Mucosal Immunomodulator Formulations via Hydroxy Fatty Acid Segmentation

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Solution Overview

Problem

Current mucosal immunomodulators do not provide sufficient options to meet diverse consumer needs for mucosal immunostimulation and immunosuppression, limiting their effectiveness in modulating mucosal immunity.

Innovation Solution

Development of mucosal immunomodulators comprising specific compounds represented by formulas (4), (5), (6), (8), (9), (10), (11), (12), and (13), and their salts, which can stimulate or suppress mucosal immunity, used as immunostimulators or immunosuppressants, and incorporated into food compositions, adjuvants, and vaccine formulations to induce M-cell differentiation and promote immune tolerance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional mucosal immunomodulators are used, then some immunostimulation effect is achieved, but the options are insufficient to meet diverse consumer needs for both immunostimulation and immunosuppression

Engineering Contradiction:
Improveversatility of mucosal immunomodulatorVSAvoidcomplexity of compound selection
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent segments the broad category of mucosal immunomodulators into distinct functional groups based on chemical structure (hydroxy unsaturated fatty acids with specific hydroxyl group positions and configurations). This segmentation allows for targeted selection of compounds for either immunostimulation or immunosuppression, thereby increasing versatility while maintaining manageable complexity through systematic classification.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent utilizes parameter changes in the chemical structure of fatty acid compounds, specifically the position and configuration of hydroxyl groups, to modulate immunological activity. By varying these structural parameters, the same base compound family can produce different immunological effects (stimulation vs. suppression), thereby enhancing versatility without requiring entirely different compound classes.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If specific hydroxy unsaturated fatty acid compounds are used to stimulate mucosal immunity, then M-cell differentiation is induced, but the mechanism requires precise structural characterization

Engineering Contradiction:
Improveefficacy of mucosal immunostimulationVSAvoiddifficulty of structural characterization
Core Design Contradiction:
ReliabilityVSDifficulty of detecting and measuring

Solution Approach 1:

The patent applies local quality by specifying the exact position and configuration of hydroxyl groups on the fatty acid chain. Rather than requiring complete structural characterization of the entire molecule, the invention identifies that specific local features (hydroxyl group at positions 9, 10, or 11 with particular stereochemistry) are sufficient to predict and ensure immunostimulatory efficacy, thereby reducing measurement complexity while maintaining reliability.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent performs preliminary structural characterization to identify and isolate compounds with the required hydroxyl group configurations before testing immunological activity. This preliminary action of selecting compounds based on known structural-activity relationships reduces the need for extensive subsequent characterization and accelerates the development process while ensuring reliable efficacy.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP3530270B1Mucosal immunomodulator
Publication Date: 2024.08.07 YAMADA BEE COMPANY INC
  • EP3530270B1 patent drawingFigure 1
  • EP3530270B1 patent drawingFigure 2
  • EP3530270B1 patent drawingFigure 3

AI summary

The present invention provides a mucosal immunomodulator comprising, as an active ingredient, at least one selected from the group consisting of compounds represented by the following formula (1), compounds represented by the following formula (2) and compounds represented by the following formula (3), and salts thereof.