申请人:Medgenix Group S.A.
公开号:US05276147A1
公开(公告)日:1994-01-04
The subject of the present invention is compounds which correspond to the following general formula: ##STR1## in which R.sub.1 and R.sub.3 independently of one another represent H, an alkyl, alkenyl, cycloalkyl, aryl, arylalkyl or an alkylaryl group, a heterocycle, or groups which are unsubstituted or substituted, in particular by one or more hydroxyl or alkoxy groups or halogen; n represents an integer from 1 to 5; i in each case takes values from 1 to n for the n successive ##STR2## links; R.sub.2, R.sub.4.sup.i and R.sub.5.sup.i independently of one another represent H, an alkyl, alkenyl, aryl, alkoxy, hydroxyalkyl, alkoxyalkyl, amido, acyl or carboxyalkyl group, or a salt, or an alkyl ester of the latter; or R.sub.4.sup.i and R.sub.5.sup.i together form an oxo group ##STR3## R.sub.6 and R.sub.7 represent H, or R.sub.6 and R.sub.7 together form an oxo group ##STR4## x represents a 5- or 6-membered heterocycle which contains at least one nitrogen atom, or, in the event that ##STR5## where R.sub.8 and R.sub.9 independently represent H, alkyl, aryl or arylalkyl, and R.sub.10 represents H, alkyl, aryl or arylalkyl. The present invention likewise relates to coordination complexes between these ligands and a metal as well as to kits containing these ligands and to reagents which permit the formation of a coordination complex between the ligand and the metals. More particularly, the present invention relates to complexes between these ligands and technetium .sup.99m Tc, which complexes can be used as diagnostic agents for brain imaging, heart imaging and blood imaging.
本发明的主题是与以下一般式相对应的化合物:##STR1## 其中R.sub.1和R.sub.3独立地表示H、烷基、烯基、环烷基、芳基、芳基烷基或烷基芳基基团、杂环、或未取代或取代的基团,特别是一个或多个羟基或烷氧基或卤素;n表示1到5的整数;i在每个n个连续的##STR2##链的情况下取值从1到n;R.sub.2、R.sub.4.sup.i和R.sub.5.sup.i独立地表示H、烷基、烯基、芳基、烷氧基、羟基烷基、烷氧基烷基、酰胺、酰基或羧基烷基团或其烷基酯;或R.sub.4.sup.i和R.sub.5.sup.i结合形成一个氧代基##STR3## R.sub.6和R.sub.7表示H,或者R.sub.6和R.sub.7一起形成一个氧代基##STR4## x表示含有至少一个氮原子的5-或6-成员杂环,或者在##STR5##的情况下,其中R.sub.8和R.sub.9独立地表示H、烷基、芳基或芳基烷基,R.sub.10表示H、烷基、芳基或芳基烷基。本发明还涉及这些配体与金属之间的配位复合物,以及包含这些配体的试剂盒和允许配体与金属形成配位复合物的试剂。更具体地说,本发明涉及这些配体与锝.sup.99m Tc之间的复合物,这些复合物可用作用于脑成像、心脏成像和血液成像的诊断剂。