公开(公告)号：US20180022747A1

公开(公告)日：2018-01-25

申请号：US15550862

申请日：2016-02-12

申请人： Dongfang MENG ,  Hong LI ,  Meng YANG ,  Manuel de Lera RUIZ ,  Sunita V. DEWNANI ,  Tianying JIAN ,  Dann L. PARKER, JR. ,  Ting ZHANG ,  Louis-Charles CAMPEAU ,  Bart HARPER ,  Harold B. WOOD ,  Jiayi XU ,  Richard BERGER ,  Jane Yang WU ,  Robert K. ORR ,  Shawn P. WALSH ,  Merck Sharp & Dohme Corp.

发明人： Dongfang Meng ,  Hong Li ,  Meng Yang ,  Manuel de Lera Ruiz ,  Sunita V. Dewnani ,  Tianying Jian ,  Dann L. Parker, Jr. ,  Ting Zhang ,  Louis-Charles Campeau ,  Harold B. Wood ,  Jiayi Xu ,  Richard Berger ,  Jane Yang Wu ,  Robert K. Orr ,  Shawn P. Walsh ,  Bart Harper

IPC分类号： C07D471/04 ,  C07D403/12 ,  C07D498/04 ,  C07D417/14 ,  C07D513/04 ,  C07D471/14 ,  C07D413/14

CPC分类号： C07D471/04 ,  A61P9/00 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/14 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

公开(公告)号：US08183275B2

公开(公告)日：2012-05-22

申请号：US12311672

申请日：2007-10-16

申请人： Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

发明人： Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

IPC分类号： A61K31/4178 ,  A61K31/4164 ,  C07D471/04 ,  C07D401/10 ,  C07D403/10 ,  C07D233/64

CPC分类号： C07D401/10 ,  C07D233/64 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04

摘要： Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

公开(公告)号：US20100204236A1

公开(公告)日：2010-08-12

申请号：US12311672

申请日：2007-10-16

申请人： Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

发明人： Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

IPC分类号： A61K31/4178 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/425 ,  A61K31/4196 ,  A61K31/4164 ,  C07D471/04 ,  C07D401/10 ,  C07D417/10 ,  C07D405/10 ,  C07D403/10 ,  C07D409/06 ,  C07D233/64 ,  A61P9/10 ,  A61P3/04

CPC分类号： C07D401/10 ,  C07D233/64 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04

摘要： Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

公开(公告)号：US10968210B2

公开(公告)日：2021-04-06

申请号：US16345913

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

发明人： Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D277/52 ,  C07D471/04 ,  C07D487/10 ,  C07D401/12 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.

公开(公告)号：US10519147B2

公开(公告)日：2019-12-31

申请号：US16061815

申请日：2016-12-15

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

发明人： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07D277/52 ,  C07D285/135 ,  A61P25/02 ,  A61P25/04 ,  A61P11/14 ,  A61P17/04

摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US20140088124A1

公开(公告)日：2014-03-27

申请号：US14123246

申请日：2012-06-01

申请人： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

发明人： Robert J. DeVita ,  QingMei Hong ,  Zhong Lai ,  Kevin D. Dykstra ,  Yang Yu ,  Jian Liu ,  Donald M. Sperbeck ,  Tianying Jian ,  Deodial Guiadeen ,  Ginger Xu-qiang Yang ,  Zhicai Wu ,  Shuwen He ,  Pauline C. Ting ,  Robert Aslanian ,  Jeffrey T. Kuethe ,  James Balkovec ,  Rongze Kuang ,  Gang Zhou ,  Heping Wu

IPC分类号： C07D401/14 ,  C07D417/14 ,  C07D493/04 ,  C07D471/04

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04

摘要： Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

摘要翻译： 本文描述的是式（I）的化合物。式I化合物作为DGAT1抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：US08293900B2

公开(公告)日：2012-10-23

申请号：US11992262

申请日：2006-09-25

申请人： Tianying Jian ,  Jian Liu ,  Ravi P. Nargund

发明人： Tianying Jian ,  Jian Liu ,  Ravi P. Nargund

IPC分类号： C07D491/00 ,  C07D491/147

CPC分类号： C07D471/10

摘要： Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新型N-酰化螺哌啶衍生物是人类黑皮质素受体的配体，特别是人黑素皮质素-4受体（MC-4R）的选择性配体。 因此，它们可用于治疗，控制或预防对调节MC-4R的疾病和病症，例如肥胖，糖尿病，尼古丁成瘾，酒精中毒，性功能障碍，包括勃起功能障碍和女性性功能障碍。

公开(公告)号：US20100184758A1

公开(公告)日：2010-07-22

申请号：US12668822

申请日：2008-07-15

申请人： Peter H. Dobbelaar ,  Wu Du ,  Liangqin Guo ,  William K. Hagmann ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Shrenik K. Shah ,  Quang T. Truong ,  Zhixiong Ye ,  James Deliureficio ,  Raman Bakshi

发明人： Peter H. Dobbelaar ,  Wu Du ,  Liangqin Guo ,  William K. Hagmann ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Shrenik K. Shah ,  Quang T. Truong ,  Zhixiong Ye ,  James Deliureficio ,  Raman Bakshi

IPC分类号： A61K31/5377 ,  C07D471/14 ,  A61K31/437 ,  C07D413/14 ,  C07D403/14 ,  A61K31/501 ,  A61K31/4995 ,  A61K31/506 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P9/12

CPC分类号： C07D471/04

摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.

摘要翻译： 结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症， 脂质障碍和高血压。 这些化合物也可用于治疗抑郁症和焦虑症。

公开(公告)号：US20090253744A1

公开(公告)日：2009-10-08

申请号：US12311006

申请日：2007-09-24

申请人： Raman K. Bakshi ,  James P. Dellureficio ,  Qingmei Hong ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Zhixiong Ye

发明人： Raman K. Bakshi ,  James P. Dellureficio ,  Qingmei Hong ,  Tianying Jian ,  Jian Liu ,  Ravi P. Nargund ,  Zhixiong Ye

IPC分类号： A61K31/4545 ,  A61K31/454 ,  C07D407/14 ,  A61P3/04

CPC分类号： C07D405/14 ,  C07D211/26 ,  C07D401/08 ,  C07D405/08 ,  C07D413/08 ,  C07D471/04 ,  C07D487/08 ,  C07D491/08 ,  C07D498/04

摘要： Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新型N-酰化螺哌啶衍生物是人类黑皮质素受体的配体，特别是人黑素皮质素-4受体（MC-4R）的选择性配体。 因此，它们可用于治疗，控制或预防对调节MC-4R的疾病和病症，例如肥胖，糖尿病，尼古丁成瘾，酒精中毒，性功能障碍，包括勃起功能障碍和女性性功能障碍。