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    NOVEL NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL DRUGS
    5.
    发明申请
    NOVEL NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL DRUGS 失效
    新型含氮杂环化合物，其制备及其作为抗菌药物使用

    公开(公告)号：US20100087648A1

    公开(公告)日：2010-04-08

    申请号：US12536096

    申请日：2009-08-05

    Applicant: Maxime Lampilas ,  David Rowlands ,  Benoit Ledoussal ,  Marie-Edith Gourdel ,  Emilie Renaud ,  Camille Pierres ,  Adel Kebsi

    Inventor： Maxime Lampilas ,  David Rowlands ,  Benoit Ledoussal ,  Marie-Edith Gourdel ,  Emilie Renaud ,  Camille Pierres ,  Adel Kebsi

    IPC: C07D471/06

    CPC classification number: C07D471/18

    Abstract: The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 form together a nitrogen-containing heterocycle with aromaticity with 5 apices containing 1, 2 or 3 nitrogen atoms, substituted on this nitrogen atom or one of these nitrogen atoms with a (CH2)m—(C(O))p—R5 group, m being equal to 0, 1, 2 or 3, p being equal to 0 or 1 and R5 representing a hydroxy group, in which case p is equal to 1, or an amino, (C1-C6)alkyl or di-(C1-C6)alkyl amino, a nitrogen-containing heterocycle with aromaticity with 5 or 6 apices containing 1 or 2 nitrogen atoms and if necessary, an oxygen or sulfur atom; it being understood that when the sub-group (C(O))p—R5 forms a carboxy, amino, (C1-C6) alkyl or di-(C1-C6) alkyl amino, group, m is different from 0 or 1; in free form or as zwitterions and salts with pharmaceutically acceptable mineral or organic bases and acids, to their preparation and to their use as antibacterial drugs.

    Abstract translation: 本发明涉及通式（I）的含氮杂环化合物，其中：R1表示（CH2）n-NH2基，n等于1或2; R2表示氢原子; R3和R4一起形成具有芳香性的含氮杂环，其中含有1,2或3个氮原子的5个顶点，在该氮原子上被这些氮原子取代，或者与（CH 2）m - （C（O） R5基团，m等于0,1,2或3，p等于0或1，R5表示羟基，在这种情况下p等于1，或氨基，（C 1 -C 6）烷基或二 - （C1-C6）烷基氨基，具有芳香性的含有5或6个含有1或2个氮原子的顶点的含氮杂环，如果需要，含氧或硫原子; 应理解，当亚组（C（O））p -R 5形成羧基，氨基，（C 1 -C 6）烷基或二 - （C 1 -C 6）烷基氨基时，m不同于0或1 ; 游离形式或与药学上可接受的矿物或有机碱和酸的两性离子和盐与其制备和作为抗菌药物的用途。

    Hepatitis B core antigen fusion proteins
    7.
    发明授权
    Hepatitis B core antigen fusion proteins 有权
    乙型肝炎核心抗原融合蛋白

    公开(公告)号：US07270821B2

    公开(公告)日：2007-09-18

    申请号：US10240917

    申请日：2001-04-09

    Applicant: Annick Gehin ,  Robert Gilbert ,  David Stuart ,  David Rowlands

    Inventor： Annick Gehin ,  Robert Gilbert ,  David Stuart ,  David Rowlands

    IPC: A61K39/00

    CPC classification number: C07K14/005 ,  A61K38/00 ,  A61K39/00 ,  A61K2039/53 ,  C07K2319/00 ,  C07K2319/40 ,  C07K2319/735 ,  C07K2319/80 ,  C12N15/62 ,  C12N2730/10122 ,  Y02A50/466

    Abstract: The hepatitis B virus (HBV) capsid is made up of a single species of protein called the core antigen (HBcAg) which self-assembles into particles. The particles are highly immunogenic and are able to present heterologous epitopes to the immune system when the epitopes are inserted into a surface-exposed region of the particles called the “e1 loop”. The structural building blocks of the particles are tightly associated dimers of HBcAg in which the adjacent e1 loops are closely juxtaposed. It is proposed that sequences inserted into the e1 loop are conformationally restrained in the assembled particles when presented in monomeric core protein. The invention seeks to solve this problem by covalently linking core proteins as tandem copies (e.g., as dimers) so that insertions can be made independently in each copy. This is particularly useful for insertion of large sequences into the e1 loop because it allows such sequences to be inserted into just one copy of the core protein per tandem repeat, thereby reducing potential conformational clashes in assembly. Alternatively, a different sequence may be inserted into each e1 loop of a tandem repeat, thus increasing the flexibility of HBcAg particles as an epitope delivery system.

    Abstract translation: 乙型肝炎病毒（HBV）衣壳由称为核心抗原（HBcAg）的单一种类的蛋白质组成，其自组装成颗粒。 当将表位插入称为“e1循环”的颗粒的表面暴露区域中时，颗粒是高度免疫原性的并且能够向免疫系统提供异源表位。 颗粒的结构构件是HBcAg的紧密相关的二聚体，其中相邻的e1环相互并置。 提出插入到e1环中的序列在单体核心蛋白中呈现时，在组装的颗粒中被构象地约束。 本发明寻求通过将核心蛋白质共价连接作为串联拷贝（例如，作为二聚体）来解决这个问题，从而可以在每个拷贝中独立地进行插入。 这对于将大序列插入到e1环中是特别有用的，因为它允许这样的序列插入到每个串联重复的核心蛋白的一个拷贝中，从而减少组装中潜在的构象冲突。 或者，可以将不同的序列插入到串联重复的每个e1环中，从而增加HBcAg颗粒作为表位递送系统的灵活性。

    Flyer bow with integral enclosed wire guide
    9.
    发明授权
    Flyer bow with integral enclosed wire guide 有权
    传单弓与集成的封闭线导轨

    公开(公告)号：US06223513B1

    公开(公告)日：2001-05-01

    申请号：US09448263

    申请日：1999-11-24

    Applicant: Jeffrey M. Post ,  David Rowlands ,  Mark Broding

    Inventor： Jeffrey M. Post ,  David Rowlands ,  Mark Broding

    IPC: D04H726

    CPC classification number: D07B3/103 ,  D01H7/30

    Abstract: An exemplary embodiment of the present invention is a flyer bow having a first surface and a second surface in opposition to the first surface. The first and second surfaces are joined to form an airfoil shape. A channel passes through the flyer bow between the first and second surface and a wire guide is disposed within the channel. There is at least one orifice through one of the first and second surface thereby establishing fluid communication between the channel and the ambient atmosphere.

    Abstract translation: 本发明的示例性实施例是具有与第一表面相对的第一表面和第二表面的传单弓。 第一和第二表面被连接以形成翼型。 一个通道穿过第一和第二表面之间的传单弓，导线器设置在通道内。 通过第一和第二表面中的一个具有至少一个孔口，从而建立通道与环境大气之间的流体连通。

    Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs
    10.
    发明授权
    Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs 失效
    含氮杂环化合物，其制备及其用作抗菌药物

    公开(公告)号：US08067435B2

    公开(公告)日：2011-11-29

    申请号：US12536096

    申请日：2009-08-05

    Applicant: Maxime Lampilas ,  David Rowlands ,  Benoit Ledoussal ,  Marie-Edith Gourdel ,  Emilie Renaud ,  Camille Pierres ,  Adel Kebsi

    Inventor： Maxime Lampilas ,  David Rowlands ,  Benoit Ledoussal ,  Marie-Edith Gourdel ,  Emilie Renaud ,  Camille Pierres ,  Adel Kebsi

    IPC: C07D471/06

    CPC classification number: C07D471/18

    Abstract: The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 form together a nitrogen-containing heterocycle with aromaticity with 5 apices containing 1, 2 or 3 nitrogen atoms, substituted on this nitrogen atom or one of these nitrogen atoms with a (CH2)m—(C(O))p—R5 group, m being equal to 0, 1, 2 or 3, p being equal to 0 or 1 and R5 representing a hydroxy group, in which case p is equal to 1, or an amino, (C1-C6)alkyl or di-(C1-C6)alkyl amino, a nitrogen-containing heterocycle with aromaticity with 5 or 6 apices containing 1 or 2 nitrogen atoms and if necessary, an oxygen or sulfur atom; it being understood that when the sub-group (C(O))p—R5 forms a carboxy, amino, (C1-C6) alkyl or di-(C1-C6) alkyl amino, group, m is different from 0 or 1; in free form or as zwitterions and salts with pharmaceutically acceptable mineral or organic bases and acids, to their preparation and to their use as antibacterial drugs.

    Abstract translation: 本发明涉及通式（I）的含氮杂环化合物，其中：R1表示（CH2）n-NH2基，n等于1或2; R2表示氢原子; R3和R4一起形成具有芳香性的含氮杂环，其中含有1,2或3个氮原子的5个顶点，在该氮原子上被这些氮原子取代，或者与（CH 2）m - （C（O） R5基团，m等于0,1,2或3，p等于0或1，R5表示羟基，在这种情况下p等于1，或氨基，（C 1 -C 6）烷基或二 - （C1-C6）烷基氨基，具有芳香性的含有5或6个含有1或2个氮原子的顶点的含氮杂环，如果需要，含氧或硫原子; 应理解，当亚组（C（O））p -R 5形成羧基，氨基，（C 1 -C 6）烷基或二 - （C 1 -C 6）烷基氨基时，m不同于0或1 ; 游离形式或与药学上可接受的矿物或有机碱和酸的两性离子和盐与其制备和作为抗菌药物的用途。

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