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5-ht4 receptor agonist compounds for treatment of cognitive disorders

A 5-HT4, Cognitive Impairment Technology for Alzheimer's and other Cognitive Impairments that addresses issues such as yet-to-be-approved treatments

Inactive Publication Date: 2012-03-28
THERAVANCE BIOPHARMA R&D IP LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] To date, no approved use of 5-HT 4 Mechanisms for Potential Utility in the Treatment of Cognitive Disorders

Method used

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  • 5-ht4 receptor agonist compounds for treatment of cognitive disorders
  • 5-ht4 receptor agonist compounds for treatment of cognitive disorders
  • 5-ht4 receptor agonist compounds for treatment of cognitive disorders

Examples

Experimental program
Comparison scheme
Effect test

example A

[0080] Formulation Example A: Hard Gelatin Capsule for Oral Administration

[0081] Compound of the invention (20 mg), starch (89 mg), microcrystalline cellulose (89 mg) and magnesium stearate (2 mg) were blended well and then passed through a No. 45 mesh U.S. sieve. The resulting composition was filled into hard gelatin capsules (200 mg of the composition per capsule).

example B

[0082] Formulation Example B: Gelatin Capsule for Oral Administration

[0083] Compound of the present invention (10 mg), polyoxyethylene sorbitan monooleate (50 mg) and starch powder (250 mg) were blended well and then filled into gelatin capsules (310 mg composition per capsule).

example C

[0084] Formulation Example C: Tablet for Oral Administration

[0085] Compound of the present invention (5 mg), microcrystalline cellulose (400 mg), fumed silicon dioxide (10 mg) and stearic acid (5 mg) were blended thoroughly and subsequently compressed to form tablets (420 mg per tablet combination).

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PUM

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Abstract

The invention relates to the use of specific 5-HT4 receptor agonist compounds for the treatment of cognitive disorders, in particular, to the use of these compounds in combination with other agents, specifically acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease and other cognitive disorders.

Description

technical field [0001] The present invention relates to specific 5-HT 4 Use of receptor agonist compounds for the treatment of cognitive disorders, in particular to the use of these compounds in combination with other agents, in particular acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease ) and other cognitive impairment uses. Background technique [0002] Worldwide, the number of older people at risk of developing dementia is growing rapidly as life expectancy increases. According to some experts, Alzheimer's disease is the most common cause of dementia in the elderly, accounting for 50-60% of all cases. In 2008, an estimated 5.2 million people were living with Alzheimer's disease in the United States alone, representing 13% of the US population over the age of 65. [0003] Alzheimer's disease is defined as progressive cognitive decline and impaired functional status inconsistent with normal aging. Insufficiency of the cholinergic system is thoug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61K31/4709A61K31/454A61K45/06A61P25/28
CPCA61K45/06A61K31/454A61K31/46A61K31/4545A61K31/4709A61K31/445A61K2300/00A61P25/00A61P25/28A61P43/00A61K2121/00
Inventor 大卫·贝亚蒂耶沈菲杰奎琳·A·M·史密斯罗伯特·默里·麦金内尔蕾·张
Owner THERAVANCE BIOPHARMA R&D IP LLC