NESACS Process Chemistry Symposium Oct. 12, 2017

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Past Speakers

Speakers Bios from April 29, 2016 Symposium

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Phillip A. Sharp - Institute Professor (highest academic rank) at the Massachusetts Institute of Technology and member of the Department of Biology and the Koch Institute for Integrative Cancer Research.

His landmark work in 1977 provided the first indications of “discontinuous genes” in mammalian cells. The discovery fundamentally changed scientists’ understanding of gene structure and earned him the 1993 Nobel Prize in Physiology or Medicine. He is a co-founder of Biogen and Alnylam Pharmaceuticals Inc.
The Sharp Lab focuses on the biology and technology of small RNAs and other types of non-coding RNAs.

http://ki.mit.edu/people/faculty/sharp

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James P. Morken -The Louise and James Vanderslice and Family Professor of Chemistry at Boston College.

James and his group have recently been in the spotlight for their work building on a Nobel Prize-winning technique that is one of the most sophisticated tools available to research chemists, the team reported in the January 1 edition of the journal Science. This new type of cross coupling reaction is expected to have an impact on the way organic compounds are manufactured especially in the Pharmaceutical Industry.

http://www.bc.edu/offices/pubaf/news/2016-jan-feb/morken_new-conjunctive-cross-coupling-catalyst.html
http://www.bc.edu/schools/cas/chemistry/people/faculty/morken.html

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Barbara Imperiali - Professor of Biology and Chemistry; MacVicar Faculty Fellow at Massachusetts Institute of Technology.

She and her group are investigating divese aspects of protein structure, function and design. Special attention is given to protein modification reactions and recently the discovery of protein glycosylation in bacterial pathogens has inspired research that focuses on understanding the role of cell surface carbohydrates in infection as well as new approaches for understanding the molecular logic of protein glycosylation pathways and processes.

http://web.mit.edu/imperiali/Home.html

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Stevan Djuric, Ph.D. - head of the global AbbVie Medicinal Chemistry Leadership Team at Abbott.

He is also responsible for the Discovery Chemistry and Technology organization within their Discovery organization and chemistry outsourcing activities. He was named an AbbVie Distinguished Research Fellow in 2015 and has been a Project Leader for groups in the Immunoscience, Metabolic Disease, and Antiinfective areas. Several of these programs have advanced compounds into clinical development and to the market including Abbott’s proprietary rapamycin analog, Zotarolimus, currently licensed to Medtronics for use on their vascular stents, marketed in the United States and and Europe.

https://www.linkedin.com/in/stevan-djuric-76968b1

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John Macor, Ph.D. -Executive Director of Immunosciences Discovery Chemistry at Bristol-Myers Squibb.

He has previously held positions at Pfizer (CNS) and Astr Arcus (cholinergic systems) before joing the Cardiovascular group at BMS in 1997. At Bristol-Myers Squibb he led the teams that discovered BMS-346567 (a dual AT1/ETA receptor antagonist presently in Phase 2 clinical trials as PS433540 for diabetic neuropathy), BMS-708163 (a gamma-secretase inhibitor for Alzheimer’s Disease that demonstrated beta-amyloid lowering in the cerebral spinal fluid of normal healthy volunteers in a Phase 1 clinical study), and BMS-927711 (rimegepant), a potent CGRP receptor antagonist for the treatment of migraine.

At present he is the inventor or co-inventor of one marketed drug (Relpax®) and a number of other compounds presently in clinical trials. Recently, Dr. Macor was awarded the 2014 Alfred Burger Award in Medicinal Chemistry (a National Award from the American Chemical Society) to “to recognize outstanding contributions to research in medicinal chemistry.” Dr. Macor was inducted into the Medicinal Chemistry Hall of Fame in August 2014.

https://www.acsmedchem.org/?nd=Macor
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Robert A. Copeland , Ph.D. - President of Research and Chief Scientific Officer at Epizyme.

Robert joined Epizyme in September 2008, from GlaxoSmithKline, where he was Vice President of Cancer Biology, Oncology Center of Excellence in Drug Discovery.

Dr. Copeland has also served on a number of advisory boards, committees and editorial boards in industry, academia, professional societies and professional journals. Before joining GSK he held scientific staff positions at Merck Research Laboratories, DuPont-Merck and Bristol-Myers Squibb and faculty positions at the University of Chicago, Pritzker School of Medicine and the University of Pennsylvania, Perelman School of Medicine. Dr. Copeland received his B.S. in chemistry from Seton Hall University, his doctorate in chemistry from Princeton University and did postdoctoral studies as the Chaim Weizmann Fellow at the California Institute of Technology. His research interest is in elucidating the determinants of drug recognition by their biological targets, and the use of this information in the discovery and design of new medicines.

He has contributed to drug discovery and development efforts leading to 17 drug candidates entering human clinical trials. These include the cancer drugs Tafinlar (Dabrafenib), Mekinist (Trametinib), fortetinib, pinometostat, tazemetostat and the antibiotic Altabax (Retapamulin). Dr. Copeland has contributed more than 200 publications to the scientific literature, holds 10 issued U. S. patents and has authored 5 books in the areas of protein science and enzymology.

His most recent book, Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, 2nd Edition (Wiley, Hoboken, NJ), published in March 2013.

https://www.linkedin.com/in/robert-copeland-6510925

October 22, 2010 at the Royal Sonesta in Cambridge

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Eric Bercot, Amgen

Eric A. Bercot was born in Klamath Falls, OR in 1977.  He completed his B.S. in Chemistry at the University of Oregon in 1999 while working in the laboratories of Michael M. Haley.  He then moved to Colorado State University, receiving a Ph.D. in 2004 working with Professor Tomislav Rovis where he investigated the use of cyclic anhydrides as eletrophilic coupling partners in transition metal mediated cross-coupling reactions.  In late 2004, Eric assumed a position in Chemical Process Research and Development at Amgen where he is currently a Senior Scientist.

Talk Title: “Discovery and Development of Efficient Approaches to Chiral Drug Targets”





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Joseph Fortunak, Howard University

For more information, click here

Talk Title: “Process Chemistry to Increase Access to Medicines in Less-Developed Countries: Medicines for the Other 5.5 Billion”



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Adam Looker, Vertex

Born and raised in upstate NY (Syracuse area), Adam received his B.S. in Chemistry from The College of Environmental Science and Forestry (ESF) in Syracuse, NY. From there, he received his Ph.D. from Yale University under the direction of Frederick Ziegler, followed by a postdoctoral appointment with Michael Crimmins at The University of North Carolina Chapel Hill. Adam joined Vertex Pharmaceuticals, Inc. in 2002 in the Chemical Development group, working on a multitude of projects spanning preclinical through commercial. His current responsibilities include oversight of a group of process chemists, lead on several projects including both early and late phase development, and coordinating efforts on building an internal Quality by Design (QbD) paradigm for current and future programs.

Talk Title:
Successful Development and Manufacture of Merimepodib (VX-497) with a Focus on Process Understanding and Real-Time Measurement

Abstract of Presentation
:

A process for the manufacture of Merimepodib (VX-497), an inosine monophosphate dehydrogenase (IMPDH) inhibitor, has been developed and efficiently scaled to produce clinical supply. The process comprises 5 steps, incorporating simple and robust chemistry that ultimately yielded 96.5 kg with a purity of 100% (by HPLC analysis) and 99.7% w/w assay. Highlights of the process are the effective use of production scale phosgene, manipulation of Schotten-Baumann reaction conditions to give a low pH procedure that avoids a critical impurity, and the use of on-line tools to better identify parameters of an intermediate hydrogenation process, as well as the API purification.

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Richard Pariza, Cedarberg Hauser

Richard Pariza received his Ph.D. degree in Organic Chemistry from Purdue University. He has more than 30 years of leadership on major projects in the pharmaceutical industry. His experience includes positions with Abbott Laboratories, OncQuest, Inc., Protarga, Inc., and Natural Pharmaceuticals. Richard has international recognition as a scientist as well as a scientific manager and leader: Chairman of the prestigious IUPAC Symposium; served on/chaired national ACS committees; frequently invited to chair sessions and lead discussions at international scientific conferences. Former founding editor and now member of the Editorial Board of Organic Process Research & Development, a Research Journal co-sponsored by the American Chemical Society and Royal Society of Chemistry (UK).

Talk Title: “Vitamin D Analogs: Ubiquitous, Important, and Potent!”






April 9, 2010 at the Royal Sonesta in Cambridge

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Melissa Ashlock, Cystic Fibrosis Foundation Therapeutics
Peter Grootenhuis, Vertex


Talk Title: Public Private Partnerships for Drug Development

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Mark Flanagan, Pfizer: Dr. Flanagan is a graduate of New York University. He received his Ph.D. in Organic Chemistry in 1995 from Colorado State University working in the research laboratory of Professor Robert M. Williams. Dr. Flanagan then went on to study as a National Institutes of Health Postdoctoral Fellow in the research group of Professor Peter G. Schultz at the University of California, Berkeley. In 1997 he joined the Immunology Group at Pfizer Global Research and Development in Groton, Connecticut. Dr. Flanagan worked for four years in Pfizer’s Immunology Group before transferring to the Antibacterials Group where he is currently a Senior Principal Scientist for Pfizer World Wide Medicinal Chemistry.

Talk Title: Discovery of
tasocitinib (CP-690,550): A Potent and Selective JAK Inhibitor for the Treatment of Autoimmune Diseases and Renal Allograft Rejection





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Daniel Kahne, Harvard University: For many years the Kahne research group has been interested in the molecular mechanisms of various antibiotics and the fundamental cellular processes they inhibit. They have primarily focused on drugs that target bacterial cell wall biosynthesis, including the beta-lactams, vancomycin, and moenomycin. They use these molecules to study the protein machines that synthesize and degrade the bacterial cell wall.

Recently, they have also become interested in understanding how the structure of cellular membranes is established and maintained. This is a stereochemical problem since biological membranes are asymmetric and require proper spatial organization of their constituent lipids and proteins in order to function correctly.
For more information, click here

Talk Title:
How Do Cells Fold Proteins Into Membranes?

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Sarah O’Connor, MIT: The O'Connor lab studies the biochemical steps that comprise the biosynthetic pathway of secondary metabolites to understand the mechanism, function and evolution of biosynthetic enzymes with the long-term goal of generating new natural products.

Understanding the enzymes that catalyze natural product synthesis may enable production of these important compounds in more tractable host organisms and may also facilitate reprogramming of biosynthetic pathways to produce "unnatural" natural products with improved pharmacological activities.
They explore the enzyme based biosynthetic pathways that generate structurally complex and clinically useful natural products. Their goals are to understand the mechanism of the individual enzymes, understand how the enzymes interact with one another and to modulate the substrate specificity of the enzymes. They take a multi-disciplinary approach to address these questions: protein expression, molecular biology, enzymology, high throughput assay design, natural product isolation and structure elucidation and chemical synthesis are key components of our research. For more information,
click here.

Talk Title: Engineering and Understanding Alkaloid Biosynthesis


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Viresh Rawal, University of Chicago: Chemistry is, ultimately, about chemical reactions-developing them, understanding them, and using them to make interesting, useful molecules. Much of the activity in my research group is aimed at discovering new ways to make complex molecules, including the design of unique strategies to certain families of natural products and the development of broadly effective methods for chemical synthesis.   The targets for our synthesis studies are selected for their intricate structures as well as their potent biological activities. We strive to devise routes that are concise, stereocontrolled, and high-yielding, and proceed through strategies that examine interesting aspects of structure and reactivity. Among the targets that we have successfully synthesized are: 5-oxo-silphiperfol-6-ene, (+)-tabersonine, geissoschizal, elisapterosin B, and strychnine. For more information, click here.

Talk Title: Simple, Chiral Hydrogen Bond Donors as Enantioselective Catalysts


October 23, 2009 at the Royal Sonesta in Cambridge

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Karl Hansen: Director of Process Chemistry, Amgen

Karl Hansen received his Bachelor of Science degree from University of Delaware in 1993.  He then completed his Ph.D. at Harvard University in 1998 working under the direction of Professor Eric Jacobsen.  Following graduation from Harvard, Karl joined the Merck Process Research Group in Rahway, NJ where he worked until 2006. He then moved to Amgen's Cambridge, Massachusetts research center as a Scientific Director.  He heads research groups in Chemical Process R&D in both Cambridge, MA and Thousand Oaks, California.

Talk title:
“Process Research and Development: Searching for the Ultimate Synthesis”
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Joel Hawkins: Global Research and Development, Pfizer

Joel Hawkins received his Ph.D. at MIT in 1986 with Professor Barry Sharpless. He went on to become an NIH Postdoctoral Fellow at Caltech with Professor Robert Grubbs.  As an Assistant Professor at the University of California at Berkeley from 1987 to 1993, he studied asymmetric Diels-Alder catalysts and fullerene chemistry.  In 1993, he moved to Pfizer where he is a Senior Research Fellow in Chemical Research and Development and is particularly interested in the development and application of new technologies for pharmaceutical process research and development.

Talk title: “Case Studies of Heterocyclic Chemistry Highlighting Flow Chemistry and Reaction Profiling”
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Sheila Magil: BioProcess Technology Consultants

Sheila Magil, Ph.D., Senior Consultant, has over 20 years of experience in analytical method development for small molecules, peptides and biologics. Her expertise includes quality, protein chemistry, and formulation development. She was formerly Sr. Manager of Analytical Development and QC at Biomeasure, Inc., and previously held positions at Waratah Pharmaceuticals, Alkermes, Bion, and HHMI at Mass. General Hospital. Dr. Magil has implemented quality systems and has managed external analytical and QC activities for multiple biopharmaceuticals.

Dr. Magil holds a Ph.D. in Biochemistry from the University of Minnesota.

Talk title: “From Clone to Clinic® - Developing a Biotechnology Product”
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Robert Norrie: Section Head Chemical Development/GMP, AMRI

Bob Norrie, Ph.D., received his B.Sc. in Chemistry and Management Studies in 1985 from Dundee Institute of Technology, Dundee, Scotland. In 1989, he completed his doctoral studies at the same establishment, under the supervision of Dr Allan. D. Dunn, and submitted his thesis titled ‘Sulfur containing analogues of deoxyvasicinone’.
 
Bob joined the Boots Company PLC, Nottingham, England in 1989 where he was employed as a medicinal chemist on the design and synthesis of novel chemical entities for the treatment of schizophrenia, depression and obesity. In 2001 he joined AMRI, where for the past eight years he has managed the small scale cGMP production group. During his time at AMRI Bob has overseen the successful completion of over 250 production campaigns.

Talk title: “Adventures in Scale Up – Case Studies and Lessons Learned”
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Dean Toste: Professor of Chemistry, UC Berkeley

F. Dean Toste received his B.Sc. and M.Sc. degrees in chemistry from the University of Toronto where he worked with Prof. Ian W. J. Still. In 1995, he began his doctoral studies at Stanford University under the direction of Professor Barry M. Trost. Following postdoctoral studies with Professor Robert H. Grubbs at Caltech, he joined the faculty at the University of California, Berkeley, in 2002, and was promoted to Associate Professor in 2006.

Research in the Toste group is primarily aimed toward the development of catalysts and catalytic reactions and methods for organic synthesis. Ultimately, they are interested in using these methods to address problems in the synthesis of complex molecules possessing interesting structural, biological and physical properties. For more information, please
click here.

Talk title: “Gold (I) Catalysts for Organic Synthesis”
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R.P. "Skip" Volante: Vice President & Global Head of Process Research, Merck

R.P. "Skip" Volante is Vice President and Global Head of Process Research, Merck Research Laboratories. Dr. Volante began his career at Merck in September 1977, as a Senior Research Chemist in Process Research. He was promoted to Research Fellow in 1983, Senior Research Fellow in 1987, Director in 1989, Senior Director in 1992, Executive Director in 1995 and Vice President and Global Head in 2004, all in Process Research.

Graduated magna cum laude from Pennsylvania State University in 1971, Dr. Volante received his Ph.D. degree from Harvard University in 1976 under the direction of Nobel Laureate, Professor E.J. Corey. He then spent one and one-half years as a post-doctoral fellow in the laboratories of Professor Jerrold Meinwald at Cornell University before joining Merck.

Prior to his current role as Vice President and Global Head of Process Research, Dr. Volante's major achievements or areas of responsibility included a number of Merck products such as IMIPENEM®, SINGLULAIR® and CRIXIVAN®. He also led the Drug Development Sub-Team (responsible for all API and Pharm Product Technology Transfer activities) for the antifungal product candidate CANCIDAS®. In addition, he has led Process Research efforts on numerous other programs and directed the team that completed the first total synthesis of the 23-membered macrolide immunosuppresant, FK-506. Dr. Volante is the author or co-author of over 100 scientific publications and is an inventor or co-inventor on over 70 US issued patents. He is a member of the American Chemical Society and the ACS Organic Division. He was Chairman of the Natural Products Gordon Conference in 1991 and served on the Pennsylvania State University College of Science Alumni Board of Directors from 1978-1986. He was president of the PSU College of Science Alumni Board of Directors from 1985-1986. Among the honors he has received are the Thomas Alva Edison Patent Award for development of the CRIXIVAN® process (1997), the MRL Divisional Scientific Award for CRIXIVAN® (1998) and the Japanese Chemical Society Synthetic Chemistry Award for the Synthesis of CRIXIVAN® (1998). He currently represents Merck as a member of the R&D Council of New Jersey.

Talk title: “Innovation as the Driver of Green Chemistry Advances in the Pharmaceutical Industry"