CAS: 53164-05-9; 2-(2-(1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1H-Indol-3-yl)Acetoxy)Acetic Acid

该化合物是一种该化合物是一种在诸如骨髓炎,风湿类动脉炎和其他炎症的情况下长期使用的一种可取选择.其活性代谢素(在多米思基)可以确保持续的治疗效果.该化合物在口服配方中可以提供可预测的药性对动能和生物利用率.乙型乙型乙型六氯环己烷的平衡性功效和安全性特征使得它成为控制慢性炎疼痛和最小不良效应的可行选择.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号75302-98-6 ACEMETACINTERT-... | CAS号19501-58-7 4-甲氧基苯肼盐酸盐 | CAS号53-86-1 吲哚美辛 | CAS号123-76-2 乙酰丙酸 | CAS号53164-03-7 Laevulinoyloxye...

合成工艺路线路线简述

  • 合成目标产物 Acemetacin 主要起始原料 Acemetacintert-Butylester
  • (文献来源)合成步骤主要原料 Acemetacintert-Butylester
吲哚美辛置于palladium On Activated Charcoal 氢气,Potassium Carbonate体系中,用 乙酸乙酯 作为反应溶剂,化学反应 4.75H,反应生成 阿西美辛
参考文献:Boltze; Brendler; Jacobi,Arzneimittel-Forschung/drug Research,1980,Vol. 30,# 8 A,P. 1314-1325
标题:Boltze; Brendler; Jacobi,Arzneimittel-Forschung/drug Research,1980,Vol. 30,# 8 A,P. 1314-1325

海关参考信息

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-5043328-A
优先权日:1986-05-09
标 题 :Formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems
发明人:WEITHMANN KLAUS U
权利人:HOECHST AG
摘要:The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.

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.
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主要参考文献


1: Sanphui P, Bolla G, Nangia A, Chernyshev V. Acemetacin cocrystals and salts: structure solution from powder X-ray data and form selection of the piperazine salt. IUCrJ. 2014 Feb 28;1(Pt 2):136-50. doi: 10.1107/S2052252514004229. eCollection 2014 Mar 1.
2: Shehata TM, Abdallah MH, Ibrahim MM. Proniosomal oral tablets for controlled delivery and enhanced pharmacokinetic properties of acemetacin. AAPS PharmSciTech. 2015 Apr;16(2):375-83. doi: 10.1208/s12249-014-0233-5. Epub 2014 Oct 16.
3: Cebeci F, Yaşar Ş, Aytekin S, Güneş P. Acemetacin-induced fixed drug eruption. Indian J Pharmacol. 2016 Mar-Apr;48(2):219-20. doi: 10.4103/0253-7613.178824.

合成参考文献


摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
摘要:Lead Optimization for Medicinal Chemists. Zaragoza Dorwald F. (2012). Wiley-VCH
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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