Dual Inhibitor Compounds Targeting c-fms and c-kit Receptors
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Solution Overview
Problem
Current treatments for diseases related to c-fms and c-kit receptors are limited in efficacy, as they often target either c-fms or c-kit individually, failing to address the dual inhibition needed for enhanced therapeutic outcomes.
Innovation Solution
Development of compounds that act as dual inhibitors of both c-fms and c-kit, as well as modulators of TrkA, TrkB, and HGK, with specific structures defined by Formula I, which can be used therapeutically and prophylactically to modulate these receptors.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If single-target inhibitors targeting only c-fms or only c-kit are used, then the treatment approach is simple, but the therapeutic efficacy is limited
Solution Approach 1:
The patent applies the universality principle by designing compound (I) that simultaneously targets multiple receptors (c-fms, c-kit, and optionally TrkA, TrkB, HGK) with a single molecular structure. The compound contains multiple functional groups that can interact with different receptor types, enabling one compound to perform multiple therapeutic functions and address multiple disease pathways concurrently, thereby improving therapeutic efficacy without requiring multiple separate treatments
Solution Approach 2:
The patent merges the inhibition activities against c-fms and c-kit receptors into a single compound (I) structure. By combining multiple pharmacophoric elements that recognize different receptor binding sites within one molecule, the invention achieves synergistic therapeutic effects and broader disease coverage while simplifying the treatment regimen from multiple drugs to one compound
2Adaptability or versatility
If dual inhibitors targeting both c-fms and c-kit are developed, then the therapeutic spectrum is broadened, but the compound development complexity increases
Solution Approach 1:
The patent extends universality by incorporating optional TrkA, TrkB, and HGK modulation capabilities into compound (I), creating a highly versatile inhibitor that can address a broader range of diseases involving these receptors. The molecular structure includes adaptable functional groups that can interact with various receptor families, allowing the same compound to be used for multiple indications and patient populations with different receptor profiles
Solution Approach 2:
The patent employs parameter changes by modifying the chemical structure of compound (I) through various substituents and functional groups to optimize binding affinity and selectivity for different receptor targets. By adjusting molecular parameters such as hydrophobicity, steric bulk, and electronic properties, the invention achieves broad therapeutic spectrum while maintaining manageable compound design complexity through systematic structure-activity relationship optimization
Data Source
AI summary
Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.