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1.发明申请公开(公告)号：US20200369657A1
公开(公告)日：2020-11-26
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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公开(公告)号：US20160075724A1
公开(公告)日：2016-03-17
申请号：US14875438
申请日：2015-10-05
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallet , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： C07F7/10 , C07D413/04 , C07D233/32 , C07D417/10 , C07D285/06 , C07D207/26 , C07D233/52 , C07D413/10 , C07D263/22 , C07D401/04
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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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：US20140221383A1
公开(公告)日：2014-08-07
申请号：US14252256
申请日：2014-04-14
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallet , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： C07D417/04 , A61K31/497 , A61K31/506 , A61K31/4439 , A61K31/433 , A61K31/427 , A61K31/421 , A61K31/4166 , A61K31/4168 , A61K31/4015 , C07D413/04 , C07D285/10 , C07D417/10 , C07D263/26 , C07D233/38 , C07D233/50 , C07D207/27 , C07D413/10 , A61K31/422 , A61K45/06 , A61K31/501
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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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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7.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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8.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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