申请人:Research Foundation Itsuu Laboratory
公开号:EP2208729A1
公开(公告)日:2010-07-21
The present invention provides a novel oxazolidinone derivative of the formula (I):
wherein
Ring A is
(A-1) a 7-membered monocyclic heterocycle containing three N atoms;
(A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or
(A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO2,
wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring;
X1 is a single bond, or a heteroatom-containing group selected from the group consisting of -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5-, and -NR6SO2-, wherein R2, R3, R4, R5 and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom-containing group;
Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and
R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents,
pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
本发明提供了一种式 (I) 的新型噁唑烷酮衍生物:
其中
环 A 是
(A-1) 包含三个 N 原子的 7 元单环杂环;
(A-2) 含两个 N 原子和一个 O 原子的 7 元单环杂环;或
(A-3) 含两个 N 原子和一个 S 原子、SO 或 SO2 的 7 元单环杂环、
其中所述单环杂环可选被取代、可选不饱和、可选与另一个环融合;
X1 是单键,或选自以下组成的含杂原子基团:-O-、-S-、-NR2-、-CO-、-CS-、-CONR3-、-NR4CO-、-SO2NR5- 和 -NR6SO2-,其中 R2、R3、R4、R5 和 R6 独立地为氢或低级烷基,或低级亚烷基或低级亚烯基,各自任选被所述含杂原子基团打断;
环 B 是任选取代的碳环或任选取代的杂环;以及
R1 是氢,或能够与噁唑烷酮抗菌剂中噁唑烷酮环的 5 位结合的有机残基、
可用作抗菌剂的其药学上可接受的盐和溶剂。