Indanyl Carboxylic Acid Compounds for Selective S1P5 Modulation
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Solution Overview
Problem
Current compounds targeting S1P5 receptors for treating neurodegenerative diseases, such as those described in WO 2016/088834 A1, lack specificity and efficacy in modulating S1P5 receptor activity.
Innovation Solution
Development of carboxylic acid containing indanyl compounds that modulate S1P5 receptors, specifically designed to bind to S1P5 and potentially treat neurodegenerative diseases by forming a pharmaceutically acceptable salt thereof.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current compounds targeting S1P5 receptors are used, then neurodegenerative diseases can be treated, but the compounds lack specificity and efficacy in modulating S1P5 receptor activity
Solution Approach 1:
The patent applies local quality by introducing a specific carboxylic acid functional group at a precise position on the indanyl ring structure. This localized modification enhances the compound's ability to specifically interact with S1P5 receptor binding sites, thereby improving modulation efficacy without requiring complex overall molecular structures.
Solution Approach 2:
The patent utilizes parameter changes by systematically varying substituents at specific positions (R1, R2, R3, R4) on the indanyl core structure. By optimizing parameters such as substituent type, position, and stereochemistry, the compounds achieve enhanced S1P5 receptor specificity and efficacy while maintaining structurally simple frameworks.
2Reliability
If compounds are designed to bind specifically to S1P5 receptors, then treatment effectiveness improves, but the complexity of compound design increases
Solution Approach 1:
The patent focuses modifications at specific local positions on the indanyl scaffold, particularly introducing carboxylic acid groups at defined positions and selecting specific substituents. This localized approach enables specific S1P5 binding through targeted molecular interactions without requiring complex multi-functional molecular architectures.
Solution Approach 2:
The patent creates composite molecular structures by combining the indanyl core framework with specific substituent groups (carboxylic acid, aryl, heteroaryl, cycloalkyl) and optional stereochemical configurations. This composite design achieves enhanced S1P5 receptor affinity and selectivity through synergistic interactions of different molecular components while maintaining overall structural simplicity.
Data Source
AI summary
Provided herein are compounds and compositions thereof for modulating S1P5. In some embodiments, the compounds and compositions are provided for treatment of neurological diseases.