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    Directed synthesis of oligophosphoramidate stereoisomers
    1.
    发明授权
    Directed synthesis of oligophosphoramidate stereoisomers 失效
    导向合成寡聚氨基磷酸酯立体异构体

    公开(公告)号：US08569515B2

    公开(公告)日：2013-10-29

    申请号：US13099630

    申请日：2011-05-03

    申请人： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

    发明人： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

    IPC分类号： C07F9/24

    CPC分类号： G01N33/5308 ,  C07F9/6552 ,  C07F9/65586 ,  Y02P20/55

    摘要： The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

    摘要翻译： 使化合物的三价磷原子与试剂反应，形成稳定的磷酸酯模拟物或说明物。 具有至少一个含有保护基团的羟基残基的磷原子的亚磷酰胺与该游离羟基反应：在第一个合成循环中，羟基通过可裂解或不可裂解的方式与固体支持物连接 接头。 在进一步的合成循环中，通过从生长的低聚物中切割保护基而产生羟基。 这导致形成与叠氮化物反应的亚磷酸三酯。 通过选择具有定义的立体定构的合成合成单体，以立体控制的方式制备式1的化合物。

    DIRECTED SYNTHESIS OF OLIGOPHOSPHORAMIDATE STEREOISOMERS
    2.
    发明申请
    DIRECTED SYNTHESIS OF OLIGOPHOSPHORAMIDATE STEREOISOMERS 失效
    指导性合成寡糖磷酸酯STEREOISOMERS

    公开(公告)号：US20110212861A1

    公开(公告)日：2011-09-01

    申请号：US13099630

    申请日：2011-05-03

    申请人： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

    发明人： Dieter Heindl ,  Dirk Kessler ,  Angelika Roesler ,  Christoph Seidel ,  Wilma Thuer

    IPC分类号： C40B40/04 ,  C07F9/24 ,  G01N33/68

    CPC分类号： G01N33/5308 ,  C07F9/6552 ,  C07F9/65586 ,  Y02P20/55

    摘要： The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

    摘要翻译： 使化合物的三价磷原子与试剂反应，形成稳定的磷酸酯模拟物或说明物。 具有至少一个含有保护基团的羟基残基的磷原子的亚磷酰胺与该游离羟基反应：在第一个合成循环中，羟基通过可裂解或不可切割的方式与固体支持物连接 接头。 在进一步的合成循环中，通过从生长的低聚物中切割保护基而产生羟基。 这导致形成与叠氮化物反应的亚磷酸三酯。 通过选择具有定义的立体定构的合成合成单体，以立体控制的方式制备式1的化合物。

    Nucleic acids encoding fusion peptides
    7.
    发明授权
    Nucleic acids encoding fusion peptides 有权
    编码融合肽的核酸

    公开(公告)号：US07348423B2

    公开(公告)日：2008-03-25

    申请号：US10969624

    申请日：2004-10-20

    申请人： Eva Hoess ,  Thomas Meier ,  Gabriele Pestlin ,  Friedrich Popp ,  Klaus Reichert ,  Rainer Schmuck ,  Bernd Schneidinger ,  Christoph Seidel ,  Wilhelm Tischer

    发明人： Eva Hoess ,  Thomas Meier ,  Gabriele Pestlin ,  Friedrich Popp ,  Klaus Reichert ,  Rainer Schmuck ,  Bernd Schneidinger ,  Christoph Seidel ,  Wilhelm Tischer

    IPC分类号： A61K39/21

    CPC分类号： C07K14/005 ,  C07K2319/00 ,  C12N2740/15022 ,  C12N2740/16122 ,  C12P21/02

    摘要： A process is disclosed for the production of an antifusogenic peptide by producing a fusion peptide of a length of about 14 to 70 amino acids in a prokaryotic host cell, comprising the steps, under such conditions that inclusion bodies of said fusion peptide are formed, of: (a) expressing in said host cell a nucleic acid encoding said fusion peptide consisting of a first peptide which is an antifusogenic peptide of a length of about 10 to 50 amino acids and a second peptide of a length of about 4 to 30 amino acids, said first peptide being N-terminally linked to said second peptide; (b) cultivating said host cell to produce said inclusion bodies; and (c) recovering said antifusogenic peptide from said inclusion bodies, wherein said recovered antifusogenic peptide consists of said fusion peptide or a peptide comprising the antifusogenic peptide of about 10 to 50 amino acids and which is a fragment cleaved from said fusion peptide. Inclusion bodies of the peptides are disclosed. Also disclosed is a nucleic acid encoding the fusion peptide consisting of a first peptide which is an antifusogenic peptide selected from the group of SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, and said sequences further consisting of glycine at the C terminal end, N-terminally linked to the second peptide.

    摘要翻译： 公开了通过在原核宿主细胞中产生约14至70个氨基酸长度的融合肽来生产抗融合肽的方法，包括以下步骤：在形成所述融合肽的包涵体的条件下， （a）在所述宿主细胞中表达编码所述融合肽的核酸，所述融合肽由长度为约10至50个氨基酸的抗融合肽的第一肽和长度为约4-30个氨基酸的第二个肽组成 所述第一肽与所述第二肽N-末端连接; （b）培养所述宿主细胞以产生所述包涵体; 和（c）从所述包涵体中回收所述抗融合肽，其中所述回收的抗融合肽由所述融合肽或包含约10至50个氨基酸的抗融合肽的肽组成，并且是从所述融合肽切割的片段。 公开了肽的包涵体。 还公开了编码由第一肽组成的融合肽的核酸，第一肽是选自SEQ ID NO：7，SEQ ID NO：8，SEQ ID NO：9，SEQ ID NO：10的抗融合肽， 所述序列进一步由C末端的甘氨酸组成，N-末端与第二肽连接。