Archived: 12th Winter Conference
on Medicinal & Bioorganic Chemistry

January 25th - 29th 2015

Steamboat Springs Resort, Colorado

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Agenda

Sunday, January 25th 2015

Innovations in Drug Candidate Development

Program Chair: Pat Verhoest, Pfizer

Dr Travis Wager Pfizer

Improving the Odds of Compound Survival in Neuroscience

Dr Anthony Estrada Genentech

Discovery of Highly Potent, Selective and Brain-Penetrant LRRK2 Inhibitors for the Treatment of Parkinson’s Disease

Dr Chris Butler Pfizer

Beta-Secretase (BACE1) Inhibitors for the Treatment of Alzheimer’s Disease

Professor Craig Lindsley Vanderbilt University

Allosteric Modulation of Muscarinic Receptors

Monday, January 26th 2015

Perfecting Directed Aromatic and Heteroaromatic Ring Functionalization

Program Chair: Victor Snieckus, Queen’s University

Dr Shane W. Krska Merck Research Laboratories

Leveraging Emerging C-H Functionalization Chemistries for Efficient Diversification of Medicinally Important Heterocycles

Professor Vladimir Gevorgyan University of Illinois

Novel Methods for Synthesis and C-H Functionalization of Arenes and Heteroarenes

Professor Jennifer Schomaker University of Wisconsin

Cu(I)-Catalyzed Arene Functionalization via 1,3-Halogen Migration

Dr Vincent Mascitti Pfizer

Recent Developments in the Sulfination of (Hetero) Aromatic Rings: Direct Access to Sulfones and Sulfonamides of Medicinal Chemistry Relevance.

Recent Innovations in Medicinal and Bioorganic Chemistry

Program Chair: Mike VanNieuwenhze, Indiana University

Professor Anthony G.M. Barrett Imperial College

Cascade Polyketide and Polyene Cyclizations: Biomimetic Total Synthesis of Hongoquercin B

Dr Paul Richardson Pfizer

Route Development for the Synthesis of EML4-ALK Inhibitor PF-06463922

Dr Rachel Stevenson Queensland University

Lipo-Peptide Glycoconjugates for Targeting Antigen Presenting Cells

Professor Jimmy Wu Dartmouth College

Identification of GLP-1 Secretagogues – Targeting Type 2 Diabetes Mellitus

Dr Tim Cushing Amgen

Targeting PI3Kd for Inflammation: Discovery and In Vivo Evaluation AMG319 and Related Inhibitors

Dr Michael Pollastri Northeastern University

Hit‐to‐lead Medicinal Chemistry for African Sleeping Sickness: An Invitation to Shared Hit‐to‐Lead Medicinal Chemistry Pursuit of Chemotypes Identified from a Kinase‐Targeted High‐Throughput Screening Campaign.

Tuesday, January 27th 2015

Mitigating Drug Induced Liver Injury (DILI) In Drug Discovery

Program Chair: Bryan Norman, Eli Lilly

Professor Kevin Park University of Liverpool

Mechanism Based Translational Biomarkers for the Prediction of Drug Induced Liver Injury

Dr Antonia Stepan Pfizer

Reactive Metabolites in Drug-Induced Liver Injury

Dr Simone Stahl AstraZeneca

Inhibition of Hepatobiliary Transporters in Drug-Induced Liver Injury

Dr Landon Whitby The Scripps Research Institute

A Chemoproteomic Platform for Profiling the Targets of Reactive Drug Metabolites

James Rinker Elsevier Life Science Solutions | Workshop

Frontiers in Synthesis

Program Chair: Anthony G.M. Barrett, Imperial College

Dr Matt Fuchter Imperial College

Histone Methyltransferase Inhibitors: Fast acting Molecules against Blood and Liver Stage Malaria Parasites

Professor Istvan Toth University of Queensland

Dendritic Vaccine Delivery Systems

Dr Gilles Tamagnan MN Imagin

Application of PET and SPECT Radiotracers in Drug Development

Dr Michael Visser Novartis Institute for Biomedical Research

Drug Discovery Efforts towards the Identification of Potent and Selective Tankyrase Inhibitors

Dr Colin Groom Cambridge Crystallographic Data Centre

Drug Discovery and Development by Design: Using the Knowledge from every Organic Crystal Structure Ever Published

Mr Mark Dornan University of Ottawa

Development of a Novel Class of Small Molecules used to Potentiate Tumor-Specific Oncolytic Virus Infection

Professor Michael VanNieuwenhze Indiana University

Novel Chemical Probes for Use in the Study of Peptidoglycan Biosynthesis

Dr Matthew Duncton Rigel

Tetrazolone as an Acid Bioisostere: ‘Clickable’ Synthesis & Applications to Marketed Drugs

Wednesday, January 28th 2015

Advances in Cellular Readouts of Target Engagement and Cell Signaling Pathway Analysis

Program Chair: Daniel Flynn, Deciphera

Dr Tyzoon Nomanbhoy ActivX Biosciences

Monitoring Target Engagement and Signaling Pathways through Chemoproteomic Interrogation of Nucleotide Binding Space

Dr Pär Nordlund Karolinski Institute

Monitoring Target Engagement using the Cellular Thermal Shift Assay for Lead Drug Development, Drug Deorphanization and Off-Target Studies

Dr Joesph Beechem NanoString

Simultaneous Analysis of Cancer Pathway Deregulation (Tumor-Centric) and Cancer Immune Response (Host-Centric)

Dr Daniel Flynn Deciphera Pharmaceuticals

Understanding and Overcoming the Vagaries of Target Engagement within the Ras-RAF-MEK-ERK Signalling Pathway

Strategies and Novel Platforms for Hit Seeking in Drug Discovery

Program Chair: Matthew M. Hayward, Pfizer

Dr Peter Dandliker Merck

ALIS Affinity Selection in Pharmaceutical Discovery

Mr Erik LaChapelle Pfizer

Discovery of a Novel Mechanism for the Regulation of Apolipoprotein E

Dr Chris Davie GlaxoSmithKline

Application of Encoded Library Technology (ELT): From Library Design to the Clinic

Dr Gabe Simon Abide Therapeutics

Discovery and Development of Irreversible Inhibitors Targeting the Serine-hydrolase Superfamily

Thursday, January 29th 2015

Emerging Therapies for Hepatitis C

Program Chair: Philippe G. Nantermet, Merck

Dr Mark Bunnage Pfizer

H2L 2020

Dr Georgia McGaughey Vertex

Integrating Design, Analysis, and Visualization into the Phenotoypic Drug Discovery Workflow

Dr Scott Cowen AstraZeneca

From Old Targets to New, The Power of FBLG to Generate Novel Chemical Equity for Important Drug Targets

Dr Izzat Raheem Merck

Discovery of Novel PDE10 Inhibitors for the Treatment of Schizophrenia Enabled by Parallel Hit-to-Lead Efforts

KEYNOTE PRESENTATION

Program Chair: Professor Anthony GM Barrett

Professor Ben Cravatt The Scripps Research Institute

Activity-Based Proteomics – Applications for Enzyme and Inhibitor Discovery

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