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    Diarylalkanes as potent inhibitors of binuclear enzymes
    1.
    发明授权
    Diarylalkanes as potent inhibitors of binuclear enzymes 有权
    二芳基烷烃作为双核酶的有效抑制剂

    公开(公告)号：US08729136B2

    公开(公告)日：2014-05-20

    申请号：US13707270

    申请日：2012-12-06

    申请人： Unigen, Inc.

    发明人： Qi Jia ,  Ji-Fu Zhao

    IPC分类号： A61K31/75

    CPC分类号： A61K8/347 ,  A61K8/31 ,  A61K8/4973 ,  A61K8/97 ,  A61K31/015 ,  A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/357 ,  A61K31/40 ,  A61K31/704 ,  A61K2800/782 ,  A61Q19/02 ,  C07C39/15 ,  C07C39/367 ,  C07C41/26 ,  C07C41/32 ,  C07C43/23 ,  C07C45/673 ,  C07C49/835 ,  C07C215/74 ,  C07D321/12 ,  Y02A50/406 ,  Y02A50/411

    摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

    摘要翻译： 本发明实现了一种将酶抑制测定与化学去除方法结合以鉴别活性植物提取物和特异性抑制双核酶功能的那些提取物中的二芳基烷烃和/或二芳基链烷醇的策略。 包括在本发明中的是由一种或多种二芳基烷烃和/或二芳基链烷醇组成的物质组合物，其抑制双核酶，特别是酪氨酸酶的活性，并且其防止黑色素过量产生。 本发明还提供了抑制双核酶，特别是酪氨酸酶的活性的方法，以及用于预防和治疗与双核酶功能相关的疾病和病症的方法。 本发明还包括一种预防和治疗与其相关的黑色素过量产生及其疾病和病症的方法。 用于预防和治疗与双核酶功能和黑色素过量产生相关的疾病和病症的方法包括向有需要的宿主施用有效量的包含一种或多种二芳基烷烃和/或二芳基链烷醇的组合物，所述二芳基烷烃和/或二芳基链烷醇合成和/或分离自 更多的植物和药学上可接受的载体。

    Processes for separating components in alkyl perfluoroalkene ether production
    2.
    发明授权
    Processes for separating components in alkyl perfluoroalkene ether production 有权
    烷基全氟烯烃生产中分离组分的方法

    公开(公告)号：US08592630B2

    公开(公告)日：2013-11-26

    申请号：US13627024

    申请日：2012-09-26

    申请人： E I Du Pont De Nemours and Company

    发明人： Robert D Lousenberg

    IPC分类号： C07C209/86 ,  C07C41/06

    CPC分类号： C07C41/16 ,  C07C41/32 ,  C07C41/38 ,  Y02P20/584 ,  C07C43/17

    摘要： Disclosed are processes for reacting a perfluorinated olefin with an alcohol, an alkali metal hydroxide, and water in the presence of a phase transfer catalyst to form a reaction product mixture that separates into an aqueous phase and an organic phase. Alcohol may be present in an effective amount sufficient to form a third phase comprising at least 50% of the phase transfer catalyst. The third phase can be separated from the organic phase. Also disclosed are methods for recovering and recycling the phase transfer catalyst used in the reaction.

    摘要翻译： 公开了在相转移催化剂存在下使全氟化烯烃与醇，碱金属氢氧化物和水反应以形成分离成水相和有机相的反应产物混合物的方法。 醇可以以足以形成包含至少50％的相转移催化剂的第三相的有效量存在。 第三相可以与有机相分离。 还公开了用于回收和再循环反应中使用的相转移催化剂的方法。

    PROCESSES FOR SEPARATING COMPONENTS IN ALKYL PERFLUOROALKENE ETHER PRODUCTION
    3.
    发明申请
    PROCESSES FOR SEPARATING COMPONENTS IN ALKYL PERFLUOROALKENE ETHER PRODUCTION 有权
    用于分离全氟代烷基醚生产中的组分的方法

    公开(公告)号：US20130079558A1

    公开(公告)日：2013-03-28

    申请号：US13627024

    申请日：2012-09-26

    申请人： E I DU PONT DE NEMOURS AND COMPANY

    发明人： Robert D. Lousenberg

    IPC分类号： C07C209/86 ,  C07C41/06

    CPC分类号： C07C41/16 ,  C07C41/32 ,  C07C41/38 ,  Y02P20/584 ,  C07C43/17

    摘要： Disclosed are processes for reacting a perfluorinated olefin with an alcohol, an alkali metal hydroxide, and water in the presence of a phase transfer catalyst to form a reaction product mixture that separates into an aqueous phase and an organic phase. Alcohol may be present in an effective amount sufficient to form a third phase comprising at least 50% of the phase transfer catalyst. The third phase can be separated from the organic phase. Also disclosed are methods for recovering and recycling the phase transfer catalyst used in the reaction.

    摘要翻译： 公开了在相转移催化剂存在下使全氟化烯烃与醇，碱金属氢氧化物和水反应以形成分离成水相和有机相的反应产物混合物的方法。 醇可以以足以形成包含至少50％的相转移催化剂的第三相的有效量存在。 第三相可以与有机相分离。 还公开了用于回收和再循环反应中使用的相转移催化剂的方法。

    Process for production of lasofoxifene or analogue thereof
    4.
    发明授权
    Process for production of lasofoxifene or analogue thereof 有权
    雷诺昔芬或其类似物的生产方法

    公开(公告)号：US08193394B2

    公开(公告)日：2012-06-05

    申请号：US12162068

    申请日：2007-01-25

    申请人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    发明人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    IPC分类号： C07C33/02

    CPC分类号： C07C67/287 ,  C07C41/24 ,  C07C41/26 ,  C07C41/32 ,  C07C67/293 ,  C07C2602/10 ,  C07D295/084 ,  C07C69/63 ,  C07C69/24 ,  C07C43/23

    摘要： Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

    摘要翻译： 本发明公开了一种生产拉索昔芬，nafoxidine或其类似物的新方法，其包括减少数量的反应步骤，具有高效率，并且实际上是有利的。 为了生产拉索昔芬或其类似物，使用由式（4）表示的化合物作为中间体。 由式（4）表示的化合物可以通过在一个步骤中进行三种成分的偶联而使用由式（1）至（3）表示的化合物作为起始化合物来制备。

    Process for the preparation of vinyl ether compounds
    6.
    发明申请
    Process for the preparation of vinyl ether compounds 审中-公开
    乙烯基醚化合物的制备方法

    公开(公告)号：US20070149828A1

    公开(公告)日：2007-06-28

    申请号：US11644958

    申请日：2006-12-26

    申请人： Takahiro Iwahama ,  Yasutaka Ishii

    发明人： Takahiro Iwahama ,  Yasutaka Ishii

    IPC分类号： C07C41/32

    CPC分类号： C07C41/32 ,  C07C2601/14 ,  C07D493/04 ,  C07C43/162

    摘要： A vinyl ether compound represented by following Formula (2): wherein R represents an organic group; and R1, R2, R3 and R4 are the same as or different from one another and each represent a hydrogen atom or an organic group, is produced by isomerizing an allyl ether compound in the presence of a base and a compound of a Group VIII element of the Periodic Table of Elements, which allyl ether compound is represented by following Formula (1): wherein R, R1, R2, R3 and R4 are as defined above.

    摘要翻译： 由下式（2）表示的乙烯基醚化合物：其中R表示有机基团; 且R 1，R 2，R 3和R 4彼此相同或不同，并且 各自表示氢原子或有机基团，通过在碱的存在下异构化烯丙基醚化合物和元素周期表的第Ⅷ族元素的化合物而制备，该烯丙基醚化合物由下式（1 ）：其中R，R 1，R 2，R 3和R 4如上定义。