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公开(公告)号：US20210214395A1
公开(公告)日：2021-07-15
申请号：US17253815
申请日：2019-06-20
发明人： Yusheng Xiong , Thomas Joseph Tucker , Chengwei Wu , Elisabetta Bianchi , Danila Branca , Angela Dawn Kerekes , Abbas M. Walji , Hubert B. Josien , Fa-Xiang Ding , Hyewon Youm , Alessia Santoprete , Raffaele Ingenito
IPC分类号： C07K7/56
摘要： Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions
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公开(公告)号：US20210284694A1
公开(公告)日：2021-09-16
申请号：US17253864
申请日：2019-06-20
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Joseph R. Stringer , Derek M. LaPlaca , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Mark W. Embrey , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , Alessia Santoprete , Roberto Costante , Immacolata Conte , Stefania Colarusso , Eric J. Gilbert , Aurash Shahripour , Yusheng Xiong
IPC分类号： C07K7/64
摘要： Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.
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3.发明授权公开(公告)号：US09877957B2
公开(公告)日：2018-01-30
申请号：US15508557
申请日：2015-08-31
发明人： Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hyewon Youm
IPC分类号： C07D217/06 , A61K31/47 , C07C13/04 , A61K31/16 , C07D417/12
CPC分类号： A61K31/47 , A61K31/16 , C07C13/04 , C07D217/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
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公开(公告)号：US20220273669A1
公开(公告)日：2022-09-01
申请号：US17611540
申请日：2020-05-18
发明人： Qingmei Hong , Jason E. Imbriglio , Angela D. Kerekes , Tanweer Khan , Claire Lankin , Derun Li , Rui Liang , Pengcheng Patrick Shao , Zhicai Wu , Yusheng Xiong , Feng Ye , Hyewon Youm , Yang Yu , Anthappan Tony Kurissery , Venukrishnan Komanduri
IPC分类号： A61K31/54 , C07D495/04 , C07D519/00 , C07D513/04 , A61K31/4545 , A61K31/438 , A61K31/444
摘要： 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 of cardiometabolic diseases including high blood pressure, heart failure, kidney disease, and diabetes in a subject.
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5.发明授权公开(公告)号：US11008313B2
公开(公告)日：2021-05-18
申请号：US16334605
申请日：2017-09-15
发明人： Jason Eugene Imbriglio , Whitney Lane Petrilli , Yusheng Xiong , Zhe Feng , Hyewon Youm , Wonsuk Chang , Rui Liang , Zhijian Lu , Jerry Andrew Taylor , Scott B. Hoyt
IPC分类号： C07D417/12 , G01N33/58
摘要： The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.
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6.发明申请公开(公告)号：US20170273966A1
公开(公告)日：2017-09-28
申请号：US15508557
申请日：2015-08-31
发明人： Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hyewon Youm
IPC分类号： A61K31/47 , C07C13/04 , A61K31/16 , C07D217/06
CPC分类号： A61K31/47 , A61K31/16 , C07C13/04 , C07D217/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to a compound represented by formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
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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
发明人： 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分类号： C07D491/107 , A61K45/06 , C07D401/14 , C07D413/14
摘要： 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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公开(公告)号：US09828369B2
公开(公告)日：2017-11-28
申请号：US15508562
申请日：2015-08-31
申请人： Merck Sharp & Dohme Corp. , Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hye Won Youm
发明人： Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hyewon Youm
IPC分类号： C07D217/02 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D413/12
CPC分类号： C07D417/12 , A61K45/06 , A61P9/10 , C07D217/02 , C07D217/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio-renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
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公开(公告)号：US20170275274A1
公开(公告)日：2017-09-28
申请号：US15508562
申请日：2015-08-31
申请人： Jason IMBRIGLIO , Clare LONDON , Zhijian LU , James TATA , Yusheng XIONG , Ming YOU , Hye Won YOUM , Merck Sharp & Dohme Corp.
发明人： Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hyewon Youm
IPC分类号： C07D417/12 , C07D217/02 , C07D401/04 , C07D405/12 , C07D401/14 , C07D413/12 , C07D401/12
CPC分类号： C07D417/12 , A61K45/06 , A61P9/10 , C07D217/02 , C07D217/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio-renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
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公开(公告)号：US11306125B2
公开(公告)日：2022-04-19
申请号：US17253815
申请日：2019-06-20
发明人： Yusheng Xiong , Thomas Joseph Tucker , Chengwei Wu , Elisabetta Bianchi , Danila Branca , Angela Dawn Kerekes , Abbas M. Walji , Hubert B. Josien , Fa-Xiang Ding , Hyewon Youm , Alessia Santoprete , Raffaele Ingenito
摘要： Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions
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