Antibody-drug conjugate containing thiazolo[5,4-b]pyridine structure and use thereof

IL330726A0Pending Publication Date: 2026-08-01BEIJING TIDE PHARMACEUTICAL CO LTD
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Patent Information

Application Number
IL330726
Authority / Receiving Office
IL · IL
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-01-17
Filing Date
2025-01-16
Publication Date
2026-08-01

AI Technical Summary

Technical Problem

Existing antibody-conjugated drug (ADC) linkers are unstable in vivo, causing cytotoxins to off-target, reduce drug efficacy and increase toxicity, and there is room for optimization of linker design.

Method used

A thiol-reactive linker with 2-(methylsulfonyl)thiazole[5,4-b]pyridine structure is used to connect antibodies and cytotoxins, improve the stability and hydrophilicity of the linker, and is suitable for coupling of a variety of biomolecular molecules.

Benefits of technology

It enhances the stability and efficacy of antibody-conjugated drugs, reduces off-target toxicity, and improves the effective load release of the drug in target tissue.

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Abstract

The present invention relates to a new thiol-reactive coupling moiety as shown in formula (I), a linker containing the coupling moiety, a linker-payload conjugate, an antibody-drug conjugate based on the linker and the use thereof, and further relates to a pharmaceutical composition containing the antibody-drug conjugate, and the use of the antibody-drug conjugate for treating and / or preventing a disease.
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