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Updated: Jun 5, 2025

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Development of dual V1a/V2 antagonists containing triazolobenzazepine scaffold
Gábor Varró1, Éva Bozó1, Krisztina Vukics1
1Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary.
Abstract:
The development of a dual V1a/V2 antagonist compound is a complex and challenging task. Conivaptan is up to now the only known V1a/V2 antagonist which was approved for the treatment of euvolemic hyponatremia. Previously, we reported RGH-122, a novel selective V1a antagonist compound. Herein, we describe several promising dual antagonist compounds, which are derived from RGH-122 by using modifications in its tail region. These modifications can result in excellent binding affinity on both V1a and V2 receptors.
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