2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry

Expanding the Druggable Genome through Cereblon-Mediated Protein Degradation (KL02)

Dr Lawrence G. HAMANN

CELGENE, Cambridge, United States

Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire (KL01)

Prof. Sarah E. REISMAN

CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States
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Prof. Sarah E. REISMAN

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Sarah E. Reisman earned a BA in Chemistry from Connecticut College in 2001, and her Ph.D. in chemistry from Yale University in 2006, under the direction of Prof. John L. Wood. From 2006–2008, Sarah worked as an NIH fellow with Prof. Eric Jacobsen at Harvard University, and then joined the faculty at the California Institute of Technology where she is now a Professor of Chemistry and a Heritage Medical Research Institute Investigator. Her laboratory seeks to discover, develop, and study new chemical reactions within the context of natural product total synthesis.

Controlling the Fate and Function of Proteins with Photopharmacology (KL03)

Prof. Dirk TRAUNER

NEW YORK UNIVERSITY, New York, United States
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Prof. Dirk TRAUNER

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http://chem.berkeley.edu/people/faculty/trauner/trauner.html

Dirk Trauner was born and raised in Linz, Austria, studied biology and chemistry at the University of Vienna, and received his undergraduate degree in chemistry from the Free University, Berlin. He then pursued graduate studies in chemistry under the direction of Prof. Johann Mulzer, with whom he moved to the University of Frankfurt and then back to Vienna where he obtained his Ph.D. Following a stint in the Austrian Army, he became a postdoctoral fellow with Prof. Samuel J. Danishefsky at the Memorial Sloan-Kettering Cancer Center. After two great years in New York City, Dr. Trauner joined the Department of Chemistry at the University of California, Berkeley, where he rose through the ranks to become an Associate Professor of chemistry (with tenure) and a member of the Lawrence Berkeley National Laboratory. In 2008, he moved to the University of Munich as a Professor of Chemistry and Chemical Genetics. In the Spring of 2017 he returned to the United States as the Janice Cutler Chair in Chemistry at New York University (Department of Chemistry). He also holds and appointment at the NYU Langone School of Medicine and is a member of the NYU Neuroscience Institute and of the Perlmutter Cancer Center.

Synthesis in the Chemical Space Age (PL18)

Prof. Timothy CERNAK

UNIVERSITY OF MICHIGAN, Ann Arbor, United States
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Prof. Timothy CERNAK

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Tim Cernak was born in Montreal, Canada in 1980. He obtained a B.Sc. in Chemistry from University of British Columbia Okanagan and there studied the aroma profile of Chardonnay wines. Following PhD training in total synthesis with Prof. Jim Gleason at McGill University, Tim was a FQRNT Postdoctoral Fellow with Tristan Lambert at Columbia University. In 2009, Tim joined the Medicinal Chemistry team at Merck Sharp & Dohme in Rahway, New Jersey. There he developed technologies for miniaturized synthesis and late-stage functionalization. In 2013, Tim moved to Merck’s Boston site. In 2018, Dr. Cernak transitioned from industry to academia and launched a lab at the University of Michigan in Ann Arbor as an Assistant Professor of Medicinal Chemistry. The Cernak Lab is exploring an interface of chemical synthesis and data science.

Organic Synthesis on a Computer: Should Medicinal Chemists Care? (PL17)

Prof. Bartosz A. GRZYBOWSKI

ULSAN NATIONAL INSTITUTE OF SCIENCE & TECHNOLOGY, Ulsan, Korea, South
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Prof. Bartosz A. GRZYBOWSKI

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Bartosz A. Grzybowski graduated summa cum laude from Yale University in 1995 and received his Ph.D. in chemistry from Harvard in 2000. After a postdoctoral fellowship at Harvard, he joined the faculty of Northwestern University in 2003 and in 2009 became Kenneth Burgess Professor of Physical Chemistry and Chemical Systems’ Engineering. From 2009 he directed the DoE Non-Equilibrium Research Center at Northwestern. In late 2014 he moved to UNIST where he is now a Distinguished Professor of Chemistry and also a Group Leader at the IBS Center for Soft and Living Matter. He is also Professor at the Institute of Organic Chemistry, Polish Academy of Sciences. His current research interests include chemical networks and systems, automated synthetic planning, theory of organic synthesis, applications of AI to chemistry, autocatalysis, and “thinking” materials.

Accelerating R&D with Augmented Intelligence (PL19)

Dr Matthias ZENTGRAF

BOEHRINGER INGELHEIM, Biberach an der Riss, Germany
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Dr Matthias ZENTGRAF

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Matthias did his PhD with Prof. Klebe and joined the Computational Chemistry group of Boehringer Ingelheim in Biberach in 2006. In 2010 he became team lead of one of the Computational Chemistry teams with a focus on respiratory diseases. Since 2017 he is “Head of Computational Chemistry“.

A Radical Way to Abeo-Steroids (PL08)

Prof. Philipp HERETSCH

FREE UNIVERSITY OF BERLIN, Berlin, Germany
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Prof. Philipp HERETSCH

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Philipp Heretsch was born in Lippstadt, Germany, in 1982. He obtained his PhD degree from Universität Leipzig (supervisor: Prof. A. Giannis) in 2009. After a postdoctoral stay with Prof. K.C. Nicolaou at The Scripps Research Institute, La Jolla, California, and at Rice University, Houston, Texas, he was appointed assistant professor at Freie Universität Berlin in 2015. Philipp Heretsch has been working on total synthesis of biologically active natural products since the beginning of his career. His group is now interested in radical C−C-bond manipulation strategies in the context of the synthesis of complex abeo-steroids, guided by biosynthetic hypotheses as well as designing flow reactors for specific use in natural product synthesis.

New Avenues in Synthesis Enabled by Organic Photoredox Catalysis (PL06)

Prof. David NICEWICZ

UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States
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Prof. David NICEWICZ

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Dave Nicewicz completed his Chemistry B.S. (2000) and M.S. (2001) degrees at the University of North Carolina, Charlotte. He then moved to the University of North Carolina, Chapel Hill where he completed his Ph.D. with Prof. Jeffrey S. Johnson in 2006. Nicewicz then was a Ruth L. Kirschstein Postdoctoral Fellow with Prof. David W. C. MacMillan. In 2009, Dave began his independent career at the UNC Chapel Hill, where his laboratory has focused on organic photoredox catalysis for the development of novel chemical reactivity. He has received awards from UNC (Ruth Hettleman Prize for Artistic and Scholarly Achievement), industry (Boehringer Ingelheim; Amgen; Eli Lilly), private foundations (Packard Fellowship in Science and Engineering; Camille Dreyfus Teacher-Scholar Award) and international recognition (The 13th Hirata Award, Nagoya University). In 2015, he was promoted to Associate Professor, and then Full Professor in 2018.

Late-Stage Functionalizations (PL07)

Prof. Tobias RITTER

MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany
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Prof. Tobias RITTER

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Tobias Ritter received his undergraduate education in Braunschweig, Germany, Bordeaux, France, Lausanne, Switzerland, and Stanford, US. He has performed undergraduate research with Prof. Barry M. Trost at Stanford, obtained his PhD working with Prof. Erick M. Carreira at ETH Zurich in 2004, and was a postdoc with Prof. Robert H. Grubbs at Caltech. In 2006, Tobias was appointed as Assistant Professor in the Department of Chemistry and Chemical Biology at Harvard, promoted to Associate Professor in 2010, and to Professor of Chemistry and Chemical Biology in 2012. Since 2015 he is director at the Max-Planck-Institut fuer Kohlenforschung in Germany, since 2018 as the Managing Director, and holds additional faculty appointments at RWTH Aachen and Massachusetts General Hospital, Boston. The Ritter lab focuses on late-stage functionalization chemistry, with a focus on fluorination methods and their application to molecular imaging. In 2011, Tobias founded SciFluor LifeScience, a clinical pharmaceutical company in Cambridge, Massachusetts.

Break-it-to-Make-it Strategies for Complex Molecule Synthesis (PL05)

Prof. Richmond SARPONG

UNIVERSITY OF CALIFORNIA, BERKELEY, Berkeley, United States
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Prof. Richmond SARPONG

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Richmond Sarpong is a Professor of Chemistry at the University of California Berkeley where he and his group specialize in synthetic organic chemistry. Richmond completed his undergraduate studies at Macalester College in St. Paul, MN and his graduate work was carried out with Prof. Martin Semmelhack at Princeton. He conducted postdoctoral studies at Caltech with Prof. Brian Stoltz. At Berkeley, Richmond’s laboratory focuses on the synthesis of bioactive complex organic molecules, with a particular focus on secondary metabolites that come from marine or terrestrial flora and fauna. Of all his professional accomplishments, Richmond is most proud of the students with whom he has worked.

Discoveries and Surprises with Natural Products (PL14)

Prof. Karl GADEMANN

UNIVERSITY OF ZÜRICH, Zürich, Switzerland
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Prof. Karl GADEMANN

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Karl Gademann (1972) was educated at ETH Zürich and Harvard University, where he worked with Prof. Dieter Seebach, Prof. Eric N. Jacobsen, and Prof. Erick M. Carreira. His previous professorial appointments include the EPFL in Lausanne and the University of Basel, where he served as full professor and dean of research. He has been elected to the board of the Swiss Academy of Sciences, and is affiliated to the NCCR Molecular Systems Engineering. In Summer 2015, Karl Gademann moved to the University of Zürich, where he serves as the chair of the department of chemistry. In addition, he also performs duties as a research councillor to the Swiss National Science Foundation. His work has been recognized by a number of international awards, including the Latsis prize, the Novartis Early Career Award, the Ruzicka Medal, The Liebig Lecture by the German Chemical Society, and the European Young Investigator Award.

Concise Synthesis of Complex Taxane Diterpene Canataxpropellane by Photochemical Dearomatization (PL15)

Prof. Tanja GAICH

UNIVERSITY OF KONSTANZ, Konstanz, Germany

Strategies for the Synthesis of Bioactive Diterpenoids (PL16)

Prof. Christopher VANDERWAL

UNIVERSITY OF CALIFORNIA, IRVINE, Irvine, United States
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Prof. Christopher VANDERWAL

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Chris Vanderwal was born in Germany (to Canadian parents). At the age of nearly five, young Chris moved with his parents to Ottawa, Canada, where he attended school, up to and including university (BSc in Biochemistry, MSc in Chemistry from the University of Ottawa). Chris moved to sunny San Diego, where he earned his PhD under the supervision of Erik Sorensen at Scripps in 2003. Chris then moved back to the cold as a Jane Coffin Childs Postdoctoral Fellow at Harvard University in the lab of Eric Jacobsen. Chris enthusiastically joined the Chemistry Department faculty at UC Irvine in 2005. In 2011, Chris was promoted to Associate Professor of Chemistry with tenure, and was named a UCI Chancellor’s Faculty Fellow. In 2013, Chris was promoted to Professor.

Total Synthesis of Chivosazole F (OC04)

Dr Simon WILLIAMS

SYNGENTA, Stein AG, Switzerland
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Dr Simon WILLIAMS

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Simon Williams did his undergraduate education in natural sciences at the University of Cambridge and continued to do a PhD on the synthesis of marine natural products with Prof. Ian Paterson. He spent a further year as a postdoc in the Paterson group before moving to the University of Zurich to work with Prof. Karl Gademann on antibiotic natural products. At the end of 2018 he started his current position as a team leader in research chemistry at Syngenta in Stein (Switzerland).

Structural Attributes Influencing Unbound Tissue Distribution (PL01)

Dr Li DI

PFIZER, Groton, United States
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Dr Li DI

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Dr. Li Di has over 25 years of experience in the pharmaceutical indus¬try including Pfizer, Wyeth and Syntex. She is currently a research fellow at Pfizer, Groton, CT. Her research interests include the areas of drug metabo¬lism, pharmacokinetics, drug-drug interactions, absorption, transporters, and blood–brain barrier. She has over 145 publications including two books and presented over 85 invited lectures. She is a recipient of the Thomas Alva Edison Patent Award, the New Jersey Association for Biomedical Research Outstanding Woman in Science Award, the Wyeth President’s Award and Peer Award for Excellence.

Metabolism of Strained Rings: Tales of the Unexpected (PL02)

Dr Martin HAYES

ASTRAZENECA, Gothenburg, Sweden
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Dr Martin HAYES

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Martin Hayes is currently Biocatalysis Leader in Hit Discovery, part of Discovery Sciences at AstraZeneca in Gothenburg, Sweden. He has over 25 years of industrial experience in drug discovery and development in large pharma and biotech with research interests in biocatalysis, biotransformation, natural products chemistry, analytical chemistry, structure elucidation and drug design. MH has held roles as a Team Leader, Design Leader and Project Leader at AstraZeneca, GlaxoSmithKline and Xenova. He led preclinical biotransformation studies on the P2Y12 blockbuster Brilinta/Brilique and DMPK design efforts for the FLAP inhibitor AZD5718 for atherosclerosis, currently in Phase 2. He is Industrial Lead for small molecule development and member of the Prosperity Partnership Management Board for the EPSRC/BBRSC PP Grant to establish a new Centre for Biocatalytic Manufacture of New Modalities (CBNM) at Manchester University (2018-2023). He was PI on the Marie Curie FP7 funded P4FIFTY project (2013-2017). He has published over 35 papers in peer-reviewed journals, holds 14 patents and was made a Fellow of the Royal Society of Chemistry in 2000. Martin worked with Prof Tom Simpson FRS at the University of Bristol on mechanistic aspects of fungal polyketide chain assembly, followed by a postdoctoral fellowship with Prof Bryan Jones at University of Toronto.

Title to be confirmed (PL04)

Leveraging In Silico ADMET and Ancillary Pharmacology to Influence Selection of Chemical Series with Increase Probability of Success (PL03)

Dr Falgun SHAH

MERCK, West Point, United States
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Dr Falgun SHAH

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Dr. Falgun is currently an Associate principal scientist and computational ADME & toxicology domain lead within the discovery chemistry group at Merck, West Point. His interest lies in applying machine learning and data mining approaches to identify potential ADME and safety liabilities within chemotypes. His current role involves influencing medicinal chemistry project teams to utilize in silico ADMET approaches during post-HTS work-up to enable them to bring high-quality chemical series forward. Prior to Merck, Falgun worked in compound safety prediction group at Pfizer for 4.5 years where he deployed in silico and informatics approaches to identify new mechanisms of organ toxicities in particularly drug-induced liver injury and cardiotoxicity. He has over 25 publications in peer-reviewed journals and multiple invited presentations. Falgun is trained as a pharmacist and holds a Ph.D. in medicinal/computational chemistry.

Dr Kenichi UMEHARA

ROCHE PHARMACEUTICAL RESEARCH AND EARLY DEVELOPMENT, Basel, Switzerland
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Dr Kenichi UMEHARA

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Kenichi Umehara is a Principal Scientist contributing to translation of the in vitro DDI results into models to understand the human situation Scientist at Roche Innovation Center (Basel, Switzerland). He obtained his PhD from the University of Toho (Japan), after working in Prof. Dr. Sugiyama’s laboratory. In 2002, Kenichi joined Astellas Pharma, then in 2009, moved to Novartis (Switzerland) to undertake postdoctoral research for hepatic clearance prediction. Subsequently, he was appointed laboratory head for DDI assessment supporting global project teams. Kenichi also has many experience in interactions with HA’s that include PBPK modeling, to propose dose adjustment with concomitant medications resulting in waiver of clinical studies. In 2018 Kenichi joined the in vitro PK and DDI group at Roche.

Expanding the Druggable Genome through Cereblon-Mediated Protein Degradation (KL02)

Dr Lawrence G. HAMANN

CELGENE, Cambridge, United States
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Dr Lawrence G. HAMANN

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Larry Hamann is currently Corporate Vice President and Global Head of Chemistry at Celgene, with responsibility for Medicinal and Computational Chemistry, Biochemistry, Structural and Chemical Biology and Screening. In > 27 years in drug discovery he has led teams responsible for more than 17 clinical stage compounds, including the FDA approved DPP4 inhibitor saxagliptin (Onglyza™) for type 2 diabetes, and first-in-class HCV NS5A inhibitor daclatasvir (Daklinza™) for hepatitis C. Prior to Celgene, Larry was Executive Director, Global Discovery Chemistry at Novartis, overseeing programs in oncology, neuroscience, respiratory, cardiovascular, and rare genetic disease. Previously, Larry was at Bristol-Myers Squibb and Ligand Pharmaceuticals. Larry holds a BS in Chemistry from the University of Detroit and a PhD in Organic Chemistry from the University of Michigan.

Targeted Protein Degradation (PL12)

Prof. Andy PHILLIPS

C4 THERAPEUTICS, Watertown, United States
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Prof. Andy PHILLIPS

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Andy Phillips is President and Chief Executive Officer of C4 Therapeutics, a biotech company that is developing a new class of small molecules that direct the machinery of the ubiquitin-proteasome system to selectively degrade disease-relevant proteins for therapeutic benefit.

Before joining C4 Therapeutics, Andy was Senior Director, Center for Development of Therapeutics at the Broad Institute of MIT and Harvard, where he led overall therapeutic efforts and provided strategic leadership for a number of major partnerships. Previously, he was a Full Professor of Chemistry at Yale University, where he received the ACS Cope Scholar Award for his research accomplishments, which included the development of small molecules aimed at modulating ‘undruggable’ targets. Prior to this, he was a Full Professor of Chemistry and Biochemistry at the University of Colorado at Boulder, where his efforts in complex molecule synthesis and targeting protein-protein interactions garnered a number of awards, including an Alfred P. Sloan Research Fellowship, an Eli Lilly Grantee Award, and a National Science Foundation CAREER Award. Andy received a B.Sc. (Hons) in biochemistry and a Ph.D. in biochemistry and chemistry from the University of Canterbury in New Zealand and completed a postdoctoral fellowship in organic chemistry at the University of Pittsburgh.

Four E3 Ligases, One Target: Towards Novel CDK6 Protacs (OC03)

Mr Christian STEINEBACH

UNIVERSITY OF BONN, Bonn, Germany
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Mr Christian STEINEBACH

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Christian Steinebach completed his undergraduate studies in Pharmacy (state examination) at the University of Bonn, Germany. In 2015, he became a licensed Pharmacist and got the Carl-Friedrich-Mohr award. He received his MSc in Drug Development in 2016. Since then he is performing his PhD studies in Pharmaceutical Chemistry supervised by Prof. Michael Gütschow at the Pharmaceutical Institute in Bonn. In 2018, he successfully applied for a PhD-related scholarship from the Bonn International Graduate School of Drug Sciences. His scientific work is devoted to the Medicinal Chemistry of Proteolysis Targeting Chimeras (PROTACs), to the design and synthesis of bioactive molecules acting by a new modality of targeted degradation of disease-causing proteins, in particular protein kinases.

Title to be confirmed (PL11)

Dr Xavier DARZACQ

UNIVERSITY OF CALIFORNIA, BERKELEY, Berkeley, United States

Membrane Proteins at the SGC – Challenges and Success Stories (PL09)

Dr Katharina DUERR

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Dr Katharina DUERR

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The Duerr group at the Structural Genomics Consortium Oxford uses structural methods (X-ray crystallography and single-particle cryo-Electron microscopy) to determine the molecular architecture of human ion channels, transporters, enzymes and other integral membrane proteins relevant to various disease conditions and human therapies. This structural work provides valuable insights into the molecular interactions of these proteins with their native substrates, small molecule drugs or therapeutic antibodies and provides a framework to develop mechanistic models for their functional activity, which are then further tested in functional experiments. Prior to joining the SGC in 2016, Katharina has been a postdoctoral researcher in the lab of Eric Gouaux at OHSU (Portland, OR), studying the structure and function of ionotropic glutamate receptors.

Discovery of Small Molecule Fascin 1 Inhibitors Using Fragment-Based Drug Discovery (OC02)

Dr Stuart FRANCIS

THE BEATSON INSTITUTE FOR CANCER RESEARCH, Glasgow, United Kingdom
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Dr Stuart FRANCIS

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- I studied Medicinal Chemistry at University of Sussex before working at Celltech Chiroscience for 2 years working on integrins and kinases against inflammatory targets.
- I Subsequently joined Organon, in 2003 which latterly became MSD, at Newhouse for 9 years working on a number of GPCR targets including Cannabinoids and aminergics.
- Since 2011 I have worked on several kinase and Protein Protein Interactions (PPI) projects with a particular interest in fragment screening and Protacs to help validate novel and challenging oncology targets.

Title to be confirmed (PL10)

Dr Matthias FRECH

MERCK, Darmstadt, Germany

Using Small Molecules to Engineer and Explore Human Immunity (PL22)

Prof. David SPIEGEL

YALE UNIVERSITY, New Haven, United States
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Prof. David SPIEGEL

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http://www.spiegelgroup.yale.edu

David Spiegel, MD, PhD is a Professor at Yale University with appointments in the departments of Chemistry and Pharmacology. He is also the Chief Scientific Advisor and co-founder of Kleo Pharmaceuticals, and serves as Founding Scientific Advisor to Kymera Therapeutics. The central focus of Professor Spiegel’s research has been the development of novel, small molecule-based strategies for manipulating and regulating human immunity and other biological processes. Over the course of his career, Dr. Spiegel has co-authored more than 50 peer-reviewed publications and has obtained over a dozen patents.

Intracellular and Tissue Specific Targeting of Therapeutic Modalities (PL21)

Dr Vadim DUDKIN

JANSSEN DISCOVERY SCIENCES, Lansdale, United States
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Dr Vadim DUDKIN

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Vadim Dudkin is Senior Director and Head, RNA & Targeted Therapeutics group within Janssen Discovery Sciences, Johnson and Johnson. Vadim is responsible for leading research teams at La Jolla, CA, Spring House, PA, and South San Francisco, CA sites focusing on nucleic acid therapeutics including oligonucleotides and large nucleic acids as well as intracellular and tissue specific targeted modalities. In his previous role at Janssen, Vadim was leading research at Centyrex internal venture. Vadim joined Janssen from Merck, where he was engaged in small molecule, vaccine and siRNA discovery.

Title to be confirmed (PL23)

Dr Valerie ODEGARD

SILVERBACK THERAPEUTICS, Seattle, United States
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Dr Valerie ODEGARD

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Valerie Odegard, Ph.D., is the Chief Scientific Officer of Silverback Therapeutics. She has over 15 years of experience in immunotherapy drug development across multiple therapeutic areas. Prior to Silverback, Dr. Odegard served as Vice President of R&D at Juno Therapeutics, where she was responsible for advancing novel cellular immunotherapies into clinical development. Prior to Juno, she held research leadership positions at Novo Nordisk and Trubion Pharmaceuticals, where she oversaw the discovery and preclinical development of therapeutics for oncology and inflammatory conditions. Dr. Odegard received her Ph.D. in Immunobiology from Yale University.

Discovery of Tumor Targeted TLR7/8 Immune-Stimulating Antibody Conjugates (ISAC) (PL20)

Dr Brian SAFINA

BOLT BIOTHERAPEUTICS, Redwood City, United States
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Dr Brian SAFINA

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Brian Safina, Ph.D., serves as vice president for Bolt Biotherapeutics, where he leads chemistry and bioconjugation toward developing novel immuno-oncology therapeutics. He joined Bolt in 2018 with over a decade of medicinal chemistry experience at Genentech. Dr. Safina has made significant contributions to the discovery of multiple clinical candidates in the areas of oncology, immunology and neuroscience. Dr. Safina holds a Ph.D. in organic chemistry from the University of California, San Diego, where he worked in the laboratories of K.C. Nicolaou.