Process for preparing immunoconjugates
AssigneeMerck Patent GmbH
InventorsMohammad Jalalian, Arnulf Heubner, Bernd Reckmann
Life of this patent
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Abstract
The invention relates to a novel process for preparing immunoconjugates consisting of haptens which are sparingly soluble or insoluble in aqueous solution and proteins/polypeptides using special solvents, in particular diethylene glycol monoalkyl ethers.
Claims21
A process for preparing an immunoconjugate comprising a hapten (A) which is sparingly soluble in aqueous solution and a protein or polypeptide (B), comprising coupling (A) and (B) in a solvent, with the optional inclusion of a crosslinker or spacer, wherein the solvent is:
- a diethylene glycol monoalkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- a diethylene glycol dialkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- 1,3-dimethyl-2-imidazolidinone;
- gamma-butyrolactone;
- glycerol formal;
- 2,2-dimethyl-4-hydroxymethyl-1,3-dioxolane;
- or a mixture thereof,
- and wherein the content of water in said solvent is from 0% to about 30% (v/V).
In a process of preparing a conjugate comprising a hapten and a protein or polypeptide, the improvement comprising coupling said hapten to the protein or polypeptide in a solvent, wherein the solvent is:
- a diethylene glycol monoalkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- a diethylene glycol dialkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- 1,3-dimethyl-2-imidazolidinone;
- gamma-butyrolactone;
- glycerol formal;
- 2,2-dimethyl-4-hydroxymethyl-1,3-dioxolane;
- or a mixture thereof,
- and wherein the content of water in said solvent is from 0% to about 30% (v/v).
A mixture containing a conjugate and a solvent, wherein the conjugate comprises:
- (A) a hapten which is sparingly soluble in aqueous solution,
- (B) a protein or polypeptide, and
- (C) optionally, a crosslinker or spacer, and the solvent is:
- a diethylene glycol monoalkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- a diethylene glycol dialkyl ether, wherein the alkyl group is C.sub.1 -C.sub.6 ;
- 1,3-dimethyl-2-imidazolidinone;
- gamma-butyrolactone;
- glycerol formal;
- 2,2-dimethyl-4-hydroxymethyl-1,3-dioxolane;
- or a mixture thereof,
- and wherein the content of water in said solvent is from 0% to about 30% (v/v).
Dependencies are inferred from the claim text.