PROFESSIONAL EVENT KEYNOTE-SPEAKER


LAM-Cancer-Conferences.jpg

Prof.Patrick Lam

Distinguished professor; Blumberg Institute, USA

TRAINING

(1984) Post- Doctoral. University of California, Los Angeles. Prof. Donald Cram (1987 Chemistry Nobel Laureate) and Prof. Michael Jung
(1980) Ph.D. University of Rochester, NY. Prof. Louis Friedrich

Appointment at the Baruch S. Blumberg Institute:

Distinguished Professor of Medicinal Chemistry

Other appointments:

Adjunct Professor of Chemistry- Drexel University College of Medicine, Philadelphia, PA. 2012-current

President, Lam Drug Discovery Consulting, LLC, Chadds Ford, PA.  2012-current

Professor of Chemistry, Pennsylvania Drug Discovery Institute, Doylestown, PA   2011-current

RESEARCH OVERVIEW

Research interest: Medicinal chemistry and drug discovery to deliver biopharmaceuticals with novel profiles, Chan-Lam Coupling Reaction.

Research staff: Joint supervision of Blumberg chemistry postdocs and visiting scientists.

RESEARCH

Dr. Lam is a medicinal chemistry and drug discovery consultant. He currently collaborates with Blumberg scientists in terms of drug discovery and jointly supervises Blumberg chemistry postdocs and visiting scientists.

Dr. Lam has 30 years of extensive experience in innovation in structure-based drug design, ADME, focused libraries, molecular recognition and nucleic acid therapeutics to deliver biopharma clinical candidates with novel profiles. He is responsible for the discovery of a total of eight clinical candidates. At Bristol Myers Squibb, Dr. Lam was the group leader/co-inventor responsible for the discovery of  Eliquis®/Apixaban, a novel Factor Xa anticoagulant recently launched on the market. Eliquis® is projected by analysts to be a transformational medicine with “block-buster” sales potential. Eliquis® was chosen as the “Best New Medicine of 2012” by Med Ad News. He and his team were awarded 2015 American Chemical Society Heroes of Chemistry Award for the discovery of Eliquis®. Dr. Lam is also the inventor of the novel cyclic urea class of HIV protease inhibitors that resulted in Mozenavir/DMP450. In Phase II clinical trial, Mozenavir was shown to be as efficacious as Merck’s Crixivan, but without the lipodystrophy side effect of Crixivan.

In recent years, he has been involved with antivirals (HBV capsid, surface antigen and cccDNA inhibitors, Dengue Fever inhibitors, HIV-DCSIGN blockers), antithrombotics (FXIa and FXa inhibitors as anticoagulants; P2Y1 and PAR4  antagonists as antiplatelet agents), PCSK9 antisense oligonucleotide (ASO) therapeutics, prodrugs and carbohydrates.

In the organic chemistry area, he is internationally known as the co-discoverer of the powerful copper-promoted Chan-Lam Coupling Reaction, a complementary reaction to the Nobel-prize winning Suzuki-Miyaura Coupling Reaction. Dr. Lam has authored 98 papers/reviews/book chapters, invented 36 patents/patent applications and presented 110 invited seminars worldwide.

RESEARCH SUMMARY

Dr. Lam is a medicinal chemistry and drug discovery consultant. He collaborates with Blumberg scientists in terms of drug discovery and jointly supervises Blumberg chemistry postdocs and visiting scientists. He is the co-discoverer of Chan-Lam Coupling Reaction.

SELECTED PUBLICATIONS:

“Chan-Lam Coupling Reaction: Copper-promoted C–Element Bond Oxidative Coupling Reaction with Boronic Acids.” Lam, P. Y. S. in “Synthetic Methods in Drug Discovery.” Balkemore, D; Doyle, P.; Fobian, Y. ed., RSC, Cambridge UK, Vol 1, Ch 7. 2016, 1, 242.

“Discovery of 4-Aryl-7-Hydroxyindoline-Based P2Y1 Antagonists as Novel Antiplatelet Agents”. Yang, W., Wang, Y., Lai, A., Qiao, J. X., Wang, T. C., Hua, J., Price, L. A.; Shen, H.; Chen, X.-Q.; Wong, P.; Watson, C.; Huang, C. S.; Seiffert, D. A.; Rehfuss, R.; Wexler, R. R.; Lam, P. Y. S.  J. Med. Chem. 2014, 57, 6150-6164.

“Identification of 1-​{2-​[4-​chloro-​1′-​(2,​2-​dimethylpropyl)​-​7-​hydroxy-​1,​2-​dihydrospiro[indole-​3,​4′-​piperidine]​-​1-​yl]​phenyl}​-​3-​{5-​chloro-​[1,​3]​thiazolo[5,​4-​b]​pyridin-​2-​yl}​urea, a potent, efficacious and orally bioavailable P2Y1 antagonist as an antiplatelet agent”. Jeon, Y. T.; Yang, W.; Qiao, J. X.; Li, L.; Ruel, R.; Thibeault, C.; Hiebert, S.; Wang, T. C.; Wang, Y.; Liu, Y.; Clark, C. G.; Wong, H. S.; Zhu, J.; Wu, D.-R.; Sun, D.; Chen, B.-C.; Mathur, A.; Chacko, S. A.; Malley, M.; Chen, X.-Q.; Shen, H.; Huang, C. S.; Schumacher, W. A.; Bostwick, J. S.; Stewart, A. B.; Price, L. A.; Hua, J.; Li, D.; Levesque, P. C.; Seiffert, D. A.; Rehfuss, R.; Wexler, R. R.; Lam, P. Y. S. Bioorg. Med. Chem. Lett.2014, 24, 1294-1298.

“Conformationally Constrained ortho-Anilino Diaryl Ureas: Discovery of 1 (2-(1′-Neopentylspiro[indoline-3,4′-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a Potent, Selective, and Bioavailable P2Y1 Antagonist”. Qiao, J. X.; Wang, T. C.; Ruel, R.; Thibeault, C.; Lheureux, A.; Schumacher, W. A.; Spronk, S. A.; Hiebert, S.; Bouthillier, G.; Lloyd, J.; Pi, Z;  Schnur, D. M.: Abell, L. M.: , Hua, J.; Price, L. A;  Liu, E. , Wu, Q.; Steinbacher, T. E.; Bostwick, J. S.; Chang, M.;  Zheng, J.; Gao, Q.; Ma, B.; McDonnell, P. A.; Huang C. S.; Rehfuss, R.; Wexler, R. A.; Lam, P. Y. S. J. Med. Chem. 2013, 56, 9275-9295

“Recent advances in Chan-Lam coupling reactions: copper-Promoted C-Heteroatom Bond Cross-Coupling Reactions with Boronic Acids and Derivatives.” Qiao, Jennifer X.; Lam, P. Y. S. in “Boronic Acids”. Ed. Hall, D., 2nded., Vol. 1, Wiley, 2011, p315-361.

“Copper-promoted Carbon-Heteroatom bond cross-coupling with boronic acids and derivatives”. Qiao, Jennifer X.; Lam, Patrick Y. S. Syn. 2011, 829-856.

“Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.” Pinto, D. J. P.; Orwat, M. J.; Koch, S.; Rossi, K. A.; Alexander, R. S.; Smallwood, A.; Wong, P. C.; Rendina, A. R.; Luettgen, J. M.; Knabb, R. M.; He, K.; Xin, B.; Wexler, R. R.; Lam, P. Y. S..  J. of Med. Chem.  2007,  50,  5339-5356.

(2012 BMS Citation Award: most cited BMS chemistry paper 2007-2012)

“Copper-Catalyzed General C-N and C-O Bond Cross-Coupling with Arylboronic Acid.” Lam, P. Y. S.; Vincent, G.; Clark, C. G.; Deudon, S.; Jadhav, P. K.    Tet. Lett.  2001, 42,  3415-3418.

(2005 BMS Citation Award: most cited BMS chemistry paper 2000-2005).

“Copper Promoted N-Arylation with Hypervalent Aryl Siloxanes and One-Pot N-Arylation with Iodobenzene at Room Temperature.” Lam, P. Y. S.; Deudon, Sophie; Averill, K. M.;  Li, R.; He, M.; DeShong, P.; Clark, C. H.. J. Am. Chem. Soc. 2000, 122, 7600-7601.

(2003 BMS Citation Award: most cited BMS chemistry paper 1998-2003)

“Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors”  P. Y. S. Lam, P. K.  Jadhav, C. J. Eyermann, C. N. Hodge, Y. Ru, L. T. Bacheler, J. L. Meek, M. J. Otto, M. M. Rayner, N. Y. Wong, C. H. Chang, P. C. Weber, D. A. Jackson, T. R. Sharpe, S. K. Erickson-Viitanen.  Science 1994, 263, 380-384.

-“The 11th most cited chemistry paper 1994-1997″ by Institute for Scientific Information, Philadelphia, PA, Vol 9, July/August, 1998;

-Highlighted in C&E News, p. 24, Jan 24, 1994. “…By a series of rational design and molecular modeling steps, the DuPont Merck group designed a set of nonpeptide cyclic ureas in which the urea carbonyl oxygen mimics the hydrogen-bonding features of this structural water molecule…”

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