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    Separation Of Ginkgolides And Bilobalide From G. Biloba
    2.
    发明申请
    Separation Of Ginkgolides And Bilobalide From G. Biloba 失效
    银杏内酯和碧萝芷的分离

    公开(公告)号：US20080108837A1

    公开(公告)日：2008-05-08

    申请号：US10579162

    申请日：2004-11-09

    申请人： Koji Nakanishi ,  Stanislav Jaracz ,  Shahid Malik ,  Hideki Ishii ,  Sergei V. Dzyuba

    发明人： Koji Nakanishi ,  Stanislav Jaracz ,  Shahid Malik ,  Hideki Ishii ,  Sergei V. Dzyuba

    IPC分类号： C07D407/14

    CPC分类号： C07D493/22

    摘要： The subject invention provides a method for separating a terpene trilactone from Ginkgo biloba plant material or from an extract of Ginkgo biloba comprising a mixture of terpene trilactones, the process comprising the steps of:a) subjecting the Ginkgo biloba plant material or the extract to column chromatography with an appropriate solvent system to produce at least a first fraction containing the terpene trilactone bilobalide, a second fraction eluted after the first fraction containing the terpene trilactones GA and GB, and a third fraction eluted after the second fraction containing at least a preponderance of the terpene trilactones GC and GJ; andb) alkylating the terpene trilactone GB of the second fraction so as to produce a first mixture including terpene trilactone GA and alkylated terpene trilactone GB; or alkylating the terpene trilactone GC of the third fraction so as produce a second mixture including terpene trilactone GJ and alkylated terpene trilactone GC, so as to thereby isolate a terpene trilactone.

    摘要翻译： 本发明提供了从银杏植物材料或银杏提取物中分离萜烯三内酯的方法，其中包括萜内三聚物的混合物，该方法包括以下步骤：a）将银杏植物材料或提取物经柱 用适当的溶剂体系进行色谱以产生至少一种含有萜烯三内酰亚叶内酰脲的第一级分，在含有萜烯三内酰胺GA和GB的第一级分之后洗脱的第二级分，以及第二级分洗脱的第三级分，其中至少含有 萜类三内酯GC和GJ; 和b）将第二级分的萜烯三内酯GB烷基化，以产生包含萜内酯GA和烷基化萜三内酯GB的第一混合物; 或烷基化第三级分的萜烯三内酰胺GC，从而产生包括萜内酯GJ和烷基化萜三内酰胺GC的第二混合物，从而分离萜烯三内酯。

    Synthesis of derivatives of ginkgolide C
    3.
    发明申请
    Synthesis of derivatives of ginkgolide C 失效
    银杏内酯衍生物的合成

    公开(公告)号：US20050119336A1

    公开(公告)日：2005-06-02

    申请号：US10925209

    申请日：2004-08-24

    申请人： Koji Nakanishi ,  Stanislav Jaracz ,  Kristian Stromgaard

    发明人： Koji Nakanishi ,  Stanislav Jaracz ,  Kristian Stromgaard

    IPC分类号： A61K31/365 ,  C07D20060101 ,  C07D307/93 ,  C07D307/94 ,  C07D311/94 ,  C07D311/96 ,  C07D493/14

    CPC分类号： C07D493/22

    摘要： The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; where R4 is an alkyl group; and R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R1 is H or —COR7, where R7 is alkyl, aryl or amino; wherein R2 is present or absent, and when present is H, —COR8 or —CO-Z-R8; where R8 is alkyl, aryl or amino; and Z is oxygen; wherein R3 is present or absent, and when present is —COR9; where R9 is alkyl or aryl; wherein only one of R2 or R3 is present in the compound; wherein only two of R, R1, R2 and R3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R3 is absent and bond b is present when R2 is absent; or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.

    摘要翻译： 本发明提供具有以下结构的银杏内酯C衍生物化合物：其中R是H或-A-Ar，其中A是烷基; 并且Ar是可以含有杂原子的芳基，并且可以是未取代的或被一至五个选自氢，烷氧基，-CH 2 CO 2， R 4，R 4，R 4，R 6， 其中R 4是烷基; 和R 5和R 6各自独立地为氢或支链或非支链烷基; 其中R 1是H或-COR 7，其中R 7是烷基，芳基或氨基; 其中R 2存在或不存在，并且当存在时为H，-COR 8或-CO-Z-R 8; 其中R 8是烷基，芳基或氨基; Z为氧; 其中R 3存在或不存在，并且当存在时为-COR 9; 其中R 9是烷基或芳基; 其中R 2和R 3中只有一个存在于化合物中; 其中R 1，R 2，R 2和R 3中只有两个是H; 并且其中a和b中的每一个表示存在或不存在的单个共价键，其中当R 3不存在时存在键a，并且当R 2' 缺席; 或该化合物的光学纯对映异构体。 此外，本发明提供了使用这些化合物抑制甘氨酸受体的活性的方法。

    Separation of ginkgolides and bilobalide from G. biloba
    4.
    发明授权
    Separation of ginkgolides and bilobalide from G. biloba 失效
    银杏和银杏内酯的分离

    公开(公告)号：US07763741B2

    公开(公告)日：2010-07-27

    申请号：US10579162

    申请日：2004-11-09

    申请人： Koji Nakanishi ,  Stanislav Jaracz ,  Shahid Malik ,  Hideki Ishii ,  Sergei V. Dzyuba

    发明人： Koji Nakanishi ,  Stanislav Jaracz ,  Shahid Malik ,  Hideki Ishii ,  Sergei V. Dzyuba

    IPC分类号： C07D407/00

    CPC分类号： C07D493/22

    摘要： The subject invention provides a method for separating a terpene trilactone from Ginkgo biloba plant material or from an extract of Ginkgo biloba comprising a mixture of terpene trilactones, the process comprising the steps of: a) subjecting the Ginkgo biloba plant material or the extract to column chromatography with an appropriate solvent system to produce at least a first fraction containing the terpene trilactone bilobalide, a second fraction eluted after the first fraction containing the terpene trilactones GA and GB, and a third fraction eluted after the second fraction containing at least a preponderance of the terpene trilactones GC and GJ; and b) alkylating the terpene trilactone GB of the second fraction so as to produce a first mixture including terpene trilactone GA and alkylated terpene trilactone GB; or alkylating the terpene trilactone GC of the third fraction so as produce a second mixture including terpene trilactone GJ and alkylated terpene trilactone GC, so as to thereby isolate a terpene trilactone.

    摘要翻译： 本发明提供了从银杏植物材料或银杏提取物中分离萜烯三内酯的方法，其中包括萜内三聚物的混合物，该方法包括以下步骤：a）将银杏植物材料或提取物经柱 用适当的溶剂体系进行色谱以产生至少一种含有萜烯三内酰亚叶内酰脲的第一级分，在含有萜烯三内酰胺GA和GB的第一级分洗脱的第二级分，以及第二级分洗脱的第三级分，其中至少含有 萜类三内酯GC和GJ; 和b）将第二级分的萜烯三内酯GB烷基化，以产生包含萜内酯GA和烷基化萜三内酯GB的第一混合物; 或烷基化第三级分的萜烯三内酰胺GC，从而产生包括萜内酯GJ和烷基化萜三内酰胺GC的第二混合物，从而分离萜烯三内酯。

    Synthesis of derivatives of ginkgolide C
    5.
    发明授权
    Synthesis of derivatives of ginkgolide C 失效
    银杏内酯衍生物的合成

    公开(公告)号：US07429670B2

    公开(公告)日：2008-09-30

    申请号：US10925209

    申请日：2004-08-24

    申请人： Koji Nakanishi ,  Stanislav Jaracz ,  Kristian Stromgaard

    发明人： Koji Nakanishi ,  Stanislav Jaracz ,  Kristian Stromgaard

    IPC分类号： C07D305/14 ,  A01K43/12

    CPC分类号： C07D493/22

    摘要： The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; where R4 is an alkyl group; and R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R1 is H or —COR7, where R7 is alkyl, aryl or amino; wherein R2 is present or absent, and when present is H, —COR8 or —CO—Z—R8; where R8 is alkyl, aryl or amino; and Z is oxygen; wherein R3 is present or absent, and when present is —COR9; where R9 is alkyl or aryl; wherein only one of R2 or R3 is present in the compound; wherein only two of R, R1, R2 and R3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R3 is absent and bond b is present when R2 is absent; or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.

    摘要翻译： 本发明提供具有以下结构的银杏内酯C衍生物化合物：其中R是H或-A-Ar，其中A是烷基; 并且Ar是可以含有杂原子的芳基，并且可以是未取代的或被一至五个选自氢，烷氧基，-CH 2 CO 2， R 4，R 4，R 4，R 6， 其中R 4是烷基; 和R 5和R 6各自独立地为氢或支链或非支链烷基; 其中R 1是H或-COR 7，其中R 7是烷基，芳基或氨基; 其中R 2存在或不存在，并且当存在时为H，-COR 8或-CO-Z-R 8; 其中R 8是烷基，芳基或氨基; Z为氧; 其中R 3存在或不存在，并且当存在时为-COR 9; 其中R 9是烷基或芳基; 其中R 2和R 3中只有一个存在于化合物中; 其中R 1，R 2，R 2和R 3中只有两个是H; 并且其中a和b中的每一个表示存在或不存在的单个共价键，其中当R 3不存在时存在键a，并且当R 2' 缺席; 或该化合物的光学纯对映异构体。 此外，本发明提供了使用这些化合物抑制甘氨酸受体的活性的方法。