Cross-linking agents, their use and preparation.

摘要

Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula: L-S-(CH2)n1-CONH-SPACER-NH-X wherein L is a leaving group selected from -H or -S-Ar, wherein Ar represents optionally substituted phenyl or pyridyl; n1=2-4; X is selected from: -CO-Y-CONHNH2, a hydrazide; <CHEM> -CO-Y-NH-CONHNH2, a semicarbazide; and -CO-Z-NH-CSNHNH2, a thiosemicarbazide; wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof; the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from a) -(CH2)n2-O-(CH2)n2-O-(CH2)n2- wherein each n2 is independently 2-4 and b) -CH2- @@-CH2)-O-(CH2)n3-O-CH2- @@-CH2- wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of omega -mercaptocarboxylic acids which lack SPACER diamine.