Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups: A new class of PPAR gamma/delta and PPAR alpha/gamma/delta agonists

MEDI 378

Louis-David Cantin, david.cantin.b@bayer.com1, Sidney Liang1, Herbert Ogutu1, Christiana I. Iwuagwu1, William H. Bullock1, Michael Burns2, Roger Clark1, Thomas Claus2, Fernando E. dela Cruz2, Michelle Daly2, Frederick J. Ehrgott1, Jeffrey S. Johnson1, James N. Livingston2, Michelle Nophsker1, Robert W. Schoenleber1, Jeffrey Shapiro2, Christopher Town3, Ling Yang2, Manami Tsutsumi2, and Xin Ma1. (1) Department of Chemistry Research, Bayer Pharmaceuticals Corporation, 400 Morgan Lane, West Haven, CT 06516, (2) Department of Metabolic Disorders Research, Bayer Pharmaceuticals Corporation, (3) Department of Research Technologies, Bayer Pharmaceuticals Corporation
Modulation of PPAR activities represents an attractive approach for the treatment of diabetes with associated cardiovascular complications. The indane acetic acid structural motif has proven useful in the generation of potent and tunable PPAR ligands. Modification of the subtituents on the linker and the heterocycle allowed for the modulation of the PPAR alpha activity, while maintaining the PPAR delta and PPAR gamma activity. Compound 2 was further evaluated in vivo, where it displayed the desired reduction of glucose levels and increase in HDL levels in various animal models.

 

General Poster Session
7:00 PM-9:00 PM, Wednesday, 13 September 2006 Moscone Center -- Hall D, Poster

Division of Medicinal Chemistry

The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006