Pyrrolidine Beta-3 Agonists for Overactive Bladder
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Solution Overview
Problem
Current medical therapies for overactive bladder are suboptimal, as many patients do not respond adequately or tolerate side effects, highlighting a need for new, well-tolerated treatments that effectively manage urinary frequency, urgency, and incontinence.
Innovation Solution
Development of novel β3-adrenergic receptor (β3AR) agonists and their pharmaceutical compositions for treating urinary disorders, specifically designed to relax bladder smooth muscle and address pathogenic states like overactive bladder.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current medical therapies for overactive bladder are used, then treatment coverage is provided, but treatment effectiveness is insufficient and side effects occur
Solution Approach 1:
The patent develops novel beta-3 adrenergic receptor agonists with optimized molecular structures (Formula I) that selectively target beta-3 receptors in the bladder. By changing the chemical parameters and receptor selectivity, the new compounds achieve superior treatment effectiveness for overactive bladder while minimizing side effects compared to existing therapies.
2Stress or pressure
If beta-3 adrenergic receptor agonists are administered, then bladder pressure is reduced and bladder capacity is increased, but residual urine volume may increase
Solution Approach 1:
The patent designs beta-3 adrenergic receptor agonists with high local selectivity for bladder tissue. The compounds preferentially bind to beta-3 receptors in the detrusor muscle, producing localized relaxation and pressure reduction without systemic effects that would cause urinary retention or increased residual volume.
3Reliability
If new beta-3 adrenergic receptor agonists are developed, then treatment efficacy is improved, but drug development complexity increases
Solution Approach 1:
The patent presents a series of compounds with systematically varied molecular structures (Formula I with different substituents R1-R6, m-n-p-q values). This segmented approach allows optimization of specific properties (efficacy, selectivity, pharmacokinetics) by modifying individual structural parameters while maintaining the core beta-3 agonist framework.
Data Source
AI summary
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.