HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF

The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety c...

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Bibliographic Details
Main Authors LIN, Shih-Yao, HSIEH, Yu-Chi, HUANG, Chiu-Chen, LIN, Rong-Hwa
Format Patent
LanguageEnglish
Published 22.04.2021
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Summary:The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.
Bibliography:Application Number: US202017118228