Archived: 10th Winter Conference
on Medicinal & Bioorganic Chemistry

January 23rd - 27th 2011

Steamboat Springs Resort, Colorado


Sunday, January 23rd 2011

Strategies Towards Enabling the Bioavailability of Agents with Poor Physical Properties

Program Chair: Philippe G. Nantermet, Merck

Dr John Higgins Merck

A Survey of Drug Delivery and Solid State Chemistry Tools to Enhance and Control Drug Absorption

Dr Nair Rodriguez-Hornedo University of Michigan

Modifying Poor Physical Drug Properties Through the Use of Prodrugs and Cyclodextrins

Dr Valentino J. Stella University of Kansas

Modifying Poor Physical Drug Properties Through the Use of Prodrugs and Cyclodextrins

Dr Jennifer Riggs-Sauthier Nektar Therapeutics

Improving the Bioavailability of Small Molecule Drugs Through the Use of Nektar’s Advanced Polymer Conjugation Technology

Monday, January 24th 2011

Irreversible Inhibitors of P450 enzymes

Program Chair: Dan Flynn & Paul Pearson

Dr Paul Pearson Pearson Pharma Partners

Time Dependent Inactivation of Cytochrome P450: Mechanisms, Kinetics and Consequences

Dr Robert Walsky Pfizer

Experimental Assessment of Time Dependent Inhibition in Drug Discovery: Practical Considerations

Dr Jan Wahlstrom Amgen

Time Dependent Inhibition of Cytochrome P450: Implications in Drug Discovery

Dr Larry C. Wienkers Amgen

Identification of Reaction Pathways Associated with Mechanism-Based Inhibition of Cytochrome P450 3A4


Program Chair: John G. Allen

Dr Chris Ross John Hopkins University

Approaches to Therapeutics for Huntington’s Disease

Dr Wenge Zhong Amgen

Structure and Property Guided Discovery of Highly Efficacious Small Molecule Beta-secretase Inhibitors for Alzheimer’s Disease

Dr Celia Dominguez CHDI Management

Potential Therapeutic treatment for Huntington’s Disease

Dr Allen Reitz ALS Biopharma

Refolding Misfolded Proteins for the Discovery of New Therapeutics to Treat ALS

Tuesday, January 25th 2011


Program Chair: Victor Snieckus

Professor John Hartwig University of Illinois

Catalytic Transformations of Arenes

Dr Scott Schultz Merck

Harnessing High-Throughput Experimentation for Catalytic Reaction Development at Merck

Professor Tomas Hudlicky Brock University

Impact of Enzymatic Catalysis on Asymmetric Total Synthesis of natural Products and Pharmaceuticals: Dioxygenations, Reductions and N-demethylations

Dr Klaus Ditrich BASF SE

ChiPros®-Optically Active Intermediates on an Industrial Scale

Wednesday, January 26th 2011

General Oral Papers

Program Chair: Matt Hayward, Pfizer

Dr Matthew Hayward Pfizer

Welcome / Introduction

Dr Michael Brodney Pfizer

beta-Secretase Inhibitors for the Treatment of Alzheimer’s Disease: A Novel Class of Spirocyclic Sulfamides

Dr Scott Wolkenberg MercK

Catechol-O-methyltransferase (COMT) Inhibitors for the Treatment of Cognitive Impairment in Schizophrenia

Dr Mark Rosen Johnson & Johnson

Discovery of Prolyl 4-Hydroxylase Inhibitors that are Potent Oral Erythropoietin Secretagogues

Dr Jeremy Major Cellzome

The Discovery of Novel Gamma-Secretase Modulators for the Treatment of Alzheimer’s Disease

Dr Vadim Dudkin Merck

Discovery and Lead Optimization of Benzotriazole Series of mGlur2 Positive Allosteric Modulators for the Treatment of Schizophrenia.

Dr Chris Helal Pfizer

Application of Parallel Medicinal Chemistry Methods for the Rapid and Efficient Optimization of Hits-to-Leads-to-Clinical Candidates

Mr Sebastian Kroll Imperial College

The Synthesis and Evaluation of BS-194: a potent, oral bioavailable CDK-Inhibitor

Dr David Williams Indiana University

Studies of Marine Cytotoxins – Total Synthesis of Peloruside B

Dr Stanley Chamberlain Inhibitex Inc

INX-08189 A Novel Double Pro-Drug and Clinical Candidate for Hepatitis C Virus


Program Chair: Dr Bryan Norman, Eli Lilly

Joe Shih, Crown Bioscience Lilly Scholar, Eli Lilly & Co (retired)

The Evolution of Cancer Drug Discovery: From the Cytotoxic Paradigm to the Targeted Therapeutics, What Lessons Have We Learned?

Thursday, January 27th 2011


Program Chair: Joe Vacca, Merck

Dr Brian A. Johns GlaxoSmithKline

Discovery of the Next Generation HIV Integrase Inhibitor S/GSK1349572

Dr Arnaud Marchand CISTIM Leuvens

The LEDGINs: First in Class Antiviral Targeting the LEDGF/p75-IN Interaction

Dr Nicholas Meanwell BMS

Inhibitors of Hepatitis C Virus

Dr Pierre L. Beaulieu Boehringer Ingelheim

Discovery of BILB1941, a Non-Nucleoside NS5B Polmerase Inhibitor for the Treatment of Hepatitis C Virus Infection

Dr Michael Sofia Pharmasset

2’-α-F, 2’-β-C-Methyl Nucleotide Prodrugs for the Treatment of HCV Infection: From Discovery to the Clinic


Program Chair: Thomas Miller, Merck

Dr Thomas Miller Merck

Epigenetics: HDACs and Beyond

Dr Anthony Gangloff Takeda San Diego

Benzimidazole and Imidazole Inhibitors of Histone Deacetylases: Synthesis and Biological Activity

Dr Stephen Shuttleworth Karus Therapeutics

Design & Development of Novel Classes of HDAC Inhibitors for the Treatment of Immune-Inflammatory Diseases & Cancer

Dr Richard Chesworth Epizyme

The Chemical Biology of Histone Methyl Transferases

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