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28 条记录 (耗时 0.047 秒)

    PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-[[(2R,3R)-2-[[[(S)-2-AMINO-3-METHYL-1-OXOBUTYL]AMINO]METHYL]TETRAHYDRO-3-FURANYL]THIO]-6-[(R)-1-HYDROXYETHYL]-4-METHYL-7-OXO-1-AZABICYCLO[3.2.0]HEPT-2-ENE-2-CARBOXYLIC ACID
    16.
    发明授权
    PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-[[(2R,3R)-2-[[[(S)-2-AMINO-3-METHYL-1-OXOBUTYL]AMINO]METHYL]TETRAHYDRO-3-FURANYL]THIO]-6-[(R)-1-HYDROXYETHYL]-4-METHYL-7-OXO-1-AZABICYCLO[3.2.0]HEPT-2-ENE-2-CARBOXYLIC ACID 失效
    （4R，5S，6S）-3 - [[（2R，3R）-2 - [[（S）-2-氨基-3-甲基-1-氧代丁基]氨基]甲基]四氢呋喃的制备中的工艺改进 -3-FURANYL] THIO] -6 - [（R）-1-羟基乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0] HEPT-2-环己基-2-羧酸

    公开(公告)号：US06649756B2

    公开(公告)日：2003-11-18

    申请号：US09901335

    申请日：2001-07-09

    申请人： Tarek Mansour ,  Phaik-Eng Sum ,  Yang-I Lin ,  Zhong Li

    发明人： Tarek Mansour ,  Phaik-Eng Sum ,  Yang-I Lin ,  Zhong Li

    IPC分类号： C07D47720

    CPC分类号： C07D477/20 ,  C07D477/08

    摘要： The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S, 6S)-3-[[2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydro-3-furanyl]thio]-6-[R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid by hydrogenation of 4-nitrobenzyl (4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-3-{[2R,3R)-2-({[(2S)-3-methyl-2-({[4-nitrobenzyl)oxy]carbonyl}amino)butanoyl]amino}methyl)-tetrahydrofuran-3-yl]thio}-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate in a biphasic solvent mixture comprising a water portion and an organic solvent portion, not containing an acid acceptor. The water portion is separated from the organic solvent portion and (4R,5S,6S)-3-[[(2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydro-3-furanyl]thio]-6-[R-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid is isolated from the separated water portion by lyophilization or reverse osmosis.

    摘要翻译： 本发明是用于生产碳青霉烯类抗菌剂（4R，5S，6S）-3 - [[2R，3R）-2 - [[[（S）-2-氨基-3-甲基-1-氧代丁基] 氨基]甲基]四氢-3-呋喃基]硫基] -6- [R）-1-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸 通过氢化（4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-3 - {[2R，3R）-2 - （{[（2S）-3- 甲基-2 - （{[4-硝基苄基）氧基]羰基}氨基）丁酰基]氨基}甲基） - 四氢呋喃-3-基]硫代} -7-氧代-1-氮杂双环[3.2.0]庚-2-烯 -2-羧酸酯在包含水部分和不含酸受体的有机溶剂部分的双相溶剂混合物中。 将水部分与有机溶剂部分分离，和（4R，5S，6S）-3 - [[（2R，3R）-2 - [[[（S）-2-氨基-3-甲基-1-氧代丁基] 氨基]甲基]四氢-3-呋喃基]硫基] -6- [R-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸从 分离的水部分通过冻干或反渗透。

    Tricyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors
    20.
    发明申请
    Tricyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors 审中-公开
    作为D类β-内酰胺酶抑制剂的三环6-亚烷基 - 青霉烯

    公开(公告)号：US20060276446A1

    公开(公告)日：2006-12-07

    申请号：US11444346

    申请日：2006-05-31

    申请人： Tarek Mansour ,  Aranapakam Venkatesan

    发明人： Tarek Mansour ,  Aranapakam Venkatesan

    IPC分类号： A61K31/43 ,  A61K31/424

    CPC分类号： A61K31/424 ,  A61K31/43 ,  Y02A50/473

    摘要： This invention relates to certain tricyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of formula I which are useful for treatment of bacterial infections having class-D enzymes associated therewith: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S or O.

    摘要翻译： 本发明涉及作为D类酶抑制剂的某些三环6-亚烷基半胱氨酸。 β-内酰胺酶水解β-内酰胺抗生素，因此成为细菌耐药的主要原因。 当与β-内酰胺抗生素组合时，本发明的化合物将提供有效治疗以防止威胁生命的细菌感染。 根据本发明，提供了可用于治疗与其相关的D类酶的细菌感染的式I化合物：其中：A和B之一表示氢，另一个表示任选取代的稠合三环杂芳基; X为S或O.