BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    111.
    发明申请
    BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS 有权
    联苯化合物有效作为MUSCARINIC受体拮抗剂

    公开(公告)号:US20110319625A1

    公开(公告)日:2011-12-29

    申请号:US13226677

    申请日:2011-09-07

    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ari, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

    Abstract translation: 本发明提供了式I的化合物:其中a,b,c,d,m,n,p,s,t,W,Ari,R1,R2,R3,R4,R6,R7和R8如 规范。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物,用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

    BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    115.
    发明申请
    BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS 有权
    联苯化合物有效作为MUSCARINIC受体拮抗剂

    公开(公告)号:US20100063096A1

    公开(公告)日:2010-03-11

    申请号:US12616957

    申请日:2009-11-12

    CPC classification number: C07D211/46 C07D405/12

    Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

    Abstract translation: 本发明提供式I化合物:其中a,b,c,p,W,A,X 1,R 1,R 2,R 3,R 6,R 7和R 8如说明书中所定义。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物,用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

    Novel antibacterial agents
    120.
    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

    CPC classification number: C07D477/12 C07D499/32 C07D499/44 C07D501/56

    Abstract: 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.

    Abstract translation: 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。

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