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    Synthesis of novel neamine derivatives and use thereof as antibacterial agents
    4.
    发明授权
    Synthesis of novel neamine derivatives and use thereof as antibacterial agents 有权
    新型神经胺衍生物的合成及其作为抗菌剂的用途

    公开(公告)号：US08729035B2

    公开(公告)日：2014-05-20

    申请号：US12735511

    申请日：2009-01-22

    申请人： Jean-Luc Decout ,  Isabelle Baussanne ,  Jerome Desire ,  Jean-Marc Paris

    发明人： Jean-Luc Decout ,  Isabelle Baussanne ,  Jerome Desire ,  Jean-Marc Paris

    IPC分类号： A61K31/70 ,  C07H15/20 ,  C07H15/22

    CPC分类号： C07H15/224

    摘要： This invention concerns compounds with the formula: in which: R1═OH or NH2; OR2, OR3, OR4 and OR5 are alcohol, ether, ester, carbonate, carbamate, sulphonate or sulphamate groups; and if R5═H if R2═R3═R4, then R2, R3 and R4≠H; if R2═H, then R3≠H and R4≠H; if R3═H, then R2≠H and R4≠H; if R4═H, then R2≠H and R3≠H; if R5≠H if R2=H, then R3≠H and R4≠H; if R3═H, then R2≠H and R4≠H; if R4═H, then R2≠H and R3≠H, their use as antibiotic agents and the process for synthesizing them.

    摘要翻译： 本发明涉及下式的化合物：其中：R1 = OH或NH2; OR2，OR3，OR4和OR5是醇，醚，酯，碳酸酯，氨基甲酸酯，磺酸酯或氨基磺酸酯基团; 如果R 2 = R 3 = R 4，如果R 5为H，那么R 2，R 3和R 4≠H; 如果R2 = H，则R3≠H，R4≠H; 如果R3 = H，则R2≠H，R4≠H; 如果R4 = H，则R2≠H，R3≠H; 如果R2 = H，则R5≠H，则R3≠H，R4≠H; 如果R3 = H，则R2≠H，R4≠H; 如果R4 = H，那么R2≠H，R3≠H，它们作为抗生素的用途和合成方法。

    COMPOUNDS FOR USE IN THE TREATMENT OF BACTERIAL INFECTION
    5.
    发明申请
    COMPOUNDS FOR USE IN THE TREATMENT OF BACTERIAL INFECTION 有权
    用于治疗细菌感染的化合物

    公开(公告)号：US20140038914A1

    公开(公告)日：2014-02-06

    申请号：US13980364

    申请日：2012-01-17

    申请人： Karine Auclair ,  Kenward Vong

    发明人： Karine Auclair ,  Kenward Vong

    IPC分类号： C07H15/224 ,  A61K31/7036 ,  A61K45/06 ,  C07H15/23

    CPC分类号： C07H15/224 ,  A61K31/7036 ,  A61K45/06 ,  A61P31/04 ,  C07H15/23 ,  C07H15/234 ,  A61K2300/00

    摘要： This invention relates to a compound of Formula 1A: or a pharmaceutically acceptable salt thereof; wherein R1 to R4, R7, R9 to R12 and Y are as defined herein. The invention further relates to pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof; and method of using same for reducing or reversing bacterial resistance to at least one aminoglycoside antibiotic.

    摘要翻译： 本发明涉及式1A化合物或其药学上可接受的盐; 其中R 1至R 4，R 7，R 9至R 12和Y如本文所定义。 本发明还涉及包含所述化合物或其药学上可接受的盐的药物组合物; 以及其用于减少或逆转对至少一种氨基糖苷类抗生素的细菌耐药性的方法。

    TREATMENT OF BACTERIAL INFECTIOUS DISEASES
    6.
    发明申请
    TREATMENT OF BACTERIAL INFECTIOUS DISEASES 有权
    治疗细菌感染性疾病

    公开(公告)号：US20130165397A1

    公开(公告)日：2013-06-27

    申请号：US13820258

    申请日：2011-09-12

    申请人： Erik Boettger ,  Andrea Vasella

    发明人： Erik Boettger ,  Andrea Vasella

    IPC分类号： A61K31/7036 ,  C07H15/224

    CPC分类号： A61K31/70 ,  A61K31/7036 ,  C07H15/224 ,  C07H17/04 ,  Y02A50/402 ,  Y02A50/481

    摘要： The present invention relates to a novel pharmacological treatment of bacterial infectious diseases in humans. Specifically the invention relates to the use of apramycin of formula (I) or apramycin derivatives to treat bacterial infectious diseases in humans. It is demonstrated that apramycin surprisingly does not have the expected high level of toxicity observed with related aminoglycoside antibiotics but actually is even significantly less toxic than compounds already used in human medicine such as gentamicin.

    摘要翻译： 本发明涉及人类细菌感染性疾病的新型药理学治疗。 具体地说，本发明涉及式（I）的安普霉素或安普霉素衍生物用于治疗人类细菌感染性疾病的用途。 据证实，阿帕霉素令人惊讶地没有预期的相关氨基糖苷类抗生素观察到的高水平的毒性，但实际上甚至比已用于人类药物（如庆大霉素）的化合物显着降低毒性。

    SYNTHESIS OF NOVEL NEAMINE DERIVATIVES AND USE THEREOF AS ANTIBACTERIAL AGENTS
    7.
    发明申请
    SYNTHESIS OF NOVEL NEAMINE DERIVATIVES AND USE THEREOF AS ANTIBACTERIAL AGENTS 有权
    新型胺衍生物的合成及其作为抗菌剂的用途

    公开(公告)号：US20100311680A1

    公开(公告)日：2010-12-09

    申请号：US12735511

    申请日：2009-01-22

    申请人： Jean-Luc Decout ,  Isabelle Baussane ,  Jerome Desire ,  Jean-Marc Paris

    发明人： Jean-Luc Decout ,  Isabelle Baussane ,  Jerome Desire ,  Jean-Marc Paris

    IPC分类号： A61K31/7036 ,  C07H15/224 ,  A61P31/00

    CPC分类号： C07H15/224

    摘要： This invention concerns compounds with the formula: in which: R1=OH or NH2; OR2, OR3, OR4 and OR5 are alcohol, ether, ester, carbonate, carbamate, sulphonate or sulphamate groups; and if R5=H if R2=R3=R4, then R2, R3 and R4≠H; if R2=H, then R3≠H and R4≠H; if R3=H, then R2≠H and R4≠H; if R4=H, then R2≠H and R3≠H; if R5≠H if R2=H, then R3≠H and R4≠H; if R3=H, then R2≠H and R4≠H; if R4=H, then R2≠H and R3≠H, their use as antibiotic agents and the process for synthesising them.

    摘要翻译： 本发明涉及具有下式的化合物：其中：R1 = OH或NH2; OR2，OR3，OR4和OR5是醇，醚，酯，碳酸酯，氨基甲酸酯，磺酸酯或氨基磺酸酯基团; 如果R 2 = R 3 = R 4，如果R 5 = H，则R 2，R 3和R 4≠H; 如果R2 = H，则R3≠H，R4≠H; 如果R3 = H，则R2≠H，R4≠H; 如果R4 = H，则R2≠H，R3≠H; 如果R2 = H，则R5≠H，则R3≠H，R4≠H; 如果R3 = H，则R2≠H，R4≠H; 如果R4 = H，那么R2≠H，R3≠H，它们作为抗生素的用途和合成方法。

    Processes for the preparation of spectinomycin analogs, novel products and intermediates therein
    9.
    发明授权
    Processes for the preparation of spectinomycin analogs, novel products and intermediates therein 失效
    制备壮观霉素类似物，新产品及其中间体的方法

    公开(公告)号：US4698436A

    公开(公告)日：1987-10-06

    申请号：US588177

    申请日：1984-03-12

    申请人： David R. White ,  Clarence J. Maring

    发明人： David R. White ,  Clarence J. Maring

    IPC分类号： C07H15/224 ,  C07D323/04

    CPC分类号： C07H15/224

    摘要： The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.

    摘要翻译： 本发明涉及制备各种壮观霉素类似物及其生物可接受的盐的新方法。 此外，本发明涉及其中的新型中间体和新型产物。 新产品是壮观霉素类似物，其可用于与壮观霉素相同的生物学目的。 本发明的方法提供了新颖的中间体，其是多功能和高反应性的环外酮。