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    • 20. 发明授权
    • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    • 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
    • US06255300B1
    • 2001-07-03
    • US09455629
    • 1999-12-07
    • Frank P. DininnoKevin D. Dykstra
    • Frank P. DininnoKevin D. Dykstra
    • C07D47714
    • C07D477/14
    • 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.
    • 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。