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    POLYOXYALKYLENE-MODIFIED LIPID AND METHOD FOR PRODUCING THE SAME
    1.
    发明申请
    POLYOXYALKYLENE-MODIFIED LIPID AND METHOD FOR PRODUCING THE SAME 有权
    多羟基烷基改性脂肪及其生产方法

    公开(公告)号：US20120253053A1

    公开(公告)日：2012-10-04

    申请号：US13431590

    申请日：2012-03-27

    申请人： Matsuo Satoshi ,  Yuji Yamamoto ,  Chika Itoh

    发明人： Matsuo Satoshi ,  Yuji Yamamoto ,  Chika Itoh

    IPC分类号： C07C233/05 ,  C07D207/404

    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。

    Polyalkylene glycol derivative and modified bio-related substance
    2.
    发明授权
    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：US08828373B2

    公开(公告)日：2014-09-09

    申请号：US11142683

    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 ,  C08F283/00 ,  C08G65/329 ,  C08G65/333 ,  C08G65/26 ,  A61K47/48

    CPC分类号： C08G65/2609 ,  A61K47/48215 ,  A61K47/60 ,  C08G65/329 ,  C08G65/333

    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, OA1 and OA2 are each 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 above oxyalkylene group added, m represents 10 to 1000, X represents a functional group capable of chemically reacting with a bio-related substance, and Y is a linker and represents an ether bond, an amide bond, a urethane bond, an ester bond, a secondary amino group, a carbonate bond, or an alkylene group containing these bonds, polydispersity Mw/Mn of the above polyalkylene glycol derivative in gel permeation chromatography satisfying the following relationship: Mw/Mn≦1.08 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为碳原子数为1〜24的烃基，OA1和OA2分别为碳原子数2〜4的氧化烯基，由R表示的基团相同 或在一个分子中彼此不同，在一个分子中由OA2表示的基团相同或不同，m为上述加成的氧化烯基的平均摩尔数，m表示10〜1000，X表示官能团 能够与生物相关物质进行化学反应的基团，Y为连接基，表示醚键，酰胺键，氨基甲酸酯键，酯键，仲氨基，碳酸酯键或含有这些基团的亚烷基 键，多分散性上述聚亚烷基二醇衍生物的Mw / Mn满足以下关系式：Mw / Mn＆nlE 1.08其中Mw表示重均分子量，Mn表示数均mol 精神重量

    Modified bio-related substance, process for producing the same, and intermediate
    4.
    发明授权
    Modified bio-related substance, process for producing the same, and intermediate 有权
    改性生物相关物质，其生产方法和中间体

    公开(公告)号：US08034981B2

    公开(公告)日：2011-10-11

    申请号：US12942554

    申请日：2010-11-09

    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： C07D249/18

    CPC分类号： C08G65/329 ,  A61K47/60 ,  C08G65/2609

    摘要： A modified bio-related substance, wherein at least one poly(alkylene glycol)oxy group represented by the following formula (1) is combined in a molecule: wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are each 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, and the groups represented by OA2 are the same or different from each other in one molecule, n and m are each average number of moles of the oxyalkylene group added, n represents 0 to 1000, and m represents 10 to 1000.

    摘要翻译： 一种改性的生物相关物质，其中至少一种由下式（1）表示的聚（亚烷基二醇）氧基在分子中组合：其中R是具有1至24个碳原子的烃基，OA1和OA2各自 具有2至4个碳原子的氧化烯基，由一个分子中由R表示的基团彼此相同或不同，并且由OA2表示的基团在一个分子中彼此相同或不同，n和m各自为 氧化烯基的平均加成摩尔数，n表示0〜1000，m表示10〜1000。

    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：US20060115450A1

    公开(公告)日：2006-06-01

    申请号：US11142683

    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 ,  C08F283/00

    CPC分类号： C08G65/2609 ,  A61K47/48215 ,  A61K47/60 ,  C08G65/329 ,  C08G65/333

    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, OA1 and OA2 are each 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 above oxyalkylene group added, m represents 10 to 1000, X represents a functional group capable of chemically reacting with a bio-related substance, and Y is a linker and represents an ether bond, an amide bond, a urethane bond, an ester bond, a secondary amino group, a carbonate bond, or an alkylene group containing these bonds, polydispersity Mw/Mn of the above polyalkylene glycol derivative in gel permeation chromatography satisfying the following relationship: Mw/Mn≦1.08 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为碳原子数为1〜24的烃基，OA 1和O 2各自为氧化烯 具有2至4个碳原子的基团，由R表示的基团在一个分子中彼此相同或不同，在一个分子中由OA 2表示的基团彼此相同或不同， m是上述氧化烯基的平均加成摩尔数，m表示10〜1000，X表示与生物相关物质发生化学反应的官能团，Y为连接基，表示醚键，酰胺键 氨基甲酸酯键，酯键，仲氨基，碳酸酯键或含有这些键的亚烷基，上述聚亚烷基二醇衍生物在凝胶渗透色谱中的多分散性Mw / Mn满足以下关系： -formulae description =“In-line Formulas”end =“lead”？> Mw / Mn <= 1.08 < in-line-formula description =“In-line Formulas”end =“tail”？>其中Mw表示重均分子量，Mn表示数均分子量。

    Polyalkylene glycol derivative and modified bio-related substance
    7.
    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
    10.
    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。