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    NOVEL HETEROCYCLIC NITROGENOUS COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS
    1.
    发明申请
    NOVEL HETEROCYCLIC NITROGENOUS COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS 失效
    新型杂环化合物，其制备及其作为抗菌药物使用

    公开(公告)号：US20100093784A1

    公开(公告)日：2010-04-15

    申请号：US12536034

    申请日：2009-08-05

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

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

    IPC分类号： A61K31/439 ,  C07D471/02 ,  A61P31/04

    CPC分类号： C07D487/18

    摘要： The invention relates to nitrogenous heterocyclic compounds of formula in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C1-C6)alk, —(CH2)m—N(C1-C6)alk2, —(CH2)m—NH—C(NH)NH2 or —(CH2)m—NH—CH═NH, m is equal to 1 or 2; R2 and R3 together form a nitrogenous heterocycle of aromatic character with 5 vertices containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R4; R4 represents hydrogen, C1-C6)alk or a chain of formula: -(A)n-(NH)o—(CH2)p—(CHR′)qR″ A represents C═O, C═NH or SO2; R′ represents hydrogen or carboxy.

    摘要翻译： 本发明涉及下式的含氮杂环化合物，其中：R1表示氢， - （CH2）m -NH2， - （CH2）m-NH（C1-C6）烷基， - （CH2）m-N（C1-C6） 烷基， - （CH2）m-NH-C（NH）NH2或 - （CH2）m-NH-CH = NH，m等于1或2; R2和R3一起形成芳族字符的含氮杂环，其中5个顶点含有1,2或3个氮原子，在氮原子上被R4取代; R 4表示氢，C 1 -C 6烷基或下式的链： - （A）n-（NH）o-（CH 2）p - （CHR'）q R“A表示C = O，C = NH或SO 2; R'表示氢或羧基。

    NOVEL NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL DRUGS
    2.
    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

    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。

    Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments
    3.
    发明授权
    Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments 失效
    取代的吡唑并[3,4-E] [二氮杂-6-5（H））及其类似物，其制备及其作为抗菌药物的用途

    公开(公告)号：US08148366B2

    公开(公告)日：2012-04-03

    申请号：US12536034

    申请日：2009-08-05

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

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

    IPC分类号： A61K31/55

    CPC分类号： C07D487/18

    摘要： The invention relates to nitrogenous heterocyclic compounds of formula (I): in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C1-C6)alk, —(CH2)m—N(C1-C6)alk2, —(CH2)m—NH—C(NH)NH2 or —(CH2)m—NH—CH═NH, m is equal to 1 or 2; R2 and R3 together form a nitrogenous heterocycle of aromatic character with 5 vertices containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R4; R4 represents hydrogen, C1-C6)alk or a chain of formula: -(A)n-(NH)o—(CH2)p—(CHR′)qR″ A represents C═O, C═NH or SO2; R′ represents hydrogen or carboxy.

    摘要翻译： 本发明涉及式（I）的含氮杂环化合物：其中：R1表示氢， - （CH2）m -NH2， - （CH2）m-NH（C1-C6）烷基， - （CH2）m-N C1-C6）烷基， - （CH2）m-NH-C（NH）NH2或 - （CH2）m-NH-CH = NH，m等于1或2; R2和R3一起形成芳族字符的含氮杂环，其中5个顶点含有1,2或3个氮原子，在氮原子上被R4取代; R 4表示氢，C 1 -C 6烷基或下式的链： - （A）n-（NH）o-（CH 2）p - （CHR'）q R“A表示C = O，C = NH或SO 2; R'表示氢或羧基。

    Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs
    4.
    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。

    AZABICYCLIC COMPOUNDS, PREPARATION THEREOF AND USE OF SAME AS DRUGS, ESPECIALLY BETA-LACTAMASE INHIBITORS
    5.
    发明申请
    AZABICYCLIC COMPOUNDS, PREPARATION THEREOF AND USE OF SAME AS DRUGS, ESPECIALLY BETA-LACTAMASE INHIBITORS 审中-公开
    异丁烯酸化合物，其制备方法及其作为药物，特别是β-乳糖酶抑制剂的用途

    公开(公告)号：US20110046102A1

    公开(公告)日：2011-02-24

    申请号：US12990312

    申请日：2009-04-24

    申请人： Benoit Ledoussal ,  Marie-Edith Gourdel

    发明人： Benoit Ledoussal ,  Marie-Edith Gourdel

    IPC分类号： C07D471/08 ,  A61K31/439 ,  A61K31/546 ,  A61P31/04

    CPC分类号： C07D471/08

    摘要： The invention concerns the compounds meeting formula (I: wherein one of R1 and R2 is a hydrogen and the other a fluorine or both represent a fluorine, in free form, in the form of zwitterions and of salts with pharmaceutically acceptable mineral or organic bases, the preparation thereof and their use as medicinal products inhibiting the action of β-lactamases by pathogenic bacteria.

    摘要翻译： 本发明涉及满足式（I）的化合物：其中R 1和R 2中的一个为氢，另一个为氟或两者为游离形式的氟，以两性离子的形式，以及与药学上可接受的矿物或有机碱形成的盐， 其制备及其作为抑制病原菌对β-内酰胺酶作用的药物的用途。