公开(公告)号：WO1994005627A1

公开(公告)日：1994-03-17

申请号：PCT/US1993008401

申请日：1993-09-07

Applicant: UAB RESEARCH FOUNDATION

Inventor： UAB RESEARCH FOUNDATION ,  SAFAVY, Ahmad ,  BUCHSBAUM, Donald, J. ,  KHAZAELI, M., B.

IPC: C07C271/02

CPC classification number: C07C259/06 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07K5/022

Abstract: The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-((tris)(2-N-benzyloxyaminocarbonylethyl)) methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as 99mTc, 186Re and 67Cu.

Abstract translation: 本公开详细描述了基于异羟肟酸的双功能螯合剂的制备及其在将金属离子与用于肿瘤或组织成像或治疗目的的蛋白质和核酸结合的用途。 本公开的一些优选方面涉及制备三羟色胺，化学名称N - （（三（（三（（（N） - 三苄基氧基氨基羰基乙基））甲基琥珀酸，其是特别可用于结合放射性核素如99mTc的异羟肟酸/ ，186Re和67Cu。