发明名称 Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same
摘要 The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.
申请公布号 US2012115897(A1) 申请公布日期 2012.05.10
申请号 US200913320101 申请日期 2009.12.24
申请人 TANG LUHONG;DAI AJUAN;WANG ZE;SUN YANG;LIU XINNING;XU LINGYAN;FANG XIN;QIU SHUANG;CAO YAQING;XU XIAOMIN;JIANG RUIXIA;WU CHAO;WUXI HONGRUI BIO-PHARMA-TECH CO., LTD . 发明人 TANG LUHONG;DAI AJUAN;WANG ZE;SUN YANG;LIU XINNING;XU LINGYAN;FANG XIN;QIU SHUANG;CAO YAQING;XU XIAOMIN;JIANG RUIXIA;WU CHAO
分类号 A61K31/436;A61K31/375;A61K31/407;A61P9/00;A61P11/00;A61P15/00;A61P19/02;A61P25/00;A61P25/28;A61P29/00;A61P35/00;C07D307/62;C07D491/052;C12P17/04;C12P17/18 主分类号 A61K31/436
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