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    Multibranched polyoxyalkylene compound and producing method thereof
    1.
    发明授权
    Multibranched polyoxyalkylene compound and producing method thereof 有权
    多分支聚氧化烯化合物及其制备方法

    公开(公告)号：US08716435B2

    公开(公告)日：2014-05-06

    申请号：US12750844

    申请日：2010-03-31

    申请人： Tsuyoshi Takehana ,  Ken-ichiro Nakamoto ,  Chika Itoh

    发明人： Tsuyoshi Takehana ,  Ken-ichiro Nakamoto ,  Chika Itoh

    IPC分类号： C08G65/34

    CPC分类号： C08G65/33337 ,  A61K47/34 ,  C08G65/2609 ,  C08G65/2648 ,  C08G65/3322 ,  C08G65/3326 ,  C08G65/33303 ,  C08G65/33372 ,  C08G65/33389 ,  C08G65/3346 ,  C08G2650/26 ,  C08G2650/60

    摘要： A multibranched polyoxyalkylene compound represented by the following formula (1): wherein R1 is the same or different and is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are the same or different and are an oxyalkylene group having 2 to 4 carbon atoms, n and m are the same or different and are an average number of moles of the oxyalkylene group added, n represents 0 to 1000, m is the same or different and represents 10 to 1000, X represents a functional group capable of reacting with an amino group, a mercapto group, an aldehyde group, a carboxyl group, a triple bond, or an azide group to form a chemical bond, and L1 and L2 are the same or different and are a single bond, an alkylene group, or an alkylene group in which at least one bond selected from an ester bond, a urethane bond, an amide bond, an ether bond, and an amino is interposed.

    摘要翻译： 由下式（1）表示的多支链聚氧化烯化合物：其中R1相同或不同，为碳原子数1〜24的烃基，OA1和OA2相同或不同，为碳数2〜4的氧化烯基 原子，n和m相同或不同，是加成的氧化烯基的平均摩尔数，n表示0〜1000，m相同或不同，表示10〜1000，X表示可与 氨基，巯基，醛基，羧基，三键或叠氮基，形成化学键，L1和L2相同或不同，为单键，亚烷基或 其中插入了选自酯键，氨基甲酸酯键，酰胺键，醚键和氨基中的至少一个的亚烷基。

    Purification method of high-molecular-weight polyoxyalkylene derivative
    2.
    发明授权
    Purification method of high-molecular-weight polyoxyalkylene derivative 有权
    高分子量聚氧化烯衍生物的纯化方法

    公开(公告)号：US08097692B2

    公开(公告)日：2012-01-17

    申请号：US12750842

    申请日：2010-03-31

    申请人： Shuichi Yoshimura ,  Ken-ichiro Nakamoto ,  Chika Itoh

    发明人： Shuichi Yoshimura ,  Ken-ichiro Nakamoto ,  Chika Itoh

    IPC分类号： C08G63/02

    CPC分类号： C08G65/30 ,  C08G65/329 ,  C08L2203/02

    摘要： A purification method in which, from a specific polyoxyalkylene derivative having a molecular weight of 8,800 to 100,000, an impurity differing in the number of hydroxyl groups is separated, the method including steps (A), (B), (C), and (D). Step (A): a step in which an aprotic organic solvent is used in an amount at least 5 times by weight the amount of the polyoxyalkylene derivative to dissolve the polyoxyalkylene derivative therein and give a solution; step (B): a step in which an adsorbent comprising an oxide containing at least one of aluminum and silicon is added to the solution in an amount 0.5 to 5 times by weight the amount of the polyoxyalkylene derivative to thereby yield a slurry; step (C): a step in which the slurry is stirred at 25° C. or higher; step (D): a step in which the polyoxyalkylene derivative is recovered from the slurry.

    摘要翻译： 一种纯化方法，其特征在于，分子量为8,800〜100,000的特定的聚氧亚烷基衍生物分离出羟基数不同的杂质，包括步骤（A），（B），（C）和（C） D）。 步骤（A）：使非质子性有机溶剂的使用量为聚氧亚烷基衍生物的量的至少5倍以溶解其中的聚氧化烯衍生物并得到溶液的步骤; 步骤（B）：将含有铝和硅中的至少一种的氧化物的吸附剂以0.5〜5倍量的量添加到溶液中，从而得到浆料的步骤; 步骤（C）：将浆料在25℃以上搅拌的步骤; 步骤（D）：从浆料中回收聚氧化烯衍生物的步骤。

    MULTIBRANCHED POLYOXYALKYLENE COMPOUND AND PRODUCING METHOD THEREOF
    3.
    发明申请
    MULTIBRANCHED POLYOXYALKYLENE COMPOUND AND PRODUCING METHOD THEREOF 有权
    多支化聚氧乙烯化合物及其制备方法

    公开(公告)号：US20100261863A1

    公开(公告)日：2010-10-14

    申请号：US12750844

    申请日：2010-03-31

    申请人： Tsuyoshi TAKEHANA ,  Ken-ichiro NAKAMOTO ,  Chika ITOH

    发明人： Tsuyoshi TAKEHANA ,  Ken-ichiro NAKAMOTO ,  Chika ITOH

    IPC分类号： C08G65/00 ,  C07D207/46 ,  C07C69/96 ,  C07C255/13 ,  C07C209/48 ,  C07C217/00 ,  C08G63/00 ,  C08F20/00 ,  C08F26/00

    CPC分类号： C08G65/33337 ,  A61K47/34 ,  C08G65/2609 ,  C08G65/2648 ,  C08G65/3322 ,  C08G65/3326 ,  C08G65/33303 ,  C08G65/33372 ,  C08G65/33389 ,  C08G65/3346 ,  C08G2650/26 ,  C08G2650/60

    摘要： A multibranched polyoxyalkylene compound represented by the following formula (1): CH2-L1-(OA1)n-L2-X CH(OA2)mOR1 CH(OA2)mOR1 CH(OA2)mOR1 CH2(OA2)mOR1   (1) wherein R1 is the same or different and is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are the same or different and are an oxyalkylene group having 2 to 4 carbon atoms, n and m are the same or different and are an average number of moles of the oxyalkylene group added, n represents 0 to 1000, m is the same or different and represents 10 to 1000, X represents a functional group capable of reacting with an amino group, a mercapto group, an aldehyde group, a carboxyl group, a triple bond, or an azide group to form a chemical bond, and L1 and L2 are the same or different and are a single bond, an alkylene group, or an alkylene group in which at least one bond selected from an ester bond, a urethane bond, an amide bond, an ether bond, and an amino is interposed.

    摘要翻译： 由下式（1）表示的多分支聚氧化烯化合物：CH2-L1-（OA1）n-L2-XCH（OA2）mOR1CH（OA2）mOR1CH（OA2）mOR1 CH2（OA2）mOR1（1） 相同或不同，为碳原子数为1〜24的烃基，OA1和OA2相同或不同，为碳原子数2〜4的氧化烯基，n和m相同或不同，为平均数 的氧化烯基的摩尔数，n表示0〜1000，m相同或不同，表示10〜1000，X表示能够与氨基，巯基，醛基，羧基反应的官能团 ，三键或叠氮基以形成化学键，并且L1和L2相同或不同，为单键，亚烷基或亚烷基，其中至少一个选自酯键， 氨基甲酸酯键，酰胺键，醚键和氨基。

    Phospholipid derivative
    5.
    发明申请
    Phospholipid derivative 有权
    磷脂衍生物

    公开(公告)号：US20060110436A1

    公开(公告)日：2006-05-25

    申请号：US10529692

    申请日：2003-09-30

    申请人： Syunsuke Ohhashi ,  Kazuhiro Kubo ,  Chika Itoh ,  Tohru Yasukohchi ,  Hiroshi Kikuchi ,  Norio Suzuki ,  Miho Kurosawa ,  Hitoshi Yamauchi

    发明人： Syunsuke Ohhashi ,  Kazuhiro Kubo ,  Chika Itoh ,  Tohru Yasukohchi ,  Hiroshi Kikuchi ,  Norio Suzuki ,  Miho Kurosawa ,  Hitoshi Yamauchi

    IPC分类号： A61K31/795 ,  C08F291/00 ,  A61K9/127

    CPC分类号： C08F8/40 ,  A61K8/14 ,  A61K8/8164 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1278 ,  A61K31/795 ,  A61Q19/00 ,  C08F220/28 ,  C08F222/06 ,  C08L53/00 ,  C08F222/04 ,  C08L2666/02

    摘要： A phospholipid derivative, utilizable for modification of liposomes and the like, which is a copolymer containing, as essential component units, a component unit A represented by the formula (1), a component unit B represented by the formula (2A) and/or the formula (2B), and a component unit C represented by the formula (3) [R1 and R2 represent hydrogen atom or methyl group, provided that R1 and R2 do not simultaneously represent methyl group; R3 represents a divalent hydrocarbon group having 1 to 3 carbon atoms; AO represents an oxyalkylene group having 2 to 4 carbon atoms; m represents an average molar number of the added oxyalkylene groups and is a number in the range represented as 4≦m≦100; R4 represents hydrogen atom, a hydrocarbon group or acyl group having 1 to 20 carbon atoms; R5CO and R6CO represent an acyl group having 8 to 24 carbon atoms; R7 represents a divalent hydrocarbon group having 2 to 4 carbon atoms; and X and Y represent hydrogen atom, an alkali metal atom, ammonium or an organic ammonium] wherein a molar ratio of the component unit A relative to a total of the component unit B and the component unit C is from 7/3 to 3/7, and the component unit C is contained at a ratio of from 1 to 4 moles per 1 mole of the copolymer.

    摘要翻译： 可用于脂质体改性的磷脂衍生物等，其是以式（1）表示的成分单元A，式（2A）表示的成分单元B和/或式 式（2B）和式（3）表示的成分单元C [R 1和R 2]表示氢原子或甲基，条件是R 0 > 1 和R 2不同时表示甲基; R 3表示具有1至3个碳原子的二价烃基; AO表示碳原子数2〜4的氧化烯基， m表示加成的氧化烯基的平均摩尔数，是在4≤M≤100的范围内的数字; R 4表示氢原子，碳原子数为1〜20的烃基或酰基， R 5 CO和R 6 CO表示具有8至24个碳原子的酰基; R 7表示具有2至4个碳原子的二价烃基; 并且X和Y表示氢原子，碱金属原子，铵或有机铵]，其中组分单元A相对于组分单元B和组分单元C的总量的摩尔比为7/3至3 / 7，组分单元C的含量相对于1摩尔共聚物为1〜4摩尔。

    Polyalkylene glycol derivative and modified bio-related substance
    6.
    发明申请
    Polyalkylene glycol derivative and modified bio-related substance 有权
    聚亚烷基二醇衍生物和改性生物相关物质

    公开(公告)号：US20060073113A1

    公开(公告)日：2006-04-06

    申请号：US11142678

    申请日：2005-06-02

    申请人： Ken-ichiro Nakamoto ,  Syunsuke Ohashi ,  Yuji Yamamoto ,  Kenji Sakanoue ,  Chika Itoh ,  Tohru Yasukohchi

    发明人： Ken-ichiro Nakamoto ,  Syunsuke Ohashi ,  Yuji Yamamoto ,  Kenji Sakanoue ,  Chika Itoh ,  Tohru Yasukohchi

    IPC分类号： A61K31/765 ,  C08G59/14

    CPC分类号： C08G65/333 ,  C08G65/2609 ,  C08G65/329

    摘要： A polyalkylene glycol derivative containing a compound of the formula (1): wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OA2 is an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, the groups represented by OA2 are the same or different from each other in one molecule, m is an average number of moles of the oxyalkylene group added, m represents 10 to 1000, and X represents a functional group capable of chemically reactive with a bio-related substance, polydispersity Mw/Mu of the above polyalkylene glycol derivative in gel permeation chromatography satisfying the following relationship: Mw/Mn≦1.07 wherein Mw represents a weight average molecular weight and Mn represents a number average molecular weight.

    摘要翻译： 含有式（1）化合物的聚亚烷基二醇衍生物：其中R是具有1至24个碳原子的烃基，OA 2是具有2至4个碳原子的氧化烯基，所表示的基团 在一个分子中，R彼此相同或不同，在一个分子中由OA 2表示的基团彼此相同或不同，m是氧化烯基的平均摩尔数 m表示10〜1000，X表示能够与生物相关物质发生化学反应的官能团，上述聚亚烷基二醇衍生物的多分散性Mw / Mu在凝胶渗透色谱中满足以下关系：＆lt; 公式描述=“在线公式”end =“lead”？> Mw / Mn <= 1.07 <？in-line-formula description =“In-line Formulas”end =“tail”？>其中Mw表示重量平均 分子量，Mn表示数均分子量。

    Polyoxyalkylene-modified lipid and method for producing the same
    9.
    发明授权
    Polyoxyalkylene-modified lipid and method for producing the same 有权
    聚氧化烯改性脂质及其制备方法

    公开(公告)号：US08785660B2

    公开(公告)日：2014-07-22

    申请号：US13431590

    申请日：2012-03-27

    申请人： Satoshi Matsuo ,  Yuji Yamamoto ,  Chika Itoh

    发明人： Satoshi Matsuo ,  Yuji Yamamoto ,  Chika Itoh

    IPC分类号： C07D207/456

    CPC分类号： C07D207/456 ,  C07C269/04 ,  C07C271/16 ,  C07D207/452

    摘要： Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, R1 and R2 are hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, R3 is a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.)

    摘要翻译： 提供了可用于化学修饰生物活性物质并且可用于药物递送系统如脂质体的硫醇反应性聚氧化烯修饰的脂质及其制备方法。 聚氧化烯修饰的脂质由下式（1）表示：（其中，R 1和R 2为彼此相同或不同且含有4〜24个碳原子的烃基，R 3为含有 1〜6个碳原子，OA为含有2〜4个碳原子的氧化烯基，n为氧化烯基的平均加成摩尔数，为5〜1000，Z为含有马来酰亚胺或碘乙酰胺的基团。