公开(公告)号：US20070155798A1

公开(公告)日：2007-07-05

申请号：US10596412

申请日：2004-12-17

申请人： Jae Rhee ,  Weon Im ,  Chong Cho ,  Sung Choi ,  Tae Lee

发明人： Jae Rhee ,  Weon Im ,  Chong Cho ,  Sung Choi ,  Tae Lee

IPC分类号： A61K31/4439 ,  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. Data supplied from the esp@cenet database—Worldwide

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相对于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菌，耐结核菌如结核分枝杆菌 和鸟分枝杆菌。 因此，包含恶唑烷酮的组合​​物用于抗生素中。 从esp @ cenet database-Worldwide提供的数据