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

申请人： Pharmacia Corporation

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.