CAS: 78266-06-5; 2,2'-((2-((3-Bromo-2,4,6-Trimethylphenyl)Amino)-2-Oxoethyl)Azanediyl)Diacetic Acid

该化合物是一种主要用于医学成像,特别是肝脏扫描的放射性药剂化合物,是一种非硝基二乙酸的衍生物,作为肝脏剂的功能,允许通过PESECT或PET扫描等成像技术对肝脏和胆囊功能进行直观化,该物质具有与肝细胞结合的能力,便于对肝功能和下垂进行评估.Mebrofenin通常通过静脉注射进行,并因其从血液流中迅速清除并被肝脏吸收而闻名,从而提高了成像的质量.其化学结构包括一个溴原子,有助于其无线电标签特性.安全剖面显示,它一般都得到良好的发作,尽管与所有放射性药物学一样,它需要谨慎地处理和管理放射性成分.

结构式图片

合成工艺路线路线简述

    📜次氮基三乙酸,3-溴-2,4,6-三甲基苯胺置于乙酸酐体系中,用 吡啶,Sodium Hydroxide,乙醇,水 作为反应溶剂,化学反应生成 美溴非林
    参考文献:N-Substituted Iminodiacetic Acids
    标题:N-Substituted Iminodiacetic Acids
    摘要:选择公式组中具有以下公式##str1##或其药学上可接受的水溶性盐中的一种化合物与锝-99M的络合物,其中r.Sub.1和r.Sub.4各自独立地为氢,甲基或乙基;r.Sub.2和r.Sub.3中的一个是1至4个碳的烷基,另一个是溴或碘;n为0,1或2,对于肝胆系统的外部成像是有用的.

    海关参考信息

    专利信息


    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    专利号:US-9220714-B2
    优先权日:2006-03-16
    标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
    发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
    权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
    摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

    专利号:US-2015352230-A1
    优先权日:2013-01-11
    标 题:Synthesis and isolation of dendrimer based imaging systems
    发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
    权利人:UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).

    专利号:US-2012232225-A1
    优先权日:2009-08-26
    标 题:Synthesis and isolation of dendrimer systems
    发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL
    权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).

    专利号:US-9402911-B2
    优先权日:2011-12-08
    标题:Multifunctional small molecules
    发明人:BAKER JR JAMES R; HUANG BAOHUA M; THOMAS THOMMEY P
    权利人:UNIV MICHIGAN REGENTS
    摘要:The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.

    专利号:US-8912323-B2
    优先权日:2009-10-30
    标题 :Multifunctional small molecules
    发明人:BAKER JR JAMES R; ZONG HONG; THOMAS THOMMEY P
    权利人:BAKER JR JAMES R; ZONG HONG; THOMAS THOMMEY P; UNIV MICHIGAN
    摘要:The present invention relates to dendrimer synthesis. Specifically, the present invention relates to triazine scaffolds capable of click chemistry for one-step synthesis of functionalized dendrimers, and methods of making and using the same.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Smet H, Martin D, Uldry E, Duran R, Girardet R, Schaefer N, Prior JO, Denys A, Halkic N, Demartines N, Melloul E. Tc-99m mebrofenin hepatobiliary scintigraphy to assess future liver remnant function before major liver surgery. J Surg Oncol. 2023 Aug 28. doi: 10.1002/jso.27426. Epub ahead of print. 48(8):719-721. doi: 10.1097/RLU.0000000000004732. Epub 2023 Jun 8.
    4: Jocius D, Vajauskas D, Samuilis A, Mikelis K, Jokubauskiene S, Strupas K, Tamosiunas AE. Assessing Liver Fibrosis Using 2D-SWE Liver Ultrasound Elastography and Dynamic Liver Scintigraphy with 99mTc-mebrofenin: A Comparative Prospective Single-Center Study. Medicina (Kaunas). 2023 Feb 28;59(3):479. doi: 10.3390/medicina59030479.
    5: Pirot C, Peyronnet D, Vigne J. Optimised quality control method for determination of the radiochemical purity of [99mTc]Tc-mebrofenin and [99mTc]Tc-etifenin in a clinical context. Eur J Hosp Pharm. 2023 Jan

    合成参考文献


    参考文献:10.1007/bf02752271
    摘要:Gupta DK, Srinivas M, Bajpai M. AIIMS clinical score: a reliable aid to distinguish neonatal hepatitis from extra hepatic biliary atresia. Indian J Pediatr. 2001 Jul;68(7):605–8. doi: 10.1007/bf02752271.
    参考文献:10.1007/s00147-002-0406-0|10.1111/j.1432-2277.2002.tb00180.x
    摘要:Saigal S, Srinivasan P, Devlin J, de Boer B, Thomas B, Portmann B, Heaton ND, O'Grady J, Rela M. Auxiliary partial orthotopic liver transplantation in acute liver failure due to hepatitis B. Transpl Int. 2002 Jul;15(7):369–73. doi: 10.1007/s00147-002-0406-0.
    参考文献:10.1007/s11095-008-9597-0
    摘要:Ghibellini G, Leslie EM, Pollack GM, Brouwer KLR. Use of Tc-99m Mebrofenin as a Clinical Probe to Assess Altered Hepatobiliary Transport: Integration of In Vitro, Pharmacokinetic Modeling, and Simulation Studies. Pharmaceutical Research. 2008 May 30;25(8):1851. doi: 10.1007/s11095-008-9597-0.
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