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1. 发明授权

US07718688B2 Nitrobenzindoles and their use in cancer therapy 失效
标题翻译：硝基苯并吲哚及其在癌症治疗中的应用
公开(公告)号：US07718688B2
公开(公告)日：2010-05-18
申请号：US11666014
申请日：2005-10-21
申请人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
发明人： William Alexander Denny , William Robert Wilson , Ralph James Stevenson , Moana Tercel , Graham John Atwell , Shangjin Yang , Adam Vorn Patterson , Frederik Bastlaan Pruijn
IPC分类号： A61K31/403 , C07D209/60
CPC分类号： C07F9/5728 , C07D209/60 , C07D403/06 , C07F9/65583
摘要： The present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and 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：本发明一般涉及硝基-1,2-二氢-3H-苯并[e]吲哚及其相关类似物及其制备方法，以及它们作为用于癌症治疗的缺氧选择性药物和放射增敏剂的用途，其单独或与辐射和/或其他抗癌药物。

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. 发明申请

US20050256191A1 Nitroaniline-based alkylating agents and their use as prodrugs 失效
标题翻译：基于硝基苯胺的烷基化剂及其作为前药的用途
公开(公告)号：US20050256191A1
公开(公告)日：2005-11-17
申请号：US10529772
申请日：2003-10-08
申请人： William Denny , Graham Atwell , Shangjin Yang , William Wilson
发明人： William Denny , Graham Atwell , Shangjin Yang , William Wilson
IPC分类号： A61P35/00 , C07C237/30 , C07C309/66 , C07C311/39 , C07D263/04 , C07D295/13 , C07D317/28 , C07C39/02 , A61K31/205
CPC分类号： C07D295/13 , C07C237/30 , C07C309/66 , C07C311/39 , C07D263/04 , C07D317/28
摘要： Nitroaniline-based unsymmetrical mustards of the general formula (I) are provided, together with methods of preparation and methods for their use as prodrugs for gene-dependent enzyme prodrug therapy (GDEPT) and cell ablation therapy in conjunction with nitroreductase enzymes as hypoxia selective cytotoxins and as anticancer agents.
摘要翻译：提供了通式（I）的基于硝基苯胺的不对称芥末，以及其制备方法和用作基因依赖性酶前体药物治疗（GDEPT）的前药的方法和与硝基还原酶作为缺氧选择性细胞毒素联合的细胞消除治疗并作为抗癌剂。

4. 发明授权

US08609851B2 Nitropyridinyl ethyleneimine compound, the pharmaceutical composition containing it, the preparation method and use thereof 有权
公开(公告)号：US08609851B2
公开(公告)日：2013-12-17
申请号：US13126907
申请日：2009-10-27
申请人： Shangjin Yang , Jianhui Yan , Ligang Wang , Xingna Guo , Shubin Li , Guoqiang Wu , Ruiya Zuo , Xin Huang , Hongtao Wang , Lingling Wang , Wenjuan Huang , Huigang Lu , Ke Feng , Fang Li , Huimin He , Yu Liu
发明人： Shangjin Yang , Jianhui Yan , Ligang Wang , Xingna Guo , Shubin Li , Guoqiang Wu , Ruiya Zuo , Xin Huang , Hongtao Wang , Lingling Wang , Wenjuan Huang , Huigang Lu , Ke Feng , Fang Li , Huimin He , Yu Liu
IPC分类号： C07D401/00
CPC分类号： C07D401/04 , C07D213/60 , C07D213/61 , C07D213/73
摘要： The present invention discloses a nitropyridinyl ethyleneimine compound as shown in the formula I and a preparation method of the same, as well as use of the compound in manufacture of a prodrug and in manufacture of a drug for treating a tumor.

5. 发明授权

US07776924B2 Nitroaniline-based alkylating agents and their use as prodrugs 失效
标题翻译：基于硝基苯胺的烷基化剂及其作为前药的用途
公开(公告)号：US07776924B2
公开(公告)日：2010-08-17
申请号：US10529772
申请日：2003-10-08
申请人： William Alexander Denny , Graham J. Atwell , Shangjin Yang , William Robert Wilson , Adam Vorn Patterson
发明人： William Alexander Denny , Graham J. Atwell , Shangjin Yang , William Robert Wilson , Adam Vorn Patterson
IPC分类号： A61K31/135 , C07C237/28
CPC分类号： C07D295/13 , C07C237/30 , C07C309/66 , C07C311/39 , C07D263/04 , C07D317/28
摘要： Nitroaniline-based unsymmetrical mustards of the general formula (I) are provided, together with methods of preparation and methods for their use as prodrugs for gene-dependent enzyme prodrug therapy (GDEPT) and cell ablation therapy in conjunction with nitroreductase enzymes as hypoxia selective cytotoxins and as anticancer agents.
摘要翻译：提供了通式（I）的基于硝基苯胺的不对称芥末，以及其制备方法和用作基因依赖性酶前体药物治疗（GDEPT）的前药的方法和与硝基还原酶作为缺氧选择性细胞毒素联合的细胞消除治疗并作为抗癌剂。

6. 发明申请

US20070032455A1 Novel nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents 失效
标题翻译：新型硝基苯基芥末和硝基苯基氮丙啶醇及其相应的磷酸盐及其作为靶向细胞毒性剂的用途
公开(公告)号：US20070032455A1
公开(公告)日：2007-02-08
申请号：US10577078
申请日：2004-10-29
申请人： William Denny , Graham Atwell , Shangjin Yang , William Wilson , Adam Patterson , Nuala Helsby
发明人： William Denny , Graham Atwell , Shangjin Yang , William Wilson , Adam Patterson , Nuala Helsby
IPC分类号： A61K31/675 , C07F9/02 , A61K31/66
CPC分类号： C07F9/091 , C07C237/32 , C07C309/66 , C07C317/48 , C07D203/14
摘要： The present invention relates to a novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cell ablation, including gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzymeprodrug therapy (ADEPT), in conjunction with nitroreductase enzymes.
摘要翻译：本发明涉及一种新的硝基苯基芥子和硝基苯基氮丙啶醇，以及它们相应的磷酸盐，用作靶向的细胞毒剂; 作为缺氧性肿瘤中的生物还原药物，以及其在细胞消融中的应用，包括基因定向酶前药治疗（GDEPT）和抗体定向酶法（ADEPT），与硝酸还原酶联用。

7. 发明申请

US20120071515A1 NITROPYRIDINYL ETHYLENEIMINE COMPOUND, THE PHARMACEUTICAL COMPOSITION CONTAINING IT, THE PREPARATION METHOD AND USE THEREOF 有权
标题翻译：硝基吡啶乙炔化合物，含有它的药物组合物，其制备方法及其用途
公开(公告)号：US20120071515A1
公开(公告)日：2012-03-22
申请号：US13126907
申请日：2009-10-27
申请人： Shangjin Yang , Jianhui Yan , Ligang Wang , Xingna Guo , Shubin Li , Guoqiang Wu , Ruiya Zuo , Xin Huang , Hongtao Wang , Lingling Wang , Wenjuan Huang , Huigang Lu , Ke Feng , Fang Li , Huimin He , Yu Liu
发明人： Shangjin Yang , Jianhui Yan , Ligang Wang , Xingna Guo , Shubin Li , Guoqiang Wu , Ruiya Zuo , Xin Huang , Hongtao Wang , Lingling Wang , Wenjuan Huang , Huigang Lu , Ke Feng , Fang Li , Huimin He , Yu Liu
IPC分类号： A61K31/4427 , A61P35/00 , C07D401/04
CPC分类号： C07D401/04 , C07D213/60 , C07D213/61 , C07D213/73
摘要： The present invention discloses a nitropyridinyl ethyleneimine compound as shown in the formula I and a preparation method of the same, as well as use of the compound in manufacture of a prodrug and in manufacture of a drug for treating a tumor.
摘要翻译：本发明公开了式I所示的硝基吡啶基亚乙基亚胺化合物及其制备方法，以及该化合物在制备前体药物和制备用于治疗肿瘤的药物中的用途。

8. 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。

9. 发明申请

US20100121091A1 Processes of preparing asymmetric dinitrobenzamide mustard compounds, intermediate compounds useful therein and products obtained therefrom 审中-公开
标题翻译：制备不对称二硝基苯甲酰胺芥末化合物的方法，其中使用的中间体化合物和由其获得的产物
公开(公告)号：US20100121091A1
公开(公告)日：2010-05-13
申请号：US12310484
申请日：2007-09-04
申请人： Graham John Atwell , William Alexander Denny , Shangjin Yang
发明人： Graham John Atwell , William Alexander Denny , Shangjin Yang
IPC分类号： C07C303/28 , C07F9/09
CPC分类号： C07D203/10 , C07C227/06 , C07C231/12 , C07C303/28 , C07C309/66 , C07C309/67 , C07D307/20 , C07F9/091 , C07C229/56 , C07C233/69
摘要： The invention relates to methods of preparing compounds of formula (II) wherein Z represents —OR1 or N(R2)R2a—, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R2a is lower alkylene (C1-C6) or H; Q is absent when R2a is H and is otherwise selected from the group consisting of H, —OH and protected forms of —OH; one of X and Y is halogen and the other is —OSO2R3, where R3 is selected from the group consisting of lower alkyl (C1-C6), phenyl and CH2phenyl. The method comprises the steps of: (a) reacting a compound of formula (I) with aziridineethanol or a 2-[(2-haloethyl)amino]ethanol in the presence of a metal halide, to form a compound of the formula (III) wherein one of X and E is halogen and the other is hydroxy, and (b) reacting the compound of formula (III) with an alkyl- or arylsulfonyl halide or alkyl- or arylsulfonyl anhydride to obtain a compound of the formula (II). The invention also relates to methods of preparing compounds of formula (IV) from the compounds of formula (II) so obtained, and to novel compounds of formula (IIb) useful as intermediates in these methods.
摘要翻译：本发明涉及制备式（II）化合物的方法，其中Z表示-OR1或N（R2）R2a，其中R1为低级亚烷基（C1-C6），R2为低级烷基或H，R2a为低级亚烷基 -C 6）或H; 当R 2a为H且Q选自H，-OH和-OH的保护形式时，Q不存在; X和Y之一是卤素，另一个是-OSO 2 R 3，其中R 3选自低级烷基（C 1 -C 6），苯基和CH 2苯基。该方法包括以下步骤：（a）在金属卤化物的存在下使式（I）化合物与氮丙啶乙醇或2 - [（2-卤代乙基）氨基]乙醇反应，形成式（III）的化合物）其中X和E之一是卤素，另一个是羟基，和（b）使式（III）化合物与烷基 - 或芳基磺酰卤或烷基 - 或芳基磺酰基酐反应得到式（II）化合物，。本发明还涉及由如此获得的式（II）化合物和式（Ⅱb）化合物制备式（Ⅳ）化合物的方法，可用作这些方法中的中间体。

10. 发明申请

US20100010094A1 Novel nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents 审中-公开
标题翻译：新型硝基苯基芥末和硝基苯基氮丙啶醇及其相应的磷酸盐及其作为靶向细胞毒性剂的用途
公开(公告)号：US20100010094A1
公开(公告)日：2010-01-14
申请号：US12461419
申请日：2009-08-11
申请人： William Alexander Denny , Graham John Atwell , Shangjin Yang , William Robert Wilson , Adam Vorn Patterson , Nuala Ann Helsby
发明人： William Alexander Denny , Graham John Atwell , Shangjin Yang , William Robert Wilson , Adam Vorn Patterson , Nuala Ann Helsby
IPC分类号： A61K31/166 , C07C233/01 , A61P35/00
CPC分类号： C07F9/091 , C07C237/32 , C07C309/66 , C07C317/48 , C07D203/14
摘要： The present invention relates to novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cell ablation, including gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug therapy (ADEPT), in conjunction with nitroreductase enzymes.
摘要翻译：本发明涉及新的硝基苯基芥子和硝基苯基氮丙啶醇与其相应的磷酸盐作为靶向细胞毒性剂的用途; 作为缺氧性肿瘤中的生物还原药物，以及其在细胞消融中的应用，包括基因定向酶前药治疗（GDEPT）和抗体定向酶前药治疗（ADEPT），与硝基还原酶联合使用。

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