Monday, 23 May 2005 - 9:05 AM
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This presentation is part of: Kinase / Virtual Screening

Development of Aniline amides Containing Alternative Cores as Orally Active P38 MAP kinase Inhibitors

Katerina Leftheris, John Hynes, Jr., Alaric Dyckman, Tianle Li, Shuqun Lin, Stephen T. Wrobleski, Hong Wu, Rosemary Zhang, Kathleen M. Gillooly, Derek Loo, Kim W. McIntyre, Sidney Pitt, Ding Ren Shen, David J Shuster, Arthur Doweyko, John Sack, Joel Barrish, John Dodd, and Gary L. Schieven. Bristol-Myers Squipp, Princeton, NJ

Overproduction of cytokines such as TNF-alpha and IL-1beta regulated by the p38alpha pathway are implicated in a wide variety of inflammatory diseases, including rheumatoid arthritis (RA). Recently, we described out initial efforts in developing potent, selective triaminotriazine and cyanopyrimidine aniline amides as inhibitors of p38alpha MAP kinase. Herin, we describe further development of the aniline amide class of p38 inhibitors to include alternative core structures. A description of the SAR development, in vivo activity, AMDE profiling and X-ray cyrstallography will be presented.

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