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    Process for producing water-soluble hyaluronic acid modification
    1.
    发明申请
    Process for producing water-soluble hyaluronic acid modification 有权
    生产水溶性透明质酸改性方法

    公开(公告)号：US20090148534A1

    公开(公告)日：2009-06-11

    申请号：US11662087

    申请日：2005-09-07

    申请人： Kenji Yasugi ,  Teruo Nakamura ,  Tsuyoshi Shimoboji ,  Mika Sato

    发明人： Kenji Yasugi ,  Teruo Nakamura ,  Tsuyoshi Shimoboji ,  Mika Sato

    IPC分类号： A61K9/14 ,  C07H1/00 ,  C07H3/00

    CPC分类号： C08B37/0072 ,  A61K47/61 ,  C08J3/075 ,  C08J3/122 ,  C08L5/08

    摘要： The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction rate of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction rate as that of the conventionally known gel.

    摘要翻译： 本发明提供实际上用作药物载体的水溶性改性HA及其制备方法。 本发明提供：通过将透明质酸的葡糖醛酸或其衍生物的羧基引入取代基而产生的水溶性改性透明质酸，其在血液中的停留时间延长到实用水平， 通过酰胺键，在非极性极性溶剂中使用BOP缩合剂，在5摩尔％以上的引入速率的下限; 及其制造方法。 此外，通过交联改性透明质酸，本发明提供即使以与常规已知凝胶相同的交联官能团引入速率也能够极长的药物持续释放的透明质酸凝胶。

    Process for producing water-soluble hyaluronic acid modification
    3.
    发明授权
    Process for producing water-soluble hyaluronic acid modification 有权
    生产水溶性透明质酸改性方法

    公开(公告)号：US08143391B2

    公开(公告)日：2012-03-27

    申请号：US11662087

    申请日：2005-09-07

    申请人： Kenji Yasugi ,  Teruo Nakamura ,  Tsuyoshi Shimoboji ,  Mika Sato

    发明人： Kenji Yasugi ,  Teruo Nakamura ,  Tsuyoshi Shimoboji ,  Mika Sato

    IPC分类号： C07H1/00 ,  C08B37/08

    CPC分类号： C08B37/0072 ,  A61K47/61 ,  C08J3/075 ,  C08J3/122 ,  C08L5/08

    摘要： The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction ratio of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction ratio as that of the conventionally known gel.

    摘要翻译： 本发明提供实际上用作药物载体的水溶性改性HA及其制备方法。 本发明提供：通过将透明质酸的葡糖醛酸或其衍生物的羧基引入取代基而产生的水溶性改性透明质酸，其在血液中的停留时间延长到实用水平， 通过酰胺键，在引发比为5摩尔％以上的下限，使用BOP缩合剂在非质子传递极性溶剂中; 及其制造方法。 此外，通过交联改性透明质酸，本发明提供即使以与常规已知凝胶相同的交联官能团引入比例，能够极长的药物持续释放的透明质酸凝胶。

    CONJUGATE OF WATER-SOLUBLE HYALURONIC ACID MODIFICATION PRODUCT WITH GLP-A ANALOGUE
    4.
    发明申请
    CONJUGATE OF WATER-SOLUBLE HYALURONIC ACID MODIFICATION PRODUCT WITH GLP-A ANALOGUE 审中-公开
    具有GLP-A类似物的水溶性羟尿酸改性产品的结合

    公开(公告)号：US20090082266A1

    公开(公告)日：2009-03-26

    申请号：US11908278

    申请日：2006-03-08

    申请人： Teruo Nakamura ,  Tatsuya Kato ,  Hideyuki Togawa ,  Kenji Yasugi ,  Hiroko Konishi ,  Yasuo Sekimori ,  Tsuyoshi Shimoboji

    发明人： Teruo Nakamura ,  Tatsuya Kato ,  Hideyuki Togawa ,  Kenji Yasugi ,  Hiroko Konishi ,  Yasuo Sekimori ,  Tsuyoshi Shimoboji

    IPC分类号： A61K38/17 ,  A61P3/00

    CPC分类号： C07K14/605 ,  A61K47/61 ,  C08B37/0072

    摘要： To provide a GLP-1 analogue long-acting prophylactic or therapeutic agent for diabetes, diabetic complications and/or obesity due to diabetes which provides an extended half-life of a GLP-1 analogue in the blood to prevent frequent administration, and is biodegradable and safe.The present invention provides a conjugate obtained by binding, to a GLP-1 analogue into which a mercapto group is incorporated, water soluble hyaluronic acid modification product obtained by incorporating a substituent via an amide bond to the carboxyl group of glucuronic acid portion of hyaluronic acid as a derivative thereof, using a specific condensing agent in an aprotic polar solvent; and a prophylactic or therapeutic agent having a durable blood glucose lowering effect for diabetes, diabetic complications or obesity.

    摘要翻译： 提供GLP-1类似物长效预防或治疗糖尿病，由于糖尿病导致的糖尿病并发症和/或肥胖症，其提供血液中GLP-1类似物的延长半衰期以防止频繁施用，并且是可生物降解的 安全。 本发明提供了通过与其中引入巯基的GLP-1类似物结合获得的缀合物，其通过将酰胺键引入到透明质酸的葡萄糖醛酸部分的羧基而获得的水溶性透明质酸改性产物 作为其衍生物，在非质子极性溶剂中使用特定的缩合剂; 以及对糖尿病，糖尿病并发症或肥胖具有持久的血糖降低作用的预防或治疗剂。