CAS: 698394-73-9; Vercirnon

结构式图片

上下游产品

4-Tert-Butyl-N-[4-Chloro-2-(Pyridine-4-Carbonyl)-Phenyl]-Benzenesulfonamide 698394-72-8
(2-氨基-5-氯苯基)-4-吡啶基甲酮 (2-Amino-5-Chlorophenyl)(Pyridin-4-yl)Methanone 105192-42-5

合成工艺路线路线简述

    📜4-Tert-Butyl-N-[4-Chloro-2-(Pyridine-4-Carbonyl)-Phenyl]-Benzenesulfonamide置于间氯过氧苯甲酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 16.0H,以35%的收率获得产物维塞诺
    参考文献:靶向 Ccr9 细胞内结合位点的化学生物学工具箱:荧光配体,新药先导物和 Protac
    标题:靶向 Ccr9 细胞内结合位点的化学生物学工具箱:荧光配体,新药先导物和 Protac
    摘要:基于细胞内 Ccr9 拮抗剂 Vercirnon,我们开发了第一个基于小分子的荧光配体,靶向 Gpcr 的细胞内变构结合位点 (Iabs).该工具能够通过 Nanobret,荧光显微镜进行结合研究,并发现具有更高亲和力的新型细胞内 Ccr9 拮抗剂.为了诱导 Ccr9 降解,我们开发了第一个针对 Gpcr 的 Iabs 的 Protac.
    DOI:10.1002/anie.202116782

    海关参考信息

    专利信息


    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2018230127-A1
    优先权日:2015-08-13
    标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
    发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

    专利号:US-10316018-B2
    优先权日:2015-08-27
    标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
    发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:CN-118955233-B
    优先权日:2024-07-27
    标题 :Synthesis method of monosubstituted bicyclo [1.1.1] pentane (BCP)

    专利号:CN-118955233-A
    优先权日:2024-07-27
    标 题:Synthesis method of monosubstituted bicyclo [1.1.1] pentane (BCP)

    供应商参考报价(招募中)

    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: Feagan BG, Sandborn WJ, D'Haens G, Lee SD, Allez M, Fedorak RN, Seidler U, Vermeire S, Lawrance IC, Maroney AC, Jurgensen CH, Heath A, Chang DJ. Randomised clinical trial: vercirnon, an oral CCR9 antagonist, vs. placebo as induction therapy in active Crohn's disease. Aliment Pharmacol Ther. 2015 Nov;42(10):1170-81. doi: 10.1111/apt.13398. Epub 2015 Sep 23. doi: 10.1016/j.bmcl.2015.06.046. Epub 2015 Jun 18. doi: 10.1007/s11894-015-0444-2. Review.
    4: Wendt E, Keshav S. CCR9 antagonism: potential in the treatment of Inflammatory Bowel Disease. Clin Exp Gastroenterol. 2015 Apr 7;8:119-30. doi: 10.2147/CEG.S48305. eCollection 2015. Review.
    5: Westphal MV, Wolfstädter BT, Plancher JM, Gatfield J, Carreira EM. Evaluation of tert-butyl isosteres: case studies of physicochemical and pharmacokinetic properties, efficacies, and activities. ChemMedChem. 2015 Mar;10(3):461-9. doi: 10.1002/cmdc.201402502. Epub 2015 Jan 28. doi: 10.1053/j.gastro.2014.08.044. Epub 2014 Sep 16. Review. doi: 10.1016/j.gtc.2014.05.012. Epub 2014 Jun 25. Review. doi: 10.1097/MOG.0000000000000077. Review. doi: 10.1111/apt.12639. Epub 2014 Jan 30. Review. doi: 10.1007/s00228-013-1592-7. Epub 2013 Oct 8.
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