C4-Modified Oleanolic Acid Derivatives for Selective IL-17 Inhibition

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Solution Overview

Problem

Current therapeutic options for autoimmune diseases and inflammatory disorders associated with excess production of IL-17 are inadequate, leading to significant symptoms and side effects, and there is a need for therapies that can effectively inhibit or reduce IL-17 levels.

Innovation Solution

Development of C4 modified oleanolic acid derivatives that can inhibit IL-17 production, providing novel compounds and pharmaceutical compositions for the prevention and treatment of diseases related to IL-17 overproduction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If therapeutic antibodies against TNF are used to treat autoimmune diseases, then symptom relief is improved, but side effects increase due to immune suppression

Engineering Contradiction:

Improvesymptom reliefVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by developing compounds that specifically inhibit IL-17 production and signaling pathways while preserving other immune functions. The C4 modified oleanolic acid derivatives and related compounds are designed to target IL-17A and IL-17F selectively, allowing effective treatment of autoimmune diseases without the broad immune suppression caused by TNF antibodies.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by modifying the chemical structure of oleanolic acid at the C4 position to create derivatives with optimized IL-17 inhibition activity. By systematically varying substituents at different positions (R1, R2, R3, R4 groups) and evaluating their biological activity, the invention identifies compounds with enhanced selectivity and reduced off-target effects compared to existing therapies.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing therapies are used for autoimmune diseases, then treatment efficacy is improved, but patient tolerance worsens

Engineering Contradiction:

Improvetreatment efficacyVSAvoidpatient tolerance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent uses small molecule compounds as intermediaries that can cross cell membranes and inhibit IL-17 production at the transcriptional and translational levels. These compounds act as mediators between the immune system and therapeutic intervention, providing a different mechanism of action compared to large protein therapeutics, which may improve tolerability while maintaining efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If IL-17 inhibition is achieved, then disease pathology is reduced, but selectivity and safety may be compromised

Engineering Contradiction:

Improvedisease controlVSAvoidselectivity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies segmentation by dividing the IL-17 inhibition strategy into multiple molecular targets and mechanisms. The compounds are designed to inhibit IL-17 production through multiple pathways (transcriptional regulation, protein stability, signaling inhibition) and to target both IL-17A and IL-17F, providing segmented approaches to achieve comprehensive disease control while maintaining selectivity.

Inventive Principle:

Principle #1Segmentation

Data Source

PatentUS12545701B2C4-modified oleanolic acid derivatives for inhibition of IL-17 and other uses

Publication Date: 2026.02.10 1 REATA PHARMA INC 2 TRUSTEES OF DARTMOUTH COLLEGE

AI summary

Disclosed herein are C4 modified oleanolic acid derivatives of the formula:as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.