Benzoxazinedione derivatives, method of producing them and uses thereof
    45.
    发明授权
    Benzoxazinedione derivatives, method of producing them and uses thereof 失效
    苯并恶嗪二酮衍生物,其制备方法和用途

    公开(公告)号:US6013647A

    公开(公告)日:2000-01-11

    申请号:US35344

    申请日:1998-03-05

    摘要: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams. In addition, said compounds, as potential prodrug forms for iron chelating agents, are suitable for use against diseases which are caused by a disorder of the iron metabolism. The invention can be employed in pharmaceutical research and in the pharmaceutical industry, and in agriculture.

    摘要翻译: 本发明涉及对应于式I的新的苯并恶嗪二酮衍生物:其中R1 = H或羧基烷基,R2 = H,烷基或苯基,R3代表衍生自氨基酸,二肽和腙的不同酸基或​​其与活性成分例如 抗生素。 化合物可以其盐形式或易裂解的酯的形式存在为游离酸。 根据本发明的化合物构成了杂环保护的邻苯二酚衍生物,并且作为抗革兰氏阴性细菌菌株的铁载体是有效的,特别是对假单胞菌和大肠杆菌和沙门氏菌菌株有效。 以它们与活性成分的缀合物的形式,例如 抗生素(作为“铁载体 - 抗生素共轭物”),它们可以将后者转运到细菌细胞中,并且可以改善或延长其抗菌作用,有时甚至与对其它β-内酰胺酶有抗性的细菌菌株有关。 此外,作为铁螯合剂的潜在前体药物形式的所述化合物适用于针对由铁代谢紊乱引起的疾病。 本发明可用于制药研究,制药工业和农业领域。