Archived Content

Mastering Medicinal Chemistry 

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Wednesday, February 22

7:55 am Chairperson's Remarks

Nicholas A. Meanwell, Ph.D., Executive Director, Medicinal Chemistry, Bristol-Myers Squibb Research & Development

KEYNOTE PRESENTATION

8:00 Hepatitis C Virus NS5A Replication Complex Inhibitors

Nicholas MeanwellNicholas A. Meanwell, Ph.D., Executive Director, Medicinal Chemistry, Bristol-Myers Squibb Research & Development

This presentation will provide an overview of the discovery and development of the hepatitis C virus (HCV) NS5A replication complex inhibitor BMS-790052, a first-in-class therapeutic for the treatment of HCV.


 

 

NOVEL STRATEGIES & APPLICATIONS IN MEDICINAL CHEMISTRY

8:30 Antibody-Drug-Conjugates (ADCs) for the Treatment of Cancer

John A. Flygare, Ph.D., Senior Scientist, Discovery Chemistry, Genentech, Inc.

Successful Antibody-Drug-Conjugates (ADCs) require assembling the correct combination of antibody, linker , and cytotoxic drug.  This presentation will review successful applications of this technology and discuss future directions of the linkers and cytotoxic drugs used in this approach.

9:00 Accessing New Chemical Space through Flow-Enabled "Forbidden" Chemistries

Neal Sach, Ph.D., Senior Principal Scientist, Oncology Medicinal Chemistry, Pfizer

A flow technology is presented with the capability to run and analyze 100-300 reactions per day. The application of this technology in accessing new chemical space in drug discovery is presented, with examples of chemistries, traditionally considered 'forbidden' in batch, exemplified.

Sponsored byIntelligent Pharma9:30 Drug Design and Development by Molecular Interaction FieldsJascha Blobel, Ph.D., Product Manager, Intelligent PharmaMolecular interaction fields are the key property of a molecule in binding to different receptors in the cell. Thanks to the constantly growing information about molecules and their associated functions in biological systems, Intelligent Pharma will present the use of comparing molecules on basis of their interaction fields to predict the functions of new and unknown molecules.

10:00 Transition to Plenary Keynote

 

PLENARY KEYNOTE SESSION 

10:10 Plenary Keynote Presentation  

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11:00  Refreshment Break in the Exhibit Hall with Poster Viewing

12:00 pm Using Chemical Biology to Increase Biochemical Understanding that Enables Therapeutic Intervention

Lyn H. Jones, Ph.D., FRSC, Senior Director & Head, Chemical Biology and Orphan & Genetics Diseases, WorldWide Medicinal Chemistry, Pfizer

The pharmaceutical industry is plagued by a low return on its investment in research and development. Successful applications of chemical biology in the drug discovery setting will be presented to illustrate a new paradigm for medicinal chemistry design at the interface with biology.

12:30 Chemical Proteomics: Applications to Compound Profiling and Target Discovery

Robert W. Johnson, Ph.D., Senior Group Leader, Structural Chemistry - Advanced Technology, Abbott Laboratories

1:00 Luncheon Presentations (Sponsorship Opportunities Available) or Lunch on Your Own

2:00 Ice Cream Refreshment Break in the Exhibit Hall with Poster Viewing 

 

PLENARY KEYNOTE SESSION 

2:30 Plenary Keynote Panel  

3:50 Refreshment Break & Poster Awards in the Exhibit Hall

 

HOT TARGETS TO WATCH: ALLOSTERIC MODULATORS

4:25 Chairperson's Remarks

Sylvain Célanire, Group Leader, Medicinal Chemistry Section, Addex Pharmaceuticals

KEYNOTE PRESENTATION

4:30 Optimization of Allosteric Modulators of GPCRs for Treatment of CNS Disorders

Jeffrey ConnP. Jeffrey Conn, Ph.D., Lee E. Limbird Professor of Pharmacology; Director, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center

Allosteric modulators of GPCRs exhibit multiple modes of efficacy that dramatically impact in vivo effects.  This new understanding provides important insights to guide medicinal chemistry efforts aimed at developing allosteric modulators that are suitable as drug candidates.
 

 

5:00 Positive Allosteric Modulation of α4β2 Neuronal Nicotinic Receptors: An Approach for Improving the Therapeutic Index of ABT-594 in the Treatment of PainMichael R. Schrimpf, Ph.D., Senior Chemistry Group Leader, Neurological Urological, Abbott LabsThe α4β2 nicotinic agonist ABT-594 demonstrated efficacy in diabetic neuropathic pain patients but had tolerability issues attributable to activity at the α3β4 subtype.  A strategy for improving the therapeutic index by co-dosing with a selective α4β2 PAM will be described.

5:30 A Drug Discovery Journey across Allosteric Modulators of Metabotropic Glutamate Receptors: from Hit to Candidate

Sylvain Célanire, Group Leader, Medicinal Chemistry Section, Addex Pharmaceuticals

Glutamate is the major excitatory neurotransmitter in the brain. It mediates its actions via the activation of both ligand gated ion channels (iGluRs) and a family of class C G-Protein Coupled Receptors known as metabotropic Glutamate Receptors (mGluRs). mGluRs play important roles in various neurological and other disorders. Individual members of mGluR family have been difficult to target selectively using conventional approaches. This is due to the high degree of conservation of the active sites of these receptors. Allosteric binding sites, however are topographically distinct from the orthosteric binding site (active site) and are less conserved within the 8-member mGluR family. As a result, allosteric modulators offer a valid strategy for developing highly selective oral small molecule therapeutics that can readily cross blood-brain barrier against each of these historically undruggable targets. Allosteric modulators represent therefore an emerging and highly attractive class of novel small molecule therapeutics to address undruggable targets for the treatment of severe CNS, metabolic, inflammatory and other disorders. Discovery and characterization of novel allosteric modulators of Class C GPCRs mGluR2, mGluR4 and mGluR5 will be presented, including extensive structure-activity and structure-property relationship studies.

HOT TARGETS IN CANCER: KINASES

6:00 Linsitinib (OSI-906), a Potent and Highly Selective Dual Inhibitor of IGF-1R and IR Currently Undergoing Clinical Testing in a Phase III Clinical Trial in ACC Patients

Mark J. Mulvihill, Ph.D., Director of Chemistry, Oncology, OSI Pharmaceuticals LLC, a subsidiary of Astellas USAdrenocortical carcinoma (ACC) is a rare and aggressive cancer of the adrenal glands. Mitotane is the only approved drug for ACC, however, its efficacy is limited (5-30% response rates) and it causes significant neurological, gastrointestinal and endocrinological toxicities, highlighting the need for safer and more effective therapies. The insulin-like growth factor receptor (IGF-1R) is a receptor tyrosine kinase implicated as a key driver of tumor growth and survival in several hematologic and solid cancers, including ACC. Over 90% of ACC tumors overexpress IGF-2, an activating ligand for both IGF-1R and IR. Our drug discovery efforts, including structure-based design and empirical medicinal chemistry efforts have resulted in the discovery of OSI-906, a potent, selective and orally available inhibitor of both IGF-1R and IR. In addition to its activity in preclinical models, OSI-906 has recently shown preliminary activity in ACC patients and is currently in a Phase III clinical trial in ACC.

6:30 Close of Day



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