申请人:NEORX CORPORATION
公开号:EP0289187A2
公开(公告)日:1988-11-02
Vinyl radiohalogenated small molecules as shown in formulae I and II:
wherein 'X is a radiohalogen, C = C is a double bond, R, and R2 represent a hydrogen atom: alkyl or substituted alkyl group, an aryl or substituted aryl group, a heteroalkyl group, a heteroaryl group, or a mixed alkylaryl group.
Y represents any of the groups as for R1 and R2, except that Y cannot be hydrogen, and bearing a functional group suitable for binding to protein under conditions that preserve the biological activity of the protein. The compounds of formulae I and II can be coupled to proteins such as monoclonal antibodies to provide reagents for diagnostic and therapeutic applications. Also metalated precursors of compounds I and II, as well as radiopharmaceutical reagent kits containing any of the subject small molecules.
乙烯基放射性卤化小分子,如式 I 和 II 所示:
其中'X 是放射卤素,C=C 是双键,R 和 R2 代表氢原子:烷基或取代烷基、芳基或取代芳基、杂烷基、杂芳基或混合烷芳基。
Y 代表与 R1 和 R2 相同的任何基团,但 Y 不能为氢,并带有适合在保持蛋白质生物活性的条件下与蛋白质结合的官能团。式 I 和式 II 的化合物可与蛋白质(如单克隆抗体)结合,为诊断和治疗应用提供试剂。此外,式 I 和式 II 化合物的金属化前体,以及含有上述任何小分子的放射性药物试剂盒。