Quinazoline BKCa Activator for Overactive Bladder
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Solution Overview
Problem
Current therapeutic agents for overactive bladder often come with side effects such as dry mouth, dizziness, and urinary retention, indicating a need for more effective and less harmful treatments that can improve bladder capacity and reduce excessive phasic contractions.
Innovation Solution
A pharmaceutical composition containing a novel quinazoline-based compound that activates BKCa channels, inducing relaxation of bladder smooth muscles and preventing excessive contractions, thereby addressing the limitations of existing treatments.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antimuscarinic agents are used to treat overactive bladder, then bladder capacity is increased and bladder contraction is inhibited, but side effects such as dry mouth, drowsiness, constipation, dizziness, and dry eyes occur
Solution Approach 1:
The patent applies parameter changes by developing a novel chemical compound with modified molecular structure (Formula 1 with specific substituents) that alters the pharmacological parameters of action. The compound maintains therapeutic efficacy through selective BKCa channel activation while changing the side effect profile by avoiding muscarinic receptor blockade, thus resolving the contradiction between treatment efficacy and side effects
Solution Approach 2:
The patent introduces an intermediary mechanism by using BKCa channel activation as a new pathway mediating bladder relaxation. Instead of directly blocking acetylcholine receptors (antimuscarinic mechanism), the compound acts through BKCa channels as an intermediary, producing smooth muscle relaxation through a different physiological pathway that avoids the side effects associated with traditional antimuscarinic action
2Reliability
If beta-3 agonists are used to relax the bladder, then overactive bladder is treated, but side effects such as urinary retention, urethral infection, and hypertension occur
Solution Approach 1:
The patent applies parameter changes by shifting from beta-3 adrenergic receptor stimulation to direct BKCa channel activation. This fundamental parameter change in the mechanism of action achieves bladder relaxation through a different physiological pathway, thereby maintaining treatment efficacy while avoiding the side effects (urinary retention, hypertension) associated with beta-3 agonist therapy
3Object-generated harmful factors
If conventional therapeutic agents are used, then bladder contraction is inhibited, but the treatment has limitations and side effects that require new therapeutic agents
Solution Approach 1:
The patent applies segmentation by dividing the treatment approach into distinct mechanistic categories: traditional antimuscarinic agents, beta-3 agonists, and the novel BKCa channel activator. This segmentation allows for selective targeting of the desired therapeutic effect (bladder relaxation) while avoiding the harmful pathways associated with conventional agents, thus expanding treatment options with reduced side effects
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 quinazoline-based compound effectively activates BKCa channels, reducing urinary frequency and urgency in both animal models and cell-based assays, with demonstrated selectivity and low toxicity, offering a promising treatment for overactive bladder with reduced side effects.
Implementation Method 1
A pharmaceutical composition containing a novel quinazoline-based compound that activates BKCa channels, inducing relaxation of bladder smooth muscles and preventing excessive contractions
Data Source
AI summary
A quinazoline-based compound is represented by Formula 1 or Formula 2. The compound can effectively activate the BKCa channels, and thus may be used for preventing or treating the overactive bladder caused by inactivation or decrease in activity of the BKCa channels. The compound can be included in a pharmaceutical composition or health function food for improving urinary function.