2-hydroxychalcone amine compounds, and preparation method and uses thereof

Abstract

The invention discloses 2-hydroxychalcone amine compounds and pharmaceutically-acceptable salts, preparation method thereof, pharmaceutical composition, and uses for preparing medicines treating and / or preventing neurodegenerative related diseases, the diseases including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntingdon's disease, HIV associated dementia, multiple sclerosis, progressive lateral sclerosis, neuropathic pain, glaucoma and other neurodegenerative diseases.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a novel 2-hydroxychalcone amine compound (I) and a pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition and a preparation method for treating and / or preventing neurodegeneration Sex-related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis, neurological Pain, glaucoma and other neurodegenerative diseases. Background technique [0002] Alzheimer's disease (AD, senile dementia) is a degenerative disease of the central nervous system mainly characterized by progressive cognitive impairment and memory impairment. The high incidence of cardiovascular disease and cancer has risen to the fourth cause of death in developed countries such as Europe and the United States. According to the report of the World...

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Problems solved by technology

In the previous research, we designed and synthesized scutellarin aglycon carbamate derivatives (CN101337956A, CN102603698A), stilbene or ethane carbamate for the acetylcholinesterase and oxidative stress factors in the pathogenesis of AD Ester compounds (CN102816090A), isoflavone carbamate compounds (CN102827131A), flavonoid alkylamine compounds (CN103087024A), genistein alkylamine compounds (CN103113340A), stilbene oxyalkylamine compounds (CN103073440A), although these compounds have good acetylcholinesterase inhibitory and antioxidant activities, but for A β 1-42 Inhibition of self-aggregation (inhibition rate at 20.0μM concentration is less than 65.0%), for Cu 2+ Induced A β 1-42 Inhibition of aggregation (inhibition rate at 20.0μM concentration is less than 65.0%) and the effect on Cu 2+ Induced A β 1-42 The aggregation disaggregation activity (the disaggregation rate at 20.0μM concentration is less than 60.0%) is not ideal, resulting in poor efficacy of these compounds on AD in animal models

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