Pyrazinone Derivatives Inhibit p38 Kinase to Reduce Lung Inflammation
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Solution Overview
Problem
Current treatments for respiratory diseases such as asthma and COPD, including corticosteroids and bronchodilators, often have limited efficacy and are associated with side effects, and there is a need for more effective agents that can target the underlying inflammation and airway inflammation pathways.
Innovation Solution
Development of pyrazinone derivatives that inhibit the p38 kinase pathway, which is involved in inflammatory processes in the lungs, allowing for local or systemic administration to regulate airway inflammation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If corticosteroids are used to treat respiratory diseases, then anti-inflammatory effects are achieved, but side effects and steroid resistance increase
Solution Approach 1:
The patent transitions from using corticosteroids to using p38 kinase inhibitors, representing a fundamental change in the therapeutic parameter (mechanism of action). This parameter change allows achieving anti-inflammatory effects through a different biochemical pathway, thereby maintaining efficacy while reducing side effects and resistance issues associated with steroids
2Reliability
If high dose inhaled corticosteroids are used, then response disparity between smokers and non-smokers is reduced, but side effects increase
Solution Approach 1:
The patent employs p38 kinase inhibitors as an alternative therapeutic agent that copies the desired anti-inflammatory effect of corticosteroids but through a different mechanism. This provides a substitute solution that achieves similar therapeutic responses in both smokers and non-smokers without the dose-dependent side effects of high-dose steroids
Data Source
AI summary
The present invention relates to pyrazinone derivatives of formula (I):wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.