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Applications of coumarin derivatives in preventing and curing serious brain diseases

A disease and drug technology, applied in the field of medicine, can solve problems such as insufficient curative effect and side effects

Inactive Publication Date: 2013-12-18
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although a wide variety of drugs are used clinically, their application is limited due to the existence or insufficient curative effect, or serious side effects

Method used

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  • Applications of coumarin derivatives in preventing and curing serious brain diseases
  • Applications of coumarin derivatives in preventing and curing serious brain diseases
  • Applications of coumarin derivatives in preventing and curing serious brain diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] 5,7-Dihydroxy-4-methyl-3-(4-(benzenesulfonyl)piperazin-1-yl)-2H-benzopyran-2-one

[0053]

[0054] m.p.231-234℃; 1 H NMR (300MHz, DMSO-d 6 , 80℃):10.400(s,1H),10.201(s,1H),7.710(m,5H),6.226(d,1H,J=2.4Hz),6.105(d,1H,J=2.4Hz), 3.855(br,1H),3.187(br,3H),2.997(br,4H),2.487(s,3H);HRMS Calcd.For C 20 h 20 N 2 NaO 6 S(M+Na + )439.0940;found.439.0932.

Embodiment 2

[0056] 3-(4-(2-Ethylbutyl)piperazin-1-yl)-5,7-dihydroxy-4methyl-2H-benzopyran-2-one

[0057]

[0058] m.p.296-299℃; 1 H NMR (300MHz, DMSO-d 6 ):δ5.927(s,1H),5.710(s,1H),2.650-3.685(br,8H),2.650(s,3H),2.120(d,2H,J=4.6Hz),1.428(m, 1H),1.281(m,4H),0.853(t,6H,J=7.2Hz).HRMS Calcd.For C 20 h 29 N 2 o 4 (M+H + )361.2127;found361.2124.

Embodiment 3

[0060] 4-(5,7-Dihydroxy-4-methyl-2-oxo-2H-benzopyran-3-yl)-N-(4-isopropylphenyl)piperazine-1-amide

[0061]

[0062] m.p.262-265℃; 1 H NMR (300MHz, DMSO-d 6 ):δ10.421(s,1H),10.186(s,1H),8.441(s,1H),7.348(dd,2H,J=8.7Hz,J=1.5Hz),7.082(dd,2H,J= 8.7Hz, J=1.5Hz), 6.258(d, 1H, J=2.4Hz), 6.124(d, 1H, J=2.4Hz), 3.459(s, 1H), 2.779-4.400(br, 8H), 2.668 (s,3H),1.174(s,3H),1.151(s,3H);HRMS Calcd.For C 24 h 28 N 3 o 5 (M+H + ) 438.2029; found 438.2007.

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Abstract

The invention discloses applications of coumarin compounds and salts thereof acceptable in pharmacy in preparation of drugs for preventing and curing brain diseases, especially for preventing or curing diseases related with neuron damage and neuron inflammation, and specifically for preventing or curing Parkinson's disease, Alzheimer's disease, cerebral ischemia, depression, and cerebral apoplexy.

Description

technical field [0001] The present invention relates to coumarin derivatives and a new medical application of such compounds, especially in the prevention and treatment of brain neurological and mental diseases such as stroke, dementia, Parkinson's disease and depression; field of medical technology. Background technique [0002] With the rapid development of modern society, the accelerated pace of life and work, coupled with the aging of the social population, major brain diseases, including neurological diseases and mental disorders (especially stroke, dementia, Parkinson, depression, etc.) Seriously endangering human health, it not only reduces the quality of life of patients, but also brings heavy economic burden to patients' families, which will also become a serious social problem. [0003] Modern medicine believes that the abnormal damage and loss of neurons is a common pathological feature of major brain diseases such as stroke, dementia, Parkinson, and depression. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K31/635A61K31/37A61K31/453A61K31/5377A61P25/00A61P25/16A61P25/28A61P9/10A61P25/24
Inventor 刘刚陈乃宏孙明娜胡金风宋修云
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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