Dication Compounds for Ultra-Short-Acting Muscle Relaxation
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Solution Overview
Problem
Current neuromuscular blockers, particularly non-depolarizing muscle relaxants, lack ultra-short-acting characteristics, necessitating the use of reversal agents that can increase medical procedures and safety uncertainties, and depolarizing agents like succinylcholine have severe side effects.
Innovation Solution
Development of bicationic compounds with a specific formula (I) that provide rapid, ultra-short-acting, and non-depolarizing muscle relaxation without the need for reversal agents, achieved through a multi-step synthesis process involving quaternary ammonium intermediates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If non-depolarizing muscle relaxants are used, then safety is improved, but duration of action is extended (cannot achieve ultra-short-acting)
Solution Approach 1:
The patent modifies the chemical structure of muscle relaxant compounds by introducing specific molecular features (formula I structure with particular substituents and stereochemistry) that alter the duration of action parameter while maintaining the non-depolarizing mechanism, achieving ultra-short-acting effects (onset <1 minute, duration 2-10 minutes) without compromising safety
Solution Approach 2:
The invention separates the desirable properties of depolarizing agents (ultra-short action) from non-depolarizing agents (safety) by creating a new class of compounds with specific structural characteristics that independently control duration of action, allowing the two properties to be optimized simultaneously
2Duration of action of moving object
If depolarizing muscle relaxant succinylcholine is used, then ultra-short-acting effect is achieved, but harmful side effects occur (elevated blood potassium, malignant hyperthermia, arrhythmia)
Solution Approach 1:
The patent converts the harmful depolarizing mechanism into a beneficial non-depolarizing mechanism while retaining the ultra-short-acting characteristic, effectively transforming a compound class with severe side effects into one that is both safe and ultra-short-acting through structural modification
Solution Approach 2:
By changing the chemical structure parameters and stereochemistry of the compounds (formula I with specific R groups and configurations), the patent alters the pharmacological profile to eliminate harmful side effects while preserving the rapid onset and short duration properties
3Reliability
If non-depolarizing muscle relaxants are used, then safety is improved, but additional medical procedures are required (reversal agents)
Solution Approach 1:
The patent creates muscle relaxant compounds that are self-limiting in their duration of action, automatically recovering within 2-10 minutes without requiring external reversal agents or additional medical interventions, thereby simplifying the medical procedure while maintaining safety
Data Source
AI summary
Provided are a dication compound, a preparation method therefor and use thereof, and specifically discloses a dication compound represented by formula (I), stereoisomers having the structure of formula (I) or a mixture of the stereoisomers, a pharmaceutically acceptable salt, a solvate, or a eutectic crystal, and a composition thereof, and use of a composition, being capable of producing neuromuscular junction retardation, formed of same with a pharmaceutically acceptable carrier in the field of preparation of a medicament for muscular flaccidity.