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    HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES
    1.
    发明申请
    HETEROCYCLIC COMPOUNDS AS INHIBITORS OF BETA-LACTAMASES 审中-公开
    作为β-Lactamases的抑制剂的杂环化合物

    公开(公告)号：US20100048528A1

    公开(公告)日：2010-02-25

    申请号：US12610562

    申请日：2009-11-02

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

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

    IPC分类号： A61K31/546 ,  A61K31/439 ,  A61K31/431

    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： 本发明公开并要求了通过抑制人或动物中的细菌和β-内酰胺酶来抑制细菌和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-乳糖抗生素组合，其中所述组合可以分开施用，一起或随时间隔开。 还公开并要求保护包含式（I）化合物或式（I）化合物与治疗有效量的β-乳糖抗生素和药学上可接受的载体的组合物的药物组合物。

    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    2.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US07232834B2

    公开(公告)日：2007-06-19

    申请号：US10659164

    申请日：2003-09-10

    申请人： Eric Bacque ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacque ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61K31/4545 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents

    摘要翻译： R 1是氢或氟的通式（I）的喹啉基丙基哌啶衍生物，R 2是羧基，羧甲基或羟甲基，R 3是 被任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的苯硫基取代或被任选被卤素或三氟甲基取代的环烷硫基（3至7成员）或与杂芳硫基 6个成员和1至4个选自N，O和S的杂原子），任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的杂原子，或者R 3是炔丙基 被如上定义的苯基或杂芳基取代，并且R 4是烷基，链烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基 以其各种异构体形式，分别或作为混合物，以及它们的盐，其制备方法和含量 ermediates和含有它们的组合物。 这些新型衍生物是有效的抗菌剂

    AZABICYCLIC COMPOUNDS, PREPARATION THEREOF AND USE OF SAME AS DRUGS, ESPECIALLY BETA-LACTAMASE INHIBITORS
    3.
    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。

    Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments
    5.
    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。

    NOVEL COMBINATIONS OF NITROGENATED HETEROCYCLIC ANTIBACTERIAL COMPOUNDS WITH OTHER ANTIBACTERIAL COMPOUNDS AND THE USE OF SAME AS DRUGS
    7.
    发明申请
    NOVEL COMBINATIONS OF NITROGENATED HETEROCYCLIC ANTIBACTERIAL COMPOUNDS WITH OTHER ANTIBACTERIAL COMPOUNDS AND THE USE OF SAME AS DRUGS 审中-公开
    硝酸酯类杂环化合物与其他抗生素化合物的新型组合及其作为药物的用途

    公开(公告)号：US20100092443A1

    公开(公告)日：2010-04-15

    申请号：US12535865

    申请日：2009-08-05

    申请人： Premavathy Levasseur ,  John Lee Pace ,  Kenneth Coleman ,  John Lowther

    发明人： Premavathy Levasseur ,  John Lee Pace ,  Kenneth Coleman ,  John Lowther

    IPC分类号： A61K35/74 ,  A61K31/551 ,  A61K31/70 ,  A61K31/43 ,  A61K31/65 ,  A61K38/14 ,  A61K31/397 ,  A61K31/545 ,  A61P31/04

    CPC分类号： C07D471/18

    摘要： The invention relates to the combination of nitrogenated heterocyclic antibacterial compounds of formula (I) with other antibacterial compounds and the use of same as drugs.The nitrogenated heterocyclic compounds are of general formula (I) wherein R1 represents a (CH2)n-NH2 or (CH2)n—NHR radical, where R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 together form an aromatic nitrogenated heterocycle with 5 apexes with 1, 2 or 3 nitrogen atoms optionally substituted by one or several R′ groups, R′ being selected in the group composed of a hydrogen atom and the alkyl radicals with 1 to 6 carbon atoms, in free form, as zwitterions, and in the form of salts of pharmaceutically acceptable inorganic or organic bases and acids. The other antibacterial compound is selected among the group comprised of beta-lactams, monobactams or penicillins, if needed combined with a beta lactamases inhibitor, aminoglycosides, glycylcyclines, tetracyclines, quinolones, glycopeptides, lipopeptides, macrolides, ketolides, lincosamides, streptogramins, oxazolidinones, polymyxins and other compounds known to have therapeutic activity on Pseudomonas aeruginosa and Enterobacteriaceae.

    摘要翻译： 本发明涉及式（I）的氮化杂环抗菌化合物与其它抗菌化合物的组合及其与药物的用途。 氮化杂环化合物具有通式（I），其中R 1表示（CH 2）n -NH 2或（CH 2）n -NHR基，其中R是（C 1 -C 6）烷基，n等于1或2; R2表示氢原子; R3和R4一起形成具有5个具有1,2或3个氮原子的顶点的芳族氮杂环，任选被一个或几个R'基团取代，R'选自由氢原子组成的组，并且具有1至6个 游离形式的碳原子作为两性离子，并且为药学上可接受的无机或有机碱和酸的盐的形式。 如果需要与β-内酰胺酶抑制剂，氨基糖苷类，甘氨酰环素，四环素，喹诺酮类，糖肽，脂肽，大环内酯类，酮内酯，林可素，链霉素，恶唑烷酮类， 已知对铜绿假单胞菌和肠杆菌科具有治疗活性的多粘菌素和其它化合物。

    Nitrogenous heterocyclic compounds, preparation thereof and use thereof as antibacterial medicaments
    10.
    发明授权
    Nitrogenous heterocyclic compounds, preparation thereof and use thereof as antibacterial medicaments 有权
    含氮杂环化合物，其制备及其作为抗菌药物的用途

    公开(公告)号：US08063219B2

    公开(公告)日：2011-11-22

    申请号：US12595120

    申请日：2008-04-11

    申请人： Maxime Lampilas ,  David Alun Rowlands ,  Adel Kebsi ,  Benoit Ledoussal ,  Camille Pierres

    发明人： Maxime Lampilas ,  David Alun Rowlands ,  Adel Kebsi ,  Benoit Ledoussal ,  Camille Pierres

    IPC分类号： A61K31/437 ,  A61P31/04 ,  C07D471/04

    CPC分类号： C07D471/18

    摘要： The invention concerns nitrogenated heterocyclic compounds, their preparation and use as antibacterial drugs, compounds of general formula (I) wherein R1 represents a (CH2)n-NHR2 or (CH2)n-NHR radical, where R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 together form an aromatic nitrogenated heterocycle with 5 apexes with 1, 2 or 3 nitrogen atoms optionally substituted by one or several R′ groups, R′ being selected in the group composed of a hydrogen atom and alkyl radicals with 1 to 6 carbon atoms; in free form, as zwitterions, and in the form of salts of pharmaceutically acceptable inorganic or organic bases and acids.

    摘要翻译： 本发明涉及氮杂环化合物，它们作为抗菌药物的制备和用途，其中R 1表示（CH 2）n -NHR 2或（CH 2）n -NHR基团的通式（I）的化合物，其中R是（C 1 -C 6） 烷基，n等于1或2; R2表示氢原子; R3和R4一起形成具有5个具有1,2或3个氮原子的顶点的芳族氮杂环，任选被一个或多个R'基团取代，R'选自由氢原子组成的组和具有1至6个碳原子的烷基 原子 游离形式，作为两性离子，以及药学上可接受的无机或有机碱和酸的盐的形式。