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.

公开(公告)号：EP1406622B1

公开(公告)日：2006-02-22

申请号：EP02737543.5

申请日：2002-06-19

申请人： Merck & Co., Inc.

发明人： BROCKUNIER, Linda ,  PARMEE, Emma ,  WEBER, Ann, E.

IPC分类号： A61K31/445 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5375 ,  C07D211/32 ,  C07D241/04 ,  C07D265/30 ,  C07D295/185 ,  C07D409/06 ,  C07D213/36 ,  C07D239/52 ,  C07D295/18 ,  C07D333/20 ,  C07D403/06 ,  C07D217/22 ,  C07D239/86 ,  C07D275/06 ,  C07D319/18 ,  C07D401/06

CPC分类号： C07D275/06 ,  C07D209/14 ,  C07D213/36 ,  C07D217/22 ,  C07D239/52 ,  C07D239/86 ,  C07D241/04 ,  C07D295/185 ,  C07D319/18 ,  C07D333/20 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

摘要： Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.

公开(公告)号：EP1554256A1

公开(公告)日：2005-07-20

申请号：EP03764528.0

申请日：2003-07-11

申请人： Merck & Co., Inc.

发明人： MATHVINK, Robert, J. ,  EDMONDSON, Scott, D. ,  WEBER, Ann, E.

IPC分类号： C07D239/72 ,  A61K31/519 ,  A61P3/06 ,  A61P3/04 ,  A61P3/08 ,  A61P5/28 ,  A61P35/00

CPC分类号： C07D471/04

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.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防其中涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及二肽基肽酶-IV酶的疾病中的用途。

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.

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.

发明人： BIFTU, Tesfaye ,  LIANG, Gui-Bai ,  QIAN, Xiaoxia ,  WEBER, Ann, E. ,  FENG, Danqing Dennis

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.

公开(公告)号：EP1784188A2

公开(公告)日：2007-05-16

申请号：EP05788858.8

申请日：2005-08-19

申请人： Merck & Co., Inc.

发明人： WEBER, Ann, E. ,  ASHTON, Wallace, T.

IPC分类号： A61K31/495 ,  A61K31/44 ,  A61K31/55 ,  A61P3/00 ,  C07D471/00 ,  C07D487/00

CPC分类号： C07D471/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04 ,  C07D513/04

摘要： The present invention is directed to novel fused triazole derivatives 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.

公开(公告)号：EP1756106A1

公开(公告)日：2007-02-28

申请号：EP05750136.3

申请日：2005-05-13

申请人： Merck & Co., Inc.

发明人： DUFFY, Joseph, L. ,  KAELIN, David, E., Jr. ,  WEBER, Ann, E. ,  KIRK, Brian, A.

IPC分类号： C07D471/04

CPC分类号： C07D207/27 ,  C07D207/10 ,  C07D211/38 ,  C07D401/08 ,  C07D401/12 ,  C07D413/08 ,  C07D471/04

摘要： The present invention is directed to novel cyclohexylalanine 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.

公开(公告)号：EP1562925A1

公开(公告)日：2005-08-17

申请号：EP03783112.0

申请日：2003-11-03

申请人： Merck & Co., Inc.

发明人： COLANDREA, Vincent, J. ,  EDMONDSON, Scott, D. ,  MATHVINK, Robert, J. ,  MASTRACCHIO, Anthony ,  WEBER, Ann, E. ,  XU, Jinyou

IPC分类号： C07D295/18 ,  C07D207/10 ,  C07D403/10 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10 ,  C07D403/12 ,  C07D471/04 ,  C07D403/06 ,  C07D487/04 ,  C07D205/04 ,  C07D211/38 ,  C07D213/64 ,  A61K31/40 ,  A61K31/395 ,  A61K31/445 ,  A61P3/10

CPC分类号： C07D205/04 ,  C07D207/10 ,  C07D211/38 ,  C07D213/64 ,  C07D295/185 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04

摘要： The present invention is directed to phenylalanine 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.

公开(公告)号：EP1406872A2

公开(公告)日：2004-04-14

申请号：EP02744447.0

申请日：2002-06-19

申请人： Merck & Co., Inc.

发明人： EDMONDSON, Scott, D. ,  PARMEE, Emma ,  WEBER, Ann, E. ,  XU, Jinyou

IPC分类号： C07D207/00 ,  A61K31/40

CPC分类号： C07D207/16 ,  C07D207/26 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/06 ,  C07D401/12 ,  C07D403/12 ,  C07D409/06 ,  C07D413/12 ,  C07D417/12

摘要： Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.

摘要翻译： 具有式I的化合物，包括其药学上可接受的盐和前药：（式I）是二肽基tidyl肽酶-IV酶（DP-IV）的抑制剂，并且可用于治疗DP-IV介导的疾病和病症，例如 非胰岛素依赖性糖尿病。

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.

IPC分类号： A61K31 ,  A61P3 ,  A61P25 ,  A61P43 ,  C07D213 ,  C07D409 ,  C07D413

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.