公开(公告)号：US08084479B2

公开(公告)日：2011-12-27

申请号：US12378195

申请日：2009-02-11

Applicant: Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

Inventor： Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

IPC: A01N43/38 ,  A01N43/78 ,  A61K31/405 ,  A61K31/425 ,  C07D277/00

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to methods of using thiazole compounds of Formula I and Formula II and compositions thereof for treating diseases mediated by protein kinase B (PKB) such as cancer and other proliferative disorders where the variables have the definitions provided herein.

Abstract translation: 本发明涉及使用式I和式II的噻唑化合物及其组合物用于治疗由蛋白激酶B（PKB）介导的疾病，例如癌症和其它增殖性疾病，其中变量具有本文提供的定义。

公开(公告)号：US07354944B2

公开(公告)日：2008-04-08

申请号：US11251846

申请日：2005-10-18

Applicant: Qingping Zeng ,  Guomin Yao ,  George Erich Wohlhieter ,  Vellarkad N. Viswanadhan ,  Andrew Tasker ,  James Thomas Rider ,  Holger Monenschein ,  Celia Dominguez ,  Matthew Paul Bourbeau

Inventor： Qingping Zeng ,  Guomin Yao ,  George Erich Wohlhieter ,  Vellarkad N. Viswanadhan ,  Andrew Tasker ,  James Thomas Rider ,  Holger Monenschein ,  Celia Dominguez ,  Matthew Paul Bourbeau

IPC: A61K31/433 ,  A61K31/4725 ,  A61K31/416 ,  A61K31/4162 ,  C07D285/135 ,  C07D217/02 ,  C07D405/04 ,  C07D417/04 ,  C07D217/00

CPC classification number: C07D417/14 ,  C07D417/04 ,  C07D471/04

Abstract: 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.

Abstract translation: 本发明涉及可用于治疗由蛋白激酶B（PKB）介导的疾病的噻二唑化合物。 本发明还涉及这种噻二唑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。

公开(公告)号：US20070173506A1

公开(公告)日：2007-07-26

申请号：US11652728

申请日：2007-01-11

Applicant: 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

Inventor： 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: A61K31/502 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/427 ,  C07D417/02

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06867217B1

公开(公告)日：2005-03-15

申请号：US09574740

申请日：2000-05-18

Applicant: Michael S. South ,  Qingping Zeng ,  Ashton T. Hamme, II ,  Melvin L. Rueppel

Inventor： Michael S. South ,  Qingping Zeng ,  Ashton T. Hamme, II ,  Melvin L. Rueppel

IPC: 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 classification number: C07D213/74 ,  C07D213/75 ,  C07D213/77 ,  C07D215/38 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D417/12

Abstract: 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.

公开(公告)号：US5493012A

公开(公告)日：1996-02-20

申请号：US71116

申请日：1993-06-02

Applicant: Steven E. Rokita ,  Tianhu Li ,  Qingping Zeng

Inventor： Steven E. Rokita ,  Tianhu Li ,  Qingping Zeng

IPC: C07D207/404 ,  C07F7/18 ,  C07H19/04 ,  C07H21/00 ,  C07H23/00 ,  C07H21/04

CPC classification number: C07D207/404 ,  C07F7/1852 ,  C07F7/1856 ,  C07H21/00 ,  C07H23/00

Abstract: 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).

Abstract translation: 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。

公开(公告)号：US20130116247A1

公开(公告)日：2013-05-09

申请号：US13639734

申请日：2011-04-05

Applicant: Qingping Zeng ,  Andras Toro ,  John Bruce Patterson ,  Warren Stanfield Wade ,  Zoltan Zubovics ,  Yun Yang ,  Zhipeng Wu

Inventor： Qingping Zeng ,  Andras Toro ,  John Bruce Patterson ,  Warren Stanfield Wade ,  Zoltan Zubovics ,  Yun Yang ,  Zhipeng Wu

IPC: A61K31/366 ,  A61K31/496 ,  A61K31/5377 ,  C07D405/04 ,  A61K31/4025 ,  C07D405/10 ,  A61K31/453 ,  C07D417/04 ,  A61K31/427 ,  A61K31/4155 ,  C07D401/04 ,  A61K31/4433 ,  C07D409/04 ,  C07D311/94 ,  A61K45/06 ,  C07D311/20

CPC classification number: 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

Abstract: 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.

Abstract translation: 直接抑制体外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。

公开(公告)号：US20110263647A1

公开(公告)日：2011-10-27

申请号：US13130255

申请日：2010-01-13

Applicant: Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  David J. ST. Jean, JR. ,  Andreas Reichelt ,  Qingyian Liu ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Carl D. Davis ,  Matthew P. Bourbeau ,  Kate S. Ashton ,  John G. Allen

Inventor： Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  David J. ST. Jean, JR. ,  Andreas Reichelt ,  Qingyian Liu ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Carl D. Davis ,  Matthew P. Bourbeau ,  Kate S. Ashton ,  John G. Allen

IPC: A61K31/4709 ,  C07D417/14 ,  A61P35/00 ,  C07D417/04

CPC classification number: C07D417/14 ,  C07D417/04

Abstract: The invention relates to thiazole 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 thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及式I的噻唑化合物及其组合物，其用于治疗由蛋白激酶B（PKB）介导的疾病，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。

公开(公告)号：US07919514B2

公开(公告)日：2011-04-05

申请号：US12077633

申请日：2008-03-19

Applicant: Holger Monenschein ,  James Thomas Rider ,  Guomin Yao ,  Qingping Zeng

Inventor： Holger Monenschein ,  James Thomas Rider ,  Guomin Yao ,  Qingping Zeng

IPC: A61K31/433 ,  C07D285/12

CPC classification number: C07D417/14 ,  C07D417/04 ,  C07D471/04

Abstract: 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.

Abstract translation: 本发明涉及可用于治疗由蛋白激酶B（PKB）介导的疾病的噻二唑化合物。 本发明还涉及这种噻二唑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。

公开(公告)号：US07919504B2

公开(公告)日：2011-04-05

申请号：US12218523

申请日：2008-07-15

Applicant: Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  Andreas Reichelt ,  Qingyian Liu ,  Matthew R. Lee ,  Xin Huang ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

Inventor： Qingping Zeng ,  Chester Chenguang Yuan ,  Guomin Yao ,  Xianghong Wang ,  Seifu Tadesse ,  Andreas Reichelt ,  Qingyian Liu ,  Matthew R. Lee ,  Xin Huang ,  Fang-Tsao Hong ,  Nianhe Han ,  Christopher H. Fotsch ,  Celia Dominguez ,  Matthew P. Bourbeau ,  John G. Allen

IPC: A61K31/47 ,  C07D401/04

CPC classification number: C07D285/135 ,  C07D417/04 ,  C07D417/14 ,  C07D495/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20110065162A1

公开(公告)日：2011-03-17

申请号：US12941530

申请日：2010-11-08

Applicant: JOHN B. PATTERSON ,  DAVID G. LONERGAN ,  GARY A. FLYNN ,  QINGPING ZENG ,  PETER V. PALLAI

Inventor： JOHN B. PATTERSON ,  DAVID G. LONERGAN ,  GARY A. FLYNN ,  QINGPING ZENG ,  PETER V. PALLAI

IPC: C12N9/99

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。