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1. 发明授权

US09198913B2 Nitroimidazooxazines and their uses in anti-tubercular therapy 有权
标题翻译：硝基咪唑并恶嗪及其在抗结核治疗中的应用
公开(公告)号：US09198913B2
公开(公告)日：2015-12-01
申请号：US12847452
申请日：2010-07-30
申请人： William Alexander Denny , Andrew Mark Thompson , Adrian Blaser , Zhenkun Ma , Brian Desmond Palmer , Hamish Scott Sutherland , Iveta Kmentova
发明人： William Alexander Denny , Andrew Mark Thompson , Adrian Blaser , Zhenkun Ma , Brian Desmond Palmer , Hamish Scott Sutherland , Iveta Kmentova
IPC分类号： A61K31/5365 , C07D498/04
CPC分类号： A61K31/5365 , C07D498/04
摘要： The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
摘要翻译：本发明涉及新型的硝基咪唑并恶嗪，其制备方法及其用作治疗结核分枝杆菌和其他微生物感染的药物，单独或与其它抗感染治疗组合。

2. 发明申请

US20120028973A1 NITROIMIDAZOOXAZINES AND THEIR USES IN ANTI-TUBERCULAR THERAPY 有权
标题翻译：硝基咪唑及其在抗血小板治疗中的应用
公开(公告)号：US20120028973A1
公开(公告)日：2012-02-02
申请号：US12847452
申请日：2010-07-30
申请人： William Alexander Denny , Andrew Mark Thompson , Adrian Blaser , Brian Desmond Palmer , Zhenkun Ma , Hamish Scott Sutherland , Iveta Kmentova
发明人： William Alexander Denny , Andrew Mark Thompson , Adrian Blaser , Brian Desmond Palmer , Zhenkun Ma , Hamish Scott Sutherland , Iveta Kmentova
IPC分类号： A61K31/5365 , A61P31/06 , C07D498/04
CPC分类号： A61K31/5365 , C07D498/04
摘要： The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
摘要翻译：本发明涉及新型的硝基咪唑并恶嗪，其制备方法及其用作治疗结核分枝杆菌和其他微生物感染的药物，单独或与其它抗感染治疗组合。

3. 发明申请

US20090281088A1 BICYCLIC NITROIMIDAZOLE-SUBSTITUTED PHENYL OXAZOLIDINONES 有权
标题翻译：双环硝基咪唑取代苯基氧杂环己烷
公开(公告)号：US20090281088A1
公开(公告)日：2009-11-12
申请号：US12411220
申请日：2009-03-25
申请人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
发明人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
IPC分类号： A61K31/5365 , C07D498/04 , A61K31/551 , A61K31/496 , A61K31/4439 , A61K31/506 , A61P31/04
CPC分类号： C07D498/04
摘要： The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
摘要翻译：本发明提供了一系列双环硝基咪唑取代的苯基恶唑烷酮，其中双环硝基咪唑药效团与苯基恶唑烷酮共价键合，其药物组合物，以及组合物用于预防和治疗细菌感染的方法。双环硝基咪唑取代的苯基恶唑烷酮对于野生型和抗性病原体菌株具有惊人的抗菌活性，因此可用于预防，控制和治疗由这些病原体引起的许多人和兽医细菌感染如结核分枝杆菌。

4. 发明授权

US07666864B2 Bicyclic nitroimidazole-substituted phenyl oxazolidinones 有权
标题翻译：双环硝基咪唑取代的苯基恶唑烷酮
公开(公告)号：US07666864B2
公开(公告)日：2010-02-23
申请号：US12411220
申请日：2009-03-25
申请人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
发明人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
IPC分类号： C07D498/04 , A61K31/424 , A61K31/5365 , A61K31/553
CPC分类号： C07D498/04
摘要： The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
摘要翻译：本发明提供了一系列双环硝基咪唑取代的苯基恶唑烷酮，其中双环硝基咪唑药效团与苯基恶唑烷酮共价键合，其药物组合物，以及组合物用于预防和治疗细菌感染的方法。双环硝基咪唑取代的苯基恶唑烷酮对于野生型和抗性病原体菌株具有惊人的抗菌活性，因此可用于预防，控制和治疗由这些病原体引起的许多人和兽医细菌感染如结核分枝杆菌。

5. 发明授权

US07094798B1 Inhibitors of checkpoint kinases (Wee1 and Chk1) 有权
标题翻译：检测点激酶抑制剂（Wee1和Chk1）
公开(公告)号：US07094798B1
公开(公告)日：2006-08-22
申请号：US10424228
申请日：2003-04-25
申请人： Richard John Booth , Ellen Myra Dobrusin , Alan Kraker , Lorna Helen Mitchell , William Alexander Denny , Jeffrey Bruce Smaill , Andrew Mark Thompson , Florence Oliver Joseph McCarthy , Ho Huat Lee , Brian Desmond Palmer
发明人： Richard John Booth , Ellen Myra Dobrusin , Alan Kraker , Lorna Helen Mitchell , William Alexander Denny , Jeffrey Bruce Smaill , Andrew Mark Thompson , Florence Oliver Joseph McCarthy , Ho Huat Lee , Brian Desmond Palmer
IPC分类号： A61K31/403 , C07D209/88
CPC分类号： C07D487/04 , C07D209/88 , C07D491/04
摘要： This invention relates to pyrrolocarbazole derivatives according formula I wherein R1, R2, R7, R8, R9, X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1
摘要翻译：本发明涉及式I的吡咯并咔唑衍生物，其中R 1，R 2，R 7，R 8， R 9，X和Y如说明书中所定义，其中所述衍生物特异性抑制检查点激酶Wee1和Chk1中的一个或两个

6. 发明申请

US20070191394A1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US20070191394A1
公开(公告)日：2007-08-16
申请号：US10598841
申请日：2005-03-07
申请人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
发明人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
IPC分类号： A61K31/519 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
摘要翻译：公开了式I化合物及其制备方法。还公开了制备式I的生物活性化合物的方法以及包含式I化合物的药学上可接受的组合物的方法。本文公开的式I化合物可用于多种应用，包括用作抗菌剂。

7. 发明授权

US07563788B2 Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents 失效
标题翻译：取代咪唑并[1,2-a]吡啶作为抗菌剂
公开(公告)号：US07563788B2
公开(公告)日：2009-07-21
申请号：US10598841
申请日：2005-03-07
申请人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
发明人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
IPC分类号： C07D413/06 , C07D413/10 , C07D471/04 , A61K31/5355 , A61K31/506 , A61K31/497 , A61K31/4355 , A61P31/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
摘要翻译：公开了式I化合物及其制备方法。还公开了制备式I的生物活性化合物的方法以及包含式I化合物的药学上可接受的组合物的方法。本文公开的式I化合物可用于多种应用，包括用作抗菌剂。

8. 发明申请

US20090275577A1 IMIDAZOPYRIDINE AND IMIDAZOPYRIMIDINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：咪达唑啶和咪唑嗪衍生物作为抗菌剂
公开(公告)号：US20090275577A1
公开(公告)日：2009-11-05
申请号：US12484263
申请日：2009-06-15
申请人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
发明人： Richard John Sciotti , Jeremy Tyson Starr , Christopher Richardson , Gordon William Rewcastle , Huifen Chen , Brian Desmond Palmer , Hamish Scott Sutherland , Julie Ann Spicer
IPC分类号： A61K31/5377 , A61K31/438 , A61P31/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.
摘要翻译：公开了式I化合物及其制备方法。还公开了制备式I的生物活性化合物的方法以及包含式I化合物的药学上可接受的组合物的方法。本文公开的式I化合物可用于多种应用，包括用作抗菌剂。

9. 发明授权

US06218388B1 Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation 失效
标题翻译：苯并咪唑用于抑制蛋白酪氨酸激酶介导的细胞增殖
公开(公告)号：US06218388B1
公开(公告)日：2001-04-17
申请号：US09459011
申请日：1999-12-10
申请人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
发明人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
IPC分类号： A61K315377
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/4439 , A61K31/5377
摘要： Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
摘要翻译：以下式I的苯并咪唑是蛋白酪氨酸激酶的抑制剂，并且可用于治疗细胞增殖。该化合物特别可用于治疗癌症，动脉粥样硬化，再狭窄和牛皮癣。

10. 发明授权

US5750782A Nitroaniline derivatives and their use as anti-tumour agents 失效
标题翻译：硝基苯胺衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US5750782A
公开(公告)日：1998-05-12
申请号：US685079
申请日：1996-07-23
申请人： William Alexander Denny , Brian Desmond Palmer , William Robert Wilson
发明人： William Alexander Denny , Brian Desmond Palmer , William Robert Wilson
IPC分类号： C07C237/34 , C07C233/65
CPC分类号： C07C237/34
摘要： The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##
摘要翻译：本发明提供了通式（1）表示的硝基苯胺衍生物，其中硝基在任何一个可用苯位置2-6取代; 其中R和A分别代表基团NO2，CN，COOR1，CONR1R2，CSNR1R2或SO2NR1R2，A在任何一个可用的苯位置2-6取代; 其中B表示在任何一个可用苯位置取代的N（CH 2 CH 2卤素）2或N（CH 2 CH 2 OSO 2 R 3）2）并且其中R 1，R 2和R 3分别代表H，或任选被羟基，醚，羧基或氨基官能团取代的低级烷基，包括环状结构，或者R 1和R 2与氮一起形成杂环结构，以及含有它们的药物制剂。这些化合物具有作为缺氧选择性细胞毒素，用于细胞毒素的还原活化前药，缺氧细胞放射增敏剂和抗癌剂的活性。

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