CAS: 186497-07-4; 2-(4-(1,3,4-Oxadiazol-2-yl)Phenyl)-N-(3-Methoxy-5-Methylpyrazin-2-yl)Pyridine-3-Sulfonamide

该化合物是一个小分子,作为内分泌素受体,具体针对内分泌素A(ETA)受体,主要调查其在治疗各种病症,包括癌症和心血管疾病方面的潜在治疗应用.Zibotentan的特征是有能力抑制内分泌素-1的影响,一种在调节血压和血管音调方面起重要作用的强大的血管抑制器.通过阻塞ETA受体,Zibotentan可以帮助减少肿瘤生长,改善受影响组织中的血液流动.该化合物在临床试验中进行了研究,特别是在前列腺癌方面,因为内分泌素的信号与肿瘤的演变有关.其药理特征包括口服生物利用率和有利的安全简介等属性,尽管有关其功效和副作用的具体细节是通过正在进行的研究来确定的.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

N-(isobutoxycarbonyl)-2-(4-methoxycarbonylphenyl)-N-(3-methoxy-5-methylpyrazin-2-yl)pyridine-3-sulphonamideN-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide ethanolamine salt N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide ammonium salt

合成工艺路线路线简述

    📜N-(Isobutoxycarbonyl) N-(3-Methoxy-5-Methylpyrazin-2-yl)-2-(4-[1,3,4-Oxadiazol-2-Yl]Phenyl)Pyridine-3-Sulphonamide置于c.I.酸性橙108,溶剂黄146体系中,用 水,异丙醇,甲苯 用作溶剂,化学反应 3.17H,以86.7%的收率获得2-(4-(1,3,4-噁二唑-2-基)苯基)-N-(3-甲氧基-5-甲基吡嗪-2-基)吡啶-3-磺酰胺
    参考文献:Wo2007/10235
    标题:Wo2007/10235

    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-2015284349-A1
    优先权日:2013-12-20
    标 题:Epidithiodiketopiperazine compounds, compositions, and methods
    发明人:BALAN CHENERA; MAHAJAN SUMIT; NAGAVARAPU USHA; GUPTA SHALABH
    权利人:GLOBAVIR BIOSCIENCES INC
    摘要:Epidithiodiketopiperazine compounds, pharmaceutical compositions based thereon and methods of their synthesis, as part of treating, inhibiting and reducing transcription and translation of hypoxia inducible genes are described.

    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.

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    主要参考文献


    1: Dawson N, Payne H, Battersby C, Taboada M, James N. Health-related quality of life in pain-free or mildly symptomatic patients with metastatic hormone-resistant prostate cancer following treatment with the specific endothelin A receptor antagonist zibotentan (ZD4054). J Cancer Res Clin Oncol. 2010 Apr 14. [Epub ahead of print] French. Epub 2009 Jul 14. Epub 2009 Feb 6.
    8: Growcott JW. Preclinical anticancer activity of the specific endothelin A receptor antagonist ZD4054. Anticancer Drugs. 2009 Feb;20(2):83-8. Review. Epub 2008 Nov 29. Review.

    合成参考文献


    参考文献:10.1002/pros.21435
    摘要:George D, Moul JW. Emerging treatment options for patients with castration-resistant prostate cancer. Prostate. 2012 Feb;72(3):338–49. doi: 10.1002/pros.21435.
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