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    POLAR ORGANIC EXTRACT OF EURYCOMA LONGIFOLIA
    1.
    发明申请
    POLAR ORGANIC EXTRACT OF EURYCOMA LONGIFOLIA 审中-公开
    欧洲长期利益有机有机提取物

    公开(公告)号：US20130046082A1

    公开(公告)日：2013-02-21

    申请号：US13494945

    申请日：2012-06-12

    Applicant: Kit Lam CHAN ,  Bin Seng Low ,  David Sue San Ho

    Inventor： Kit Lam CHAN ,  Bin Seng Low ,  David Sue San Ho

    IPC: C07D493/08 ,  C07D311/10 ,  C07H17/075 ,  C07H15/26

    CPC classification number: A61K36/185

    Abstract: The present invention provides a composition including a polar organic extract of Eurycoma longifolia and a fraction derived from the polar organic extract, said composition comprising of quassinoids, coumarins, their glycosides, analogues and derivatives, which exhibits bioactivity of increasing spermatozoa production and spermatozoa quality in terms of morphology and motility, as well as increasing testosterone synthesis and release from cells of males. The extraction method of E. longifolia plant to produce the polar organic extract, and the subsequent purification to produce the fraction of polar organic extract containing the quassinoids, coumarins, their glycosides, analogues and derivatives, and uses for manufacturing a preparation for infertility treatment are also provided. The fraction of polar organic extract containing the quassinoids, coumarins, their glycosides, analogues and derivatives is formulated for medical applications via several routes of administration.

    Abstract translation: 本发明提供了一种组合物，其包含长尾a的极性有机提取物和衍生自极性有机提取物的级分，所述组合物包含类醌，香豆素，其糖苷，类似物和衍生物，其显示出增加精子产生和精子质量的生物活性 形态和运动条件，以及增加男性睾酮合成和释放。 E. longifolia植物的生产极性有机提取物的提取方法，随后的纯化生产含有类醌，香豆素，其糖苷，类似物和衍生物的极性有机提取物的部分，以及用于制造不孕症治疗的制剂的用途是 也提供。 含有类醌，香豆素，其糖苷，类似物和衍生物的极性有机提取物的部分通过几种给药途径配制用于医疗应用。

    Coumarin spherules/beads having unique morphology
    2.
    发明授权
    Coumarin spherules/beads having unique morphology 失效
    香豆素球/珠具有独特的形态

    公开(公告)号：US5693342A

    公开(公告)日：1997-12-02

    申请号：US405232

    申请日：1995-03-16

    Applicant: Eric Cervos ,  Pierre Labourt-Ibarre ,  Eraclis Statiotis

    Inventor： Eric Cervos ,  Pierre Labourt-Ibarre ,  Eraclis Statiotis

    IPC: C07D311/08 ,  C07D311/10 ,  C07D311/12 ,  C07D311/14 ,  A61K9/14

    CPC classification number: C07D311/08

    Abstract: Free-flowing, non-agglomerating and attrition resistant, substantially spherical solid beads/spherules of a coumarin compound, advantageously having a particle size ranging from 100 .mu.m to 2,000 .mu.m, a loose bulk density ranging from 0.25 to 0.8 and a compressive strength ranging from 500 to 10,000 N/m.sup.2, dissolve rapidly in ethanol and are conveniently prepared by prilling/fragmenting a melt of the coumarin compound into a stream of a cooling gas.

    Abstract translation: 香豆素化合物的自由流动，非附聚和耐磨损，基本上球形的固体珠/小球，有利地具有100μm至2,000μm的粒度，0.25至0.8的松散堆积密度和0.25至0.8的压缩强度 范围在500至10,000N / m 2之间，迅速溶解在乙醇中，通过将香豆素化合物的熔体造粒/碎裂成冷却气体流方便地制备。

    Process for producing coumarin derivatives
    4.
    发明授权
    Process for producing coumarin derivatives 失效
    生产香豆素衍生物的方法

    公开(公告)号：US5231194A

    公开(公告)日：1993-07-27

    申请号：US631316

    申请日：1990-12-21

    Applicant: Tamio Shirafuji ,  Kiyomi Sakai ,  Kensen Okusako

    Inventor： Tamio Shirafuji ,  Kiyomi Sakai ,  Kensen Okusako

    IPC: B01J23/64 ,  C07D311/10

    CPC classification number: B01J23/64 ,  C07D311/10

    Abstract: A process for producing a coumarin derivative represented by formula (II): ##STR1## wherein R.sub.1 to R.sub.4 are as defined in the specification, comprising the step of: subjecting to a ring formation and dehydrogenation reaction a 3-(2-cyclohexanoyl)-propionic acid ester derivative represented by formula (I): ##STR2## wherein R.sub.1 to R.sub.4 are as defined in the specification, the ring formation and dehydrogenation reaction being (1) conducted by use of a catalyst comprising a carrier having supported thereon palladium and either of chromium oxide and chromium hydroxide, or (2) conducted by use of a catalyst comprising a carrier having supported thereon palladium or a catalyst comprising a carrier having supported thereon palladium and either of chromium oxide and chromium hydroxide, in the presence of a promoter which is at least one member selected from the group consisting of magnesium trisilicate, zirconia, metallic chromium, and metallic tungsten.

    Preparation of alkylated or non-alkylated dihydrocoumarin together with the corresponding alkylated, or non-alkylated, coumarin
    5.
    发明授权
    Preparation of alkylated or non-alkylated dihydrocoumarin together with the corresponding alkylated, or non-alkylated, coumarin 失效
    与相应的烷基化或非烷基化的香豆素一起制备烷基化或非烷基化二氢香豆素

    公开(公告)号：US3891678A

    公开(公告)日：1975-06-24

    申请号：US39151673

    申请日：1973-08-24

    Applicant: STAMICARBON

    Inventor： VERHEIJEN EGIDIUS J M ,  THOMA JOZEF A ,  DEUMENS JOHANNES J M

    IPC: B01J23/00 ,  C07B61/00 ,  C07D311/00 ,  C07D311/06 ,  C07D311/08 ,  C07D311/10 ,  C07D311/20 ,  C07D7/26

    CPC classification number: C07D311/20 ,  C07D311/06 ,  C07D311/08

    Abstract: A process for dehydrogenating hexahydrocoumarin or alkylated derivatives thereof is disclosed, wherein the selection of specific process conditions allows substantial amounts of coumarin or alkylated derivatives thereof to be produced along with dihydrocoumarin or alkylated derivatives thereof. The hexahydrocoumarin or derivatives are contacted with the catalyst at about the dehydrogenation temperature and then are dehydrogenated in the presence of a Group VIII metal dehydrogenation catalyst in the liquid phase at a temperature of 200*-375*C while removing hydrogen from the reaction zone, and the reaction product contains coumarin or alkylated derivatives thereof in a molar ratio of coumarin compounds:dihydrocoumarin compounds of at least 1:5. Coumarin and dihydrocoumarin, as well as alkylated derivatives thereof, are known compounds which are used in the fragance industry.

    Abstract translation: 公开了一种使六氢香豆素或其烷基化衍生物脱氢的方法，其中特定工艺条件的选择允许与二氢香豆素或其烷基化衍生物一起产生大量的香豆素或其烷基化衍生物。 六氢香豆素或衍生物在约脱氢温度下与催化剂接触，然后在第Ⅷ族金属脱氢催化剂存在下，在液相中，在200-375℃的温度下脱氢，同时从反应区除去氢气， 并且反应产物含有以香豆素化合物：二氢香豆素化合物的摩尔比为至少1:5的香豆素或其烷基化衍生物。

    Method for preparing coumarin and derivatives thereof
    7.
    发明授权
    Method for preparing coumarin and derivatives thereof 失效
    香豆素及其衍生物的制备方法

    公开(公告)号：US5872265A

    公开(公告)日：1999-02-16

    申请号：US809189

    申请日：1997-03-17

    Applicant: Stefano Alini ,  Livius Cotarca ,  Pietro Delogu

    Inventor： Stefano Alini ,  Livius Cotarca ,  Pietro Delogu

    IPC: C07D311/08 ,  B01J23/44 ,  C07D311/10

    CPC classification number: C07D311/10

    Abstract: A process for producing coumarin and substituted coumarins starting from substituted hexahydrocoumarins or from substituted dihydrocoumarins. The process includes dehydrogenation in the presence of catalysts based on metals of Group VIII of the periodic table of the elements and in the presence of at least one easily reducible organic compound. The invention allows to achieve exceptionally high yields that do not require the recycling of the hexahydrocoumarin or of the dihydrocoumarin that are present at the end of the reaction, and also allows to achieve high selectivity and easy purification.

    Abstract translation: PCT No.PCT / EP95 / 02687第 371日期1997年3月17日 102（e）1997年3月17日PCT PCT 1995年7月11日PCT公布。 出版物WO96 / 09298 日期1996年3月28日从取代的六氢香豆素或取代的二氢香豆素开始生产香豆素和取代香豆素的方法。 该方法包括在基于元素周期表第Ⅷ族金属的催化剂存在下和在至少一种易于还原的有机化合物存在下脱氢。 本发明允许获得非常高的产率，其不需要在反应结束时存在的六氢香豆素或二氢香豆素的再循环，并且还允许实现高选择性和容易的纯化。

    Process for producing 3,4-dihydrocoumarin derivatives
    9.
    发明授权
    Process for producing 3,4-dihydrocoumarin derivatives 失效
    3,4-二氢香豆素衍生物的制备方法

    公开(公告)号：US5237075A

    公开(公告)日：1993-08-17

    申请号：US839285

    申请日：1992-02-24

    Applicant: Tamio Shirafuji ,  Kiyomi Sakai ,  Kensen Okusako ,  Itaru Kawata ,  Yasumoto Simazu ,  Tetuya Suzuta

    Inventor： Tamio Shirafuji ,  Kiyomi Sakai ,  Kensen Okusako ,  Itaru Kawata ,  Yasumoto Simazu ,  Tetuya Suzuta

    IPC: C07D311/10 ,  C07D311/20

    CPC classification number: C07D311/10 ,  C07D311/20

    Abstract: A process for producing a 3,4-dihydrocoumarin compound represented by formula (II): ##STR1## wherein R.sub.1 to R.sub.4 are as defined in the specification, comprising the steps of:(1) heating a 3-(2-cyclohexanoyl)propionic acid ester compound represented by formula (I): ##STR2## wherein R.sub.1 R.sub.5 are as defined in the specification, in the presence of at least one solid metal catalyst, thereby to allow said compound of formula (I) to undergo ring formation and dehydrogenation to yield said 3,4-dihydrocoumarin compound of formula (II) and, as a by-product, a coumarin compound represented by formula (III): ##STR3## wherein R.sub.1 to R.sub.4 are as defined above; (2) adding a catalyst which is as defined above to said reaction mixture, or bringing said reaction mixture into contact with oxygen to activate said catalyst used in said ring formation and dehydrogenation, without separating said coumarin compound from the reaction mixture that has undergone said ring formation and dehydrogenation; and(3) partially hydrogenating said by-product coumarin compound in said reaction mixture with hydrogen so as to convert said coumarin compound to a 3,4-dihydrocoumarin compound.

    Abstract translation: 制备由式（II）表示的3,4-二氢香豆素化合物的方法：其中R 1至R 4如说明书中所定义，其包括以下步骤：（1）加热3-（2- 环己酰基）丙酸酯化合物：其中R1 R5如说明书中所定义，在至少一种固体金属催化剂存在下，从而使所述式（I）化合物与式 进行环形成和脱氢，得到式（II）的3,4-二氢香豆素化合物，作为副产物，由式（III）表示的香豆素化合物：其中R 1至R 4为 以上定义 （2）向所述反应混合物中加入如上定义的催化剂，或使所述反应混合物与氧接触以活化所述环形成和脱氢中使用的所述催化剂，而不将所述香豆素化合物与已经经历所述反应混合物的反应混合物分离 环形成和脱氢; 和（3）用氢将所述反应混合物中的所述副产物香豆素化合物部分氢化，以将所述香豆素化合物转化为3,4-二氢香豆素化合物。

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