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Small Molecule Drug Conjugates
专利权人:
Philochem AG
发明人:
Nikolaus Krall,Willy Decurtins,Dario Neri,Jörg Scheuermann,Moreno Wichert
申请号:
US15226439
公开号:
US20170035892A1
申请日:
2016.08.02
申请国别(地区):
US
年份:
2017
代理人:
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.
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