CAS: 180384-57-0; N-(2-(2-(2H-Tetrazol-5-yl)Pyridin-4-yl)-6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)Pyrimidin-4-yl)-5-Isopropylpyridine-2-Sulfonamide

该化合物是一种选择性的内分泌素受体,主要针对内分泌素-1(ET-1)受体,在血管收缩和心血管调节中起着重要作用,被归类为小分子,并经常在肺动脉高血压和心脏衰竭等条件下被调查其潜在的治疗用途.Tezosentan对内分泌素A和B受体表现出高度的亲和性,尽管对内泌素A和B受体而言,这种受体更具选择性.该化合物通常在临床环境中施用,并研究其对减少血压和改善肝动力学的影响.其化学结构包括一个有助于其药理特性的磺酰胺组.Tezosentan的行动机制涉及阻断内泌素-1的影响,导致血管血管进化和改善血液流动.尽管它在临床试验中表现出了希望,但其使用可能因副作用和需要谨慎的病人监测而受到限制.总的来说,Tezosen代表了心血管药理学研究的一个重要领域.

结构式图片

MSDS等安全信息

    上下游产品

    5-Isopropyl-Pyridine-2-Sulfonic Acid [6-Chloro-5-(2-Methoxy-Phenoxy)-2-[2-(1H-Tetrazole-5-yl)-Pyridine-4-Yl]-Pyrimidine-4-Yl]-Amide 257876-29-2
    Pyridin-2-Yl-Carbamic Acid 2-[6-(5-Isopropyl-Pyridine-2-Sulfonylamino)-5-(2-Methoxy-Phenoxy)-2-Morpholin-4-Yl-Pyrimidin-4-Yloxy]-Ethyl Ester 179400-71-6

    合成工艺路线路线简述

      📜Pyridin-2-Yl-Carbamic Acid 2-[6-(5-Isopropyl-Pyridine-2-Sulfonylamino)-5-(2-Methoxy-Phenoxy)-2-Morpholin-4-Yl-Pyrimidin-4-Yloxy]-Ethyl Ester,氯化铵,叠氮化钠 以to Form 5-Isopropyl-Pyridine-2-Sulfonic Acid {6-(2-Hydroxy-Ethoxy)-5-(2-Methoxy-Phenoxy)-2-[2-(1H-Tetrazol-5-yl)-Pyridin-4-Yl]-Pyrimidin-4-Yl}-Amide的收率获得替唑生坦
      参考文献:Process For The Manufacture Of 2,5-Disubstituted Pyridines
      标题:Process For The Manufacture Of 2,5-Disubstituted Pyridines
      摘要:本发明涉及一种制备式(I)的2,5-二取代吡啶的方法,其中包括以下步骤:A)将式(II)的化合物r.Sup.1-Ch.Dbd.Ch-R.Sup.2(II)与式(III)的丙烯酸化合物反应,以形成式(Iv)的化合物;B)在无水条件下将式(Iv)的化合物与氢卤酸反应.其中,R.Sup.1表示低碳基,R.Sup.2表示二(低碳基)氨基或具有氮原子上的游离价键的5-或6-成员的-N-杂环基团,X表示卤素.

      海关参考信息

      专利信息


      专利号:US-2008287407-A1
      优先权日:2003-12-10
      标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
      发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
      权利人:NITROMED INC
      摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

      专利号:US-8487108-B2
      优先权日:2005-11-14
      标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
      发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
      权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
      摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

      专利号:US-6004965-A
      优先权日:1994-12-20
      标题 :Sulfonamides
      发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI
      权利人:HOFFMANN LA ROCHE
      摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.

      专利号:TW-201518323-A
      优先权日:2013-07-25
      标题 :Synthesis of biological conjugates of APELIN polypeptides

      专利号:US-2010160351-A1
      优先权日:2008-12-19
      标题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
      发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE
      权利人:NUON THERAPEUTICS INC
      摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: n n n n n n n n n n n n or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.

      专利号:WO-2010071865-A1
      优先权日:2008-12-19
      标 题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
      发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE
      权利人:NUON THERAPEUTICS INC; JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE
      摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.

      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: Mommerot A, Denault AY, Dupuis J, Carrier M, Perrault LP. Cardiopulmonary bypass is associated with altered vascular reactivity of isolated pulmonary artery in a porcine model: therapeutic potential of inhaled tezosentan. J Cardiothorac Vasc Anesth. 2014 Jun;28(3):698-708. doi: 10.1053/j.jvca.2013.12.013. doi: 10.1053/j.jvca.2013.01.023. Epub 2013 Mar 21. doi: 10.1002/jcb.24383.
      4: Leskelä HV, Vuolteenaho O, Koivula MK, Taskinen P, Ruskoaho H, Peltonen T, Lehenkari P. Tezosentan inhibits uptake of proinflammatory endothelin-1 in stenotic aortic valves. J Heart Valve Dis. 2012 Jan;21(1):23-30. doi: 10.1007/s00134-012-2484-5. Epub 2012 Feb 14. doi: 10.1016/j.kjms.2011.10.019. Epub 2012 Jan 14. doi: 10.1007/s00228-011-1157-6. Epub 2011 Nov 20. doi: 10.1111/j.1748-1716.2011.02339.x. Epub 2011 Aug 12. doi: 10.1111/j.1440-1681.2011.05540.x. doi: 10.3346/jkms.2009.24.5.782. Epub 2009 Sep 23.
      11: Gulmen S, Kiris I, Narin C, Ceylan BG, Mermi B, Sutcu R, Meteoglu I. Tezosentan reduces the renal injury induced by abdominal aortic ischemia-reperfusion in rats. J Surg Res. 2009 Nov;157(1):e7-e13. doi: 10.1016/j.jss.2008.08.011. Epub 2008 Oct 24. doi: 10.1177/0091270008330157. doi: 10.1097/SHK.0b013e31819e2cbb. doi: 10.1016/j.avsg.2008.10.003. Epub 2009 Jan 9. doi: 10.1111/j.1399-6576.2008.01834.x. Epub 2008 Dec 15. doi: 10.1002/lt.21621.

      合成参考文献


      参考文献:10.1371/journal.pone.0021534
      摘要:Fenhammar J, Andersson A, Forestier J, Weitzberg E, Sollevi A, Hjelmqvist H, Frithiof R. Endothelin Receptor A Antagonism Attenuates Renal Medullary Blood Flow Impairment in Endotoxemic Pigs. PLoS ONE. 2011 Jul 08;6(7):e21534. doi: 10.1371/journal.pone.0021534.
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