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1. 发明申请

US20120202832A1 KINASE INHIBITORS, PRODRUG FORMS THEREOF AND THEIR USE IN THERAPY 有权
标题翻译：激素抑制剂，其制剂及其在治疗中的使用
公开(公告)号：US20120202832A1
公开(公告)日：2012-08-09
申请号：US13390398
申请日：2010-09-02
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling (Annie) Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling (Annie) Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
IPC分类号： A61K31/519 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy- and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.
摘要翻译：本发明提供了式I的激酶抑制剂：其中：（1）R 1是H，和（a）R 2是（3-氯苄基）氧基，R 3是氯; （b）R2和R3与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; （c）R2是2-吡啶基甲氧基，R3是氯; （d）R2和R3均为氯; （e）R 2是氯，R 1是溴; （f）R2和R3都是溴; （g）R2是氟，R3是乙炔基; （h）R2是氯，R3是乙炔基; （i）R2是溴，R3是乙炔基; （j）除了当R 1与R 3结合在一起的3位时，在4-位上，R 2是溴并且R 3是氟; （k）R2是2-吡啶基甲氧基，R3是氟; 或（1）R 2是2-吡啶基甲氧基，R 1是溴; 或（2）R 1，R 2和R 3中的至少一个选自苄氧基，3-氯苄氧基和2-吡啶基甲氧基，当R 1，R 2和R 3中的至少一个不是苄氧基，3-氯苄氧基或2-吡啶基甲氧基时，其余的独立地选自H，卤素和C 2 -C 4炔基，条件是当R 1，R 2和R 3中的一个是苄氧基或2-吡啶基甲氧基时，R 1，R 2和R 3中的另外两个不是H; 或（3）R 1，R 2和R 3中的两个与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; 另一个选自H，卤素和C 2 -C 4炔基。还提供了还原前药，其包含如上定义的激酶抑制剂和直接或间接连接于激酶抑制剂的氮的还原性触发剂。还提供了包含激酶抑制剂或前药的药物组合物，以及这些组合物在治疗中的用途，特别是用于治疗癌症。

2. 发明授权

US09101632B2 Kinase inhibitors, prodrug forms thereof and their use in therapy 有权
标题翻译：激酶抑制剂，其前药形式及其在治疗中的用途
公开(公告)号：US09101632B2
公开(公告)日：2015-08-11
申请号：US13390398
申请日：2010-09-02
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling Annie Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling Annie Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
IPC分类号： A61K31/519 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy-and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.
摘要翻译：本发明提供了式I的激酶抑制剂：其中：（1）R 1是H，和（a）R 2是（3-氯苄基）氧基，R 3是氯; （b）R2和R3与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; （c）R2是2-吡啶基甲氧基，R3是氯; （d）R2和R3均为氯; （e）R 2是氯，R 1是溴; （f）R2和R3都是溴; （g）R2是氟，R3是乙炔基; （h）R2是氯，R3是乙炔基; （i）R2是溴，R3是乙炔基; （j）除了当R 1与R 3结合在一起的3位时，在4-位上，R 2是溴并且R 3是氟; （k）R2是2-吡啶基甲氧基，R3是氟; 或（1）R 2是2-吡啶基甲氧基，R 1是溴; 或（2）R 1，R 2和R 3中的至少一个选自苄氧基，3-氯苄氧基和2-吡啶基甲氧基，当R 1，R 2和R 3中的至少一个不是苄氧基，3-氯苄氧基或2-吡啶基甲氧基时，其余的独立地选自H，卤素和C 2 -C 4炔基，条件是当R 1，R 2和R 3中的一个是苄氧基或2-吡啶基甲氧基时，R 1，R 2和R 3中的另外两个不是H; 或（3）R 1，R 2和R 3中的两个与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; 另一个选自H，卤素和C 2 -C 4炔基。还提供了还原前药，其包含如上定义的激酶抑制剂和直接或间接连接于激酶抑制剂的氮的还原性触发剂。还提供了包含激酶抑制剂或前药的药物组合物，以及这些组合物在治疗中的用途，特别是用于治疗癌症。

3. 发明授权

US09073916B2 Prodrug forms of kinase inhibitors and their use in therapy 有权
标题翻译：激酶抑制剂的前体形式及其在治疗中的应用
公开(公告)号：US09073916B2
公开(公告)日：2015-07-07
申请号：US13138429
申请日：2010-03-11
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Michael Patrick Hay , William Alexander Denny , William Robert Wilson , Guo-Liang Lu , Robert Forbes Anderson , Ho Huat Lee , Amir Ashoorzadeh
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Michael Patrick Hay , William Alexander Denny , William Robert Wilson , Guo-Liang Lu , Robert Forbes Anderson , Ho Huat Lee , Amir Ashoorzadeh
IPC分类号： A61K31/5377 , A61K31/519 , A61K31/4178 , A61K31/517 , A61K31/4709 , C07D403/12 , C07D403/14 , C07D401/12 , C07D405/14 , C07D471/04 , C07D239/94
CPC分类号： C07D471/04 , A61K31/4178 , A61K31/4709 , A61K31/517 , A61K31/519 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.
摘要翻译：本发明提供了包含激酶抑制剂和还原活化的片段化芳族硝基杂环或芳族硝基碳环触发剂的新型前药化合物，其中化合物携带正电荷。在优选的实施方案中，化合物具有式I：其中：X是任何带负电的抗衡离子; R 1是式 - （CH 2）nTr的基团，其中Tr是芳族硝基杂环或芳族硝基碳环， - （CH 2）nTr用作还原活化的片段触发子; n为0〜6的整数。 R2，R3和R4可以各自独立地选自叔胺激酶抑制剂（R2）（R3）（R4）N的脂族或芳族基团，或者R2，R3和R4中的两个可以形成脂族或芳族杂环胺环的激酶抑制剂，或R 2，R 3和R 4中的一个可以不存在，R2，R3和R4中的两个形成激酶抑制剂的芳族杂环胺环。本发明的化合物可用于治疗增殖性疾病如癌症。

4. 发明申请

US20120077811A1 PRODRUG FORMS OF KINASE INHIBITORS AND THEIR USE IN THERAPY 有权
标题翻译：激素形式的激素抑制剂及其在治疗中的使用
公开(公告)号：US20120077811A1
公开(公告)日：2012-03-29
申请号：US13138429
申请日：2010-03-11
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Michael Patrick Hay , William Alexander Denny , William Robert Wilson , Guo-Liang Lu , Robert Forbes Anderson , Ho Huat Lee , Amir Ashoorzadeh
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Michael Patrick Hay , William Alexander Denny , William Robert Wilson , Guo-Liang Lu , Robert Forbes Anderson , Ho Huat Lee , Amir Ashoorzadeh
IPC分类号： A61K31/5377 , C07D403/14 , C07D401/14 , C07D405/14 , C07D401/12 , A61P35/00 , C07D403/12 , C07D239/94 , A61K31/519 , A61K31/4178 , A61K31/517 , A61K31/4709 , C07D471/04 , C07D413/14
CPC分类号： C07D471/04 , A61K31/4178 , A61K31/4709 , A61K31/517 , A61K31/519 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor.The compounds of the invention are useful in treating proliferative diseases such as cancer.
摘要翻译：本发明提供了包含激酶抑制剂和还原活化的片段化芳族硝基杂环或芳族硝基碳环触发剂的新型前药化合物，其中化合物携带正电荷。在优选的实施方案中，化合物具有式I：其中：X是任何带负电的抗衡离子; R1是式 - （CH2）nTr的基团，其中Tr是芳族硝基杂环或芳族硝基碳环，和 - （CH2）nTr作为还原活化的片段触发剂; n为0〜6的整数。 R2，R3和R4可以各自独立地选自叔胺激酶抑制剂（R2）（R3）（R4）N的脂族或芳族基团，或者R2，R3和R4中的两个可以形成脂族或芳族杂环胺环的激酶抑制剂，或R 2，R 3和R 4中的一个可以不存在，R2，R3和R4中的两个形成激酶抑制剂的芳族杂环胺环。本发明的化合物可用于治疗增殖性疾病如癌症。

5. 发明申请

US20150299230A1 Novel Prodrugs And Methods Of Use Thereof 有权
标题翻译：新型药物及其使用方法
公开(公告)号：US20150299230A1
公开(公告)日：2015-10-22
申请号：US14423359
申请日：2013-08-22
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Amir Ashoorzadeh , Christopher Paul Guise , Alexandra Marie Mowday , David Francis Ackerley , Elsie May Williams , Janine Naomi Copp , Auckland University Limited , Victoria Link Limited
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Amir Ashoorzadeh , Christopher Paul Guise , Alexandra Marie Mowday , David Francis Ackerley , Elsie May Williams , Janine Naomi Copp
IPC分类号： C07F9/09 , C07C309/69 , C07D295/13 , C07C317/36 , C07D295/104
CPC分类号： C07F9/09 , C07C255/58 , C07C309/66 , C07C309/69 , C07C317/36 , C07C317/48 , C07D295/104 , C07D295/13 , C07D295/192 , C07F9/091
摘要： The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.
摘要翻译：本发明涉及用作靶向细胞毒性剂的化合物及其使用方法。特别地，本发明涉及对人AKR1C3酶代谢基本上抗性的前药，使用所述化合物的细胞消融方法和使用所述化合物治疗癌症和其它过度增殖性病症的方法。

6. 发明申请

US20130295011A1 BACTERIAL NITROREDUCTASE ENZYMES AND METHODS RELATING THERETO 审中-公开
标题翻译：细菌氮氧化酶酶及其相关方法
公开(公告)号：US20130295011A1
公开(公告)日：2013-11-07
申请号：US13810434
申请日：2011-07-18
申请人： Christopher Paul Guise , David Francis Ackerley , Amir Ashoorzadeh , Janine Naomi Copp , Jack Urquhart Flanagan , Alexandra Marie Mowday , Adam Vorn Patterson , Gareth Adrian Prosser , Jeffrey Bruce Smaill , Sophie Phillipa Syddall , Elsie May Williams
发明人： Christopher Paul Guise , David Francis Ackerley , Amir Ashoorzadeh , Janine Naomi Copp , Jack Urquhart Flanagan , Alexandra Marie Mowday , Adam Vorn Patterson , Gareth Adrian Prosser , Jeffrey Bruce Smaill , Sophie Phillipa Syddall , Elsie May Williams
IPC分类号： C12N9/00 , C12Q1/26 , A61K38/44 , A61K51/04
CPC分类号： A61K51/0495 , A61K38/44 , A61K47/556 , C12N9/0028 , C12N9/0036 , C12Q1/26 , Y02A50/473
摘要： The invention relates generally to bacterial nitroreductase enzymes and methods of use thereof: More particularly, although not exclusively, said enzymes have use in non-invasive imaging techniques, monitoring of therapeutic cell populations and gene-directed enzyme prodrug therapy. The invention also relates to the use of bacterial nitroreductase enzymes in radioimaging and/or ablation of biological agents and to compositions of use in such methods.
摘要翻译：本发明一般涉及细菌硝基还原酶及其使用方法：更具体地，尽管不是唯一地，所述酶可用于非侵入性成像技术，监测治疗性细胞群体和基因定向酶前药治疗。本发明还涉及细菌硝基还原酶在生物制剂的放射成像和/或消融中的用途以及在这些方法中使用的组合物。

7. 发明授权

US10357577B2 Bacterial nitroreductase enzymes and methods relating thereto 有权
公开(公告)号：US10357577B2
公开(公告)日：2019-07-23
申请号：US13810434
申请日：2011-07-18
申请人： Christopher Paul Guise , David Francis Ackerley , Amir Ashoorzadeh , Janine Naomi Copp , Jack Urquhart Flanagan , Alexandra Marie Mowday , Adam Vorn Patterson , Gareth Adrian Prosser , Jeffrey Bruce Smaill , Sophie Phillipa Syddall , Elsie May Williams
发明人： Christopher Paul Guise , David Francis Ackerley , Amir Ashoorzadeh , Janine Naomi Copp , Jack Urquhart Flanagan , Alexandra Marie Mowday , Adam Vorn Patterson , Gareth Adrian Prosser , Jeffrey Bruce Smaill , Sophie Phillipa Syddall , Elsie May Williams
IPC分类号： A61K51/04 , A61K38/44 , C12Q1/26 , A61K47/54 , C12N9/02 , C12N9/06
摘要： The invention relates generally to bacterial nitroreductase enzymes and methods of use thereof: more particularly, although not exclusively, the enzymes have use in non-invasive imaging techniques, monitoring of therapeutic cell populations and gene-directed enzyme prodrug therapy. The invention also relates to the use of bacterial nitroreductase enzymes in radioimaging and/or ablation of biological agents and to compositions of use in such methods.

8. 发明授权

US09505791B2 Prodrugs and methods of use thereof 有权
标题翻译：前药及其使用方法
公开(公告)号：US09505791B2
公开(公告)日：2016-11-29
申请号：US14423359
申请日：2013-08-22
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Amir Ashoorzadeh , Christopher Paul Guise , Alexandra Marie Mowday , David Francis Ackerley , Elsie May Williams , Janine Naomi Copp
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Amir Ashoorzadeh , Christopher Paul Guise , Alexandra Marie Mowday , David Francis Ackerley , Elsie May Williams , Janine Naomi Copp
IPC分类号： C07F9/09 , C07C255/58 , C07C309/66 , C07C317/48 , C07D295/13 , C07D295/192 , C07C309/69 , C07C317/36 , C07D295/104
CPC分类号： C07F9/09 , C07C255/58 , C07C309/66 , C07C309/69 , C07C317/36 , C07C317/48 , C07D295/104 , C07D295/13 , C07D295/192 , C07F9/091
摘要： The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.
摘要翻译：本发明涉及用作靶向细胞毒性剂的化合物及其使用方法。特别地，本发明涉及对人AKR1C3酶代谢基本上抗性的前药，使用所述化合物的细胞消融方法和使用所述化合物治疗癌症和其它过度增殖性病症的方法。

9. 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。

10. 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。

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