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Solution Overview

Problem

Current therapies for targeting cytidine triphosphate synthase 1 (CTPS1) are non-selective and face issues with toxicity and efficacy, while selective inhibitors are lacking, particularly in addressing immune and cancer cell proliferation.

Innovation Solution

Development of novel benzamide compounds that selectively inhibit CTPS1, offering potential therapeutic benefits in conditions such as autoimmune diseases, cancer, and vascular recovery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If non-selective CTPS inhibitors are used, then CTPS1 inhibition is achieved, but toxicity and efficacy issues arise due to lack of selectivity

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention segments the CTPS enzyme into two distinct isozymes (CTPS1 and CTPS2) and develops inhibitors that selectively target CTPS1. This segmentation allows the therapeutic agent to affect only the pathological pathway (CTPS1 in immune and cancer cells) while leaving normal physiological functions (mediated by CTPS2) intact, thereby resolving the contradiction between efficacy and toxicity

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by creating inhibitors with specific molecular structures (benzamide compounds with particular substituent patterns) that exhibit preferential binding affinity for CTPS1 over CTPS2. This localized specificity ensures that the harmful inhibitory effect is concentrated on the target isozyme while sparing the non-target isozyme, thus improving therapeutic index

Inventive Principle:

Principle #3Local quality

2Productivity

If selective CTPS1 inhibitors are developed, then immune and cancer cell proliferation is reduced, but novel therapeutic agents are required

Engineering Contradiction:

Improvecell proliferation controlVSAvoiddrug development complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The invention systematically varies molecular parameters of benzamide compounds (substituents at different positions, ring structures, chain lengths) to optimize selectivity and potency against CTPS1. By changing these chemical parameters, the patent achieves effective inhibition of pathological cell proliferation while navigating the complexity of developing novel selective agents

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP3717465B1compounds

Publication Date: 2026.01.21 STEP PHARMA SAS

AI summary

Compounds of formula (I) and related aspects.