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    Process for the production of a pemetrexed salt
    63.
    发明授权
    Process for the production of a pemetrexed salt 有权
    培美曲塞盐生产工艺

    公开(公告)号：US09051322B2

    公开(公告)日：2015-06-09

    申请号：US13070114

    申请日：2011-03-23

    申请人： ShangHong Chen ,  HuangHsiung Lin

    发明人： ShangHong Chen ,  HuangHsiung Lin

    IPC分类号： C07D487/04 ,  A61P35/00

    CPC分类号： C07D487/04 ,  C07B2200/13

    摘要： A process of making a pemetrexed salt comprising: a) reacting a compound of formula II or an acid salt thereof, wherein each of R1 and R2 is independently a C1-C6 alkyl group, with an aqueous basic solution at a temperature of no more than 10° C. to obtain a first mixture comprising the pemetrexed salt; b) isolating the pemetrexed salt from the first mixture.

    摘要翻译： 一种制备培美曲塞盐的方法，包括：a）使式II化合物或其酸式盐，其中R 1和R 2各自独立地为C 1 -C 6烷基，与碱水溶液的温度不超过 10℃，以获得包含培美曲塞盐的第一混合物; b）从第一混合物中分离培美曲塞的盐。

    Inhibition-based high-throughput screen strategy for cell clones
    64.
    发明授权
    Inhibition-based high-throughput screen strategy for cell clones 有权
    用于细胞克隆的基于抑制的高通量屏幕策略

    公开(公告)号：US08765370B2

    公开(公告)日：2014-07-01

    申请号：US12792924

    申请日：2010-06-03

    申请人： Wei-Kuang Liu ,  Min-Pey Ding

    发明人： Wei-Kuang Liu ,  Min-Pey Ding

    IPC分类号： C12Q1/68 ,  C12N5/00 ,  C07H21/04

    CPC分类号： C12N15/1086 ,  C07K2319/60 ,  C12N15/85 ,  C12N2840/203 ,  C40B50/06

    摘要： A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.

    摘要翻译： 公开了一种用于筛选靶蛋白的高水平表达的细胞的方法。 该方法包括向多个宿主细胞中引入编码靶蛋白和抑制剂的宿主细胞中的内源选择性标记的DNA构建体，筛选携带用于表达内源选择性标记的DNA构建体的宿主细胞，以及分离 具有降低的可选择标记表达的细胞。 还公开了构建成在宿主细胞内表达靶蛋白和抑制剂的DNA构建体。

    Vector for inhibition-based high-throughput screen strategy
    65.
    发明授权
    Vector for inhibition-based high-throughput screen strategy 有权
    矢量为基于抑制的高通量屏幕策略

    公开(公告)号：US08642327B2

    公开(公告)日：2014-02-04

    申请号：US13231436

    申请日：2011-09-13

    申请人： Wei-Kuang Liu ,  Min-Pey Ding

    发明人： Wei-Kuang Liu ,  Min-Pey Ding

    IPC分类号： C12N15/00

    CPC分类号： C12N15/1086 ,  C07K2319/60 ,  C12N15/85 ,  C12N2840/203 ,  C40B50/06

    摘要： A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.

    摘要翻译： 公开了一种用于筛选靶蛋白高水平表达的细胞的方法。 该方法包括向多个宿主细胞中引入编码靶蛋白和抑制剂的宿主细胞中的内源选择性标记的DNA构建体，筛选携带用于表达内源选择标记的DNA构建体的宿主细胞，以及分离 具有降低的可选择标记表达的细胞。 还公开了构建成在宿主细胞内表达靶蛋白和抑制剂的DNA构建体。

    Synthesis of decitabine
    66.
    发明授权
    Synthesis of decitabine 有权
    地西他滨的合成

    公开(公告)号：US08586729B2

    公开(公告)日：2013-11-19

    申请号：US12572578

    申请日：2009-10-02

    申请人： Julian Paul Henschke ,  Xiaoheng Zhang ,  Jianbo Yu ,  Kun Hu ,  Lijun Mei

    发明人： Julian Paul Henschke ,  Xiaoheng Zhang ,  Jianbo Yu ,  Kun Hu ,  Lijun Mei

    IPC分类号： C08B37/00 ,  C07H5/04 ,  C07H5/06

    CPC分类号： C07H13/08 ,  C07H19/12

    摘要： A method for producing a β-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula I; and b) quenching the reaction mixture of step a) with a base. The β-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.

    摘要翻译： 一种制备富含β-的受保护的地西他滨的方法，包括：a）在催化剂存在下将受保护的2-脱氧 - 呋喃核糖与受保护的5-氮杂胞嘧啶偶联，形成包含式I的受保护的地西他滨的反应混合物; 和b）将碱的步骤a）的反应混合物淬灭。 如此制备的β-富集的保护的地西他滨可以去保护以产生高产率和纯度的地西他滨产品。

    Process for the preparation of cladribine
    67.
    发明授权
    Process for the preparation of cladribine 有权
    克拉屈滨制备工艺

    公开(公告)号：US08232387B2

    公开(公告)日：2012-07-31

    申请号：US12857939

    申请日：2010-08-17

    申请人： Julian Paul Henschke ,  Xiaoheng Zhang ,  Guodong Chu ,  Lijun Mei ,  Yung Fa Chen

    发明人： Julian Paul Henschke ,  Xiaoheng Zhang ,  Guodong Chu ,  Lijun Mei ,  Yung Fa Chen

    IPC分类号： C07H19/00 ,  C07H19/22 ,  A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/173 ,  C07H1/00

    摘要： A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step and then a purification step. Following the coupling, the desired N-9-glycosylated β-anomer of the nucleoside is directly isolated as a solid from the coupling reaction mixture by filtration in relatively high purity and yield, and it does not require purification.

    摘要翻译： 通过将O-保护的2-脱氧 - 呋喃核糖与甲硅烷基化的2-氯腺嘌呤直接偶联，然后在单独的步骤中将所得的被保护的核苷脱保护，然后进行纯化步骤，提供API级克拉屈滨的制备方法。 偶联后，通过过滤以相对较高的纯度和产率将核苷的所需N-9-糖基化 - 单体直接从偶联反应混合物中分离为固体，并且不需要纯化。

    INHIBITION-BASED HIGH-THROUGHPUT SCREEN STRATEGY FOR CELL CLONES
    70.
    发明申请
    INHIBITION-BASED HIGH-THROUGHPUT SCREEN STRATEGY FOR CELL CLONES 有权
    基于抑制的细胞克隆的高通量筛选策略

    公开(公告)号：US20100317532A1

    公开(公告)日：2010-12-16

    申请号：US12792924

    申请日：2010-06-03

    申请人： Wei-Kuang LIU ,  Min-Pey Ding

    发明人： Wei-Kuang LIU ,  Min-Pey Ding

    IPC分类号： C40B30/00 ,  C12Q1/68 ,  C12N15/63

    CPC分类号： C12N15/1086 ,  C07K2319/60 ,  C12N15/85 ,  C12N2840/203 ,  C40B50/06

    摘要： A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.

    摘要翻译： 公开了一种用于筛选靶蛋白高水平表达的细胞的方法。 该方法包括向多个宿主细胞中引入编码靶蛋白和抑制剂的宿主细胞中的内源选择性标记的DNA构建体，筛选携带用于表达内源选择标记的DNA构建体的宿主细胞，以及分离 具有降低的可选择标记表达的细胞。 还公开了构建成在宿主细胞内表达靶蛋白和抑制剂的DNA构建体。