CAS: 74711-43-6; 2-(10-Oxo-10,11-Dihydrodibenzo[b,F]Thiepin-2-yl)Propanoic Acid

该化合物是一种主要用于其止痛和抗炎特性的非类固醇抗炎药物(NSAID),它有选择性地抑制环氧酶-2(COX-2),减少丙烯酸酯合成,同时尽量减少与非选择性COX抑制作用相关的肠胃副作用.Zaltoprofen在减轻与风湿性关节炎,骨质炎和手术后不适症有关的疼痛和炎痛方面表现出了强大的功效.它迅速吸收和长时间的行动使它适合于管理急性和慢性疼痛.该化合物显示出一种有利的安全性特征,比传统的非典性肺炎低了致癌潜力.Zaltoprofen通常作为口服药片或热剂而成,在临床应用中提供多功能.

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上下游产品

2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid methyl ester zaltoprofen sodium hydrogencarbonate methyl 5-(1-methoxycarbonylethyl)-2-phenylthiophenylacetate

合成工艺路线路线简述

    5-(1-羧乙基)-2-(苯硫基)苯乙酸置于磷酸体系中,60.0~75.0 °C,600.01 Kpa 条件下,反应生成 扎托布洛芬
    参考文献:微通道反应器在扎托布洛芬的环合反应中的应用及扎托布洛芬的环合方法
    标题:微通道反应器在扎托布洛芬的环合反应中的应用及扎托布洛芬的环合方法
    摘要:本发明属于药物合成技术领域,具体公开了一种扎托布洛芬的环合方法及微通道反应器在该过程中的应用.本发明中,环合于反应温度为60~90°C,控制流量至5~10 Ml/min,压降6 Bar,物料通过时间为5~10S,扎托布洛芬中间体ⅱ5‑(2‑丙酸基)‑2‑苯硫基苯乙酸与多聚磷酸与磷酸的质量比为1︰3~4︰0.5的条件下在微通道反应器中进行,物料进入微通道反应器前将搅拌均匀的物料加热到60~70oc.利用微通道反应器可较大程度提高环合收率,缩短反应时间,稳定产品质量,后处理难度大幅度降低,污染程度得到极大改善.

    海关参考信息

    专利信息


    专利号:US-2012029226-A1
    优先权日:2009-02-06
    标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives
    发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE
    权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE
    摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.

    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-8304409-B2
    优先权日:2002-07-03
    标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
    发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
    权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
    摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 nitrosated NSAID, 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 nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:US-2024287041-A1
    优先权日:2021-05-20
    标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
    发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

    专利号:US-5633983-A
    优先权日:1994-09-13
    标 题:Systems and methods for performing phonemic synthesis
    发明人:COKER CECIL H
    权利人:LUCENT TECHNOLOGIES INC
    摘要:Systems and methods for performing phonemic synthesis which operate to generate an output data set of acoustic B parameters from a received textual data set wherein the output data set represents patterns of transition from one speech excitation state to another. The textual data set is converted to a plurality of phonetic data sets, at least one phone descriptor is assigned to each of the phonemic data sets, and the output data set is generated by processing the phonetic data sets as a non-linear function of a speech excitation control variable whereby the collective contributions of the phonetic data sets are determined for each pattern of transition from one speech excitation state to another. The speech excitation control variable represents selected portions of a human vocal system.
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    主要参考文献


    1: Jia L, Hu C, Wang H, Liu Y, Liu X, Zhang YY, Li W, Wang LX, Cao YF, Fang ZZ. Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential. Chirality. 2015 Jun;27(6):359-63. doi: 10.1002/chir.22436. Epub 2015 Apr 22. doi: 10.1213/ANE.0b013e31821c693c. Epub 2011 Apr 25. doi: 10.1016/j.ijpharm.2013.05.059. Epub 2013 Jun 4. doi: 10.3109/08982104.2015.1120746. Epub 2016 Jan 19. doi: 10.1016/S1674-8301(11)60007-9.
    6: Shah HA, Patel RP. Statistical modeling of zaltoprofen loaded biopolymeric nanoparticles: Characterization and anti-inflammatory activity of nanoparticles loaded gel. Int J Pharm Investig. 2015 Jan-Mar;5(1):20-7. doi: 10.4103/2230-973X.147229.
    7: Cui H, Quan P, Zhao H, Wen X, Song W, Xiao Y, Zhao Y, Fang L. Mechanism of Ion-Pair Strategy in Modulating Skin Permeability of Zaltoprofen: Insight from Molecular-Level Resolution Based on Molecular Modeling and Confocal Laser Scanning Microscopy. J Pharm Sci. 2015 Oct;104(10):3395-403. doi: 10.1002/jps.24543. Epub 2015 Jun 17. doi: 10.1159/000324532. Epub 2011 Mar 25. doi: 10.15171/apb.2015.073. Epub 2015 Nov 30.

    合成参考文献


    参考文献:10.1007/bf02252931
    摘要:Taniguchi Y, Deguchi Y, Noda K. Interaction between enoxacin, a new antimicrobial, and nimesulide, a new non-steroidal anti-inflammatory agent in mice. Inflamm Res. 1996 Aug;45(8):376–9. doi: 10.1007/bf02252931.
    参考文献:10.2165/11587280-000000000-00000
    摘要:Tomé AM, Filipe A. Quinolones: review of psychiatric and neurological adverse reactions. Drug Saf. 2011 Jun 01;34(6):465–88. doi: 10.2165/11587280-000000000-00000.
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