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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

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。

3. 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。

4. 发明授权

US07629332B2 Nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents 失效
标题翻译：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：US07629332B2
公开(公告)日：2009-12-08
申请号：US10577078
申请日：2004-10-29
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： A61K31/66 , C07F9/02
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 tumors, and to their use in cell ablation, including gene-directed enzyme-prodrug therapy (GPEPT) 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（GPEPT）和抗体定向酶法（ADEPT）与硝酸还原酶联用。

5. 发明申请

US20080119442A1 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：US20080119442A1
公开(公告)日：2008-05-22
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： A61K31/675 , C07D403/02 , C07D209/56 , C07F9/547
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。

6. 发明授权

US5891886A Treatment of cancers 失效
标题翻译：癌症治疗
公开(公告)号：US5891886A
公开(公告)日：1999-04-06
申请号：US921331
申请日：1997-08-29
申请人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
发明人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
IPC分类号： A61K31/473 , A61K31/44 , C07C233/77 , C07D219/08
CPC分类号： A61K31/00 , A61K31/473
摘要： A new treatment schedule for administration of N-�2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.
摘要翻译：用于施用N- [2-（二甲基氨基）乙基]吖啶-4-甲酰胺和其它相关的羧酰胺抗癌药物的新的治疗方案，其中药物以分次给药方案施用，其包含频繁间隔的两次或更多次给药，用于例如每小时。提及产生血浆水平的循环峰/谷的时间表。该化合物可用于规避癌症中的多药耐药性，并且可以例如与其它细胞毒性药物，特别是非地头性II抑制剂组合使用。包括黑色素瘤和晚期结肠癌的治疗。

7. 发明授权

US5696131A Treatment of cancers 失效
标题翻译：癌症治疗
公开(公告)号：US5696131A
公开(公告)日：1997-12-09
申请号：US387565
申请日：1995-02-13
申请人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
发明人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
IPC分类号： A61K31/473 , A61K31/165
CPC分类号： A61K31/00 , A61K31/473
摘要： A new treatment schedule for administration of N-�2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.
摘要翻译：用于施用N- [2-（二甲基氨基）乙基]吖啶-4-甲酰胺和其它相关的羧酰胺抗癌药物的新的治疗方案，其中药物以分次给药方案施用，其包含频繁间隔的两次或更多次给药，用于例如每小时。提及产生血浆水平的循环峰/谷的时间表。该化合物可用于规避癌症中的多药耐药性，并且可以例如与其它细胞毒性药物，特别是非地头性II抑制剂组合使用。包括黑色素瘤和晚期结肠癌的治疗。

8. 发明授权

US07235578B2 Processes for preparing 3-substituted 1-(chloromethyl)-1,2-dihydro-3H-[ring fused indol-5-yl-(amine-derived)] compounds and analogues thereof, and to products obtained therefrom 失效
标题翻译：制备3-取代的1-（氯甲基）-1,2-二氢-3H- [环稠合吲哚-5-基 - （胺衍生的）]化合物及其类似物的方法，以及由此得到的产物
公开(公告)号：US07235578B2
公开(公告)日：2007-06-26
申请号：US10514893
申请日：2003-05-19
申请人： William Alexander Denny , Shanjin Yang , Graham John Atwell , Scott Charles Jeffrey
发明人： William Alexander Denny , Shanjin Yang , Graham John Atwell , Scott Charles Jeffrey
IPC分类号： A61K31/403 , C07D209/60
CPC分类号： C07D401/06 , A61K31/404 , C07D209/60 , C07D487/04 , Y02A50/473
摘要： The invention provides processes of preparing 3-substituted 1-(chloromethyl)- 1,2-dihydro-3H-[ring fused indol-5-yl(amine-derived)] compounds of formula (I) and its analogues, or a physiologically functional derivative thereof, (I), wherein A and B together may represent a fused optionally substituted benezene, naphthalene, pyridine, furan or a pyrrole ring, where the optional substituents are represented by Y; X is halogen or OSO2R, and W is selected from NO2, NHOH, N(R3)2NHR3, NHCO2R3, N(phthaloyl) or NH2, or W is further selected from the group (a), wherein J is selected from OH or H, and P is a group which is a substrate suitable for a nitroreductase or carboxypeptidase enzyme. The invention is also directed to the use of compounds of formula (I) prepared by the processes of the invention as cytotoxins for cancer therapy and as prodrugs for gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug theraphy (ADEPT).
摘要翻译：本发明提供制备式（I）及其类似物的3-取代的1-（氯甲基）-1,2-二氢-3H- [环稠合的吲哚-5-基（胺衍生的）其中A和B一起可以表示稠合的任选取代的茚，萘，吡啶，呋喃或吡咯环，其中任选的取代基由Y表示; X是卤素或OSO 2 R，W选自NO 2，NHOH，N（R 3）2， NH 3，NH 3，N 3，N（邻苯二甲酰基）或NH 2，或W进一步选自组（a），其中J选自OH或H，P是适合于硝基还原酶或羧肽酶的底物。本发明还涉及通过本发明的方法制备的式（I）化合物作为细胞毒素用于癌症治疗和用作基因定向酶前药治疗（GDEPT）和抗体指导的酶 - 前药治疗（ ADEPT）。

9. 发明授权

US07064117B2 Anti-cancer 2,3-dihydro-1H-pyrrolo[3,2-f]quinoline complexes of cobalt and chromium 失效
标题翻译：钴和铬的抗癌2,3-二氢-1H-吡咯并[3,2-f]喹啉配合物
公开(公告)号：US07064117B2
公开(公告)日：2006-06-20
申请号：US10470155
申请日：2002-01-22
申请人： William Alexander Denny , William Robert Wilson , David Charles Ware , Graham John Atwell , Jared Bruce Milbank , Ralph James Stevenson
发明人： William Alexander Denny , William Robert Wilson , David Charles Ware , Graham John Atwell , Jared Bruce Milbank , Ralph James Stevenson
IPC分类号： C07D471/04 , A61K31/475
CPC分类号： C07D471/04 , C07D257/00 , C07F11/005 , C07F15/065
摘要： This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.
摘要翻译：本发明涉及一类杂环及其金属络合物，特别涉及这些化合物在制备前体药物中的用途，或作为可在缺氧条件下通过酶或通过治疗电离辐射活化的前药，用于治疗癌症。本发明还涉及这些杂环和相应的金属络合物在制备药物中的用途以及包括杂环或其金属络合物的组合物以及制备这些化合物的方法。

10. 发明授权

US06251933B1 Seco precursors of cyclopropylindolines and their use as prodrugs 失效
标题翻译：环丙基吲哚啉的山梨醇前体及其作为前药的用途
公开(公告)号：US06251933B1
公开(公告)日：2001-06-26
申请号：US09319771
申请日：1999-06-11
申请人： William Alexander Denny , Moana Tercel , Graham John Atwell , Jared Milbank
发明人： William Alexander Denny , Moana Tercel , Graham John Atwell , Jared Milbank
IPC分类号： A61K31404
CPC分类号： C07D403/12 , C07D209/10 , C07D209/12
摘要： A compound which is a 6-substituted seco indoline of the formula (I): wherein: X is halogen or OSO2R where R represents H or C1-5 alkyl optionally substituted with from 1 to 4 hydroxyl, acid (COOH) or amino groups which amino may be optionally substituted by one or two C1-5 alkyl groups; Y is N02, N3, NHOH, NHR, NRR, N═NR, N(O)RR, SR or SSR, where R is defined as above, but that in the case where Y is SSR or N═NR, then R can also be another moiety of formula (I); or Y is a group of formula:
摘要翻译：化合物，其为式（I）的6-取代的仲二氢吲哚：其中：X为卤素或OSO2R，其中R为H或任选被1至4个羟基，酸（COOH）或氨基取代的C 1-5烷基，氨基可以任选地被一个或两个C 1-5烷基取代; Y是N 2，N 3，NHOH，NHR，NRR，N = NR，N（O）RR，SR或SSR，其中R如上所定义，在Y是SSR或N = NR的情况下，R也可以是式（I）的另一部分;或Y是下式的基团：

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