Archived: 14th Winter Conference
on Medicinal & Bioorganic Chemistry
January 27th - 31st 2019
Steamboat Springs Resort, Colorado
Agenda
Sunday, January 27th 2019
Drug Hunting
Program Chair: Dr Daniel Flynn, Deciphera Pharmaceuticals
The Invention of MK-8262, a CETP Inhibitor Backup to Anacetrapib (with best in class properties)
Cell Cycle Intervention Beyond Palbociclib; Preclinical Discovery of a CDK2/4/6 Inhibitor
TRK Inhibitor LOXO-101 and back up LOXO-195
Networking Session
Welcome Reception
Monday, January 28th 2019
Immuno-oncology
Program Chair: Dr Wes Trotter, Merck
Novel STING Agonists for Immuno-oncology
Discovery of BMS-986158, an Oral BET Inhibitor
Targeting the Adenosine Pathway with Non-Nucleoside Inhibitors of CD73
Design of Selective, Heme-binding Inhibitors of Tryptophan-2,3-dioxygenase (TDO)
Structural and in-Silico Chemistry
Program Chair: Dr Georgia McGaughey, Vertex
Giving Med Chemists the Comp Chem Tools for What They Want and What They Need
Computational Methods Help Find Chemical Matter to Uncover Novel Biology
The Role of Water Molecule in Ketohexokinase Inhibitor Design
Impact of Computational Chemistry Post Candidate Selection and Translating Lessons Learned back into Discovery
Tuesday, January 29th 2019
Chemical Biology for Drug Discovery
Program Chair: Dr Paola Castaldi, AstraZeneca
Reimagining Druggability using Chemoproteomic Platforms
Mapping Binding Site Hotspots in the Global Proteome by Photo-affinity Labeling Mass Spectrometry
Chemical Biology to provide insight into Small Molecule Targeting of BCL6
Targeted Protein Degradation
Potential New Therapies for the Treatment of Chronic Pain
Program Chair: Dr Sarah Skerratt, Vertex
Overview of Current Therapies for the Treatment of Pain
Breathe Easy: Mechanistic Insights Enable a Path Forward for Highly Selective Nav1.7 Inhibitors
Harnessing Opioid Receptor Signaling to Improve Pain Therapeutics
Discovery And Optimization Of A Novel CGRP Receptor Antagonist Chemotype For The Treatment of Migraine
TRPA1: A Pain Target or a Painful Target?
Structure-Based Drug Discovery in the Search for Nav1.7 Inhibitors
Wednesday, January 30th 2019
Recent Advances in Targeting Autophagy
Program Chair: Professor Jay Debnath (UCSF)
Complexities of Targeting Autophagy to Treat Human Disease
Targeting the Autophagy-Initiating Kinase ULK1
Combined Targeting of MAP Kinase Signalling and Autophagy for the Future Therapy of Cancers Driven by the RAS Pathway
Advances in Targeting Lysosomotrophic Agents
Advances in Synthesis and Medicinal Chemistry
Program Chair: Professor Darren Dixon, University of Oxford
Discovery and Evaluation of Non-Nitrocatechol COMT Inhibitors for Treatment of Psychiatric Conditions
Intrinsic Aminomethyl Pyridine Enables Regioselective C-H Arylation in the Synthesis of IKur Inhibitor, BMS-919373
Development of Inhibitors of MsbA: From HTS to Gram-negative Wild-type Activity
Hit-to-lead Medicinal Chemistry Targeting Neglected Tropical Diseases
Targeting of the Glutamine Antagonist DON (6-Diazo-5-oxo-L-norleucine) via Prodrug Approach
The Role of Solution Conformation in Structure-Guided Fragment Optimization
Pyridyl Urea Sulfonamide Inhibitors of NaV1.7: Intramolecular Hydrogen Bonding Leads to Improved Properties and Exposure
New Broad Scope Strategies for Amine Synthesis
Thursday, January 31st 2019
Photoredox Catalysis
Program Chair: Dr Dan DiRocco, Merck
Recent Advances in the Remote Functionalization of Aliphatic C-H Bonds via Decatungstate Photocatalysis
Enablement of Photoredox Csp2-Csp3 Cross Coupling Reactions
Scaling Catalytic Photochemistry with Lasers
Photoredox Catalysis – An Enabling Platform for Discovery and Development
Controlling Catalysis with Visible Light
KEY NOTE PRESENTATION
Program Chair: Professor Michael Vannieuwenhze, Indiana University
Translational Chemistry
Networking Session
Poster Session & Pre-Dinner Drinks
Networking Session
Conference Dinner
Short course
Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery
Tuesday 29th January 2019: 12.00 – 4.00 pm
& Wednesday 30th January 2019: 12.00 – 4.00 pm