Small Molecule Drug Conjugates

摘要

A targeted therapeutic agent comprising a compound of formula I:;B-L-D  (I),;wherein: B is a low molecular weight binding moiety for Carbonic Anhydrase IX (CAIX); D is a drug moiety; and L is a linker group that undergoes cleavage in vivo for releasing said drug moiety in an active form. The drug moiety is suitably a cytotoxic agent for targeted delivery to cancer cells expressing CAIX. The binding moiety B suitably comprises a sulfonamidothiadiazole moiety. The binding moiety B may comprise one, two or more groups capable of binding to CAIX. The linker group suitably comprises a disulfide bond and/or a triazole group and/or a cleavable peptide group.

主权项

1. A targeted therapeutic agent comprising a compound of formula:
B-L-D  (I), wherein:
B is a low molecular weight binding moiety for Carbonic Anhydrase IX (CAIX);D is a drug moiety;L is a linker that undergoes cleavage in vivo for releasing said drug moiety in an active form;
wherein said linker comprises a polar or charged moiety; and
wherein said polar or charged moiety is an oligomer comprising from 1 to about 20 monomers selected from the group consisting of natural and non-natural amino acids, saccharides, (meth)acrylic acid and salts thereof, hydroxyethyl (meth)acrylate, and ethylene glycol.