Invented by Marc Stefan Robillard, Ronny Mathieu Versteegen, Wolter ten Hoeve, Raffaella Rossin, Tagworks Pharmaceuticals BV

Chemically cleavable groups are becoming increasingly popular in the field of drug discovery and development. These groups are designed to be attached to drug molecules and can be selectively removed under specific conditions, allowing for the release of the active drug at the desired site of action. This technology has the potential to revolutionize drug delivery and improve the efficacy and safety of drugs. The market for chemically cleavable groups is expected to grow significantly in the coming years. According to a report by MarketsandMarkets, the global market for chemically cleavable groups is projected to reach $1.3 billion by 2025, growing at a CAGR of 6.5% from 2020 to 2025. The increasing demand for targeted drug delivery systems, the growing prevalence of chronic diseases, and the need for more efficient drug development processes are some of the key factors driving the growth of this market. One of the major advantages of chemically cleavable groups is their ability to improve the pharmacokinetics and pharmacodynamics of drugs. By attaching these groups to drug molecules, researchers can control the release of the drug and ensure that it reaches the desired site of action. This can help to reduce the side effects of drugs and improve their efficacy. Chemically cleavable groups are also being used to develop new drug delivery systems. For example, researchers are exploring the use of these groups in the development of prodrugs, which are inactive drug molecules that are converted into active drugs once they are inside the body. By using chemically cleavable groups, researchers can design prodrugs that are activated only in specific tissues or cells, reducing the risk of toxicity and improving the therapeutic index. The market for chemically cleavable groups is highly competitive, with several companies offering a range of products and services. Some of the key players in this market include Merck KGaA, Thermo Fisher Scientific, and Sigma-Aldrich Corporation. These companies are investing heavily in research and development to develop new and innovative chemically cleavable groups and drug delivery systems. In conclusion, the market for chemically cleavable groups is expected to grow significantly in the coming years, driven by the increasing demand for targeted drug delivery systems and the need for more efficient drug development processes. This technology has the potential to revolutionize drug delivery and improve the efficacy and safety of drugs, making it an exciting area of research and development for the pharmaceutical industry.

The Tagworks Pharmaceuticals BV invention works as follows

The use of reactive components from the Diels-Alder reaction with inverse electron demand for chemical masking and demasking in vitro is disclosed. This method can be used in chemical reactions, and in particular, in the synthesis biomolecules. On solid supports. “The reactice components include a dienophile (especially a trans-cyclooctene) and a diene (particularly a tetrazine).

Background for Chemically cleavable groups

Trigger

Activator

EXAMPLES

Further Considerations Regarding the Actuator

Construct-Trigger

The Combination and Reaction between the Construct-Trigger Activator and the Activator

Spacers

Further embodiment 1

Further embodiment 2

Further embodiment 3

EXAMPLES

General Examples

Example 1

3,6-dibenzyl-1,2,4,5-tetrazine (4)

Synthesis of 3,6-diisopropyl-1,2,4,5-tetrazine (5)

3,6-dimethyl-1,2,4,5-tetrazine (8)

3-methyl-6-(pyridin-3-yl)-1,2,4,5-tetrazine (10)

3-methyl-6-(pyridin-4-yl)-1,2,4,5-tetrazine (11)

3-methyl-6-(3-methylpyridin-2-yl)-1,2,4,5-tetrazine (12)

3-methyl-6-phenyl-1,2,4,5-tetrazine (14)

Example 2

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