CAS: 126268-81-3; Mivobulin Isethionate

该化合物是合成化合物,主要以其在药理学领域的应用而闻名,特别是作为抗菌剂.它属于微囊抑制剂的类别,通过干扰微生物的正常组装和分解而起作用,从而抑制细胞分裂.这个机制使它成为癌症治疗的候选体,因为它可以针对迅速分解的细胞.异硫酸盐形式增加了其溶解性和稳定性,这对于其生物利用率和治疗效力至关重要.Mivubulin的特征是其特定的分子结构,其中包括一个核心,它与形成微囊的蛋白质管素相互作用.它的药理动力特性,如吸收,分布,代谢和排泄,对于决定其临床用途和剂量至关重要.与许多止血药剂一样,潜在的副作用可能包括对正常细胞的毒性,从而需要在治疗过程中进行仔细监测.总的来说,Mivubulin是定向癌症治疗中的一项重大进步,其研究正在优化临床环境中的用途.

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      📜(-)-(S)-N-(5-氨基-2-甲基-3-苯基-L,2-二氢吡啶并[3,4-B]吡嗪-7-基)氨基甲酸乙酯 反应生成(-)-(S)-N-(5-氨基-2-甲基-3-苯基-L,2-二氢吡啶并[3,4-B]吡嗪-7-基)氨基甲酸乙酯2-羟基乙基磺酸盐
      参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 1994,34,11-16
      标题:Journal Of Labelled Compounds And Radiopharmaceuticals 1994,34,11-16

      海关参考信息

      专利信息


      专利号:US-8598153-B2
      优先权日:2006-09-22
      标题 :Method of treatment using fatty acid synthesis inhibitors
      发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN
      权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME
      摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.

      专利号:US-10793557-B2
      优先权日:2018-04-03
      标题 :Sting agonist compounds
      发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHILDERS MATTHEW LLOYD; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIM JONGWON; LU MIN; OTTE RYAN D; TROTTER BENJAMIN WESLEY
      权利人:MERCK SHARP & DOHME
      摘要:Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

      专利号:US-2011104052-A1
      优先权日:2007-12-03
      标 题 :Methods of synthesis and use of chemospheres
      发明人:BARNETT BRADLEY POWERS; GESCHWIND JEFFREY
      权利人:UNIV JOHNS HOPKINS
      摘要:The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.

      专利号:US-11702430-B2
      优先权日:2018-04-03
      标 题:Aza-benzothiophene compounds as STING agonists
      发明人:ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T
      权利人:MERCK SHARP & DOHME LLC; ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T
      摘要:Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , R 9 , A, X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.

      专利号:US-11685761-B2
      优先权日:2017-12-20
      标 题:Cyclic di-nucleotide compounds as sting agonists
      发明人:ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN-LIAN
      权利人:MERCK SHARP & DOHME; ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN LIAN; MERCK SHARP & DOHME LLC
      摘要:A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

      专利号:US-10766919-B2
      优先权日:2015-08-13
      标 题 :Cyclic di-nucleotide compounds as sting agonists
      发明人:ALTMAN MICHAEL D; ANDRESEN BRIAN; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LIANG RUI; LIM JONGWON; LIU HONG; LU MIN; NORTHRUP ALAN B; OTTE RYAN D; SIU TONY; TROTTER BENJAMIN WESLEY; TRUONG QUANG T; WALSH SHAWN P; ZHAO KAKE
      权利人:MERCK SHARP & DOHME
      摘要:A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base 1 , Base 2 , Y, Y a , X a , X a1 , X b , X b1 , X c , X c1 , X d , X d1 , R 1 , R 1a , R 2 , R 2a , R 3 , R 4 , R 4a , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , and R 8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Kunschner LJ, Fine H, Hess K, Jaeckle K, Kyritsis AP, Yung WK. CI-980 for the treatment of recurrent or progressive malignant gliomas: national central nervous system consortium phase I-II evaluation of CI-980. Cancer Invest. 2002;20(7-8):948-54. . A phase II study of CI-980 in previously untreated extensive small cell lung cancer: an Ohio State University phase II research consortium study. Cancer Invest. 2002;20(2):192-8.
      15: Barbier P, Peyrot V, Dumortier C, D'Hoore A, Rener GA, Engelborghs Y. Kinetics of association and dissociation of two enantiomers, NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI 980), to tubulin. Biochemistry. 1996 Feb 13;35(6):2008-15.

      合成参考文献


      参考文献:10.1007/bf00173678
      摘要:Smith M, Ho PT. Pediatric drug development: a perspective from the Cancer Therapy Evaluation Program (CTEP) of the National Cancer Institute (NCI). Invest New Drugs. 1996;14(1):11–22. doi: 10.1007/bf00173678.
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