REGγ-Targeting Compound for Immune Response Enhancement

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for cancer and other immunodeficiency-related diseases are limited, and there is a need for targeted therapies that can enhance immune responses, particularly in contexts where REGγ-mediated immunosuppression is a factor.

Innovation Solution

A compound of formula (I) is described, which can be used alone or in combination with a distinct therapeutic agent, such as an immune checkpoint inhibitor, to target REGγ and enhance immune responses in immunodeficient subjects, including those with cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If REGγ-mediated immunosuppression is present, then immune response is suppressed, but targeting REGγ requires development of new compounds

Engineering Contradiction:
Improveimmune responseVSAvoidcompound structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The compound of formula (I) acts as an intermediary substance that binds to REGγ, preventing REGγ from mediating immunosuppression. This small molecule mediator disrupts the harmful interaction between REGγ and the immune system, converting the suppressed immune state into an activated state without requiring direct genetic manipulation or complex biological agents.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical parameter space by developing a small molecule compound with specific structural features (formula I) that can modulate REGγ activity. By altering the chemical composition and structure of regulatory molecules, the patent achieves a shift from immunosuppressive to immunostimulatory conditions, enhancing antigen presentation and immune activation.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If conventional treatments are used, then treatment options are limited, but new therapeutic approaches require combination therapies

Engineering Contradiction:
Improvetreatment optionsVSAvoidtherapy combination
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent merges the REGγ-targeting compound of formula (I) with distinct therapeutic agents such as immune checkpoint inhibitors to create combination therapies. This merging of multiple therapeutic mechanisms—REGγ inhibition plus checkpoint blockade—produces synergistic effects that overcome the limitations of conventional single-agent treatments, expanding adaptability while managing complexity through rational drug combination.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The compound of formula (I) serves multiple functions: it directly inhibits REGγ-mediated immunosuppression, enhances antigen presentation, and can be combined with various distinct therapeutic agents including immune checkpoint inhibitors, cancer therapies, and treatments for immunodeficiency-related diseases. This multi-functionality allows a single compound to address multiple therapeutic needs across different disease contexts.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If REGγ activity is high, then antigen presentation is reduced, but enhancing immune response requires blocking REGγ interaction with proteasome

Engineering Contradiction:
Improveantigen presentationVSAvoidREGγ-mediated suppression
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention converts the harmful effect of REGγ-mediated immunosuppression into a beneficial therapeutic opportunity. By designing a compound that specifically targets and blocks REGγ activity, the patent transforms the previously harmful immunosuppressive pathway into a therapeutic vulnerability that can be exploited to enhance antigen presentation and activate immune responses against cancer and other diseases.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The compound of formula (I) performs preliminary anti-action by preemptively blocking REGγ before it can mediate immunosuppression. The compound binds to REGγ or its interaction partners, preventing the formation of immunosuppressive complexes and anticipating the harmful effect before it occurs, thereby maintaining immune system functionality.

Inventive Principle:
Principle #9Preliminary anti-action

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compound effectively inhibits the negative effects of REGγ on immune responses, leading to enhanced antigen presentation and immune activation, which can improve treatment outcomes for cancers and other immunodeficiency-related diseases.

Implementation Method 1

the production of MHC-I immune responses relies on the proteasomal system, the major proteolytic system in eukaryotic cells. At the core of this system lies the 20S proteasome or core particle, a multicatalytic protease complex

Methodology Applied
Scientific EffectProteasomal degradation: Enzyme

Implementation Method 2

The REG family, also known as 11S or PA28, consists of three distinct 28 kDa subunits (α, β, and γ), which have the capacity to assemble into two ring-shaped heptameric regulatory complexes

Methodology Applied
Scientific EffectProteolytic cleavage: Enzyme

Data Source

PatentEP4537820A1Compound and combinations comprising said compound to improve immune response
Publication Date: 2025.04.16 INSTITUT GUSTAVE ROUSSY
  • EP4537820A1 patent drawingFigure 1a
  • EP4537820A1 patent drawingFigure 1b
  • EP4537820A1 patent drawingFigure 2a~2c

AI summary

The present invention relates to the field of medicine. It more particularly relates to a compound of formula (I), and to pharmaceutical combinations and compositions comprising such a compound preferably together with at least one distinct therapeutic agent, as well as to uses thereof for treating an immunodeficient subject, in particular for preventing or treating a disease or symptom such as a cancer, an inflammation, a neurodegenerative disease or an infection.