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Agent for preventing or treating tauopathy

A technology of protein disease and therapeutic agent, applied in the field of prevention or treatment of protein tauopathies, can solve problems such as poor cognitive function and 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, in general, after 48 weeks or more, the cognitive function is worse than the cognitive function before treatment (Non-Patent Document 6)

Method used

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  • Agent for preventing or treating tauopathy
  • Agent for preventing or treating tauopathy
  • Agent for preventing or treating tauopathy

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0128] 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 (Flowlac90, Meggle Japan), 16.50 g of crystalline cellulose (Ceolus PH302, Asahi Kasei chemicals) and croscarmellose sodium were added by sieving through a sieve with a mesh size of 850 μm. (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. This mixed powder was compressed using a double arc pestle with a tablet diameter of 8.5 mm, and was compressed by a tablet press (HT-P18A, Tobacco Iron Works) at a compression pressure of about 12 kN to obtain a round tablet of 250 mg. shaped die. Utilize coating machine: DRC-200 (powrex) i...

preparation example 2

[0130] 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 this mixed powder, and it mixed for 30 minutes. This mixed powder was tableted using a double arc pestle with a tablet diameter of 8.5 mm at about 10 kN to obtain 250 mg of round bare tablets. Coating agent (Opadry 03F44057, 00F440000 (hypromellose 2910: 71.5%, PEG 6000: 14.166%, talc: 7.167%, titanium oxide: 7.067%, iron oxide: 0.1%) was applied to the bare tablet, Japan Colorcon) was coated at a ratio of 8 mg per tablet, and a small amount of carnauba wax was added to obtain film-coated tablets.

preparation example 3

[0132] 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 compression-molded with a dry granulator, and the shaped solid is sized. Add mannitol 26.21g, ethyl cellulose (ETHOCEL100FP premium, Dow Chemical) 7.50g, crystalline cellulose (ceolus KG-1000, Asahi Kasei Chemicals) 3.75g, crospovidone ( Kollidon CL-SF, BASF) 3.75 g and croscarmellose sodium 0.75 g 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 double-arc pestle with a tablet diameter of 8.5 mm at a tableting pressure of about 7 kN to obtain 315 mg of round bare tablets. The bare tablets were coated with a coating agent at a rate of 9 mg per tablet, and then a small amount of carnauba wax was added to obtain film-coated tablets.

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PUM

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Abstract

The present invention addresses the problem of providing an agent and a method for suppressing the progression of tauopathy such as Alzheimer-type dementia. 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof has an effect of decreasing the level of phosphorylated tau protein and on decreasing the level of amyloid-beta protein in the brain parenchyma, and is useful as a prophylactic or therapeutic agent for tauopathy. Thus, it is possible to prevent or treat tauopathy by administering 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof.

Description

technical field [0001] The present invention relates to a method for tauopathies containing 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof as an active ingredient prophylactic or therapeutic agent. Background technique [0002] Dementia is a neurodegenerative disease in which cognitive function is significantly reduced due to brain atrophy, cerebrovascular disease, and the like. Dementia is classified into several types depending on the cause, and 60% to 80% of all dementia patients are Alzheimer's dementia (AD) (Non-Patent Document 1). The pathogenesis of AD is complicated, and it is considered to be caused by the aggregation of amyloid β protein (Aβ) to form senile plaques or the aggregation of phosphorylated Tau protein (p-Tau) to cause changes in neurofibrils (Non-Patent Document 2). The number of patients with AD is estimated to be about 1.16 million or more in Japan. Since the incidence rate becomes higher as the age increases, the numbe...

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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