Targeted tumor PD-L1 PET (Polyethylene Terephthalate) imaging agent labeling precursor, imaging agent as well as synthesis method and application of imaging agent
The invention discloses a PET (Polyethylene Terephthalate) imaging agent labeled precursor for targeting tumor PD-L1, an imaging agent as well as a synthesis method and application of the imaging agent. The structure of the PET imaging agent labeled precursor is as shown in a formula I in the specification. According to the present invention, the design is scientific, the conception is ingenious, the action mode of the molecule and the target protein is creatively explored by using the theoretical calculation, and the appropriate Linker and the chelating fragment are introduced according to the property of the molecule so as to design the novel tumor targeting PD-L1 macrocyclic peptide nuclide precursor; and the combination mode of the precursor is explored through theoretical calculation, and the reasonability of the design is verified. After the precursor compound is labeled with < 68 > Ga, a compound shown in a formula II can be obtained, and the compound has good stability, excellent pharmacokinetics, good binding specificity with tumor PD-L1, relatively high tumor uptake and relatively high tumor to muscle uptake ratio, and has a good clinical application prospect..
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Patent| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Europäisches Patentamt - (2023) vom: 29. Aug. Zur Gesamtaufnahme - year:2023 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
GE SHUSHAN [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2023-08-29, Last update posted on www.tib.eu: 2023-12-05, Last updated: 2023-12-08 |
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| Patentnummer: |
CN116655744 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA018528570 |
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| 520 | |a The invention discloses a PET (Polyethylene Terephthalate) imaging agent labeled precursor for targeting tumor PD-L1, an imaging agent as well as a synthesis method and application of the imaging agent. The structure of the PET imaging agent labeled precursor is as shown in a formula I in the specification. According to the present invention, the design is scientific, the conception is ingenious, the action mode of the molecule and the target protein is creatively explored by using the theoretical calculation, and the appropriate Linker and the chelating fragment are introduced according to the property of the molecule so as to design the novel tumor targeting PD-L1 macrocyclic peptide nuclide precursor; and the combination mode of the precursor is explored through theoretical calculation, and the reasonability of the design is verified. After the precursor compound is labeled with < 68 > Ga, a compound shown in a formula II can be obtained, and the compound has good stability, excellent pharmacokinetics, good binding specificity with tumor PD-L1, relatively high tumor uptake and relatively high tumor to muscle uptake ratio, and has a good clinical application prospect. | ||
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