1st Alpine Winter Conference on Medicinal and Synthetic Chemistry

The final programme is now available!

Spread the word with #AlpineWinterConference

Sunday January 28, 2018
17:00Opening Remarks
17:15KL01 - 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)
18:15Poster Session & Welcome Reception
20:15End of Day 1
Monday January 29, 2018
Session 1: Advances in Synthetic Methods
Session Chair
Nuno MAULIDE
(UNIVERSITY OF VIENNA, Vienna, Austria)
08:30PL01 - Assembly Line Synthesis
Varinder K. AGGARWAL
(UNIVERSITY OF BRISTOL, Bristol, United Kingdom)
09:00PL02 - Photochemical Reactions en route to Structurally Complex Molecules
Thorsten BACH
(TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany)
09:30Coffee Break
10:00PL03 - Expanding the Potential of Organocatalysis with Light
Paolo MELCHIORRE
(INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA (ICIQ), Tarragona, Spain)
10:30OC01 - Exploring 3-D Pharmaceutical Space: New CH Functionalisation Reactions of Oxygen and Sulfur Heterocycles
Peter O'BRIEN
(UNIVERSITY OF YORK, York, United Kingdom)
11:00End of the morning session
Session 2: Addressing Preclinical Toxicity – Approaches and Lessons Learned
Session Chair
Andy PEAT
(GLAXOSMITHKLINE, United States)
17:30PL04 - Mechanism-Based Toxicities Associated With NAMPT Inhibition and Related Mitigation Strategies
Peter DRAGOVICH
(GENENTECH INC., San Francisco, United States)
18:00PL05 - Utilizing in Depth Understanding of a Molecules Off-Target Profile to Tailor Clinical and Preclinical Safety Assessments
Douglas THOMSON
(CELLZOME GMBH, Heidelberg, Germany)
18:30Coffee Break
19:00PL06 - Reducing Bioactivation Potential of Drug Candidates: Implications for Preclinical Drug Optimization
Andreas BRINK
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
19:30OC02 - Small Structural Changes Leading to Major Impact on Safety: Developing Safety Strategies in Medicinal Chemistry
Martin PETTERSSON
(PFIZER, Cambridge, United States)
20:00Panel Discussion
20:45End of Day 2
Tuesday January 30, 2018
Session 3: Advances in Lead Generation
Session Chair
Doris RIETHER
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany)
08:30PL07 - ADAS (Affinity Directed Automated Synthesis): A New Technology to Accelerate Lead Generation
Eva Maria MARTIN
(ELI LILLY, Madrid, Spain)
09:00PL08 - A Chemist’s Guide to Modern Phenotypic Drug Discovery
Monika ERMANN
(EVOTEC LTD, Oxfordshire, United Kingdom)
09:30Coffee Break
10:00OC03 - CDK8 Inhibitors with Pre-Engineerd Long Residence Time, Exhibiting Efficacy in Tumor Xenograft Models
Koen HEKKING
(MERCACHEM-SYNCOM, Nijmegen, The Netherlands)
10:30PL09 - From Multiple Hit Series to (Pre)Clinical Candidates Using DNA-Encoded Library Technology
Sanne SCHRODER GLAD
(NUEVOLUTION A/S, Copenhagen, Denmark)
11:00End of the morning session
Session 4: Chemical Biology in Drug and Target Discovery
Session Chair
Matthew HAYWARD
(PFIZER, Groton, United States)
17:30PL10 - Fluorescent and Bioluminescent Sensor Proteins
Kai JOHNSSON
(MAX-PLANCK INSTITUTE FOR MEDICAL RESEARCH, Heidelberg, Germany)
18:00OC04 - Chemical Physiology of Antibody Conjugates and Natural Products
Gonçalo BERNARDES
(INSTITUTO DE MEDICINA MOLECULAR, LISBON, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
18:30Coffee Break
19:00KL02 - Activity-based proteomics – Protein and Ligand Discovery on a Global Scale
Benjamin CRAVATT
(THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States)
20:00End of Day 3
Wednesday January 31, 2018
Session 5: Alternative Modalities
Session Chair
Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States)
08:30PL11 - Intracellular Delivery of Macromolecules
David TELLERS
(MERCK & CO. INC (MSD), West Point, United States)
09:00PL12 - New Modalities Probe and Hit Finding for Challenging Targets in Cardiovascular and Metabolic Diseases
Eric VALEUR
(ASTRAZENECA, Västra Frölunda, Sweden)
09:30Coffee Break
10:00PL13 - Messenger RNA as a Novel Therapeutic Approach
Kerry BENENATO
(MODERNA THERAPEUTICS, Cambridge, United States)
10:30OC05 - Proteolysis Targetting Chimera: A New Frontier in Medicinal Chemistry
Niall ANDERSON
(GLAXOSMITHKLINE, Hertfordshire, United Kingdom)
11:00End of the morning session
Session 6: Late Stage Functionalization
Session Chair
Guido KOCH
(TOPADUR PHARMA AG, Schlieren, Switzerland)
17:30PL14 - New Chemical Tools for the Late Stage Functionalization of Biomolecules
Matthew GAUNT
(UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
18:00PL15 - The Quest for Efficient Ligands in Asymmetric C-H Functionalizations
Nicolai CRAMER
(ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE, Lausanne, Switzerland)
18:30Coffee Break
19:00PL16 - Catalytic Approaches to Simplifying Synthesis
Darren J. DIXON
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
19:30OC06 - Synthetic Routes to Oxindoles via Metal Catalysis
Mark LAUTENS
(UNIVERSITY OF TORONTO, Toronto, ON, Canada)
20:00End of the Scientific Programme on Day 4
21:00Conference Dinner
23:00End of Day 4
Thursday February 1, 2018
Session 7: Challenges and Opportunities in Fragment Based Drug Discovery
Session Chair
Alison WOOLFORD
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
08:30PL17 - Drug Discovery for Challenging Targets by X-ray Crystallographic Fragment Screening
Tom HEIGHTMAN
(ASTEX THERAPEUTICS, Cambridge, United Kingdom)
09:00PL18 - The Impact of Fragments on Drug Discovery
Rod HUBBARD
(UNIVERSITY OF YORK & VERNALIS, Cambridge, United Kingdom)
09:30Coffee Break
10:00PL19 - Fragment Based Discovery of Small Molecule MRCK Inhibitors
Mairi SIME
(BEATSON INSTITUTE FOR CANCER RESEARCH, Bearsden Glasgow , United Kingdom)
10:30OC07 - Fragment-Centric Methodologies for the Discovery of DOT1L Inhibitors
Christoph GAUL
(NOVARTIS, Basel, Switzerland)
11:00End of the morning session
Session 8: Drug Discovery Tales
Session Chair
Sarah SKERRATT
(VERTEX PHARMACEUTICALS, Oxon, United Kingdom)
17:10OC08 - Discovery of Allosteric Malt1 Protease Inhibitors with High in Vivo Efficacy
Jean QUANCARD
(NOVARTIS, Basel, Switzerland)
17:30OC09 - 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)
17:50OC10 - Molecular Accessibility - Measuring and Understanding the Intracellular Free Concentration of Drugs During Lead Optimisation
Mike HANN
(GLAXOSMITHKLINE, Stevenage, United Kingdom)
18:10OC11 - 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)
18:30Coffee Break
19:00KL03 - Novel Approaches in the Design of CNS Drug Candidates and PET Ligands
Anabella VILLALOBOS
(BIOGEN, Cambridge, United States)
19:45Closing Remarks
20:00End of Symposium

Copyright 2018 LD Organisation  |  rue Michel de Ghelderode 33/02 B-1348  Louvain-la-Neuve (Belgium)  Tel. +32 10 454777  |   |  VAT: BE 0464819842
Developed and powered by Antalys