Invention Grant
- Patent Title: Sulfamide linkers for use in bioconjugates
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Application No.: US17135703Application Date: 2020-12-28
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Publication No.: US11957763B2Publication Date: 2024-04-16
- Inventor: Sander Sebastiaan Van Berkel , Ryan Heesbeen , Jorge Merijn Mathieu Verkade , Maria Antonia Wijdeven , Floris Louis Van Delft
- Applicant: SYNAFFIX B.V.
- Applicant Address: NL Oss
- Assignee: SYNAFFIX B.V.
- Current Assignee: SYNAFFIX B.V.
- Current Assignee Address: NL Oss
- Agency: Foley & Lardner LLP
- Agent Sunit Talapatra
- Priority: EP 154739 2016.02.08
- Main IPC: C07K14/00
- IPC: C07K14/00 ; A61K47/68 ; C07K14/435 ; C07K16/32

Abstract:
The invention relates to a novel linker for use in bioconjugates such as antibody-drug-conjugates. The linker according to the invention is represented by formula:
wherein:
BM is a branching moiety;
E is a capping group;
SG is a sulfamide group;
b, c, d, e, g, i, k, l are independently 0 or 1;
f is an integer in the range of 1 to 10;
Sp1, Sp2, Sp3, Sp4, Sp5 and Sp6 are a spacer moieties;
Z1 and Z2 are connecting groups.
The linker according to the invention is useful in the preparation of linker-conjugates and bioconjugates, and can be used for (a) improving conjugation efficiency in the preparation of the bioconjugate, (b) reducing aggregation during the preparation of the bioconjugate and/or of the bioconjugate, (c) increasing stability of the bioconjugate, and/or (d) increasing therapeutic index of the bioconjugate.
wherein:
BM is a branching moiety;
E is a capping group;
SG is a sulfamide group;
b, c, d, e, g, i, k, l are independently 0 or 1;
f is an integer in the range of 1 to 10;
Sp1, Sp2, Sp3, Sp4, Sp5 and Sp6 are a spacer moieties;
Z1 and Z2 are connecting groups.
The linker according to the invention is useful in the preparation of linker-conjugates and bioconjugates, and can be used for (a) improving conjugation efficiency in the preparation of the bioconjugate, (b) reducing aggregation during the preparation of the bioconjugate and/or of the bioconjugate, (c) increasing stability of the bioconjugate, and/or (d) increasing therapeutic index of the bioconjugate.
Public/Granted literature
- US20210353766A1 SULFAMIDE LINKERS FOR USE IN BIOCONJUGATES Public/Granted day:2021-11-18
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