Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Technetium-99m-labeled isonitrile-containing PEG chain modified FAPI derivative as well as preparation method and application thereof

A technology of CN-PEG-FAPI and derivatives, which is applied in the field of FAPI derivatives and preparation, and can solve the problem of low uptake value

Active Publication Date: 2021-08-03
BEIJING NORMAL UNIVERSITY
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative in 2020 (patent application number: 202011382815.2), but the uptake of the drug in tumors is low and it is taken up in non-target organs such as liver and kidney Higher, so the performance is more excellent 99m Tc-labeled FAPI tumor imaging agent is worth developing

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Technetium-99m-labeled isonitrile-containing PEG chain modified FAPI derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing PEG chain modified FAPI derivative as well as preparation method and application thereof
  • Technetium-99m-labeled isonitrile-containing PEG chain modified FAPI derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0029] The present invention is described in detail below through the examples: a technetium-99m-labeled isonitrile-containing PEG chain-modified FAPI derivative, the general structural formula of which is [ 99m Tc-(CN-PEG-FAPI) 6 ] + , its structural formula is as follows:

[0030]

[0031] In the structural formula: with 99m Tc +The core is the central core, and the carbon atom of the isonitrile in the ligand molecule of CN-PEG-FAPI and 99m Tc(I) coordinates to form a six-coordinated [ 99m Tc-(CN-PEG-FAPI) 6 ] + Complexes. n is an integer greater than 0.

[0032] A method for preparing FAPI derivatives modified by technetium-99m-labeled PEG chains containing isocyanides, the preparation steps are as follows:

[0033] a: Synthesis of ligand CN-PEG-FAPI:

[0034] Weigh an appropriate amount of FAPI into a round bottom flask, add an appropriate amount of DMF to dissolve, then add an appropriate amount of triethylamine and compound 1, and react at room temperature. ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a technetium-99m-labeled isonitrile-containing PEG chain modified FAPI derivative with a structural general formula of [<99m>Tc-(CN-PEG-FAPI)6]<+>, and a preparation method and an application thereof. The [<99m>Tc-(CN-PEG-FAPI)6]<+> complex is obtained through two steps of synthesis of a ligand CN-PEG-FAPI and preparation of the [<99m>Tc-(CN-PEG-FAPI)6]<+>. The complex is simple and convenient to prepare, high in radiochemical purity, good in stability, low in non-target organ uptake in tumor-bearing mice, high in uptake and good in retention in tumor parts, and specific in uptake in tumors, and is a novel tumor imaging agent with popularization and application values.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, in particular to a technetium-99m labeled isonitrile-containing PEG chain-modified FAPI derivative, a preparation method and an application. Background technique [0002] Fibroblast activating protein (FAP) is an important target in tumor diagnosis and treatment in recent years, and the use of radionuclide-labeled fibroblast activating protein inhibitor (FAPI) and its derivatives as tumor radiopharmaceuticals has become a current research hotspot. Our research group developed a technetium-99m-labeled isocyanide-containing FAPI derivative in 2020 (patent application number: 202011382815.2), but the uptake of the drug in tumors is low and it is taken up in non-target organs such as liver and kidney Higher, so the performance is more excellent 99m Tc-labeled FAPI tumor imaging agent is worth developing. [0003] Polyethylene glycol (PEG) is a neutral, non-toxic high molecular polymer with uniq...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D401/12C07F13/00A61K51/06C08G65/333
CPCC07D401/12C07F13/005A61K51/065C08G65/33396Y02P20/55
Inventor 张俊波阮晴江雨豪冯俊红王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com