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1. 发明授权

US08809300B2 Depolymerized glycosaminoglycan from Thelenota ananas and preparation method thereof 有权
标题翻译：来自Thelenota ananas的解聚糖胺聚糖及其制备方法
公开(公告)号：US08809300B2
公开(公告)日：2014-08-19
申请号：US13512142
申请日：2010-10-25
申请人： Jinhua Zhao , Hui Kang , Mingyi Wu , Weizhen Zeng , Zi Li , Yuan Gao , Jing Cui , Zhiguo Wang , Hanlin Feng , Lin Yu
发明人： Jinhua Zhao , Hui Kang , Mingyi Wu , Weizhen Zeng , Zi Li , Yuan Gao , Jing Cui , Zhiguo Wang , Hanlin Feng , Lin Yu
IPC分类号： A61K31/726 , A61K31/715 , C08B37/00 , C07H5/06 , A61P7/02 , A61K31/737
CPC分类号： A61K31/737 , A61K31/726 , C08B37/0063
摘要： Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3−), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3− is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.
摘要翻译：公开了来自Thelenota ananas（dTHG）的解聚糖胺聚糖（dTHG），其重均分子量为约8000-20000Da，其单糖组分为乙酰半乳糖胺（GalNAc），葡糖醛酸（GlcUA），岩藻糖（Fuc）或其硫酸盐表达为-OSO3-），其中GalNAc：GlcUA：Fuc：-OSO3-的摩尔比为约1：（1±0.3）：（1±0.3）：（3.5±0.5）。所述dTHG是一种有效的因子X的内源性抑制剂，其具有良好的抗凝血和抗血栓形成活性，可用于预防和/或治疗血栓性疾病。还提供了一种制备所述dTHG的方法，其包括以下步骤：1）从Thelenota ananas的体壁提取并获得岩藻糖基化的糖胺聚糖（THG）; 2）解聚THG，通过过氧化物解聚法或第四周期过渡金属离子催化剂催化的过氧化物解聚方法得到dTHG; 3）去除dTHG中具有较低和/或更高分子量的杂质。

2. 发明申请

US20120270834A1 DEPOLYMERIZED GLYCOSAMINOGLYCAN FROM THELENOTA ANANAS AND PREPERATION METHOD THEREOF 有权
标题翻译：来自THENENOTA ANANAS的分解的谷氨酰胺聚糖及其制备方法
公开(公告)号：US20120270834A1
公开(公告)日：2012-10-25
申请号：US13512142
申请日：2010-10-25
申请人： Jinhua Zhao , Hui Kang , Mingyi Wu , Weizhen Zeng , Zi LI , Yuan Gao , Jing Cui , Zhiguo Wang , Hanlin Feng , Lin Yu
发明人： Jinhua Zhao , Hui Kang , Mingyi Wu , Weizhen Zeng , Zi LI , Yuan Gao , Jing Cui , Zhiguo Wang , Hanlin Feng , Lin Yu
IPC分类号： A61K31/726 , A61P7/02 , C08B37/00
CPC分类号： A61K31/737 , A61K31/726 , C08B37/0063
摘要： Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3−), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3− is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.
摘要翻译：公开了来自Thelenota ananas（dTHG）的解聚糖胺聚糖（dTHG），其重均分子量为约8000-20000Da，其单糖组分为乙酰半乳糖胺（GalNAc），葡糖醛酸（GlcUA），岩藻糖（Fuc）或其硫酸盐表达为-OSO3-），其中GalNAc：GlcUA：Fuc：-OSO3-的摩尔比为约1：（1±0.3）：（1±0.3）：（3.5±0.5）。所述dTHG是一种有效的因子X的内源性抑制剂，其具有良好的抗凝血和抗血栓形成活性，可用于预防和/或治疗血栓性疾病。还提供了一种制备所述dTHG的方法，其包括以下步骤：1）从Thelenota ananas的体壁提取并获得岩藻糖基化的糖胺聚糖（THG）; 2）解聚THG，通过过氧化物解聚法或第四周期过渡金属离子催化剂催化的过氧化物解聚方法得到dTHG; 3）去除dTHG中具有较低和/或更高分子量的杂质。

3. 发明申请

US20080293643A1 Crystalline Form I of 3,4'5-Trihydroxy-Stilbene-3-B-D Glucoside 有权
标题翻译： 3,4'5-三羟基 - 二苯乙烯-3-B-D葡萄糖苷的结晶形式I
公开(公告)号：US20080293643A1
公开(公告)日：2008-11-27
申请号：US12097321
申请日：2006-08-28
申请人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
发明人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
IPC分类号： A61K31/7048 , C07G3/00 , A61P43/00
CPC分类号： C07H15/20
摘要： The present invention relates to a novel crystalline form of a Compound 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. Crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.
摘要翻译：本发明涉及化合物3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷（多聚糖）的新结晶形式及其制备和应用的方法，以及含有结晶形式的药物组合物 I的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷。本发明的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的结晶形式I具有稳定的晶体形态，确定的熔点和良好的化学稳定性。这种新型形式的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷具有制备固体制剂所需的性质，并且在配制时易于制成并容易形成，这允许原料材料成本较高，生产操作更加容易，工业药品生产质量更易于控制，而且储存更方便。

4. 发明申请

US20080261902A1 Pharmaceutical composition containing polydatin and its application 审中-公开
标题翻译：含有多聚糖的药物组合物及其应用
公开(公告)号：US20080261902A1
公开(公告)日：2008-10-23
申请号：US12157810
申请日：2008-06-13
申请人： Jinhua Zhao , Hui Kang , Weizhen Zeng , Lijuan Zhang , Dan Zhu , Chuangui Huang , Hong Chen , Hanlin Feng , Lin Yu , Xuliang Huang , Guiling Zhao , Kesen Zhao
发明人： Jinhua Zhao , Hui Kang , Weizhen Zeng , Lijuan Zhang , Dan Zhu , Chuangui Huang , Hong Chen , Hanlin Feng , Lin Yu , Xuliang Huang , Guiling Zhao , Kesen Zhao
IPC分类号： A61K31/7034 , A61P7/04
CPC分类号： A61K31/7034 , A61K9/0019
摘要： A composition includes polydatin and solvent for dissolving the polydatin, wherein the solvent comprises alcohol in a range between 40 and 95% by volume, propanediol in a range between 0 and 60% by volume, and water in remaining volume. The concentration of the polydatin must be at least 6 mg/ml. The composition has good stability in cold preservation. The composition is in a pharmaceutically acceptable administrative form selected from the group consisting of an intravenous injection, and intramuscular injection, an oral administration, a spray solution, and an aerosol form.
摘要翻译：一种组合物包括用于溶解多聚糖的多聚糖和溶剂，其中该溶剂包含体积范围为40至95体积％的丙二醇，体积为0至60体积％的丙二醇和剩余体积的水。多聚糖的浓度必须至少为6 mg / ml。该组合物在冷藏中具有良好的稳定性。组合物是选自静脉内注射和肌内注射，口服给药，喷雾溶液和气雾剂形式的药学上可接受的行政形式。

5. 发明授权

US08575115B2 Crystalline form I of 3,4′5-trihydroxy-stilbene-3-β-D glucoside 有权
标题翻译： 3,4'5-三羟基 - 二苯乙烯-3-β-D葡萄糖苷的结晶形式I
公开(公告)号：US08575115B2
公开(公告)日：2013-11-05
申请号：US12097321
申请日：2006-08-28
申请人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
发明人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H15/20
摘要： The present invention relates to a novel crystalline form of a Compound 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. Crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.
摘要翻译：本发明涉及化合物3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷（多聚糖）的新结晶形式及其制备和应用的方法，以及含有结晶形式的药物组合物 I的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷。本发明的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的结晶形式I具有稳定的结晶形态，确定的熔点和良好的化学稳定性。这种3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的新形式具有制备固体制剂所需的性质，并且在配制时易于制成并易于成型，这允许原料材料成本较高，生产操作更加容易，工业药品生产质量更易于控制，而且储存更方便。

6. 发明申请

US20080176810A1 Use of 3, 4', 5-Trihydroxy-Stilbene-3-Beta-D-glucoside in Prepartion of Medicines For Treating and/or Preventing Ischemic Heart Disease 审中-公开
标题翻译： 3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷在制备药物治疗和/或预防缺血性心脏病方面的应用
公开(公告)号：US20080176810A1
公开(公告)日：2008-07-24
申请号：US11720451
申请日：2005-11-14
申请人： Jinhua Zhao , Jiangping Xu , Hui Kang , Bing Wang , Jing Li , Hanlin Feng , Lin Yu
发明人： Jinhua Zhao , Jiangping Xu , Hui Kang , Bing Wang , Jing Li , Hanlin Feng , Lin Yu
IPC分类号： A61K31/7028 , A61P9/10
CPC分类号： A61K31/7032
摘要： The present invention provides new use of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside has efficacies of anti-myocardial ischemia by intravenous injection and/or oral administration. It is advantageous that 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside as anti-myocardial ischemia drug is used to prepare the medicine for treating and/or preventing ischemic heart disease.
摘要翻译：本发明提供3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的新用途。 3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷通过静脉注射和/或口服给药具有抗心肌缺血的功效。使用3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷作为抗心肌缺血药物来制备用于治疗和/或预防缺血性心脏病的药物。

7. 发明申请

US20080009453A1 Pharmceutical Compositions Containing Polydatin or Its Salts and Their Application 审中-公开
标题翻译：含有多聚糖或其盐的药物组合物及其应用
公开(公告)号：US20080009453A1
公开(公告)日：2008-01-10
申请号：US10492405
申请日：2003-08-04
申请人： Jinhua Zhao , Hui Kang , Kesen Zhao , Xuliang Huang , Guiling Zhao , Jing Li , Hanlin Feng , Guanghui Yao , Qian Yao , Shengzhao Lin , Qi Zhou
发明人： Jinhua Zhao , Hui Kang , Kesen Zhao , Xuliang Huang , Guiling Zhao , Jing Li , Hanlin Feng , Guanghui Yao , Qian Yao , Shengzhao Lin , Qi Zhou
IPC分类号： A61K31/7034 , A61P7/00 , A61P9/00
CPC分类号： A61K31/7032
摘要： The invention discloses pharmaceutical compositions containing polydatin or its pharmaceutically acceptable salts with the effect of improving microcirculation, and their application in preparing drugs which can improve microcirculation. The compositions are an non-gastrointestinal injection preparation, the preparation can be an aqueous solution which have pH 7.0-10.0 comprising 5-50% propandiol. The dosage forms of the compositions may be lyophilizing powder injection, oral form, suppository of procto-administration and other forms of administrations comprising unguent, ointment, paste film coating and the like. The compositions may be used to treat and/or prevent diseases related to microcirculation blockage. The unit form may contain 1-1000 mg polydatin or its derivatives. The invention solves the problem of using polydatin to improve microcirculation. The composition of the invention can be used in treating shock, cardiac and cerebrovascular diseases, diseases of sense organs, diabetes complication, vaculitis related to blockage of blood vessel, hemorrhoid related to circulation obstruction, skin injury and burn.
摘要翻译：本发明公开了含有多糖或其药学上可接受的盐的药物组合物，其具有改善微循环的作用，以及它们在制备可改善微循环的药物中的应用。组合物是非消化道注射制剂，该制剂可以是含有5-50％丙二醇的pH 7.0-10.0的水溶液。组合物的剂型可以是冷冻干燥粉末注射剂，口服剂型，直接给药栓剂和包括无制剂，软膏剂，糊剂涂膜等的其它形式的给药。组合物可用于治疗和/或预防与微循环阻塞有关的疾病。单位形式可能含有1-1000 mg多聚糖或其衍生物。本发明解决了使用多聚糖改善微循环的问题。本发明的组合物可用于治疗休克，心脑血管疾病，感觉器官疾病，糖尿病并发症，与血管阻塞有关的空洞炎，与循环障碍相关的痔疮，皮肤损伤和烧伤。

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