Exatecan-derived topoisomerase-1 inhibitor pharmaceutical composition and use thereof

Novel exatecan-derived compounds with alcohol and amine groups address the limitations of existing topoisomerase-1 inhibitors by enhancing potency and activity across diverse cancer cell lines, providing effective oncological treatments.

JP2026035660AInactive Publication Date: 2026-03-04MERCK SHARP & DOHME LLC
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2025-11-20
Publication Date
2026-03-04
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current topoisomerase-1 inhibitors, such as exatecan derivatives, lack diversity in structure and efficacy across various cancer cell lines, necessitating the development of novel compounds with enhanced potency and activity.

Method used

Development of exatecan-derived compounds containing alcohol and amine groups, represented by specific structural formulas, which are cytotoxic and exhibit broad antitumor activity.

Benefits of technology

The novel compounds demonstrate potent cytotoxic effects against multiple cancer cell lines, offering improved therapeutic options in oncological treatments.

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Patent Text Reader

Abstract

To provide a topoisomerase-1 inhibitor derived from an exatecan skeleton, which can be used for oncological treatment.SOLUTION: The present disclosure is also directed to alcohol- and amine-containing exatecan derivatives comprising a structure of Formula (I), and pharmaceutically acceptable salts or solvates thereof, pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions in the prevention or treatment of cancer and / or tumors.SELECTED DRAWING: None
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Citation Information

Patent Citations

  • Camptothecin derivative and conjugate thereof

    CN112125915A

  • Exatecan compound, antibody drug conjugate thereof and application of Exatecan compound and antibody drug conjugate

    CN113816969A

  • Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics

    US11103593B2

  • Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease

    US20100062008A1

  • Ligand-drug conjugate of exatecan analogue, preparation method therefor and application thereof

    US20210353764A1