公开(公告)号：US20210284694A1

公开(公告)日：2021-09-16

申请号：US17253864

申请日：2019-06-20

申请人： Merck Sharp & Dohme corp. ,  Ra Pharmaceuticals, Inc.

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.

公开(公告)号：US09877957B2

公开(公告)日：2018-01-30

申请号：US15508557

申请日：2015-08-31

申请人： 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： 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.

公开(公告)号：US20170273965A1

公开(公告)日：2017-09-28

申请号：US15508550

申请日：2015-08-31

申请人： Merck Sharp & Dohme Corp.

发明人： Jason Imbriglio ,  Rui Liang ,  Clare London ,  Kenneth Marby ,  James Tata ,  Ming You ,  Yusheng Xiong

IPC分类号： A61K31/47 ,  A61K31/16 ,  C07C13/04 ,  C07D217/06

CPC分类号： A61K31/47 ,  A61K31/16 ,  C07C13/04 ,  C07D217/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D411/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

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, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US20170216250A1

公开(公告)日：2017-08-03

申请号：US15484508

申请日：2017-04-11

申请人： Merck Sharp & Dohme Corp.

发明人： Hong-Ping Guan ,  Jose M. Castro-Perez ,  Harry R. Davis ,  Samuel E. Engel ,  Douglas G. Johns ,  Songnian Lin ,  Stephen F. Previs ,  Thomas P. Roddy ,  Liangsu Wang ,  Sheng-Ping Wang ,  Yusheng Xiong

IPC分类号： A61K31/397 ,  A61K31/404 ,  A61K31/415 ,  A61K9/24

CPC分类号： A61K31/397 ,  A61K9/209 ,  A61K31/194 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/44 ,  A61K45/06 ,  A61K2300/00

摘要： Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.

公开(公告)号：US20140235667A1

公开(公告)日：2014-08-21

申请号：US14346403

申请日：2012-09-17

申请人： MERCK SHARP & DOHME CORP.

发明人： Amjad Ali ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Michael Lo ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Brent Whitehead ,  Yusheng Xiong

IPC分类号： A61K31/437 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04

摘要： This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及结构式为I或其药学上可接受的盐的咪唑并吡啶基化合物，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

公开(公告)号：US20220281886A1

公开(公告)日：2022-09-08

申请号：US17611553

申请日：2020-05-18

申请人： Merck Sharp & Dohme Corp.

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.

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.

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.

公开(公告)号：US20210214395A1

公开(公告)日：2021-07-15

申请号：US17253815

申请日：2019-06-20

申请人： Merck Sharp & Dohme Corp.

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

公开(公告)号：US09567333B2

公开(公告)日：2017-02-14

申请号：US14886563

申请日：2015-10-19

申请人： Merck Sharp & Dohme Corp.

发明人： D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Clare London ,  John MacLean ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04

摘要： This invention relates to triazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及结构式的三唑并吡啶基化合物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。