Mu Opioid Receptor Modulators

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes a new class of chemical compounds that specifically modulate the activity of the mu opioid receptor (MOR), which is a protein primarily responsible for the pain-relieving effects of traditional opioid drugs like morphine and fentanyl. These novel compounds are designed to activate MOR signaling mainly through the G protein pathway, but with minimal activation of the arrestin pathway. This signaling bias aims to preserve effective pain relief (analgesia) while significantly reducing common and dangerous side effects of opioids such as respiratory depression, constipation, and addiction. The patent also provides detailed methods for synthesizing these compounds and demonstrates their improved safety and efficacy in preclinical tests.

Use CasesContent extracted from patent full text and abstract with AI.

• Treatment of moderate to severe pain without the high risk of respiratory depression and constipation typically associated with opioids.
• Pharmaceutical development of safer painkillers for hospital, outpatient, or chronic use (e.g., post-surgical, cancer, neuropathic pain).
• Treatment and prevention of opioid overdose, potentially by acting as safer alternatives or assisting in withdrawal protocols.
• Management of opioid addiction by providing less-addictive pain relief options.
• Treatment of psychiatric disorders such as depression or anxiety when linked to or influenced by opioid receptor activity.

BenefitsContent extracted from patent full text and abstract with AI.

• Provides strong pain relief (analgesia) comparable to traditional opioids but with a significantly reduced risk of respiratory depression and constipation.
• Lower risk of dependence and addiction compared to conventional opioids like morphine, fentanyl, or heroin.
• Minimizes common opioid side effects, leading to improved patient safety and comfort.
• Enables new therapeutic approaches for pain management without the severe adverse outcomes that limit current opioid use.
• Could be used in populations where classic opioids are especially dangerous (e.g., elderly, those with respiratory conditions, or with history of substance abuse).
• The compounds are highly selective for mu opioid receptors with minimal activity at other opioid subtypes, reducing unwanted off-target effects.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.