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    • 2. 发明申请
    • OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING
    • 具有7层杂环的氧杂环丁酮衍生物
    • US20100256355A1
    • 2010-10-07
    • US12733954
    • 2008-10-01
    • Hideyuki SuzukiIwao UtsunomiyaKoichi ShudoTsutomu IwakiTatsuro Yasukata
    • Hideyuki SuzukiIwao UtsunomiyaKoichi ShudoTsutomu IwakiTatsuro Yasukata
    • C07D487/04C07D255/02C07D487/14
    • C07D413/14C07D271/02C07D413/10C07D471/14C07D487/04Y02P20/55
    • 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,任选地不饱和且任选地与另一个环稠合; X 1为单键或选自-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,各自任选被所述含杂原子基团中断; 环B是任选取代的碳环或任选取代的杂环; R 1为氢,或可用于作为抗菌剂使用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的恶唑烷酮环的5位的有机残基。
    • 4. 发明授权
    • Compound having heterocyclic ring
    • 具有杂环的化合物
    • US08148362B2
    • 2012-04-03
    • US12225819
    • 2007-03-30
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • A61K31/00C07D255/00
    • C07D273/06C07D255/02C07D413/10C07D413/14C07D417/14C07D471/14Y02P20/55
    • 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; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 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; R1 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.
    • 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 - , - C - , - CONR 3 - , - NR 4 CO-,-SO 2 NR 5 - 和-NR 6 SO 2 - 或低级烷基)或其中一个前述基团可以介入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; R1是氢,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。
    • 5. 发明申请
    • Novel Compound Having Heterocyclic Ring
    • 具有杂环的新型化合物
    • US20090299059A1
    • 2009-12-03
    • US12225819
    • 2007-03-30
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • C07D413/10
    • C07D273/06C07D255/02C07D413/10C07D413/14C07D417/14C07D471/14Y02P20/55
    • 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; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 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; R1 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.
    • 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 - , - C - , - CONR 3 - , - NR 4 CO-,-SO 2 NR 5 - 和-NR 6 SO 2 - 或低级烷基)或其中一个前述基团可以介入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; R1是氢,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。
    • 7. 发明申请
    • OXAZOLIDINONE DERIVATIVE HAVING FUSED RING
    • 具有熔融环的氧杂环丁酮衍生物
    • US20110098471A1
    • 2011-04-28
    • US13000411
    • 2009-06-23
    • Issei KatohToshiaki AokiHideyuki SuzukiIwao UtsunomiyaNorikazu KurodaTsutomu Iwaki
    • Issei KatohToshiaki AokiHideyuki SuzukiIwao UtsunomiyaNorikazu KurodaTsutomu Iwaki
    • C07D487/04C07D471/04
    • C07D471/04C07D487/04
    • The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof; wherein ring A is ring B is a benzene ring optionally substituted with lower alkyl; ring C is an optionally substituted six-membered heterocycle containing at least one nitrogen atom and one to three double bond(s) in the ling wherein the atom at the point of attachment to ring B is a carbon atom; ring D is an optionally substituted five-membered ring containing one or two double bond(s) in the ring; A1 and A2 are independently nitrogen or carbon; m is 0 or 1; R represents H, —NHC(═O)RA, —NHC(═S)RA, —NH-het1, —O-het1, —S-het1, —S(═O)-het1, —S(═O)2-het1, het2, —CONHRA, —OH, lower alkyl, lower alkoxy or lower alkenyl; and het1 and het2 are independently a heterocyclic group; with the proviso that the fused ring C-D is not
    • 本发明提供了包含式(I)的恶唑烷酮衍生物或其药学上可接受的盐或溶剂化物的新型抗微生物药物: 其中环A是环B是任选被低级烷基取代的苯环; 环C是任选被取代的六元杂环,其含有至少一个氮原子和一至三个双键,其中与环B连接点处的原子是碳原子; 环D是在环中含有一个或两个双键的任选取代的五元环; A1和A2独立为氮或碳; m为0或1; R表示H,-NHC(= O)RA,-NHC(= S)RA,-NH-het1,-O-het1,-S-het1,-S(= O)-het1,-S(= 2-het1,het2,-CONHRA,-OH,低级烷基,低级烷氧基或低级烯基; het1和het2独立地是杂环基; 条件是稠环C-D不是