1st Alpine Winter Conference on Medicinal and Synthetic Chemistry

 St. Anton, Austria    January 28

Keynote Speakers

Erick M. CARREIRA
KL01 - Recent Developments in Strategies and Tactics Towards the Synthesis of Complex Secondary Metabolites as Enabling Tools for the Study of Biology and Medicine
Benjamin CRAVATT
KL02 - Activity-based proteomics – Protein and Ligand Discovery on a Global Scale
Anabella VILLALOBOS
KL03 - Novel Approaches in the Design of CNS Drug Candidates and PET Ligands

Addressing Preclinical Toxicity – Approaches and Lessons Learned

Andreas BRINK
PL06 - Reducing Bioactivation Potential of Drug Candidates: Implications for Preclinical Drug Optimization
Peter DRAGOVICH
PL04 - Mechanism-Based Toxicities Associated With NAMPT Inhibition and Related Mitigation Strategies
Martin PETTERSSON
OC02 - Small Structural Changes Leading to Major Impact on Safety: Developing Safety Strategies in Medicinal Chemistry
Douglas THOMSON
PL05 - Utilizing in Depth Understanding of a Molecules Off-Target Profile to Tailor Clinical and Preclinical Safety Assessments
 
 

Advances in Lead Generation

Monika ERMANN
PL08 - A Chemist’s Guide to Modern Phenotypic Drug Discovery
Koen HEKKING
OC03 - CDK8 Inhibitors with Pre-Engineerd Long Residence Time, Exhibiting Efficacy in Tumor Xenograft Models
Eva Maria MARTIN
PL07 - ADAS (Affinity Directed Automated Synthesis): A New Technology to Accelerate Lead Generation
Sanne SCHRODER GLAD
PL09 - From Multiple Hit Series to (Pre)Clinical Candidates Using DNA-Encoded Library Technology
 
 

Advances in Synthetic Methods

Varinder K. AGGARWAL
PL01 - Assembly Line Synthesis
Thorsten BACH
PL02 - Photochemical Reactions en route to Structurally Complex Molecules
Paolo MELCHIORRE
PL03 - Expanding the Potential of Organocatalysis with Light
Peter O'BRIEN
OC01 - Exploring 3-D Pharmaceutical Space: New CH Functionalisation Reactions of Oxygen and Sulfur Heterocycles
 
 

Alternative Modalities

Niall ANDERSON
OC05 - Proteolysis Targetting Chimera: A New Frontier in Medicinal Chemistry
Kerry BENENATO
PL13 - Messenger RNA as a Novel Therapeutic Approach
David TELLERS
PL11 - Intracellular Delivery of Macromolecules
Eric VALEUR
PL12 - New Modalities Probe and Hit Finding for Challenging Targets in Cardiovascular and Metabolic Diseases
 
 

Challenges and Opportunities in Fragment Based Drug Discovery

Christoph GAUL
OC07 - Fragment-Centric Methodologies for the Discovery of DOT1L Inhibitors
Jean-Francois GUICHOU
OC12 - Rational Design of Small-Molecules Inhibitors of Human Cyclophilins with a Pan Viral Activities by Fragment Based Drug Design Using a Linking Strategy
Tom HEIGHTMAN
PL17 - Drug Discovery for Challenging Targets by X-ray Crystallographic Fragment Screening
Rod HUBBARD
PL18 - The Impact of Fragments on Drug Discovery
 
 

Chemical Biology in Drug and Target Discovery

Gonçalo BERNARDES
OC04 - Chemical Physiology of Antibody Conjugates and Natural Products
Kai JOHNSSON
PL10 - Fluorescent and Bioluminescent Sensor Proteins
 

Late Stage Functionalization

Nicolai CRAMER
PL15 - The Quest for Efficient Ligands in Asymmetric C-H Functionalizations
Darren J. DIXON
PL16 - Catalytic Approaches to Simplifying Synthesis
Matthew GAUNT
PL14 - New Chemical Tools for the Late Stage Functionalization of Biomolecules
Mark LAUTENS
OC06 - Synthetic Routes to Oxindoles via Metal Catalysis
 
 

Drug Discovery Tales

OC10 - Molecular Accessibility - Measuring and Understanding the Intracellular Free Concentration of Drugs During Lead Optimisation
Holger MONENSCHEIN
OC09 - Discovery of Tak-041: A Potent and Selective Gpr139 Agonist for the Treatment of Negative Symptoms Associated with Schizophrenia
Jean QUANCARD
OC08 - Discovery of Allosteric Malt1 Protease Inhibitors with High in Vivo Efficacy
Brian RAYMER
OC11 - Discovery of a Ketohexokinase Inhibitor for the Treatment of Nafld/Nash: Fragment-to-Candidate via Structure-Based Drug Design and Parallel Chemistry