CAS: 20168-99-4; Cinmetacin

该化合物是一种非类固醇抗炎药物(NSAID),属于非异丙酸类,主要用于止痛和抗炎特性,能够有效治疗关节炎和其他炎性疾病等症状; 辛麦色素的化学结构具有1-甲基-2-(4-甲基苯基)乙酸酯的化学结构,有助于其药理活动; 致力于抑制环氧酶酶(COX-1和COX-2),从而减少作为炎症和疼痛媒介的丙烯菊酯的合成; 辛麦氏素一般是口服的,并因行动较快而闻名. 但是,与其他非传染性疾病ID一样,它可能与胃肠侧效应,心血管风险和肾损伤有关,特别是长期使用. 其安全状况需要谨慎考虑,因为存在前的病人需要仔细研究其安全情况. 总的来说, 辛麦氏素是治疗疼痛和炎的潜在作用,但必须加以监测,以缓解其不良作用.

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    专利信息


    专利号:US-8546532-B2
    优先权日:2008-04-17
    标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
    发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
    权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
    摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

    专利号:US-8420850-B2
    优先权日:2010-05-14
    标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers
    发明人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE
    权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA
    摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.

    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-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    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.

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    主要参考文献


    1: Montero MT, Pouplana R, Valls O, García S. On the binding of cinmetacin and indomethacin to human serum albumin. J Pharm Pharmacol. 1986 Dec;38(12):925-7. Italian. Italian.

    合成参考文献


    摘要:Medicamentos de Actualidad., 15(397), 1979
    摘要:Arzneimittel-Forschung. Drug Research., 23(1690), 1973 []
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