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US 12,090,211 B2Granted
Methods for preparing antibody drug conjugates
AssigneeGenentech, Inc.
InventorsThomas Pillow, Peter Dragovich
Life of this patent
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Abstract
The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.
Claims13
An antibody-drug conjugate of Formula IV:
- or a pharmaceutically acceptable salt thereof, wherein
- Ab is an antibody;
- R1, R2, R3, and R4 are independently selected from the group consisting of H, optionally substituted branched or linear C1-C5 alkyl, and optionally substituted C3-C6 cycloalkyl, or R3 and R4 taken together with the carbon atom to which they are bound form a C3-C6 cycloalkyl ring,
- wherein said optionally substituted alkyl or cycloalkyl may be substituted with alkyl, cycloalkyl, aryl, heteroaryl, hydroxyl, nitrile, halo, alkoxy, haloalkoxy, arylalkoxy, acyloxy, alkylthio, sulfonate, amino, alkylamino, acylamino, carbamoyl, alkylcarbamoyl, or nitro;
- D is:
- wherein the carbonyl in Formula IV is covalently bonded to the secondary nitrogen in D;
- and
- p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.
5 more elements
Dependencies are inferred from the claim text.