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.

公开(公告)号：EP2131657A1

公开(公告)日：2009-12-16

申请号：EP08726028.7

申请日：2008-02-25

申请人： Merck & Co., Inc.

发明人： HOYT, Scott, B. ,  OK, Dong ,  OK, Hyun, O. ,  LONDON, Clare ,  DUFFY, Joseph, L.

IPC分类号： A01N43/62 ,  A61K31/55

CPC分类号： C07D281/10 ,  C07D245/06 ,  C07D267/14

摘要： The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.

公开(公告)号：EP2032539A2

公开(公告)日：2009-03-11

申请号：EP07795744.7

申请日：2007-06-05

申请人： Merck & Co., Inc.

发明人： HOYT, Scott, B. ,  LONDON, Clare ,  OK, Dong ,  PARSONS, William, H.

IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P29/00 ,  A61P29/02

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzazepinone compounds represented by Formula (I), 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, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, 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.