Prodrugs of benzimidazol-1,2-YL amide compounds

Prodrug compounds of benzimidazol-1,2-yl amides address the solubility issues of Kv7.2/7.3 activators, enhancing their effectiveness for intravenous administration and treating conditions like status epilepticus by improving solubility and stability.

WO2026042005A1 Publication Date: 2026-02-26BIOHAVEN THERAPEUTICS LTD
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Patent Information

Application Number
PCT/IB2025/058358
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-18
Filing Date
2025-08-18
Publication Date
2026-02-26

AI Technical Summary

Technical Problem

Current Kv7.2/7.3 activators, such as benzimidazol-1,2-yl amides, have unsuitable aqueous solubility for intravenous, subcutaneous, or other parenteral formulations, limiting their effectiveness in treating conditions like status epilepticus.

Method used

Development of prodrug compounds of benzimidazol-1,2-yl amides with improved aqueous solubility and stability, which chemically or enzymatically release a pharmaceutically-active Kv7 activator for intravenous or parenteral administration.

Benefits of technology

The prodrugs enhance solubility and stability, enabling effective release of the active compound in plasma, thereby improving treatment efficacy for neurological disorders such as status epilepticus.

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Abstract

Provided for herein are prodrug compounds of benzimidazol-1,2-yl amide Kv7 activators. Particularly, the prodrug compounds have improved properties for stable formulation for treatment of Kv7 associated disorders, including seizure disorders. Also provided for are pharmaceutical compositions of said prodrug compounds and methods of treatment for seizure disorders including status epilepticus and others.
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