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1.发明申请公开(公告)号：US20210403479A1
公开(公告)日：2021-12-30
申请号：US17288626
申请日：2019-11-04
Applicant: Merck Sharp & Dohme Corp.
Inventor： Wensheng Yu , Joseph Kozlowski , Dane James Clausen , Jian Liu , Younong Yu , Ming Wang , Bing Li
IPC: C07D487/10 , C07D403/12 , C07D413/14 , C07D401/14 , C07D401/12 , C07D471/04 , C07D417/14 , C07D498/10 , C07D405/14 , A61K45/06
Abstract: The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4 and A are as defined herein. 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 treating or preventing HIV infection in a subject.
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公开(公告)号：US20180030036A1
公开(公告)日：2018-02-01
申请号：US15534029
申请日：2015-12-07
Applicant: Ting ZHANG , Yi-Heng CHEN , Liangqin GUO , Alan HARUZA , Tianying JIAN , Bing LI , Dongfang MENG , Dann L. PARKER, JR. , Edward C. SHERER , Harold B. WOOD , Isao SAKURADA , MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD
Inventor： Ting Zhang , Yi-Heng Chen , Liangqin Guo , Alan Hruza , Tianying Jian , Bing Li , Dongfang Meng , Dann L. Parker , Edward C. Sherer , Harold B. Wood , Isao Sakurada
IPC: C07D403/12 , C07D401/14 , C07D401/12 , C07D471/04
CPC classification number: C07D403/12 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
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公开(公告)号：US09527875B2
公开(公告)日：2016-12-27
申请号：US14418147
申请日：2013-07-31
Applicant: Merck Sharp & Dohme Corp.
Inventor： William K. Hagmann , Ravi P. Nargund , Timothy A. Blizzard , Hubert Josien , Purakkattle Biju , Christopher W. Plummer , Qun Dang , Bing Li , Derun Li , Linus S. Lin , Mingxiang Cui , Bin Hu , Jinglai Hao , Zhengxia Chen
IPC: C07D417/12 , A61K31/4353 , C07F9/58 , C07D401/14 , C07D221/16 , C07D401/12 , A61K31/435 , A61K31/444 , A61K45/06 , A61K31/4412 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/675 , C07D405/12 , C07D409/14
CPC classification number: C07F9/58 , A61K31/435 , A61K31/4412 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D221/16 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07D417/12
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Abstract translation: 结构式（I）的新型化合物及其药学上可接受的盐是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和 高甘油三酯血症
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![NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES](/abs-image/US/2015/10/08/US20150284411A1/abs.jpg.150x150.jpg)
公开(公告)号：US20150284411A1
公开(公告)日：2015-10-08
申请号：US14419774
申请日：2013-08-19
Applicant: James M. APGAR , Ashok ARASAPPAN , Tesfaye BIFTU , Ping CHEN , Danqing FENG , Erin GUIDRY , Jacqueline HICKS , Ahmet KEKEC , Kenneth LEAVITT , Bing LI , Troy MCCRACKEN , Iyassu SEBHAT , Xiaoxia QIAN , Lan WEI , Robert WILKENING , Zhicai WU , Merck Sharp & Dohme Corp.
Inventor： James M. Apgar , Ashok Arasappan , Tesfaye Biftu , Ping Chen , Danqing Feng , Erin Guidry , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Troy McCracken , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC: C07D519/00 , A61K31/438 , A61K45/06 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/437 , A61K31/506
CPC classification number: C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , 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：US11530250B2
公开(公告)日：2022-12-20
申请号：US16980579
申请日：2019-03-18
Applicant: Merck Sharp & Dohme Corp. , Ahmet Kekec , Nancy Jo Kevin , Bing Li , Songnian Lin , Craig A. Parish , Weijuan Tang
Inventor： Ahmet Kekec , Nancy Jo Kevin , Bing Li , Songnian Lin , Craig A. Parish , Weijuan Tang
Abstract: The present invention relates to tyrosine-specific functionalized insulin analogs and processes of making such tyrosine-specific functionalized insulin analogs using R-3H-1,2,4-triazoline-3,5-(4H)diones (PTAD).
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Patent Agency Ranking
公开(公告)号：US20180305352A1
公开(公告)日：2018-10-25
申请号：US15769414
申请日：2016-10-25
Applicant: MERCK SHARP & DOHME CORP.
Inventor： David J. Witter , Tesfaye Biftu , Purakkattle Biju , Stephane L. Bogen , Qingmei Hong , Chunhui Huang , Xianhai Huang , Bing Li , Min K. Park , David L. Sloman
IPC: C07D471/04 , C07D519/00 , A61P35/02
CPC classification number: C07D471/04 , A61P35/02 , C07D491/10 , C07D498/08 , C07D519/00
Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US09834563B2
公开(公告)日：2017-12-05
申请号：US15039607
申请日：2014-12-17
Applicant: Merck Sharp & Dohme Corp.
Inventor： William K. Hagmann , Bing Li , Jason W. Szewczyk , Bowei Wang , Dann Parker , Timothy Blizzard , Hubert Josien , Purakkattle Biju , Harry Chobanian , Candido Gude , Ravi P. Nargund , Barbara Pio , Qun Dang , Linus S. Lin , Bin Hu , Mingxiang Cui , Zhengxia Chen , Meibi Dai , Zaihong Zhang , Ying Lv , Lili Tian
IPC: A61K31/506 , C07D493/04 , A61K45/06 , C07D213/64 , A61K31/44 , C07D409/12 , A61K31/4436 , C07D401/04 , A61K31/4545 , C07D471/04 , A61K31/437 , C07D405/12 , A61K31/4433 , C07D401/12 , A61K31/4439 , A61K31/443 , C07D239/34 , A61K31/505 , C07D451/06 , A61K31/46 , C07D221/20 , A61K31/438 , C07D213/74 , C07D417/04
CPC classification number: C07D493/04 , A61K31/437 , A61K31/438 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/46 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/64 , C07D213/74 , C07D221/20 , C07D239/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D451/06 , C07D471/04
Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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公开(公告)号：US09527839B2
公开(公告)日：2016-12-27
申请号：US14420090
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: C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/4184 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/5377 , A61K45/06
CPC classification number: C07D417/14 , A61K31/4184 , A61K31/4196 , A61K31/427 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D405/12 , C07D405/14 , C07D413/14
Abstract: Novel compounds described herein 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: 本文所述的新型化合物是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：US10189819B2
公开(公告)日：2019-01-29
申请号：US15534029
申请日：2015-12-07
Applicant: MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD
Inventor： Ting Zhang , Yi-Heng Chen , Liangqin Guo , Alan Hruza , Tianying Jian , Bing Li , Dongfang Meng , Dann L. Parker , Edward C. Sherer , Harold B. Wood , Isao Sakurada
IPC: C07D403/12 , C07D401/14 , C07D401/12 , C07D471/04 , C07D413/14 , C07D413/12 , 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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
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公开(公告)号：US09868733B2
公开(公告)日：2018-01-16
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 , C07D519/00 , A61K31/366 , A61K31/397 , A61K31/4985 , A61K31/19 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/5377 , C07C53/18
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.
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