Antikörper-Arzneimittel Konjugale

摘要

Conjugates of drugs and antibodies or antigen-recognising fragments are prepared with a linker consisting of a malonate; of the formula wherein Ab is an antibody or antigen-recognizing fragment thereof, which recognizes an antigen associated with a cell to which delivery of the drug is desirable; Q is -NH-, -O-, or -S-; R-Q- is the residue of a drug having a reactively-available amino, hydroxy or thiol function; R<1> is a carboxylic acid protecting group; Y is -O-, -NH-, -NCH3- or -NC2H5-; n is an integer from 1 to about 8; m is an integer from 1 to about 10.