Application of 10B-containing compound in preparation of medicine specifically combined with beta amyloid protein

A technology of amyloid and compounds, applied in the fields of compounds containing group 3/13 elements of the periodic table, active ingredients of boron compounds, medical preparations containing active ingredients, etc., can solve the problems of undiscovered and undiscovered applications

Inactive Publication Date: 2017-10-31
NEUBORON MEDTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Neutron capture therapy technology is a treatment technology with strong pertinence, good effect and less damage to normal tissues. However, in the process of using neutron capture therapy technology to treat diseases, it is often necessary to have a thermal neutron capture cross-section Large nuclides and compounds that can specifically bind to lesions or certain types of substances in lesions are mediated. A compound that can specifically bind to β-amyloid protein has not been found as a drug for the treatment of Alzheimer's disease However, the use of compounds containing nuclides with large cross-sections for thermal neutron capture has not yet been found in the preparation of drugs that specifically bind to β-amyloid

Method used

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  • Application of 10B-containing compound in preparation of medicine specifically combined with beta amyloid protein
  • Application of 10B-containing compound in preparation of medicine specifically combined with beta amyloid protein
  • Application of 10B-containing compound in preparation of medicine specifically combined with beta amyloid protein

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] containing 10 The preparation method of the compound of B

[0073] The present invention contains 10 The preparation process of the compound of B is shown in Reaction Formula II, and the specific preparation steps are as follows:

[0074] Step 1: 90mmol of 2-acetylfuran was dissolved in 40mL of dimethylformamide (DMF), and 108mmol of N-bromosuccinimide (NBS) was added thereto at 0°C, and the mixture was After stirring overnight at room temperature, the reaction mixture contained 1-(5-bromo-2-furyl)ethanone.

[0075] The reaction mixture described in step 1 was diluted with ethyl acetate, and filtered, and the organic phase in the filtrate was washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, concentrated, and then separated by chromatography to obtain 1- (5-Bromo-2-furyl)ethanone.

[0076] 1 H NMR (500MHz, CDCl 3 ,δ,ppm):2.46(3H.s),6.49(1H,d,J=3.4Hz),7.12(1H,d,J=3.4Hz).MS m / z 188(M+H) + .

[0077] Step 2: Add 5.3mmol o...

Embodiment 2

[0088] containing 10 Application of the compound of B in the preparation and specific binding of β-amyloid protein

[0089] Due to the existence of the blood-brain barrier (BBB), it is difficult for most compounds to enter the brain through the blood stream. For many drugs, they cannot exert their efficacy if they cannot pass through the blood-brain barrier. In general, water-soluble drugs are difficult to pass through the blood-brain barrier, while fat-soluble drugs have better permeability than water-soluble drugs. The dissolution, absorption, distribution, and transport of drugs in the body are related to the water solubility and fat solubility of the drug, that is, the oil-water partition coefficient (logP). The oil-water partition coefficient is the logarithmic value of the ratio of the partition coefficient of the drug in n-octanol and water phase. The larger the logP value, the more lipophilic the substance is, and vice versa, the more soluble in water.

[0090] It i...

Embodiment 3

[0096] Simulation Test of Neutron Capture Therapy System Eliminating Amyloid Beta Protein

[0097] This embodiment uses boric acid (H 3 10 BO 3 ) instead of containing 10 The compound of B (including compound I and compound II), wherein boronic acid (H 3 10 BO 3 ) in the boron element is 10 B, Bovine serum albumin (BSA) is used to simulate β-amyloid protein, and the mixed solution composed of boric acid and bovine serum albumin is placed in the neutron beam environment generated by the neutron capture therapy device, and analyzed by SDS-PAGE gel electrophoresis The effect of neutrons on bovine serum albumin and its effect on H 3 10 BO 3 Effect of neutron beams on bovine serum albumin in the presence of conditions.

[0098] (1) The effect of neutrons on bovine serum albumin

[0099] Use ultrapure water to prepare a BSA solution with a concentration of 0.01% (w / w), store the prepared solution at 4°C and perform experimental operations. Take 1mL of the BSA solution an...

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Abstract

The invention provides application of a 10B-containing compound in preparation of a medicine specifically combined with a beta amyloid protein, wherein the medicine specifically combined with the beta amyloid protein can reduce or eliminate the beta amyloid protein in an irradiation process of a neutron beam transmitted by a neutron capture treatment device after the beta amyloid protein is combined, so that Alzheimer's disease is further treated. The invention provides a new method for treatment of the Alzheimer's disease.

Description

technical field [0001] The present invention relates to the application of a compound in the preparation and specific binding drug of β-amyloid protein, especially a compound containing 10 Application of the compound of B in the preparation and specific binding of β-amyloid protein. Background technique [0002] Alzheimer's disease (AD) is a latent, progressive and irreversible brain disease with a high incidence in people over 65 years old. The current goal of AD treatment is to maintain physical function and capacity while slowing or delaying symptoms. Medications for mild to moderate AD include the acetylcholinesterase inhibitors donepezil, rivastigmine, and galantamine. Donepezil is also used to treat moderate to severe AD, alone or in combination with the N-methyl-D-aspartate receptor antagonist memantine. These neurotransmitter-modulating drugs temporarily improve symptoms, but patients still experience progressive cognitive deterioration, as well as psychosis, agit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/69A61P25/28A61N5/10
CPCA61K31/69A61N5/103A61N5/1048A61N5/1077A61N2005/109A61K41/0095A61P25/28C07D207/00C07D207/02C07D207/04C07F5/02A61N5/1042A61N2005/1094A61N2005/1095A61N2005/1098
Inventor 陈瑞芬何静刘渊豪
Owner NEUBORON MEDTECH
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