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公开(公告)号：US11014920B2
公开(公告)日：2021-05-25
申请号：US16461825
申请日：2017-11-13
Applicant: Merck Sharp & Dohme Corp.
Inventor： Jacqueline D. Hicks , Brian Alexander McKittrick , Brent R. Whitehead , Matthew Lombardo , Xiaoqing Han , Jerry A. Taylor , Hong Dong Chu , Sung-Sau So , Peter Orth , Zhicai Wu
IPC: C07D417/14 , A61P7/02 , C07D401/12 , C07D409/12 , C07D409/14 , C07D417/12
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 XIIa inhibitors.
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公开(公告)号：US10800827B2
公开(公告)日：2020-10-13
申请号：US16199774
申请日：2018-11-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： Songnian Lin , Lin Yan , Pei Huo , Dmitri Pissarnitski , Danqing Feng , Ravi Nargund , Yuping Zhu , Ahmet Kekec , Christina B. Madsen-Duggan , Zhi-Cai Shi , Zhicai Wu , Yingjun Mu
Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
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公开(公告)号：US20200262831A1
公开(公告)日：2020-08-20
申请号：US16461825
申请日：2017-11-13
Applicant: Merck Sharp & Dohme Corp.
Inventor： Jacqueline D. Hicks , Brian Alexander McKittrick , Brent R. Whitehead , Matthew Lombardo , Xiaoqing Han , Jerry A. Taylor , Hong Dong Chu , Sung-Sau So , Peter Orth , Zhicai Wu
IPC: C07D417/14 , A61P7/02 , C07D417/12 , C07D409/12 , C07D409/14 , C07D401/12
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 XIIa inhibitors.
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公开(公告)号：US09382243B2
公开(公告)日：2016-07-05
申请号：US14419842
申请日：2013-08-16
Applicant: Merck Sharp & Dohme Corp.
Inventor： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC: C07D471/02 , A61K31/00 , C07D471/04 , A61K31/366 , A61K31/397 , A61K31/4985 , A61K31/437 , A61K31/444 , A61K45/06
CPC classification number: C07D471/04 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/4985 , A61K45/06 , A61K2300/00
Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US20150218149A1
公开(公告)日：2015-08-06
申请号：US14420024
申请日：2013-08-15
Applicant: Merck Sharp & Dohme Corp.
Inventor： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC: C07D417/14 , A61K31/4184 , C07D405/14 , A61K31/4192 , C07D413/14 , A61K31/4985 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/366 , A61K31/397 , C07D405/12 , A61K31/5377
CPC classification number: C07D417/14 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/427 , A61K31/4985 , A61K31/506 , A61K31/5377 , C07D405/12 , C07D405/14 , C07D413/14
Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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Patent Agency Ranking
公开(公告)号：US20150210685A1
公开(公告)日：2015-07-30
申请号：US14419842
申请日：2013-08-16
Applicant: Merck Sharp & Dohme Corp.
Inventor： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC: C07D471/04 , A61K31/444 , A61K45/06 , A61K31/437
CPC classification number: C07D471/04 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/4985 , A61K45/06 , A61K2300/00
Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
Abstract translation: 结构式（I）的新化合物是AMP-蛋白激酶的活化剂，并且可用于治疗，预防和抑制由AMPK活化的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US20150203487A1
公开(公告)日：2015-07-23
申请号：US14419825
申请日：2013-08-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： James M. Apgar , Tesfaye Biftu , Ping Chen , Danqing Feng , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu , Ashok Arasappan
IPC: C07D471/04 , A61K31/437 , C07D519/00 , C07C53/18 , A61K31/4985 , A61K31/5377 , A61K31/496 , A61K31/366 , A61K31/397 , A61K31/444 , A61K31/19
CPC classification number: C07D471/04 , A61K31/19 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/5377 , C07C53/18 , C07D519/00 , A61K2300/00
Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
Abstract translation: 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US08952166B2
公开(公告)日：2015-02-10
申请号：US13951096
申请日：2013-07-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Fa-Xiang Ding , Shuzhi Dong , Jessica Frie , Xin Gu , Jinlong Jiang , Alexander Pasternak , Haifeng Tang , Zhicai Wu , Yang Yu , Takao Suzuki
IPC: C07D471/10 , C07D307/88 , C07D498/20 , C07D519/00 , C07D471/20 , A61K31/438 , A61K31/46 , A61K31/435 , A61K31/4995 , A61K31/5386 , A61K45/06 , C07D451/00
CPC classification number: C07D498/20 , A61K31/435 , A61K31/46 , A61K31/4995 , A61K31/5386 , A61K45/06 , C07D451/00 , C07D471/10 , C07D471/20 , C07D519/00
Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 该化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和水滞留有关的病症的医学病症。
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9.发明申请PREPARATION AND USE OF BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS 有权双酚A衍生物作为PAR-1受体拮抗剂的制备和使用公开(公告)号：US20150025046A1
公开(公告)日：2015-01-22
申请号：US14383176
申请日：2013-02-27
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Mihir Mandal , Timothy A. Blizzard , Helen Chen , Harry Chobanian , Yan Guo , Barbara Pio , Zhicai Wu , Tesfaye Biftu , William J. Greenlee , Johnny Zhaoning Zhu
IPC: C07D405/06 , A61K45/06 , C07D405/14 , C07D401/06 , A61K31/4439 , C07D413/14 , A61K31/444 , A61K31/443 , C07D417/14
CPC classification number: C07D405/06 , A61K31/365 , A61K31/4365 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/616 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61K2300/00
Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
Abstract translation: 本发明涉及下式的双环烟肼衍生物或其药学上可接受的盐，其中：X是-O - ， - N（R），-C（R 8）（R 9）或-C（O） - ; 并且Y是-O - ， - N（R），-C（R 8）（R 9）或-C（O） - ，其余变量在本文中描述。 本发明的化合物是PAR-1受体的有效抑制剂。 本发明化合物可用于治疗或预防诸如ACS，二级预防心肌梗塞或中风或PAD的疾病状态。
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公开(公告)号：US20220281886A1
公开(公告)日：2022-09-08
申请号：US17611553
申请日：2020-05-18
Applicant: Merck Sharp & Dohme Corp.
Inventor： Frank Bennett , Jason E. Imbriglio , Angela D. Kerekes , Tanweer Khan , Claire Lankin , Derun Li , Zhicai Wu , Yusheng Xiong , Hyewon Youm , Yang Yu , Feng Ye , Anthappan Tony Kurissery , Venukrishnan Komanduri
IPC: C07D491/107 , A61K45/06 , C07D401/14 , C07D413/14
Abstract: The present invention relates to Compounds of Formula I: I and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of cardiometabolic diseases including high blood pressure, heart failure, kidney disease, and diabetes in a subject.
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