GPR40-Activating Phenyl-Propionic Acid Derivatives

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Solution Overview

Problem

Current compounds for treating hyperglycemia and diabetes, particularly those activating the GPR40 receptor, are limited in their therapeutic efficacy and specificity.

Innovation Solution

Development of substituted (2-aryloxy-acetylamino)-phenyl-propionic acid derivatives and their physiologically tolerated salts, which are designed to activate the GPR40 receptor, offering new potential treatments for hyperglycemia and diabetes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing compounds for treating hyperglycemia and diabetes are used, then some therapeutic effect is achieved, but the therapeutic efficacy and specificity are limited

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidspecificity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically modifying molecular parameters of the compound structure, including substituting hydrogen atoms at specific positions (R1-R9) with various functional groups (halogens, alkyl groups, hydroxyl groups, carboxyl groups, etc.), changing the molecular weight, logP values, and other physicochemical properties to optimize both therapeutic efficacy and specificity for GPR40 receptor activation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite molecular structures by combining multiple functional groups and structural motifs within a single molecule, integrating the phenyl-propionic acid core with various aryl substituents and functional groups to achieve enhanced therapeutic effects and improved specificity compared to single-functional compounds

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP2590931B1(2-aryloxy-acetylamino)-phenyl-propionic acid derivatives and their use as medicament
Publication Date: 2014.04.30 SANOFI SA(FR)
  • EP2590931B1 patent drawing
  • EP2590931B1 patent drawing
  • EP2590931B1 patent drawing

AI summary

The invention relates to substituted (2-aryloxy-acetylamino)-phenyl-proprionic acid derivatives of formula I and the physiologically tolerable salts thereof. The compounds are suitable, for example, for treating diabetes, because they effect increased insulin release by activating the GPR40 receptor.