Publication number: 20060084688
Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.
Type:
Application
Filed:
January 28, 2005
Publication date:
April 20, 2006
Inventors:
Thomas Barta, Daniel Becker, Louis Bedell, Terri Boehm, Jeffery Carroll, Gary DeCrescenzo, Theresa Fletcher, John Freskos, Daniel Getman, Gunnar Hanson, Susan Hockerman, Carol Howard, Stephen Kolodziej, Madeleine Li, Joseph McDonald, Deborah Mischke, Patrick Mullins, Joseph Rico, Nathan Stehle, Clara Villamil
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
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