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130 条记录 (耗时 0.032 秒)

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

    公开(公告)号：US5734047A

    公开(公告)日：1998-03-31

    申请号：US761738

    申请日：1996-12-05

    申请人： Choung U. Kim ,  Muzammil M. Mansuri ,  Peter F. Misco ,  John A. Wichtowski

    发明人： Choung U. Kim ,  Muzammil M. Mansuri ,  Peter F. Misco ,  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## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

    摘要翻译： 由通式 + TR 表示的新型头孢烯衍生物，其中Ar是任选取代的亲脂性苯基，萘基，苯并噻唑基或吡啶基; R 1表示式（VIII）的基团，其中R 8和R 9各自独立地为氢，C 1 -C 6烷基或（C 1 -C 6）烷氧基羰基，所述C 1 -C 6烷基任选被1-5个羟基或C 1 -C 6 烷氧基 m为0或1; A是任选被1-5个羟基取代的C 2 -C 10烷基; 且R 2和R 3各自独立地为氢或C 1 -C 6烷基。 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。

    Carbapenem antibiotics
    5.
    发明授权
    Carbapenem antibiotics 失效

    公开(公告)号：US4665170A

    公开(公告)日：1987-05-12

    申请号：US822576

    申请日：1986-01-27

    申请人： Choung U. Kim ,  Peter F. Misco, Jr.

    发明人： Choung U. Kim ,  Peter F. Misco, Jr.

    IPC分类号： C07D295/088 ,  C07D477/20 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D295/088 ,  C07D477/20

    摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

    Carbapenem antibiotics
    6.
    发明授权
    Carbapenem antibiotics 失效
    卡巴布本抗生素

    公开(公告)号：US4640799A

    公开(公告)日：1987-02-03

    申请号：US762735

    申请日：1985-08-05

    申请人： Choung U. Kim ,  Peter F. Misco, Jr.

    发明人： Choung U. Kim ,  Peter F. Misco, Jr.

    IPC分类号： C07D295/088 ,  C07D477/20 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D295/088 ,  C07D477/20

    摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

    摘要翻译： 公开了新的碳青霉烯衍生物，其特征在于具有式“IMAGE”的2-取代基，其中A表示任选被一个或多个C 1 -C 4烷基取代的亚环戊基，亚环己基或C 2 -C 6亚烷基; R 5表示（a）任选取代的脂族，脂环族，脂环族 - 脂族，芳基，芳脂族，杂芳基，杂脂肪族基，杂环基或杂环基 - 脂族基团或（b）二价亚苯基或C1-C4亚烷基， 环以形成桥连多环基团; 并且表示季铵化的含氮非芳族杂环。 这些衍生物可用作有效的抗菌剂。

    Thymidine derivatives and therapeutic method of use
    8.
    发明授权
    Thymidine derivatives and therapeutic method of use 失效
    胸苷衍生物及其治疗方法

    公开(公告)号：US5306722A

    公开(公告)日：1994-04-26

    申请号：US939232

    申请日：1992-09-02

    申请人： Choung U. Kim ,  Bing Y. Luh ,  Peter F. Misco

    发明人： Choung U. Kim ,  Bing Y. Luh ,  Peter F. Misco

    IPC分类号： A61K31/505 ,  A61P31/12 ,  C07D405/04 ,  C07H19/06 ,  C07D403/04

    CPC分类号： C07H19/06

    摘要： Thymidine kinase inhibitor of formula I ##STR1## in which R is C.sub.1-6 alkyl or AR(CH.sub.2).sub.n --, wherein Ar represents phenyl optionally substituted with one to five same or different halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; and n equals one to six.A further aspect of the present invention provides a method of inhibiting viral thymidine kinase. Yet another aspect of the invention relates to treating herpes simplex viral infections in mammals. Yet another aspect of the invention provides a pharmaceutical formulation.

    摘要翻译： 式I的胸苷激酶抑制剂（*化学结构*）I其中R是C 1-6烷基或AR（CH 2）n - ，其中Ar表示任选被1至5个相同或不同的卤素，C 1-6烷基或C 1 -C 6烷基取代的苯基， 6烷氧基; n等于1到6。 本发明的另一方面提供了抑制病毒胸苷激酶的方法。 本发明的另一方面涉及治疗哺乳动物中的单纯疱疹病毒感染。 本发明的另一方面提供一种药物制剂。