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US 2020/0368206 A1Published application
Compositions and methods for delivery of macromolecules
AssigneeThe Regents of the University of California
InventorsNiren Murthy, Joachim Justad Roeise, Chung Hak Taing
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Abstract
The present disclosure provides endosomal disruptors, which are useful for facilitating delivery of a macromolecule to the cytoplasm of a cell. The present disclosure provides compositions comprising an endosomal disruptor and a macromolecule. The present disclosure provides methods of delivering a macromolecule to the cytoplasm of a cell.
Claims20
An endosomal disruptor of the formula (I):
- (M-Z-A-T)-Y (I)
- wherein:
- M is a hydrophilic masking group;
- Z is a cleavable linker capable of cleavage with an endosome to release M and produce an endosomal disrupting surfactant;
- A is a masked hydrophobic group comprising:
- a cyclic group selected from an aryl, a substituted aryl, a heteroaryl, a substituted heteroaryl, a saturated carbocycle, a substituted saturated carbocycle, a heterocycle and a substituted heterocycle;
- and
- a hydrophobic chain;
- T is a hydrophilic tail group:
- and
- Y is an optional group selected from a terminal group, a linker, a chemoselective tag (e.g. configured to conjugate a cell targeting agent or a macromolecule), a member of a specific binding pair, a linked biomolecule and a linked cell delivery agent;
- or a pharmaceutically acceptable salt or a solvate thereof.
9 more elements
Dependencies are inferred from the claim text.