Thiazolidine linker for the conjugation of drugs to antibodies

摘要

In one aspect, there is provided a protein-drug conjugate compound comprising a protein covalently attached by a linker to one or more drug moieties, wherein the linker has a half-life of from 1 hour to 50 hours in phosphate buffered saline at 37° C. A carbonyl derivative of LU103793 is also described that can be used in a protein-drug conjugate compound comprising an antibody covalently attached by a linker to the drug moiety comprising, consisting or consisting essentially of the carbonyl derivative.

主权项

1. An antibody-drug conjugate comprising a protein attached by a linker to one or more drugs, wherein the linker comprises a heterocyclic 1,3-substituted five- or six-member ring, having the following structure: wherein X and Y are, each independently, selected from the group consisting of sulphur, nitrogen and oxygen wherein n, m independently vary between 0 and 1, provided that n and m are not both 0; and wherein R1 and/or R2 are selected from the group consisting of a drug or an antibody molecule to which the linker is attached, and wherein the linker has a half-life of from about 1hour to about 50 hours in phosphate buffered saline at 37° C.