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1. 发明申请

US20080113028A1 Novel Block Copolymer, Micelle Preparation, And Anticancer Agent Containing The Same As Active Ingredient 审中-公开
标题翻译：新型嵌段共聚物，胶束制剂和含有其作为活性成分的抗癌剂
公开(公告)号：US20080113028A1
公开(公告)日：2008-05-15
申请号：US11662834
申请日：2005-09-16
申请人： Kazuhisa Shimizu , Keizou Ishikawa , Takeshi Nakanishi
发明人： Kazuhisa Shimizu , Keizou Ishikawa , Takeshi Nakanishi
IPC分类号： A61K31/337 , A61K9/14
CPC分类号： C08G81/00 , A61K9/1075 , A61K31/337 , A61K47/34
摘要： A medicinal preparation is desired which has no harmful side effects such as hypersensitive reaction, heightens the water solubility of a sparingly water-soluble anticancer agent, maintains a high drug concentration in the blood, accumulates a drug in a tumor tissue at a high concentration, heightens the pharmacological effect of the sparingly water-soluble anticancer agent, and diminishes the side effects of the anticancer agent. Provided are: a novel block copolymer which can be a drug carrier having no harmful side effects such as hypersensitive reaction; a micelle preparation in which micelles are formed and which contains a sparingly water-soluble anticancer agent, especially paclitaxel, incorporated in the micelles in an amount necessary for a disease treatment without bonding it to the block copolymer and which can heighten the solubility of the drug in water; and an anticancer agent which comprises the micelle preparation as a medical ingredient, maintains a high concentration in the blood, has more potent drug activity, and is reduced in toxicity.
摘要翻译：需要一种没有过敏反应等有害副作用的药物制剂，提高微水溶性抗癌剂的水溶性，维持血药浓度高，以高浓度积聚在肿瘤组织中的药物，提高微水溶性抗癌剂的药理作用，降低抗癌剂的副作用。提供：新型嵌段共聚物，其可以是不具有过敏反应的有害副作用的药物载体; 胶束制剂，其中形成胶束并且其含有微波水溶性抗癌剂，特别是紫杉醇，其以胶束的形式掺入到胶束中，其量不需要将其粘合到嵌段共聚物上，并且可以提高药物的溶解度在水里; 和包含胶束制剂作为医药成分的抗癌剂，在血液中保持高浓度，具有更强的药物活性，毒性降低。

2. 发明申请

US20050214375A1 Process for producing block copolymer/drug composite 审中-公开
标题翻译：制备嵌段共聚物/药物复合材料的方法
公开(公告)号：US20050214375A1
公开(公告)日：2005-09-29
申请号：US10517729
申请日：2003-06-18
申请人： Takeshi Nakanishi , Kazuhisa Shimizu
发明人： Takeshi Nakanishi , Kazuhisa Shimizu
IPC分类号： A61K9/127 , A61K9/19 , A61K31/704 , A61K31/785 , A61K47/30 , A61K47/34 , A61K47/48 , A61P35/00 , C08G73/10 , C08L71/10 , A61K9/14
CPC分类号： A61K31/785 , A61K9/19 , A61K47/34 , A61K47/6907 , C08G73/1092 , C08L71/10 , C08L2666/20
摘要： A process for producing a block copolymer-drug composite that can be industrialized, wherein neither dialysis nor ultrafiltration is performed and wherein halogenated hydrocarbons are not used. The process for producing a block copolymer-drug composite is characterized by comprising the steps of dissolving an AB type block copolymer composed of hydrophilic polymer structure moiety and hydrophobic polyamino aid structure moiety together with a drug in water or a mixed solvent of water and a low-boiling-point organic solvent miscible with water and concentrating the resultant solution.
摘要翻译：一种生产可工业化的嵌段共聚物 - 药物复合材料的方法，其中不进行透析或超滤，并且不使用卤代烃。制备嵌段共聚物 - 药物复合材料的方法的特征在于包括以下步骤：将由亲水性聚合物结构部分组成的AB型嵌段共聚物和疏水性聚氨基辅助结构部分与药物溶解在水或水和低的混合溶剂中沸点有机溶剂与水混溶并浓缩所得溶液。

3. 发明授权

US07138490B2 Block copolymer reduced in impurity content, polymeric carrier, pharmaceutical preparations in polymeric form and process for the preparation of the same 有权
标题翻译：嵌段共聚物降低杂质含量，聚合物载体，聚合物形式的药物制剂及其制备方法
公开(公告)号：US07138490B2
公开(公告)日：2006-11-21
申请号：US10481347
申请日：2002-06-19
申请人： Takeshi Nakanishi , Kazuhisa Shimizu , Ryuji Uehara , Masanobu Suzuki
发明人： Takeshi Nakanishi , Kazuhisa Shimizu , Ryuji Uehara , Masanobu Suzuki
IPC分类号： C07K1/107 , C07K1/00 , C07K1/14 , C07K2/00 , A61K38/00 , A61K38/02
CPC分类号： A61K31/704 , A61K47/645
摘要： A process for purification which permits satisfactory removal of impurities from a block copolymer consisting essentially of polyethylene glycols and poly(acidic amino acid) and is suitable for the production of a polymeric carrier having a pharmaceutically acceptable purity; a process for producing such a polymeric carrier; a block copolymer reduced in impurity content; a polymeric carrier as described above; pharmaceutical preparations in polymeric form, produced by the use of the carrier; and a method of subjecting polyethylene glycols and poly(acidic amino acids)—which are impurities contained in the block copolymer—to treatment with either an ion-exchange resin or a partition/absorption resin and then determining the quantities of them with a gel filtration column.
摘要翻译：一种纯化方法，其允许从基本上由聚乙二醇和聚（酸性氨基酸）组成的嵌段共聚物中令人满意地除去杂质，并且适用于生产具有药学上可接受的纯度的聚合物载体; 制备这种聚合物载体的方法; 嵌段共聚物杂质含量降低; 如上所述的聚合物载体; 通过使用载体生产的聚合物形式的药物制剂; 和使用嵌段共聚物中含有的杂质的聚乙二醇和聚（酸性氨基酸）与离子交换树脂或分隔/吸收树脂一起处理，然后用凝胶过滤法测定它们的量柱。