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1.发明授权
公开(公告)号：EP1278520B1
公开(公告)日：2006-03-01
申请号：EP00978439.8
申请日：2000-11-09
申请人： Merck & Co., Inc.
发明人： BIFTU, Tesfaye , FENG, Danqing, D. , LIANG, Gui-Bai , PONPIPOM, Mitree, M. , QIAN, Xiaoxia , FISHER, Michael, H. , WYVRATT, Matthew, J.
IPC分类号： A61K31/445 , C07D401/14
CPC分类号： C07D401/14 , A23K20/116 , A23K50/75 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
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2.发明授权3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权3-氨基-4-PHENYLBUTANSÄUREDERIVATEALS抑制剂的二肽为糖尿病治疗或预防
公开(公告)号：EP1624874B1
公开(公告)日：2009-11-04
申请号：EP04751840.2
申请日：2004-05-10
申请人： Merck & Co., Inc.
IPC分类号： C07D487/04 , A61K31/55 , A61P3/10
CPC分类号： C07D487/04
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives 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.
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3.发明公开AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权AMINOTETRAHYDROPYRANE ALS二肽基肽酶IV抑制剂为糖尿病治疗或预防
公开(公告)号：EP2001883A2
公开(公告)日：2008-12-17
申请号：EP07754011.0
申请日：2007-03-26
申请人： Merck & Co., Inc.
发明人： BIFTU, Tesfaye , WEBER, Ann, E.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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.
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4.发明公开AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权氨基环己烷ALS二肽基肽酶IV抑制剂，用于治疗或 预防糖尿病
公开(公告)号：EP1978804A2
公开(公告)日：2008-10-15
申请号：EP07716819.3
申请日：2007-01-19
申请人： Merck & Co., Inc.
发明人： BIFTU, Tesfaye , COX, Jason , FENG, Danqing , MASTRACCHIO, Anthony , QIAN, Xiaoxia , WEBER, Ann, E.
IPC分类号： A01N29/02 , A61K31/035
CPC分类号： C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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.
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5.发明授权BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权杂环β-氨基债券作为二肽用于治疗或抑制剂 预防糖尿病
公开(公告)号：EP1556362B1
公开(公告)日：2008-03-26
申请号：EP03796347.7
申请日：2003-10-14
申请人： Merck & Co., Inc.
IPC分类号： C07D243/08 , A61P3/10 , A61K31/551 , A61K38/04
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
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.
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6.发明公开3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权3-氨基-4-PHENYLBUTANSÄUREDERIVATEALS抑制剂的二肽为糖尿病治疗或预防
公开(公告)号：EP1624874A2
公开(公告)日：2006-02-15
申请号：EP04751840.2
申请日：2004-05-10
申请人： Merck & Co., Inc.
IPC分类号： A61K31/55 , A61P3/10 , C07D491/00
CPC分类号： C07D487/04
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives 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.
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7.发明公开OXADIAZOLE BENZENESULFONAMIDES AS SELECTIVE $g(b) 3? AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY 失效唑BENZOSULFONAMIDE AS选择性β-3用于治疗糖尿病和肥胖症肾上腺素能受体激动剂
公开(公告)号：EP0906310A1
公开(公告)日：1999-04-07
申请号：EP97929769.0
申请日：1997-06-03
申请人： MERCK & CO., INC.
发明人： BIFTU, Tesfaye , FENG, Danqing, Dennis , FISHER, Michael, H. , KUO, Chan-Hwa , LIANG, Gui-Bai , WEBER, Ann, E. , NAYLOR, Elizabeth, M.
CPC分类号： C07D213/40 , C07D409/14 , C07D413/12 , C07D413/14
摘要： Oxadiazole substituted benzenesulfonamides 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.
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8.发明授权HEXAHYDRODIAZEPINONES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权HEXAHYDRODIAZEPINONE AS二肽基肽IV用于治疗或抑制剂 预防糖尿病
公开(公告)号：EP1651623B1
公开(公告)日：2008-12-17
申请号：EP04779221.3
申请日：2004-07-27
申请人： Merck & Co., Inc.
IPC分类号： C07D243/08 , A61P3/10 , A61K31/551
CPC分类号： C07D243/14 , C07D401/06 , C07D487/04
摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-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.
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9.发明公开BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权杂环β-氨基债券作为二肽用于治疗或抑制剂 预防糖尿病
公开(公告)号：EP1556362A2
公开(公告)日：2005-07-27
申请号：EP03796347.7
申请日：2003-10-14
申请人： Merck & Co., Inc.
IPC分类号： C07D243/08 , A61P3/10 , A61K31/551
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
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.
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10.发明公开AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权AMINOTETRAHYDROPYRANE ALS二肽基肽酶IV抑制剂为糖尿病治疗或预防
公开(公告)号：EP2019677A2
公开(公告)日：2009-02-04
申请号：EP07794835.4
申请日：2007-05-11
申请人： Merck & Co., Inc.
发明人： BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , WEBER, Ann, E.
IPC分类号： A61K31/535 , A61K31/54
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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.
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