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A class of radioactive PET imaging agents targeting interferon gene stimulators

A technology targeting imaging agents and stimulating factors, applied in the field of medical imaging, can solve the problem of lack of molecular imaging probes targeting STING, and achieve good chemical stability, high radiochemical yield and specific activity, high Effects of uptake and specificity

Active Publication Date: 2022-04-08
THE FIFTH AFFILIATED HOSPITAL SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the visualization of STING in tumors in vivo to guide clinical medication. The reason is that there is a lack of molecular imaging probes targeting STING.

Method used

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  • A class of radioactive PET imaging agents targeting interferon gene stimulators
  • A class of radioactive PET imaging agents targeting interferon gene stimulators
  • A class of radioactive PET imaging agents targeting interferon gene stimulators

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0026] Synthesis of compound 3-1: when n=1 in the general structural formula, it is compound 3-1, and its labeling route and preparation method are as follows:

[0027]

[0028] The specific marking process includes the following steps:

[0029] 1) Preparation

[0030] Take 1 mL of Kryptofix222 / K prepared in the second step 2 CO 3 Wash the QMA cartridge with the mixed solution of the mixed solution, and collect the eluent; heat the nitrogen blower to 110°C, dry the eluent, and then add 0.5 mL of anhydrous acetonitrile continuously, remove the remaining water by azeotropic distillation, press Cover and cool to room temperature for later use;

[0031] 2) Labeling of compound 2-1:

[0032] Dissolve 2 mg of compound 1-1 in 0.2 mL of anhydrous acetonitrile, extract it with a 1 mL syringe, and add it to the dried [ 18 F] Fluoride ion, Kryptofix222 / K 2 CO 3 In the mixture, the reaction mixture was heated at 90 °C for 20 minutes. After the reaction mixture was cooled to roo...

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Abstract

The invention discloses a class of interferon gene stimulating factor (STING) targeting imaging agent, which is based on the structure of benzothiophene and composed of radionuclide 18 F marker, which can be used for PET imaging of interferon gene stimulators, its general structural formula is shown in formula A, where n=1‑5: formula A where the benzothiophene structure is used as a targeting group, and polyethylene glycol alcohol as a hydrophilic group, 18 F is a radioactive group. The molecular targeting imaging agent has excellent targeting and specificity to interferon gene stimulators, and can be used for PET imaging to monitor inflammation and immune responses produced by tumors. The molecule can specifically distinguish immune responses of different severities, and meets the conditions of being used as an imaging agent for immune monitoring.

Description

technical field [0001] The invention belongs to the technical field of medical imaging, and in particular relates to a PET imaging agent targeting an interferon gene stimulating factor and a marking method and application thereof. Background technique [0002] Inflammation plays an important role in host defense as part of innate immunity and is involved in cellular recovery and regeneration. Inflammation is also closely related to many diseases, such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), atherosclerosis, asthma, lung injury, neurodegenerative diseases (such as Alzheimer's disease), and Cancer, etc., but the pathogenic mechanism is still unclear. Tumor immunotherapy is an effective treatment method to restore the body's normal anti-tumor immune response, control and eliminate tumors. But not all tumor patients can benefit from it, which is mainly due to differences in immune responses in the tumor microenvironment of different patients. [0003] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D333/70C07B59/00A61K51/04A61K101/02
CPCC07D333/70C07B59/002A61K51/0431C07B2200/05
Inventor 单鸿许多李丹肖义泰朱天星
Owner THE FIFTH AFFILIATED HOSPITAL SUN YAT SEN UNIV
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