Archived: 10th Winter Conference
on Medicinal & Bioorganic Chemistry
January 23rd - 27th 2011
Steamboat Springs Resort, Colorado
Agenda
Sunday, January 23rd 2011
Strategies Towards Enabling the Bioavailability of Agents with Poor Physical Properties
Program Chair: Philippe G. Nantermet, Merck
A Survey of Drug Delivery and Solid State Chemistry Tools to Enhance and Control Drug Absorption
Modifying Poor Physical Drug Properties Through the Use of Prodrugs and Cyclodextrins
Modifying Poor Physical Drug Properties Through the Use of Prodrugs and Cyclodextrins
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
Time Dependent Inactivation of Cytochrome P450: Mechanisms, Kinetics and Consequences
Experimental Assessment of Time Dependent Inhibition in Drug Discovery: Practical Considerations
Time Dependent Inhibition of Cytochrome P450: Implications in Drug Discovery
Identification of Reaction Pathways Associated with Mechanism-Based Inhibition of Cytochrome P450 3A4
Neurodegeneration
Program Chair: John G. Allen
Approaches to Therapeutics for Huntington’s Disease
Structure and Property Guided Discovery of Highly Efficacious Small Molecule Beta-secretase Inhibitors for Alzheimer’s Disease
Potential Therapeutic treatment for Huntington’s Disease
Refolding Misfolded Proteins for the Discovery of New Therapeutics to Treat ALS
Tuesday, January 25th 2011
Catalysis
Program Chair: Victor Snieckus
Catalytic Transformations of Arenes
Harnessing High-Throughput Experimentation for Catalytic Reaction Development at Merck
Impact of Enzymatic Catalysis on Asymmetric Total Synthesis of natural Products and Pharmaceuticals: Dioxygenations, Reductions and N-demethylations
ChiPros®-Optically Active Intermediates on an Industrial Scale
Wednesday, January 26th 2011
General Oral Papers
Program Chair: Matt Hayward, Pfizer
Welcome / Introduction
beta-Secretase Inhibitors for the Treatment of Alzheimer’s Disease: A Novel Class of Spirocyclic Sulfamides
Catechol-O-methyltransferase (COMT) Inhibitors for the Treatment of Cognitive Impairment in Schizophrenia
Discovery of Prolyl 4-Hydroxylase Inhibitors that are Potent Oral Erythropoietin Secretagogues
The Discovery of Novel Gamma-Secretase Modulators for the Treatment of Alzheimer’s Disease
Discovery and Lead Optimization of Benzotriazole Series of mGlur2 Positive Allosteric Modulators for the Treatment of Schizophrenia.
Application of Parallel Medicinal Chemistry Methods for the Rapid and Efficient Optimization of Hits-to-Leads-to-Clinical Candidates
The Synthesis and Evaluation of BS-194: a potent, oral bioavailable CDK-Inhibitor
Studies of Marine Cytotoxins – Total Synthesis of Peloruside B
INX-08189 A Novel Double Pro-Drug and Clinical Candidate for Hepatitis C Virus
KEYNOTE PRESENTATION
Program Chair: Dr Bryan Norman, Eli Lilly
The Evolution of Cancer Drug Discovery: From the Cytotoxic Paradigm to the Targeted Therapeutics, What Lessons Have We Learned?
Thursday, January 27th 2011
Antivirals
Program Chair: Joe Vacca, Merck
Discovery of the Next Generation HIV Integrase Inhibitor S/GSK1349572
The LEDGINs: First in Class Antiviral Targeting the LEDGF/p75-IN Interaction
Inhibitors of Hepatitis C Virus
Discovery of BILB1941, a Non-Nucleoside NS5B Polmerase Inhibitor for the Treatment of Hepatitis C Virus Infection
2’-α-F, 2’-β-C-Methyl Nucleotide Prodrugs for the Treatment of HCV Infection: From Discovery to the Clinic
Epigenetics
Program Chair: Thomas Miller, Merck
Epigenetics: HDACs and Beyond
Benzimidazole and Imidazole Inhibitors of Histone Deacetylases: Synthesis and Biological Activity
Design & Development of Novel Classes of HDAC Inhibitors for the Treatment of Immune-Inflammatory Diseases & Cancer
The Chemical Biology of Histone Methyl Transferases
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