CAS: 77181-69-2; 5-((E)-2-Bromovinyl)-1-((2R,3S,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)Pyrimidine-2,4(1H,3H)-Dione

该化合物是一种与抗病毒特性的核核素的类似物,主要对抗酶病毒(VZV)和1型类虫病毒(HSV-1)有效,其行动机制涉及通过纳入病毒基因组有选择地抑制病毒DNA合成,导致链条终止,苏维埃丁表现出高生物利用率和低浓度的有力活动,使其成为定向抗病毒疗法的候选对象,然而,其临床使用由于潜在的药物相互作用,特别是与氟胺的相互作用而受到限制,这可能导致剧毒. 研究继续探索其衍生物及其在抗病毒疗法中的应用,强调其特性和对抗VZV的效力.

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上下游产品

CAS号87877-27-8 1-(2,3,5-tri-O-... | CAS号86359-94-6 (2R,3R,4S,5R)-2...

合成工艺路线路线简述

    📜3-(1-(β-D-Arabinofuranosyl)Uracil-5-yl)-Acrylic Acid置于potassium Hydrogencarbonate,N-溴代丁二酰亚胺(Nbs)体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 6.0H,以21.8%的收率获得产物索立夫定
    参考文献:Nucleosides For Suppressing Or Reducing The Development Of Resistance In Cytostatic Therapy
    标题:Nucleosides For Suppressing Or Reducing The Development Of Resistance In Cytostatic Therapy
    摘要:该发明涉及特殊的核苷,例如,公式i所示的核苷,其中r1-R5如本文所述,并且涉及含有这些核苷的药物.此外,该发明涉及在癌症患者细胞毒治疗中抑制或减少耐药形成的方法中使用这种核苷.

    海关参考信息

    专利信息


    专利号:US-2022233673-A1
    优先权日:2019-06-04
    标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
    发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
    权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
    摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

    专利号:US-9522932-B2
    优先权日:2004-03-04
    标 题 :Phosphonate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production
    发明人:HERDEWIJN PIET; PANNECOUQUE CHRISTOPHE; WU TONGFEI; DE CLERCQ ERIK
    权利人:LEUVEN K U RES & DEV
    摘要:The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

    专利号:US-2020239500-A1
    优先权日:2018-04-04
    标 题 :Compositions and Methods for Synthesis of Phosphorylated Molecules

    专利号:US-2009298708-A1
    优先权日:2006-08-23
    标题 :2'-deoxy-2'-fluoro-beta-d-arabinonucleoside 5'-triphosphates and their use in enzymatic nucleic acid synthesis
    发明人:MASAD DAMHA J; GENG PENG CHANG
    权利人:MASAD DAMHA J; GENG PENG CHANG
    摘要:The invention relates to arabinose modified nucleoside 5′ triphosphates and to the biosynthesis and amplification of oligonucleotides containing and/or from templates containing arabinose modified nucleosides. The invention further relates to methods of generating modified oligonucleotide libraries for use in selection strategies, such as SELEX. The arabinose modified oligonucleotides of the invention are useful for modulating target nucleic acid expression, such as RNA.

    专利号:US-9907753-B2
    优先权日:2010-03-19
    标 题 :Lipid vesicle compositions and methods of use
    发明人:IRVINE DARRELL J; MOON JAEHYUN
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Manolopoulos VG, Ragia G. Fluoropyrimidine Toxicity: the Hidden Secrets of DPYD. Curr Drug Metab. 2024;25(2):91-95. doi: 10.2174/0113892002296707240311105527.
    23:100531. doi: 10.1016/j.imu.2021.100531. Epub 2021 Feb 10.
    3: Shiraki K, Tan L, Daikoku T, Takemoto M, Sato N, Yoshida Y. Viral ribonucleotide reductase attenuates the anti-herpes activity of acyclovir in contrast to amenamevir. Antiviral Res. 2020 Aug;180:104829. doi: 10.1016/j.antiviral.2020.104829. Epub 2020 Jun 20. 16(11):1231-41. doi: 10.2174/1568026615666150915111933. 43(10):1505-21. doi: 10.1124/dmd.115.065698. Epub 2015 Aug 10.

    合成参考文献


    摘要:Kiso to Rinsho. Clinical Report., 24(925), 1990
    参考文献:10.1016/j.antiviral.2003.10.003
    摘要:Andrei G, De Clercq E, Snoeck R. In vitro selection of drug-resistant varicella-zoster virus (VZV) mutants (OKA strain): differences between acyclovir and penciclovir Antiviral Res. 2004 Mar;61(3):181–7. doi: 10.1016/j.antiviral.2003.10.003.
    参考文献:10.1128/aac.29.3.524
    摘要:Machida H. Comparison of susceptibilities of varicella-zoster virus and herpes simplex viruses to nucleoside analogs. Antimicrob Agents Chemother. 1986 Mar;29(3):524–6.
    参考文献:10.2165/00003495-199448040-00004
    摘要:Nikkels AF, Piérard GE. Recognition and treatment of shingles. Drugs. 1994 Oct;48(4):528–48. doi: 10.2165/00003495-199448040-00004.
    参考文献:10.1023/a:1016165101921
    摘要:Ueda S, Yamaoka K, Yui J, Shigematsu A, Nakagawa T. Evaluation of capacity-limited first-pass effect through liver by three-points sampling in portal and hepatic veins and systemic artery. Pharm Res. 2002 Jun;19(6):852–7. doi: 10.1023/a:1016165101921.
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