TARGETING RADIOACTIVE IMMUNOREAGENTS

摘要

A targeting radioactive immunoreagent comprises a metal radionuclide ion, a complexing agent, and an immunoreactive group covalently bonded to said complexing agent, the complexing agent having structure (A-I), wherein R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R1 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R2 represents hydroxy, carboxy, hydroxyalkyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, hydrazinylylidenediacetic acid, or a salt of such acids, or two R2 groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one, preferably two alkylene groups forming part of the ring structure; R3 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R4 represents hydrogen or a protein reactive group; n is 0 to 4, o is 0 or 1, m is 0 or 1; provided that at least one of n and m is 0 and at least one of R, R?1, R3 and R4¿ is a protein reactive group. In a composition of matter aspect, this invention provides novel terpyridines and phenanthrolines. Preferred terpyridines have the structure (A-I) above wherein n=1, m=0 and R is a substituted phenyl containing an alkyl or alkoxy substituent and a protein reactive group. Preferred phenanthrolines have the structure (A-I) above wherein n=0, m=1 and at least one R4 is a protein reactive group. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.