Crosslinking agent, crosslinking method, method of controlling gene expression, and method of examining gene function
    3.
    发明授权
    Crosslinking agent, crosslinking method, method of controlling gene expression, and method of examining gene function 有权
    交联剂,交联方法,基因表达控制方法及检测基因功能的方法

    公开(公告)号:US08084625B2

    公开(公告)日:2011-12-27

    申请号:US11817311

    申请日:2006-02-27

    IPC分类号: C07D311/02 C07D311/00

    摘要: The present invention provides a crosslinking agent which have photodegradable protective groups at two ends to crosslink double-stranded nucleic acid, a nucleic acid and a protein or a polypeptide, or proteins or polypeptides, in particular, double-stranded RNA; a method for crosslinking a double-stranded RNA or the like using the same; a method for regulating gene expression, which can control the expression of a target gene at an arbitrary timing and location; and a method for examining a gene function.According to the present invention, crosslinking between double-stranded nucleic acids between a nucleic acid and a protein or a polypeptide, or between proteins or polypeptides, in particular, between double-stranded RNA can be easily formed, and in addition, the crosslinking can also be easily removed, so that the expression of a target gene can be easily controlled at an arbitrary timing and location with high efficiency. Hence, as a result, function examination and/or identification of a gene that is expressed at a specific timing and location can be performed. In addition, the RNAi effect of a double-stranded RNA (siRNA) that cannot be easily inhibited by a conventional caged compound can be inhibited, and the expression of a target gene can be easily controlled at an arbitrary timing and location.

    摘要翻译: 本发明提供一种交联剂,其在两端具有可光降解的保护基以交联双链核酸,核酸和蛋白质或多肽,或蛋白质或多肽,特别是双链RNA; 使用该双链RNA等进行交联的方法; 调控基因表达的方法,其可以在任意的时间和位置控制靶基因的表达; 以及检测基因功能的方法。 根据本发明,可以容易地形成在核酸和蛋白质或多肽之间或蛋白质或多肽之间,特别是双链RNA之间的双链核酸之间的交联,此外,交联可以 也容易除去,从而能够以高效率容易地在任意的时间和位置控制靶基因的表达。 因此,可以进行在特定的时间和位置表达的基因的功能检查和/或识别。 此外,可以抑制不能容易地被常规笼状化合物抑制的双链RNA(siRNA)的RNAi效应,并且可以容易地在任意的时间和位置控制靶基因的表达。

    Preparation of alkylated or non-alkylated dihydrocoumarin together with the corresponding alkylated, or non-alkylated, coumarin
    4.
    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

    申请人: STAMICARBON

    摘要: 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.

    摘要翻译: 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。

    Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV
    7.
    发明申请
    Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV 有权
    制备HCV大环蛋白酶抑制剂的方法和中间体

    公开(公告)号:US20140228574A1

    公开(公告)日:2014-08-14

    申请号:US14345980

    申请日:2012-09-21

    IPC分类号: C07D453/02 C07C235/82

    摘要: Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water-miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I).

    摘要翻译: 本发明公开了一种通过外消旋的4-羟基-1,2-环戊烷二羧酸的水溶液制备式(Ⅳ)的辛可尼定盐的方法,该水溶液通过加入水 - 向水溶液中混溶的有机溶剂,再次不除水,将辛可尼定加入含水有机溶剂溶液中,得到内酯酸的辛可尼定盐。 使辛啶啶盐结晶,得到对映体纯化的结晶内酯酸辛可尼定盐(IV)。 对映体纯盐是式(I)的HCV抑制剂化合物的合成中的中间体。