Tetrazines/trans-cyclooctenes in solid phase synthesis of labeled peptides
US-2015359913-A1 · Dec 17, 2015 · US
US10183082B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10183082-B2 |
| Application number | US-201515505214-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 9, 2015 |
| Priority date | Sep 9, 2014 |
| Publication date | Jan 22, 2019 |
| Grant date | Jan 22, 2019 |
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18 F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-mino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an 18 F. The 18 F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.
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We claim: 1. An 18 F labeled IDO1 imaging construct, comprising a molecule having the following structure: 2. A method of performing positron emission tomography (PET), comprising injecting a solution comprising an 18 F labeled IDO1 imaging construct into a patient suspected of having cancer; and imaging the patient with PET, wherein the 18 F labeled IDO1 imaging construct comprises a molecule having the following structure: 3. The method according to claim 2 , wherein the cancer is breast cancer. 4. The method according to claim 2 , further comprising administering a treatment for the cancer to the patient before, during, or after injecting the solution. 5. The method according to claim 4 , wherein the treatment comprises administration of surgery, radiation, chemotherapy, immunotherapy, or a combination of two or more of the foregoing. 6. The method according to claim 4 , wherein the treatment comprises administering an inhibitor of indoleamine 2,3-dioxygenase-1 (IDO1) to the patient. 7. The method according to claim 4 , wherein the treatment comprises administering a combination of an inhibitor of indoleamine 2,3-dioxygenase-1 (IDO1) and a different cancer treatment simultaneously or consecutively. 8. The method according to claim 4 , wherein the patient is human. 9. A method for treating cancer in a patient, comprising administering a treatment for the cancer to the patient; and injecting a solution comprising an 18 F labeled IDO1 imaging construct into the patient, wherein the 18 F labeled IDO1 imaging construct comprises a molecule having the following structure:
having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole · CPC title
1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles · CPC title
having two nitrogen atoms and only one oxygen atom · CPC title
Preparations for testing in vivo · CPC title
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