Composition for diagnosing amyloid-related disease

An amyloid and related technology, applied in the preparations for in vivo experiments, in vivo radioactive preparations, organic chemistry, etc., can solve problems such as non-entered diseases

Inactive Publication Date: 2009-08-12
NAGASAKI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Therefore, these reported compounds have not yet entered into practical app

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  • Composition for diagnosing amyloid-related disease
  • Composition for diagnosing amyloid-related disease
  • Composition for diagnosing amyloid-related disease

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] experimental method

[0110] Reagents and Instruments

[0111] Amyloid β protein (human, 1-42) [TFA type] was purchased from Peptide Institute, Inc., and special grade reagents were used as other reagents. Measured using Varian Gemini 300 and tetramethylsilane as internal standard 1 H-NMR.

[0112] (1) Synthesis of chalcone derivatives containing aromatic heterocycles

[0113] Synthesis of (E)-3-(4-(dimethylamino)phenyl)-1-(5-iodothiophen-2-yl)prop-2-en-1-one (1)

[0114] 256 mg (1 mmol) of 5-acetyl-2-iodothiophene and 149 mg (1 mmol) of 4-dimethylaminobenzaldehyde were dissolved in ethanol (20 mL), and 10% aqueous potassium hydroxide solution (30 mL) was added to the mixture under ice-cooling middle. React at room temperature for 6 h, then add 30 mL of purified water, and filter the precipitated crystals by suction. The crystals were washed with 50% aqueous ethanol and dried to obtain target compound 1. Yield 238mg (62.1% yield). 1 H NMR (300MHz, CDCl 3 )δ...

Embodiment 2

[0132] experimental method

[0133] Reagents and Instruments

[0134] As radioactive iodine-125 ( 125 I) Iodine-125 (3.7 GBq / mL) manufactured by MP Biomedicals, Inc. was used. At a flow rate of 1.0 mL / min, Cosmosil 5C manufactured by Nacalai Tesque Inc. was used 18 -AR-II column (4.6×150mm) and ultrapure water: acetonitrile=3:7 as eluent, reversed-phase HPLC. Using Varian Gemini 300 with tetramethylsilane as internal standard, measure 1 HNMR. Mass spectrometry was performed using a JEOL IMS-DX300. Using 12PLC plate 20 x 20cm manufactured by MERCK - Silica Gel 60F 254 , 2 mm for preparative TLC. Amyloid β protein (human, 1-42) was purchased from Peptide Institute, Inc., and special grade reagents were used as other reagents.

[0135] (1) Synthesis of chalcone derivatives

[0136] Synthesis of 4-bromo-4'-nitrochalcone (1)

[0137] 4-Nitroacetophenone (1.67g, 10.1mmol) and 4-bromobenzaldehyde (1.86g, 10.0mmol) were dissolved in ethanol (10mL), and 10% potassium hydr...

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Abstract

There is provided a composition comprising a compound represented by general formula (I), wherein R 1 represents a 5-iodothiophen-2-yl group or the like, and R 2 represents a 4-dimethylaminophenyl group or the like. This composition is useful for diagnosis of an amyloid-related disease such as Alzheimer's disease because the compound has high binding specificity to amyloid protein, high permeability through the blood-brain barrier, and a property of being rapidly eliminated from sites other than senile plaques in the brain.

Description

technical field [0001] The present invention relates to a composition for diagnosing amyloid-related diseases such as Alzheimer's disease, a method for screening therapeutic or preventive drugs for amyloid-related diseases using the above-mentioned composition, and evaluating A method for treating or preventing an amyloid-related disease. Background technique [0002] With the rapid aging of the population in recent years, an increase in the number of patients suffering from dementia-related diseases including Alzheimer's disease (AD) has become a serious social problem. Currently, Hasegawa Scale, ADAS and MMSE are available methods for clinical diagnosis of AD. All of these methods quantitatively assess reduced cognitive function in AD-suspect individuals and are commonly used. In addition, image diagnostic methods (MRI, CT, etc.) are used supplementarily. However, these diagnostic methods are insufficient to definitively diagnose AD, and development of senile plaques an...

Claims

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Application Information

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IPC IPC(8): A61K51/00C07D213/61C07D233/64C07D277/24C07D307/42C07D333/28C07D333/36C07D409/06
Inventor 中山守雄原武卫小野正博
Owner NAGASAKI UNIVERSITY
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