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11. 发明授权

US06306891B1 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US06306891B1
公开(公告)日：2001-10-23
申请号：US09323519
申请日：1999-06-01
申请人： Harold G. Selnick , Melissa Egbertson , Daria Jean Hazuda , James P. Guare, Jr. , John S. Wai , Steven D. Young , David L. Clark , Julio C. Medina
发明人： Harold G. Selnick , Melissa Egbertson , Daria Jean Hazuda , James P. Guare, Jr. , John S. Wai , Steven D. Young , David L. Clark , Julio C. Medina
IPC分类号： A61K3140
CPC分类号： A61K45/06 , A61K31/40 , A61K31/445 , A61K2300/00
摘要： Nitrogen-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：含氮杂芳基二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

12. 发明授权

US08003648B2 Heterocyclic GPR40 modulators 失效
标题翻译：杂环GPR40调节剂
公开(公告)号：US08003648B2
公开(公告)日：2011-08-23
申请号：US12613418
申请日：2009-11-05
申请人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , XianYun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
发明人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , XianYun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
IPC分类号： A61K31/498 , A61K31/42 , A61K31/426 , A61K31/4245 , A61K31/443 , C07D261/06 , C07D277/22 , C07D271/06 , C07D413/02 , C07D241/36 , A61P3/10 , A61P9/00
CPC分类号： C07D261/08 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

13. 发明授权

US07816367B2 Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders 有权
公开(公告)号：US07816367B2
公开(公告)日：2010-10-19
申请号：US10591214
申请日：2005-02-24
申请人： Michelle Akerman , Jonathan Houze , Daniel C. H. Lin , Jiwen Liu , Jian Luo , Julio C. Medina , Wei Qiu , Jeffrey D. Reagan , Rajiv Sharma , Stephen J. Shuttleworth , Ying Sun , Jian Zhang , Liusheng Zhu , Jinqian Liu , Zhihua Ma , Yingcai Wang , Michael J. Schmitt
发明人： Michelle Akerman , Jonathan Houze , Daniel C. H. Lin , Jiwen Liu , Jian Luo , Julio C. Medina , Wei Qiu , Jeffrey D. Reagan , Rajiv Sharma , Stephen J. Shuttleworth , Ying Sun , Jian Zhang , Liusheng Zhu , Jinqian Liu , Zhihua Ma , Yingcai Wang , Michael J. Schmitt
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D277/24 , C07D277/30
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L1-P-L2-M-X-L3-A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.

14. 发明授权

US07687526B2 Benzo-fused compounds for use in treating metabolic disorders 失效
标题翻译：用于治疗代谢紊乱的苯并稠合化合物
公开(公告)号：US07687526B2
公开(公告)日：2010-03-30
申请号：US11900014
申请日：2007-09-06
申请人： Sean P. Brown , Paul Dransfield , Jonathan B. Houze , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Michael J. Schmitt , Rajiv Sharma , Yingcai Wang
发明人： Sean P. Brown , Paul Dransfield , Jonathan B. Houze , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Michael J. Schmitt , Rajiv Sharma , Yingcai Wang
IPC分类号： A61K31/4192 , A61K31/192 , C07D249/04 , C07C59/13
CPC分类号： C07D233/64 , C07C51/09 , C07C51/367 , C07C51/47 , C07C235/34 , C07C2602/10 , C07D207/327 , C07D213/55 , C07D231/12 , C07D239/26 , C07D249/10 , C07D257/04 , C07D261/08 , C07D263/32 , C07D277/587 , C07D285/12 , C07D333/24 , C07C59/72
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I：其中本文提供变量和A的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

15. 发明授权

US06433187B1 Certain polycyclic compounds useful as tubulin-binding agents 失效
标题翻译：某些多环化合物可用作微管蛋白结合剂
公开(公告)号：US06433187B1
公开(公告)日：2002-08-13
申请号：US09464217
申请日：1999-12-15
申请人： David Clark , Walter Frankmoelle , Jonathan Houze , Juan C. Jaen , Julio C. Medina
发明人： David Clark , Walter Frankmoelle , Jonathan Houze , Juan C. Jaen , Julio C. Medina
IPC分类号： C07D33708
CPC分类号： C07D401/06 , A61K31/382 , C07C311/20 , C07C311/21 , C07C2603/30 , C07C2603/32 , C07D409/06 , C07D409/14 , C07D493/04
摘要： Derivatives of known tubulin-binding compounds are provided in which a (poly)fluorobenzene, a fluoropyridine, or a fluoronitrobenzene moiety is incorporated or added to the structure. These derivatives can be used as antimitotic agents and can be considered covalent modifiers of tubulin. The strategy developed for each of the compounds is to i) append a fluorinated electrophile (e.g., pentafluorophenylsulfonamido, 2-fluoropyridyl, or 3,5-dinitro-4-fluorophenyl) to an existing functional group in a natural product, ii) replace an aromatic ring in a natural product with a fluorinated electrophile, or iii) attach a fluorinated electrophile to an open valence in a portion of the molecule that will not interfere with recognition and binding to the tubulin site. Derivatives are provided based on colchicine, steganacin, podophyllotoxin, nocodazole, combretastatin, curacin A, vinblastine, vincristine, dolastatin, 2-methoxyestradiol, dihydroxy-pentamethoxyflavanone and others.
摘要翻译：提供了已知的微管蛋白结合化合物的衍生物，其中（聚）氟苯，氟代吡啶或氟硝基苯部分被结合或添加到该结构中。这些衍生物可用作抗有丝分裂剂并且可以被认为是微管蛋白的共价修饰剂。为每种化合物制定的策略是i）将天然产物中的现有官能团上的氟化亲电体（例如五氟苯基磺酰胺基，2-氟吡啶基或3,5-二硝基-4-氟苯基）具有氟化亲电体的天然产物中的芳香环，或iii）在分子的一部分中将氟化亲电体连接至开放价态，其不会干扰识别和结合微管蛋白位点。衍生物基于秋水仙碱，steganacin，鬼臼毒素，诺考达唑，考布他汀，curacin A，长春花碱，长春新碱，多卡他汀，2-甲氧基雌二醇，二羟基 - 五甲氧基黄酮等。

16. 发明申请

US20120115811A1 PHENYLANALINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS 有权
标题翻译：用于治疗胰岛素相关疾病和病症的苯胺衍生物
公开(公告)号：US20120115811A1
公开(公告)日：2012-05-10
申请号：US13148296
申请日：2010-02-12
申请人： Xiaohui Du , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Yong-Jae Kim , Leping Li , Jinqian Liu , Mike Elias Lizarzaburu , Julio C. Medina , Wang Shen , Simon Turcotte , Ming Yu
发明人： Xiaohui Du , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Yong-Jae Kim , Leping Li , Jinqian Liu , Mike Elias Lizarzaburu , Julio C. Medina , Wang Shen , Simon Turcotte , Ming Yu
IPC分类号： A61K31/4439 , C07D417/12 , C07D401/14 , C07D401/04 , A61K31/444 , A61K31/506 , A61K31/427 , A61P3/10 , A61P3/04 , A61P3/00 , A61P29/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P1/00 , A61P35/00 , A61P25/00 , A61K31/702 , C07D417/14
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
摘要翻译：本文提供了式I的化合物：其中A，B，X，R 1，R 2和下标n如以下公开内容所定义。还提供了包含该化合物的组合物，以及其用于例如治疗2型糖尿病和2型糖尿病相关病症的方法。

17. 发明申请

US20110190330A1 SPIROCYCLIC GPR40 MODULATORS 有权
标题翻译：螺旋GPR40调制器
公开(公告)号：US20110190330A1
公开(公告)日：2011-08-04
申请号：US13119951
申请日：2009-10-13
申请人： Sean P. Brown , Paul Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , XianYun Jiao , Sujen Lai , An-Rong Li , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang , Ming Yu , Liusheng Zhu
发明人： Sean P. Brown , Paul Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , XianYun Jiao , Sujen Lai , An-Rong Li , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang , Ming Yu , Liusheng Zhu
IPC分类号： A61K31/4418 , C07C69/757 , C07C62/34 , C07D213/64 , C07D249/08 , C07D311/96 , C07D217/24 , C07D231/12 , A61K31/216 , A61K31/192 , A61K31/4196 , A61K31/352 , A61K31/415 , A61K31/426 , A61P3/10
CPC分类号： C07C62/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/643 , C07D217/24 , C07D253/065 , C07D277/22 , C07D311/04 , C07D401/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式IA，IB，I'A或I'B：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

18. 发明申请

US20100075974A1 HETEROCYCLIC GPR40 MODULATORS 失效
标题翻译：杂环GPR40调制器
公开(公告)号：US20100075974A1
公开(公告)日：2010-03-25
申请号：US12613418
申请日：2009-11-05
申请人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
发明人： Hilary Beck , Paul Dransfield , Zice Fu , Jonathan B. Houze , Xian Yun Jiao , Todd J. Kohn , SuJen Lai , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio C. Medina , Michael J. Schmitt , Rajiv Sharma , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang
IPC分类号： A61K31/498 , C07D261/06 , A61K31/42 , C07D277/22 , A61K31/426 , C07D271/06 , A61K31/4245 , C07D413/02 , A61K31/443 , C07D241/36 , A61P3/10 , A61P9/00
CPC分类号： C07D261/08 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

19. 发明授权

US06583161B1 Benzenesulfonamides and benzamides as therapeutic agents 失效
标题翻译：苯磺酰胺和苯甲酰胺作为治疗剂
公开(公告)号：US06583161B1
公开(公告)日：2003-06-24
申请号：US09736040
申请日：2000-12-12
申请人： Julio C. Medina
发明人： Julio C. Medina
IPC分类号： A61K3144
CPC分类号： C07D213/70 , C07C311/29 , C07D213/76 , C07D239/56 , C07D239/60 , C07D317/64 , C07D327/04 , C07D491/04
摘要： The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
摘要翻译：本发明提供了与新型芳族衍生物有关的化合物，组合物和方法及其作为药理学活性剂的用途。该组合物特别用作治疗疾病状态，特别是癌症，牛皮癣，血管再狭窄，感染，动脉粥样硬化和高胆固醇血症中的药理作用，或作为用于开发此类药物的铅化合物。

20. 发明授权

US06380249B1 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US06380249B1
公开(公告)日：2002-04-30
申请号：US09323417
申请日：1999-06-01
申请人： Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
发明人： Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
IPC分类号： A61K31215
CPC分类号： C07D213/64 , C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90 , C07C69/738 , C07C217/60 , C07C229/34 , C07C229/42 , C07C233/63 , C07C235/60 , C07C255/41 , C07C271/16 , C07C271/28 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D209/12 , C07D241/12 , C07D253/08 , C07D263/58 , C07D295/088 , C07D295/155 , C07D295/192 , C07D333/22
摘要： Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：某些六元芳族和杂芳族二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制的抑制剂。这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

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