公开(公告)号：US09365599B2

公开(公告)日：2016-06-14

申请号：US14063724

申请日：2013-10-25

Applicant: KOREA ATOMIC ENERGY RESEARCH INSTITUTE

Inventor： Young-Don Hong ,  Sun Ju Choi ,  So-Young Lee ,  jae cheong Lim ,  Dong Eun Lee

IPC: A61K47/48 ,  C07F13/00 ,  C07D475/04

CPC classification number: C07F13/00 ,  A61K47/547 ,  C07D475/04

Abstract: Novel N3S1 chelator-folate derivatives, a preparation method thereof, and a composition for diagnosis and treatment of tumor including the same as an active ingredient are provided. The novel N3S1 chelator-folate derivatives or a pharmaceutically acceptable salt thereof are easily introduced into the cells using receptor binding to tumor expressing α-folate receptor (α-FR). Accordingly, the folate derivatives, labeled with radioisotope such as technetium, or rhenium, can be advantageously used for the diagnosis and treatment of tumor using tumor imaging and irradiation from the isotope, and therefore, can be widely used for the purpose of labeling a variety of radiopharmaceuticals.

Abstract translation: 提供新型N3S1螯合剂 - 叶酸衍生物，其制备方法和用于诊断和治疗肿瘤的组合物，包括其作为活性成分。 使用受体结合表达α-叶酸受体（α-FR）的肿瘤，可以容易地将新型N3S1螯合剂叶酸衍生物或其药学上可接受的盐引入细胞。 因此，使用放射性同位素如锝或铼标记的叶酸衍生物可以有利地用于使用来自同位素的肿瘤成像和照射来诊断和治疗肿瘤，因此可广泛用于标记品种的目的 的放射性药物。