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1.发明公开AROMATIC SULFONE HYDROXAMIC ACIDS AND THEIR USE AS PROTEASE INHIBITORS 审中-公开芳香SULFONHYDROXAMSÄUREN及其使用蛋白酶抑制剂
公开(公告)号：EP1472244A1
公开(公告)日：2004-11-03
申请号：EP02789749.5
申请日：2002-11-19
发明人： BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , BOEHM, Terri, L. , CARROLL, Jeffery, N. , DECRESCENZO, Gary, A. , FOBIAN, Yvette, M. , FRESKOS, John, N. , GETMAN, Daniel, P. , HOCKERMAN, Susan, L. , HOWARD, Carol, Pearcy , KASSAB, Darren, J. , KOLODZIEJ, Steve, A. , LI, Madeleine, H. , MCDONALD, Joseph, J. , MISCHKE, Deborah, A. , RICO, Joseph, G. , STEHLE, Nathan, W. , TOLLEFSON, Michael, B. , VILLAMIL, Clara, I.
IPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D335/02 , C07D211/66 , C07D401/12 , C07D417/06 , C07D417/12 , C07D413/12
CPC分类号： C07D401/14 , C07D211/66 , C07D231/12 , C07D233/56 , C07D249/08 , C07D309/08 , C07D335/02 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.
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2.发明公开ARYLSULFONYLHYDROXAMIC ACID AND AMIDE DERIVATIVES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开作者芳基磺酰基异羟肟酸和酰胺和它们作为蛋白酶抑制剂衍生物
公开(公告)号：EP1515951A1
公开(公告)日：2005-03-23
申请号：EP03742193.0
申请日：2003-06-25
发明人： CHEN, Yiyuan , FRESKOS, John, N. , GASIECKI, Alan, F. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KHANNA, Ish, K. , KOLODZIEJ, Steve, A. , MANTEGANI, Sergio , MASSA, Mark, A. , MCDONALD, Joseph, J. , MISCHKE, Deborah, A. , NAGY, Mark, A. , PERRONE, Ettore , SCHMIDT, Michelle, A. , SPANGLER, Dale, P. , TALLEY, John, J. , TRIVEDI, Mahima , WYNN, Thomas, A. , RICO, Joseph, G.
IPC分类号： C07D213/34 , C07D211/66 , C07D335/02 , C07D309/08 , C07D405/12 , A61K31/33 , C07C317/24 , A61K31/16
CPC分类号： C07D241/12 , C07C317/46 , C07D211/66 , C07D213/34 , C07D309/08 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as 'matrix metalloprotease' or 'MMP') activity and/or aggrecanase activity. These compounds generally correspond in structure to formula (I): wherein Al, A2, A3, El, E2, E3, and E4 are as defined in this patent. This invention also is directed to compositions of such compounds, intermediates for the syntheses of such compounds, methods for making such compounds, and methods for treating conditions associated with MMP activity and/or aggrecanase activity, particularly pathological conditions.
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