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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PIPERIDINYL-AND PIPERAZINYL-SULFONYLMETHYL HYDROXAMIC ACIDS AND THEIR USE AS PROTEASE INHIBITORS 审中-公开哌啶基和PIPERAZINYLSULFONYLMETHYLHYDROXAMSÄUREN及其作为蛋白酶抑制剂
公开(公告)号：EP1689743A2
公开(公告)日：2006-08-16
申请号：EP04810297.4
申请日：2004-11-03
发明人： BROWN, David, L. , GRAPPERHAUS, Margaret, L. , KASSAB, Darren, J. , MASSA, Mark, A. , MCDONALD, Joseph, J. , MULLINS, Patrick, B. , RICO, Joseph, G. , SCHMIDT, Michelle, A.
IPC分类号： C07D407/12
CPC分类号： C07D401/14 , C07D211/66 , C07D211/96 , C07D309/08 , C07D401/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to formula (I); (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
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3.发明公开HETEROARYLSULFONYLMETHYL HYDROXAMIC ACIDS AND AMIDES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开HETEROARYLSULFONYLMETHYLHYDROXAMSÄUREN和酰胺及其作为蛋白酶抑制剂
公开(公告)号：EP1565459A2
公开(公告)日：2005-08-24
申请号：EP03812052.3
申请日：2003-11-24
发明人： BECKER, Daniel, P. , CARROLL, Jeffery, N. , FOBIAN, Yvette, M. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KASSAB, Darren, J. , MASSA, Mark, A. , MCDONALD, Joseph, J. , NAGY, Mark, A. , PITZELE, Barnett, S. , RICO, Joseph, G. , SCHMIDT, Michelle, A. , SPANGLER, Dale, P.
IPC分类号： C07D409/00
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as 'matrix metalloprotease' or 'MMP') activity and/or aggrecanase activity. 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, tumor necrosis factors (or 'TNFs'), and/or aggrecanase activity, particularly pathological conditions.
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4.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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公开(公告)号：EP1504094A2
公开(公告)日：2005-02-09
申请号：EP03750115.2
申请日：2003-05-10
CPC分类号： C07K7/06 , C07K7/08 , C07K14/78 , C12Q1/37 , C12Q2337/00 , G01N2333/96486 , G01N2500/02
摘要： This invention is directed generally to peptide compounds and salts, and particularly to peptide compounds and salts that are useful as protease substrates, such as matrix metalloprotease (“MMP”) substrates. This invention also is directed to methods for making such compounds and salts, as well as amino acids that may, for example, be used in such methods. This invention is further directed to methods for using such compounds and salts to, for example, evaluate the effectiveness of potential protease inhibitors and to detect or monitor a disease associated with protease activity.
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6.发明公开PIPERIDINYL-AND PIPERAZINYL-SULFONYLMETHYL HYDROXAMIC ACID AND THEIR USE AS PROTEASE INHIBITORS 审中-公开哌啶基和PIPERAZINYLSULFONYLMETHYL肟和它们作为蛋白酶抑制剂
公开(公告)号：EP1501827A2
公开(公告)日：2005-02-02
申请号：EP03718529.5
申请日：2003-04-25
发明人： BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , BOEHM, Terri, L. , BROWN, David, L. , CARROLL, Jeffery, N. , CHEN, Yiyuan , FOBIAN, Yvette , FRESKOS, John, N. , GASIECKI, Alan, F. , GRAPPERHAUS, Margaret , HEINTZ, Robert, M. , HOCKERMAN, Susan, L. , KASSAB, Darren, J. , KHANNA, Ish, Kumar , KOLODZIEJ, Stephen, A. , MASSA, Mark , MCDONALD, Joseph , MISCHKE, Brent, V. , MISCHKE, Deborah, A. , MULLINS, Patrick, B. , NAGY, Mark , RICO, Joseph, G. , SCHMIDT, Michelle, A. , STEHLE, Nathan, W. , TALLEY, John, J. , VILLAMILL, Clara, I. , WANG, Lijuan, Jane , WYNN, Thomas, A.
IPC分类号： C07D407/12 , C07D309/08 , C07D211/66 , C07D211/96 , C07D409/14 , C07D417/14 , C07D413/12 , C07D213/74 , C07D401/04 , C07D407/14 , A61K31/496 , A61K31/4535 , A61P35/00
CPC分类号： C07D213/74 , C07D211/66 , C07D211/96 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： This invention is directed generally to proteinase (also known as 'protease') inhibitors, and more particularly, to piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids that inter alia, inhibit matrix metalloproteinase (also known as 'matrix metalloprotease' or 'MMP') activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to formula (I), (Wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
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