公开(公告)号：EP0904079B1

公开(公告)日：2004-03-24

申请号：EP97905669.4

申请日：1997-01-31

申请人： MERCK & CO., INC.

发明人： ADAMS, Alan, D. ,  BERGER, Gregory, D. ,  BERGMAN, Jeffrey, P. ,  BERGER, Joel, P. ,  HAN, Wei ,  LEIBOWITZ, Mark, D. ,  MOLLER, David, E. ,  SANTINI, Conrad ,  SAHOO, Soumya ,  TOLMAN, Richard, L. ,  YOUNG, Jonathan, R.

IPC分类号： A61K31/47 ,  A61K31/40 ,  A61K31/35 ,  A61K31/34 ,  C07D401/00 ,  C07D209/04 ,  C07D307/77 ,  C07D311/64 ,  C07D311/78

CPC分类号： C07D311/16 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K45/06 ,  C07D209/08 ,  C07D217/06 ,  C07D231/56 ,  C07D239/74 ,  C07D249/18 ,  C07D261/20 ,  C07D263/57 ,  C07D271/08 ,  C07D271/12 ,  C07D275/04 ,  C07D307/79 ,  C07D307/82 ,  C07D307/83 ,  C07D307/91

摘要： The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

公开(公告)号：EP1040102A1

公开(公告)日：2000-10-04

申请号：EP98963283.1

申请日：1998-12-18

申请人： MERCK & CO., INC.

发明人： SAHOO, Soumya, P. ,  TOLMAN, Richard, L. ,  HAN, Wei ,  BERGMANN, Jeffrey ,  SANTINI, Conrad ,  LOMBARDO, Vicki, R. ,  DESAI, Ranjit ,  BOUERES, Julia, K. ,  GRATALE, Dominick, F.

IPC分类号： C07D277/34 ,  C07D417/12 ,  A61K31/425

CPC分类号： C07D263/44 ,  C07D277/34 ,  C07D417/12

摘要： Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR α, δ and/or η mediated diseases, disorders and conditions.

摘要翻译： 取代的5-芳基-2,4-噻唑烷二酮是PPAR的有效激动剂，因此可用于治疗，控制或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPAR α，δ和/或η介导的疾病，病症和病症。

公开(公告)号：EP0904079A1

公开(公告)日：1999-03-31

申请号：EP97905669.0

申请日：1997-01-31

申请人： MERCK & CO., INC.

发明人： ADAMS, Alan, D. ,  BERGER, Gregory, D. ,  BERGMAN, Jeffrey, P. ,  BERGER, Joel, P. ,  HAN, Wei ,  LEIBOWITZ, Mark, D. ,  MOLLER, David, E. ,  SANTINI, Conrad ,  SAHOO, Soumya ,  TOLMAN, Richard, L. ,  YOUNG, Jonathan, R.

IPC分类号： A61K31 ,  A61K45 ,  A61P3 ,  A61P9 ,  C07D209 ,  C07D217 ,  C07D231 ,  C07D239 ,  C07D249 ,  C07D261 ,  C07D263 ,  C07D271 ,  C07D275 ,  C07D307 ,  C07D311

CPC分类号： C07D311/16 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K45/06 ,  C07D209/08 ,  C07D217/06 ,  C07D231/56 ,  C07D239/74 ,  C07D249/18 ,  C07D261/20 ,  C07D263/57 ,  C07D271/08 ,  C07D271/12 ,  C07D275/04 ,  C07D307/79 ,  C07D307/82 ,  C07D307/83 ,  C07D307/91

摘要： The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

公开(公告)号：EP2112880A2

公开(公告)日：2009-11-04

申请号：EP07862712.2

申请日：2007-12-10

申请人： Merck & Co., Inc.

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

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： C07D211/26 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： Bipiperidyl 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：EP1040102B1

公开(公告)日：2007-01-24

申请号：EP98963283.1

申请日：1998-12-18

申请人： Merck & Co., Inc.

发明人： SAHOO, Soumya, P. ,  TOLMAN, Richard, L. ,  HAN, Wei ,  BERGMANN, Jeffrey ,  SANTINI, Conrad ,  LOMBARDO, Vicki, R. ,  DESAI, Ranjit ,  BOUERES, Julia, K. ,  GRATALE, Dominick, F.

IPC分类号： C07D277/34 ,  C07D263/44 ,  C07D417/12 ,  A61K31/425

CPC分类号： C07D263/44 ,  C07D277/34 ,  C07D417/12

摘要： Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR α, δ and/or η mediated diseases, disorders and conditions.

公开(公告)号：EP1194146B1

公开(公告)日：2006-07-19

申请号：EP00944694.9

申请日：2000-06-16

申请人： Merck & Co., Inc.

发明人： SAHOO, Soumya, P. ,  SANTINI, Conrad ,  BOUERES, Julia, K. ,  HECK, James, V. ,  METZGER, Edward ,  LOMBARDO, Victoria, K.

IPC分类号： C07D277/34 ,  A61K31/426 ,  A61K31/427 ,  A61K31/497 ,  C07D417/12

CPC分类号： C07D277/34 ,  C07D417/12

摘要： Substituted 5-aryl-2,4-thiazolidinediones or 5-aryl-2,4-oxazolidinediones that also carry a second substituent in the 5-position of the heterocyclic ring are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR α, δ and/or η mediated diseases, disorders and conditions.

摘要翻译： 在杂环5位还带有第二个取代基的取代的5-芳基-2,4-噻唑烷二酮或5-芳基-2,4-恶唑烷二酮是有效的PPAR激动剂，因此可用于治疗，对照 或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPARα，δ和/或η介导的疾病，病症和病症。

公开(公告)号：EP0882029B1

公开(公告)日：2003-04-02

申请号：EP97904210.8

申请日：1997-01-31

申请人： MERCK & CO., INC.

发明人： ADAMS, Alan, D. ,  BERGER, Joel, P. ,  BERGER, Gregory, D. ,  FITCH, Kenneth, J. ,  GRAHAM, Donald, W. ,  JONES, Anthony, B. ,  VON LANGEN, Derek ,  LEIBOWITZ, Mark, D. ,  MOLLER, David, E. ,  PATCHETT, Arthur, A. ,  SANTINI, Conrad ,  SAHOO, Soumya, P. ,  TOLMAN, Richard, L. ,  TOUPENCE, Richard, B. ,  WALSH, Thomas, F.

IPC分类号： C07D261/20 ,  C07D275/04 ,  A61K31/42 ,  A61K31/425 ,  C07D263/56 ,  C07D231/56 ,  C07D249/18 ,  C07D239/74 ,  A61K31/505 ,  A61K31/415 ,  A61K31/41

CPC分类号： C07D311/16 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K45/06 ,  C07D209/08 ,  C07D217/04 ,  C07D231/56 ,  C07D239/74 ,  C07D249/18 ,  C07D261/20 ,  C07D263/57 ,  C07D271/08 ,  C07D275/04 ,  C07D307/79 ,  C07D307/82 ,  C07D307/91

摘要： The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

公开(公告)号：EP0882029A1

公开(公告)日：1998-12-09

申请号：EP97904210.0

申请日：1997-01-31

申请人： MERCK & CO., INC.

发明人： ADAMS, Alan, D. ,  BERGER, Joel, P. ,  BERGER, Gregory, D. ,  FITCH, Kenneth, J. ,  GRAHAM, Donald, W. ,  JONES, Anthony, B. ,  VON LANGEN, Derek ,  LEIBOWITZ, Mark, D. ,  MOLLER, David, E. ,  PATCHETT, Arthur, A. ,  SANTINI, Conrad ,  SAHOO, Soumya, P. ,  TOLMAN, Richard, L. ,  TOUPENCE, Richard, B. ,  WALSH, Thomas, F.

IPC分类号： A61K31 ,  A61K45 ,  A61P3 ,  C07D209 ,  C07D217 ,  C07D231 ,  C07D239 ,  C07D249 ,  C07D261 ,  C07D263 ,  C07D271 ,  C07D275 ,  C07D307 ,  C07D311

CPC分类号： C07D311/16 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K45/06 ,  C07D209/08 ,  C07D217/04 ,  C07D231/56 ,  C07D239/74 ,  C07D249/18 ,  C07D261/20 ,  C07D263/57 ,  C07D271/08 ,  C07D275/04 ,  C07D307/79 ,  C07D307/82 ,  C07D307/91

摘要： The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

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：EP1988900A2

公开(公告)日：2008-11-12

申请号：EP07751385.1

申请日：2007-02-20

申请人： Merck & Co., Inc.

发明人： ADAMS, Alan, D. ,  SANTINI, Conrad

IPC分类号： A61K31/496

CPC分类号： C07D471/04 ,  C07D401/14

摘要： The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.