CONJUGATED PROTEINS AND PEPTIDES

摘要

Novel compounds of the general formula:;;in which X represents a polymer,

Q represents a linking group;

W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety;

each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and

either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR2 via two nucleophilic moieties.

主权项

1. A process for the preparation of a compound of the general formula:in which X represents a polymer,
Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR2 via two nucleophilic moieties;which comprises reacting a compound of the general formula:
X-Q-W′-CR1R1′—CR2.L.L′  (II)in which X and Q have the meanings given for the general formula I;
W′ represents an electron-withdrawing moiety; either R1 represents a hydrogen atom or a C1-4alkyl group, R1′ represents a hydrogen atom, and each of L and L′ independently represents a leaving group; or R1 represents a hydrogen atom or a C1-4alkyl group, L represents a leaving group, and R1′ and L′ together represent a bond; or R1 and L together represent a bond and R1′ and L′ together represent a bond; and R2 represents a hydrogen atom or a C1-4 alkyl group;with a protein or a peptide containing at least one nucleophilic group, and optionally subsequently with a second molecule containing a nucleophilic group;and if desired, converting the resulting compound of the general formula I in which W represents an electron-withdrawing moiety into a corresponding compound in which W represents a moiety preparable by reduction of an electron-withdrawing moiety.