Multi-Kinase Inhibitor Compounds for Syk and GCN2 Targeting
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Solution Overview
Problem
Current treatments for diseases such as rheumatoid arthritis, systemic lupus, asthma, and certain cancers are limited by the narrow therapeutic window of cytotoxic agents and the ability of cancer cells to develop resistance, highlighting the need for targeted therapies that inhibit multiple survival mechanisms and modulate signal transduction pathways.
Innovation Solution
Development of furopyridine derivatives and other compounds that selectively inhibit Syk, BTK, Src, Zap70, Fak, Pyk2, FLT3, or Jak kinases, as well as the GCN2 kinase, to regulate signal transduction and interfere with tumor metabolism, thereby addressing immune evasion and tumor progression.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If cytotoxic agents are used to treat diseases such as rheumatoid arthritis, systemic lupus, asthma, and certain cancers, then therapeutic efficacy is improved, but the narrow therapeutic window and development of resistance worsen treatment outcomes
Solution Approach 1:
The patent changes the molecular parameters of the therapeutic agents by developing novel kinase inhibitor compounds with specific chemical structures (formula I) that target multiple kinase pathways simultaneously, thereby improving therapeutic efficacy while expanding the therapeutic window through multi-target inhibition
Solution Approach 2:
The patent applies multi-functionality by designing compounds that inhibit multiple kinase targets (Syk, BTK, Src, Zap70, Fak, Pyk2, FLT3, Jak, and GCN2) simultaneously, allowing a single agent to address multiple survival mechanisms and signal transduction pathways involved in disease pathogenesis
2Reliability
If targeted therapies inhibit multiple survival mechanisms and modulate signal transduction pathways, then therapeutic efficacy is improved, but device complexity increases
Solution Approach 1:
The patent merges multiple therapeutic functions into a single compound by designing multi-kinase inhibitors that simultaneously target Syk, BTK, Src, Zap70, Fak, Pyk2, FLT3, Jak, and GCN2 kinases, thereby simplifying the treatment regimen while maintaining broad pathway inhibition
Solution Approach 2:
The patent creates universal kinase inhibitor compounds with broad-spectrum activity against multiple kinase families, allowing one agent to perform multiple therapeutic functions and reduce the complexity of combination therapies
Data Source
AI summary
Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus