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    Bis quaternary MRSA cephem derivatives
    1.
    发明授权
    Bis quaternary MRSA cephem derivatives 失效
    双季MRSA头孢烯衍生物

    公开(公告)号：US06265394B1

    公开(公告)日：2001-07-24

    申请号：US09366854

    申请日：1999-08-04

    申请人： Roman Z. Sterzycki ,  Oak K. Kim ,  Yasutsugu Ueda ,  Stanley V. D'Andrea ,  Dane M. Springer

    发明人： Roman Z. Sterzycki ,  Oak K. Kim ,  Yasutsugu Ueda ,  Stanley V. D'Andrea ,  Dane M. Springer

    IPC分类号： A61K31545

    CPC分类号： C07D501/00

    摘要： Provided by the present invention are cephem derivatives represented by the general formula wherein Ar is an optionally substituted lipophilic phenyl, naphthyl or pyridyl group; L1 and L2 are (C1-C6)alkylene optionally substituted with hydroxy or oxo and/or optionally interrupted with a vinylene group, S, O, aryl, heteroaryl, in which R1 is H or (C1-C6)alkyl; A is CO2H, PO3H, SO3H, tetrazolyl or x′{circle around (−)} is a pharmaceutically acceptable anion; and Q is an quaternized nitrogen group. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

    摘要翻译： 通过本发明提供的是由通式化合物Ar表示的头孢烯衍生物是任选取代的亲脂性苯基，萘基或吡啶基; L 1和L 2是任选被羟基或氧代取代的（C 1 -C 6）亚烷基和/或任选地被其中R 1是H或（C 1 -C 6）烷基的亚乙烯基，S，O，芳基，杂芳基， A是CO 2 H，PO 3 H，SO 3 H，四唑基orx'（（ - ）周围）是药学上可接受的阴离子; Q为季铵化氮。 衍生物是革兰氏阳性抗菌剂，特别适用于治疗耐甲氧西林金黄色葡萄球菌引起的疾病。

    Substituted 4-thio pyridones
    2.
    发明授权
    Substituted 4-thio pyridones 失效
    取代的4-硫代吡啶酮

    公开(公告)号：US5668290A

    公开(公告)日：1997-09-16

    申请号：US697384

    申请日：1996-08-23

    申请人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Yu Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    发明人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Yu Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    IPC分类号： C07D501/00 ,  C07D501/36 ,  C07D213/44

    CPC分类号： C07D501/00

    摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).

    摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团：其中Ar是亲脂性任选取代的苯基，萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基，其中R9和R10各自独立地为氢或C1-C6烷基， 所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断，并且R 2和R 3各自独立地为氢，烷基或氨基烷基为革兰氏阳性抗菌剂，特别可用于治疗由甲氧西林抗性引起的疾病 金黄色葡萄球菌（以下也称为MRSA或耐甲氧西林金黄色葡萄球菌）。

    Cephalosporin derviatives
    3.
    发明授权
    Cephalosporin derviatives 失效
    头孢菌素衍生物

    公开(公告)号：US5620969A

    公开(公告)日：1997-04-15

    申请号：US427778

    申请日：1995-04-25

    申请人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Y. Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    发明人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Y. Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    IPC分类号： C07D501/00 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).

    摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团：其中Ar是亲脂性任选取代的苯基，萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基，其中R9和R10各自独立地为氢或C1-C6烷基， 所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断，并且R 2和R 3各自独立地为氢，烷基或氨基烷基为革兰氏阳性抗菌剂，特别可用于治疗由甲氧西林抗性引起的疾病 金黄色葡萄球菌（以下也称为MRSA或耐甲氧西林金黄色葡萄球菌）。