Pyrazole Derivative Composition for ROS Inhibition in Oxidative Stress

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Solution Overview

Problem

Current treatments for diseases related to oxidative stress, such as cancer, inflammatory diseases, fibrotic diseases, neurodegenerative diseases, liver diseases, and skin diseases, are inadequate in effectively inhibiting reactive oxygen species (ROS) production, leading to significant tissue damage and disease progression.

Innovation Solution

Development of a novel pyrazole derivative with excellent oxidative stress inhibitory activity, including its optical isomers, solvates, isotopic variants, and pharmaceutically acceptable salts, which can be used to inhibit ROS production and treat associated diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for oxidative stress-related diseases, then disease management is attempted, but ROS production inhibition is insufficient leading to tissue damage and disease progression

Engineering Contradiction:
ImproveROS production inhibition efficacyVSAvoidtissue damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing a novel pyrazole derivative with specific chemical structure parameters (formula 1 with defined substituents A, B, and R) that achieves superior ROS production inhibition compared to conventional treatments. The compound represents a change in chemical parameters to improve therapeutic efficacy for oxidative stress-related diseases

Inventive Principle:
Principle #35Parameter changes

2Reliability

If ROS production is not effectively inhibited, then current treatments can be administered, but oxidative damage continues causing disease progression in cancer, fibrotic diseases, and other conditions

Engineering Contradiction:
Improveoxidative stress inhibitionVSAvoiddisease progression
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent employs parameter changes by introducing a novel pyrazole derivative with specific molecular structure parameters that provides sustained and effective oxidative stress inhibition. This addresses the insufficient duration and efficacy of current treatments in preventing disease progression

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4163277B1Novel pyrazole derivatives
Publication Date: 2026.01.14 APTABIO THERAPEUTICS INC
  • EP4163277B1 patent drawingFigure 1
  • EP4163277B1 patent drawingFigure 2
  • EP4163277B1 patent drawingFigure 3a

AI summary

The Present invention provides a novel pyrazole derivative compound represented by Chemical formula 1, a stereoisomer thereof, a solvate thereof, an isotopic variant thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. (In the above, A, B and R, and the like are the same as defined in the description of the invention.).