Diarylamine Compounds Modulating c-Kit Receptor Activity
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Solution Overview
Problem
Current treatments for diseases associated with c-kit receptor activity, such as certain cancers, are limited by the inability to effectively modulate the receptor's activity without causing unintended side effects.
Innovation Solution
Development of diarylamine compounds with heterocyclic groups, including pyrimidines, that specifically modulate c-kit receptor activity to prevent, inhibit, or ameliorate the pathology of associated diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for c-kit receptor-associated diseases are used, then disease symptoms can be addressed, but unintended side effects occur due to inability to effectively modulate receptor activity
Solution Approach 1:
The patent applies local quality by designing diarylamine compounds with specific heterocyclic groups (such as pyrimidines) that are tailored to interact with particular regions or conformations of the c-kit receptor. This localized molecular design enables selective modulation of the receptor's active state, achieving effective disease treatment while minimizing unintended side effects through precise target engagement rather than broad receptor suppression
2Reliability
If broad-spectrum c-kit receptor modulation is attempted, then disease pathology can be inhibited, but specificity is reduced leading to off-target effects
Solution Approach 1:
The patent employs parameter changes by systematically varying molecular parameters of the diarylamine compounds, including the specific heterocyclic group attached to the aniline nitrogen, substitution patterns on aromatic rings, and spatial configuration. These parameter adjustments fine-tune the compounds' binding affinity and selectivity for the c-kit receptor, enabling precise modulation that distinguishes between pathological and normal receptor functions
Data Source
AI summary
Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.