公开(公告)号：EP2121661A1

公开(公告)日：2009-11-25

申请号：EP07862966.4

申请日：2007-12-14

申请人： Merck & Co., Inc.

发明人： WOOD, Harold, B. ,  ADAMS, Alan, D. ,  FREEMAN, Stanley ,  SZEWCZYK, Jason, W. ,  SANTINI, Conrad ,  HUANG, Yong

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/549 ,  A61K31/541 ,  A61K31/5355 ,  A61P3/10

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D413/14

摘要： Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

公开(公告)号：EP1546142A2

公开(公告)日：2005-06-29

申请号：EP03791782.0

申请日：2003-08-28

申请人： Merck & Co., Inc.

发明人： ACTON, John, J., III ,  MEINKE, Peter, T. ,  WOOD, Harold, B. ,  BLACK, Regina, M.

IPC分类号： C07D413/04 ,  A61K31/42

CPC分类号： C07D413/14 ,  C07D413/04

摘要： Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

公开(公告)号：EP1909789A2

公开(公告)日：2008-04-16

申请号：EP06787175.6

申请日：2006-07-14

申请人： Merck & Co., Inc.

发明人： MEINKE, Peter, T. ,  SHI, Guo, Q. ,  WOOD, Harold, B.

IPC分类号： A61K31/44 ,  A61K31/433 ,  A61K31/4245 ,  C07D401/02

CPC分类号： C07D417/14

摘要： Pyridinyloxyphenyl and pyridinyloxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

公开(公告)号：EP1765329A2

公开(公告)日：2007-03-28

申请号：EP05763714.2

申请日：2005-06-28

申请人： Merck & Co., Inc.

发明人： LIU, Kun ,  MEINKE, Peter, T. ,  WOOD, Harold, B.

IPC分类号： A61K31/404 ,  C07D209/04

CPC分类号： C07D413/14 ,  C07D413/10

摘要： Indoles of Formula (I) having -X-aryl-(CH2)x#191-oxazolidinedione and -X-heteroaryl-(CH2)X-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and -X-is a bond or -CH2-, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

摘要翻译： 在吲哚环的N原子上具有-X-芳基 - （CH 2）x＃191-恶唑烷二酮和-X-杂芳基 - （CH 2）x - 恶唑烷二酮取代基的式（I）的吲哚，其中x为0或1， -X-是键或-CH 2 - ，它们的噻唑烷二酮类似物是PPARγ激动剂或部分激动剂，并且可用于治疗和控制II型糖尿病，包括高血糖症，血脂异常，高脂血症，高胆固醇血症，高甘油三酯血症和肥胖症 通常与2型糖尿病有关。

公开(公告)号：EP1537078A1

公开(公告)日：2005-06-08

申请号：EP03791952.9

申请日：2003-08-27

申请人： Merck & Co., Inc.

发明人： ACTON, John, J., III ,  DEBENHAM, Sheryl, D. ,  LIU, Kun ,  MEINKE, Peter, T. ,  WOOD, Harold, B. ,  BLACK, Regina, M.

IPC分类号： C07D209/12 ,  A61K31/404 ,  A61P3/10 ,  C07D401/04 ,  C07D209/36 ,  C07D413/04 ,  C07D209/30 ,  C07D401/06 ,  C07D405/06 ,  C07D403/12 ,  C07D209/10

CPC分类号： C07D209/10 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/36 ,  C07D401/04 ,  C07D401/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/04

摘要： Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

摘要翻译： 具有芳氧基链烷酸取代基或芳基链烷酸取代基的吲哚是PPARγ的激动剂或部分激动剂，并且可用于治疗和控制II型糖尿病症状的高血糖症，以及血脂异常，高脂血症，高胆固醇血症，高甘油三酯血症和肥胖症， 通常与2型糖尿病有关。

公开(公告)号：EP1861382A1

公开(公告)日：2007-12-05

申请号：EP06736976.9

申请日：2006-03-03

申请人： Merck & Co., Inc.

发明人： WOOD, Harold, B. ,  MEINKE, Peter, T. ,  SHI, Guo, Q. ,  ZHANG, Yong

IPC分类号： C07D261/20 ,  C07D307/80 ,  C07D413/04 ,  C07D403/04 ,  C07D239/34 ,  A61K31/416 ,  A61K31/423 ,  A61K31/4439 ,  A61K31/513 ,  A61P3/10

CPC分类号： C07D401/04 ,  C07D239/34 ,  C07D261/20 ,  C07D307/80 ,  C07D403/04 ,  C07D413/04

摘要： Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

公开(公告)号：EP1753423A2

公开(公告)日：2007-02-21

申请号：EP05812065.0

申请日：2005-05-26

申请人： Merck & Co., Inc.

发明人： LIU, Weiguo ,  WOOD, Harold, B. ,  LAU-PHUA, Fiona Wai-Yu

IPC分类号： A61K31/42 ,  C07D413/04

CPC分类号： C07D413/14

摘要： Benzourea compounds of Formula I having aryl-(CH2)x-oxazolidinedione or aryl-(CH2)x-thiazolidinedione substituents on one of the N atoms of the benzourea ring, wherein x is 0 or 1, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia and other symptoms such as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity, that are often associated with type 2 diabetes.

公开(公告)号：EP1515721A1

公开(公告)日：2005-03-23

申请号：EP03734548.5

申请日：2003-06-11

申请人： Merck & Co., Inc.

发明人： CHEN, Meng Hsin ,  LIU, Luping ,  MEINKE, Peter, T. ,  NATARAJAN, Ravi ,  PARSONS, William, H. ,  SHEN, Dong-Ming ,  SHU, Min ,  STELMACH, John, E. ,  WOOD, Harold, B. ,  ZHANG, Fengqi ,  WISNOSKI, David ,  DOHERTY, James, B.

IPC分类号： A61K31/445

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/18 ,  C07D403/10 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07H15/26

摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

公开(公告)号：EP1067925A1

公开(公告)日：2001-01-17

申请号：EP99915076.6

申请日：1999-03-29

申请人： MERCK & CO., INC.

发明人： LIU, Kun ,  JONES, Anthony, B. ,  WOOD, Harold, B. ,  ZHANG, Bei

IPC分类号： A61K31/405 ,  C07D209/08

CPC分类号： A61K31/64 ,  A61K31/10 ,  A61K31/455 ,  A61K31/47 ,  A61K38/28 ,  A61K45/06 ,  C07D209/12 ,  C07D409/10 ,  A61K31/28 ,  A61K2300/00

摘要： Compounds of formula (I) as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.