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1. 发明申请

US20120115897A1 Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same 有权
标题翻译：（乙酸）丙酸抗坏血酸酯，其制备方法和含有其的药物
公开(公告)号：US20120115897A1
公开(公告)日：2012-05-10
申请号：US13320101
申请日：2009-12-24
申请人： Luhong Tang , Ajuan Dai , Ze Wang , Yang Sun , Xinning Liu , Lingyan Xu , Xin Fang , Shuang Qiu , Yaqing Cao , Xiaomin Xu , Ruixia Jiang , Chao Wu
发明人： Luhong Tang , Ajuan Dai , Ze Wang , Yang Sun , Xinning Liu , Lingyan Xu , Xin Fang , Shuang Qiu , Yaqing Cao , Xiaomin Xu , Ruixia Jiang , Chao Wu
IPC分类号： A61K31/436 , C07D491/052 , C12P17/04 , C12P17/18 , A61K31/375 , A61K31/407 , A61P29/00 , A61P19/02 , A61P25/00 , A61P25/28 , A61P35/00 , A61P15/00 , A61P11/00 , A61P9/00 , C07D307/62
CPC分类号： C07D307/62 , C07D405/12 , C07D491/04 , C07D491/052 , C12P17/04 , C12P17/16 , C12P17/188 , C12Y301/01003
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.
摘要翻译：本发明设计和合成芳基（乙酸）丙酸非甾体抗炎药物如布洛芬，酮洛芬和萘普生的抗坏血酸酯衍生物，以及衍生物与药物酸或药物碱的加成盐。以布洛芬为代表的非甾体抗炎药是常见的解热止痛药。本发明除抗炎作用外，具有明显的解热镇痛作用，安全性好，不仅适用于成人，而且适用于老年人，婴儿和儿童。芳基（乙酸）丙酸抗坏血酸酯可以转化为抗坏血酸酯衍生物，并且衍生物的加成盐与药物酸或药物碱性可以改善其水溶性，有助于静脉内施用，减少发病时间，提高生物利用度降低对胃肠道的刺激作用，增强血液渗透屏障的穿透能力，可用作新型药物，用于消炎止痛，止痛，止痛，治疗关节炎，痛经，多发性硬化，肺炎囊性纤维化，以及早产儿动脉导管未闭，预防和治疗脑中风，缺氧缺血性脑损伤，老年性痴呆和某些癌症。

2. 发明授权

US08703975B2 Aryl (ethanoic) propanoic acid ascorbyl ester, preparation method thereof and medicament containing the same 有权
标题翻译：（乙酸）丙酸抗坏血酸酯，其制备方法和含有它的药物
公开(公告)号：US08703975B2
公开(公告)日：2014-04-22
申请号：US13320101
申请日：2009-12-24
申请人： Luhong Tang , Ajuan Dai , Ze Wang , Yang Sun , Xinning Liu , Lingyan Xu , Xin Fang , Shuang Qiu , Yaqing Cao , Xiaomin Xu , Ruixia Jiang , Chao Wu
发明人： Luhong Tang , Ajuan Dai , Ze Wang , Yang Sun , Xinning Liu , Lingyan Xu , Xin Fang , Shuang Qiu , Yaqing Cao , Xiaomin Xu , Ruixia Jiang , Chao Wu
IPC分类号： C07D307/62
CPC分类号： C07D307/62 , C07D405/12 , C07D491/04 , C07D491/052 , C12P17/04 , C12P17/16 , C12P17/188 , C12Y301/01003
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.
摘要翻译：本发明设计和合成芳基（乙酸）丙酸非甾体抗炎药物如布洛芬，酮洛芬和萘普生的抗坏血酸酯衍生物，以及衍生物与药物酸或药物碱的加成盐。以布洛芬为代表的非甾体抗炎药是常见的解热止痛药。本发明除抗炎作用外，具有明显的解热镇痛作用，安全性好，不仅适用于成人，而且适用于老年人，婴儿和儿童。芳基（乙酸）丙酸抗坏血酸酯可以转化为抗坏血酸酯衍生物，并且衍生物的加成盐与药物酸或药物碱性可以改善其水溶性，有助于静脉内施用，减少发病时间，提高生物利用度降低对胃肠道的刺激作用，增强血液渗透屏障的穿透能力，可用作新型药物，用于消炎止痛，止痛，止痛，治疗关节炎，痛经，多发性硬化，肺炎囊性纤维化，以及早产儿动脉导管未闭，预防和治疗脑中风，缺氧缺血性脑损伤，老年性痴呆和某些癌症。

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