Bifunctional Hydroxyquinolinone Compounds for Dual Receptor Bronchodilation
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Solution Overview
Problem
Current treatments for pulmonary disorders like asthma and COPD often require combinations of beta-2 adrenergic receptor agonists and muscarinic receptor antagonists, which can have limitations in terms of pharmacokinetics and efficacy, particularly in providing long-lasting bronchodilation.
Innovation Solution
Development of phenyl hydroxyacetic ester derivatives that act as both muscarinic receptor antagonists and beta-2 adrenergic receptor agonists, offering elevated affinity for M3 muscarinic receptors and prolonged bronchodilating activity, potentially simplifying treatment by combining both mechanisms in a single molecule.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If combination therapy with beta-2 agonists and muscarinic antagonists is used, then bronchodilation efficacy is improved, but treatment complexity and pharmacokinetic management worsen
Solution Approach 1:
The patent merges two separate pharmacological agents (beta-2 agonist and muscarinic antagonist) into a single bifunctional molecule that contains both activity centers. This single molecule can simultaneously activate beta-2 receptors and block muscarinic receptors, providing the therapeutic benefits of combination therapy while simplifying administration to a single inhalation dose.
Solution Approach 2:
The invention creates a universal bronchodilator molecule that performs multiple functions: it acts as both a beta-2 adrenergic receptor agonist and a muscarinic receptor antagonist. This multi-functional molecule addresses multiple pathological mechanisms in asthma and COPD simultaneously, improving efficacy while reducing treatment complexity.
2Duration of action of moving object
If short-acting bronchodilators are administered frequently, then bronchodilation coverage is improved, but patient compliance and convenience worsen
Solution Approach 1:
The bifunctional compound provides prolonged bronchodilation action that maintains therapeutic effect over an extended period. By designing the molecule with appropriate pharmacokinetic properties, the drug achieves continuous useful action throughout the dosing interval, reducing the frequency of administration and improving patient convenience.
3Reliability
If combination of separate beta-2 agonist and muscarinic antagonist molecules is used, then dual mechanism action is achieved, but pharmacokinetic variability increases
Solution Approach 1:
The patent combines two separate molecules into one unified bifunctional molecule. This ensures that both the beta-2 agonist and muscarinic antagonist activities are delivered simultaneously in fixed stoichiometric proportions, eliminating pharmacokinetic variability between separate formulations and ensuring consistent dual mechanism action in every dose.
Data Source
AI summary
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmaceutical active ingredients.