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公开(公告)号：US08912206B2
公开(公告)日：2014-12-16
申请号：US13511062
申请日：2010-11-16
IPC分类号： C07D491/08 , A61K31/505
CPC分类号： C07D491/08
摘要： The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
摘要翻译： 本发明涉及嘧啶醚衍生物，包含嘧啶醚衍生物的组合物，以及使用嘧啶醚衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与G- 蛋白偶联受体（GPCR）。
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公开(公告)号：US20110166167A1
公开(公告)日：2011-07-07
申请号：US13003716
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
IPC分类号： A61K31/519 , C07D519/00 , A61P3/10
CPC分类号： C07D519/00
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
摘要翻译： 本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢紊乱，心血管疾病或与该活动相关的病症的方法 的G蛋白偶联受体（GPCR）。 化合物为结构（I）。
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公开(公告)号：US20120214805A1
公开(公告)日：2012-08-23
申请号：US13504363
申请日：2010-10-28
IPC分类号： A61K31/5386 , A61K31/439 , C07D498/08 , A61P3/00 , C07D451/02 , A61P3/10 , A61P3/04 , A61K31/506 , C07D491/08
CPC分类号： C07D491/08 , C07D498/08
摘要： The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译： 本发明涉及桥连双环哌啶衍生物，包含桥连双环哌啶衍生物的组合物，以及使用桥连双环哌啶衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 GPR119在患者体内的活动。
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4.发明申请公开(公告)号：US20110118286A1
公开(公告)日：2011-05-19
申请号：US13054347
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
IPC分类号： A61K31/519 , C07D487/04 , A61P3/00
CPC分类号： C07D487/04 , C07D473/30 , C07D473/34
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
摘要翻译： 本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，糖尿病并发症，代谢障碍，心血管疾病或 与患者G蛋白偶联受体（GPCR）的活性相关的紊乱。
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公开(公告)号：US08815876B2
公开(公告)日：2014-08-26
申请号：US13003716
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Bernard R. Neustadt , Samuel Chackalamannil , William J. Greenlee
IPC分类号： C07D519/00 , A61K31/519 , A61P13/12 , A61P3/04
CPC分类号： C07D519/00
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
摘要翻译： 本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢紊乱，心血管疾病或与该活动相关的病症的方法 的G蛋白偶联受体（GPCR）。 化合物为结构（I）。
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6.发明申请公开(公告)号：US20110166165A1
公开(公告)日：2011-07-07
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： A61K31/519 , C07D487/04 , A61P3/04 , A61P3/10 , A61P3/00
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译： 本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 在患者中G蛋白偶联受体（GPCR）如GPR119的活性。
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7.发明申请C6-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权C6-SPIRO三嗪二氧化物作为BACE抑制剂，组合物及其使用公开(公告)号：US20160264538A1
公开(公告)日：2016-09-15
申请号：US14653671
申请日：2013-12-16
申请人： Jared N. CUMMING , Jack D. SCOTT , Andrew W. STAMFORD , Ulrich ISERLOH , Santhosh Francis NEELAMKAVIL , Pengcheng Patrick SHAO , Jonathan E. WILSON , MERCK SHARP & DOHME CORP.
发明人： Jared N. Cumming , Jack D. Scott, JR. , Andrew W. Stamford , Ulrich Iserloh , Santhosh Francis Neelamkavil , Pengcheng Patrick Shao , Jonathan E. Wilson
IPC分类号： C07D285/24 , C07D471/04 , C07D417/12 , C07D513/10 , C07D519/00
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
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8.发明授权公开(公告)号：US08822480B2
公开(公告)日：2014-09-02
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： C07D519/00 , A61K31/519 , A61P13/12 , A61P3/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译： 本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 在患者中G蛋白偶联受体（GPCR）如GPR119的活性。
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公开(公告)号：US20120232073A1
公开(公告)日：2012-09-13
申请号：US13508652
申请日：2010-11-16
申请人： Santhosh Francis Neelamkavil , Dipshikha Biswas , Samuel Chackalamannil , Bernard R. Neustadt , Andrew Stamford , Hong Liu
发明人： Santhosh Francis Neelamkavil , Dipshikha Biswas , Samuel Chackalamannil , Bernard R. Neustadt , Andrew Stamford , Hong Liu
IPC分类号： A61K31/519 , C07D498/04 , C07D473/28 , A61P3/00 , A61K31/5383 , A61K31/52 , A61P3/10 , A61P3/04 , C07D487/04 , C07D473/00
CPC分类号： C07D487/04 , A61K31/4965 , A61K31/519 , A61K45/06 , C07D498/04 , C07D519/00 , A61K2300/00
摘要： The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
摘要翻译： 本发明涉及稠合双环嘧啶衍生物，包含稠合的双环嘧啶衍生物的组合物，以及使用稠合的双环嘧啶衍生物用于治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 患者中的G蛋白偶联受体（GPCR）。
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公开(公告)号：US09409918B2
公开(公告)日：2016-08-09
申请号：US13504363
申请日：2010-10-28
IPC分类号： C07D295/182 , C07D491/08 , C07D498/08
CPC分类号： C07D491/08 , C07D498/08
摘要： The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译： 本发明涉及桥连双环哌啶衍生物，包含桥连双环哌啶衍生物的组合物，以及使用桥连双环哌啶衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与 GPR119在患者中的活动。
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