Invention Grant
- Patent Title: Phosphate based linkers for intracellular delivery of drug conjugates
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Application No.: US15301564Application Date: 2015-03-30
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Publication No.: US10550190B2Publication Date: 2020-02-04
- Inventor: Robert M. Garbaccio , Jeffrey Kern , Philip E. Brandish , Sanjiv Shah , Linda Liang , Ying Sun , Jianing Wang , Nick Knudsen , Andrew Beck , Anthony Manibusan , Dennis Gately
- Applicant: Merck Sharp & Dohme Corp. , Ambrx, Inc.
- Applicant Address: US NJ Rahway US CA La Jolla
- Assignee: Merck Sharp & Dohme Corp.,Ambrx, Inc.
- Current Assignee: Merck Sharp & Dohme Corp.,Ambrx, Inc.
- Current Assignee Address: US NJ Rahway US CA La Jolla
- Agent David Van Goor; Anna Cocuzzo
- International Application: PCT/US2015/023247 WO 20150330
- International Announcement: WO2015/153401 WO 20151008
- Main IPC: C07J71/00
- IPC: C07J71/00 ; A61K47/54 ; C07F9/09 ; C07K16/28

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).
Public/Granted literature
- US20170182181A1 PHOSPHATE BASED LINKERS FOR INTRACELLULAR DELIVERY OF DRUG CONJUGATES Public/Granted day:2017-06-29
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