公开(公告)号：EP3076959B1

公开(公告)日：2018-07-04

申请号：EP14868525.8

申请日：2014-12-01

申请人： Merck Sharp & Dohme Corp.

发明人： BARA, Thomas ,  CHOBANIAN, Harry ,  GUO, Yan ,  JOSIEN, Hubert ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher W. ,  YANG, Cangming ,  XIAO, Dong

IPC分类号： C07C59/72 ,  C07C255/59 ,  C07D221/04 ,  C07D231/12 ,  C07D333/24 ,  C07D417/04 ,  C07D249/04 ,  C07D471/04 ,  C07D207/333 ,  C07D277/42 ,  C07D209/08 ,  C07D209/12 ,  C07D213/64 ,  A61K31/075 ,  A61K45/06 ,  A61P3/10

CPC分类号： C07C59/72 ,  A61K31/192 ,  A61K31/277 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61K45/06 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/06 ,  C07C2602/08 ,  C07D207/333 ,  C07D209/08 ,  C07D209/12 ,  C07D213/64 ,  C07D221/04 ,  C07D231/12 ,  C07D249/04 ,  C07D277/42 ,  C07D333/24 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP2627178B1

公开(公告)日：2018-05-02

申请号：EP11833150.3

申请日：2011-10-06

申请人： Merck Sharp & Dohme Corp.

发明人： PALANI, Anandan ,  ASLANIAN, Robert, G. ,  BOYCE, Christopher, W. ,  MAZZOLA, Robert, D.,Jr. ,  MCKITTRICK, Brian, A. ,  MCCORMICK, Kevin, D. ,  QIN, Jun ,  TANG, Haiqun ,  XIAO, Dong ,  YU, Younong ,  CALDWELL, John, P. ,  KELLEY, Elizabeth, Helen ,  ZHANG, Hongjun ,  SILIPHAIVANH, Phieng ,  MACCOSS, Rachel, N. ,  METHOT, Joey, L. ,  GAUUAN, Jolicia Polivina ,  JIANG, Qin ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DONG, Li ,  HUANG, Xianhai ,  SHAO, Ning ,  ZHOU, Wei ,  DHONDI, Pawan, K. ,  RAO, Ashwin, U.

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/91 ,  A61K31/517 ,  A61K31/5395 ,  A61K31/55 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10

摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.

公开(公告)号：EP1885726B1

公开(公告)日：2016-12-14

申请号：EP06759539.7

申请日：2006-05-11

申请人： Merck Sharp & Dohme Corp.

发明人： PALANI, Anandan ,  SU, Jing ,  XIAO, Dong ,  HUANG, Xianhai ,  RAO, Ashwin, U. ,  CHEN, Xiao ,  TANG, Haiqun ,  QIN, Jun ,  HUANG, Ying ,  ASLANIAN, Robert, G. ,  MCKITTRICK, Brian

IPC分类号： C07D491/04

CPC分类号： C07D471/04 ,  C07D491/04 ,  C07D491/052

公开(公告)号：EP3013333A1

公开(公告)日：2016-05-04

申请号：EP14816671.3

申请日：2014-06-19

申请人： Merck Sharp & Dohme Corp.

发明人： HE, Shuwen ,  LAI, Zhong ,  DAI, Xing ,  XIAO, Dong ,  LONDON, Clare ,  ZORN, Nicolas ,  NARGUND, Ravi ,  PALANI, Anandan ,  MCCOMAS, Casey, C. ,  LI, Peng ,  PENG, Xuanjia

IPC分类号： A61K31/343

CPC分类号： A61K31/454 ,  A61K31/404 ,  A61K31/423 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

公开(公告)号：EP2627178A1

公开(公告)日：2013-08-21

申请号：EP11833150.3

申请日：2011-10-06

申请人： Merck Sharp & Dohme Corp.

发明人： PALANI, Anandan ,  ASLANIAN, Robert, G. ,  BOYCE, Christopher, W. ,  MAZZOLA, Robert, D.,Jr. ,  MCKITTRICK, Brian, A. ,  MCCORMICK, Kevin, D. ,  QIN, Jun ,  TANG, Haiqun ,  XIAO, Dong ,  YU, Younong ,  CALDWELL, John, P. ,  KELLEY, Elizabeth, Helen ,  ZHANG, Hongjun ,  SILIPHAIVANH, Phieng ,  MACCOSS, Rachel, N. ,  METHOT, Joey, L. ,  GAUUAN, Jolicia, Polivina ,  JIANG, Qin ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DONG, Li ,  HUANG, Xianhai ,  SHAO, Ning ,  ZHOU, Wei ,  DHONDI, Pawan, K. ,  RAO, Ashwin, U.

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/91 ,  A61K31/517 ,  A61K31/5395 ,  A61K31/55 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10

摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH
2 receptor.

公开(公告)号：EP2953461B1

公开(公告)日：2020-04-22

申请号：EP14749562.6

申请日：2014-02-03

申请人： Merck Sharp & Dohme Corp.

发明人： DAI, Xing ,  LIU, Hong ,  PALANI, Anandan ,  HE, Shuwen ,  LAI, Zhong ,  NARGUND, Ravi ,  MARCANTONIO, Karen ,  XIAO, Dong ,  BROCKUNIER, Linda, L. ,  ZORN, Nicolas ,  DANG, Qun ,  PENG, Xuanjia ,  LI, Peng

IPC分类号： A61K31/519 ,  A61P31/14 ,  C07D471/14

公开(公告)号：EP3013333B1

公开(公告)日：2019-03-27

申请号：EP14816671.3

申请日：2014-06-19

申请人： Merck Sharp & Dohme Corp.

发明人： HE, Shuwen ,  LAI, Zhong ,  DAI, Xing ,  XIAO, Dong ,  LONDON, Clare ,  ZORN, Nicolas ,  NARGUND, Ravi ,  PALANI, Anandan ,  MCCOMAS, Casey, C. ,  LI, Peng ,  PENG, Xuanjia

IPC分类号： C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/343 ,  A61P31/04

公开(公告)号：EP3307067A1

公开(公告)日：2018-04-18

申请号：EP16808075.2

申请日：2016-06-06

申请人： Merck Sharp & Dohme Corp.

发明人： ZHENG, Junying ,  WON, Walter ,  BERLIN, Michael ,  TING, Pauline ,  LI, Guoqing ,  XIAO, Dong ,  WANG, Hongwu ,  ASLANIAN, Robert

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： A61K31/4162 ,  A01N43/80 ,  A61K31/497 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  C07D487/10 ,  A01N25/04

摘要： Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: "Z", R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：EP3076959A1

公开(公告)日：2016-10-12

申请号：EP14868525.8

申请日：2014-12-01

申请人： Merck Sharp & Dohme Corp.

发明人： BARA, Thomas ,  CHOBANIAN, Harry ,  GUO, Yan ,  JOSIEN, Hubert ,  MILLER, Michael ,  PIO, Barbara ,  PLUMMER, Christopher W. ,  YANG, Cangming ,  XIAO, Dong

IPC分类号： A61K31/075

CPC分类号： C07C59/72 ,  A61K31/192 ,  A61K31/277 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61K45/06 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/06 ,  C07C2602/08 ,  C07D207/333 ,  C07D209/08 ,  C07D209/12 ,  C07D213/64 ,  C07D221/04 ,  C07D231/12 ,  C07D249/04 ,  C07D277/42 ,  C07D333/24 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP3013834A1

公开(公告)日：2016-05-04

申请号：EP14817438.6

申请日：2014-06-19

申请人： Merck Sharp & Dohme Corp.

发明人： DAI, Xing ,  LIU, Hong ,  PALANI, Anandan ,  HE, Shuwen ,  NARGUND, Ravi ,  XIAO, Dong ,  ZORN, Nicolas ,  DANG, Qun ,  MCCOMAS, Casey, C. ,  PENG, Xuanjia ,  LI, Peng ,  SOLL, Richard

IPC分类号： C07D498/04

CPC分类号： A61K31/5365 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D475/02 ,  C07D498/04

摘要： The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. (I)

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这类化合物的合成，以及这些化合物用于抑制HCV NS5B聚合酶活性，用于治疗或预防HCV感染的用途的式I化合物和 在基于细胞的系统中抑制HCV病毒复制和/或病毒产生。 （一世）