公开(公告)号：EP1021424B1

公开(公告)日：2003-02-26

申请号：EP97931009.1

申请日：1997-06-18

申请人： PHARMACIA & UPJOHN COMPANY

发明人： MITCHELL, Mark, A. ,  SCHOSTAREZ, Heinrich, J. ,  MAGGIORA, Linda, L. ,  LINDBERG, Thomas, J.

IPC分类号： C07D285/135 ,  C07D417/12 ,  C07K5/06 ,  A61K31/41

CPC分类号： C07D285/135 ,  A61K38/00 ,  C07D417/12 ,  C07K5/06165

摘要： The present invention provides novel thiadiazole amide derivatives represented by formula (I). The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.

公开(公告)号：EP1021424A1

公开(公告)日：2000-07-26

申请号：EP97931009.1

申请日：1997-06-18

申请人： PHARMACIA & UPJOHN COMPANY

发明人： MITCHELL, Mark, A. ,  SCHOSTAREZ, Heinrich, J. ,  MAGGIORA, Linda, L. ,  LINDBERG, Thomas, J.

IPC分类号： C07D285/135 ,  C07D417/12 ,  C07K5/06 ,  A61K31/41

CPC分类号： C07D285/135 ,  A61K38/00 ,  C07D417/12 ,  C07K5/06165

摘要： The present invention provides novel thiadiazole amide derivatives represented by formula (I). The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.

摘要翻译： 本发明提供由式（I）表示的新型噻二唑酰胺衍生物。 本发明化合物抑制来自基质金属蛋白酶家族的各种酶，主要是基质溶素，因此可用于治疗基质金属内蛋白酶疾病，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，骨质疏松症如骨质疏松症，肿瘤转移（侵袭和 生长），牙周炎，牙龈炎，角膜溃疡，皮肤溃疡，胃溃疡，炎症和其他与结缔组织降解有关的疾病。

公开(公告)号：EP0793646B1

公开(公告)日：2001-09-05

申请号：EP95939672.2

申请日：1995-11-13

申请人： PHARMACIA & UPJOHN COMPANY

发明人： LARSEN, Scott, D. ,  VAILLANCOURT, Valerie, A. ,  MAY, Paul, D. ,  TANIS, Steven, P. ,  TUCKER, John, A. ,  MEGLASSON, Martin, D. ,  SCHOSTAREZ, Heinrich, J.

IPC分类号： C07C281/16 ,  C07C281/18 ,  A61K31/195

CPC分类号： A61K31/195 ,  A61K31/198 ,  C07C281/16 ,  C07C281/18

公开(公告)号：EP0793646A1

公开(公告)日：1997-09-10

申请号：EP95939672.0

申请日：1995-11-13

申请人： PHARMACIA & UPJOHN COMPANY

发明人： LARSEN, Scott, D. ,  VAILLANCOURT, Valerie, A. ,  MAY, Paul, D. ,  TANIS, Steven, P. ,  TUCKER, John, A. ,  MEGLASSON, Martin, D. ,  SCHOSTAREZ, Heinrich, J.

IPC分类号： A61K31 ,  A61P3 ,  C07C281

CPC分类号： A61K31/195 ,  A61K31/198 ,  C07C281/16 ,  C07C281/18

摘要： The present invention provides novel compounds of the formulae (I): AG-(CH2)n-CO2R1 and (II) or pharmacologically acceptable salts thereof, wherein AG is: a) N-aminoguanidine, b) N,N'-diaminoguanidine, or c) N,N',N'-triaminoguanidine; and n, R?1 and R2¿ have the meanings given in the description as well as a new use for the compounds of formula (III) wherein R3 has the meanings given in the description for the treatment of non-insulin dependent diabetes mellitus (NIDDM).