Pyrrolidine Beta-3 Agonists for Overactive Bladder Treatment
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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 treatments that effectively manage urinary frequency, urgency, and incontinence.
Innovation Solution
Development of novel β3-adrenergic receptor (β3AR) agonists, specifically compounds of Formula I, which are used in pharmaceutical compositions to treat or prevent disorders mediated through β3AR, offering a new approach to relax bladder smooth muscle and address urinary disorders.
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 suboptimal and side effects occur
Solution Approach 1:
The patent applies parameter changes by developing novel chemical compounds with modified molecular structures (Formula I) that selectively target β3-adrenergic receptors. This structural parameter change in the therapeutic agent enables improved treatment effectiveness through selective relaxation of detrusor smooth muscle while minimizing side effects associated with non-selective therapies
2Ease of operation
If β3AR agonists are administered, then bladder smooth muscle relaxation is achieved, but potential side effects from receptor activation must be managed
Solution Approach 1:
The patent applies local quality by designing compounds that selectively activate β3-adrenergic receptors in specific tissues (detrusor smooth muscle, adipose tissue) while minimizing activation in other organs. This selective local action achieves effective bladder relaxation while reducing systemic side effects through tissue-specific receptor subtype targeting
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.


