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1. (WO2015114171) SMALL MOLECULE DRUG CONJUGATES

Pub. No.:    WO/2015/114171    International Application No.:    PCT/EP2015/052214
Publication Date: Fri Aug 07 01:59:59 CEST 2015 International Filing Date: Wed Feb 04 00:59:59 CET 2015
IPC: A61K 47/48
A61P 35/00
Applicants: EIDGENOESSISCHE TECHNISCHE HOCHSCHULE ZURICH
Inventors: KRALL, Nikolaus
DECURTINS, Willy
NERI, Dario
SCHEUERMANN, Jörg
WICHERT, Moreno
Title: SMALL MOLECULE DRUG CONJUGATES
Abstract:
A targeted therapeutic agent comprising a compound of formula (I): B–L–D, 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.