Method for the synthesis of trifunctional maleimide-antibody complex

摘要

The present invention is directed to a method for extending the length of one of the three linker arms of the compound of Formula I in the production of novel trifunctional antibody-like compounds. Formula I is defined as follows: ##STR1## wherein X is ##STR2## wherein k=1 or 0; wherein Z is ##STR3## wherein s=1 or 0; wherein n=1 or 0;P Pwherein q=1 or 0;PPwherein Y is ##STR4## wherein Y' is ##STR5## wherein p or m may be the same or different and are integers ranging from 0 to 20 with the provisos that when n=0, the sum of m and p is an integer ranging from 1 to 20, whereas when n=1, p and m are each an integer that is at least 1 and the sum of p and m is an integer ranging from 2 to 20; PPwherein R.sup.1 is straight or branched chain lower alkyl having from 1 to 6 carbon atoms or lower alkoxy having from 1-6 carbon atoms; andPPwherein R.sup.2 is hydrogen, phenyl, --COOH, or straight or branched chain lower alkyl having from 1-6 carbon atoms, with the proviso that the lower alkyl moiety may be mono substituted by --NH.sub.2, --OH, or --COOH.PPThe compound of the present invention is useful as a trivalent coupling agent for linking Fab'-like fragments to form both bifunctional and trifunctional antibody-like compounds.