公开(公告)号：US20180362518A1

公开(公告)日：2018-12-20

申请号：US16061815

申请日：2016-12-15

申请人： Thomas J. GRESHOCK ,  James MULHEARN ,  Liangqin GUO ,  Ting ZHANG ,  Deping WANG ,  Ronald M. KIM ,  Mark E. LAYTON ,  Michael J. KELLY, III ,  Rajan ANAND ,  Tianying JIAN ,  Philippe NANTERMET ,  Anthony J. ROECKER ,  Walter WON ,  Gang ZHOU ,  Merck Sharp & Dohme Corp.

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 ,  C07D285/135 ,  C07D277/52 ,  A61P11/14 ,  A61P17/04 ,  A61P25/04 ,  A61P25/02

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

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 Na 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：US07329673B2

公开(公告)日：2008-02-12

申请号：US10548350

申请日：2004-03-31

申请人： Liangqin Guo ,  Shuwen He ,  Tianying Jian ,  Yingjie Lai ,  Jian Liu ,  Ravi P. Nargund ,  Iyassu K. Sebhat ,  Feroze Ujjainwalla ,  Zhixiong Ye ,  Jonathan R. Young

发明人： Liangqin Guo ,  Shuwen He ,  Tianying Jian ,  Yingjie Lai ,  Jian Liu ,  Ravi P. Nargund ,  Iyassu K. Sebhat ,  Feroze Ujjainwalla ,  Zhixiong Ye ,  Jonathan R. Young

IPC分类号： A61K31/438 ,  C07D221/20 ,  C07D401/02

CPC分类号： A61K31/445 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists 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 activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新的N-酰化螺哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，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：US20060183904A1

公开(公告)日：2006-08-17

申请号：US10548350

申请日：2004-03-31

申请人： Liangqin Guo ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Yingjie Lai ,  Ravi Nargund ,  Iyassu Sebhat ,  Feroze Ujjainwalla ,  Zhixiong Ye ,  Jonathan Young

发明人： Liangqin Guo ,  Shuwen He ,  Tianying Jian ,  Jian Liu ,  Yingjie Lai ,  Ravi Nargund ,  Iyassu Sebhat ,  Feroze Ujjainwalla ,  Zhixiong Ye ,  Jonathan Young

IPC分类号： C07D401/00 ,  C07D453/00

CPC分类号： A61K31/445 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists 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 activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

摘要翻译： 某些新的N-酰化螺哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，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：US06680299B2

公开(公告)日：2004-01-20

申请号：US09917107

申请日：2001-07-27

申请人： Yat Sun Or ,  Ly Tam Phan ,  Zhaolin Wang ,  Tianying Jian

发明人： Yat Sun Or ,  Ly Tam Phan ,  Zhaolin Wang ,  Tianying Jian

IPC分类号： A61K3170

CPC分类号： C07H17/08

摘要： There are described novel 4′ substituted 16-membered macrolides and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

摘要翻译： 描述了新颖的4'取代的16元大环内酯和药学上可接受的组合物，其包含治疗有效量的本发明化合物与药学上可接受的载体的组合。 还描述了通过向哺乳动物施用含有治疗有效量的本发明化合物的药物组合物以及制备这些化合物的方法来治疗细菌感染的方法。

公开(公告)号：US10351558B2

公开(公告)日：2019-07-16

申请号：US15550862

申请日：2016-02-12

申请人： Merck Sharp & Dohme Corp. ,  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

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 ,  C07D417/14 ,  A61P9/00 ,  C07D413/14 ,  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：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：US06576615B2

公开(公告)日：2003-06-10

申请号：US10007744

申请日：2001-11-08

申请人： Ly Tam Phan ,  Tianying Jian ,  Yao-Ling Qiu ,  Yat Sun Or

发明人： Ly Tam Phan ,  Tianying Jian ,  Yao-Ling Qiu ,  Yat Sun Or

IPC分类号： A61K3170

CPC分类号： C07H17/08

摘要： There are described novel 4′ substituted tylosin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

摘要翻译： 描述了新颖的4'取代的泰乐菌素类似物和药学上可接受的组合物，其包含治疗有效量的本发明化合物与药学上可接受的载体的组合。 还描述了一种通过向哺乳动物施用含有治疗有效量的本发明化合物的药物组合物及其制备方法来治疗细菌感染的方法。

公开(公告)号：US20180030036A1

公开(公告)日：2018-02-01

申请号：US15534029

申请日：2015-12-07

申请人： Ting ZHANG ,  Yi-Heng CHEN ,  Liangqin GUO ,  Alan HARUZA ,  Tianying JIAN ,  Bing LI ,  Dongfang MENG ,  Dann L. PARKER, JR. ,  Edward C. SHERER ,  Harold B. WOOD ,  Isao SAKURADA ,  MERCK SHARP & DOHME CORP. ,  MOCHIDA PHARMACEUTICAL CO., LTD

发明人： Ting Zhang ,  Yi-Heng Chen ,  Liangqin Guo ,  Alan Hruza ,  Tianying Jian ,  Bing Li ,  Dongfang Meng ,  Dann L. Parker ,  Edward C. Sherer ,  Harold B. Wood ,  Isao Sakurada

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D471/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

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.