Formula (I) c-KIT Inhibitor Compounds for Aberrant c-KIT Signaling
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Solution Overview
Problem
Current therapies for treating diseases characterized by aberrant c-KIT pathway signaling, such as cancer, inflammatory, and autoimmune diseases, lack effective inhibitors of c-KIT kinase activity.
Innovation Solution
Development of compounds with specific structures, such as those of Formula (I), which act as inhibitors of c-KIT kinase, and their formulation into pharmaceutical compositions for administration to patients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used for treating diseases with aberrant c-KIT pathway signaling, then treatment is provided, but effective inhibition of c-KIT kinase activity is not achieved
Solution Approach 1:
The patent applies parameter changes by modifying molecular structure parameters to create compounds with optimized c-KIT inhibition activity. The compounds of Formula (I) feature specific structural parameters including a 5-membered nitrogen-containing heteroaryl ring (Ring A), a 9- or 10-membered bicyclic nitrogen-containing heteroaryl ring (Ring B), and specific substituent patterns (R1-R5) that are tuned to achieve effective c-KIT kinase inhibition, thereby resolving the contradiction between therapeutic effectiveness and c-KIT inhibition capability
Solution Approach 2:
The patent applies segmentation by dividing the inhibitor molecule into distinct functional segments: Ring A (5-membered nitrogen-containing heteroaryl), Ring B (9- or 10-membered bicyclic nitrogen-containing heteroaryl), and substituent groups (R1-R5). This segmented molecular architecture allows each component to contribute specifically to c-KIT binding and inhibition, enabling reliable therapeutic effectiveness through targeted kinase activity suppression
2Adaptability or versatility
If compounds of Formula (I) are developed to inhibit c-KIT kinase, then c-KIT kinase activity is effectively inhibited, but new pharmaceutical compositions and methods must be created
Solution Approach 1:
The patent applies universality by creating a broad pharmaceutical composition system that can address multiple diseases characterized by aberrant c-KIT pathway signaling. The compounds of Formula (I) serve as universal c-KIT inhibitors applicable to various conditions including cancer, inflammatory diseases, and autoimmune disorders, thereby achieving effective kinase inhibition without proportionally increasing pharmaceutical composition complexity
Data Source
AI summary
Provided herein are inhibitors of c-KIT kinase, pharmaceutical compositions comprising said inhibitory compounds, and methods for using said c-KIT kinase inhibitory compounds for the treatment of cancer, inflammatory, allergic, or autoimmune diseases, and other disorders characterized by aberrant c-KIT pathway signaling.