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1. 发明授权

US08940332B2 High-molecular weight conjugate of podophyllotoxins 有权
标题翻译：鬼臼毒素的高分子量结合物
公开(公告)号：US08940332B2
公开(公告)日：2015-01-27
申请号：US12226962
申请日：2007-05-16
申请人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
发明人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
IPC分类号： A61K9/14 , A61K31/7048 , A61K9/00 , A61K31/365 , A61K47/48 , C08G65/331 , C08G65/332 , C08G73/10 , C08G83/00 , C08L71/02 , A61K47/26 , C08L77/00
CPC分类号： A61K31/7048 , A61K9/0019 , A61K31/365 , A61K47/26 , A61K47/60 , C08G65/331 , C08G65/3314 , C08G65/3324 , C08G73/1092 , C08G83/00 , C08L71/02 , C08L77/00 , C08L2203/02 , C08L2205/05 , C08L2666/20
摘要： A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.
摘要翻译：已经要求一种新颖的鬼臼毒素衍生物，其能够释放药物而不依赖于生物酶，并且可以预期其具有有效的治疗效果并且可溶于水。具有聚乙二醇结构单元和两种或更多种琥珀酸单酰胺结构单元的聚合物，特别是鬼臼毒素的聚合物缀合物，其中聚乙二醇/聚天冬氨酸共聚物的羧酸基和鬼臼毒酚羟基并通过酯键连接。

2. 发明申请

US20090162313A1 High-Molecular Weight Conjugate of Podophyllotoxins 有权
标题翻译：鬼臼毒素的高分子量偶联物
公开(公告)号：US20090162313A1
公开(公告)日：2009-06-25
申请号：US12226962
申请日：2007-05-16
申请人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
发明人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
IPC分类号： A61K31/765 , A61P35/00
CPC分类号： A61K31/7048 , A61K9/0019 , A61K31/365 , A61K47/26 , A61K47/60 , C08G65/331 , C08G65/3314 , C08G65/3324 , C08G73/1092 , C08G83/00 , C08L71/02 , C08L77/00 , C08L2203/02 , C08L2205/05 , C08L2666/20
摘要： [PROBLEMS] A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded.[MEANS FOR SOLVING PROBLEMS] A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.
摘要翻译： [问题]需要能够释放药物而不依赖于生物酶并且可以预期具有有效治疗效果并且可溶于水的新型鬼臼毒素衍生物。用于解决问题的方法具有聚乙二醇结构单元和两种或更多种琥珀酸单酰胺结构单元的聚合物，特别是鬼臼毒素的聚合物缀合物，其中聚乙二醇/聚天冬氨酸共聚物的羧酸基和鬼臼毒素的羟基和连接的通孔提供酯键。

3. 发明授权

US09346923B2 Method for manufacturing block copolymer 有权
标题翻译：制备嵌段共聚物的方法
公开(公告)号：US09346923B2
公开(公告)日：2016-05-24
申请号：US14241924
申请日：2012-08-31
申请人： Keiichirou Yamamoto , Masayuki Kitagawa
发明人： Keiichirou Yamamoto , Masayuki Kitagawa
IPC分类号： C08G65/333 , C08G73/10 , C08G81/00 , C08G69/10 , C08G69/40 , C08G73/14
CPC分类号： C08G81/00 , C08G65/3315 , C08G65/333 , C08G65/33334 , C08G69/10 , C08G69/40 , C08G73/14
摘要： Providing a method for producing a compound represented by formula (1) from a compound represented by formula (2), by which the additive amount of an aryl (C1-C8) alkyl alcohol which may have a substituent and the amount of residual carboxyl groups of pAsp (polyaspartic acid) are controlled.A production method including obtaining a compound represented by formula (1) by allowing a compound represented by formula (2) to react with an aryl (C1-C8) alkyl alcohol which may have a substituent, and a carbodiimide-based compound in an amount of 2(x+y) equivalents or more relative to the amount of carboxyl groups in formula (2) (sum of x and y), in a solvent at 15° C. to 30° C. for 2 hours to 48 hours, is used.
摘要翻译：提供由式（2）表示的化合物制备由式（1）表示的化合物的方法，其中可以具有取代基的芳基（C1-C8）烷基醇的添加量和残留的羧基的量的pAsp（聚天冬氨酸）被控制。一种制备方法，包括通过使式（2）表示的化合物与可以具有取代基的芳基（C1-C8）烷基醇反应得到式（1）表示的化合物和碳二亚胺类化合物相对于式（2）中的羧基量（x和y的总和）为2（x + y）当量或更多，在15℃至30℃的溶剂中2小时至48小时，用来。

4. 发明申请

US20140288244A1 Method For Manufacturing Block Copolymer 有权
标题翻译：制备嵌段共聚物的方法
公开(公告)号：US20140288244A1
公开(公告)日：2014-09-25
申请号：US14241924
申请日：2012-08-31
申请人： Keiichirou Yamamoto , Masayuki Kitagawa
发明人： Keiichirou Yamamoto , Masayuki Kitagawa
IPC分类号： C08G81/00
CPC分类号： C08G81/00 , C08G65/3315 , C08G65/333 , C08G65/33334 , C08G69/10 , C08G69/40 , C08G73/14
摘要： Providing a method for producing a compound represented by formula (1) from a compound represented by formula (2), by which the additive amount of an aryl (C1-C8) alkyl alcohol which may have a substituent and the amount of residual carboxyl groups of pAsp (polyaspartic acid) are controlled.A production method including obtaining a compound represented by formula (1) by allowing a compound represented by formula (2) to react with an aryl (C1-C8) alkyl alcohol which may have a substituent, and a carbodiimide-based compound in an amount of 2(x+y) equivalents or more relative to the amount of carboxyl groups in formula (2) (sum of x and y), in a solvent at 15° C. to 30° C. for 2 hours to 48 hours, is used.
摘要翻译：提供由式（2）表示的化合物制备由式（1）表示的化合物的方法，其中可以具有取代基的芳基（C1-C8）烷基醇的添加量和残留的羧基的量的pAsp（聚天冬氨酸）被控制。一种制备方法，包括通过使式（2）表示的化合物与可以具有取代基的芳基（C1-C8）烷基醇反应得到式（1）表示的化合物和碳二亚胺类化合物相对于式（2）中的羧基量（x和y的总和）为2（x + y）当量或更多，在15℃至30℃的溶剂中2小时至48小时，用来。

5. 发明申请

US20090239782A1 High-molecular weight conjugate of resorcinol derivatives 审中-公开
标题翻译：间苯二酚衍生物的高分子量缀合物
公开(公告)号：US20090239782A1
公开(公告)日：2009-09-24
申请号：US12311086
申请日：2007-09-27
申请人： Masaharu Nakamura , Masayuki Kitagawa , Keiichirou Yamamoto , Chieko Seno
发明人： Masaharu Nakamura , Masayuki Kitagawa , Keiichirou Yamamoto , Chieko Seno
IPC分类号： A61K38/02 , C07K2/00 , A61P35/00
CPC分类号： A61K31/787 , C08G69/10 , C08G73/1092 , C08G81/00 , C08G2650/38
摘要： Provided is a high-molecular weight conjugate of resorcinol derivatives which is excellent in water solubility and stability and has high antitumor activity even when used in a smaller total drug amount than the resorcinol derivatives. The high-molecular weight conjugate of resorcinol derivatives comprises a structure in which a carboxyl group of polymer moiety having a carboxyl group in the side chain and polyethylene glycol moiety is linked to a hydroxyl group of resorcinol derivatives via an ester bond.
摘要翻译：提供了间苯二酚衍生物的高分子量缀合物，其水溶性和稳定性优异，并且即使以比间苯二酚衍生物更小的总药物量使用也具有高抗肿瘤活性。间苯二酚衍生物的高分子量缀合物包括其侧链中具有羧基的聚合物部分的羧基和聚乙二醇部分通过酯键与间苯二酚衍生物的羟基连接的结构。

6. 发明申请

US20060067910A1 High-molecular weight derivatives of camptothecins 有权
公开(公告)号：US20060067910A1
公开(公告)日：2006-03-30
申请号：US10532670
申请日：2003-10-29
申请人： Masayuki Kitagawa , Kazuya Okamoto
发明人： Masayuki Kitagawa , Kazuya Okamoto
IPC分类号： A61K31/785 , C08G63/91
CPC分类号： C07D491/22 , A61K31/4745 , A61K47/60 , A61K47/645
摘要： It is intended to provide water-soluble derivative of camptothecins which are excellent in therapeutic effect and suitable for chemotherapy for cancer. Namely, a water-soluble high-molecular weight derivative of camptothencins being excellent in sustained-release which is obtained by ester-bonding a carboxylic acid group of a polyethylene glycol-polycarboxylic acid polymer to a phenolic hydroxyl group of phenolic camptothencins.

7. 发明授权

US06820166B2 System for associating a function to an entity capable of communicating data across an interface 失效
标题翻译：用于将功能与能够通过接口通信数据的实体相关联的系统
公开(公告)号：US06820166B2
公开(公告)日：2004-11-16
申请号：US09757314
申请日：2001-01-09
申请人： Masayuki Kitagawa
发明人： Masayuki Kitagawa
IPC分类号： G06F1300
CPC分类号： G06F13/4068
摘要： The present invention relates to a method and system for selecting one of the two functions. The system in accordance with one embodiment of the invention includes a first entity that has a host function and a device function, and a second entity that has at least one of the two functions. The system further includes a detector and a selecting mechanism. The detector detects the second entity when the first entity is connected to the second entity. The selecting mechanism responds to an output of the detector and selects one out of the host and device functions of the first entity.
摘要翻译：本发明涉及一种用于选择两个功能之一的方法和系统。根据本发明的一个实施例的系统包括具有主机功能和设备功能的第一实体以及具有两个功能中的至少一个功能的第二实体。该系统还包括检测器和选择机构。当第一实体连接到第二实体时，检测器检测第二实体。选择机制响应于检测器的输出，并从第一实体的主机和设备功能中选出一个。

8. 发明授权

US5179084A Antiviral phosphoric acid esters of oxetanocins 失效
标题翻译：氧化亚油酸的抗性磷酸酯
公开(公告)号：US5179084A
公开(公告)日：1993-01-12
申请号：US504393
申请日：1990-04-04
申请人： Seiichi Saito , Shigeru Hasegawa , Masayuki Kitagawa , Nobuyoshi Shimada , Katsutoshi Takahashi , Jun-ichi Seki , Hiroo Hoshino , Yukihiro Nishiyama , Kenichi Matsubara , Takemitsu Nagahata
发明人： Seiichi Saito , Shigeru Hasegawa , Masayuki Kitagawa , Nobuyoshi Shimada , Katsutoshi Takahashi , Jun-ichi Seki , Hiroo Hoshino , Yukihiro Nishiyama , Kenichi Matsubara , Takemitsu Nagahata
IPC分类号： C07H19/02
CPC分类号： C07H19/02
摘要： The present invention relates to phosphoric acid esters of oxetanocins having an antiviral activity which are represented by general formula (I): ##STR1## wherein R.sub.1 represents a phosphoric acid ester residue, X represents hydrogen, hydroxy or hydroxymethyl group, and B represents a purine base residue, and pharmacologically acceptable salts thereof.

9. 发明申请

US20120116051A1 Polymer Conjugate Of Bioactive Substance Having Hydroxy Group 有权
标题翻译：具有羟基的生物活性物质的共轭物
公开(公告)号：US20120116051A1
公开(公告)日：2012-05-10
申请号：US13319175
申请日：2010-05-12
申请人： Masayuki Kitagawa , Chieko Seno , Keiko Ebara , Kazutoshi Takashio
发明人： Masayuki Kitagawa , Chieko Seno , Keiko Ebara , Kazutoshi Takashio
IPC分类号： C08H1/00 , A61P9/10 , A61P17/14 , A61P29/00 , A61P35/00
CPC分类号： C08G69/10 , A61K31/167 , A61K31/19 , A61K31/195 , A61K31/337 , A61K31/365 , A61K31/4745 , A61K31/52 , A61K31/573 , A61K31/704 , A61K31/7052 , A61K31/7068 , A61K47/60 , A61K47/645 , C08G69/40 , C08G69/48
摘要： A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX—CY represents CH—CH or C═C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].
摘要翻译：需要生物活性物质的聚合物缀合物，其使药物释放与生物酶无关并且可以预期具有高治疗效果。提供了一种生理活性物质的聚合物缀合物，其包含聚乙二醇部分和具有两个或更多个羧基的聚合物的嵌段共聚物，其中由通式（I）或通式（II）表示的取代基与嵌段共聚物中的至少一个侧链羧基通过酰胺键[在式中，R8和R9各自独立地为氢原子或可具有取代基的（C1-C6）烷基，R10为氢原子（可以具有取代基的C 1 -C 40的烷基，可以具有取代基的（C 1〜C 40）芳烷基，可以具有取代基的芳香族基，具有被保护的羧基的氨基酸残基，取代基，CX-CY表示CH-CH或C = C（双键），A表示通过从具有一个或多个羟基的生理活性物质除去一个或多个羟基之一而获得的残基]。

10. 发明申请

US20100234537A1 POLYMER CONJUGATE OF TAXANE 有权
标题翻译： TAXANE的聚合物
公开(公告)号：US20100234537A1
公开(公告)日：2010-09-16
申请号：US12225230
申请日：2007-03-22
申请人： Masayuki Kitagawa , Keizou Ishikawa , Takeshi Onda
发明人： Masayuki Kitagawa , Keizou Ishikawa , Takeshi Onda
IPC分类号： C08G69/48
CPC分类号： C08G65/33324 , A61K31/337 , A61K47/60 , A61K47/645 , C08G65/329 , C08G69/10 , C08G69/40 , C08G69/48 , C08L2203/02
摘要： [Problems] To provide a novel taxane derivative which can release the medicinal substance in a bioenzyme-independent manner, is expected to have an effective therapeutic efficacy, and has a water-solubility.[Means for Solving Problems] Disclosed is a polymer conjugate of a taxane, which comprises a polymer having a polyethylene glycol moiety and two or more succinic acid monoamide moieties and a taxane, wherein a carboxylate group in the polymer and an alcoholic hydroxyl group in the taxane are bound to each other via an ester bonding.
摘要翻译： [问题]为了提供能够以不依赖生物酶的方式释放药物的新型紫杉烷衍生物，预期具有有效的治疗功效，并且具有水溶性。解决问题的手段公开了紫杉烷的聚合物缀合物，其包含具有聚乙二醇部分和两个或多个琥珀酸单酰胺部分的聚合物和紫杉烷，其中聚合物中的羧酸酯基团和紫杉烷通过酯键相互结合。

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