Indanyl Carboxylic Acid Compounds for Selective S1P5 Modulation
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Solution Overview
Problem
Current treatments for neurodegenerative diseases, such as Alzheimer's and multiple sclerosis, lack effective compounds that modulate sphingosine-1-phosphate receptor 5 (S1P5) to address the underlying cellular mechanisms contributing to these conditions.
Innovation Solution
Development of carboxylic acid containing indanyl compounds that modulate S1P5, which are administered to subjects in need, thereby targeting the receptor and potentially alleviating symptoms of neurodegenerative diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for neurodegenerative diseases are used, then existing therapeutic options are available, but effective modulators for S1P5 receptors are lacking
Solution Approach 1:
The patent segments the therapeutic approach by developing specific compounds that selectively modulate S1P5 receptors, separating this target from other S1P receptor subtypes. This allows for targeted treatment of neurodegenerative diseases through S1P5-specific modulation while leaving other receptor pathways unaffected.
Solution Approach 2:
The patent employs parameter changes by modifying molecular structures (varying R1, R2, R3 substituents and L linkers) to optimize S1P5 binding affinity and selectivity. This systematic variation of chemical parameters enables the development of effective S1P5 modulators where none previously existed.
2Adaptability or versatility
If compounds of Formula (I) are developed to modulate S1P5, then therapeutic options for neurodegenerative diseases are expanded, but structural complexity of the compounds increases
Solution Approach 1:
The patent creates a universal scaffold structure (Formula I) that can accommodate multiple substituent variations while maintaining S1P5 modulatory activity. This core structure serves multiple therapeutic purposes across different neurodegenerative diseases, reducing the need for entirely separate compound designs for each application.
Solution Approach 2:
The patent applies local quality by introducing specific substituents at defined positions (R1 on aromatic ring, R2 and R3 on piperidine/piperazine ring) to optimize S1P5 interaction. This localized modification approach allows for precise tuning of molecular properties without requiring complete structural redesign.
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.