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

VSEngineering 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

Engineering Contradiction:
Improvetherapeutic effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

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.

Inventive Principle:
Principle #35Parameter changes

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.

Inventive Principle:
Principle #3Local quality

2Reliability

If existing benzilic acid ester compounds are used, then some therapeutic effect is achieved, but insufficient intraurethral pressure increase occurs

Engineering Contradiction:
Improvetherapeutic effectVSAvoidintraurethral pressure
Core Design Contradiction:
ReliabilityVSStress or pressure

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.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3006427B1Fluorinated benzilic acid ester compound and salt thereof
Publication Date: 2017.11.15 TAIHO PHARMA CO LTD
  • EP3006427B1 patent drawingFigure 1
  • EP3006427B1 patent drawing
  • EP3006427B1 patent drawing

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.