The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 04, 2020

Filed:

Mar. 30, 2015
Applicants:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Ambrx, Inc., La Jolla, CA (US);

Inventors:

Robert M. Garbaccio, Lansdale, PA (US);

Jeffrey Kern, Gilbertsville, PA (US);

Philip E. Brandish, Needham, MA (US);

Sanjiv Shah, Wakefield, MA (US);

Linda Liang, Mountain View, CA (US);

Ying Sun, San Diego, CA (US);

Jianing Wang, San Diego, CA (US);

Nick Knudsen, Escondido, CA (US);

Andrew Beck, San Diego, CA (US);

Anthony Manibusan, San Diego, CA (US);

Dennis Gately, San Diego, CA (US);

Assignees:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Ambrx, Inc., La Jolla, CA (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07J 71/00 (2006.01); A61K 47/54 (2017.01); C07F 9/09 (2006.01); C07K 16/28 (2006.01);
U.S. Cl.
CPC ...
C07K 16/2866 (2013.01);
Abstract

Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).


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