Fatty Acid Derivatives for Stable Delivery of Endogenous Bioactivity

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Solution Overview

Problem

Current treatments for inflammation, itch, pain, autoimmunity, and atherosclerosis are inadequate in maintaining the effects of endogenous bioactive compounds while ensuring stability, activity, and ease of delivery.

Innovation Solution

Development of fatty acid derivatives with specific structural modifications to maintain the effects of endogenous bioactive compounds, enhancing stability, activity, and ease of delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for inflammation, itch, pain, autoimmunity, and atherosclerosis, then patient treatment is available, but the treatments fall short of demonstrated need in maintaining effects of endogenous bioactive compounds while ensuring stability, activity, and ease of delivery

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidstability, activity, and ease of delivery
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of endogenous bioactive compounds (such as fatty acids) to create derivatives with improved stability and delivery properties. Specific structural parameters including chain length, degree of unsaturation, and functional groups are altered to optimize both therapeutic effectiveness and pharmacokinetic properties, resolving the contradiction between maintaining biological activity and improving stability/delivery

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating hybrid molecules that combine elements of endogenous bioactive compounds with synthetic modifications. These composite fatty acid derivatives integrate natural bioactivity with engineered stability and delivery characteristics, allowing simultaneous achievement of therapeutic reliability and improved adaptability for clinical use

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If fatty acid derivatives with structural modifications are developed, then stability and activity are enhanced, but the complexity of compound structure increases

Engineering Contradiction:
Improvestability of fatty acid derivativeVSAvoidstructural complexity of compound
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies local quality by making targeted, localized modifications to specific regions of the fatty acid molecule rather than comprehensive structural changes. Specific functional groups or carbon positions are modified to confer stability while preserving the overall molecular framework and biological recognition elements, thus enhancing stability without proportionally increasing complexity

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs segmentation by dividing the fatty acid molecule into distinct functional domains (hydrophobic tail, functional group region, carboxyl head) and optimizing each segment independently. This modular approach allows stability enhancements in specific regions without requiring complex modifications throughout the entire molecule, managing complexity while improving composition stability

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS12479812B2Fatty acid derivatives and their use
Publication Date: 2025.11.25 THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
  • US12479812B2 patent drawing
  • US12479812B2 patent drawing
  • US12479812B2 patent drawing

AI summary

This disclosure concerns fatty acid derivatives, pharmaceutical compositions comprising the fatty acid derivatives, and methods of using the fatty acid derivatives, for example, to treat inflammation, chronic itch, chronic pain, an autoimmune disorder, atherosclerosis, a skin disorder, arthritis, a neurodegenerative disorder, or a psychiatric disorder in a subject. In some embodiments, the fatty acid derivative is a compound, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, having a structure according to:wherein X is from 1-16 carbons in length, Z is aliphatic from 1-16 carbons in length, or is not present, Y is selected from:R1, R2, and R3 are independently hydrogen or lower alkyl, R4 is lower alkyl, hydroxyl, carboxyl, or amine, R5 is hydrogen, lower alkyl, or halide, R6 is hydroxyl or substituted thiol, and each R7 is independently hydrogen or fluoride or is not present and the adjacent carbons form alkyne.