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    PROCESS FOR MANUFACTURING A GLUTAMIC ACID DERIVATIVE AND A PYROGLUTAMIC ACID DERIVATIVE AND A NOVEL INTERMEDIATE IN THE MANUFACTURE THEREOF
    3.
    发明申请
    PROCESS FOR MANUFACTURING A GLUTAMIC ACID DERIVATIVE AND A PYROGLUTAMIC ACID DERIVATIVE AND A NOVEL INTERMEDIATE IN THE MANUFACTURE THEREOF 失效
    制造谷氨酸衍生物和吡咯烷酸衍生物的方法及其制备中的新型中间体

    公开(公告)号：US20100010234A1

    公开(公告)日：2010-01-14

    申请号：US12500135

    申请日：2009-07-09

    申请人： Yusuke AMINO

    发明人： Yusuke AMINO

    IPC分类号： C07D403/06 ,  C07D207/26 ,  C07F7/02

    CPC分类号： C07D207/28 ,  C07C229/36 ,  Y02P20/55

    摘要： Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.

    摘要翻译： 谷氨酸衍生物，特别是莫纳甜，可以通过用烷基化剂烷基化4-保护的羟基焦谷氨酸衍生物以制备4-保护的羟基-4-烷基谷氨酸衍生物，然后进行水解和脱保护的步骤，可以方便地制备。 4-保护的羟基焦谷氨酸衍生物很容易由羟脯氨酸生成。 4-保护的羟基焦谷氨酸衍生物特别适用于有效制备高光学纯度的莫纳甜，因为它可以在4-位选择性地立体选择性烷基化，烷基化后可容易地转化为谷氨酸 酸衍生物。

    METHOD OF PROVIDING PREPARATION FOR TOPICAL APPLICATION AND SUPPLEMENT MEETING CLIENT'S NEEDS
    7.
    发明申请
    METHOD OF PROVIDING PREPARATION FOR TOPICAL APPLICATION AND SUPPLEMENT MEETING CLIENT'S NEEDS 审中-公开
    提供局部应用准备和补充会议客户需求的方法

    公开(公告)号：US20080182894A1

    公开(公告)日：2008-07-31

    申请号：US12020791

    申请日：2008-01-28

    申请人： Yoshinobu TAKINO ,  Koichiro SAGAWA ,  Yusuke AMINO

    发明人： Yoshinobu TAKINO ,  Koichiro SAGAWA ,  Yusuke AMINO

    IPC分类号： A61K31/335 ,  A61K31/198 ,  G06F19/00 ,  A61K31/165

    CPC分类号： A61K8/678 ,  A23L33/30 ,  A61K8/0212 ,  A61K8/97 ,  A61Q7/00 ,  A61Q19/00 ,  A61Q19/08

    摘要： The present invention provides a method of efficiently providing, to a client, a preparation for topical application and a supplement suitable for the client. This method entails inputting the part desired by the client to be improved and an improvement effect desired for the part into a system, which will determine the composition of nutritional components of a preparation for topical application and a supplement that are suitable for the improvement effect desired for the part to be improved by referring to a database, in which compositions of nutritional components of supplements are registered in advance.

    摘要翻译： 本发明提供了一种向客户有效地提供用于局部应用的准备物和适合于客户的补充剂的方法。 该方法需要输入要改进的客户期望的部分和将部分所需的改进效果进入系统，这将确定用于局部应用的制剂的营养成分的组成以及适合于所需改善效果的补充剂 通过参照其中预先登记补充剂的营养成分的组成的数据库来改进该部分。

    SUBSTITUTED BENZYL ESTER DERIVATIVE AND USE THEREOF
    9.
    发明申请
    SUBSTITUTED BENZYL ESTER DERIVATIVE AND USE THEREOF 有权
    取代苄基酯衍生物及其用途

    公开(公告)号：US20090203774A1

    公开(公告)日：2009-08-13

    申请号：US12345249

    申请日：2008-12-29

    申请人： Yusuke AMINO ,  Yoshinobu Takino

    发明人： Yusuke AMINO ,  Yoshinobu Takino

    IPC分类号： A23L1/30 ,  A61K31/357 ,  A61K31/225 ,  C07D317/44 ,  C07C53/00 ,  C07C57/00

    CPC分类号： C07D317/54 ,  A23L33/10 ,  A61K8/37 ,  A61K8/4973 ,  A61Q19/00 ,  C07C69/24 ,  C07C69/28 ,  C07C69/533 ,  C12P7/62

    摘要： The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I′) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group. According to the present invention, a stable capsinoid derivative is provided, and a pharmaceutical composition, a food composition, a cosmetic composition and the like containing the derivative as an active ingredient can be provided.

    摘要翻译： 本发明涉及含有一种或多种下式（I'）表示的化合物的药物组合物，食品组合物或化妆品组合物，其中R1是氢原子，羟基，甲氧基或 乙氧基，R2是羟基，甲氧基或乙酰氧基，或者R1和R2组合任选地形成亚甲二氧基，R由下式表示，其中Y是亚乙基或亚乙烯基，m和n 各自为0〜7的整数，其满足m + n = 2〜8，R3和R4各自独立地为氢原子，甲基或乙基，条件是：（1）当R1为甲氧基 ，则R2不是羟基; 和（2）当R1是羟基时，R2不是羟基和乙酰氧基。 根据本发明，提供稳定的类毒素衍生物，并且可以提供含有该衍生物作为有效成分的药物组合物，食品组合物，化妆品组合物等。

    ESTER DERIVATIVE AND USE THEREOF
    10.
    发明申请
    ESTER DERIVATIVE AND USE THEREOF 有权
    雌激素衍生物及其用途

    公开(公告)号：US20090170942A1

    公开(公告)日：2009-07-02

    申请号：US12237142

    申请日：2008-09-24

    申请人： Yusuke AMINO ,  Yoshinobu Takino

    发明人： Yusuke AMINO ,  Yoshinobu Takino

    IPC分类号： A61K31/23 ,  C07C53/00 ,  A61P7/00

    CPC分类号： C07C69/28 ,  A23L33/10 ,  A61K8/37 ,  A61Q19/00 ,  C07C69/533 ,  C07C69/734

    摘要： A compound represented by the following formula (I′) wherein X1 is a methylene group, an ethylene group, a trimethylene group or a vinylene group, X2 is a divalent group represented by the following formula A or B, Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=0 to 8, R1 and R2 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that when X1 is a methylene group, then X2 is not a divalent group represented by the formula A, and when X1 is a vinylene group, then X2 is not a divalent group represented by the formula A. The compound is a stable capsinoid derivative, and is useful as an active ingredient of an external blood circulation enhancer or a cosmetic composition, a pharmaceutical composition, or a food composition.

    摘要翻译： 由下式（I'）表示的化合物，其中X1是亚甲基，亚乙基，三亚甲基或亚乙烯基，X2是由下式A或B表示的二价基团，Y是亚乙基或 亚乙烯基，m和n各自为0〜7的整数，其满足m + n = 0〜8，R1和R2各自独立地为氢原子，甲基或乙基，条件是当X1为 亚甲基，则X2不是由式A表示的二价基团，当X1是亚乙烯基时，X2不是由式A表示的二价基团。化合物是稳定的类毒素衍生物，可用作 外部血液循环增强剂或化妆品组合物的活性成分，药物组合物或食品组合物。