , Ho Huat Lee , Karin Pchalek , Frederik Bastiaan Pruijn , Bronwyn Gae Siim , William Robert Wilson , Shangjin Yang
IPC分类号： A61K31/5377 , C07D253/10 , A61K31/53 , C07D413/06 , C07D491/048 , A61P35/00
CPC分类号： C07D253/10 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D491/056
摘要： The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明涉及式I的新型三环1,2,4-三嗪-1-氧化物和新型三环1,2,4-三嗪-1,4-二氧化物及其相关类似物及其制备方法及其用途低氧选择性药物和用于癌症治疗的放射增敏剂，单独或与辐射和/或其它抗癌药物组合。

3. 发明授权

US07816521B2 1,2,4-benzotriazine-1,4-dioxides 有权
标题翻译： 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。

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