Bristol-Myers Squibb Lecture

Wednesday, May 2nd
Dr. Patrick Y Lam
“Structure-based discovery of Factor Xa inhibitors as novel anticoagulants and copper-promoted C-X bond cross-coupling via organometalloids”

4:15pm - 5:15pm
Braun Lecture Hall
S.G.Mudd Chemistry Building
Stanford University


This is the first of two special lectures hosted by the Bristrol-Myers Squibb Company in support of synthetic organic chemistry. The second lecture will be given by Professor Emeritus Albert Eschenmoser, Swiss Federal Institute of Technology and will start at 5:30.

These lectures are free and open to the public. All Stanford University Chemistry students are encouraged to attend this special event.

About the lecture:
The leading cause of death in developed countries continues to be cardiovascular events, primarily due to thrombosis (undesirable blood clot). Factor Xa is a critical enzyme in the coagulation pathway and has emerged as a prime target for the discovery of new anticoagulants. Using structure-based drug design tools, molecular recognition principles and combinatorial chemistry, we have discovered a class of potent, orally-bioavailable pyrazole Factor Xa inhibitors. This lecture will detail the design and discovery of this class of inhibitors which has advanced to Phase III human clinical trials. During the discovery process, we have a need for new reactions for N-arylation. We have developed the copper-promoted C-X bond cross-coupling reaction using organometalloids. This reaction can potentially be as useful as the complementary Suzuki-Miyaura’s palladium catalyzed C-C bond cross-coupling reaction. A comparison of our copper chemistry with Buchwald-Hartwig’s palladium-catalyzed N-arylation chemistry will also be discussed.

About Lam:
Patrick Y. Lam is currently a director in the Discovery Chemistry Department at Bristol-Myers Squibb Co. He received his Ph.D. from the University of Rochester (Dr. Louis Friedrich) in 1980 and was a postdoctoral fellow in UCLA (Prof. Mike Jung and the late Prof. Don Cram). He joined DuPont in 1984 and moved to BMS in 2001. In recent years, he has been involved with HIV protease inhibitors, Factor Xa inhibitors and anti-platelet agents. His research interest is in the application of new technologies in synthetic methodology, combichem, molecular recognition, computer-aided drug design tools and structural biology to drug discovery in order to deliver clinical candidates with novel structures and biological properties. Patrick has received numerous awards including two BMS Citation Awards for the most cited BMS chemistry publications, 2004 and 2006; Ondetti Cushman Innovation Award, BMS, 2003. Summit Award, DuPont-Merck, 1993. He serves on the Editorial Board of Current Medicinal Chemistry, Medicinal Chemistry, Letters in Drug Design & Discovery, Medicinal Research Reviews; member of Long Range Planning Committee of ACS Medicinal Chemistry Division (1997-2000).

Questions
Please contact Patricia Dwyer at 650-723-4770.