Optimization of Physicochemical Properties of Pyridone-Based EP3 Receptor Antagonists
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2021)
Janssen Res & Dev LLC
Abstract
A novel series of pyridone-based EP3 receptor antagonists was optimized for good physical properties and oral bioavailability in rodents. The lead compounds 3h, 3l and 4d displayed good in vitro profiles, moderate to good metabolic stability and good rodent PK profiles with low clearance, high oral exposure and acceptable half-life.
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Key words
EP3,PGE2,Pyridone,Metabolic stability
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