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    Carbapenem antibacterials with gram-negative activity and processes for their preparation
    1.
    发明授权
    Carbapenem antibacterials with gram-negative activity and processes for their preparation 有权
    具有革兰氏阴性活性的碳青霉烯类抗生素及其制备方法

    公开(公告)号：US08557979B2

    公开(公告)日：2013-10-15

    申请号：US13560169

    申请日：2012-07-27

    申请人： Woo-Baeg Choi ,  Ewa Kowalik

    发明人： Woo-Baeg Choi ,  Ewa Kowalik

    IPC分类号： C07D487/00

    CPC分类号： C07D477/14 ,  A61K31/397 ,  A61K45/06 ,  Y02P20/55 ,  A61K2300/00

    摘要： The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    摘要翻译： 本发明提供了用于治疗细菌感染的β-甲基碳青霉烯化合物和药物组合物，以及使用这些化合物和/或组合物治疗这种感染的方法。 本发明包括将有效量的碳青霉烯化合物或其盐和/或前药给予需要这种治疗的宿主。 本发明也在合成有机化学领域，并且具体提供了可用作抗菌剂的改进的β-甲基碳青霉烯合成方法。

    Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
    3.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane 有权
    2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号：US20060276492A1

    公开(公告)日：2006-12-07

    申请号：US11390861

    申请日：2006-03-28

    申请人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    发明人： Dennis Liotta ,  Raymond Schinazi ,  Woo-Baeg Choi

    IPC分类号： A61K31/513 ,  C07D409/04

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。

    2'-deoxy-L-nucleosides
    4.
    发明申请
    2'-deoxy-L-nucleosides 审中-公开
    2'-脱氧-L-核苷

    公开(公告)号：US20050090660A1

    公开(公告)日：2005-04-28

    申请号：US10996875

    申请日：2004-11-23

    申请人： Kyoichi Watanabe ,  Woo-Baeg Choi

    发明人： Kyoichi Watanabe ,  Woo-Baeg Choi

    IPC分类号： C07H19/067 ,  C07F7/18 ,  C07H1/06 ,  C07H19/00 ,  C07H19/06 ,  C07H19/073 ,  C07H19/09 ,  C07H19/16 ,  C07H19/167 ,  C07H19/173 ,  C07H19/19 ,  C12N15/10 ,  C07H19/048 ,  C07H19/22

    CPC分类号： C07H19/06 ,  C07H1/06 ,  C07H19/16 ,  C12N15/1003

    摘要： This invention provides processes for the preparation of compounds having the structure: wherein X and Y are same or different, and H, OH, OR, SH, SR, NH2, NHR′, or NR′R″ Z is H, F, Cl, Br, I, CN, or NH2. R is hydrogen, halogen, lower alkyl of C1-C6 or aralkyl, NO2, NH2, NHR′, NR′R″, OH, OR, SH, SR, CN, CONH2, CSNH2, CO2H, CO2R′, CH2CO2H, CH2CO2R′, CH═CHR, CH2CH═CHR, or C═CR. R′ and R″ are same or different, and lower alkyl of C1-C6. R13 is hydrogen, alkyl, acyl, phosphate (monophosphate, diphosphate, triphosphate, or stabilized phosphate) or silyl; and

    摘要翻译： 本发明提供了具有以下结构的化合物的制备方法：其中X和Y相同或不同，且H，OH，OR，SH，SR，NH 2，NHR'或NR'R “Z是H，F，Cl，Br，I，CN或NH 2。 R是氢，卤素，C 1 -C 6的低级烷基或芳烷基，NO 2，NH 2， ，NHR'，NR'R“，OH，OR，SH，SR，CN，CONH 2，CSNH 2，CO 2 H ，CO 2 R 2，CH 2 CO 2 H，CH 2 CO 2，/ SUB R'，CH-CHR，CH 2 CH-CHR或C-CR。 R'和R“相同或不同，C 1 -C 6低级烷基。 R 13是氢，烷基，酰基，磷酸酯（单磷酸酯，二磷酸酯，三磷酸酯或稳定的磷酸酯）或甲硅烷基; “img id =”custom-character-00001“he =”2.56mm“wi =”46.20mm“file =”US20050090660A1-20050428-P00999.TIF“alt =”在提交时丢失或难以辨认“img-content =” 字符“img-format =”tif“/>

    CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION
    7.
    发明申请
    CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION 有权
    具有消极活性的卡巴宁抗菌素及其制备方法

    公开(公告)号：US20100160284A1

    公开(公告)日：2010-06-24

    申请号：US12705716

    申请日：2010-02-15

    申请人： Woo-Baeg Choi ,  Ewa Kowalk

    发明人： Woo-Baeg Choi ,  Ewa Kowalk

    IPC分类号： A61K31/397 ,  C07D477/14 ,  A61P31/04

    CPC分类号： C07D477/14 ,  A61K31/397 ,  A61K45/06 ,  Y02P20/55 ,  A61K2300/00

    摘要： The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

    摘要翻译： 本发明提供了用于治疗细菌感染的碳青霉烯类化合物和药物组合物，以及使用这些化合物和/或组合物治疗这种感染的方法。 本发明包括将有效量的碳青霉烯化合物或其盐和/或前药给予需要这种治疗的宿主。 本发明也在合成有机化学领域中，并且具体提供了可用作抗菌剂的改进的碳青霉烯类甲基化合物的合成方法。

    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane
    9.
    发明申请
    Antiviral activity and resolution of 2-hydroxymethyl-5(5-fluorocytosin-1-yl)-1,3-oxathiolane 审中-公开
    2-羟甲基-5（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷的抗病毒活性和拆分

    公开(公告)号：US20090048190A1

    公开(公告)日：2009-02-19

    申请号：US12150964

    申请日：2008-05-02

    申请人： Dennis C. Liotta ,  Raymond F. Schinazi ,  Woo-Baeg Choi

    发明人： Dennis C. Liotta ,  Raymond F. Schinazi ,  Woo-Baeg Choi

    IPC分类号： A61K31/506 ,  A61K31/7052 ,  A61P31/12

    CPC分类号： C07D327/04 ,  A61K31/513 ,  C07D405/04 ,  C07D411/04 ,  C07H19/06 ,  C07H19/10 ,  Y10S514/885

    摘要： A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

    摘要翻译： 公开了用于治疗人体中HIV和HBV感染的方法和组合物，其包括给予有效量的2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷，其药学上可接受的衍生物 ，包括5'或N4烷基化或酰化衍生物或其药学上可接受的盐在药学上可接受的载体中。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。