Cephem compounds having broad antibacterial spectrum
    33.
    发明授权
    Cephem compounds having broad antibacterial spectrum 失效
    头孢烯化合物具有广泛的抗菌谱

    公开(公告)号:US07696354B2

    公开(公告)日:2010-04-13

    申请号:US12100307

    申请日:2008-04-09

    IPC分类号: C07D277/38

    摘要: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.

    摘要翻译: 下式的化合物:其中T是S,SO或O; X是卤素,CN,任选被低级烷基,低级烷基,低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基(其中取代基是 任选取代的单低级烷基,任选取代的低级亚烷基或任选取代的低级亚烷基); Z +是任选取代的,阳离子和含N原子的杂环基团),酯,氨基保护的化合物,其中氨基与噻唑环 在7-位,或其药学上可接受的盐或溶剂化物。

    Novel antibacterial agents
    36.
    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。

    Broad -spectrum cephem compounds
    37.
    发明申请
    Broad -spectrum cephem compounds 失效
    广谱光谱化合物

    公开(公告)号:US20050153950A1

    公开(公告)日:2005-07-14

    申请号:US10507502

    申请日:2003-03-18

    摘要: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.

    摘要翻译: 下式的化合物:其中T是S,SO或O; X是卤素,CN,任选被低级烷基,低级烷基,低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基(其中取代基是 任选取代的单低级烷基,任选取代的低级亚烷基或任选取代的低级亚烷基); Z +是任选取代的阳离子和含N原子的杂环基),酯,氨基保护的化合物 其中氨基与7-位的噻唑环或其药学上可接受的盐或溶剂化物的键合。

    Cephem compound having catechol group
    40.
    发明授权
    Cephem compound having catechol group 有权
    具有儿茶酚基的头孢烯化合物

    公开(公告)号:US09145425B2

    公开(公告)日:2015-09-29

    申请号:US13639412

    申请日:2011-04-04

    摘要: This invention provides Cephem compounds having the formula: or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, a pharmaceutical composition thereof, and a method for treating a bacterial infectious disease with the compound, the ester, the protected compound, the salt, or the solvate thereof, wherein the symbols in the formula are defined in the specification. The compounds exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and/or Gram positive bacteria, preferably beta-lactamase producing Gram negative bacteria, more preferably, multi-drug resistant microbials, in particular, Class B type metallo-beta-lactamase producing Gram negative bacteria, and still preferably extended-spectrum beta-lactamase (ESBL) producing bacteria. The compounds most preferably do not exhibit cross-resistance against known Cephem drugs or Carbapenem drugs.

    摘要翻译: 本发明提供具有下式的Cephem化合物:或酯,7-侧链上的环上的氨基上的被保护的化合物,其药学上可接受的盐或溶剂合物,其药物组合物和 化合物,酯,受保护化合物,盐或其溶剂化物的细菌感染性疾病,其中式中的符号在说明书中定义。 该化合物对各种细菌(包括革兰氏阴性细菌和/或革兰氏阳性细菌,优选β-内酰胺酶产生革兰氏阴性细菌,更优选多药耐药性微生物,特别是B类金属β- 产生革兰氏阴性细菌的内酰胺酶,更优选延长的β-内酰胺酶(ESBL)产生细菌。 该化合物最优选不表现出对已知的Cephem药物或碳青霉烯类药物的抗药性。