Tocopherol derivatives and method for preparation thereof
    1.
    发明授权
    Tocopherol derivatives and method for preparation thereof 有权
    生育酚衍生物及其制备方法

    公开(公告)号:US06410752B1

    公开(公告)日:2002-06-25

    申请号:US09756179

    申请日:2001-01-09

    IPC分类号: C07F906

    摘要: An object of the present invention is to provide the tocopherol derivatives represented by the following formula (I), and their salts: Wherein, R1, R2 and R3 are H or methyl group, and at least one positions selected from group consisting of the R1, R2 and R3 positions are methyl group; and, A is CH2—CH(CH3)— or CH═C(CH3)— The other object of the present invention is to provide a method for preparing the above tocopherol derivatives. The tocopherol derivatives is prepared by reacting tocopherol with phosphorous oxychloride in an equivalent ratio of 1:1˜1.3, in presence of an organic base, in an organic solvent; reacting the tocopherol dichlorophosphate produced by the above reaction with 3-aminopropanol in presence of an organic base, in an organic solvent; and, hydrolyzing the above products. The tocopherol derivatives according to the present invention can be hydrolyzed by biological enzymes in a living body to produce tocopherol and 3-aminopropane phosphate. And they can induce physiological activities including recovery of injured skin, prevention from aging of bio-membrane, etc. Also, the tocopherol derivatives according to the present invention have improved stability, safety to skin and anti-oxidant effect superior to preceding tocopherol and its derivatives.

    摘要翻译: 本发明的目的是提供由下式(I)表示的生育酚衍生物及其盐:其中,R1,R2和R3为H或甲基,以及至少一个选自R1 R2和R3位是甲基; 并且A是CH 2 -CH(CH 3) - 或CH = C(CH 3) - 本发明的另一个目的是提供一种制备上述生育酚衍生物的方法。 生育酚衍生物通过在有机碱存在下,在有机溶剂中使生育酚与磷酰氯以1:1〜1.3的当量比反应制备; 在有机溶剂中,通过上述反应生成的生育酚二氯磷酸与有机碱存在下的3-氨基丙醇反应; 并且水解上述产物。根据本发明的生育酚衍生物可以通过活体中的生物酶水解以产生生育酚和3-氨基丙烷磷酸酯。 它们可以诱导生理活性,包括恢复受伤的皮肤,防止生物膜老化等。此外,根据本发明的生育酚衍生物具有改善的稳定性,对皮肤的安全性和优于前述生育酚的抗氧化作用及其 衍生品

    Sesamol derivatives or their salts, the process for preparing the same, and the skin external composition containing the same
    3.
    发明授权
    Sesamol derivatives or their salts, the process for preparing the same, and the skin external composition containing the same 有权
    芝麻酚衍生物或其盐,其制备方法以及含有它们的皮肤外用组合物

    公开(公告)号:US07943599B2

    公开(公告)日:2011-05-17

    申请号:US11921180

    申请日:2006-05-29

    IPC分类号: A61K31/66 C07F9/12

    摘要: The present invention relates to a sesamol derivative or its salt, and a skin external composition containing the same. More particularly, the invention relates to a sesamol derivative or its salt, which consists of sesamol and 3-aminopropane phosphoric acid, linked with each other by a phosphoric acid diester bond, and can be degraded into sesamol and 3-aminopropane phosphoric acid by enzymes present on the skin so as to simultaneously show the physiological activities of sesamol and 3-aminopropane phosphoric acid, as well as a preparation method thereof and a skin external composition containing the same.

    摘要翻译: 本发明涉及一种芝麻酚衍生物或其盐,以及包含其的皮肤外用组合物。 更具体地,本发明涉及由芝麻酚和3-氨基丙烷磷酸组成的芝麻酚衍生物或其盐,其通过磷酸二酯键彼此连接,并且可以通过酶降解成芝麻酚和3-氨基丙烷磷酸 存在于皮肤上,以同时显示西沙莫酚和3-氨基丙烷磷酸的生理活性,以及​​其制备方法和含有它们的皮肤外用组合物。

    Sesamol Derivatives or Their Salts, The Process for Preparing the Same, and the Skin External Composition Containing the Same
    5.
    发明申请
    Sesamol Derivatives or Their Salts, The Process for Preparing the Same, and the Skin External Composition Containing the Same 有权
    芝麻素衍生物或其盐,其制备方法和含有其的皮肤外用组合物

    公开(公告)号:US20090131686A1

    公开(公告)日:2009-05-21

    申请号:US11921180

    申请日:2006-05-29

    IPC分类号: C07F9/655 A61Q19/08

    摘要: The present invention relates to a sesamol derivative or its salt, and a skin external composition containing the same. More particularly, the invention relates to a sesamol derivative or its salt, which consists of sesamol and 3-aminopropane phosphoric acid, linked with each other by a phosphoric acid diester bond, and can be degraded into sesamol and 3-aminopropane phosphoric acid by enzymes present on the skin so as to simultaneously show the physiological activities of sesamol and 3-aminopropane phosphoric acid, as well as a preparation method thereof and a skin external composition containing the same.

    摘要翻译: 本发明涉及一种芝麻酚衍生物或其盐,以及包含其的皮肤外用组合物。 更具体地,本发明涉及由芝麻酚和3-氨基丙烷磷酸组成的芝麻酚衍生物或其盐,其通过磷酸二酯键彼此连接,并且可以通过酶降解成芝麻酚和3-氨基丙烷磷酸 存在于皮肤上,以同时显示西沙莫酚和3-氨基丙烷磷酸的生理活性,以及​​其制备方法和含有它们的皮肤外用组合物。