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;
R¹ 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.
药物与
抗体或抗原识别片段的共轭物是用
丙二酸盐组成的连接体制备的,其连接体的
化学式为
式中
Ab 是
抗体或其抗原识别片段,它能识别与
细胞相关的抗原,而药物正是要输送到细胞中;
Q 是-NH-、-O-或-S-;
R-Q- 是具有可反应的
氨基、羟基或
硫醇功能的药物残基;
R¹ 是
羧酸保护基团;
Y 是-O-、-NH-、-NCH₃- 或-NC₂H₅-;
n 是 1 至 8 的整数;
m 是 1 至约 10 的整数。