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：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：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：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：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：US07888345B2

公开(公告)日：2011-02-15

申请号：US12308209

申请日：2007-06-05

申请人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

发明人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P29/02

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

摘要翻译： 由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎 抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。