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US 11,666,581 B2Granted
PROTAC antibody conjugates and methods of use
AssigneeGenentech, Inc.
InventorsThomas Pillow, Jack Sadowsky, Leanna Staben, Steven Staben, Binqing Wei, Ingrid Wertz, Pragya Adhikari, Nicole Blaquiere, Peter Dragovich, Wayne Fairbrother
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Abstract
The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
Claims22
A conjugate having the chemical structure
- Ab-(L1-D)p,
- wherein
- D is a PROTAC having the structure E3LB-L2-PB, wherein
- E3LB is an E3 ligase binding group covalently bound to L2, wherein the E3 ligase is a tetrahydro-benzodiazepinone or a pharmaceutically acceptable salt thereof, and
- wherein E3LB is
- L2 is a linker covalently bound to E3LB and PB, and
- PB is a protein binding group covalently bound to L2;
- Ab is an antibody covalently bound to L1;
- L1 is a linker covalently bound to Ab and D;
- and
- p has a value from about 1 to about 8.
8 more elements
Dependencies are inferred from the claim text.