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1. (WO2018004338) CLEAVABLE TETRAZINE USED IN BIO-ORTHOGONAL DRUG ACTIVATION

Pub. No.:    WO/2018/004338    International Application No.:    PCT/NL2017/050427
Publication Date: Fri Jan 05 00:59:59 CET 2018 International Filing Date: Wed Jun 28 01:59:59 CEST 2017
IPC: A61K 47/54
A61K 47/69
B82Y 5/00
C07D 257/08
Applicants: TAGWORKS PHARMACEUTICALS B.V.
Inventors: ROBILLARD, Marc Stefan
TEN HOEVE, Wolter
HOEBEN, Freek Johannes Maria
VERSTEEGEN, Ronny Mathieu
JANSSEN, Hendricus Marie
VAN ONZEN, Arthur Henry Antoon Marie
ROSSIN, Raffaella
Title: CLEAVABLE TETRAZINE USED IN BIO-ORTHOGONAL DRUG ACTIVATION
Abstract:
Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit comprising a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine comprising a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of said Construct.