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11. 发明申请

US20070173506A1 Thiazole compounds and methods of use 有权
标题翻译：噻唑化合物和使用方法
公开(公告)号：US20070173506A1
公开(公告)日：2007-07-26
申请号：US11652728
申请日：2007-01-11
申请人： Qingping Zeng , John Allen , Matthew Bourbeau , Celia Dominguez , Christopher Fotsch , Nianhe Han , Fang-Tsao Hong , Xin Huang , Matthew Lee , Aiwen Li , Qingyian Liu , James Rider , Seifu Tadesse , Andrew Tasker , Vellarkad Viswanadhan , Xianghong Wang , Kurt Weiler , George Wohlhieter , Guomin Yao , Chester Yuan
发明人： Qingping Zeng , John Allen , Matthew Bourbeau , Celia Dominguez , Christopher Fotsch , Nianhe Han , Fang-Tsao Hong , Xin Huang , Matthew Lee , Aiwen Li , Qingyian Liu , James Rider , Seifu Tadesse , Andrew Tasker , Vellarkad Viswanadhan , Xianghong Wang , Kurt Weiler , George Wohlhieter , Guomin Yao , Chester Yuan
IPC分类号： A61K31/502 , A61K31/4745 , A61K31/4709 , A61K31/427 , C07D417/02
CPC分类号： C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
摘要翻译：本发明涉及式I和式II的噻唑化合物及其用于治疗由蛋白激酶B（PKB）介导的疾病的组合物，其中变量具有本文提供的定义。本发明还涉及这种噻唑化合物及其组合物治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病的治疗用途。

12. 发明授权

US06867217B1 Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade 失效
公开(公告)号：US06867217B1
公开(公告)日：2005-03-15
申请号：US09574740
申请日：2000-05-18
申请人： Michael S. South , Qingping Zeng , Ashton T. Hamme, II , Melvin L. Rueppel
发明人： Michael S. South , Qingping Zeng , Ashton T. Hamme, II , Melvin L. Rueppel
IPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D215/38 , C07D401/12 , C07D417/12 , C07D521/00 , A61K31/535 , A61K31/517 , C07D401/00 , C07D417/00 , C07D453/02
CPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D215/38 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D417/12
摘要： The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

13. 发明授权

US5493012A Ion triggered alkylation of biological targets by silyloxy aromatic agents 失效
标题翻译：离子触发由甲硅烷氧基芳香剂引发生物靶标的烷基化
公开(公告)号：US5493012A
公开(公告)日：1996-02-20
申请号：US71116
申请日：1993-06-02
申请人： Steven E. Rokita , Tianhu Li , Qingping Zeng
发明人： Steven E. Rokita , Tianhu Li , Qingping Zeng
IPC分类号： C07D207/404 , C07F7/18 , C07H19/04 , C07H21/00 , C07H23/00 , C07H21/04
CPC分类号： C07D207/404 , C07F7/1852 , C07F7/1856 , C07H21/00 , C07H23/00
摘要： A silyloxy aromatic derivative capable of alkylating a target biological molecule when activated by ionic strength. A sequence directed reagent may be constructed by conjugating a methyl silyloxy aromatic derivative to a hexamethyiamino linker attached to either the 5' or 3' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to ionic activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the activated silyloxy aromatic derivative. In a preferred embodiment, a nitrophenyl or bromo group is attached to a methyl group of the silyloxy aromatic derivative. This reagent may be similarly linked to an oligonucleotide probe. Activation of the alkylating agent by an ionic signal (X) which may naturally occur, or may be introduced into the media containing the target molecule, such as by the introduction of a salt (MX).
摘要翻译：当通过离子强度活化时，能够将靶生物分子烷基化的甲硅烷氧基芳族衍生物。序列导向试剂可以通过将甲基甲硅烷氧基芳族衍生物与连接于寡核苷酸的5'或3'末端的六甲基氨基接头缀合来构建。将该修饰的DNA片段退火至其互补序列允许在离子活化后进行靶修饰。该反应的产物是由活化的甲硅烷氧基芳族衍生物的DNA烷基化产生的试剂和靶链之间的共价交联。在优选的实施方案中，硝基苯基或溴基连接到甲硅烷氧基芳族衍生物的甲基上。该试剂可以类似地连接到寡核苷酸探针。通过离子信号（X）活化烷基化剂，其可以天然存在，或者可以通过引入盐（MX）引入含有靶分子的介质中。

14. 发明授权

US08614253B2 IRE-1α inhibitors 有权
标题翻译： IRE-1α抑制剂
公开(公告)号：US08614253B2
公开(公告)日：2013-12-24
申请号：US12941530
申请日：2010-11-08
申请人： John Bruce Patterson , David Gregory Lonergan , Gary A. Flynn , Qingping Zeng , Peter V. Pallai
发明人： John Bruce Patterson , David Gregory Lonergan , Gary A. Flynn , Qingping Zeng , Peter V. Pallai
IPC分类号： A61K31/11
CPC分类号： C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
摘要： Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译：在体外直接抑制IRE-1α活性的化合物，其前药和药学上可接受的盐。这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病，并可用作单一药剂或联合疗法。

15. 发明申请

US20090275592A1 Heterocyclic modulators of PKB 有权
标题翻译： PKB的杂环调节剂
公开(公告)号：US20090275592A1
公开(公告)日：2009-11-05
申请号：US12218754
申请日：2008-07-16
申请人： Qingping ZENG , Dawei ZHANG , Guomin YAO , George E. WOHLHIETER , Xianghong WANG , James RIDER , Andreas REICHELT , Holger MONENSCHEIN , Fang-Tsao HONG , James R. FALSEY , Celia DOMINGUEZ , Matthew P. BOURBEAU , John G. ALLEN
发明人： Qingping ZENG , Dawei ZHANG , Guomin YAO , George E. WOHLHIETER , Xianghong WANG , James RIDER , Andreas REICHELT , Holger MONENSCHEIN , Fang-Tsao HONG , James R. FALSEY , Celia DOMINGUEZ , Matthew P. BOURBEAU , John G. ALLEN
IPC分类号： A61K31/502 , C07D237/26 , A61P35/00
CPC分类号： C07D413/04 , C07D263/48 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/14 , C07D417/04
摘要： The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
摘要翻译：本发明涉及用于治疗由蛋白激酶B（PKB）介导的疾病的式I的杂环化合物及其组合物，其中变量具有本文提供的定义。本发明还涉及这些化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病状态中的治疗用途。

16. 发明申请

US20080269243A1 Thiadiazole compounds and methods of use 有权
公开(公告)号：US20080269243A1
公开(公告)日：2008-10-30
申请号：US12077634
申请日：2008-03-19
申请人： Holger Monenschein , G. Erich Wohlhieter , Qingping Zeng
发明人： Holger Monenschein , G. Erich Wohlhieter , Qingping Zeng
IPC分类号： A61K31/496 , C07D417/14 , A61K31/4725
CPC分类号： C07D417/14 , C07D417/04 , C07D471/04
摘要： The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

17. 发明授权

US06528517B1 Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents 失效
标题翻译：合成具有拓扑异构酶II和四联体相互作用的喹诺酮类似物用作抗肿瘤剂
公开(公告)号：US06528517B1
公开(公告)日：2003-03-04
申请号：US09245019
申请日：1999-02-04
申请人： Laurence H. Hurley , Qingping Zeng , Yan Kwok , Jongsik Gam , Sean M. Kerwin
发明人： Laurence H. Hurley , Qingping Zeng , Yan Kwok , Jongsik Gam , Sean M. Kerwin
IPC分类号： A61K3144
CPC分类号： C07D498/06 , C07D498/16
摘要： The present invention discloses a novel quinobenzoxazine self-assembly complex on DNA and on the topoisomerase II-DNA complex. The related model is used to design a new series of quinobenzoxazines, pyridobenzophenoxazines, pyrridonaphthophenoxazines, and other related compounds that may exhibit anticancer or antibiotic activity. The anticancer activity of these compounds is thought to operate via stabilization of the topoisomerase II-DNA complex and/or interaction with G-quadruplexes, while the antibiotic activity of these compounds derives from their ability to inhibit gyrase, the bacterial type II topoisomerase.
摘要翻译：本发明公开了一种新的喹苯偶氮自组装DNA和拓扑异构酶II-DNA复合物的复合物。相关模型用于设计一系列可能具有抗癌活性或抗生素活性的喹喔啉恶唑，吡啶并苯并恶嗪，吡哆苯并吩ox嗪等相关化合物。认为这些化合物的抗癌活性通过拓扑异构酶II-DNA复合物的稳定化和/或与G-四链体相互作用而起作用，而这些化合物的抗生素活性来源于它们抑制细菌II型拓扑异构酶促旋酶的能力。

18. 发明授权

US5831073A Ion triggered alkylation of biological targets by silyloxy aromatic agents 失效
标题翻译：离子触发由甲硅烷氧基芳香剂引发生物靶标的烷基化
公开(公告)号：US5831073A
公开(公告)日：1998-11-03
申请号：US603221
申请日：1996-02-20
申请人： Steven E. Rokita , Tianhu Li , Qingping Zeng
发明人： Steven E. Rokita , Tianhu Li , Qingping Zeng
IPC分类号： C07D207/404 , C07F7/18 , C07H19/04 , C07H21/00 , C07H23/00
CPC分类号： C07F7/1852 , C07D207/404 , C07F7/1856 , C07H21/00 , C07H23/00
摘要： A silyloxy aromatic derivative capable of alkylating a target biological molecule when activated by ionic strength. A sequence directed reagent may be constructed by conjugating a methyl silyloxy aromatic derivative to a hexamethylamino linker attached to either the 5' or 3' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to ionic activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the activated silyloxy aromatic derivative. In a preferred embodiment, a nitrophenyl or bromo group is attached to a methyl group of the silyloxy aromatic derivative. This reagent may be similarly linked to an oligonucleotide probe. Activation of the alkylating agent by an ionic signal (X) which may naturally occur, or may be introduced into the media containing the target molecule, such as by the introduction of a salt (MX).
摘要翻译：当通过离子强度活化时，能够将靶生物分子烷基化的甲硅烷氧基芳族衍生物。序列导向的试剂可以通过将甲基甲硅烷氧基芳族衍生物与连接到寡核苷酸的5'或3'末端的六甲基氨基接头共轭来构建。将该修饰的DNA片段退火至其互补序列允许在离子活化后进行靶修饰。该反应的产物是由活化的甲硅烷氧基芳族衍生物的DNA烷基化产生的试剂和靶链之间的共价交联。在优选的实施方案中，硝基苯基或溴基连接到甲硅烷氧基芳族衍生物的甲基上。该试剂可以类似地连接到寡核苷酸探针。通过离子信号（X）活化烷基化剂，其可以天然存在，或者可以通过引入盐（MX）引入含有靶分子的介质中。

19. 发明授权

US09040714B2 IRE-1α inhibitors 有权
标题翻译： IRE-1α抑制剂
公开(公告)号：US09040714B2
公开(公告)日：2015-05-26
申请号：US13639734
申请日：2011-04-05
申请人： Qingping Zeng , Andras Toro , John Bruce Patterson , Warren Stanfield Wade , Zoltan Zubovics , Yun Yang , Zhipeng Wu
发明人： Qingping Zeng , Andras Toro , John Bruce Patterson , Warren Stanfield Wade , Zoltan Zubovics , Yun Yang , Zhipeng Wu
IPC分类号： C07D311/16 , C07D405/10 , C07D417/04 , A61K31/366 , A61K31/343 , A61K31/352 , A61K31/37 , A61K31/381 , A61K31/4025 , A61K31/404 , A61K31/4045 , A61K31/415 , A61K31/4155 , A61K31/4172 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/4433 , A61K31/4439 , A61K31/452 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D311/20 , C07D311/94 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： A61K31/366 , A61K31/343 , A61K31/352 , A61K31/37 , A61K31/381 , A61K31/4025 , A61K31/404 , A61K31/4045 , A61K31/415 , A61K31/4155 , A61K31/4172 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/4433 , A61K31/4439 , A61K31/452 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D217/02 , C07D217/08 , C07D311/12 , C07D311/16 , C07D311/20 , C07D311/22 , C07D311/94 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/10 , C07D409/04 , C07D417/04 , Y02A50/389 , Y02A50/393
摘要： Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
摘要翻译：在体外直接抑制IRE-1α活性的化合物，其前体药物和药学上可接受的盐。这些化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病或者与调节的IRE1依赖性衰变（RIDD）相关的疾病，并可用作单一药物或联合疗法。

20. 发明申请

US20120270877A1 IRE-1alpha INHIBITORS 有权
标题翻译： IRE-1α抑制剂
公开(公告)号：US20120270877A1
公开(公告)日：2012-10-25
申请号：US13505530
申请日：2010-11-01
申请人： Qingping Zeng , Warren S. Wade , John Bruce Patterson
发明人： Qingping Zeng , Warren S. Wade , John Bruce Patterson
IPC分类号： A61K31/496 , A61K31/495 , C07D207/14 , A61K31/40 , A61K31/402 , C07D401/04 , C07D413/04 , A61K31/5377 , C07D211/58 , A61K31/451 , A61K31/5375 , A61K31/454 , C07D249/06 , A61K31/4192 , C07D413/06 , C07D401/06 , C07D207/16 , C07D403/06 , C07D401/12 , A61K31/4545 , A61K31/4439 , C07D295/26 , C07D295/16 , C07D417/06 , C07D409/12 , A61K31/4025 , C07D413/12 , C07D333/24 , A61K31/381 , A61K31/426 , C07D239/26 , A61K31/505 , C07D239/38 , A61P37/00 , A61P35/00 , A61P31/12 , C12N9/99 , C07D295/112
CPC分类号： C07D487/08 , C07C59/74 , C07C65/30 , C07C69/738 , C07C235/78 , C07C235/84 , C07D207/08 , C07D207/14 , C07D207/16 , C07D211/26 , C07D211/58 , C07D211/62 , C07D211/66 , C07D211/98 , C07D213/36 , C07D213/38 , C07D213/74 , C07D213/81 , C07D213/82 , C07D239/26 , C07D239/38 , C07D249/06 , C07D263/34 , C07D277/12 , C07D277/18 , C07D277/42 , C07D277/56 , C07D295/108 , C07D295/112 , C07D295/185 , C07D295/192 , C07D295/26 , C07D295/32 , C07D307/68 , C07D333/38 , C07D333/40 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The invention provides compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译：本发明提供在体外直接抑制IRE-1α活性的化合物，其前药和药学上可接受的盐。这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病，并可用作单一药剂或联合疗法。

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