S1P5-Modulating Compounds for Oligodendrocyte and Myelin Support

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Solution Overview

Problem

Current treatments for neurodegenerative diseases do not effectively modulate the sphingosine-1-phosphate receptor S1P5, which is crucial for oligodendrocyte function and myelin sheath formation in the central nervous system.

Innovation Solution

Development of compounds that modulate S1P5, specifically targeting the S1P5 receptor to treat neurodegenerative diseases such as Alzheimer's, multiple sclerosis, and amyotrophic lateral sclerosis, by administering effective amounts of these compounds or their pharmaceutical compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for neurodegenerative diseases, then general symptom management is achieved, but effective modulation of S1P5 receptor is not achieved

Engineering Contradiction:
ImproveS1P5 modulation efficacyVSAvoidineffective treatment outcome
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of S1P5 modulating compounds. The invention describes specific chemical formulas (Formula I, II, III, IV, V) with defined substituent groups (R1-R8, L, X1, X2) that optimize the molecular parameters to achieve effective S1P5 receptor modulation, thereby resolving the inadequacy of current treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses S1P5 receptor as an intermediary target to treat neurodegenerative diseases. The compounds developed in this invention specifically bind to and modulate the S1P5 receptor, which then mediates therapeutic effects on oligodendrocyte function and myelin sheath formation, indirectly treating the underlying disease mechanisms

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If S1P5 is targeted to improve oligodendrocyte function, then neurodegenerative disease treatment is enhanced, but treatment specificity to CNS is required

Engineering Contradiction:
Improveoligodendrocyte function improvementVSAvoidoff-target effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds with specific molecular characteristics that preferentially interact with S1P5 receptors in the central nervous system. The chemical structures (Formulas I-V) are optimized to have appropriate lipophilicity, molecular weight, and functional groups that enable selective binding to CNS-expressed S1P5 receptors while minimizing interactions with other tissue receptors

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20260022094A1Compounds for the Treatment of Neurodegenerative Diseases
Publication Date: 2026.01.22 CELGENE CORP
  • US20260022094A1 patent drawing
  • US20260022094A1 patent drawing
  • US20260022094A1 patent drawing

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.