Heterocyclic Anticancer Compounds for MAPK Resistance Durability
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Solution Overview
Problem
Existing cancer treatments, particularly those targeting the MAPK pathway, face challenges with drug resistance and limited durability, necessitating the development of compounds that can effectively treat cancer and prevent resistance.
Innovation Solution
Development of novel heterocyclic derivatives, including pharmaceutically acceptable salts, solvates, cocrystals, tautomers, racemates, enantiomers, or diastereomers, which exhibit activity against various types of cancer, including non-melanoma skin cancer and non-small cell lung cancer, by targeting key signaling pathways.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If receptor tyrosine kinase inhibitors and other kinase inhibitors are used to treat cancer, then anti-tumor effect is achieved, but drug resistance develops and clinical anti-tumor effect becomes non-durable
Solution Approach 1:
The patent modifies the chemical structure of known kinase inhibitors by introducing specific heterocyclic derivatives with modified R1-R6 substituents, changing molecular parameters to overcome resistance mechanisms while maintaining anti-tumor activity
Solution Approach 2:
The invention creates composite therapeutic approaches by combining heterocyclic derivative compounds with existing anti-cancer agents in combination therapies, achieving synergistic effects that prevent resistance development
2Reliability
If EGFR inhibitors are used to treat cancer, then tumor growth is inhibited, but resistance develops within 9 to 19 months
Solution Approach 1:
The patent introduces heterocyclic derivatives with modified chemical parameters (substituents at R1-R6 positions) that change the pharmacological properties of EGFR inhibitors, extending the duration of effective anti-tumor activity beyond the typical 9-19 month resistance development timeline
Solution Approach 2:
The invention employs preliminary action by designing heterocyclic derivatives that preemptively address resistance mechanisms through their unique molecular structure, preventing resistance development before it occurs rather than responding after resistance emerges
Data Source
AI summary
The present invention relates to a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof: formula (I) and to pharmaceutical compositions comprising a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, in the treatment of cancer. Further aspects of the present invention include combination therapies in which a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, is used in combination with a known anti-cancer agent.