Phenylmaleimide Linker Agents

JP2025513101A5Pending Publication Date: 2026-03-18FIREFLY BIO INC
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Patent Information

Application Number
JP2024554159
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2022-07-21
Filing Date
2023-03-10
Publication Date
2026-03-18

AI Technical Summary

Technical Problem

The complexity of linkers connecting targeted peptides to cytotoxic drugs in existing antibody-drug conjugates (ADCs) has led to limited progress in the development of novel effective therapies.

Method used

The branched chain phenol maleimide compound is used as a carrier to form a stable co-gross by binding to the antibody or ligand, and the stability is improved and non-targeted absorption is reduced using water-soluble groups.

Benefits of technology

Improves the stability of antibody-drug co-composites and the consistency of drug-to-antibody ratio (DAR), extends the time of existence in the systemic circulation, while reducing non-targeting activity.

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Abstract

Disclosed are compounds useful as linker-payload compounds, the compounds having the following structure (I) as a stereoisomer, enantiomer or tautomer thereof, or a pharma- ceutically acceptable salt, solvate or prodrug thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , R 4a , and R 4b is as defined herein. Additional compounds, conjugates, methods of preparation, pharmaceutical compositions, and methods of treatment related to the conjugates of the compounds of structure (I) and a targeting moiety, or binding fragments thereof, are also provided. JPEG2025513101000528.jpg48154
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