Conjugated biological molecules and their preparation

摘要

Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via an amine group; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two amine groups; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via amine groups in said molecule, preferably via a disulphide bridge.;

主权项

1. A process which comprises reacting a compound of the general formulain which one of X and X′ represents a polymer, and the other represents a hydrogen atom;
Q independently represents a linking group; W′ represents an electron-withdrawing group, or, if X′ represents a polymer, X-Q-W′ together represents an electron withdrawing group; A represents a C1-5 alkylene or alkenylene chain; B represents a bond or a C1-4 alkylene or alkenylene chain; and each L independently represents a leaving group;with compounds of the general formulae Z1Nu and Z2Nu in successive steps, wherein Z1 are Z2 are separate proteins, and each Nu independently represents an amine group, or with a compound of the formula Z(Nu)2 in which Z represents a single protein, and each Nu independently represents an amine group.