Patent review of novel compounds targeting opioid use disorder (2018-2024)

Opioids have served as a cornerstone in pain management for decades. However, the emergence of increasingly potent synthetic analogs brings forth a range of side effects, including respiratory depression, tolerance, dependence, constipation, and, more importantly, the development of severe and debilitating opioid use disorder (OUD). Search for therapeutics to mitigate OUD has been challenging, and this has called for novel approaches that include the design of small molecules targeting neuronal circuits involved in addiction (opioid, dopamine, serotonin, norepinephrine, and glutamate receptors, etc.).

In this review, we retrieve and discuss two dozen (24) relevant patents filed in the past six (6) years that focus on novel small-molecule therapeutics for OUD. The chemical entities disclosed were highlighted, and specific examples were provided where necessary.

Several chemical entities targeting both opioid and non-opioid targets are under consideration for treating OUD. Our search for patents covering such compounds revealed embodiments with diverse chemistry. Understanding the public impact of OUD and the rapidly evolving landscape of substance abuse underscores the urgent need for a thorough reevaluation of strategies to address these challenges. This includes the development of small molecules with unique mechanisms of action for OUD treatment.