3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry

Title to be announced

Prof. Angela KOEHLER

MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States

Functionalization of N-Heterocycles using Li, Mg, and Zn Organometallics

Prof. Paul KNOCHEL

LUDWIG MAXIMILIANS UNIVERSITY, Munich, Germany
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Prof. Paul KNOCHEL

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http://www.knochel.cup.uni-muenchen.de/index.php?id=8,0,0,1,0,0

Paul Knochel has been a full professor for organic chemistry at the Ludwig-Maximilians-University Munich/Germany (LMU) since 1999. He did his undergraduate studies at the University of Strasbourg (France) and his Ph.D at the ETH-Zürich with Prof. D. Seebach. He spent 4 years at the CNRS at the University Pierre and Marie Curie in Paris with Prof. J.-F. Normant and one year of post-doctoral studies at Princeton University in the laboratory of Prof. M. F. Semmelhack. In 1987, he accepted a position as Assistant Professor at the University of Michigan at Ann Arbor, MI. In 1991, he became Full Professor at this university and in 1992, he moved to Philipps-University at Marburg (Germany) as C4-Professor in Organic Chemistry. His research interests include the development of novel organometallic reagents and methods for use in organic synthesis, asymmetric catalysis and natural product synthesis.

Title to be announced

Dr Wendy YOUNG

MPM CAPITAL POWERING BREAKTHROUGHS IN LIFE SCIENCES, Brisbane, United States

Enabling Fragment-based Drug Discovery (FBDD) with Automated Synthesis Technologies

Dr Rachel GRAINGER

ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
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Dr Rachel GRAINGER

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Rachel Grainger obtained her MChem from University of Bath in 2010, before moving to Queen Mary University of London to complete her PhD on transition metal catalysis with Prof. Igor Larrosa. She spent two years working with Prof. Matthew Gaunt at the University of Cambridge as a Postdoctoral Research Associate focussing on the development of nanoscale HTE for organic synthesis. In March 2017 she joined Astex Pharmaceuticals’ Sustaining Innovation Postdoctoral program where she established automated synthesis capabilities (HTE and flow) within the company. As of 2019, Rachel is Senior Research Associate in Astex’s Synthesis Technology Group, her role involves the development and implementation of cutting-edge technologies (robotic enabled HTE, photoredox, flow etc.) to enable synthetic challenges on live drug discovery projects.

Rapid Development of Robust Reactions and Multi-Step Syntheses

Prof. Alexei LAPKIN

UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
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Prof. Alexei LAPKIN

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Alexei Lapkin graduated with an MChem from Novosibirsk State University, specialising in membrane gas separation. He then worked at Boreskov Institute of Catalysis prior to moving to the University of Bath where he was employed as a research officer, which allowed him to complete his PhD in the area of multiphase membrane catalysis. His research interests are digitalisation of R&D and developing clean chemical manufacturing processes.

Studies with Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Dr Agustin CASIMIRO-GARCIA

PFIZER, United States
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Dr Agustin CASIMIRO-GARCIA

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Agustin Casimiro-Garcia is an Associate Research Fellow in the Pfizer Medicine Design group in Cambridge, MA, USA. He has worked at Pfizer since 2000. His research at Pfizer has been in the areas of cardiovascular and metabolic diseases, inflammation and immunology disorders, fibrotic diseases, and more recently oncology. His current research interests include phenotypic drug discovery, covalent inhibition, and approaches to pursue challenging targets. Agustin obtained his Ph.D. in Medicinal Chemistry from Purdue University and carried out postdoctoral studies at Rensselaer Polytechnic Institute.

Title to be announced

Dr Matthew CHEESEMAN

THE INSTITUTE OF CANCER RESEARCH, Sutton, United Kingdom

Reversible-covalent Inhibitors of the Kinase Activity of FGFR4

Dr Robin FAIRHURST

NOVARTIS, Basel, Switzerland
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Dr Robin FAIRHURST

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Robin is currently an Associate Director in the Oncology Chemistry Group in Basel, Switzerland, serving as a Project Leader/Medicinal Chemist. He has occupied this position since 2007, contributing to several kinase inhibitor projects including the PI3Kα selective inhibitor alpelisib, the pan-PI3K inhibitor CLR457, and the FGFR4 inhibitor roblitinib, and more recently he has been involved in the discovery of DFF332, an allosteric inhibitor of the transcription factor HIF2α. Prior to this Robin spent 11 years in the Respiratory Disease Chemistry Group within Novartis in Horsham, England, contributing to several GPCR and enzyme inhibitor projects including the discovery of the once-daily inhaled β2-adrenoceptor agonist indacaterol. Robin started his industrial career in Ciba Central Research, Macclesfield, England, joining an organophosphorus chemistry group exploring modified nucleic acids for antisense applications. A position he held up until the merger of Ciba with Sandoz in 1996 that resulted in the formation of Novartis. He received a PhD in Chemistry from the University of Loughborough working with Professor Harry Heaney developing synthetic methodology around acyliminium ion chemistry, and made Postdoctoral studies with Professor Philip Magnus at the University of Texas at Austin working on the synthesis of the enediyne natural product dynemicin.

Exploring and exploiting propellanes

Prof. Ed ANDERSON

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Ed ANDERSON

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Ed Anderson is Professor of Organic chemistry at the University of Oxford. He has research interests across synthetic organic chemistry, with a particular focus on the development of new synthetic methods, and the synthesis of bioactive molecules. In the former area, his research encompasses catalysis (including transition metal, asymmetric, and photoredox catalysis), bioisosteres, the reactivity of heteroatom-substituted alkynes, and mechanistic study. His work in target-oriented synthesis included antiparasitic natural products, polyketides, and the development of cascade processes in synthesis. Ed was an undergraduate at Oxford, then moved to Cambridge for his PhD with Prof Andrew Holmes. After postdoctoral research with Profs Erik Sorensen (Scripps Research Institute) and Ian Paterson (Cambridge), he took up an EPSRC Advanced Research Fellowship at Oxford, and was appointed as a Lecturer in 2009, with promotion to Professor in 2016. He is the recipient of the 2019 Novartis Chemistry Lectureship and the 2020 RSC Bader award, and is currently the head of Organic Chemistry at Oxford.

The Next Generation of BCPs: Exploring Substitutions on the Bridge

Dr Xiaoshen MA

MERCK & CO., INC, Boston, United States
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Dr Xiaoshen MA

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I am currently a senior scientist in the Department of Discovery Chemistry at Merch Research Laboratories in Boston, Massachusetts. In addition to my research for pipeline programs, I also conduct independent research as side projects in the development of novel synthetic methods accessing pharmaceutically relevant structures. We recently reported a series of publications focused on the synthesis of novel bicyclo[1.1.1]pentanes (BCPs), especially BCP analogues with substituents on the methylene positions. I hope to share with you our journey towards the discovery of these methodologies as well as some unpublished results. Before joining Merck, I conducted my PhD studies under the supervision of Prof. Seth B. Herzon at Yale University focusing on the topics of alkene hydrofunctionalization via hydrogen atom transfer mechanism, late-stage C H functionalization of (+)-pleuromutilin derivatives, and the host-release-factor in 0marine symbiotic systems.

Synthesis and Functionalization of Cyclopropane Derivatives

Dr Sophie ROUSSEAUX

UNIVERSITY OF TORONTO, Toronto, Canada
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Dr Sophie ROUSSEAUX

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Sophie Rousseaux is an Assistant Professor in the Department of Chemistry at the University of Toronto. She also holds a Canada Research Chair (Tier 2) in Organic Chemistry since 2016. Her group’s research interests include organic synthesis, catalysis, and organometallic chemistry. She is particularly interested in the synthesis and functionalization of small rings and nitrile-containing building blocks. Prior to joining the faculty at U of T in 2015, Sophie obtained her PhD from the University of Ottawa, working with Prof. Keith Fagnou and with Prof. Stephen L. Buchwald (MIT). She carried out postdoctoral studies as an NSERC postdoctoral fellow and Glasstone Research Fellow at the University of Oxford, working with Prof. Harry Anderson.

Dearomative Functionalizations: From Simple Arenes to Complex Molecules

Dr David SARLAH

UNIVERSITY OF ILLINOIS, Urbana, United States
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Dr David SARLAH

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David Sarlah is an associate professor of chemistry at the University of Illinois at Urbana-Champaign and adjunct associate professor at the University of Pavia. He was born in Slovenia, where he earned his B.S. degree from the University of Ljubljana. He obtained his Ph.D. in 2011 with Professor K. C. Nicolaou at The Scripps Research Institute, and then joined the laboratory of Professor Erick M. Carriera at ETH Zürich. In 2014, he started his independent career at Illinois, which explores both the chemical synthesis of biologically active natural products and method development. Some of his recent accomplishments include an NSF Career Award, 2019 Grammaticakis-Neumann Award, 2019 BMS Unrestricted Grant Award in Synthetic Chemistry, 2019 Amgen Young Investigator Award, 2019 Eli Lilly Organic Chemistry Award, ERC Starting Grant 2019, 2020 FMC New Investigator Award, and 2021 Arthur C. Cope Scholar Award.

Intracellular Oligonucleotide Distribution and Protein Binding

Dr Alice GHIDINI

ASTRAZENECA, Gothenburg, Sweden
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Dr Alice GHIDINI

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Dr Alice Ghidini has a broad background in nucleic acids technology gained during her doctoral and postdoctoral studies in the labs of three pioneers of the field, Roger Stromberg (Karolinska Institute), Peter Dervan (California Institute of Technology), and Jonathan Hall (ETH Zurich). During her studies in their laboratories, she accumulated expertise on the interaction between oligonucleotides and proteins/RNA targets, specifically though her work on RNA-based artificial enzymes, PNA triplexes, and antisense technologies. She lately developed the first single strand oligonucleotide-based PROTAC proof of concept, designed to degrade RNA-binding proteins. In 2021 she joined the Oligonucleotide platform of AstraZeneca as an Assistant Principal Scientist in the Biophysics department where she is studying the influence of ASOs’ proteins binding on their toxicity and potency.

Lessons in Transcellular Membrane Permeability Re-Learned

Dr Mike HANN

GSK MEDICINES RESEARCH CENTRE, Stevenage, United Kingdom
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Dr Mike HANN

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After completing his PhD in organic chemistry in 1980, Mike has worked in Pharma R&D initially as a medicinal chemist and then as a computational chemist. He joined Glaxo in 1986 and was responsible for helping initially build and then lead the computational chemistry department. He went on to lead the biophysics and protein crystallography activities including developing fragments theory and practice in lead identification. His current role is in looking at new technologies in early discovery to help reduce attrition in drug discovery, with particular interest in chemical biology, target tractability, drug distribution at cellular and subcellular resolution. Mike is a GSK Senior Fellow Alumni and an Adjunct Professor in the chemistry department at Imperial College London.

Molecular Chameleonicity and Cell Permeability of Drugs and PROTACs in the bRo5 Space

Prof. Jan KIHLBERG

UPPSALA UNIVERSITY, Uppsala, Sweden
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Prof. Jan KIHLBERG

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Professor Jan Kihlberg holds a chair in Organic Chemistry at Uppsala University, Sweden since 2013. His key research interests are to understand what properties convey cell permeability, aqueous solubility and target binding to drugs and PROTACs in the beyond rule of 5 space and to translate this knowledge into guidelines for design. His group is also involved in synthesis of macrocycles as ligands for difficult-to-drug targets. He has published 167 peer reviewed articles, 16 research reviews and four book chapters Before moving to Uppsala Prof. Kihlberg spent ten years at AstraZeneca R&D in Gothenburg, seven of which as Director of Medicinal Chemistry. He obtained his PhD in organic chemistry at Lund University in 1988.

Monitoring Drug Selectivity and Target Engagement Across Systems – Thermal Shift Assay in Drug Discovery

Dr Anna RUTKOWSKA-KLUTE

GSK, Heidelberg, Germany
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Dr Anna RUTKOWSKA-KLUTE

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After completing her PhD in molecular biology, Anna has worked as postdoc at European Molecular Biology Laboratory (EMBL) Heidelberg in the field of chemical biology. At Cellzome/GSK since 2014, Anna was first focusing on the development of methods to measure direct drug-target binding in cellular systems (e.g. the thermal shift assay, the click-probe based approach) as well as their application to support drug discovery at GSK and to and cellular drug disposition. Currently, Anna is a GSK Associate Fellow and works as a Scientific Leader in the Functional Genomics department leading the Cellular Assays and Biomarker Group aiming on in depth pre-clinical characterization of drug mode of action to support development of new treatments in the context of oncology diseases.

Innovative Strategies to Target Non-Coding RNAs with Synthetic Ligands

Dr Maria DUCA

UNIVERSITY OF CÔTE D'AZUR, Nice, France
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Dr Maria DUCA

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Dr. Maria DUCA is head of Targeting of Nucleic Acids research group in the Institute of Chemistry of Nice (Université Côte d’Azur - CNRS). After undergraduate studies in Pharmacy and Medicinal Chemistry (Faculty of Pharmacy, University of Bologna, Italy), she obtained her PhD in Molecular Biochemistry under the supervision of Dr. Paola B. Arimondo (National Natural History Museum, Paris, France) working on topoisomerase II inhibitors. A 2- year post-doctoral training in Sydney Hecht’s lab (Department of Chemistry, University of Virginia, USA) allowed her to pursue the study of nucleic acids working on targeted protein mutagenesis. After CNRS recruitment as a Research Scientist in 2007, her research activities focus on the targeting of non-coding RNAs using synthetic small molecules toward innovative therapeutic approaches for anticancer, antiviral and antimicrobial applications.

Design and Discovery of Clinical Candidate eFT226, a First-in-Class Inhibitor of the RNA Helicase eIF4A

Dr Christian NILEWSKI

GENENTECH, South San Francisco, United States
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Dr Christian NILEWSKI

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Christian Nilewski conducted his undergraduate studies at the University of Dortmund and the University of Münster in Germany. A synthetic organic chemist by training, he received his PhD in 2011 from ETH Zurich (Switzerland) under the supervision of Prof. Dr. Erick M. Carreira and conducted postdoctoral studies with Prof. K. C. Nicolaou at The Scripps Research Institute (La Jolla, California) and Rice University (Houston, Texas). Dr. Nilewski started his career as a Medicinal Chemist in 2014 at eFFECTOR Therapeutics in San Diego, California, where he was involved in several oncology drug discovery projects and contributed to the design and discovery of first-in-class small molecule inhibitors of eukaryotic initiation factors eIF4A (eFT226/zotatifin, currently in Phase 1) and eIF4E (currently undergoing preclinical development in collaboration with Pfizer). In 2019, Dr. Nilewski joined Genentech in South San Francisco, California, as a Scientist in the Small Molecule Discovery Chemistry Department.

Drugging RNA – A Structure-based Approach

Dr Jennifer PETTER

ARRAKIS THERAPEUTICS, Waltham, United States
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Dr Jennifer PETTER

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Dr. Jennifer Petter is the Founder and CSO of Arrakis Therapeutics. Previously she was Vice President of Chemistry at Celgene, Vice President of Drug Discovery at Avila Therapeutics, Vice President of Research at Mersana Therapeutics, Director of Small Molecule Drug Discovery at Biogen, Section Head in Oncology Chemistry at Sandoz/Novartis, and Assistant Professor of Chemistry at the University of Pittsburgh. Dr. Petter graduated from Dartmouth College with an AB in chemistry, earned her PhD in organic chemistry at Duke University with Ned Porter, and was a post-doctoral fellow in Ron Breslow’s group at Columbia University. She has ushered multiple compounds into the clinic for the treatment of cancer, cardiovascular disease, autoimmune disorders, and sepsis.

Title to be announced

Dr Nicolas THOMÄ

FRIEDRICH MIESCHER INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland

Title to be announced

Prof. Ang LI

SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, Shanghai, China

Title to be announced

Prof. Ruben MARTIN

INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA, Tarragona, Spain

Computationally Augmented Total Synthesis

Dr Timothy NEWHOUSE

YALE UNIVERSITY, New Haven, United States
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Dr Timothy NEWHOUSE

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Tim was born in New Hampshire and grew up in New England, northeastern U.S. He received his B.A. in Chemistry from Colby College (2005) in Waterville, ME, where he was mentored by Prof. Dasan M. Thamattoor. He completed his Ph.D. studies in 2010 at The Scripps Research Institute in La Jolla, CA, with Prof. Phil S. Baran. During his time at Scripps, he also worked in the laboratories of Prof. Donna G. Blackmond. He then returned to the east coast for postdoctoral studies with Prof. E.J. Corey at Harvard University. He joined the faculty at Yale in 2013, and as of 2018 he is an Associate Professor at Yale University in the Department of Chemistry. Tim’s research focuses on computational strategies and synthetic methodologies. He has received numerous awards, including the ACS Cope Scholar award, NSF CAREER Award, Sloan Research Fellowship, Camile Dreyfus Teacher Scholar Award, Genentech Research Innovation Award, and Amgen Young Investigator Award.

Understanding the PKPD and ADME of PF-07059013: An Allosteric Modulator of a High Abundance Target

Dr Kevin BEAUMONT

ASTRAZENECA, Cambridge, United Kingdom
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Dr Kevin BEAUMONT

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Kevin Beaumont has worked in the pharmaceutical industry for 37 years. Throughout that time he has worked extensively in the drug metabolism field, especially as it relates to drug discovery support. His major area of expertise is in the modulation of physicochemistry to affect drug disposition and in prediction of human pharmacokinetics. He is author on over 50 peer reviewed publications. Kevin has spent the majority of his career at Pfizer in both the UK and US. In 2020,Kevin returned to the UK and is currently with AstraZeneca supporting Oncology R&D with DMPK expertise.

Basic Concepts in TMDD

Dr David FAIRMAN

GSK, Cambridge, United Kingdom
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Dr David FAIRMAN

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David Fairman is a Senior Director in the Clinical Pharmacology, Modelling and Simulation group at GSK. He specialises in translational pharmacology within the early drug development phase and biologics PKPD. He has worked extensively on developing translational mechanistic models and leading collaborations developing QSP models covering areas including asthma and diabetes. Previous experience includes translational and clinical PKPD modelling at MedImmune and preclinical modelling at Pfizer (Sandwich UK). David has a BsC in pharmacology from the Open University, an MsC in Modelling & Simulation from the University of Manchester and has authored or co-authored over 15 scientific papers and is a co-inventor on patents covering 4 novel biological agents.