Pyrrolidine Beta-3 Agonists for Overactive Bladder Treatment

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

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-adrenergic receptor (β3AR) agonists, specifically compounds of Formula I, which are used in pharmaceutical compositions to treat or prevent disorders mediated through β3AR, offering a new approach to relax bladder smooth muscle and address urinary disorders.

Engineering Contradictions & Design Principles

VSEngineering 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

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing novel chemical compounds with modified molecular structures (Formula I) that selectively target β3-adrenergic receptors. This structural parameter change in the therapeutic agent enables improved treatment effectiveness through selective relaxation of detrusor smooth muscle while minimizing side effects associated with non-selective therapies

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If β3AR agonists are administered, then bladder smooth muscle relaxation is achieved, but potential side effects from receptor activation must be managed

Engineering Contradiction:
Improvebladder relaxation efficacyVSAvoidreceptor-mediated side effects
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds that selectively activate β3-adrenergic receptors in specific tissues (detrusor smooth muscle, adipose tissue) while minimizing activation in other organs. This selective local action achieves effective bladder relaxation while reducing systemic side effects through tissue-specific receptor subtype targeting

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS8354403B2Pyrrolidine derived beta 3 adrenergic receptor agonists
Publication Date: 2013.01.15 MERCK SHARP & DOHME LLC
  • US8354403B2 patent drawing
  • US8354403B2 patent drawing
  • US8354403B2 patent drawing

AI summary

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.