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99mtc marked multivalence sugar fan-shaped dendrimer complex, application thereof, multivalence sugar fan-shaped dendrimer ligand and preparation method thereof

A dendrimer, polyvalent saccharide technology, applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, which can solve the problems of slow clearance rate, influence on accurate assessment of liver function, influence on affinity, etc.

Active Publication Date: 2016-06-15
INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

The number of coupled galactosyl groups (sugar density) on each molecular backbone will affect the affinity of ASGPr, and then affect its pharmacokinetic properties in vivo; on the other hand, due to the large polymer ASGPr probe The molecular size of the molecule makes it often have high non-specific uptake in organs such as liver and spleen due to cell phagocytosis, and the clearance rate in normal tissues is slow
These factors will affect the establishment of the imaging model and data processing, thereby affecting the accurate assessment of liver function

Method used

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  • 99mtc marked multivalence sugar fan-shaped dendrimer complex, application thereof, multivalence sugar fan-shaped dendrimer ligand and preparation method thereof
  • 99mtc marked multivalence sugar fan-shaped dendrimer complex, application thereof, multivalence sugar fan-shaped dendrimer ligand and preparation method thereof
  • 99mtc marked multivalence sugar fan-shaped dendrimer complex, application thereof, multivalence sugar fan-shaped dendrimer ligand and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The preparation of embodiment 1 ligand

[0071] refer to figure 1 (Take 2LA-G1-HYNIC-1 as an example).

[0072] 1. Synthesis of fan-shaped dendrimers G1, G2, and G3 with ethylenediamine as the core

[0073] 1.5 g of ethylenediamine was dissolved in 100 mL of dichloromethane, and 2.18 g of di-tert-butyl dicarbonate dissolved in 20 mL of dichloromethane was added dropwise in an ice-water bath. React overnight at room temperature. After the precipitate was removed, the solvent was removed by rotary evaporation, then dissolved in 50 mL of ethyl acetate, and washed 3 times with saturated sodium chloride solution. The organic phase was collected, dried and the solvent was spin-dried to obtain 1.1 g of N-tert-butoxycarbonylethylenediamine with a yield of 69%.

[0074] 1 HNMR (400MHz,D 2 O)δ: 1.45(s,9H,tBuCH 3 ),2.80(t,2H,CH 2 ),3.17(m,2H,CH 2 ),5.0(s,1H,NH 2 ).

[0075] 0.6 g of N-tert-butoxycarbonylethylenediamine was dissolved in 5 mL of methanol, and 10 mL of met...

Embodiment 299

[0092] Example 2 99m Tc(2LA-G1-HYNIC)(Tricine) 2 preparation of

[0093] Take 2LA-G1-HYNIC-10.05mg and dissolve in 0.5mL phosphate buffer (0.2mol / L, pH6.0, containing 30mg co-ligand Tricine), add 2mg / mL SnCl after all dissolved 2 2H 2 O solution 10μL, shake well. Add fresh at the end 99m TCO 4 - Eluent 0.5mL (37MBq), fully shake, seal and react in boiling water bath for 20min. get 99m Tc(2LA-G1-HYNIC)(Tricine) 2 .

[0094] The HiTrap desalting gel column (SephadexG25) was equilibrated with 25mL eluent (0.05mol / L, pH7.5 phosphate buffer), and the flow rate was controlled between 1 and 10mL / min. Mark 0.25mL 99m Tc(2LA-G1-HYNIC)(Tricine) 2 Use a 1mL syringe to load the sample, first rinse with 1.25mL eluent, and then collect 1mL eluent to obtain a sample that removes impurities and has a recovery rate of >95%. 99m Tc(2LA-G1-HYNIC)(Tricine) 2 solution.

[0095] Identified by chromatography and radio-HPLC, the retention time is 7.2 min, and the radiochemical purity i...

Embodiment 39

[0097] Example 3 9m Tc(4LA-G2-HYNIC)(Tricine) 2 preparation of

[0098] Take 4LA-G2-HYNIC-20.1mg and dissolve in 0.5mL phosphate buffer (0.2mol / L, pH6.0, containing 25mg co-ligand Tricine), add 2mg / mL SnCl after all dissolved 2 2H 2 O solution 10μL, shake well. Add fresh at the end 99m TCO 4 - Eluent 0.5mL (37MBq), fully shake, seal and react in boiling water bath for 20min. get 99m Tc(4LA-G2-HYNIC)(Tricine) 2 .

[0099] The HiTrap desalting gel column (SephadexG25) was equilibrated with 25mL eluent (0.05mol / L, pH7.5 phosphate buffer), and the flow rate was controlled between 1 and 10mL / min. Mark 0.25mL 99m Tc(4LA-G2-HYNIC)(Tricine) 2 Use a 1mL syringe to load the sample, first rinse with 1.25mL eluent, and then collect 1mL eluent to obtain a sample that removes impurities and has a recovery rate of >95%. 99m Tc(4LA-G2-HYNIC)(Tricine) 2 solution.

[0100] Identified by chromatography and radio-HPLC, its retention time is 7.3 min, and its radiochemical purity is ...

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Abstract

The invention provides a 99mTc marked multivalence sugar fan-shaped dendrimer complex with the formula being 99mTc(R-HYNIC)(Tricine)m(L)n and further provides application of the complex, a multivalence sugar fan-shaped dendrimer ligand for preparing the complex and a preparation method thereof. The multivalence sugar fan-shaped dendrimer ligand can form the 99mTc marked complex with a co-ligand, a selectable coligand and radioactive pertechnetate, the complex is high in radiation chemical purity, good in stability and biological performance, high in specific activity, high in liver uptake value and target-to-non-target ratio, capable of being used as a hepatic cell asialoglycoprotein receptor SPECT photographic developer, easy and convenient to prepare and low in cost and has the large-scale and wide-application value.

Description

technical field [0001] The invention relates to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a 99m Tc-labeled polyvalent sugar fan-shaped dendrimer complexes and their uses can be used to prepare the 99m Multivalent sugar fan-shaped dendrimer ligands of Tc-labeled complexes and methods for their preparation. Background technique [0002] Liver disease has always been one of the global important public health problems. Statistics from the World Health Organization show that there are about 350 million HBV carriers worldwide, accounting for 5% of the world's population, and about 170 million HCV-infected people. my country is a country with a high incidence of liver diseases, and the number of liver diseases accounts for about 1 / 3 of the global number of liver diseases. Every year, 110,000 people die of liver cancer, accounting for 45% of the world's liver cancer deaths. Early diagnosis of liver diseases such as chron...

Claims

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Application Information

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IPC IPC(8): C07H15/04C08G83/00A61K51/06A61K103/10
CPCY02P20/55C07H15/04A61K51/06C08G83/003
Inventor 杨文江刘宇薛井泉汪建军张延华
Owner INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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