公开(公告)号：US20150274672A1

公开(公告)日：2015-10-01

申请号：US14434524

申请日：2013-10-11

申请人： Mariappan CHELLIAH ,  Hong Dong CHU ,  Jason M. COX ,  John S. DEBENHAM ,  Keith EAGEN ,  Ping LAN ,  Clare LONDON ,  Michael A. PLOTKIN ,  Unmesh SHAH ,  Christopher Joseph SINZ ,  Zhongxiang SUN ,  Henry M. VACCARO ,  Skikanth KATRAMAN ,  MERCK SHARP & DOHME CORP.

发明人： Mariappan Chelliah ,  Hong Dong Chu ,  Jason M. Cox ,  John S. Debenham ,  Keith Eagen ,  Ping Lan ,  Clare London ,  Michael A. Plotkin ,  Unmesh Shah ,  Christopher Joseph Sinz ,  Zhongxiang Sun ,  Henry M. Vaccaro ,  Srikanth Venkatraman

IPC分类号： C07D221/20 ,  C07D401/04 ,  C07D491/107 ,  C07D405/10

CPC分类号： C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/10 ,  C07D491/107

摘要： The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.

摘要翻译： 本发明涉及由式（I）表示的化合物及其药学上可接受的盐，其可用于治疗或预防糖尿病，高脂血症，肥胖，炎症相关疾病及相关疾病和病症。 该化合物可用作G蛋白偶联受体GPR120的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US20140275133A1

公开(公告)日：2014-09-18

申请号：US14350930

申请日：2012-10-08

申请人： Hong Shen ,  Jason M. Cox ,  Hong Dong Chu

发明人： Hong Shen ,  Jason M. Cox ,  Hong Dong Chu

IPC分类号： C07D413/04 ,  C07D413/14 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/506 ,  A61K31/454

CPC分类号： C07D413/04 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  C07D263/44 ,  C07D413/14

摘要： The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).

摘要翻译： 本发明涉及可用于治疗醛固酮介导的疾病的式（I）化合物及其药学上可接受的盐。 本发明还涉及制备式（I）化合物，其可能用于治疗上述疾病和为此目的制备药物的方法，以及包含式（I）化合物的药物组合物。

公开(公告)号：US08716482B2

公开(公告)日：2014-05-06

申请号：US13390708

申请日：2010-09-15

申请人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

发明人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

IPC分类号： C07D211/32 ,  A61K31/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及结构式I的新型取代氨基哌啶，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-κV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20120149683A1

公开(公告)日：2012-06-14

申请号：US13390708

申请日：2010-09-15

申请人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

发明人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

IPC分类号： A61K31/454 ,  C07D401/12 ,  A61K31/497 ,  C07D401/06 ,  A61P3/10 ,  C07D487/04 ,  A61K31/4985 ,  C07D413/06 ,  A61K31/5377 ,  C07D211/56 ,  A61K31/4545

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及结构式I的新型取代氨基哌啶，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-κV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20190352294A1

公开(公告)日：2019-11-21

申请号：US16461849

申请日：2017-11-13

申请人： Ashwin RAO ,  Brian Alexander MCKITTRICK ,  Matthew LOMBARDO ,  Jacqueline D. HICKS ,  Amy Bittner MCCRACKEN ,  Hong Dong CHU ,  Sung-Sau SO ,  Peter ORTH ,  Zhicai WU ,  Ping LAN ,  John S. DEBENHAM ,  Brent R. WHITEHEAD ,  Jerry A. TAYLOR ,  Zhongxiang SUN ,  Revathi Reddy KATIPALLY ,  Jonathan E. GABLE ,  Markus K. DAHLGREN ,  Sathesh P. BHAT ,  Merck Sharp & Dohme Corp.

发明人： Ashwin U. Rao ,  Brian Alexander McKittrick ,  Matthew Lombardo ,  Jacqueline D. Hicks ,  Amy Bittner McCracken ,  Hong Dong Chu ,  Sung-Sau So ,  Peter Orth ,  Zhicai Wu ,  Ping Lan ,  John S. Debenham ,  Brent R. Whitehead ,  Jerry A. Taylor ,  Zhongxiang Sun ,  Revathi Reddy Katipally ,  Jonathan E. Gable ,  Markus K. Dahlgren ,  Sathesh P. Bhat

IPC分类号： C07D413/14 ,  C07D495/04 ,  A61P7/02

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 thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.