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1. 发明授权

US07897619B2 Heterocyclic modulators of PKB 有权
标题翻译： PKB的杂环调节剂
公开(公告)号：US07897619B2
公开(公告)日：2011-03-01
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： A61K31/47 , A61K31/416 , C07D217/02 , C07D231/56
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。

2. 发明申请

US20090270445A1 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：US20090270445A1
公开(公告)日：2009-10-29
申请号：US12378195
申请日：2009-02-11
申请人： 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
发明人： 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分类号： A61K31/427 , A61K31/437 , A61P35/00
CPC分类号： C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04
摘要： 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.
摘要翻译：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。

3. 发明授权

US07514566B2 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：US07514566B2
公开(公告)日：2009-04-07
申请号：US11652728
申请日：2007-01-11
申请人： 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
发明人： 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分类号： A61K31/425 , C07D277/00
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。

4. 发明授权

US08084479B2 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：US08084479B2
公开(公告)日：2011-12-27
申请号：US12378195
申请日：2009-02-11
申请人： 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
发明人： 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分类号： A01N43/38 , A01N43/78 , A61K31/405 , A61K31/425 , C07D277/00
CPC分类号： C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04
摘要： 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.
摘要翻译：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。

5. 发明授权

US07919504B2 Thiadiazole modulators of PKB 失效
标题翻译： PKB的噻二唑调节剂
公开(公告)号：US07919504B2
公开(公告)日：2011-04-05
申请号：US12218523
申请日：2008-07-15
申请人： 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
发明人： 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分类号： A61K31/47 , C07D401/04
CPC分类号： C07D285/135 , C07D417/04 , C07D417/14 , C07D495/04
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。

6. 发明申请

US20090298836A1 Thiadiazole modulators of PKB 失效
标题翻译： PKB的噻二唑调节剂
公开(公告)号：US20090298836A1
公开(公告)日：2009-12-03
申请号：US12218523
申请日：2008-07-15
申请人： 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
发明人： 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分类号： A61K31/502 , C07D417/10 , A61K31/433 , C07D417/04 , A61K31/4365 , A61P35/00 , A61K31/4439 , A61K31/4725 , C07D417/14 , A61K31/517
CPC分类号： C07D285/135 , C07D417/04 , C07D417/14 , C07D495/04
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。

7. 发明申请

US20110263647A1 FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：氟代喹啉取代噻唑化合物及其使用方法
公开(公告)号：US20110263647A1
公开(公告)日：2011-10-27
申请号：US13130255
申请日：2010-01-13
申请人： 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
发明人： 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分类号： A61K31/4709 , C07D417/14 , A61P35/00 , C07D417/04
CPC分类号： C07D417/14 , C07D417/04
摘要： 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.
摘要翻译：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。

8. 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。

9. 发明授权

US07026326B2 Substituted heterocyclic compounds and methods of use 有权
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US07026326B2
公开(公告)日：2006-04-11
申请号：US10438553
申请日：2003-05-13
申请人： Guo-Qiang Cao , Celia Dominguez , Martin H. Goldberg , Fang-Tsao Hong , Kelvin K. C. Sham , Seifu Tadesse , Nuria A. Tamayo , Kurt E. Weiler , Dawei Zhang , Hongyu Liao
发明人： Guo-Qiang Cao , Celia Dominguez , Martin H. Goldberg , Fang-Tsao Hong , Kelvin K. C. Sham , Seifu Tadesse , Nuria A. Tamayo , Kurt E. Weiler , Dawei Zhang , Hongyu Liao
IPC分类号： A61K31/505
CPC分类号： C07D401/04
摘要： The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
摘要翻译：本发明涉及具有通式的化合物或其药学上可接受的盐，其中R 1是饱和或不饱和的5-，6-或7-元环，其含有0,1,2或 3个选自N，O和S的原子，其中环可以与苯并稠合，并被0,1或2个氧代基取代，并且其中R 1是另外被取代的; R 2是取代的C 1-6烷基。还包括预防或治疗炎症，类风湿性关节炎，斑节病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗死，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒引起的肌痛（CMV），流感，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的化合物d 以上所述。

10. 发明申请

US20050038010A1 Substituted heterocyclic compounds and methods of use 有权
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050038010A1
公开(公告)日：2005-02-17
申请号：US10438553
申请日：2003-05-13
申请人： Guo-Qiang Cao , Celia Dominguez , Martin Goldberg , Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Nuria Tamayo , Kurt Weiler , Dawei Zhang , Hongyu Liao
发明人： Guo-Qiang Cao , Celia Dominguez , Martin Goldberg , Fang-Tsao Hong , Kelvin Sham , Seifu Tadesse , Nuria Tamayo , Kurt Weiler , Dawei Zhang , Hongyu Liao
IPC分类号： A61K31/444 , A61K31/4545 , A61K31/501 , A61K31/506 , A61P1/04 , A61P1/18 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P33/06 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P39/02 , C07D401/04 , C07D401/14 , A61K31/553 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/55
CPC分类号： C07D401/04
摘要： The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
摘要翻译：本发明涉及具有通式的化合物或其药学上可接受的盐，其中R 1是饱和或不饱和的含有0,1,2或3个选自N，，O和S，其中所述环可以与苯并稠合，并被0,1或2个氧代基取代，并且其中R 1另外被取代; R 2是取代的C 1-6烷基。还包括预防或治疗炎症，类风湿性关节炎，斑节病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征（ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病，中风，心肌梗死，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒引起的肌痛（CMV），流感，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的化合物d 以上所述。

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