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：US09708336B2

公开(公告)日：2017-07-18

申请号：US15110431

申请日：2015-01-16

申请人： Merck Sharp & Dohme Corp.

发明人： Mihir Mandal ,  Haifeng Tang ,  Li Xiao ,  Jing Su ,  Guoqing Li ,  Shu-Wei Yang ,  Weidong Pan ,  Haiqun Tang ,  Reynalda DeJesus ,  Jacqueline Hicks ,  Matthew Lombardo ,  Hong Chu ,  William Hagmann ,  Alex Pasternak ,  Xin Gu ,  Jinlong Jiang ,  Shuzhi Dong ,  Fa-Xiang Ding ,  Clare London ,  Dipshikha Biswas ,  Katherine Young ,  David N. Hunter ,  Zhiqiang Zhao ,  Dexi Yang

IPC分类号： C07D491/048 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D401/04 ,  C07D409/10 ,  C07D487/04 ,  C07D471/10 ,  C07D471/04 ,  C07D451/04 ,  C07D417/14 ,  C07D417/10 ,  C07D413/10 ,  C07D401/14 ,  C07D405/12 ,  C07D405/10 ,  C07D403/10 ,  C07D401/10 ,  C07D413/14 ,  C07D405/14 ,  A61K31/41 ,  C07D257/04 ,  A61K31/197 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427

CPC分类号： C07D491/048 ,  A61K31/197 ,  A61K31/407 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D257/04 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  Y02A50/473 ,  A61K2300/00

摘要： The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

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：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：US10568876B2

公开(公告)日：2020-02-25

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： C07D413/12 ,  A61K31/47 ,  C07D217/06 ,  A61K31/16 ,  C07C13/04

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：US20170020879A1

公开(公告)日：2017-01-26

申请号：US15139361

申请日：2016-04-27

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 ,  Min K. Park ,  Paul Ratcliffe ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： A61K31/519 ,  A61K31/444 ,  C07D487/04 ,  C07D471/04

CPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/444 ,  C07D471/04 ,  C07D487/04

摘要： This invention relates to pyrazolopyridyl 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： 或其药学上可接受的盐，其中所述变量在本文中定义。 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：US09518055B2

公开(公告)日：2016-12-13

申请号：US14885187

申请日：2015-10-16

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 ,  C07D487/04

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

摘要： This invention relates to imidazopyridyl 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.

公开(公告)号：US09193724B2

公开(公告)日：2015-11-24

申请号：US14346438

申请日：2012-09-17

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。