OSI Pharmaceuticals to give talk at Protein Kinases meeting May 27-28, Boston
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Andrew Crew will give a presentation on “Imidazo[1,5-a]pyrazines: Selective and Orally Efficacious mTORC1/2 Inhibitors” at the 5th Annual Protein Kinases in Drug Discovery conference to be held this year in Boston, MA on May 27-28, 2010 by GTCbio. The presentation will describe the identification of a series of imidazo[1,5-a]pyrazines that, through a combination of empirical medicinal chemistry exploration and use of a PI3K?-derived homology model, provided potent and selective inhibitors of both mTORC1 and mTORC2 with broad spectrum anti-tumor activity in vivo. Benefits of Dr. Crew’s presentation include: - Description of SAR within the imidazopyrazine series - Control of in vitro ADMET properties - Optimization of oral PK - Demonstration of efficacy in multiple xenograft models Andy Crew joined OSI in 2002 and has been the multidisciplinary project team leader for OSI’s c-Kit/KDR and mTORC1/2 kinase projects culminating in the development/clinical agents OSI-930, OSI-817 and OSI-027. Currently he is co-head of the OSI Cancer Chemistry department in NY with leadership oversight for multiple advanced and exploratory projects, external collaborations and computational chemistry. Prior to OSI, Andy worked at Tularik Ltd. (formerly Protherics Molecular Design Ltd) for 6 years, where he worked on the structure-based design and synthesis of inhibitors of the serine proteases factors Xa and VIIa, urokinase and tryptase. Prior to Tularik, Andy worked at Knoll-BASF Pharma (formerly Boots Pharmaceuticals) for 6 years working on neurological diseases, specifically on the discovery of dopamine D1/D5 receptor antagonists, and D2 antagonist/5-HT1A agonist approaches as atypical antipsychotics for the treatment of schizophrenia. Andy received his Ph.D. in Organic Chemistry in 1991 from the University of Liverpool, UK under Dr. Dick Storr working on “Approaches to Heterocyclic Analogues of o-Xylylene.” He received his BSc degree (First Class Hons) in Applied Chemistry in 1987 from the University of Wales Institute of Science and Technology in Cardiff, UK. Also presenting at the Protein Kinase conference are prestigious organizations including AstraZeneca, Bristol-Myers Squibb, Dana-Farber, Dartmouth, Genentech, GlaxoSmithKline, Harvard, Roche, Merck, Pfizer, Tufts, UCSD, Wyeth and other leaders in the kinase industry. The 5th Protein Kinases in Drug Discovery conference features presentations on new technology for kinase target and inhibitor identification and screening, kinase selectivity, kinase drug design, kinase targets & inhibitors in oncology, kinase targets & inhibitors in CNS disorders, and kinase targets & inhibitors in inflammatory disorders. For more information, visit http://www.gtcbio.com. User comments, Ratings and Reviews
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