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    Phosphonomethoxy carbocyclic nucleosides and nucleotides
    5.
    发明授权
    Phosphonomethoxy carbocyclic nucleosides and nucleotides 失效
    膦基甲氧基碳环核苷酸和核苷酸

    公开(公告)号：US5744600A

    公开(公告)日：1998-04-28

    申请号：US357561

    申请日：1994-12-16

    申请人： Muzammil M. Mansuri ,  John C. Martin ,  Thomas W. Hudyma ,  Joanne J. Bronson ,  Louis M. Ferrara

    发明人： Muzammil M. Mansuri ,  John C. Martin ,  Thomas W. Hudyma ,  Joanne J. Bronson ,  Louis M. Ferrara

    IPC分类号： C07F9/6512 ,  A61K31/675 ,  C07F9/6561 ,  C07D473/18 ,  C07D473/34

    CPC分类号： C07F9/65121

    摘要： A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino; R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; and B is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio; and the pharmaceutically acceptable acid addition, metal, and amine salts thereof. The compositions of the invention are useful for, among other things, antiviral agents.

    摘要翻译： 式I或式II的化合物其中R 1和R 2独立地是氢，羟基，氯，氟，溴或具有1至5个碳原子并且选自具有烃的酰氧基的有机取代基 1至4个碳原子的烷氧基，烷硫基，氨基，烷基氨基和二烷基氨基; R3和R4独立地是氢，或具有1至12个碳原子并且选自烷基，烯基，芳基和芳烷基的有机膦酸酯取代基; 并且B是选自嘧啶，嘌呤，三嗪，脱氮嘌呤和三唑的杂环基，其通过环氮原子连接，任选被1-3个选自羟基，巯基，氨基，肼基的取代基取代 ，氟，氯，溴，碘，C 1至C 3烷基，C 2 -C 3烯基，C 2 -C 3卤代烯基，C 1 -C 3烷氧基和C 1 -C 3烷硫基; 及其药学上可接受的酸加成盐，金属盐和胺盐。 本发明的组合物尤其可用于抗病毒剂。

    Cephalosporin derivatives
    6.
    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。