Publication number: 20060074243
Abstract: 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 A1, A2, A3, E1, 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.
Type:
Application
Filed:
November 10, 2005
Publication date:
April 6, 2006
Inventors:
Daniel Becker, Yiyuan Chen, John Freskos, Alan Gasiecki, Margaret Grapperhaus, Donald Hansen, Robert Heintz, Darren Kassab, Ish Khanna, Stephen Kolodziej, Sergio Mantegani, Mark Massa, Joseph McDonald, Deborah Mischke, Mark Nagy, Ettore Perrone, Joseph Rico, Michelle Schmidt, Dale Spangler, John Talley, Mahima Trivedi, Thomas Wynn
Publication number: 20050009838
Abstract: 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 the following formula: (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.
Type:
Application
Filed:
April 25, 2003
Publication date:
January 13, 2005
Inventors:
Thomas Barta, Daniel Becker, Louis Bedell, Terri Boehm, David Brown, Jeffery Carroll, Yiyuan Chen, Yvette Fobian, John Freskos, Alan Gasiecki, Margaret Grapperhaus, Robert Heintz, Susan Hockerman, Darren Kassab, Ish Khanna, Stephen Kolodziej, Mark Massa, Joseph McDonald, Brent Mischke, Deborah Mischke, Patrick Mullins, Mark Nagy, Monica Norton, Joseph Rico, Michelle Schmidt, Nathan Stehle, John Talley, William Vernier, Clara Villamil, Lijuan Wang, Thomas Wynn
