Pyrazole Derivative p38 Kinase Inhibitor for COPD Exacerbation Recovery

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Solution Overview

Problem

Current treatments for acute exacerbations of chronic obstructive pulmonary disease (COPD) are inadequate, requiring prolonged hospitalization and often result in incomplete recovery, with existing maintenance and rescue therapies providing only marginal benefits.

Innovation Solution

The use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or its pharmaceutically acceptable salt, hydrate, or solvate, administered as a single oral dose, which acts as a p38 kinase inhibitor to accelerate recovery from acute exacerbations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of time

If existing maintenance and rescue therapies are used for acute exacerbations of COPD, then patients receive standard treatment, but hospitalization time is prolonged and recovery is incomplete

Engineering Contradiction:
Improvehospitalization timeVSAvoidrecovery completeness
Core Design Contradiction:
Loss of timeVSReliability

Solution Approach 1:

The patent applies parameter changes by using a p38 kinase inhibitor with specific pharmacological properties (selective inhibition of p38α and p38β isoforms) to alter the disease course. The compound changes the temporal parameter of recovery by accelerating the return to stable disease state, thereby reducing hospitalization time while improving recovery completeness compared to existing therapies

Inventive Principle:
Principle #35Parameter changes

2Productivity

If existing therapies are used for acute exacerbations of COPD, then treatment is provided, but the therapies provide only marginal benefits and require prolonged hospitalization

Engineering Contradiction:
Improverecovery accelerationVSAvoidtreatment complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent extracts the specific pathological mechanism (p38 kinase activity) from the complex inflammatory cascade in COPD exacerbations. By targeting this single key enzyme with a selective inhibitor, the treatment achieves accelerated recovery without requiring complex multi-target regimens, thus improving productivity while maintaining manageable treatment complexity

Inventive Principle:
Principle #2Taking out (Extraction)

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

This treatment significantly reduces hospitalization time, improves lung function, and may reduce the need for steroids, potentially delaying the onset of the next exacerbation, offering a disease-modifying effect in the short term.

Implementation Method 1

WO 2005/009973 discloses various pyrazole- and midazole-based compounds or pharmaceutically acceptable derivatives thereof that have cytokine inhibitory activity. It discloses such compounds can be used to treat conditions associated with p38 kinases

Methodology Applied
Scientific Effectp38 kinase inhibition: Enzyme

Data Source

PatentEP2827860B1Use of a pyrazole derivative in the treatment of acute exacerbations of chronic obstructive pulmonary disease
Publication Date: 2016.10.26 MEREO BIOPHARMA 1
  • EP2827860B1 patent drawing
  • EP2827860B1 patent drawing
  • EP2827860B1 patent drawing

AI summary

Use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of acute exacerbations of chronic obstructive pulmonary disease. Treatment may involve a single dose of the active ingredient by oral administration.