CAS: 91714-94-2; 2-(2-Amino-3-(4-Bromobenzoyl)Phenyl)Acetic Acid

该化合物是一种主要用于治疗白内障手术后发炎和疼痛的眼科治疗眼科的非类固醇抗炎药物(NSAID),其特点是能够抑制环氧酶酶,这种酶在发炎过程中起着关键作用,将芳烃酸转化成prostalandins.Bromfenac通常作为一种眼滴溶液来配制,允许尽可能少系统吸收的局部治疗.该化合物以其行动较快的开始和长期治疗效果而闻名,使其在控制发炎方面行之有效.其化学结构包括一个溴原子,有助于其药性特性.Bromfenac一般都受到很好的注意,尽管潜在的副作用可能包括眼部不适,燃烧或施用时会发作.与任何药物一样,它必须遵循施用指南,并咨询保健专业人员,以便适当使用,特别是在有眼前状况的病人或其他使用眼科药物的人.

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上下游产品

7-(4-溴苯甲酰)-1,3-二氢-2H-吲哚-2-酮 7-(4-Bromobenzoyl)Indolin-2-One 91713-91-6

合成工艺路线路线简述

    2-氨基苯乙酸置于aluminum (Iii) Chloride,硫酸,三乙胺体系中,用 乙醇,二氯甲烷,甲苯 作为反应溶剂,化学反应 3.0H,反应生成 溴芬酸钠
    参考文献:一种溴芬酸钠新合成方法
    标题:一种溴芬酸钠新合成方法
    摘要:本发明公开了一种溴芬酸钠新合成方法,属于药物合成技术领域,包括其特征在于制备方法包括:以邻氨基苯乙酸为起始原料,通过酰化反应得到中间体ⅰ;中间体ⅰ经磺化反应得到中间体ⅱ;中间体ⅱ与对溴苯甲酰氯发生取代反应得到中间体ⅲ;中间体ⅲ经水解后得到溴芬酸;溴芬酸和氢氧化钠反应得到最终的成品溴芬酸钠;本发明的有益效果是:避免了现有技术中因合成方法原因产生的含吲哚环的杂质产生;避免了现有技术中因使用磷酸或冰醋酸产生酸式盐而导致最终成品ph超标问题,避免了因溴芬酸钠成品制备物料配比原因导致水分过低的质量问题,同时本合成方法简单易控,适于工业化生产.

    海关参考信息

    专利信息


    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    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-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    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.
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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Bromfenac. 2018 Dec 3.
    10:2099-2111. doi: 10.2147/OPTH.S86971.
    3: Hoy SM. Bromfenac Ophthalmic Solution 0.07%: A Review of Its Use After Cataract Surgery. Clin Drug Investig. 2015 Aug;35(8):525-9. doi: 10.1007/s40261-015-0309-3. 10(14):2379-85. doi: 10.1517/14656560903188425. 15(7):e249400. doi: 10.1136/bcr-2022-249400.

    合成参考文献


    参考文献:10.2147/opth.s7633
    摘要:Reddy R, Kim SJ. Critical appraisal of ophthalmic ketorolac in treatment of pain and inflammation following cataract surgery. Clin Ophthalmol. 2011;5():751–8.
    参考文献:10.1185/03007995.2011.597663
    摘要:Silverstein SM, Cable MG, Sadri E, Peace JH, Fong R, Chandler SP, Gow JA, Klier SM, McNamara TR; Bromfenac Ophthalmic Solution Once Daily (Bromday) Study Group. Once daily dosing of bromfenac ophthalmic solution 0.09% for postoperative ocular inflammation and pain. Curr Med Res Opin. 2011 Sep;27(9):1693–703. doi: 10.1185/03007995.2011.597663.
    参考文献:10.1016/j.ophtha.2011.04.035
    摘要:Henderson BA, Gayton JL, Chandler SP, Gow JA, Klier SM, McNamara TR; Bromfenac Ophthalmic Solution (Bromday) Once Daily Study Group. Safety and efficacy of bromfenac ophthalmic solution (Bromday) dosed once daily for postoperative ocular inflammation and pain. Ophthalmology. 2011 Nov;118(11):2120–7. doi: 10.1016/j.ophtha.2011.04.035.
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