Quinoline derivatives which act as kappa-opioid receptor antagonists
Novel κ-opioid receptor antagonist compounds, particularly quinoline derivatives, address the limitations of existing KOR antagonists by providing rapid and selective KOR antagonism, effectively treating depression, anxiety, and substance abuse disorders through enhanced dopamine regulation and sleep normalization.
Patent Information
- Application Number
- HK62026123000
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-08-18
- Filing Date
- 2026-05-07
- Publication Date
- 2026-07-17
- Estimated Expiration
- 2044-02-15
AI Technical Summary
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.
Development of novel κ-opioid receptor antagonist compounds, specifically quinoline derivatives of formula (I) and (II), with improved selectivity and potency, designed to rapidly and effectively target KORs, thereby regulating downstream signaling pathways to treat various disorders.
The novel compounds provide rapid therapeutic effects on disorders like depression, anxiety, and substance abuse by selectively antagonizing KORs, enhancing dopamine function, normalizing sleep disturbances, and reducing stress-induced neuroadaptation, without causing somnolence.