14th Winter Conference – Provisional
on Medicinal & Bioorganic Chemistry

January 27th - 31st 2019

Steamboat Springs Resort, Colorado

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Agenda

Sunday, January 27th 2019

Drug Hunting

Program Chair: Dr Daniel Flynn, Deciphera Pharmaceuticals

Dr Petr Vachal Merck

The Invention of MK-8262, a CETP Inhibitor Backup to Anacetrapib (with best in class properties)

Dr Kevin Freeman-Cook Pfizer

Targeting the Cell Cycle for the Treatment of Cancer

Dr Sandra Filla Eli Lilly

Lasmiditan: The Long Road Home for a Novel Therapy for Acute Migraine Treatment

Dr Josh Bilenker LOXO (Drug Hunter Award)

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

Dr Jared Cumming Merck

Novel STING Agonists for Immuno-oncology

Dr Paul Scola BMS

Discovery of a Macrocyclic Peptide Inhibitor of Programmed Death-Ligand 1 (PD-L1)

Dr Cynthia Parrish GSK

Targeting the Adenosine Pathway with Non-Nucleoside Inhibitors of CD73

Dr Brendan Parr Genentech

Design of Selective, Heme-binding Inhibitors of Tryptophan-2,3-dioxygenase (TDO)

Structural and in-Silico Chemistry

Program Chair: Dr Georgia McGaughey, Vertex

Dr Meihua Tu Pfizer

The Role of Water Molecule in Ketohexokinase Inhibitor Design

Dr Yuan Wang Novartis

Computational Methods Help Find Chemical Matter to Uncover Novel Biology

Dr Clara Christ Bayer

Five years of Binding Free Energy Calculations at Bayer: Impact and Future Directions

Dr Ed Sherer Merck

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

Professor Laura Kiessling MIT

Glycans in Health and Disease

Professor Christina Woo Harvard

Mapping Binding Site Hotspots in the Global Proteome by Photo-affinity Labeling Mass Spectrometry

Dr Ron Tomlinson AstraZeneca

Chemical Degraders for Target Validation: Revealing Biology on the Oncogenic Transcription Factor BCL6

Dr Andy Phillips C4 Therapeutics

Targeted Protein Degradation

Potential New Therapies for the Treatment of Chronic Pain

Program Chair: Dr Sarah Skerratt, Vertex

Dr Sarah Skerratt Vertex

Overview of Current Therapies for the Treatment of Pain

Dr Mark Layton Merck

Breathe Easy: Mechanistic Insights Enable a Path Forward for Highly Selective Nav1.7 Inhibitors

Professor Laura Bohn Scripps

Harnessing Opioid Receptor Signaling to Improve Pain Therapeutics

Dr Brendan Crowley Merck

Discovery And Optimization Of A Novel CGRP Receptor Antagonist Chemotype For The Treatment of Migraine

Dr Leena Otsomaa Orion

TRPA1: A Pain Target or a Painful Target?

Dr Steven McKerrall Genentech

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)

Professor Jay Debnath UCSF

Complexities of Targeting Autophagy to Treat Human Disease

Professor Kevan Shokat UCSF

Targeting the Autophagy-Initiating Kinase ULK1

Professor Martin McMahon University of Utah

Combined Targeting of MAP Kinase Signalling and Autophagy for the Future Therapy of Cancers Driven by the RAS Pathway

Professors Ravi Amaravadi & Jeffrey Winkler University of Pennsylvania

Advances in Targeting Lysosomotrophic Agents

Advances in Synthesis and Medicinal Chemistry

Program Chair: Professor Darren Dixon, University of Oxford

Professor Darren Dixon University of Oxford

New Broad Scope Strategies for Amine Synthesis

Dr Dominic Reynolds H3 Biomedicine

Discovery of H3B-8800, A Novel, Orally Bioavailable, Small Molecule, Splice Modulator

Professor James Barrow Lieber Institute for Brain Development

Discovery of Novel Treatments for Visceral Pain via GABA Signaling

Dr Zhi-Cai Shi Merck

Enabling the Application of Photoredox Catalysis in Medicinal Chemistry

Please submit an abstract for consideration See the Submissions Tab under Registration above or click link below:

https://www.eventsforce.net/su/frontend/reg/tAbsSubmitterLogin.csp?pageID=46882&eventID=134

Thursday, January 31st 2019

Photoredox Catalysis

Program Chair: Dr Dan DiRocco, Merck

Dr Dani Schultz Merck

Recent Advances in the Remote Functionalization of Aliphatic C-H Bonds via Decatungstate Photocatalysis

Dr Thomas Knauber Pfizer

Enablement of Photoredox Csp2-Csp3 Cross Coupling Reactions

Dr Kaid Harper Abbvie

Scaling Catalytic Photochemistry with Lasers

Professor Corey Stephenson University of Michigan

Photoredox Catalysis – An Enabling Platform for Discovery and Development

Professor Tomislav Rovis University of Columbia

New Tools for Catalysis

KEY NOTE PRESENTATION

Program Chair: Professor Victor Snieckus, Queen's University

5.00 - 6.00pm
Professor Phil S. Baran The Scripps Research Institute

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 (includes boxed Lunch) & Wednesday 30th January 2019: 12.00 – 4.00 pm (includes boxed lunch) – prices below.

Course Description

The discovery of new therapeutic agents is met with significant challenges in preclinical discovery and development.  Both efficacy and safety endpoints must be adequately assessed prior to testing a new investigational agent in humans.  Perhaps the most challenging part of drug discovery is the mitigation of safety risks that arise during most drug discovery optimization efforts.  Successful drug discovery teams will properly design and execute experiments that can best assess and discharge risks prior to first human dose (FHD), in the context of anticipated human drug exposures.  This course highlights the important role that medicinal chemists play in identifying, understanding and mitigating common preclinical safety risks.  Information regarding best practices for avoidance and early detection of common toxicology issues will also be discussed.  Finally, the course will describe some of the common pitfalls in toxicological data interpretation and how to best use the data to inform a lead optimization strategy to deliver safe small molecule drug candidates.

Who should attend?

While the focus is on medicinal chemistry methods, this course will benefit all scientists who participate in the cross functional execution of drug discovery programs.  Medicinal chemists, toxicologists, biologists, pharmacologists, pharmacokineticists and program managers will all gain valuable insights into modern preclinical safety assessment strategies.

Course Content Highlights

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery–Part 1 (4 hrs) – Tuesday 29th January 2019, 12.00 – 4.00 pm (includes boxed lunch)

  • Principles of Toxicology and Safety Assessment
  • The Investigational New Drug (IND) Application
  • Target Assessment, Predictive Toxicology and In Silico Methods
  • Preferred Drug Properties to Minimize Toxicological Risks
  • Safety Assessment and Flow Scheme Design in Lead Optimization
  • Case Studies and Problem Sessions

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery–Part 2 (4 hrs) Wednesday 30th January 2019, 12.00 – 4.00 pm (includes boxed lunch)

  • Drug Metabolism and Bioactivation
  • Toxicophores and Structure Alerts
  • Mechanisms and mitigation strategies for Drug Induced Liver Injury (DILI)
  • Mitigating Common Off-Target Safety Concerns
  • Clinical Candidate Selection and FHD Enablement
  • Case Studies and Problem Sessions

Instructor Biography 

Bryan H. Norman received his Ph.D. at Emory University and was an NIH Postdoctoral Fellow at Penn State University.  After three years at Monsanto/Searle, Bryan joined Eli Lilly and Company in 1993, where he led multiple cross functional drug discovery efforts, many of which culminated in clinical candidates for oncology, endocrine and pain indications.  In addition to his expertise in medicinal chemistry, Bryan has significant cross functional drug discovery experience and expertise in additional disciplines, such as biomarkers, pharmacokinetic/pharmacodynamic (PK/PD) relationships, mechanisms of drug metabolism and toxicology.  He has specific expertise in the mechanisms and mitigation strategies to avoid drug-induced liver injury (DILI).  The breadth of his background has led to his service on many Due Diligence teams to assess potential in-license opportunities.  Bryan is a Volume Editor and serves on the Editorial Board of Burger’s Medicinal Chemistry, Drug Discovery and Development.  He is currently on the Board of Directors of the Medicinal and Bioorganic Chemistry Foundation and serves on various grant review committees.  He has published over 45 papers in peer-reviewed scientific journals and given many invited lectures at scientific conferences and universities.  His most recent research interests have focused on the identification of mechanisms associated with drug-induced liver injury and the discovery of novel analgesic agents for use in chronic pain.  He is currently an independent medicinal chemistry consultant and drug discovery course instructor.

Prices:

Industrial/Academic rates of $500/$300 (for both days)
Industrial/Academic rates of $275/$175 (for one day)

Please book your place or places when you book to attend the conference.

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