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1. 发明授权

EP2009012B1 NOVEL COMPOUND HAVING HETEROCYCLIC RING 有权
标题翻译： WITH杂环新连接
公开(公告)号：EP2009012B1
公开(公告)日：2014-06-25
申请号：EP07740496.0
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi Co., Ltd.
发明人： SUZUKI, Hideyuki , HIZATATE, Shoji , UTSUNOMIYA, Iwao , SHUDO, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55

2. 发明公开

EP2208729A1 OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING 审中-公开
标题翻译： OXAZOLIDINONDERIVAT MIT 7-GLIEDRIGEM HETERORING
公开(公告)号：EP2208729A1
公开(公告)日：2010-07-21
申请号：EP08836063.1
申请日：2008-10-01
申请人： Research Foundation Itsuu Laboratory , Shionogi&Co., Ltd.
发明人： SUZUKI, Hideyuki , UTSUNOMIYA, Iwao , SHUDO, Koichi , IWAKI, Tsutomu , YASUKATA, Tatsuro
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D471/14 , C07D487/04
CPC分类号： C07D413/14 , C07D271/02 , C07D413/10 , C07D471/14 , C07D487/04 , Y02P20/55
摘要： 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 SO 2 ,
wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring;
X 1 is a single bond, or a heteroatom-containing group selected from the group consisting of -O-, -S-, -NR 2 -, -CO-, -CS-, -CONR 3 -, -NR 4 CO-, -SO 2 NR 5 -, and -NR 6 SO 2 -, wherein R 2 , R 3 , R 4 , R 5 and R 6 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
R 1 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.
摘要翻译：本发明提供了式（I）的新型恶唑烷酮衍生物：其中环A为（A-1）含有三个N原子的7-元单环杂环; （A-2）含有两个N原子和一个O原子的7-元单环杂环; 或（A-3）含有两个N原子和一个S原子，SO或SO 2的7-元单环杂环，其中所述单环杂环任选被取代，任选地不饱和并任选地与另一个环稠合; X 1是单键或选自-O - ， - S - ， - NR 2 - ， - CO - ， - CS - ， - CONR 3 - ， - NR 4 CO- ，-SO 2 NR 5 - 和-NR 6 SO 2 - ，其中R 2，R 3，R 4，R 5和R 6独立地为氢或低级烷基，或低级亚烷基或低级亚烯基，各自任意地被所述杂原子包含组; 环B是任选取代的碳环或任选取代的杂环; R 1为氢的化合物，或可用作抗菌剂的恶唑烷酮抗微生物剂，其药学上可接受的盐和溶剂合物中能够结合恶唑烷酮环的5-位的有机残基。

3. 发明公开

EP2009012A1 NOVEL COMPOUND HAVING HETEROCYCLIC RING 有权
标题翻译： NEER VERBINDUNG MIT HETEROCYCLISCHEM RING
公开(公告)号：EP2009012A1
公开(公告)日：2008-12-31
申请号：EP07740496.0
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi Co., Ltd.
发明人： SUZUKI, Hideyuki , HIZATATE, Shoji , UTSUNOMIYA, Iwao , SHUDO, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55
摘要： The invention provides a novel oxazolidinone derivative represented by the formula (I):

wherein
Ring A is optionally substituted or fused and represents
(A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom;
X 1 is a single bond, -O-, -S-, -NR 2 -, -CO-, -CS-, - CONR 3 -, -NR 4 CO-, -SO 2 NR 5 -, and -NR 6 SO 2 - (wherein R 2 - R 6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene;
Ring B is optionally substituted carbocycle or optionally substituted heterocycle;
R 1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent,
and an antibacterial agent containing the same.
摘要翻译：本发明提供由式（I）表示的新型恶唑烷酮衍生物：其中环A任选被取代或稠合并且代表（A-1）含有至少三个N原子的至少七元单环杂环; （A-2）至少含有至少两个N原子和至少一个O原子的6元单环杂环; 或（A-3）至少含有至少两个N原子和至少一个S原子的7元单环杂环; X 1是单键，-O - ， - S-，-NR 2 - ， - CO - ， - CS-， - CONR 3 - ， - NR 4 CO - ， - SO 2 NR 5 - 和-NR 6 SO 2 - （其中R 2 -R 6独立地是氢或低级烷基）或其中一个前述基团可以介导的低级亚烷基或低级亚烯基; 环B是任选取代的碳环或任选取代的杂环; R 1为氢，或能够与恶唑烷酮抗微生物剂中的恶唑烷酮环的5位结合的有机残基，以及含有该残基的抗菌剂。

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