Pregabalin derivative and application thereof
A technology of pregabalin and derivatives, applied to new pregabalin derivatives and their application fields, can solve problems such as wide application and limitation of side effects, and achieve significant anti-acetylcholinesterase and butyrylcholinesterase activities, Clearly selective effect
Active Publication Date: 2010-12-15
INST OF ANALYSIS GUANGDONG ACAD OF SCI (CHINA NAT ANALYTICAL
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Problems solved by technology
Acetylcholinesterase inhibitors such as tacrine, physostigmine, galantamine, zidoperidine, and huperzine A can enhance the cognitive ability of AD patients, but most drugs are used because of their central or peripheral system side effects. Its wide application is limited
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Abstract
The invention relates to a pregabalin derivative shown in formula I and application thereof in medicine for resisting senile dementia. Acetylcholinesterase in vitro test model shows that the pregabalin derivative has remarkable acetylcholinesterase resistance activity so as to be used for preparing the medicine for resisting senile dementia. The pregabalin derivative has the chemical structural formula shown by the formula I, and R in the formula is defined by the specification. Formula I.
Description
technical field The invention relates to the field of medicinal chemistry, in particular, the invention relates to new pregabalin derivatives and applications thereof. technical background With the aging of the world's population, Alzheimer's disease (commonly known as senile dementia, Alzheimer's disease, AD) has become one of the main diseases that threaten the life of the elderly in their later years. AD is an irreversible progressive degenerative disease of the brain. The clinical manifestation is memory loss accompanied by other cognitive function impairments, which leads to the loss of the ability to synthesize visual, auditory, tactile, olfactory and other information in advanced patients, resulting in the inability of patients to live independently. The pathogenesis of AD is complex, and the etiology is not yet fully understood, so far there is no good cure or reverse the course of the drug. At present, there are mainly three theories about the etiology of AD: firs...
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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/08C07D295/096C07C227/20A61K31/222A61K31/40A61K31/4453A61K31/5375A61P25/28
Inventor 俞亮潘文龙宋化灿万一千宋森川陈智勇陈泳孙一峰
Owner INST OF ANALYSIS GUANGDONG ACAD OF SCI (CHINA NAT ANALYTICAL
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