公开(公告)号：US20120329174A1

公开(公告)日：2012-12-27

申请号：US13460120

申请日：2012-04-30

申请人： Kenneth N. RAYMOND ,  Tood M. CORNEILLIE ,  Jide XU

发明人： Kenneth N. RAYMOND ,  Tood M. CORNEILLIE ,  Jide XU

IPC分类号： C07F5/00 ,  G01N21/64 ,  C07D487/18

CPC分类号： G01N33/582 ,  G01N2458/40

摘要： The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open-structured ligands.

摘要翻译： 本发明提供了一类新的大环化合物以及在金属（例如镧系元素）离子和本发明的化合物之间形成的络合物。 优选的配合物在水性介质中表现出高稳定性以及镧系元素离子发光的高量子产率，而不需要第二活化剂。 优选的化合物在其大环结构内掺入羟基间苯二酰胺部分，其特征在于与各种多肽例如抗体和蛋白质以及高动力学稳定性令人惊奇的低非特异性结合。 这些特征将它们与已知的开放结构的配体区分开来。