St. Anton, Austria January 28
Opening Remarks
KL01 - Recent Developments in Strategies and Tactics Towards the Synthesis of Complex Secondary Metabolites as Enabling Tools for the Study of Biology and Medicine
Erick M. CARREIRA
ETH ZÜRICH, Zürich, Switzerland
Poster Session & Welcome Reception
End of Day 1
Session Chair
Nuno MAULIDE
UNIVERSITY OF VIENNA, Vienna, Austria
PL02 - Photochemical Reactions en route to Structurally Complex Molecules
Thorsten BACH
TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany
Coffee Break
PL03 - Expanding the Potential of Organocatalysis with Light
Paolo MELCHIORRE
INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA (ICIQ), Tarragona, Spain
OC01 - Exploring 3-D Pharmaceutical Space: New CH Functionalisation Reactions of Oxygen and Sulfur Heterocycles
Peter O'BRIEN
UNIVERSITY OF YORK, York, United Kingdom
End of the morning session
Session Chair
Andy PEAT
GLAXOSMITHKLINE, Durham, United States
PL04 - Mechanism-Based Toxicities Associated With NAMPT Inhibition and Related Mitigation Strategies
Peter DRAGOVICH
GENENTECH INC., San Francisco, United States
PL05 - Utilizing in Depth Understanding of a Molecules Off-Target Profile to Tailor Clinical and Preclinical Safety Assessments
Douglas THOMSON
CELLZOME GMBH, Heidelberg, Germany
Coffee Break
PL06 - Reducing Bioactivation Potential of Drug Candidates: Implications for Preclinical Drug Optimization
Andreas BRINK
F. HOFFMANN-LA ROCHE, Basel, Switzerland
OC02 - Small Structural Changes Leading to Major Impact on Safety: Developing Safety Strategies in Medicinal Chemistry
Martin PETTERSSON
PFIZER, Cambridge, United States
Panel Discussion
End of Day 2
Session Chair
Doris RIETHER
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany
PL07 - ADAS (Affinity Directed Automated Synthesis): A New Technology to Accelerate Lead Generation
Eva Maria MARTIN
ELI LILLY, Madrid, Spain
PL08 - A Chemist’s Guide to Modern Phenotypic Drug Discovery
Monika ERMANN
EVOTEC LTD, Oxfordshire, United Kingdom
Coffee Break
OC03 - CDK8 Inhibitors with Pre-Engineerd Long Residence Time, Exhibiting Efficacy in Tumor Xenograft Models
Koen HEKKING
MERCACHEM-SYNCOM, Nijmegen, The Netherlands
PL09 - From Multiple Hit Series to (Pre)Clinical Candidates Using DNA-Encoded Library Technology
Sanne SCHRODER GLAD
NUEVOLUTION A/S, Copenhagen, Denmark
End of the morning session
Session Chair
Matthew HAYWARD
PFIZER, Groton, United States
PL10 - Fluorescent and Bioluminescent Sensor Proteins
Kai JOHNSSON
MAX-PLANCK INSTITUTE FOR MEDICAL RESEARCH, Heidelberg, Germany
OC04 - Chemical Physiology of Antibody Conjugates and Natural Products
Gonçalo BERNARDES
INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
Coffee Break
KL02 - Activity-based proteomics – Protein and Ligand Discovery on a Global Scale
Benjamin CRAVATT
THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States
End of Day 3
Session Chair
Philippe NANTERMET
MERCK & CO. INC (MSD), West Point, United States
PL11 - Intracellular Delivery of Macromolecules
David TELLERS
MERCK & CO. INC (MSD), West Point, United States
PL12 - New Modalities Probe and Hit Finding for Challenging Targets in Cardiovascular and Metabolic Diseases
Eric VALEUR
ASTRAZENECA, IMED BIOTECH UNIT, Cambridge, United States
Coffee Break
PL13 - Messenger RNA as a Novel Therapeutic Approach
Kerry BENENATO
MODERNA THERAPEUTICS, Cambridge, United States
OC05 - Proteolysis Targetting Chimera: A New Frontier in Medicinal Chemistry
Niall ANDERSON
GLAXOSMITHKLINE, Hertfordshire, United Kingdom
End of the morning session
Session Chair
Guido KOCH
NOVARTIS PHARMA AG, Schlieren, Switzerland
PL14 - New Chemical Tools for the Late Stage Functionalization of Biomolecules
Matthew GAUNT
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
PL15 - The Quest for Efficient Ligands in Asymmetric C-H Functionalizations
Nicolai CRAMER
ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE, Lausanne, Switzerland
Coffee Break
PL16 - Catalytic Approaches to Simplifying Synthesis
Darren J. DIXON
UNIVERSITY OF OXFORD, Oxford, United Kingdom
OC06 - Synthetic Routes to Oxindoles via Metal Catalysis
Mark LAUTENS
UNIVERSITY OF TORONTO, Toronto, ON, Canada
End of the Scientific Programme on Day 4
Conference Dinner
End of Day 4
Session Chair
Alison WOOLFORD
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
PL17 - Drug Discovery for Challenging Targets by X-ray Crystallographic Fragment Screening
Tom HEIGHTMAN
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
PL18 - The Impact of Fragments on Drug Discovery
Rod HUBBARD
UNIVERSITY OF YORK & VERNALIS, Cambridge, United Kingdom
Coffee Break
OC12 - Rational Design of Small-Molecules Inhibitors of Human Cyclophilins with a Pan Viral Activities by Fragment Based Drug Design Using a Linking Strategy
Jean-Francois GUICHOU
CBS INSERM U1054, Montpellier, France
OC07 - Fragment-Centric Methodologies for the Discovery of DOT1L Inhibitors
Christoph GAUL
NOVARTIS, Basel, Switzerland
End of the morning session
Session Chair
Sarah SKERRATT
VERTEX PHARMACEUTICALS, London, United Kingdom
OC08 - Discovery of Allosteric Malt1 Protease Inhibitors with High in Vivo Efficacy
Jean QUANCARD
NOVARTIS, Basel, Switzerland
OC09 - Discovery of Tak-041: A Potent and Selective Gpr139 Agonist for the Treatment of Negative Symptoms Associated with Schizophrenia
Holger MONENSCHEIN
TAKEDA CALIFORNIA, INC, San Diego, United States
OC10 - Molecular Accessibility - Measuring and Understanding the Intracellular Free Concentration of Drugs During Lead Optimisation
EYEDPHARMA
OC11 - Discovery of a Ketohexokinase Inhibitor for the Treatment of Nafld/Nash: Fragment-to-Candidate via Structure-Based Drug Design and Parallel Chemistry
Brian RAYMER
PFIZER, Cambridge, United States
Coffee Break
KL03 - Novel Approaches in the Design of CNS Drug Candidates and PET Ligands
Anabella VILLALOBOS
BIOGEN, Cambridge, United States
Closing Remarks
End of Symposium