Flavanone Derivative BKCa Channel Activator for OAB
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Solution Overview
Problem
Current therapeutic options for overactive bladder syndrome (OAB) often have side effects and reduced efficacy due to their inability to specifically target urinary bladder smooth muscle, highlighting the need for novel BKCa channel activators with higher specificity and efficacy.
Innovation Solution
Development of a pharmaceutical composition containing flavanone derivatives, such as kurarinone, which effectively activate the BKCa channel by stabilizing its open form, thereby enhancing channel activity without requiring additional intracellular Ca2+.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapeutic options for OAB are used, then they can treat overactive bladder syndrome, but they cause side effects and have reduced efficacy due to inability to specifically target urinary bladder smooth muscle
Solution Approach 1:
The patent applies local quality by designing compounds that specifically target BKCa channels in urinary bladder smooth muscle cells. The chemical structures (compounds of formula 1 and 2) are engineered to interact with the specific binding site of BKCa channels, allowing selective activation of this channel subtype in bladder tissue while minimizing effects on other smooth muscle or tissue types. This localized specificity resolves the contradiction by concentrating therapeutic action where needed (bladder smooth muscle) while reducing harmful effects elsewhere in the body.
Solution Approach 2:
The patent employs parameter changes by modifying the chemical structure parameters of flavanone derivatives to optimize BKCa channel activation. Specific substitutions at positions R1-R6 in the molecular structure alter the compound's affinity and selectivity for BKCa channels. By tuning these chemical parameters, the invention achieves enhanced efficacy through stronger channel activation while maintaining safety through reduced off-target effects, thus resolving the efficacy-side effect contradiction.
2Reliability
If BKCa channel activators are developed to specifically target urinary bladder smooth muscle, then efficacy is improved, but complexity of compound structure increases
Solution Approach 1:
The patent achieves specificity through local quality by introducing targeted substitutions at specific positions (R1-R6) on the flavanone core structure. Rather than completely redesigning the molecule, the invention modifies local regions of the compound to enhance binding affinity for BKCa channels. This approach maintains reasonable structural simplicity while achieving the desired specificity for urinary bladder smooth muscle targeting.
Solution Approach 2:
The patent uses composite material principles by combining a known flavanone scaffold with specific functional groups and substituents. The base flavanone structure provides a stable framework with favorable pharmacokinetic properties, while added substituents confer BKCa channel selectivity. This composite approach allows the invention to achieve high specificity without excessive molecular complexity, as the core structure remains relatively simple and well-understood.
Data Source
AI summary
The present invention relates to novel compounds capable of activating BKCa channels. The use of a composition of the present invention can effectively activate the BKCa channels, and can be used for prevention or treatment of various diseases caused by the deactivation of BKCa channels or the degradation of BKCa channel activity.