Processes and compounds for the preparation of topoisomerase i inhibitor linker-payloads

WO2025191470A1PCT designated stage Publication Date: 2025-09-18ASTRAZENECA AB +1
View PDF 3 Cites 0 Cited by

Patent Information

Application Number
PCT/IB2025/052592
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-03-12
Filing Date
2025-03-11
Publication Date
2025-09-18

AI Technical Summary

Technical Problem

The existing synthetic route for producing Topoisomerase I inhibitor linker-payloads, such as AZ'0133, is not economically viable for large-scale manufacturing and has environmental impact, with issues in amination reactions using certain amine sources leading to impurity formation.

Method used

A new synthetic route involving a palladium catalyst and specific bases like caesium carbonate or tripotassium phosphate, along with optimized reaction conditions, is employed to produce compounds like tert-Butyl (4-acetamido-5-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)carbamate and N-(4-((Diphenylmethylene)amino)-8-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide, improving reaction efficiency and reducing impurities.

Benefits of technology

The new process enhances the production of Topoisomerase I inhibitor linker-payloads by minimizing impurity formation and reducing costs, making it suitable for large-scale manufacturing with improved environmental sustainability.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure IB2025052592_18092025_PF_FP_ABST
    Figure IB2025052592_18092025_PF_FP_ABST
Patent Text Reader

Abstract

This specification relates to processes and intermediate compounds involved in the preparation of Topoisomerase I inhibitor (TOPO1i) linker-payloads suitable for the synthesis of antibody conjugates.
Need to check novelty before this filing date? Find Prior Art

Citation Information

Patent Citations

  • Compounds and conjugates thereof

    WO2020200880A1

  • Synthesis method of 5, 8-diamino-3, 4-dihydro-2H-1-naphthalenone and intermediate compound adopted therein

    CN115703712A

  • Camptothecin compound and conjugate thereof

    WO2023109965A1