合成目标产物 Retigabine 主要起始原料 {4-[(4-Fluorobenzil)Ammino]-2-Nitrofenil}Carbammato Di Etile
(文献来源)合成步骤主要原料 {4-[(4-Fluorobenzil)Ammino]-2-Nitrofenil}Carbammato Di Etile
2-氨基-5-(4-氟苯亚甲基氨基)硝基苯置于1 % Platinum And 2% Vanadium On Carbon Sodium Tetrahydroborate,氢气,Sodium Ethanolate,Sodium Hydroxide体系中,用 乙醇 用作溶剂,20.0~75.0 °C,200.0 Kpa 条件下,反应 4.5H,反应生成瑞替加滨 参考文献: Process For The Preparation Of Retigabine[fr] Procédé De Préparation De Rétigabine 标题: Process For The Preparation Of Retigabine[fr] Procédé De Préparation De Rétigabine 摘要:这项发明涉及一种新颖的化学合成过程,用于合成2-乙氧羰氨基-5-(4-氟苯甲氨基)-硝基苯,并将其用于制备2-氨基-4-(4-氟苯甲氨基)-1-乙氧羰氨基苯(利替加宾/依曾加宾)及其多形式.
专利号:EP-2665702-A1 优先权日:2011-01-18 标 题 :Process for the preparation of retigabine 发明人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL 权利人:GLAXO GROUP LTD 摘要:This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
专利号:US-9102593-B2 优先权日:2011-01-18 标 题 :Process for the preparation of retigabine 发明人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL 权利人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL; GLAXO GROUP LTD 摘要:This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
专利号:US-2024207302-A1 优先权日:2021-04-01 标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof 发明人:CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO 权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO 摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.
专利号:US-2024300894-A1 优先权日:2021-03-19 标 题:Prodrugs of kv7 channel openers 发明人:CREAN CHRISTOPHER S; BROWN EDWARD G 权利人:XYZAGEN INC 摘要:Prodrugs of pharmacologically active 1,2,4-triaminobenzene derivatives of the General Formula (I); or pharmaceutically acceptable salts thereof, where the symbols R 1 , R 2 , R 3 , R 4 , R 5 and R 6a , R 6b , and R 6c and where the symbol Z are defined. Methods for the synthesis, purification, testing and use as prodrugs of pharmacologically-active agents at Kv7 ion channels are provided.
专利号:EP-4630405-A1 优先权日:2022-12-06 标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要:Gunthorpe MJ et al; Epilepsia 53 (3): 412-24 (2012) 摘要:Physicians Desk Reference 68th ed, Montvale, NJ: Thomson PDR, 2014 摘要:European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Trobalt p.13-4 (2011). Available from, as of February 12, 2014: 摘要:21 CFR Sections 1308.11-1308.15 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