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    Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs
    2.
    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

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

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

    IPC分类号： C07D471/06

    CPC分类号： C07D471/18

    摘要： 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.

    摘要翻译： 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。

    Method and apparatus for fail safe configuration
    3.
    发明授权
    Method and apparatus for fail safe configuration 失效
    用于故障安全配置的方法和装置

    公开(公告)号：US06173420B2

    公开(公告)日：2001-01-09

    申请号：US08961793

    申请日：1997-10-31

    申请人： Ramu V. Sunkara ,  Luk S. Ho ,  Paul F. Mackin ,  David Rowlands

    发明人： Ramu V. Sunkara ,  Luk S. Ho ,  Paul F. Mackin ,  David Rowlands

    IPC分类号： G06F1100

    CPC分类号： G06F11/1415 ,  G06F9/44505

    摘要： A method and apparatus for configuring a software application on a cluster is provided. A configuration coordinator executing on a configuration manager communicates with one or more configuration slaves executing on a set of nodes that are operating as a cluster. The configuration coordinator sends messages to the one or more configuration slaves to initiate a configuration operation for a software application. Each configuration slave automatically performs a series of actions to configure the node on which it resides. When all the nodes complete the configuration operation for the software, the process is complete. While performing the series of actions, the configuration slaves generate logs that reflect their progress in performing the series of actions. If a problem occurs during performance of the series of actions, the configuration slave that encounters the problem indicates to the configuration coordinator that an error occurred. The configuration coordinator responds to the error by causing the configuration slaves to roll back changes made during performance of the series of actions. The configuration slaves that have begun but not completed the series of actions inspect their logs to determine which changes to roll back. By automatically configuring software on a cluster, and automatically rolling back changes on all cluster nodes in the event of an error during the configuration process, the cluster configuration process is made atomic, automatic, and significantly faster and less error-prone than manual cluster-wide configuration operations.

    摘要翻译： 提供了一种用于在集群上配置软件应用的方法和装置。 在配置管理器上执行的配置协调器与在作为集群操作的一组节点上执行的一个或多个配置从站进行通信。 配置协调器向一个或多个配置从站发送消息，以启动软件应用程序的配置操作。 每个配置从站自动执行一系列操作来配置其所在的节点。 当所有节点完成软件的配置操作时，该过程完成。 在执行一系列操作时，配置从站会生成反映其执行一系列操作的进度的日志。 如果在执行一系列操作期间发生问题，则遇到此问题的配置从站将向配置协调器指示发生错误。 配置协调器通过使配置从站回滚执行一系列操作期间所做的更改来响应错误。 已经开始但尚未完成的配置从站系列操作检查其日志以确定要回滚的更改。 通过在集群中自动配置软件，并在配置过程中发生错误时自动回滚所有集群节点上的更改，集群配置过程的原子化，自动化和显着更快，并且比手动集群 - 宽配置操作。

    Heterocyclic compounds as inhibitors of beta-lactamases
    8.
    发明申请
    Heterocyclic compounds as inhibitors of beta-lactamases 有权
    杂环化合物作为β-内酰胺酶的抑制剂

    公开(公告)号：US20050020572A1

    公开(公告)日：2005-01-27

    申请号：US10898754

    申请日：2004-07-26

    申请人： Jozsef Aszodi ,  Claude Fromentin ,  Maxime Lampilas ,  David Rowlands

    发明人： Jozsef Aszodi ,  Claude Fromentin ,  Maxime Lampilas ,  David Rowlands

    IPC分类号： C07D487/08 ,  A61K31/397 ,  A61K31/4188 ,  A61K31/439 ,  A61K31/519 ,  A61K31/55 ,  A61P31/04 ,  A61P43/00 ,  C07D471/08 ,  C07D498/08

    CPC分类号： A61K31/439 ,  A61K31/55 ,  A61K2300/00

    摘要： This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.

    摘要翻译： 本发明公开并要求通过抑制人或动物中的细菌β-内酰胺酶抑制细菌β-内酰胺酶和治疗细菌感染的方法，包括向所述人或所述动物施用治疗有效量的化合物或其药学上可接受的盐 式（I）单独或与β-内酰胺抗生素组合，其中所述组合可以分开施用，一起或随时间隔开。 还公开和要求保护包含式（I）化合物或式（I）化合物与治疗有效量的β-内酰胺抗生素和药学上可接受的载体的组合物的药物组合物。

    Hepatitis B core antigen fusion proteins
    9.
    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

    申请人： Annick Gehin ,  Robert Gilbert ,  David Stuart ,  David Rowlands

    发明人： Annick Gehin ,  Robert Gilbert ,  David Stuart ,  David Rowlands

    IPC分类号： A61K39/00

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

    摘要： 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.

    摘要翻译： 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。