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1. 发明授权

US08435962B2 Triacetyl-3-hydroxyphenyladenosine and its use for regulating blood fat 有权
标题翻译：三乙酰基-3-羟基苯基腺苷及其用于调节血脂的用途
公开(公告)号：US08435962B2
公开(公告)日：2013-05-07
申请号：US13255153
申请日：2009-03-10
申请人： Haibo Zhu , Song Wu , Linghua Hao , Kai Qu , Ping Zhu , Xing Wang , Wei Li
发明人： Haibo Zhu , Song Wu , Linghua Hao , Kai Qu , Ping Zhu , Xing Wang , Wei Li
IPC分类号： A01N43/04 , A61K31/70 , C07H19/20
CPC分类号： A61K31/7076 , C07H19/167
摘要： The invention discloses triacetyl-3-hydroxyphenyladenosine represented by formula (I), the preparation, the pharmaceutical composition and the use thereof. Specially, the invention discloses a new compound of 2′,3′,5′-tri-O-acetyl-N6-(3-hydroxyphenyl)adenosine. Using hypoxanthine nucleoside as starting material, the compound is prepared by acetylating with acetic anhydride, chlorinating with thionyl chloride, and being substituted with 3-hydroxy aniline. The invention also discloses the pharmaceutical composition comprising triacetyl-3-hydroxyphenyladenosine. The dosage forms of the said pharmaceutical composition include tablet, capsule, pill, injection, sustained release preparation, controlled release preparation or particulate delivery system. The medicament for treatment or precaution of hyperlipemia prepared by the compound of the invention has the advantages of significant hypolipidemic activity, less toxicity and adverse effect as well as slow metabolism in vivo.
摘要翻译：本发明公开了由式（I）表示的三乙酰基-3-羟基苯基腺苷，其制备方法，药物组合物及其用途。特别地，本发明公开了一种新的2'，3'，5'-三-O-乙酰基-N6-（3-羟基苯基）腺苷化合物。使用次黄嘌呤核苷作为起始原料，该化合物通过用乙酸酐乙酰化制备，用亚硫酰氯氯化，并被3-羟基苯胺取代。本发明还公开了包含三乙酰基-3-羟基苯基腺苷的药物组合物。所述药物组合物的剂型包括片剂，胶囊，丸剂，注射剂，缓释制剂，控制释放制剂或颗粒递送系统。用于治疗或预防本发明化合物制备的高脂血症的药物具有明显的降血脂活性，较低毒性和不良反应以及体内代谢缓慢的优点。

2. 发明申请

US20120053143A1 TRIACETYL-3-HYDROXYPHENYLADENOSINE AND ITS USE FOR REGULATING BLOOD FAT 有权
标题翻译：三硝基-3-羟基苯基腺苷及其用于调节血液脂肪
公开(公告)号：US20120053143A1
公开(公告)日：2012-03-01
申请号：US13255153
申请日：2009-03-10
申请人： Haibo Zhu , Song Wu , Linghua Hao , Kai Qu , Ping Zhu , Xing Wang , Wei Li
发明人： Haibo Zhu , Song Wu , Linghua Hao , Kai Qu , Ping Zhu , Xing Wang , Wei Li
IPC分类号： A61K31/7076 , C07H1/00 , A61P3/06 , C07H19/167
CPC分类号： A61K31/7076 , C07H19/167
摘要： The invention discloses triacetyl-3-hydroxyphenyladenosine represented by formula (I), the preparation, the pharmaceutical composition and the use thereof. Specially, the invention discloses a new compound of 2′,3′,5′-tri-O-acetyl-N6-(3-hydroxyphenyl)adenosine. Using hypoxanthine nucleoside as starting material, the compound is prepared by acetylating with acetic anhydride, chlorinating with thionyl chloride, and being substituted with 3-hydroxy aniline. The invention also discloses the pharmaceutical composition comprising triacetyl-3-hydroxyphenyladenosine. The dosage forms of the said pharmaceutical composition include tablet, capsule, pill, injection, sustained release preparation, controlled release preparation or particulate delivery system. The medicament for treatment or precaution of hyperlipemia prepared by the compound of the invention has the advantages of significant hypolipidemic activity, less toxicity and adverse effect as well as slow metabolism in vivo.
摘要翻译：本发明公开了由式（I）表示的三乙酰基-3-羟基苯基腺苷，其制备方法，药物组合物及其用途。特别地，本发明公开了一种新的2'，3'，5'-三-O-乙酰基-N6-（3-羟基苯基）腺苷化合物。使用次黄嘌呤核苷作为起始原料，该化合物通过用乙酸酐乙酰化制备，用亚硫酰氯氯化，并被3-羟基苯胺取代。本发明还公开了包含三乙酰基-3-羟基苯基腺苷的药物组合物。所述药物组合物的剂型包括片剂，胶囊，丸剂，注射剂，缓释制剂，控制释放制剂或颗粒递送系统。用于治疗或预防本发明化合物制备的高脂血症的药物具有明显的降血脂活性，较低毒性和不良反应以及体内代谢缓慢的优点。

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