申请人:Amersham International plc
公开号:US05690904A1
公开(公告)日:1997-11-25
Tetradentate ligands are used to form neutral 99m-technetium complexes which may be useful as radiopharmaceuticals e.g. as brain imaging agents. The ligands have the structure ##STR1## where n is 2 or 3, m is 0-4, R is H or substituted or unsubstituted C.sub.1 -C.sub.6 alkyl, provided that one CR.sub.2 group adjacent the starred nitrogen atom represents CO and forms with the adjacent N atom, a --CONH-- amide group, Y is unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, and one of X and X' represents H or a labile thiol protecting group while the other is unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, alkenyl or alkynyl.
四齿配体被用来形成中性的99m锝配合物,这些配合物可能用作放射性药物,例如用作脑成像剂。这些配体具有结构##STR1##其中n为2或3,m为0-4,R为H或取代或未取代的C.sub.1 -C.sub.6烷基,条件是与星号氮原子相邻的一个CR.sub.2基团代表CO,并与相邻的N原子形成一个--CONH--酰胺基团,Y为未取代或取代的C.sub.1 -C.sub.6烷基,X和X'中的一个代表H或一种不稳定的硫醇保护基,而另一个是未取代或取代的C.sub.1 -C.sub.6烷基、烯基或炔基。