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    TRICYCLIC ANTIBIOTICS
    2.
    发明申请
    TRICYCLIC ANTIBIOTICS 有权
    TRICYCLIC抗生素

    公开(公告)号：US20120245345A1

    公开(公告)日：2012-09-27

    申请号：US13511292

    申请日：2010-12-17

    申请人： Bérangère Gaucher ,  Franck Hubert Danel ,  XiaoHu Tang ,  Tong Xie ,  Lin Xu

    发明人： Bérangère Gaucher ,  Franck Hubert Danel ,  XiaoHu Tang ,  Tong Xie ,  Lin Xu

    IPC分类号： C07D491/052 ,  C07D498/14 ,  C07D495/04 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D491/04 ,  C07D491/052 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14

    摘要： Compound of formula (I): wherein A1 represents —O—, —S— or —N—R3; A2 represents —CH2—, —O—, —N—R4, —C(═O)— or —CH(O—R4)—; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C═O or a group selected from —C2H4NH—, —C2H4O—, and —C2H4S— being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is un-substituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of X1 and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.

    摘要翻译： 式（I）化合物：其中A1表示-O - ， - S-或-N-R 3; A 2表示-CH 2 - ， - O - ， - N-R 4，-C（= O） - 或-CH（O-R 4） - ; A3表示C3-C8亚环烷基; 饱和和不饱和的4至8元杂环基与1,2或3个选自氮，氧和硫的杂原子，该基团A3为未取代或取代的; A4表示C1-C4亚烷基，C2-C4亚烯基，> C = O或选自-C2H4NH-，-C2H4O-和-C2H4S-的基团，其通过碳原子连接到相邻的NR5-基团; 并且G表示未取代或取代的芳基或杂芳基，R 1和R 2彼此独立地表示氢或选自羟基，卤素，巯基，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 1 -C 6烷硫基，C 1 -C 6烷基羰基氧基，C 1 -C 6烷基磺酰氧基，C 1 -C 6杂烷基羰氧基，C 5 -C 6杂环羰基氧基，C 1 -C 6杂烷氧基，其中杂烷基，杂烷氧基或杂环基包含1,2或3个选自氮，氧和硫的杂原子，其中烷基部分 是未取代的或进一步取代的; R 3，R 4和R 5彼此独立地表示氢或C 1 -C 6烷基; X 1和X 2彼此独立地表示氮原子或CR 2，条件是X 1和X 2中的至少一个表示氮原子; m为1; （CH 2）m部分任选被C 1 -C 4烷基取代; 卤素，羧基，羟基，C 1 -C 4烷氧基，C 1 -C 4烷基羰基氧基，氨基，单 - 或二 - （C 1 -C 4烷基）氨基或酰氨基n是0,1或2或其药学上可接受的盐对于用作药物是有价值的 用于治疗细菌感染。

    Tricyclic Antibiotics
    4.
    发明申请
    Tricyclic Antibiotics 有权
    三环抗生素

    公开(公告)号：US20140235855A1

    公开(公告)日：2014-08-21

    申请号：US14124144

    申请日：2012-06-11

    申请人： Berangere Gaucher ,  Franck Hubert Danel ,  Tong Xie ,  Lin Xu

    发明人： Berangere Gaucher ,  Franck Hubert Danel ,  Tong Xie ,  Lin Xu

    IPC分类号： C07D498/04 ,  C07D491/052 ,  C07D495/04 ,  C07D491/147

    CPC分类号： C07D498/04 ,  C07D491/052 ,  C07D491/14 ,  C07D491/147 ,  C07D495/04

    摘要： Compounds of formula (I), wherein A1 represents —O—, —S— or —CH2—; A2 represents —CH2— or —O—; A3 represents C3-C8-cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, —C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; m is 0 or 1; n is 1; the —(CH2)n— group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.

    摘要翻译： 式（I）化合物，其中A 1表示-O - ， - S-或-CH 2 - ; A2表示-CH2-或-O-; A3表示C3-C8-亚环烷基; 饱和或不饱和的4至8元杂环基与1,2或3个选自氮或氧的杂原子，该基团A3为未取代或取代的; A4表示C1-C4亚烷基，-C（= O） - ; G表示未取代或取代的芳基或杂芳基; X1表示氮原子或CR1; R1表示氢原子或卤素原子; R1表示氢原子; m为0或1; n为1; - （CH 2）n - 基团是未取代的或取代的; p为0或1; 或其药学上可接受的盐对于用作治疗细菌感染的药物是有价值的。

    Tracking variable information in optimized code
    6.
    发明授权
    Tracking variable information in optimized code 有权
    跟踪优化代码中的变量信息

    公开(公告)号：US08656377B2

    公开(公告)日：2014-02-18

    申请号：US12813404

    申请日：2010-06-10

    申请人： Lin Xu ,  Weiping Hu ,  Yongkang Zhu

    发明人： Lin Xu ,  Weiping Hu ,  Yongkang Zhu

    IPC分类号： G06F9/45

    CPC分类号： G06F8/437

    摘要： Embodiments are directed to tracking variable location information in optimized code and efficiently collecting and storing reaching definition information. A computer system receives a portion of source code at a compiler, where the compiler is configured to compile and optimize the source code for execution. The computer system tags selected variables in the source code with a tag, where the tag is configured to provide location information for the variable. The computer system optimizes the received portion of source code including changing at least one of the tagged variables. The computer system also tracks the tagged variables as the variables are changed by the compiler during code optimization and persists the variable location information, so that the persisted variable location information is available to other compiler components.

    摘要翻译： 实施例涉及在优化代码中跟踪可变位置信息并有效地收集和存储到达定义信息。 计算机系统在编译器处接收一部分源代码，其中编译器被配置为编译和优化用于执行的源代码。 计算机系统使用标签将源代码中的选定变量标记，其中标签被配置为提供变量的位置信息。 计算机系统优化所接收的源代码部分，包括改变至少一个标记变量。 计算机系统还跟踪标记的变量，因为编码器在代码优化期间改变了变量，并且持续存在变量位置信息，使得持久变量位置信息可用于其他编译器组件。

    Process for the manufacture of epoxy triazole derivatives
    8.
    发明授权
    Process for the manufacture of epoxy triazole derivatives 有权
    制备环氧三唑衍生物的方法

    公开(公告)号：US08076494B2

    公开(公告)日：2011-12-13

    申请号：US12872599

    申请日：2010-08-31

    申请人： Marc Muller ,  Lin Xu

    发明人： Marc Muller ,  Lin Xu

    IPC分类号： C07D309/12 ,  C07D319/06 ,  C07C49/225 ,  C07C49/233 ,  C07F7/18

    CPC分类号： C07D309/12 ,  Y02P20/55

    摘要： Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).

    摘要翻译： 公开了制备式（I）化合物的方法，其中Hal表示氟或氯，并且R 1和R 2彼此独立地表示氢或Hal; 在该方法中将式（II）化合物转化为相应的烷基，氟烷基或芳基磺酸酯，然后在极性非亲核溶剂中，在合适的冠醚存在下，与碱金属亚硝酸盐反应， 温度为-10〜50℃，得到式（I）的化合物。

    Process for the manufacture of bridged monobactam intermediates
    9.
    发明申请
    Process for the manufacture of bridged monobactam intermediates 失效
    桥联单体中间体的制备方法

    公开(公告)号：US20110178291A1

    公开(公告)日：2011-07-21

    申请号：US12676580

    申请日：2008-09-15

    申请人： Marc Muller ,  Xiaoping Wu ,  Lin Xu

    发明人： Marc Muller ,  Xiaoping Wu ,  Lin Xu

    IPC分类号： C07D205/00 ,  C07C269/00

    CPC分类号： C07C271/54 ,  C07C271/22 ,  C07D487/04

    摘要： A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).

    摘要翻译： 制备具有顺式构型的式（I）化合物的方法，其中R 1表示1-苯基-C 1 -C 4烷基或1-萘基-C 1 -C 4烷基，其中R 1的苯基或萘基部分是未取代或取代的 与一个或多个C 1 -C 4烷氧基和R 1的烷基部分的2-，3-和/或4-位上的碳原子独立地为R 1的苯基或萘基部分且彼此独立地是未取代的或未取代的 被C1-C4烷氧基和/或甲硅烷氧基取代，或优选未被取代或被每个碳原子一个C1-C4烷氧基和/或甲硅烷氧基取代，R2代表C1-C6烷基或未取代或取代的苄基，其中 处理其中R 3表示C 1 -C 6烷基或未取代或取代的苄基的式（II）化合物，并且R 1和R 2具有与式（I）中相同的含义。 在液体非质子溶剂中在0℃或更低的温度下用碱处理足以获得式（I）化合物的时间段。

    Process for the manufacture of epoxy triazole derivatives
    10.
    发明申请
    Process for the manufacture of epoxy triazole derivatives 有权

    公开(公告)号：US20110021794A1

    公开(公告)日：2011-01-27

    申请号：US12872599

    申请日：2010-08-31

    申请人： Marc Muller ,  Lin Xu

    发明人： Marc Muller ,  Lin Xu

    IPC分类号： C07D309/32 ,  C07C45/68

    CPC分类号： C07D309/12 ,  Y02P20/55

    摘要： Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).