Fluorinated Benzilic Acid Ester for Stress Urinary Incontinence
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Solution Overview
Problem
Current treatments for stress urinary incontinence, such as duloxetine, have side effects and are not approved in all countries, necessitating a new drug that increases intraurethral pressure to effectively address this common type of urinary incontinence.
Innovation Solution
A fluorinated benzilic acid ester compound, represented by specific chemical formulas, is developed to serve as a prophylactic and therapeutic agent, increasing intraurethral pressure and addressing stress urinary incontinence by enhancing urethral baseline pressure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If duloxetine is used to treat stress urinary incontinence, then therapeutic effect is achieved, but side effects such as suicide risk and lack of approval in major countries occur
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of benzilic acid ester compounds through fluorine substitution at specific positions (R1 and R2) and varying the alkoxy group (R3). This structural parameter modification results in compounds with improved therapeutic profiles that maintain efficacy while reducing harmful side effects associated with duloxetine.
Solution Approach 2:
The patent applies local quality by introducing fluorine atoms at specific localized positions (R1 and R2) on the benzilic acid ester molecular structure. This localized modification at specific sites enhances the compound's pharmacological properties, achieving better therapeutic effect with reduced side effects compared to non-fluorinated analogs.
2Reliability
If existing benzilic acid ester compounds are used, then some therapeutic effect is achieved, but insufficient intraurethral pressure increase occurs
Solution Approach 1:
The patent applies parameter changes by systematically varying the fluorine substitution pattern (R1 and R2) and alkoxy group (R3) in benzilic acid ester compounds. These parameter modifications result in compounds that produce significantly greater intraurethral pressure increases compared to existing non-fluorinated or less-optimized benzilic acid ester derivatives.
Data Source
Figure 1

AI summary
A benzilic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted fluorinated lower alkyl, is disclosed.