Synthesis and SAR of hydroxyethylamine-based phenylcarboxyamides as BACE-1 inhibitors

MEDI 297

Yong-Jin Wu, yong-jin.wu@bms.com1, Yunhui Zhang1, Andrew Good, andrew.good@bms.com2, Lorin A. Thompson1, Catherine R. Burton3, Jeremy H Toyn3, Charles F. Albright3, and John E. Macor1. (1) Department of Neuroscience Chemistry, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06443, (2) Department of Computer-Aided Drug Design, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06443, (3) Department of Neuroscience Biology, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06443
A series of N-((2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE-1 inhibitors. A variety of P2 and P3 substituents have been explored, and these efforts have culminated in the identification of several 3,5-disubstituted benzamides with potent BACE-1 inhibitory activity.
 

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