Novel dispirodiketopiperazine compound
Novel ligand-dispirodiketopiperazine compound conjugates, particularly antibody-drug conjugates, leverage dispirodiketopiperazine structures as cytotoxic payloads, addressing the lack of effective use in ADCs and demonstrating potent antitumor activity by targeting tumor cells.
WO2026134311A1 Publication Date: 2026-06-25DAIICHI SANKYO CO LTD
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Patent Information
- Application Number
- PCT/JP2025/044437
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-12-20
- Filing Date
- 2025-12-19
- Publication Date
- 2026-06-25
AI Technical Summary
Technical Problem
The existing ADCs do not effectively utilize dispirodiketopiperazine compounds as cytotoxic payloads, and their potential antitumor activity remains unexplored.
Method used
Development of novel ligand-dispirodiketopiperazine compound conjugates, particularly antibody-drug conjugates, utilizing specific dispirodiketopiperazine structures as cytotoxic substances, linked via a linker to antibodies targeting tumor cells, such as anti-B7-H3, anti-CDH6, anti-CD30, or anti-CD70 antibodies, demonstrating potent cytotoxic activity and antitumor effects.
Benefits of technology
The novel ligand-dispirodiketopiperazine compound conjugates exhibit selective cytotoxicity and antitumor effects by delivering cytotoxic drugs specifically to cancer cells, enhancing treatment efficacy.
✦ Generated by Eureka AI based on patent content.
Abstract
The present invention addresses the problem of providing a novel cytotoxic substance, in particular, a novel cytotoxic substance suitable as a payload of a ligand-drug conjugate, and a ligand-drug conjugate containing the cytotoxic substance. The present invention relates to a dispirodiketopiperazine compound represented by formula (VIII), or to a novel ligand-drug conjugate represented by formula (I), which contains the compound as a payload.
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