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