Sunday 28/01/2018 |
17:00 | Opening Remarks |
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17:15 | 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) |
18:15 | Poster Session & Welcome Reception |
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20:15 | End of Day 1 |
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Monday 29/01/2018 |
| Session 1: Advances in Synthetic Methods
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| Session Chair |
Nuno MAULIDE (UNIVERSITY OF VIENNA, Vienna, Austria) |
08:30 | PL01 - Assembly Line Synthesis |
Varinder K. AGGARWAL (UNIVERSITY OF BRISTOL, Bristol, United Kingdom) |
09:00 | PL02 - Photochemical Reactions en route to Structurally Complex Molecules |
Thorsten BACH (TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany) |
09:30 | Coffee Break |
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10:00 | PL03 - Expanding the Potential of Organocatalysis with Light |
Paolo MELCHIORRE (INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA (ICIQ), Bologna, Italy) |
10:30 | OC01 - Exploring 3-D Pharmaceutical Space: New CH Functionalisation Reactions of Oxygen and Sulfur Heterocycles |
Peter O'BRIEN (UNIVERSITY OF YORK, York, United Kingdom) |
11:00 | End of the morning session |
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| Session 2: Addressing Preclinical Toxicity – Approaches and Lessons Learned
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| Session Chair |
Andy PEAT (GLAXOSMITHKLINE, Durham, United States) |
17:30 | PL04 - Mechanism-Based Toxicities Associated With NAMPT Inhibition and Related Mitigation Strategies |
Peter DRAGOVICH (GENENTECH INC., San Francisco, United States) |
18:00 | PL05 - Utilizing in Depth Understanding of a Molecules Off-Target Profile to Tailor Clinical and Preclinical Safety Assessments |
Douglas THOMSON (CELLZOME GMBH, Heidelberg, Germany) |
18:30 | Coffee Break |
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19:00 | PL06 - Reducing Bioactivation Potential of Drug Candidates: Implications for Preclinical Drug Optimization |
Andreas BRINK (F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
19:30 | OC02 - Small Structural Changes Leading to Major Impact on Safety: Developing Safety Strategies in Medicinal Chemistry |
Martin PETTERSSON (PFIZER, Cambridge, United States) |
20:00 | Panel Discussion |
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20:45 | End of Day 2 |
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Tuesday 30/01/2018 |
| Session 3: Advances in Lead Generation
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| Session Chair |
Doris RIETHER (BOEHRINGER INGELHEIM, Biberach an der Riss, Germany) |
08:30 | PL07 - ADAS (Affinity Directed Automated Synthesis): A New Technology to Accelerate Lead Generation |
Eva Maria MARTIN (ELI LILLY, Madrid, Spain) |
09:00 | PL08 - A Chemist’s Guide to Modern Phenotypic Drug Discovery |
Monika ERMANN (EVOTEC LTD, Oxfordshire, United Kingdom) |
09:30 | Coffee Break |
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10:00 | OC03 - CDK8 Inhibitors with Pre-Engineerd Long Residence Time, Exhibiting Efficacy in Tumor Xenograft Models |
Koen HEKKING (MERCACHEM-SYNCOM, Nijmegen, The Netherlands) |
10:30 | PL09 - From Multiple Hit Series to (Pre)Clinical Candidates Using DNA-Encoded Library Technology |
Sanne SCHRODER GLAD (NUEVOLUTION A/S, Copenhagen, Denmark) |
11:00 | End of the morning session |
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| Session 4: Chemical Biology in Drug and Target Discovery
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| Session Chair |
Matthew HAYWARD (PFIZER, Groton, United States) |
17:30 | PL10 - Fluorescent and Bioluminescent Sensor Proteins |
Kai JOHNSSON (MAX-PLANCK INSTITUTE FOR MEDICAL RESEARCH, Heidelberg, Germany) |
18:00 | OC04 - Chemical Physiology of Antibody Conjugates and Natural Products |
Gonçalo BERNARDES (INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom) |
18:30 | Coffee Break |
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19:00 | KL02 - Activity-based proteomics – Protein and Ligand Discovery on a Global Scale |
Benjamin CRAVATT (THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States) |
20:00 | End of Day 3 |
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Wednesday 31/01/2018 |
| Session 5: Alternative Modalities
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| Session Chair |
Philippe NANTERMET (MERCK & CO. INC (MSD), West Point, United States) |
08:30 | PL11 - Intracellular Delivery of Macromolecules |
David TELLERS (MERCK & CO. INC (MSD), West Point, United States) |
09:00 | PL12 - New Modalities Probe and Hit Finding for Challenging Targets in Cardiovascular and Metabolic Diseases |
Eric VALEUR (ASTRAZENECA, IMED BIOTECH UNIT, Cambridge, United States) |
09:30 | Coffee Break |
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10:00 | PL13 - Messenger RNA as a Novel Therapeutic Approach |
Kerry BENENATO (MODERNA THERAPEUTICS, Cambridge, United States) |
10:30 | OC05 - Proteolysis Targetting Chimera: A New Frontier in Medicinal Chemistry |
Niall ANDERSON (GLAXOSMITHKLINE, Hertfordshire, United Kingdom) |
11:00 | End of the morning session |
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| Session 6: Late Stage Functionalization
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| Session Chair |
Guido KOCH (NOVARTIS PHARMA AG, Schlieren, Switzerland) |
17:30 | PL14 - New Chemical Tools for the Late Stage Functionalization of Biomolecules |
Matthew GAUNT (UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom) |
18:00 | PL15 - The Quest for Efficient Ligands in Asymmetric C-H Functionalizations |
Nicolai CRAMER (ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE, Lausanne, Switzerland) |
18:30 | Coffee Break |
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19:00 | PL16 - Catalytic Approaches to Simplifying Synthesis |
Darren J. DIXON (UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
19:30 | OC06 - Synthetic Routes to Oxindoles via Metal Catalysis |
Mark LAUTENS (UNIVERSITY OF TORONTO, Toronto, ON, Canada) |
20:00 | End of the Scientific Programme on Day 4 |
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21:00 | Conference Dinner |
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23:00 | End of Day 4 |
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Thursday 01/02/2018 |
| Session 7: Challenges and Opportunities in Fragment Based Drug Discovery
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| Session Chair |
Alison WOOLFORD (ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) |
08:30 | PL17 - Drug Discovery for Challenging Targets by X-ray Crystallographic Fragment Screening |
Tom HEIGHTMAN (ASTEX PHARMACEUTICALS, Cambridge, United Kingdom) |
09:00 | PL18 - The Impact of Fragments on Drug Discovery |
Rod HUBBARD (UNIVERSITY OF YORK & VERNALIS, Cambridge, United Kingdom) |
09:30 | Coffee Break |
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10:00 | 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) |
10:30 | OC07 - Fragment-Centric Methodologies for the Discovery of DOT1L Inhibitors |
Christoph GAUL (NOVARTIS, Basel, Switzerland) |
11:00 | End of the morning session |
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| Session 8: Drug Discovery Tales
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| Session Chair |
Sarah SKERRATT (VERTEX PHARMACEUTICALS, London, United Kingdom) |
17:10 | OC08 - Discovery of Allosteric Malt1 Protease Inhibitors with High in Vivo Efficacy |
Jean QUANCARD (NOVARTIS, Basel, Switzerland) |
17:30 | 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) |
17:50 | OC10 - Molecular Accessibility - Measuring and Understanding the Intracellular Free Concentration of
Drugs During Lead Optimisation |
(EYEDPHARMA) |
18:10 | 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) |
18:30 | Coffee Break |
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19:00 | KL03 - Novel Approaches in the Design of CNS Drug Candidates and PET Ligands |
Anabella VILLALOBOS (BIOGEN, Cambridge, United States) |
19:45 | Closing Remarks |
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20:00 | End of Symposium |
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