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Amyloid-beta protein level decreasing agent

A technology of reducing amyloid protein and agents, which can be used in drug delivery, organic active ingredients, nervous system diseases, etc., and can solve problems such as deterioration of cognitive function

Pending Publication Date: 2020-01-14
FUJIFILM RI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even if these drugs show a temporary cognitive function improvement effect at the beginning of use, the cognitive function will deteriorate compared with the cognitive function before treatment after 48 weeks or more (Non-Patent Document 6)

Method used

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  • Amyloid-beta protein level decreasing agent
  • Amyloid-beta protein level decreasing agent

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0095]0.9726 g of magnesium stearate (magnesium stearate, Merck) was added to 174.03 g of the maleate salt of compound A, and mixed for 30 minutes. This mixed powder was compressed and molded with a dry granulator (TF-LABO (roller pressure 3 MPa), Freund Industries), and the molded solid was sized. To 60.0 g of the obtained sized powder, 49.51 g of lactose (FlowLac 90, Meggle Japan), 16.50 g of crystalline cellulose (CEOLUS PH302, Asahi Kasei Chemicals) and cross-linked carboxymethyl fiber were added after sieving through a sieve with an aperture of 850 μm. Sodium Primellose (Primellose, DMV Japan) 6.67 g, mixed for 10 minutes. 0.6667 g of magnesium stearate was added to this mixed powder, and it mixed for 30 minutes. For this mixed powder, a tablet press machine (HT-P18A, Hata Tekkosho (Japanese original: バブルアール面) pestle with a tablet diameter of 8.5 mm and a compression pressure of about 12 kN was used. Iron Works)) to perform tablet compression to obtain a 250 mg circular...

preparation example 2

[0097] 60.90 g of mannitol (Parteck M200, Merck) and 3.60 g of croscarmellose sodium were added to 53.70 g of the maleate salt of compound A, and mixed for 10 minutes. 1.80 g of magnesium stearate was added to the mixed powder, and mixed for 30 minutes. This mixed powder was tableted using a pestle with double R sides with a tablet diameter of 8.5 mm at a tableting pressure of about 10 kN to obtain one 250 mg round plain tablet. The plain tablet is coated with a coating agent (Opadry (オパドライ) 03F44057, 00F440000 (hypromellose 2910: 71.5%, Macrogol 6000: 14.166%, talc: 7.167%, titanium oxide: 7.067%) at a rate of 8 mg per tablet. , ferric oxide: 0.1%), Japan Colorcon), add a trace amount of carnauba wax to obtain film-coated tablets.

preparation example 3

[0099] 11.11 g of magnesium stearate was added to 1988.89 g of the maleate salt of compound A, and mixed for 30 minutes. The mixed powder is compressed into a dry granulator, and the formed solid is sized. Add mannitol 26.21g, ethyl cellulose (Ethocel 100FP premium, Dow Chemicals) 7.50g, crystalline cellulose (CEOLUS KG-1000, Asahi Kasei Chemicals) 3.75g, cross-linked polydimensional fiber in 107.13g of the obtained sized powder. Ketone (Kollidon CL-SF, BASF) 3.75g and croscarmellose sodium 0.75g were mixed for 30 minutes. 0.90 g of magnesium stearate was added to the mixed powder, and mixed for 5 minutes. This mixed powder was tableted using a pestle with double R sides with a tablet diameter of 8.5 mm at a tableting pressure of about 7 kN to obtain one 315 mg round plain tablet. The plain tablet was coated with a coating agent at a ratio of 9 mg per tablet, and a small amount of carnauba wax was added to obtain a film-coated tablet.

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Abstract

The present invention addresses the problem of providing a pharmaceutical agent and a method for suppressing the progression of diseases such as Alzheimer-type dementia indicating an increase in the level of amyloid-beta protein in the brain. 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof has an effect of decreasing the level of amyloid-beta protein in the brain parenchyma, and hence is effective as an agent for decreasing the level of amyloid-beta protein in the brain. By administering 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof, itis possible to prevent or treat diseases in which an increase in the level of amyloid-beta protein in the brain occurs, such as Alzheimer-type dementia.

Description

technical field [0001] The present invention relates to a β- Amyloid amount reducing agent. Background technique [0002] Dementia is a neurodegenerative disease in which cognitive function is significantly reduced due to brain atrophy, cerebrovascular disorders, and the like. Dementia can be classified into several types depending on the cause, but 60% to 80% of all dementia patients are Alzheimer-type dementia (AD) (Non-Patent Document 1). The pathogenesis of AD is complicated, but it is considered that the cause is senile plaques formed by aggregation of β-amyloid protein (Aβ), or changes in neurofibrils caused by aggregation of phosphorylated tau protein (p-Tau) (Non-Patent Document 2) . The number of patients with AD is estimated to be about 1.16 million or more in Japan. Since the older the age, the higher the incidence rate, the number of patients will increase rapidly in the future with the aging of society, and it is expected that the burden on the patient's fam...

Claims

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Application Information

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IPC IPC(8): A61K31/397A61P25/28
CPCA61K31/397A61P25/28A61K9/0053
Inventor 小林博松本喜彦
Owner FUJIFILM RI PHARMA
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