CAS: 146961-76-4; L-Alanyl-N-[(1Alpha,5Alpha,6Alpha)-3-[6-Carboxy-8-(2,4-Difluorophenyl)-3-Fluoro-5,8-Dihydro-5-Oxo-1,8-Naphthyridin-2-Yl]-3-Azabicyclo[3.1.0]Hex-6-Yl]-L-Alaninamide

该化合物是一种合成的氟己酮抗生素,主要用于抗菌特性,其特点是对各种抗菌性细菌的广泛光谱活动,使其有效治疗各种感染;该化合物具有典型的氟丙酮的双环核心结构,包括增强自身能力和活动范围的一个氟原子; 氨特罗福辛工作,抑制细菌DNAgyrase和四氧异构体酶,对DNA复制和转录至关重要的酶,从而防止细菌生长和扩散; 其药用植物特征通常包括良好的口服生物利用率和组织渗透,从而能够有效治疗系统感染; 此外,它可能表现出氟丙酮的副作用,例如胃肠扰动和对中心健康的潜在影响; 与所有抗生素一样,适当使用对最大限度地减少抗生素抗药性的风险至关重要. 总的来说,阿勒特罗福克辛是防止细菌感染武器库中一种宝贵的选择,特别是在其他抗生素无效的情况下.

结构式图片

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      专利信息


      专利号:US-9353057-B2
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
      发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
      权利人:XENOPORT INC
      摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:WO-2009094569-A2
      优先权日:2008-01-25
      标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

      专利号:US-2005222431-A1
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

      专利号:US-7227028-B2
      优先权日:2003-12-30
      标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

      专利号:US-2007244331-A1
      优先权日:2003-12-30
      标 题 :Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Mukherjee J. Post-approval translational research itself has diverse ethics. Am J Bioeth. 2010 Aug;10(8):43-4. doi: 10.1080/15265161.2010.496525. doi: 10.1016/j.cbi.2010.07.017. Epub 2010 Jul 23. doi: 10.1056/NEJMp0901474. doi: 10.1111/j.1471-8847.2008.00239.x. Epub 2008 Jul 28. doi: 10.1111/j.1471-8847.2008.00238.x. Epub 2008 Jul 15. Epub 2007 Oct 24.
      8: Willyard C. Pfizer lawsuit spotlights ethics of developing world clinical trials. Nat Med. 2007 Jul;13(7):763. Epub 2007 Jun 29.
      10: Starr JA, Ragucci KR. Thrombocytopenia associated with intravenous ciprofloxacin. Pharmacotherapy. 2005 Jul;25(7):1030-4.

      合成参考文献


      参考文献:10.1016/j.drudis.2011.05.007
      摘要:Chen M, Vijay V, Shi Q, Liu Z, Fang H, Tong W. FDA-approved drug labeling for the study of drug-induced liver injury. Drug Discov Today. 2011 Aug;16(15-16):697–703. doi: 10.1016/j.drudis.2011.05.007.
      摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
      摘要:Annals of Pharmacotherpy., 34(330), 2000 []
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