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    Oxazolidinone derivatives
    1.
    发明授权
    Oxazolidinone derivatives 有权
    恶唑烷酮衍生物

    公开(公告)号：US09163043B2

    公开(公告)日：2015-10-20

    申请号：US13863216

    申请日：2013-04-15

    申请人： DONG-A ST CO., LTD.

    发明人： Jae Keol Rhee ,  Weon Bin Im ,  Chong Hwan Cho ,  Sung Hak Choi ,  Tae Ho Lee

    IPC分类号： C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07F9/6558 ,  C07D417/14 ,  C07F9/653

    CPC分类号： A61K31/4439 ,  A61K31/675 ,  C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07F9/653 ,  C07F9/65583

    摘要： The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

    摘要翻译： 本发明涉及恶唑烷酮的新衍生物，其方法和药物组合物，其包含用于抗生素的衍生物。 本发明的恶唑烷酮衍生物显示出对广谱细菌的抑制活性和较低的毒性。 通过使具有羟基的化合物与氨基酸或磷酸酯反应制备的前药在对水的溶解性方面具有优异的效果。 此外，本发明的衍生物可以对各种人和动物病原体（包括葡萄球菌，肠球菌和链球菌）等革兰阳性菌，拟杆菌和梭菌等厌氧微生物和结核分枝杆菌等耐酸微生物产生有效的抗菌活性 和鸟分枝杆菌。 因此，包含恶唑烷酮的组合​​物用于抗生素中。

    NOVEL OXAZOLIDINONE DERIVATIVES
    2.
    发明申请
    NOVEL OXAZOLIDINONE DERIVATIVES 有权
    新型氧杂环丁酮衍生物

    公开(公告)号：US20130281492A1

    公开(公告)日：2013-10-24

    申请号：US13863216

    申请日：2013-04-15

    申请人： DONG-A ST CO., LTD.

    发明人： Jae Keol Rhee ,  Weon Bin Im ,  Chong Hwan Cho ,  Sung Hak Choi ,  Tae Ho Lee

    IPC分类号： C07D413/14

    CPC分类号： A61K31/4439 ,  A61K31/675 ,  C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07F9/653 ,  C07F9/65583

    摘要： The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

    摘要翻译： 本发明涉及恶唑烷酮的新衍生物，其方法和药物组合物，其包含用于抗生素的衍生物。 本发明的恶唑烷酮衍生物显示出对广谱细菌的抑制活性和较低的毒性。 通过使具有羟基的化合物与氨基酸或磷酸酯反应制备的前药在对水的溶解性方面具有优异的效果。 此外，本发明的衍生物可以对各种人和动物病原体（包括葡萄球菌，肠球菌和链球菌）等革兰阳性菌，拟杆菌和梭菌等厌氧微生物和结核分枝杆菌等耐酸微生物产生有效的抗菌活性 和鸟分枝杆菌。 因此，包含恶唑烷酮的组合​​物用于抗生素中。