| Sunday, August 1, 1999 - Evening |
| 6:00-7:00 PM | Dinner | |
| 7:15-7:30 PM | Welcome and Orientation | |
Chemokine Receptor Antagonists
Jay Luly, Discussion Leader |
| 7:30 PM | Introduction and Overview | Jay Luly |
| 7:40 PM | Overview of Chemokine Biology | Craig Gerard |
| 8:05 PM | Discussion | |
| 8:15 PM | Development of Chemokine Receptor
Antagonists | Christine M. Tarby |
| 8:40 PM | Discussion | |
| 8:50 PM | Discovery and Evaluation of Small
Molecule CXCR2 Antagonists | Katherine Widdowson |
| 9:15 PM | Discussion | |
| 9:25 PM | Small Molecule Antagonists of the
CCR1 Chemokine Receptor: Therapeutic
Application | Richard Horuk |
| 9:50 PM | Discussion | |
| 10:00 PM | CLOSE | |
| Monday, August 2, 1999 - Morning |
New Opportunities in the Modulation of Lipids and the Treatment of Atherosclerosis
Scott Biller, Discussion Leader |
| 8:45 AM | Greetings and Announcements | |
| 9:00 AM | Introduction and Overview | Scott Biller |
| 9:05 AM | Intervention in Atherosclerosis - Targets
for the New Millennium | Peter Libby |
| 9:40 AM | Discussion | |
| 9:50 AM | Inhibition of CETP - A Novel Mechanism
for the Elevation of HDL Cholesterol | Hanno Wild |
| 10:20 AM | Discussion | |
| 10:30 AM | Coffee Break | |
| 10:50 AM | Discovery and Antiatherosclerotic
Activity of 15-Lipoxygenase Inhibitors | B.K. Trivedi |
| 11:15 AM | Discussion | |
| 11:25 AM | Dramatic Inhibition of Atherogenic
Lipoprotein Production by MTP Inhibitors | Scott Biller |
| 12:00 PM | Discussion | |
| 12:10 PM | CLOSE - LUNCH | |
| Monday, August 2, 1999 - Evening |
Intervention in Cell Cycle Regulation
Ellen Dobrusin, Discussion Leader |
| 7:30 PM | Introduction and Overview | Ellen Dobrusin |
| 7:40 PM | Cell Cycle Regulatory Events as Targets
for Drug Discovery | Edward Harlow |
| 8:05 PM | Discussion | |
| 8:15 PM | Novel Inhibitors of Cyclin-Dependent Kinase-2 (CDK2) | Phil Harris |
| 8:40 PM | Discussion | |
| 8:50 PM | Novel ATP Site Inhibitors of the Cyclin
Dependent Kinases | Wesley K.M. Chong |
| 9:15 PM | Discussion | |
| 9:25 PM | UCN-01: Pre-Clinical and Early
Clinical Studies | Edward A. Sausville |
| 9:50 PM | Discussion | |
| 10:00 PM | CLOSE | |
| Tuesday, August 3, 1999 - Morning |
Caspase Inhibitors
Robert Zamboni, Discussion Leader |
| 9:00 AM | Introduction and Overview | Robert Zamboni |
| 9:10 AM | Caspase Inhibitors as Novel Therapeutic
Agents for Inflammation and Apoptosis
Mediated Diseases | Winnie Wong |
| 9:40 AM | Discussion | |
| 9:50 AM | Inhibitors of Caspase 3 & 7 - Executioners of
Apoptosis | Dennis Lee |
| 10:20 AM | Discussion | |
| 10:30 AM | Coffee Break | |
| 10:50 AM | Solid Phase Synthesis of Selective
Caspase-3 Inhibitors | Erich Grimm |
| 11:20 AM | Discussion | |
| 11:30 AM | The Design of VX-740, a Potent
Inhibitor of IL-1 Beta Converting Enzyme | Mark Murcko |
| 12:00 PM | Discussion | |
| 12:10 PM | CLOSE - LUNCH | |
| Tuesday, August 3, 1999 - Evening |
Leukocyte Cell Adhesion
Terry Kelly, Discussion Leader |
| 7:30 PM | Introduction and Overview | Terry Kelly |
| 7:40 PM | The Role of Leukocyte Adhesion
Molecules in Health and Disease | T. Kei Kishimoto |
| 8:05 PM | Discussion | |
| 8:15 PM | Inhibitors of Integrin α4ß1 | Steven Adams |
| 8:40 PM | Discussion | |
| 8:50 PM | Biophysical Studies of CD11a and CD11b
I-Domain: Crystallography, Calorimetry
and Cations | Eric Baldwin |
| 9:15 PM | Discussion | |
| 9:25 PM | Small Molecule Antagonists of LFA-1
Mediated Cell Adhesion | Terry Kelly |
| 9:50 PM | Discussion | |
| 10:00 PM | CLOSE | |
| Wednesday, August 4, 1999 - Morning |
Alpha-1 Adrenergic Antagonists
Mark Bock, Discussion Leader |
| 9:00 AM | Introduction and Overview | Mark Bock |
| 9:10 AM | Benign Prostatic Hyperplasia:
Pathophysiology, Pharmacology,
and Therapeutic Targets | Theodore P. Broten |
| 9:40 AM | Discussion | |
| 9:50 AM | Alpha-1a Antagonist GG818 and
and QTc Prolongation | David Drewry |
| 10:20 AM | Discussion | |
| 10:30 AM | Coffee Break | |
| 10:50 AM | Pyrimidine-4-carboxamide Derivatives.
A Prototype Series of Functional
Uroselective Alpha-1 Antagonists for the
Treatment of Benign Prostatic Hypertrophy. | Pascal George |
| 11:20 AM | Discussion | |
| 11:30 AM | New Generation of Alpha-1a Selective
Antagonists for the Treatment of Benign
Prostatic Hyperplasia | Bharat Lagu |
| 12:00 PM | Discussion | |
| 12:10 PM | CLOSE - LUNCH | |
| 5:00-6:00 PM | Poster Session: Philip Hipskind, Poster Chair |
| Wednesday, August 4, 1999 - Evening |
Oral Bioavailability
Leo Herbette, Discussion Leader |
| 7:30 PM | Introduction and Overview | Leo Herbette |
| 7:40 PM | Oral Bioavailability - In Vitro Approaches | Mehran Yazdanian |
| 8:05 PM | Discussion | |
| 8:15 PM | Overview of Drug Membrane Interactions | Leo Herbette |
| 8:40 PM | Discussion | |
| 8:50 PM | Early Stage Pharmacokinetic and Physicochemical Screens in Support of Drug Discovery | Gary Caldwell |
| 9:15 PM | Discussion | |
| 9:25 PM | Lipid Bilayer Parameters: Theoretical
Considerations | Tony Hopfinger |
| 9:50 PM | Discussion | |
| 10:00 PM | CLOSE | |
| Thursday, August 5, 1999 - Morning |
Special Topics in Medicinal Chemistry
John Macor, Discussion Leader |
| 9:00 AM | From Concept to Clinic: Discovery of
CP-101,606, An NMDA Antagonist Selective
for Receptors Containing the NR2B Subunit | Bert Chenard |
| 9:30 AM | Discussion | |
| 9:45 AM | From Concept to Clinic: Discovery of
BMS-193884, A Potent and Selective
Endothelin Receptor (ETA) Antagonist | Joel Barrish |
| 10:15 AM | Discussion | |
| 10:30 AM | Break | |
| 10:45 AM | Discovery of TR-14035 - An Orally Active
Dual α4ß1/α4ß7 Small Molecule Integrin
Antagonist | Elias Lazarides |
| 11:15 AM | Discussion | |
| 11:30 AM | Design of p38 MAP Kinase Inhibitors for IL-1 and
TNS Mediated Diseases | Francesco Salituro |
| 12:00 PM | Discussion | |
| 12:15 PM | CLOSE - LUNCH | |
| 5:00-6:00 PM | Poster Session: Philip Hipskind, Poster Chair |
| Thursday, August 5, 1999 - Evening |
Special Lecture at the Invitation of the Chair
|
| 8:00 PM | Drug Discovery: The Path Forward | Gene Cordes |
