- 专利标题: Hydroquinone compounds, preparation methods therefor, and use in anti-tumor or immunomodulation therapy
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申请号: US16988525申请日: 2020-08-07
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公开(公告)号: US11738000B2公开(公告)日: 2023-08-29
- 发明人: Xuemin Zhang , Xinhua He , Tao Zhou , Zhenggang Liu , Tao Li
- 申请人: Biomedical Analysis Center, Academy Of Military Medical Sciences , Institute Of Pharmacology And Toxicology, Academy Of Military Medical Sciences
- 申请人地址: CN Beijing
- 专利权人: BIOMEDICAL ANALYSIS CENTER, ACADEMY OF MILITARY MEDICAL SCIENCES,INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES
- 当前专利权人: BIOMEDICAL ANALYSIS CENTER, ACADEMY OF MILITARY MEDICAL SCIENCES,INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES
- 当前专利权人地址: CN Beijing; CN Beijing
- 代理机构: McCoy Russell LLP
- 优先权: CN 1610037849.5 2016.01.20
- 分案原申请号: US16069814
- 主分类号: A61K31/09
- IPC分类号: A61K31/09 ; A61K31/23 ; A61K31/325 ; C07C69/78 ; C07C271/44 ; C07C69/28 ; C07D265/30 ; C07C271/56 ; A61K31/222 ; C07C69/16 ; A61P37/04 ; A61P35/04 ; A61K31/135
摘要:
Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I,
wherein X is C═O or CH2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.
wherein X is C═O or CH2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.
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