Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    11.
    发明授权
    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
    碳青霉烯抗菌化合物,含有这些化合物的组合物和治疗方法

    公开(公告)号:US06277843B1

    公开(公告)日:2001-08-21

    申请号:US09421078

    申请日:1999-10-19

    IPC分类号: C07D47714

    摘要: The present invention relates to carbapenem antibacterial agents of the formula I: as well as salts and hydrates thereof. Pharmaceutical compositions and methods of treatment are also included wherein X is present or absent, when present, represents a members selected from the group consisting of: CH2, C(R)2, C═CR2, O, S(O)x, with x equal to 0, 1 or 2; C(O), C(O)O, OC(O) and NR—.

    摘要翻译: 本发明涉及式I的碳青霉烯类抗生素及其盐和水合物。 还包括药物组合物和治疗方法,其中X存在或不存在,当存在时,表示选自以下的成员:CH 2,C(R)2,C = CR 2,O,S(O)x,与 x等于0,1或2; C(O),C(O)O,OC(O)和NR-。

    Penem antibacterial compounds, compositions and methods of treatment
    12.
    发明授权
    Penem antibacterial compounds, compositions and methods of treatment 失效
    Penem抗菌化合物,组合物和治疗方法

    公开(公告)号:US06271222B1

    公开(公告)日:2001-08-07

    申请号:US09298223

    申请日:1999-04-23

    申请人: Frank P. Dininno

    发明人: Frank P. Dininno

    IPC分类号: C07D499887

    CPC分类号: C07D499/88

    摘要: The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for anti-MRSA activity replaces the non-releaseable liphophilic side-chains found in 2-aryl and 2-benzothiazolylthio carbapenem compounds. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.

    摘要翻译: 本发明涉及青霉素抗菌剂,其中抗MRSA活性所必需的通过亚甲基接头连接到碳青霉烯核上的可释放的亲脂性芳族侧链替代2-芳基和2芳基中发现的不可释放的亲脂侧链 苯并噻唑基硫代碳青霉烯化合物。 该化合物被包括至少一个阳离子基团的各种取代基进一步取代。化合物由式I表示:还包括药物组合物和使用方法。

    7-Substituted methyl cephalosporins derivatives and analogues thereof
    17.
    发明授权
    7-Substituted methyl cephalosporins derivatives and analogues thereof 失效
    7-取代的甲基头孢菌素衍生物及其类似物

    公开(公告)号:US4296111A

    公开(公告)日:1981-10-20

    申请号:US48551

    申请日:1979-06-14

    IPC分类号: C07D501/00

    CPC分类号: C07D501/00

    摘要: Disclosed are antibiotic 7-(substituted methyl) cephalosporins, derivatives and nuclear analogues thereof; wherein the methyl substituent is, inter alia, hydroxyl, ketonic oxygen, imino nitrogen, amino or thio. Also disclosed are processes for the preparation of such compounds and their pharmaceutically acceptable salt, ester and amide derivatives; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译: 公开了抗生素7-(取代的甲基)头孢菌素,其衍生物和核类似物; 其中甲基取代基尤其是羟基,酮氧,亚氨基氮,氨基或硫代。 还公开了制备这些化合物及其药学上可接受的盐,酯和酰胺衍生物的方法; 包含这些化合物的药物组合物; 和治疗方法,包括当指出抗生素效应时施用这些化合物和组合物。

    Halophenoxy substituted carbapenem antibacterial compounds
    18.
    发明授权
    Halophenoxy substituted carbapenem antibacterial compounds 失效
    卤代苯氧基取代的碳青霉烯类抗菌化合物

    公开(公告)号:US06310055B2

    公开(公告)日:2001-10-30

    申请号:US09311519

    申请日:1999-05-13

    IPC分类号: A61K31407

    CPC分类号: C07D477/14

    摘要: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2 -position with a iodophenoxy linked through a group —Z—CH2—; The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: wherein Z represents trans-ethenediyl or ethynediyl. Pharmaceutical compositions and methods of use are also included.

    摘要翻译: 本发明涉及碳青霉烯类抗菌剂,其中碳青霉烯核在2-位被与通过基团-Z-CH2-基团连接的碘苯氧基取代; 该化合物进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式I表示:其中Z代表反式 - 乙烯二基或乙炔二基。还包括药物组合物和使用方法。

    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    20.
    发明授权
    Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
    碳青霉烯抗菌化合物,含有这些化合物的组合物和治疗方法

    公开(公告)号:US06255300B1

    公开(公告)日:2001-07-03

    申请号:US09455629

    申请日:1999-12-07

    IPC分类号: C07D47714

    CPC分类号: C07D477/14

    摘要: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH2—O— group. The compounds of the invention are represented by formula I: wherein A represent O, S or —CH2— attached at position 3, 4 or 6; Q is selected from the group consisting of: &agr; represents O, S or NRs; &bgr;, &dgr;, &ggr;, &mgr; and &sgr; represent CRt, N or N+Rs, provided that no more than one of &bgr;, &dgr;, &ggr;, &mgr; and &sgr; is N+Rs, balanced by L− or a carboxylate anion. Salts and hydrates thereof are included. The iodo-substituted phenyl ring is further substituted with various substituent groups including at least one cationic group. Pharmaceutical compositions and methods of treatment are also included.

    摘要翻译: 本发明涉及碳青霉烯类抗菌剂,其中碳青霉烯核在2位被碘取代的苯基通过CH2-O-基团连接。 本发明的化合物由式I表示:其中A表示在3,4或6位上连接的O,S或-CH 2; Q选自:α表示O,S或NR; β,δ,γ,μ和σ表示CRt,N或N + Rs,条件是β,δ,γ,μ和σ的不超过一个为N + Rs,由L-或羧酸根阴离子平衡。 包括其盐和水合物。 碘取代的苯环进一步被包括至少一个阳离子基团的各种取代基取代。 还包括药物组合物和治疗方法。