公开(公告)号：US06812367B2

公开(公告)日：2004-11-02

申请号：US10463547

申请日：2003-06-18

申请人： Kenji Sakanoue ,  Kouzoh Sanchika ,  Tohru Yasukohchi

发明人： Kenji Sakanoue ,  Kouzoh Sanchika ,  Tohru Yasukohchi

IPC分类号： C07C4318

CPC分类号： C08G65/2609 ,  C08L2203/02

摘要： Polyethylene glycol for use in fields with application to a living body wherein the sum of the contents of ethylene glycol and diethylene glycol in the polyethylene glycol is less than or equal to that expressed in the following formula [I]: Sum ⁢   ⁢ of ⁢   ⁢ ethylene ⁢   ⁢ glycol ⁢   ⁢ and ⁢   ⁢ diethylene ⁢   ⁢ glycol ⁢   ⁢ contents ⁢   ⁢ ( ppm ) = 150 × 2900 × 0.85 ( x - 150 ) / 44 x [ I ] wherein x represents the average molecular weight of the polyethylene glycol, and the polyethylene glycol has an average molecular weight ranging from 190 to 1,050.

摘要翻译： 聚乙二醇用于应用于生物体的领域，其中聚乙二醇中乙二醇和二甘醇的含量之和小于或等于下式[I]表示的含量：其中x表示平均分子量 聚乙二醇的重量，聚乙二醇的平均分子量为190〜1050。

公开(公告)号：US5463066A

公开(公告)日：1995-10-31

申请号：US349368

申请日：1994-12-05

申请人： Tsuyoshi Miyazaki ,  Kouzoh Sanchika ,  Mitsuhiro Nishida ,  Tohru Yasukohchi ,  Shigeru Kitano ,  Akinori Suginaka ,  Yoshihito Kadoma

发明人： Tsuyoshi Miyazaki ,  Kouzoh Sanchika ,  Mitsuhiro Nishida ,  Tohru Yasukohchi ,  Shigeru Kitano ,  Akinori Suginaka ,  Yoshihito Kadoma

IPC分类号： A61K9/127 ,  A61K47/48 ,  C07D233/64 ,  C07F9/6506 ,  C08G65/332 ,  C08G65/335

CPC分类号： C08G65/3328 ,  A61K47/48238 ,  A61K47/48815 ,  A61K9/1271 ,  C07F9/65061 ,  C08G65/335

摘要： A novel and useful phospholipid derivative to be used for a reactive vesicle-forming agent, which is represented by the following general formula (1): ##STR1## in which R.sup.1 C(.dbd.O) and R.sup.2 C(.dbd.O) represent each an aliphatic acyl group, R.sup.3 denotes hydrogen atom or methyl group, OA represents an oxyalkylene group of 2-4 carbon atoms, n indicates the average addition mole number of added oxyalkylene group and is 1-1,000, p is 0 or 1, X represents ##STR2## with q and r being each an integer of 0 to 4 or 1 to 4, respectively, and M denotes hydrogen atom or an alkali metal atom.

摘要翻译： 用于反应性泡囊形成剂的新型有用的磷脂衍生物，其由以下通式（1）表示：各自为脂族酰基，R 3表示氢原子或甲基，OA表示氧化烯基 2-4个碳原子，n表示加成的氧化烯基的平均加成摩尔数，为1-1000，p为0或1，X为4或1〜4，M为氢原子或碱金属原子 。

公开(公告)号：US06455639B1

公开(公告)日：2002-09-24

申请号：US09367642

申请日：1999-08-19

申请人： Tohru Yasukohchi ,  Kouzoh Sanchika ,  Chika Itoh ,  Kei-ichi Maruyama

发明人： Tohru Yasukohchi ,  Kouzoh Sanchika ,  Chika Itoh ,  Kei-ichi Maruyama

IPC分类号： C08G6528

CPC分类号： C08G65/2609 ,  C08G65/30 ,  G01N30/90

摘要： An oxirane derivative and process for preparation of the same, having a high purity characterized in terms of gel permeation chromatography and thin layer chromatography. The oxirane derivative is useful as a starting material for medical purposes, and mainly drug delivery systems.

摘要翻译： 一种环氧乙烷衍生物及其制备方法，具有以凝胶渗透色谱和薄层色谱为特征的高纯度。 环氧乙烷衍生物可用作医疗用途的原料，主要用于药物输送系统。

公开(公告)号：US5767284A

公开(公告)日：1998-06-16

申请号：US868261

申请日：1997-06-03

申请人： Kouzoh Sanchika ,  Tohru Yasukohchi ,  Kei-ichi Maruyama ,  Syunsuke Ohhashi

发明人： Kouzoh Sanchika ,  Tohru Yasukohchi ,  Kei-ichi Maruyama ,  Syunsuke Ohhashi

IPC分类号： C08G65/32 ,  A61K47/48 ,  C07D207/46 ,  C08G65/30 ,  C08G65/329 ,  C08G65/332 ,  C08G65/333 ,  C07D207/12

CPC分类号： A61K47/48215 ,  C08G65/30 ,  C08G65/329 ,  C08G65/33337

摘要： A process for producing a polyoxyalkylene derivative substituted with succinimidyl group which comprises reacting a polyoxyalkylene compound having carboxyl group at ends with N-hydroxysuccinimide in an inert solvent in the presence of dicyclohexylcarbodiimide; filtering an obtained reaction product; and crystallizing the polyoxyalkylene derivative substituted with succinimidyl group by adding isopropyl alcohol to a filtrate obtained by the filtration, an amount by weight of isopropyl alcohol being 1 to 100 times as much as an amount by weight of the polyoxyalkylene compound having carboxyl group at ends. Materials can be handled with safety in the process of the present invention, and a highly pure polyoxyalkylene derivative substituted with succinimidyl group which does not cause turbidity in an aqueous solution and has an excellent quality as a material for drugs can be produced.

摘要翻译： 一种制备被琥珀酰亚胺基取代的聚氧化烯衍生物的方法，包括在二环己基碳二亚胺的存在下，在惰性溶剂中使具有羧基的聚氧化烯化合物与N-羟基琥珀酰亚胺反应; 过滤得到的反应产物; 并将通过过滤得到的滤液中加入异丙醇使用琥珀酰亚胺基取代的聚氧化烯衍生物结晶，异丙醇的重量比在末端具有羧基的聚氧化烯化合物的重量的1〜100倍。 可以在本发明的方法中安全地处理材料，并且可以制备用琥珀酰亚胺基取代的高纯度聚氧化烯衍生物，其不会在水溶液中引起浊度并且具有作为药物的材料的优良品质。

公开(公告)号：US20050208671A1

公开(公告)日：2005-09-22

申请号：US11019189

申请日：2004-12-23

申请人： Nobuko Takano ,  Kouzoh Sanchika

发明人： Nobuko Takano ,  Kouzoh Sanchika

IPC分类号： G01N30/86 ,  G01N33/00

CPC分类号： G01N30/8624 ,  G01N30/8631

摘要： An object the invention is to provide a method of analyzing the activation ratio of terminals of a polyoxyalkylene derivative so that the ratio can be accurately measured at a high precision even when the polyoxyalkylene derivative has a high molecular weight. The activation ratio of terminal of a polyoxyalkylene derivative having a terminal active group capable of bonding with a biologically active substance having a molecular weight of 1000 to 100000 is analyzed. The active group is labeled using a labeling reagent having an ionic functional group. The polyoxyalkylene derivative is then analyzed by means of liquid chromatography using an ion-exchange column and an RI detector outputting a chromatogram. The activation ratio of terminal is obtained based on percentage of an area of a peak corresponding to the active group in the chromatogram.

摘要翻译： 本发明的目的是提供一种分析聚氧亚烷基衍生物的末端的活化比例的方法，即使聚氧亚烷基衍生物具有高分子量也能以高精度精确测定该比例。 分析具有能够与分子量为1000〜100000的生物活性物质结合的末端活性基团的聚氧化烯衍生物的末端的活化率。 使用具有离子官能团的标记试剂对活性基团进行标记。 然后使用离子交换柱和输出色谱图的RI检测器通过液相色谱分析聚氧化烯衍生物。 基于色谱图中与活性基团对应的峰面积的百分比获得末端的活化比例。

公开(公告)号：US06620976B2

公开(公告)日：2003-09-16

申请号：US10106219

申请日：2002-03-27

申请人： Kenji Sakanoue ,  Kouzoh Sanchika ,  Tohru Yasukohchi

发明人： Kenji Sakanoue ,  Kouzoh Sanchika ,  Tohru Yasukohchi

IPC分类号： C07C4311

CPC分类号： C08G65/2609 ,  C08L2203/02

摘要： Polyethylene glycol for use in fields with application to a living body wherein the sum of the contents of ethylene glycol and diethylene glycol in the polyethylene glycol is less than or equal to that expressed in the following formula [I]: Sum ⁢   ⁢ of ⁢   ⁢ ethylene ⁢   ⁢ glycol ⁢   ⁢ and ⁢   ⁢ diethylene ⁢   ⁢ glycol ⁢   ⁢ contents ⁢   ⁢ ( ppm ) = 150 × 2900 × 0.85 ( x - 150 ) / 44 x [ I ] wherein x represents the average molecular weight of the polyethylene glycol, and the polyethylene glycol has an average molecular weight ranging from 190 to 1,050.

摘要翻译： 聚乙二醇用于应用于生物体的领域，其中聚乙二醇中乙二醇和二甘醇的含量之和小于或等于下式[I]表示：其中x表示平均分子量 聚乙二醇的重量，聚乙二醇的平均分子量为190〜1050。

公开(公告)号：US5872191A

公开(公告)日：1999-02-16

申请号：US867985

申请日：1997-06-03

申请人： Kouzoh Sanchika ,  Tohru Yasukohchi ,  Kei-ichi Maruyama ,  Syunsuke Ohhashi

发明人： Kouzoh Sanchika ,  Tohru Yasukohchi ,  Kei-ichi Maruyama ,  Syunsuke Ohhashi

IPC分类号： C07D207/46 ,  C08G65/32 ,  C08G65/329 ,  C08G65/332 ,  C08G65/333 ,  C08L71/02

CPC分类号： C08G65/329 ,  C08G65/33337

摘要： A process for producing a polyoxyalkylene derivative substituted with succinimidyl group which comprises reacting a polyoxyalkylene compound having carboxyl group at ends with N-hydroxysuccinimide in an inert solvent in the presence of dicyclohexylcarbodiimide; dissolving an obtained reaction product into chloroform, an amount by weight of chloroform being 0.5 to 10 times as much as an amount by weight of the polyoxyalkylene compound having carboxyl group at ends; and crystallizing the polyoxyalkylene derivative substituted with succinimidyl group by adding an aliphatic hydrocarbon having 5 to 8 carbon atoms to a resultant solution, an amount by weight of the aliphatic hydrocarbon being 2 to 10 times as much as an amount by weight of chloroform. Materials can be handled with safety, and a highly pure polyoxyalkylene derivative substituted with succinimidyl group which does not cause turbidity in an aqueous solution and has an excellent quality as a material for drugs can be produced.

摘要翻译： 一种制备被琥珀酰亚胺基取代的聚氧化烯衍生物的方法，包括在二环己基碳二亚胺的存在下，在惰性溶剂中使具有羧基的聚氧化烯化合物与N-羟基琥珀酰亚胺反应; 将得到的反应产物溶解在氯仿中，氯仿的重量为末端具有羧基的聚氧化烯化合物的重量的0.5〜10倍; 并通过向所得溶液中加入碳原子数为5〜8的脂肪族烃而使被琥珀酰亚胺基取代的聚氧化烯衍生物结晶化，所述脂肪族烃的重量比为氯仿的2〜10倍。 可以安全地处理材料，并且可以制备用琥珀酰亚胺基取代的高纯度聚氧化烯衍生物，其不会在水溶液中引起浊度并且具有作为药物的材料的优良品质。

公开(公告)号：US5540935A

公开(公告)日：1996-07-30

申请号：US349362

申请日：1994-12-05

申请人： Tsuyoshi Miyazaki ,  Kazuo Maruyama ,  Motoharu Iwatsuru ,  Kouzoh Sanchika ,  Mitsuhiro Nishida ,  Tohru Yasukohchi ,  Shigeru Kitano ,  Akinori Suginaka ,  Yoshihito Kadoma

发明人： Tsuyoshi Miyazaki ,  Kazuo Maruyama ,  Motoharu Iwatsuru ,  Kouzoh Sanchika ,  Mitsuhiro Nishida ,  Tohru Yasukohchi ,  Shigeru Kitano ,  Akinori Suginaka ,  Yoshihito Kadoma

IPC分类号： A61K9/127 ,  A61K47/48 ,  C07F9/6506 ,  C08G65/332 ,  C08G65/335

CPC分类号： A61K9/1271 ,  A61K47/48823 ,  C07F9/65061 ,  C08G65/3328 ,  C08G65/335 ,  Y10T428/2984

摘要： A reactive vesicle comprising, as a vesicle-forming component, a reactive phospholipid derivative represented by the following general formula (1) and a functional substance-fixed vesicle prepared by reacting the reactive vesicle with a functional substance: ##STR1## in which R.sup.1 C(.dbd.O) and R.sup.2 C(.dbd.O) each represent an aliphatic acyl group, R.sup.3 denotes hydrogen atom or methyl group, OA represents an oxyalkylene group of 2-4 carbon atoms, n indicates the average number of moles of added oxyalkylene group and is 1-1,000, p is 0 or 1, X represents ##STR2## with q and r each being an integer of 0 to 4 or 1 to 4, respectively, and M denotes hydrogen atom or an alkli metal atom.

摘要翻译： 1.一种活性囊泡，其特征在于，作为泡囊形成成分，含有由以下通式（1）表示的反应性磷脂衍生物和通过使所述活性囊泡与功能性物质反应制备的功能性物质固定的囊泡： 其中R1C（= O）和R2C（= O）各自表示脂族酰基，R3表示氢原子或甲基，OA表示2-4个碳原子的氧化烯基，n表示加入的氧化烯基团的平均摩尔数 并且为1-1,000，p为0或1，X表示，其中q和r各自为0至4或1至4的整数，M表示氢原子或烷基金属原子。