Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes

US10434197B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-10434197-B2
Application numberUS-201113811568-A
CountryUS
Kind codeB2
Filing dateJul 21, 2011
Priority dateJul 23, 2010
Publication dateOct 8, 2019
Grant dateOct 8, 2019

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

Official abstract text for this publication.

A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.

First claim

Opening claim text (preview).

What is claimed is: 1. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct. 2. The Diels-Alder adduct of claim 1 , wherein the tetrazine residue of the Diels-Alder adduct is covalently bound to a biomolecule. 3. The Diels-Alder adduct of claim 2 , wherein the biomolecule is in an animal or human. 4. The Diels-Alder adduct of claim 2 , wherein the tetrazine residue is a residue formed by reaction of the biomolecule with a compound according to structure 13 5. The Diels-Alder adduct of claim 2 , wherein the tetrazine residue is a residue formed by reaction of the biomolecule with a compound according to structure 24 6. The Diels-Alder adduct of claim 2 , wherein the radionuclide is 18 F. 7. The Diels-Alder adduct of claim 6 , wherein the trans-cyclooctene residue is a residue of the compound according to structure 9 8. The Diels-Alder adduct of claim 6 , wherein the trans-cyclooctene residue is a residue of the compound according to structure 17 9. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 5 10. The compound according to structure 9 11. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the trans-cyclooctene residue is a residue of the compound according to structure 17 12. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 13 13. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 24 14. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 14 15. The compound according to structure 15 16. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 18 17. The compound according to structure 19 18. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the adduct is the compound according to structure 20 19. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 22 20. A Diels-Alder adduct of a trans-cyclooctene with a tetrazine, wherein the adduct bears a substituent labeled with a radionuclide, wherein the substituent is a substituent on the trans-cyclooctene residue of the Diels-Alder adduct, wherein the tetrazine residue is a residue of the compound according to structure 29 21. The compound accordina to structure 31

Assignees

Inventors

Classifications

  • containing three or more hetero rings · CPC title

  • linked by a chain containing hetero atoms as chain links · CPC title

  • conjugates with a carrier being an organic compounds · CPC title

  • C07D257/08Primary

    Six-membered rings · CPC title

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What does patent US10434197B2 cover?
A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.
Who is the assignee on this patent?
Fox Joseph M, Hassink Matthew, Blackman Melissa, and 5 more
What technology area does this patent fall under?
Primary CPC classification A61K51/0497. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Oct 08 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).