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
Engineering 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
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
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
Data Source
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.


