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Patent US10722591

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 Independent Claims

  • Claim 1. A compound of formula (I): F--[W-L.sup.3-L.sup.2-L.sup.1-D].sub.x (I) wherein: D is a TLR7/8 agonist moietyL.sup.1 is a self-eliminating linkerL.sup.2 is a cleavable linkerL.sup.3 is a conjugation linkerW is O, S, or N.sup.10R.sup.10 is H or C.sub.1-C.sub.8 alkylx is an integer from 1 to 500F is a conjugation moietyand the TLR7/8 agonist moiety is a 1H-imidazo[4,5-c]quinoline derivative.

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