Fused Ring Compounds and ADC Conjugates for Tumor Targeting
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Solution Overview
Problem
Current ADC drugs face challenges such as low potency of cytotoxicity, narrow therapeutic windows, and issues with drug loading rates, limiting their effectiveness in treating various cancers.
Innovation Solution
A conjugate represented by Formula (C) or its stereoisomers, racemates, isotopologues, or pharmaceutically acceptable salts, featuring a targeting moiety (Tp) linked through a chemical bond or linker (L) to a group (G) with specific structural components, designed to enhance targeted delivery and cytotoxicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If ADC drugs use conventional cytotoxic agents and linkers, then the drug can be delivered to target tumor cells, but the cytotoxicity potency is insufficient and therapeutic window is narrow
Solution Approach 1:
The patent modifies the chemical structure of the cytotoxic agent by introducing specific fused ring systems with defined substituent patterns (R1-R10 groups) to enhance cytotoxic potency while maintaining selective toxicity. The structural parameters of the drug molecule are optimized to improve therapeutic efficacy and widen the therapeutic window.
Solution Approach 2:
The patent creates a composite ADC structure combining a monoclonal antibody with a specifically designed cytotoxic agent featuring fused ring systems. This composite approach integrates the targeting capability of antibodies with the enhanced cytotoxicity of the modified drug molecule, achieving both selective delivery and potent killing activity.
2Quantity of substance
If ADC drugs increase drug loading rate, then more cytotoxic agents can be delivered, but the molecular structure design becomes more complex and stability may be compromised
Solution Approach 1:
The patent divides the cytotoxic agent into modular components with specific fused ring systems and substituent groups that can be systematically varied. This segmentation allows for optimized drug loading while maintaining manageable molecular complexity through standardized structural units.
Solution Approach 2:
The patent designs a universal cytotoxic agent structure with fused ring systems that can serve multiple functions: maintaining stability, enabling high drug loading, and providing potent cytotoxicity. The modular design allows this single structural framework to fulfill multiple requirements simultaneously.
3Ease of operation
If ADC drugs use first-generation murine antibodies, then the concept of targeted delivery is established, but the cytotoxicity is not potent enough and targets are low-expressed
Solution Approach 1:
The patent significantly modifies the cytotoxic agent structure from conventional agents to fused ring systems with specific substituent patterns, transforming the potency parameter while preserving the targeted delivery mechanism established by monoclonal antibodies.
Data Source
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AI summary
The present disclosure relates to a fused ring compound, a conjugate thereof and the use thereof. The compound and the conjugate of the present disclosure have good activity of inhibiting tumor cells, stability, and in vivo drug efficacy in animals.