Quinoline derivatives which act as kappa-opioid receptor antagonists

Novel κ-opioid receptor antagonist compounds with improved pharmacokinetics and selectivity address the limitations of existing KOR antagonists, providing rapid and effective treatment for depression, anxiety, and substance abuse disorders.

HK40135118APending Publication Date: 2026-07-17THE SCRIPPS RES INST
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Patent Information

Authority / Receiving Office
HK · HK
Patent Type
Applications
Current Assignee / Owner
THE SCRIPPS RES INST
Filing Date
2026-05-07
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing kappa-opioid receptor (KOR) antagonists exhibit delayed onset of action, poor blood-brain barrier penetration, and inadequate pharmacokinetics, limiting their effectiveness in treating conditions such as depression, anxiety, and substance abuse disorders.

Method used

Development of novel κ-opioid receptor antagonist compounds, specifically quinoline derivatives of formula (I) and (II), with improved pharmacokinetics and selectivity for KOR over μ-opioid receptors, designed to address these limitations.

Benefits of technology

The novel compounds provide rapid and selective KOR antagonism, effectively treating a wide range of disorders including depression, anxiety, substance abuse, and sleep disturbances without adverse effects like somnolence, thereby offering a more effective therapeutic approach.

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Abstract

Disclosed herein are kappa-opioid receptor (KOR) antagonist compounds of Formula (I), Formula (II) and their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds are useful in methods of treating a variety of diseases and disorders adapted to KOR antagonism, including substance abuse disorders, depression, anxiety, and other psychiatric conditions.
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