Opioid Receptor Ligands Modulating Side Effects
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Solution Overview
Problem
There is a need for new opioid receptor modulators with reduced side effects for the treatment of pain and associated disorders, as existing opioid analgesics often cause adverse effects such as nausea, vomiting, drowsiness, and lethargy, and are not effective for conditions like immune dysfunction, inflammation, and psychiatric disorders.
Innovation Solution
Development of opioid receptor ligands with specific chemical structures that act as agonists or antagonists, modulating opioid receptor activity to treat pain and related disorders, including the use of compounds with structures described in Formulas I to IX, which can be administered in pharmaceutical compositions to elicit therapeutic effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If morphine is administered to treat pain, then pain relief is achieved, but side effects such as nausea, vomiting, drowsiness, and lethargy occur
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of opioid compounds through systematic variation of substituents at specific positions (R1-R6) on the morphinan skeleton. This structural parameter optimization allows tuning of receptor selectivity and affinity, thereby maintaining analgesic effectiveness while reducing unwanted side effects by preferentially activating μ-receptors over other opioid receptor subtypes
Solution Approach 2:
The patent implements local quality by introducing specific substituent groups at defined positions on the molecular structure. Each substituent (e.g., fluorine at R3, methyl groups at R1 and R5) provides localized functional modifications that enhance receptor binding selectivity and affinity, thereby improving the therapeutic index by separating analgesic effects from side effect profiles
2Adaptability or versatility
If existing opioid analgesics are used, then pain relief is provided, but they are not effective for immune dysfunction, inflammation, and psychiatric disorders
Solution Approach 1:
The patent achieves universality by designing opioid compounds with enhanced multi-target activity. The optimized structures demonstrate ability to modulate not only pain pathways but also immune function, inflammatory responses, and psychiatric conditions, thereby providing a single therapeutic agent with broad-spectrum efficacy across multiple disease states
Data Source
AI summary
This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.