申请人:PRESIDENT AND FELLOWS OF HARVARD COLLEGE
公开号:EP1238978A2
公开(公告)日:2002-09-11
The compounds of the present invention comprise a tropane compound or ligand that selectively binds to tropane recognition sites, e.g., neuron transporters such as that DAT. The tropane ligand is radiolabeled with a radioactive technetium or rhenium by a chelating ligand which is attached to the tropane ligand by a linker.
Tropane compounds or ligands useful in the pratice of the present invention can generally be represented by formula II where R1 and R2 are defined as above and where R1 can also be substituted at the C4 position of the tropane ring:
Any tropane compound of the general formula II is useful in the present invention so long as it binds to DAT.
Useful tropane analogs have a 3α-group,i.e., are of the boat configuration. Intermediates for the synthesis of the radiolabeled tropanes are claimed.
本发明的化合物包括一种选择性地结合到对氮杂环戊烷识别位点(如神经元转运体,如 DAT)的对氮杂环戊烷化合物或配体。通过螯合配体对托烷配体进行放射性锝或铼标记,螯合配体通过连接体连接到托烷配体上。
在本发明实践中有用的托烷化合物或配体一般可用式 II 表示,其中 R1 和 R2 的定义如上,R1 也可以在托烷环的 C4 位被取代:
只要能与 DAT 结合,通式 II 的任何托烷化合物在本发明中都是有用的。
有用的托烷类似物具有 3α 基团,即具有舟形构型。本发明要求合成放射性标记的托烷的中间体。