P38 MAP kinase naphthyridinone inhibitors

MEDI 356

Rowena Ruzek, rowena_ruzek@merck.com, Department of Medicinal Chemistry, Merck & Co., Inc, WP14-2, PO Box 4, 770 Sumneytown Pike, West Point, PA 19486
Rheumatoid arthritis (RA) is a disease of the connective tissue characterized by inflammation of the peripheral joints resulting in stiffness and pain. This condition may lead to deformation and destruction of the joints. One biological target of interest is the p38 MAP (mitogen activated protein) kinase. This enzyme has been implicated as a factor in inflammatory and autoimmune diseases such as RA and Crohn's disease. P38 is an integral part of a biochemical pathway that leads to the release of proinflammatory cytokines, such as tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1), both of which are known to cause inflammation and pain. Inhibition of p38 activity should also inhibit TNF-α release. Small molecule inhibitors of p38 MAP kinase have been synthesized in an effort to provide a treatment for RA with increased enzymatic and cellular potency, as well as a more convenient dosing regimen for patients.
 

Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007