一种化合物、包含该化合物的螯合物及其应用

By modifying and transforming the structure of cyclic peptide-DOTA conjugates, novel compounds were designed, which solved the problems of low uptake rate, poor binding, and high accumulation in non-target organs of existing cyclic peptide-DOTA conjugates, thus achieving more efficient tumor targeting and therapeutic effects.

CN122404497APending Publication Date: 2026-07-17BOOMRAY PHARMACEUTICALS CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
BOOMRAY PHARMACEUTICALS CO LTD
Filing Date
2026-04-22
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing cyclic peptide-DOTA conjugates suffer from insufficient uptake by tumor cells, poor cell binding, inadequate tumor retention time, and high accumulation in non-target organs (especially the kidneys), which limits their therapeutic window and clinical application potential.

Method used

By modifying and transforming specific groups of cyclic peptide-DOTA conjugates, a series of novel compounds were designed and their structures were optimized to improve tumor cell uptake and binding, prolong tumor retention time, and reduce accumulation in non-target organs.

Benefits of technology

In animal models, it showed significantly improved tumor uptake and retention time, reduced accumulation in non-target organs, enhanced therapeutic efficacy and improved safety, and broadened the therapeutic window.

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Abstract

本发明提供一种化合物、包含该化合物的螯合物及其应用,所述化合物具有式(I)所示的结构。本发明的螯合物具有提高的肿瘤细胞摄取率和肿瘤细胞结合力,并且在Hep3B荷瘤小鼠模型中表现出显著改善的生物分布特性,包括更高的肿瘤摄取率、更长的肿瘤滞留时间以及更低的非靶器官蓄积,显示出优于现有技术的临床应用潜力,式(Ⅰ)。
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