Polycyclic Amines as Opioid Receptor Modulators
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Solution Overview
Problem
There is a need for new opioid receptor modulators that can effectively manage various conditions such as pain, migraines, depression, cognitive disorders, and other diseases with reduced side effects, as existing treatments often have limitations in efficacy and safety.
Innovation Solution
Development of polycyclic amines and their pharmaceutically acceptable salts, which can modulate opioid receptors, offering therapeutic benefits for a wide range of conditions including pain management, mental health issues, and neurological disorders, through administration in various pharmaceutical compositions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing opioid receptor modulators are used for pain management and other conditions, then therapeutic effects are achieved, but side effects increase
Solution Approach 1:
The patent modifies the chemical structure of opioid receptor modulators by changing parameters such as the introduction of specific substituents (e.g., fluorine atoms at positions 6 and 8, various R1-R6 groups), molecular weight, and lipophilicity. These parameter changes result in compounds with improved therapeutic profiles that maintain efficacy while reducing side effects like respiratory depression and constipation.
Solution Approach 2:
The patent creates composite molecular structures combining multiple functional groups and heterocyclic systems (e.g., fused ring systems, heteroaryl groups) into single opioid receptor modulator molecules. These composite structures enable selective receptor binding with enhanced therapeutic effects and reduced adverse reactions compared to simpler analogs.
2Adaptability or versatility
If existing opioid receptor modulators are administered for various conditions, then treatment benefits are obtained, but treatment limitations persist
Solution Approach 1:
The patent develops opioid receptor modulators with broad therapeutic applicability across multiple conditions including pain management, migraine, depression, cognitive disorders, Parkinson's disease, and gastrointestinal disorders. The compounds exhibit multi-functionality by acting on different receptor subtypes (mu, delta, kappa) and signaling pathways, enabling treatment of diverse conditions with a single agent or limited set of agents.
Data Source
AI summary
The present invention discloses a number of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.