公开(公告)号：EP2136803A1

公开(公告)日：2009-12-30

申请号：EP08742913.0

申请日：2008-04-15

申请人： Merck & Co., Inc.

发明人： BALKOVEC, James, M. ,  THIERINGER, Rolf ,  WADDELL, Sherman, T.

IPC分类号： A61K31/4196 ,  A61P35/00

CPC分类号： A61K31/4196 ,  A61K31/4245

摘要： The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.

公开(公告)号：EP1474139A2

公开(公告)日：2004-11-10

申请号：EP03705952.4

申请日：2003-01-28

申请人： Merck & Co., Inc.

发明人： BALKOVEC, James, M. ,  THIERINGER, Rolf ,  MUNDT, Steven, S. ,  HERMANOWSKI-VOSATKA, Anne ,  GRAHAM, Donald, W. ,  PATEL, Gool, F. ,  ASTER, Susan, D. ,  WADDELL, Sherman, T. ,  OLSON, Steven, H. ,  MALETIC, Milana

IPC分类号： A61K31/4196 ,  C07D249/12 ,  C07D249/16

CPC分类号： A61K31/4196 ,  A61K45/06 ,  C07D249/08 ,  C07D249/12 ,  C07D249/14 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/14 ,  C07D513/04 ,  A61K2300/00

摘要： Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.

公开(公告)号：EP1940393A2

公开(公告)日：2008-07-09

申请号：EP06817031.5

申请日：2006-10-16

申请人： Merck & Co., Inc.

发明人： WADDELL, Sherman, T. ,  BALKOVEC, James, M. ,  KEVIN, Nancy, J. ,  GU, Xin

IPC分类号： A61K31/41

CPC分类号： C07D413/08

摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

摘要翻译： 结构式I的三唑衍生物是11β-羟基类固醇脱氢酶-1的选择性抑制剂。 这些化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合症和其他与NIDDM相关的症状。

公开(公告)号：EP1797034A1

公开(公告)日：2007-06-20

申请号：EP05777427.5

申请日：2005-08-03

申请人： Merck & Co., Inc.

发明人： WADDELL, Sherman, T. ,  BALKOVEC, James, M. ,  SANTORELLI, Gina, M. ,  LEEMAN, Aaron, H. ,  MALETIC, Milana ,  GU, Xin

IPC分类号： C07D209/02 ,  C07D221/22 ,  A61K31/403 ,  A61K31/46

CPC分类号： C07D209/02 ,  C07C317/44 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2603/74 ,  C07D223/14

摘要： Sulfonyl derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.

公开(公告)号：EP1638947A2

公开(公告)日：2006-03-29

申请号：EP04753355.9

申请日：2004-05-26

申请人： Merck & Co., Inc.

发明人： WADDELL, Sherman, T. ,  SANTORELLI, Gina, M. ,  MALETIC, Milana, M. ,  LEEMAN, Aaron, H. ,  GU, Xin ,  GRAHAM, Donald, W. ,  BALKOVEC, James, M. ,  ASTER, Susan, D.

IPC分类号： C07D249/08 ,  C07D249/16 ,  A61K31/4196

CPC分类号： C07D249/08 ,  C07D249/16 ,  C07D413/08 ,  C07D487/04

摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

公开(公告)号：EP1090001A1

公开(公告)日：2001-04-11

申请号：EP99931871.0

申请日：1999-06-23

申请人： MERCK & CO., INC.

发明人： RATCLIFFE, Ronald, W. ,  WADDELL, Sherman, T. ,  MORGAN, Jerry, D., II ,  BLIZZARD, Timothy, A.

IPC分类号： C07D477/14 ,  A61K31/40

CPC分类号： C07D477/14

摘要： Compounds of formula (I): as well as pharmaceutically acceptable salts thereof are disclosed.

公开(公告)号：EP1973915A2

公开(公告)日：2008-10-01

申请号：EP07709583.4

申请日：2007-01-09

申请人： Merck & Co., Inc.

发明人： KEVIN, Nancy, J. ,  GU, Xin ,  WADDELL, Sherman, T.

IPC分类号： C07D487/02 ,  A61K31/4196 ,  A61K31/506

CPC分类号： C07D249/08 ,  C07D413/08

摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

公开(公告)号：EP1581515B1

公开(公告)日：2007-10-10

申请号：EP03814074.5

申请日：2003-12-16

申请人： Merck & Co., Inc.

发明人： WADDELL, Sherman, T. ,  SANTORELLI, Gina, M. ,  MALETIC, Milana, M. ,  LEEMAN, Aaron, H. ,  GU, Xin ,  GRAHAM, Donald, W. ,  BALKOVEC, James, M. ,  ASTER, Susan, D.

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D413/08 ,  A61K31/4196 ,  A61K31/4245 ,  A61P3/10

CPC分类号： C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/08 ,  C07D405/04 ,  C07D409/04 ,  C07D413/08 ,  C07D417/08

摘要： Triazole derivatives of structural formula (I) are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

公开(公告)号：EP1653949A2

公开(公告)日：2006-05-10

申请号：EP04779954.9

申请日：2004-08-03

申请人： Merck & Co., Inc.

发明人： GAO, Ying-Duo ,  GU, Xin ,  KEVIN, Nancy, J. ,  WADDELL, Sherman, T.

IPC分类号： A61K31/415 ,  C07D231/16

CPC分类号： C07D231/14 ,  C07D405/04 ,  C07D409/04

摘要： Pyrazole carboxamides of structural formula (I) are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

公开(公告)号：EP0750620A1

公开(公告)日：1997-01-02

申请号：EP95914683.0

申请日：1995-03-10

申请人： Merck & Co., Inc.

发明人： BLIZZARD, Timothy, A. ,  RATCLIFFE, Ronald, W. ,  WADDELL, Sherman, T. ,  SZUMILOSKI, Sandra, P. ,  WILKENING, Robert, R. ,  WILDONGER, Kenneth, J.

IPC分类号： C07D477 ,  A61K31 ,  A61P31

CPC分类号： C07D477/20

摘要： Carbapenems of formula (I) are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.