Beta-3 Adrenergic Receptor 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 treatments that effectively manage urinary frequency, urgency, and incontinence.
Innovation Solution
Development of novel β3-adrenoceptor agonist compounds, specifically defined by Formula I or their pharmaceutically acceptable salts, which are administered to relax bladder smooth muscle and treat disorders mediated through β3-adrenoceptors.
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 β3-adrenoceptor agonist compounds with optimized molecular structures (Formula I) that enhance therapeutic effectiveness while reducing side effects. The chemical parameters of the compounds are systematically modified to improve selectivity for β3AR over other adrenergic receptors, thereby increasing treatment reliability and reducing harmful effects on other physiological systems.
Solution Approach 2:
The patent employs the copying principle by creating new compounds that replicate and enhance the beneficial effects of existing β3AR agonists (such as mirabegron) while eliminating their limitations. The novel compounds copy the successful mechanism of β3AR-mediated detrusor relaxation but with improved pharmacological properties through structural optimization.
2Adaptability or versatility
If many patients do not respond adequately to current treatments, then treatment coverage is reduced, but the need for alternative therapies increases
Solution Approach 1:
The patent applies universality by developing β3AR agonist compounds that can effectively treat multiple manifestations of overactive bladder syndrome (urgency, frequency, incontinence) through a single mechanism. The compounds provide broad therapeutic coverage by targeting the underlying pathophysiology of detrusor overactivity, making them applicable to diverse patient populations with varying symptom profiles.
3Ease of operation
If patients are unable to tolerate current treatments, then treatment accessibility is reduced, but the need for better-tolerated therapies increases
Solution Approach 1:
The patent converts the potential harm of off-target adrenergic receptor activation into benefit by designing compounds with high selectivity for β3AR. This selectivity prevents activation of β1AR (which could cause cardiac side effects) and β2AR (which could cause bronchial relaxation), thereby improving tolerability while maintaining or enhancing therapeutic efficacy through targeted β3AR-mediated detrusor relaxation.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The β3-adrenoceptor agonist compounds provide effective relaxation of the detrusor muscle, reducing bladder pressure, increasing bladder capacity, and prolonging micturition intervals without increasing residual urine volume, thus addressing the symptoms of overactive bladder.
Implementation Method 1
β3-adrenoceptor agonist compounds, specifically defined by Formula I or their pharmaceutically acceptable salts, which are administered to relax bladder smooth muscle
Implementation Method 2
Agents that relax bladder smooth muscle, such as β3AR agonists, are expected to be effective for treating such urinary disorders
Data Source
AI summary
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.