Sapogenin derivatives and their use in the treatment of cognitive dysfunction

A technology of use, alkyl, applied in the field of sapogenin derivatives and their use in the treatment of cognitive impairment, can solve the problems of lack of synaptic transmission, no data provided, defects, etc.

Inactive Publication Date: 2008-03-19
PHYTOPHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantages in the above three traditional approaches for the treatment of AD / SDAT are: ACh precursor supplementation, agonist replacement and inhibition of acetylcholinesterase
However, this disclosure is of dubious value, since it is well recognized that there is no infectious factor for a very large number of symptoms characterized by a lack of synaptic transmission, so the basic premise of the so-called invention is flawed
In addition, they do not provide any kind of data that would enable those skilled in the art to select a preferred compound from the large number of compounds they require

Method used

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  • Sapogenin derivatives and their use in the treatment of cognitive dysfunction
  • Sapogenin derivatives and their use in the treatment of cognitive dysfunction
  • Sapogenin derivatives and their use in the treatment of cognitive dysfunction

Examples

Experimental program
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Effect test

Embodiment 1

[0171] In CHO cell lines expressing recombinant human muscarinic receptors in vitro, the number of muscarinic receptors tended to decrease over time. The muscarinic receptor density was increased after 72 hours of incubation with saponin derivatives of the invention (1-10 μm).

[0172] method:

[0173] Effects of saponin derivatives of the present invention on muscarinic receptor density in CHO cells expressing recombinant human muscarinic receptors.

[0174] Chinese hamster ovary (CHO) cells expressing high levels of receptor (-2.2 pmole receptor / mg protein) were cultured in flasks (150 ml) for 24 hours before starting the assay. Vehicle (DMSO) and saponin derivatives (1 and 10 [mu]M) were added to the medium for 48 hours. The culture medium was removed, the cells were scraped and resuspended in Hanks' solution, centrifuged, and incubated with [ 3 H]-QNB was incubated for 30 min followed by a liquid scintillation counter to determine the level of m receptor. Determination...

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PUM

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Abstract

The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical composition are also disclosed.

Description

[0001] This application is a divisional application of a Chinese patent application with the application number 00813605.X (PCT / GB00 / 03745) and the invention title "Saponin Derivatives and Their Use in the Treatment of Cognitive Impairment". technical field [0002] The present invention relates to saponin derivatives and their use in the treatment of cognitive disorders and similar conditions, and to compositions for such treatment. The invention also relates to the treatment of conditions characterized by defects in the number and function of membrane-bound receptors. In the following, the invention will be described primarily with reference to the treatment of Alzheimer's disease (AD) and Alzheimer's-type senile dementia (SDAT), in which defects of many receptor types are shown. However, it should be understood that the present invention generally relates to the treatment of symptoms due to inherent pathological conditions and / or exposure to harmful environmental conditions...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P25/28A61K31/575A61P25/14C07J9/00C07J71/00A23L1/30A61K36/18A61K36/896A61P21/04A61P25/16
CPCC07J71/00C07J71/0005C07J9/00A61P21/04A61P25/04A61P25/14A61P25/16A61P25/28
Inventor P·巴勒克拉夫J·汉森P·冈宁D·里斯夏宗勤胡雅儿
Owner PHYTOPHARM LTD
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