Beta-3 Adrenergic 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, well-tolerated treatments that effectively manage urinary frequency, urgency, and incontinence.

Innovation Solution

Development of novel β3-adrenoceptor agonist compounds, specifically defined by Formula Ia, Ib, and Id, which are potent agonists of the β3-adrenoceptor, for treating overactive bladder and other conditions by administering them to provide a therapeutically effective dosage.

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 Ia, Ib, Id) that alter the pharmacological parameters of β3-adrenoceptor agonists. These structural modifications aim to improve therapeutic effectiveness while reducing side effects by optimizing receptor selectivity and affinity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses β3-adrenoceptor agonist compounds as intermediary substances that mediate the therapeutic effect by binding to and activating β3-adrenergic receptors in the detrusor muscle. This intermediary mechanism provides a more selective pathway compared to existing treatments, improving effectiveness while minimizing harmful side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If many patients do not respond adequately to current treatments, then treatment coverage is provided, but therapeutic response is insufficient

Engineering Contradiction:
Improvetreatment coverageVSAvoidtherapeutic response
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent employs parameter changes by creating a series of chemically modified compounds with varying substituents and structural features (as defined in Formula Ia, Ib, Id). This allows optimization of pharmacological parameters to achieve better therapeutic responses across different patient populations while maintaining broad treatment coverage.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite molecular structures combining different functional groups and structural elements in the β3-adrenoceptor agonist compounds. These composite structures enable enhanced receptor interaction and improved therapeutic responses by integrating multiple pharmacophoric features into single molecules.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP2595483B1Novel pyrrolidine derived beta 3 adrenergic receptor agonists
Publication Date: 2017.03.22 MERCK SHARP & DOHME CORP

AI summary

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ß3-adrenoceptor. (I).