Novel antibacterial agents
    1.
    发明申请
    Novel antibacterial agents 审中-公开
    新型抗菌剂

    公开(公告)号:US20090111737A1

    公开(公告)日:2009-04-30

    申请号:US12082666

    申请日:2008-04-11

    IPC分类号: A61K38/14 C07K7/00 A61P43/00

    摘要: This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

    摘要翻译: 本发明涉及作为抗菌剂的新型多结合化合物(试剂)。 本发明的多相结合化合物包含2-10个配体,其通过连接体或连接体共价连接,其中所述各单体(即,未连接)状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地,本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体,其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域,转肽酶,转肽酶的底物, β-内酰胺酶,pencillinase酶,头孢菌素酶,转糖基酶或转糖基酶酶底物; 优选地,配体选自β-内酰胺或糖肽类抗菌剂。

    Novel antibacterial agents
    7.
    发明申请
    Novel antibacterial agents 审中-公开
    新型抗菌剂

    公开(公告)号:US20070196859A1

    公开(公告)日:2007-08-23

    申请号:US11603329

    申请日:2006-11-21

    摘要: This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked ) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, penicillinase enzyme, cephalosporinase enzyme, a transglycosylase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

    摘要翻译: 本发明涉及作为抗菌剂的新型多结合化合物(试剂)。 本发明的多相结合化合物包含2-10个配体,其通过连接体或连接体共价连接,其中所述各单体(即,未连接)状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地,本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体,其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域,转肽酶,转肽酶的底物, β-内酰胺酶,青霉素酶,头孢菌素酶,转糖基酶或转糖基酶酶底物; 优选地,配体选自β-内酰胺或糖肽类抗菌剂。