1st Alpine Winter Conference on Medicinal and Synthetic Chemistry

 St. Anton, Austria    January 28

Programme


17:00

Opening Remarks

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

20:15

End of Day 1

Session 1: Advances in Synthetic Methods

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

10:00

PL03 - Expanding the Potential of Organocatalysis with Light

Paolo MELCHIORRE
INSTITUTE OF CHEMICAL RESEARCH OF CATALONIA (ICIQ), Tarragona, Spain
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

Session 2: Addressing Preclinical Toxicity – Approaches and Lessons Learned

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

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

20:45

End of Day 2

Session 3: Advances in Lead Generation

Session Chair

Doris RIETHER
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, 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

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

Session 4: Chemical Biology in Drug and Target Discovery

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

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

Session 5: Alternative Modalities

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

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

Session 6: Late Stage Functionalization

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

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

21:00

Conference Dinner

23:00

End of Day 4

Session 7: Challenges and Opportunities in Fragment Based Drug Discovery

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

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

Session 8: Drug Discovery Tales

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

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

20:00

End of Symposium