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PRO-DRUGS OF NSAIAS WITH VERY HIGH SKIN AND MEMBRANES PENETRATION RATES AND THEIR NEW MEDICINAL USES
专利权人:
YU Chongxi
发明人:
YU, Chongxi,于崇曦,XU, Lina,徐麗娜
申请号:
HK16109604.1
公开号:
HK1221467A
申请日:
2016.08.11
申请国别(地区):
HK
年份:
2017
代理人:
摘要:
The novel positively charged non-steroidal anti-inflammatory drugs shown in general formulas (1, 2a, 2b, 2c or 2d), namely structural formulas 1, 2a, 2b, 2c or 2d, have been designed and synthesized. The compounds represented by the general formulas (1, 2a, 2b, 2c or 2d), namely structural formulas 1, 2a, 2b, 2c or 2d, can be prepared through reaction between the metal salts, organic alkali salts or immobilized alkali salts of the non-steroidal anti-inflammatory drugs and appropriate halides. The positively charged amino in a prodrug of the invention greatly improves the solubility of the drugs in water and can further combine with negative charges on the phosphate terminal groups of a biological membrane. Thus, the local concentrations of the drugs on the biological membrane or the outer side of the skin are very high so as to facilitate the diffusion of the prodrugs from high-concentration areas to low-concentration areas. The biological membrane can be slightly disturbed through the combination so as to allow parts of space for the fat soluble parts of the prodrugs. When molecules of the biological membrane move, the biological membrane is slightly squeezed due to the combination effects of the prodrugs, and when the amino is not protonized, the amino in the prodrugs is separated from the phosphate terminal groups of the biological membrane, and the prodrugs completely penetrate into the biological membrane. When the amino in the prodrugs moves to the other side of the biological membrane and therefore the amino is protonized, the prodrugs are drawn into the cytoplasm, a half-liquid-state aqueous solution or a suspension solution. The prodrugs can be used for the treatment and prevention of diabetes mellitus (type I and/or type II), pathoglycemia and dyslipidemia, apoplexia, myocardial infarction and other cardiac and cardiovascular diseases, an Alzheimers disease, a Parkinsons disease and other neurodegenerative diseases, psoriasis, discoid lupus erythematosus,
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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