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Patent US10722591
Issued 2020-07-28
Cleavable Conjugates Of Tlr7/8 Agonist Compounds, Methods For Preparation, And Uses Thereof
The present disclosure relates to cleavable conjugates (for example, particle-based or antibody-based conjugates) of TLR7/8 agonists (for example, 1H-imidazo[4,5-c]quinoline derivatives) containing a conjugation linker, a cleavable linker, and a self-eliminating linker. The present disclosure also related to methods for preparation of the cleavable conjugates, uses thereof for stimulating an effective immune response, and uses thereof for the treatment of cancer.
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- 1. A compound of formula (I):
F—[W-L3-L2-L1-D]x (I)
D is a TLR7/8 agonist moiety; L1 is a self-eliminating linker; L2 is a cleavable linker; L3 is a conjugation linker; W is O, S, or N10; R10 is H or C1-C8 alkyl; x is an integer from 1 to 500; F is a conjugation moiety; and the TLR7/8 agonist moiety is a 1H-imidazo[4,5-c]quinoline derivative.
