发明公开
EP1515951A1 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
- 专利标题： ARYLSULFONYLHYDROXAMIC ACID AND AMIDE DERIVATIVES AND THEIR USE AS PROTEASE INHIBITORS
- 专利标题（中）： 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
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申请号： EP03742193.0申请日： 2003-06-25
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公开(公告)号： EP1515951A1公开(公告)日： 2005-03-23
- 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.
- 申请人： Pharmacia Corporation
- 申请人地址： 700 Chesterfield Parkway West Chesterfield, MO 63017-1732 US
- 专利权人： Pharmacia Corporation
- 当前专利权人： Pharmacia Corporation
- 当前专利权人地址： 700 Chesterfield Parkway West Chesterfield, MO 63017-1732 US
- 代理机构： Albrecht, Thomas, Dr.
- 优先权： US391329P 20020625
- 国际公布： WO2004000811 20031231
- 主分类号： C07D213/34
- IPC分类号： C07D213/34 ; C07D211/66 ; C07D335/02 ; C07D309/08 ; C07D405/12 ; A61K31/33 ; C07C317/24 ; A61K31/16
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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