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公开(公告)号：US20130131042A1
公开(公告)日：2013-05-23
申请号：US13810946
申请日：2011-08-12
Applicant: Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
Inventor： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
IPC: C07D498/10 , C07D519/00
CPC classification number: C07D498/10 , C07D519/00
Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用反应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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公开(公告)号：US20160376272A1
公开(公告)日：2016-12-29
申请号：US15116547
申请日：2015-02-06
Applicant: Santhosh F. NEELAKAVIL , Scott D. EDMONDSON , Alan W. HRUZA , Zahid HUSSAIN , Charles LESBURG , Remond MONINGKA , Merck Sharp & Dohme Corp.
Inventor： Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
IPC: C07D471/08 , C07D487/08
CPC classification number: C07D471/08 , C07D487/08
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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Patent Agency Ranking
公开(公告)号：US20170044183A1
公开(公告)日：2017-02-16
申请号：US15305421
申请日：2015-04-21
Applicant: Yeon-Hee Lim , Zhuyan Guo , Amjad Ali , Scott D. Edmondson , Weiguo Liu , Giocanda V. Gallo-Etienne , Heping Wu , Ying-Duo Gao , Andrew W. Stamford , Younong Yu , Nancy J. Kevin , Rajan Anand , Deyou Sha , Santhosh F. Neelamkavil , Zahid Hussain , Puneet Kumar , Remond Moningka , Joseph L. Duffy , Jiayi Xu , Yu Jiang , Anjan Chakrabarti , Hiroki Sone
Inventor： Yeon-Hee Lim , Zhuyan Guo , Amjad Ali , Scott D. Edmondson , Weiguo Liu , Giocanda V. Gallo-Etienne , Heping Wu , Ying-Duo Gao , Andrew W. Stamford , Younong Yu , Nancy J. Kevin , Rajan Anand , Deyou Sha , Santhosh F. Neelamkavil , Zahid Hussain , Puneet Kumar , Remond Moningka , Joseph L. Duffy , Jiayi Xu , Yu Jiang , Anjan Chakrabarti , Hiroki Sone
IPC: C07D498/20 , C07F9/6561 , C07D487/10 , C07D498/10 , C07D471/10
CPC classification number: C07D498/20 , C07D471/10 , C07D487/10 , C07D498/10 , C07F9/6561
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract translation: 本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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公开(公告)号：US08742110B2
公开(公告)日：2014-06-03
申请号：US13810946
申请日：2011-08-12
Applicant: Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
Inventor： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
IPC: C07D215/00 , C07D229/00 , A61K31/44 , A61K31/397
CPC classification number: C07D498/10 , C07D519/00
Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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公开(公告)号：US09944643B2
公开(公告)日：2018-04-17
申请号：US15116547
申请日：2015-02-06
Applicant: MERCK SHARP & DOHME CORP. , Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
Inventor： Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
IPC: C07D471/08 , C07D487/08
CPC classification number: C07D471/08 , C07D487/08
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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公开(公告)号：US20160347757A1
公开(公告)日：2016-12-01
申请号：US15116659
申请日：2015-02-06
Applicant: Santhosh F. NEELAMKAVIL , Scott D. EDMONDSON , Zhuyan GUO , Alan W. HRUZA , Zahid HUSSAIN , Charles A. LESBURG , Remond MONINGKA , Anthony K. OGAWA , Rudrajit MAL , MERCK SHARP & DOHME CORP
Inventor： Santhosh F. Neelamkavil , Scott D. Edmondson , Zhuyan Guo , Alan W. Hruza , Zahid Hussain , Charles A. Lesburg , Remond Moningka , Anthony K. Ogawa , Rudrajit Mal
IPC: C07D487/08 , C07D471/08
CPC classification number: C07D487/08 , C07D471/08
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract translation: 本发明提供式（I）的化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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公开(公告)号：US20130040978A1
公开(公告)日：2013-02-14
申请号：US13641767
申请日：2011-05-13
Applicant: Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Paul E. Finke , Yi Zang , Michael A. Plotkin , F. Anthony Romero , Remond Moningka , Zahid Hussain
Inventor： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Paul E. Finke , Yi Zang , Michael A. Plotkin , F. Anthony Romero , Remond Moningka , Zahid Hussain
IPC: C07D498/10 , C07D519/00 , A61P25/22 , A61P3/04 , A61P3/00 , A61P25/24 , A61K31/438 , A61P3/10
CPC classification number: C07D498/10 , C07D519/00
Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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