Application of small molecular compound in preparation of medicine for inhibiting Tau protein expression quantity

Abstract

The invention discloses an application of a small molecular compound in preparation of a medicine for inhibiting Tau protein expression quantity, and particularly relates to an application of 2', 3'-dialdehyde adenosine (ADDA) or in-vivo metabolite, a tautomer, a stereoisomer, a pharmaceutically acceptable salt, a hydrate and / or a solvate thereof in preparation of a Tau protein inhibitor. The invention relates to a medicine for treating the central nervous system diseases. According to the application disclosed by the invention, the effect of the ADDA compound in inhibiting the expression of the human Tau protein is illuminated for the first time, and a candidate medicine is provided for treating Alz-heimer disease (AD) and Parkinson's disease.

Description

technical field [0001] The present invention relates to the field of medicine, in particular, the present invention relates to the application of a small molecular compound in the preparation of drugs for inhibiting the expression of Tau protein. Background technique [0002] Alzheimer's disease (Alzheimer disease, AD), also known as senile dementia, is a degenerative disease of the central nervous system with an insidious onset and a chronic progressive course. It is the most common type of senile dementia. [Burns A et al, BMJ., 338:467-471, 2009; WHO, "Dementia Fact sheet N°362", 2015] Mainly manifested as progressive memory impairment, cognitive dysfunction, personality changes and language disorders Mental symptoms that seriously affect social, occupational and life functions [National Institute on Aging, "About Alzheimer's Disease: Symptoms", 2012]. With the aging of the population, the incidence of AD is increasing year by year, seriously endangering the physical and ...

AI Technical Summary

Problems solved by technology

In 2008, TauRx announced the results of phase II clinical trials at a meeting, but the results caused great controversy: the data showed that the two low-dose regimens of the drug were effective for moderate patients (not early patients), and the clinical design The plan was also seriously questioned, and the company did not publish the complete data of the clinical trial after the meeting

Similar to GSK-3 inhibitors, the side effects of these drugs are also difficult to control

In 2012, Bristol-Myers Squibb (BMS) started a clinical phase I trial to evaluate the safety of the microtubule stabilizer epothiloneD, but after the end of the clinical trial, BMS terminated the development of this indication

[0027] At present, there is no report on the use of ADDA for the preparation of inhibitors of Tau protein, and the application in the preparation of drugs for the treatment of senile dementia and Parkinson's disease

Images