Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Pla China

Biomedical Analysis Center, Academy of Military Medical Sciences

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences

Biomedical Anaylsis Center, Academy of Military Medical Sciences

Xinhua He

Tao Li

Tao Zhou

Xuemin Zhang

Zhenggang Liu

Bohua Zhong

He H Liu

Nan Zhao

Yanping Zhang

Yunfeng Li

Rui Xue

Youzhi Zhang

Hongxia Chen

Meiying Li

Yongguang Wang

Shengming Wu

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&#x2550;O or CH; 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.

Hydroquinone compounds, preparation methods therefor, and use in anti-tumor or immunomodulation therapy

The present invention relates to a stable crystal form, i.e. form A, of 2-tert-butyl-4-methoxyphenol, and to a new preparation method for the 2-tert-butyl-4-methoxyphenol; and the use of the 2-tert-butyl-4-methoxyphenol and the stable crystal form thereof, i.e. form A, in preparing antitumor drugs or immunomodulator drugs. The stable crystal form, i.e. form A, as expressed by a powder X-ray diffraction pattern in an angle of 2&#x3b8;, using Cu-K&#x3b1; radiation, has at least 3 absorption peaks selected from the following positions: 6.27&#xb1;0.10, 6.94&#xb1;0.10, 12.27&#xb1;0.10, 13.36&#xb1;0.10, 14.01&#xb1;0.10, 14.79&#xb1;0.10, 15.31&#xb1;0.10, 17.05&#xb1;0.10, 18.30&#xb1;0.10, 19.00&#xb1;0.10, 20.47&#xb1;0.10, 20.98&#xb1;0.10, 22.37&#xb1;0.10, 23.68&#xb1;0.10, 24.55&#xb1;0.10, 25.37&#xb1;0.10, 30.83&#xb1;0.10, 33.12&#xb1;0.10, 40.50&#xb1;0.10, 42.81&#xb1;0.10.

Method for preparing 2-tert-butyl-4-methoxyphenol and new crystal form thereof

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&#x2550;O or CH; 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 (T&#xbd;=12&#x2dc;24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoid environmental oxidation and increase the environmental stability of drugs containing the compounds.

The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein Ris H or methyl; each Ris independently &#x2014;Ror &#x2014;OR, each Ris independently C-Calkyl, C-Ccycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits. 

Acyclic nucleoside phosphonate derivatives and medical uses thereof

The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R, Rand n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug. 

Amine compounds and medical uses thereof

Growing community of inventors

Beijing, China

Xinhua He