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21. 发明授权

US08557841B2 Heterocyclic aromatic compounds useful as growth hormone secretagogues 有权
公开(公告)号：US08557841B2
公开(公告)日：2013-10-15
申请号：US13493448
申请日：2012-06-11
申请人： Guixue Yu , Jun Li , William R. Ewing , Richard B. Sulsky , James J. Li , Joseph Anthony Tino
发明人： Guixue Yu , Jun Li , William R. Ewing , Richard B. Sulsky , James J. Li , Joseph Anthony Tino
IPC分类号： C07D401/02 , A61K31/437
CPC分类号： C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04
摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1′, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

22. 发明申请

US20130184284A1 DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF 有权
公开(公告)号：US20130184284A1
公开(公告)日：2013-07-18
申请号：US13549767
申请日：2012-07-16
申请人： William R. Ewing , Yeheng Zhu , Chongqing Sun , Yanting Huang , Maheswaran Sivasamban Karatholuvhu , Scott A. Bolton , Laxman Pasunoori , Sunil Kumar Mandal , Philip M. Sher
发明人： William R. Ewing , Yeheng Zhu , Chongqing Sun , Yanting Huang , Maheswaran Sivasamban Karatholuvhu , Scott A. Bolton , Laxman Pasunoori , Sunil Kumar Mandal , Philip M. Sher
IPC分类号： A61K31/506 , A61K31/454 , A61K31/439 , C07D401/12 , A61K31/4545 , A61K45/06 , C07D401/14 , A61K31/498 , A61K31/501 , C07D471/04 , A61K31/437 , C07D413/12 , A61K31/497
CPC分类号： A61K31/506 , A61K31/437 , A61K31/439 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/498 , A61K31/501 , A61K45/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D451/02 , C07D453/06 , C07D471/04 , C07D471/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.

23. 发明申请

US20100022457A1 Sustained release glp-1 receptor modulators 审中-公开
标题翻译：持续释放的glp-1受体调节剂
公开(公告)号：US20100022457A1
公开(公告)日：2010-01-28
申请号：US12227780
申请日：2006-11-08
申请人： Feng Qian , William R. Ewing , Claudio Mapelli , Douglas James Riexinger , Ving G. Lee , Richard B. Sulsky , Yeheng Zhu , Tasir Shamsul Haque , Rogelio L. Martinez , Vijay Naringrekar , Nina Ni , Lori S. Burton
发明人： Feng Qian , William R. Ewing , Claudio Mapelli , Douglas James Riexinger , Ving G. Lee , Richard B. Sulsky , Yeheng Zhu , Tasir Shamsul Haque , Rogelio L. Martinez , Vijay Naringrekar , Nina Ni , Lori S. Burton
IPC分类号： A61K38/08
CPC分类号： A61K33/30 , A61K33/26 , A61K33/32 , A61K38/08 , A61K38/26 , A61K45/06 , C07K14/605 , A61K2300/00
摘要： The present invention provides novel pharmaceutical compositions comprising a human glucagon-like peptide-1 (GLP-1)-receptor modulator as an active ingredient in a sustained release formulation.
摘要翻译：本发明提供了包含人胰高血糖素样肽-1（GLP-1） - 受体调节剂作为持续释放制剂中的活性成分的新型药物组合物。

24. 发明申请

US20080242593A1 HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS 审中-公开
标题翻译：人类GLUCAGON-PEPTIDE-1调节剂及其在治疗糖尿病及相关病症中的应用
公开(公告)号：US20080242593A1
公开(公告)日：2008-10-02
申请号：US12041266
申请日：2008-03-03
申请人： William R. Ewing , Claudio Mapelli , Richard B. Sulsky , Tasir Shamsul Haque , Ving G. Lee , Douglas James Riexinger , Rogelio L. Martinez , Yeheng Zhu
发明人： William R. Ewing , Claudio Mapelli , Richard B. Sulsky , Tasir Shamsul Haque , Ving G. Lee , Douglas James Riexinger , Rogelio L. Martinez , Yeheng Zhu
IPC分类号： A61K38/28 , C07D213/02 , A61K38/08 , C07K7/06 , A61P3/10
CPC分类号： C07K7/06 , A61K38/00 , C07K14/605
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
摘要翻译：本发明提供了具有与天然GLP-1肽相似或优于天然GLP-1肽的生物活性的新型人胰高血糖素样肽-1（GLP-1） - 受体调节剂，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1受体调节剂表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。本发明的肽在糖尿病的功效模型中显示出所需的药代动力学性质和期望的效力。

25. 发明授权

US07368458B2 Bicyclic heterocycles as cannabinoid receptor modulators 有权
标题翻译：双环杂环作为大麻素受体调节剂
公开(公告)号：US07368458B2
公开(公告)日：2008-05-06
申请号：US11330541
申请日：2006-01-12
申请人： Chongqing Sun , William R. Ewing , Yanting Huang
发明人： Chongqing Sun , William R. Ewing , Yanting Huang
IPC分类号： C07D471/02 , C07D487/02 , A61K31/4375
CPC分类号： C07D471/04
摘要： The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, n, Y and Z are described herein.
摘要翻译：本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的治疗剂。该化合物具有通式I：包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 3，本文描述了SUP，3a，R 4，A，B，n，Y和Z。

26. 发明授权

US07262195B2 Compounds useful as motilin agonists and method 有权
标题翻译：可用作胃动素激动剂和方法的化合物
公开(公告)号：US07262195B2
公开(公告)日：2007-08-28
申请号：US10940240
申请日：2004-09-14
申请人： James J. Li , Hannguang J. Chao , Joseph A. Tino , William R. Ewing
发明人： James J. Li , Hannguang J. Chao , Joseph A. Tino , William R. Ewing
IPC分类号： A61K31/50 , C07D237/00 , C07D487/00
CPC分类号： C07D471/20 , A61K31/495 , A61K31/50
摘要： Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —CO2R4, —SO2N(R4)R4a, —SO2R4, CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.
摘要翻译：提供了可用于治疗胃肠蠕动障碍并且具有其结构或其药学上可接受的盐，其前药酯及其所有立体异构体的化合物，其中R 1和R 2 独立地选自氢，烷基，芳基，环烷基，烯基，炔基，芳基烷基，杂芳基，杂芳基烷基或杂环烷基; Z选自-CON（R 4 S）R 4a，-CO 2 R 4，-SO 3， N 2（R 4）R 4a，-SO 2 R 4，CN R 4a和R 4a相同或不同并且独立地选自氢，烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基或R 1， 4和R 4a可以连接在一起形成杂环。 R 4b选自氢，卤素，羟基，CN，OCF 3，CF 3，CONH 2， SO 2 H 2，CH 2 CH 3，NHCOCH 3或NHCO 2 CH 3， SUB> 3 Q是取代的双环杂环。还提供了使用这些化合物治疗胃肠蠕动障碍的方法。

27. 发明授权

US07238671B2 Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions 有权
标题翻译：人胰高血糖素样肽-1模拟物及其在治疗糖尿病和相关病症中的应用
公开(公告)号：US07238671B2
公开(公告)日：2007-07-03
申请号：US10419399
申请日：2003-04-21
申请人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
发明人： Sesha Iyer Natarajan , Claudio Mapelli , Margarita M. Bastos , Michael Bernatowicz , Ving Lee , William R. Ewing
IPC分类号： A61K38/08 , C07K7/04 , A61K38/00 , A61K38/02 , A61K38/16 , C07K2/00 , C07K7/08 , C07K1/00 , C07K1/14 , C07K1/107
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.
摘要翻译：本发明提供了模拟天然GLP-1肽的生物学活性的新型人胰高血糖素样肽-1（GLP-1）肽模拟物，因此可用于治疗或预防与GLP活性相关的疾病或病症。此外，本发明提供新颖的化学修饰的肽，其不仅刺激II型糖尿病患者的胰岛素分泌，而且产生其它有益的促胰岛素反应。这些合成肽GLP-1模拟物表现出增加的蛋白水解切割的稳定性，使其成为口服或肠胃外给药的理想治疗候选物。

28. 发明授权

US07166603B2 Dihydropyrimidone inhibitors of calcium channel function 有权
标题翻译：二氢嘧啶酮抑制剂钙通道功能
公开(公告)号：US07166603B2
公开(公告)日：2007-01-23
申请号：US10897215
申请日：2004-07-22
申请人： Natesan Murugesan , Gregory S. Bisacchi , William R. Ewing , Guixue Yu , Zhengxiang Gu , Todd Friends , Minsheng Zhang
发明人： Natesan Murugesan , Gregory S. Bisacchi , William R. Ewing , Guixue Yu , Zhengxiang Gu , Todd Friends , Minsheng Zhang
IPC分类号： C07D239/22 , A61K31/513 , C07D403/06
CPC分类号： C07D239/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds having the formula, enantiomers, diastereomers, solvates and salts thereof, where R1, R2, R3, R4, A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.
摘要翻译：具有式的化合物，其对映异构体，非对映异构体，溶剂合物和盐，其中R 1，R 2，R 3，R 4，本文所述的A，X和J是钙通道功能的抑制剂，并且可用于治疗钙通道依赖性疾病，包括高血压。

29. 发明授权

US6034093A Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds 失效
标题翻译：取代的磺酸N - [（氨基亚氨基甲基）苯基烷基] - 杂环基酰胺化合物
公开(公告)号：US6034093A
公开(公告)日：2000-03-07
申请号：US130336
申请日：1998-08-06
申请人： William R. Ewing , Michael R. Becker , Yong Mi Choi-Sledeski , Heinz W. Pauls , Daniel G. McGarry , Roderick S. Davis , Alfred P. Spada
发明人： William R. Ewing , Michael R. Becker , Yong Mi Choi-Sledeski , Heinz W. Pauls , Daniel G. McGarry , Roderick S. Davis , Alfred P. Spada
IPC分类号： C07D205/085 , C07D207/14 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D401/02 , A61K31/40 , A61K31/435
CPC分类号： C07D207/273 , C07D205/085 , C07D207/14 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14
摘要： The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
摘要翻译：式I的化合物显示出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。更具体地说，它们是因子Xa活性的抑制剂。本发明涉及式I化合物，其含有式I化合物的组合物及其用途，其用于治疗患有或经受生理条件的患者，其可通过施用活性抑制剂而改善因子Xa。

30. 发明授权

US5240007A Apparatus and method for moving a tissue stress sensor for applanating an artery 失效
标题翻译：用于移动组织应变传感器的装置和方法
公开(公告)号：US5240007A
公开(公告)日：1993-08-31
申请号：US700009
申请日：1991-05-14
申请人： Kenneth J. Pytel , Stephen A. Martin , Robert D. Butterfield , William R. Ewing
发明人： Kenneth J. Pytel , Stephen A. Martin , Robert D. Butterfield , William R. Ewing
IPC分类号： A61B5/022
CPC分类号： A61B5/021 , A61B5/02241
摘要： An artery applanation actuator for use in a system for noninvasively determining the intra-arterial blood pressure of a user incorporates a fluid actuator to effect movement of a sensor. The movement of the sensor is effective for applanating an artery of interest and measuring the stress of the tissue overlaying the artery of interest. Alternative embodiments of the artery applanation actuator are presented wherein an electric motor is used to activate a rotating arm which has a sensor located thereon. The rotation of the arm causes the sensor to contact and press against the tissue overlying the artery of interest. The artery applanation actuator is presented having a protective sheath surrounding the sensor to protect the sensor against inadvertent contact.
摘要翻译：用于非侵入性地确定使用者的动脉内血压的系统中的动脉压平致动器包括流体致动器以实现传感器的移动。传感器的运动对于平坦化感兴趣的动脉和测量覆盖感兴趣的动脉的组织的应力是有效的。提出了动脉压平致动器的替代实施例，其中使用电动机来启动具有位于其上的传感器的旋转臂。臂的旋转导致传感器接触并压靠在感兴趣的动脉上方的组织。动脉挤压致动器具有围绕传感器的保护护套，以保护传感器免于意外接触。

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