CAS: 175463-14-6; (Z)-7-(3-(Aminomethyl)-4-(Methoxyimino)Pyrrolidin-1-yl)-1-Cyclopropyl-6-Fluoro-4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxylic Acid

该化合物是一种合成的氟己酮抗生素,其抗药性广泛,针对克己阳性细菌和克己阴性细菌,其行动机制包括抑制细菌DNAgyraase和Topo异构体IV,有效地干扰了DNA复制和转录;Gemifloxancin展示了对呼吸性病原体,包括血清球肺炎(包括抗青霉素菌株),流感嗜血杆菌和马哈西拉催生素的抗生素的抗体.该化合物表现出有利的药性,口服生物利用率高,组织渗透广泛,特别是在肺部,其双重目标抑制降低了抗体发展的可能性,与早先的氟丙酮相比,Gemifloxacinacin主要用于治疗慢性支气炎的社区性肺炎和急性细菌恶化.

结构式图片

上下游产品

CAS号44981-94-4 N-(2-氰基乙基) 甘氨酸乙酯 | CAS号773826-73-6 3-氨基甲基-4-羟基-1-吡... | CAS号197143-33-2 N-B°C-3-氰基-4-羟基吡咯烷 | CAS号175463-32-8 1-B°C-3-氰基-4-吡咯烷酮 | CAS号266353-18-8 N-tert-butoxyca... | CAS号175463-34-0 4-叔丁氧羰基氨甲基-1-N-... | CAS号175463-35-1 tert-butyl 3-(t... | CAS号197143-34-3 4-(N-tert-butox...

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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-8093381-B2
    优先权日:2007-05-24
    标题:Method of synthesis of fluoroquinolones
    发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS
    权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX
    摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.

    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:US-8399502-B2
    优先权日:2008-09-17
    标 题 :Analogs of indole-3-carbinol and their use as agents against infection
    发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
    权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
    摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

    专利号:US-2023364251-A1
    优先权日:2020-08-06
    标 题:Methods for the synthesis of protein-drug conjugates
    发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
    权利人:CIDARA THERAPEUTICS INC
    摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.

    专利号:US-2010203587-A1
    优先权日:2009-01-13
    标 题:Use of dna gyrase inhibitors for in vitro polypeptide synthesis reactions
    发明人:VOLOSHIN ALEXEI M; ZAWADA JAMES F; GOLD DANIEL
    权利人:SUTRO BIOPHARMA INC
    摘要:The present invention provides methods and compositions useful for in vitro polypeptide synthesis reactions. The methods involve the use of DNA gyrase inhibitors to prevent bacterial contamination in lysates used for in vitro production of polypeptides. The compositions include contamination-free cell lysates for in vitro protein synthesis reactions.
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    主要参考文献


    1: Foroughipour M, Nezamzadeh-Ejhieh A. CaTiO3/g-C3N4 heterojunction-based composite photocatalyst: Part I: Experimental design, kinetics, and scavenging agents' effects in photocatalytic degradation of gemifloxacin. Chemosphere. 2023 May 24;334:139019. doi: 10.1016/j.chemosphere.2023.139019. Epub ahead of print. 13(7):1234. doi: 10.3390/diagnostics13071234.
    3: Faisal M, Ahmed J, Jalalah M, Alsareii SA, Alsaiari M, Harraz FA. Rapid elimination of antibiotic gemifloxacin mesylate and methylene blue over Pt nanoparticles dispersed chitosan/g-C3N4 ternary visible light photocatalyst. Environ Sci Pollut Res Int. 2023 May;30(22):61710-61725. doi: 10.1007/s11356-023-26456-w. Epub 2023 Mar 18. 30(1):2185180. doi: 10.1080/10717544.2023.2185180.
    5: Jang MG, Cha S, Kim S, Lee S, Lee KE, Shin KH. Application of tree-based machine learning classification methods to detect signals of fluoroquinolones using the Korea Adverse Event Reporting System (KAERS) database. Expert Opin Drug Saf. 2023 Feb

    合成参考文献


    参考文献:10.1016/j.ijantimicag.2011.05.011
    摘要:Vallet CM, Marquez B, Ngabirano E, Lemaire S, Mingeot-Leclercq MP, Tulkens PM, Van Bambeke F. Cellular accumulation of fluoroquinolones is not predictive of their intracellular activity: studies with gemifloxacin, moxifloxacin and ciprofloxacin in a pharmacokinetic/pharmacodynamic model of uninfected and infected macrophages. Int J Antimicrob Agents. 2011 Sep;38(3):249–56. doi: 10.1016/j.ijantimicag.2011.05.011.
    摘要:Kilincalp S, Deveci M, Coban S, Basar O, Yuksel O. A new cause of acute hepatitis: gemifloxacin. Acta Gastroenterol Belg. 2012 Dec;75(4):460–1.
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