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Updated: Apr 20, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
N-Aryl azacycles as novel sodium channel blockers
Stephen M Lynch1, Laykea Tafesse1, Kevin Carlin1
1Discovery Research, Purdue Pharma L.P., 6 Cedarbrook Drive, Cranbury, NJ 08512, United States.
Abstract:
We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and electrophysiological functional assays. Analogs from this series possessed selectivity over hERG, reasonable oral exposure in rat PK studies and are predicted to have limited CNS penetration.
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