公开(公告)号：EP1694654A2

公开(公告)日：2006-08-30

申请号：EP04800897.3

申请日：2004-11-05

申请人： Merck & Co., Inc.

发明人： PARK, Min, K. ,  CHAKRAVARTY, Prasun, K. ,  ZHOU, Bishan ,  GONZALEZ, Edward ,  OK, Hyun ,  PALUCKI, Brenda ,  PARSONS, William, H. ,  SISCO, Rosemary ,  FISHER, Michael, H.

IPC分类号： C07D249/10 ,  A61K31/4196 ,  A61P25/00

CPC分类号： C07D249/10 ,  C07D403/10

摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).

公开(公告)号：EP2064204A1

公开(公告)日：2009-06-03

申请号：EP07837478.2

申请日：2007-08-29

申请人： Merck & Co., Inc.

发明人： OGAWA, Anthony ,  UJJAINWALLA, Feroze ,  VANDE BUNTE, Ellen, K. ,  CHU, Lin ,  ONDEYKA, Debra ,  KOPKA, Ihor ,  LI, Bing ,  OK, Hyun ,  PATEL, Minal, J. ,  XU, Jinyou ,  SISCO, Rosemary

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4427 ,  A61K31/501 ,  A61P9/10

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

摘要： The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

公开(公告)号：EP1385508B1

公开(公告)日：2008-05-21

申请号：EP02753819.8

申请日：2002-03-22

申请人： Merck & Co., Inc.

发明人： ASHTON, Wallace, T. ,  CALDWELL, Charles, G. ,  OK, Hyun ,  PARMEE, Emma, R. ,  WEBER, Ann, E.

IPC分类号： A61K31/40 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4178 ,  A61K31/4436 ,  A61K31/4535 ,  C07D207/09 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D417/04 ,  A61P3/10

CPC分类号： C07D417/06 ,  C07D207/09 ,  C07D277/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV 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.

公开(公告)号：EP1385508A1

公开(公告)日：2004-02-04

申请号：EP02753819.8

申请日：2002-03-22

申请人： Merck & Co., Inc.

发明人： ASHTON, Wallace, T. ,  CALDWELL, Charles, G. ,  OK, Hyun ,  PARMEE, Emma, R. ,  WEBER, Ann, E.

IPC分类号： A61K31/40 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4178 ,  A61K31/4436 ,  A61K31/4535 ,  C07D207/09 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D417/04 ,  C07D417/12

CPC分类号： C07D417/06 ,  C07D207/09 ,  C07D277/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV 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.

公开(公告)号：EP0915847A1

公开(公告)日：1999-05-19

申请号：EP97934091.0

申请日：1997-07-21

申请人： MERCK & CO., INC.

发明人： FISHER, Michael, H. ,  NAYLOR, Elizabeth, M. ,  OK, Hyun ,  PARMEE, Emma, R. ,  SHIH, Thomas ,  WEBER, Ann, E.

IPC分类号： C07D277 ,  A61K31 ,  A61P1 ,  A61P3 ,  A61P25 ,  A61P43 ,  C07C311 ,  C07D209 ,  C07D213 ,  C07D215 ,  C07D233 ,  C07D261 ,  C07D271 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D413 ,  C07D417 ,  C07D471 ,  C07D491 ,  C07D495 ,  C07D519

CPC分类号： C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides are selective β3 adrenergic receptor agonists with very little β1 and β2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used as reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

公开(公告)号：EP0757674A1

公开(公告)日：1997-02-12

申请号：EP95917116.0

申请日：1995-04-21

申请人： MERCK & CO., INC.

发明人： FISHER, Michael, H. ,  NAYLOR, Elisabeth, M. ,  OK, Dong ,  WEBER, Ann, E. ,  SHIH, Thomas ,  OK, Hyun

IPC分类号： A61K31 ,  A61P1 ,  A61P3 ,  A61P25 ,  C07C311 ,  C07D209 ,  C07D213 ,  C07D215 ,  C07D233 ,  C07D261 ,  C07D263 ,  C07D271 ,  C07D401 ,  C07D405 ,  C07D413 ,  C07D417 ,  C07D471

CPC分类号： C07D213/73 ,  C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides having formula (I), are selective β3 adrenergic receptor agonists with very little β1 and β2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.