公开(公告)号：WO2012087861A1

公开(公告)日：2012-06-28

申请号：PCT/US2011/065716

申请日：2011-12-19

申请人： MERCK SHARP & DOHME CORP. ,  SCHERING CORPORATION ,  BOYCE, Christopher, W. ,  DEGRADO, Sylvia Joanna ,  CHEN, Xiao ,  QIN, Jun ,  MAZZOLA, Robert, D., Jr. ,  YU, Younong ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  XIAO, Dong ,  ASLANIAN, Robert George ,  WU, Jie ,  RAO, Ashwin Umesh ,  SILIPHAIVANH, Phieng ,  METHOT, Joey Lee ,  ZHANG, Hongjun ,  KELLEY, Elizabeth Helen ,  BROWN, William Colby ,  JIANG, Qin ,  GAUUAN, Jolicia Polivina ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DHONDI, Pawan, K. ,  DONG, Li ,  FEVRIER, Salem ,  HUANG, Xianhai ,  VACCARO, Henry, M.

发明人： BOYCE, Christopher, W. ,  DEGRADO, Sylvia Joanna ,  CHEN, Xiao ,  QIN, Jun ,  MAZZOLA, Robert, D., Jr. ,  YU, Younong ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  XIAO, Dong ,  ASLANIAN, Robert George ,  WU, Jie ,  RAO, Ashwin Umesh ,  SILIPHAIVANH, Phieng ,  METHOT, Joey Lee ,  ZHANG, Hongjun ,  KELLEY, Elizabeth Helen ,  BROWN, William Colby ,  JIANG, Qin ,  GAUUAN, Jolicia Polivina ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DHONDI, Pawan, K. ,  DONG, Li ,  FEVRIER, Salem ,  HUANG, Xianhai ,  VACCARO, Henry, M.

IPC分类号： C07D241/36 ,  A61K31/498

CPC分类号： C07D241/42 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D241/38 ,  C07D241/44 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

摘要： The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J 1 , J 2 , R 1 , R 2 , R 3 , R 22 , R a , R b , R c , R d , X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with with uncontrolled or inappropriate stimulation of CRTH 2 function.

摘要翻译： 本发明提供了式（I）的某些喹喔啉和氮杂 - 喹喔啉及其药学上可接受的盐，其中J1，J2，R1，R2，R3，R22，Ra，Rb，Rc，Rd，X，Y，b，n ，和q如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能有关的疾病或病症的方法。

公开(公告)号：WO2015073342A1

公开(公告)日：2015-05-21

申请号：PCT/US2014/064722

申请日：2014-11-10

申请人： MERCK SHARP & DOHME CORP. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  COLLETTI, Steven, L. ,  DANG, Qun ,  DHONDI, Pawan, K. ,  GUDE, Candido ,  JOSIEN, Hubert ,  KAR, Nam Fung ,  NAIR, Anilkumar, G. ,  NARGUND, Ravi, P. ,  YANG, De-Yi ,  XIAO, Dong ,  ZHU, Cheng

发明人： BIFTU, Tesfaye ,  BIJU, Purakkattle ,  COLLETTI, Steven, L. ,  DANG, Qun ,  DHONDI, Pawan, K. ,  GUDE, Candido ,  JOSIEN, Hubert ,  KAR, Nam Fung ,  NAIR, Anilkumar, G. ,  NARGUND, Ravi, P. ,  YANG, De-Yi ,  XIAO, Dong ,  ZHU, Cheng

IPC分类号： C07D221/16

CPC分类号： C07D221/16 ,  A61K9/20 ,  A61K31/435 ,  A61K31/444 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/12 ,  C07D487/04 ,  C07D487/10

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：WO2012051036A1

公开(公告)日：2012-04-19

申请号：PCT/US2011/055054

申请日：2011-10-06

申请人： MERCK SHARP & DOHME CORP. ,  SCHERING CORPORATION ,  ASLANIAN, Robert, G. ,  BOYCE, Christopher, W. ,  MAZZOLA, Robert, D., Jr. ,  MCKITTRICK, Brian, A. ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  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.

发明人： ASLANIAN, Robert, G. ,  BOYCE, Christopher, W. ,  MAZZOLA, Robert, D., Jr. ,  MCKITTRICK, Brian, A. ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  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.

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.

摘要翻译： 本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态 受体。