公开(公告)号：US09173873B2

公开(公告)日：2015-11-03

申请号：US14346403

申请日：2012-09-17

申请人： 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

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

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.

公开(公告)号：US20130317057A1

公开(公告)日：2013-11-28

申请号：US13811059

申请日：2011-07-20

申请人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

发明人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

IPC分类号： C07D401/04 ,  C07D413/14 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4439 ,  C07D471/04

CPC分类号： C07D401/04 ,  A61K31/4184 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  C07D413/14 ,  C07D471/04

摘要： The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

摘要翻译： 本发明涉及结构式（I）的化合物及其药学上可接受的盐。 本发明的化合物对选择性抑制CYP11B2有效，因此可用于治疗或预防与升高的醛固酮水平相关的病症，包括但不限于高血压和心力衰竭。

公开(公告)号：US09351973B2

公开(公告)日：2016-05-31

申请号：US14346518

申请日：2012-09-17

申请人： 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

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： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/519 ,  A61P9/12 ,  A61P13/12 ,  A61P9/00 ,  A61P9/10 ,  A61P1/16

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： 本发明涉及以下结构式的吡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。

公开(公告)号：US09382226B2

公开(公告)日：2016-07-05

申请号：US13811059

申请日：2011-07-20

申请人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jiaqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

发明人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jiaqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

IPC分类号： C07D401/04 ,  C07D413/14 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/4709

CPC分类号： C07D401/04 ,  A61K31/4184 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  C07D413/14 ,  C07D471/04

摘要： The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

摘要翻译： 本发明涉及结构式（I）的化合物及其药学上可接受的盐。 本发明的化合物对选择性抑制CYP11B2有效，因此可用于治疗或预防与升高的醛固酮水平相关的病症，包括但不限于高血压和心力衰竭。

公开(公告)号：US09073929B2

公开(公告)日：2015-07-07

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/41 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

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

摘要翻译： 本发明涉及式I的三环三唑类似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成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20140045819A1

公开(公告)日：2014-02-13

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D487/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

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

摘要翻译： 本发明涉及式I的三环三唑类似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成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20150320733A1

公开(公告)日：2015-11-12

申请号：US14651491

申请日：2013-12-17

申请人： Scott B. HOYT ,  Jerry Andrew TAYLOR ,  Clare LONDON ,  Yusheng XIONG ,  Andrew John COOKE ,  MERCK SHARP & DOHME CORP.

发明人： Scott B. Hoyt ,  Jerry Andrew Taylor ,  Clare London ,  Yusheng Xiong ,  Andrew John Cooke

IPC分类号： A61K31/4439 ,  A61K31/497 ,  C07D403/14 ,  C07D401/04 ,  A61K31/4725

CPC分类号： A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14

摘要： This invention relates to indazole compounds of the structural formula: (structure represented) 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 or amelioration of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及结构式为（结构式）的吲唑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，以及可能用于治疗或改善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：US5545790A

公开(公告)日：1996-08-13

申请号：US164272

申请日：1993-12-09

申请人： Margaret M. Wu ,  Yusheng Xiong

发明人： Margaret M. Wu ,  Yusheng Xiong

IPC分类号： C07C2/42 ,  C07C2/00

CPC分类号： C07C2/42 ,  C07C2103/90 ,  C07C2521/08 ,  C07C2523/26

摘要： A catalytic process for the dimerization of norbornene and/or norbornadiene using a reduced valence state Group VIB metal oxide as the catalyst, preferably Cr(II) on a porous support such as silica. The product norbornene dimer or norbornadiene dimer is obtained in high yield and high stereospecificity at greater than 90 weight percent of the exo-trans-exo stereoisomer. The norbornene dimer is useful as a high energy density fuel. The norbornadiene dimer can be further functionalized to yield novel chemical intermediates or polymerized or copolymerized with other olefins. The norbornadiene dimer can also be hydrogenated for high energy fuel applications.

摘要翻译： 使用还原价态VIB族金属氧化物作为催化剂使降冰片烯和/或降冰片二烯二聚的催化方法，优选在多孔载体如二氧化硅上的Cr（II）。 得到的产物降冰片烯二聚体或降冰片二烯二聚物以高产率和高立体定向性获得，其大于90重量％的外 - 反 - 立体异构体。 降冰片烯二聚体可用作高能量密度燃料。 降冰片二烯二聚体可以进一步官能化以产生新的化学中间体或与其它烯烃聚合或共聚。 降冰片二烯二聚体也可以被氢化用于高能燃料应用。