CAS: 115256-11-6; N-(4-(2-(Methyl(2-(4-(Methylsulfonamido)Phenoxy)Ethyl)Amino)Ethyl)Phenyl)Methanesulfonamide

该化合物是一种主要用作治疗性纤维化和性颤动的抗心律剂的药物化合物,它有选择性地抑制了在心脏再极化中起着关键作用的延迟固化钾电流(IKr)的快速成分;多菲化物的特征是能够延长心组织中的行动潜在持续时间和耐受期,从而帮助恢复正常的心脏节奏;该物质一般是口服的,并因其在患有性纤维化的病人中保持鼻弦节律的功效而闻名;然而,它与心律紊乱的危险有关,特别是在肾损伤的病人或服用某些伴生药物的病人中.多菲化物主要通过肾脏进行新陈代谢,需要在治疗期间仔细监测肾功能;其化学结构包括双环核心,有助于其药性特性.与任何药物一样,在开用甲虫时必须考虑潜在的副作用和抗反作用.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号3144-09-0 甲基磺酰胺 | CAS号124-63-0 甲基磺酰氯 | CAS号115256-12-7 1-(4-methanesul... | CAS号3383-72-0 2-氯乙基-4-硝基苯基醚 | CAS号85176-37-0 Benzeneethanami... | CAS号115287-37-1 N-甲基-4-硝基-N-[2-... | CAS号115256-13-8 N-甲基-N-4-氨基苯氧乙基... | CAS号7143-01-3 甲基磺酸酐 | CAS号69447-84-3 4-硝基苯乙胺氢溴酸盐

合成工艺路线路线简述

  • 合成目标产物 Dofetilide 主要起始原料 N-Methyl-N-(2-(4-Nitrophenoxy)Ethyl)-2-(4-Nitrophenyl)Ethanamine
  • (文献来源)合成步骤主要原料 N-Methyl-N-(2-(4-Nitrophenoxy)Ethyl)-2-(4-Nitrophenyl)Ethanamine
N-甲基-[2-(4-硝基-苯基)-乙基]-胺置于镍 氢气,Potassium Carbonate,Sodium Iodide体系中,用 乙醇,二氯甲烷,乙腈 用作溶剂,25.0 °C,303.98 Kpa 条件下,反应 88.0H,反应生成多非利特
参考文献:Selective Class Iii Antiarrhythmic Agents. 1. Bis(Arylalkyl)Amines
标题:Selective Class Iii Antiarrhythmic Agents. 1. Bis(Arylalkyl)Amines
摘要:A Series Of Bis(Arylalkyl)Amines Is Described And Their Effects On Prolonging Effective Refractory Period In Isolated Cardiac Tissue Listed. Most Compounds Prolonged The Cardiac Action Potential Without Significantly Altering The Maximum Rate Of Depolarization And May Be Defined As Selective Class Iii Antiarrhythmic Agents. It Was Found That A Particularly Advantageous Structural Feature Was To Have A Methanesulfonamido Moiety On Both Of The Aryl Rings. Thus,Compound 16 [1-(4-Methanesulfonamidophenoxy)2-[n-(4-Methanesulfonamidophene Thyl)-N-Methylamine]Ethane] Was Selected For Further Investigations. The Compound Is Highly Potent And Selective Class Iii Agent Which Acts By Blockade Of Cardiac Potassium Channels.
Doi:10.1021/jm00166A011

海关参考信息

专利信息


专利号:US-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

专利号:WO-2025077857-A1
优先权日:2023-10-13
标题:Use of prmt5 inhibitor in treatment of tumors or cancers
发明人:YAO BING; GU XIAOHUI; MAO WEIFENG; ASWAD FRED JULLIEN; JOSEPH JAMES DAVID; LI MINGXI
权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD
摘要:The present disclosure describes a novel molecule having protein arginine methyltransferase 5 inhibitory activity, and methods for synthesis and use of a compound. Specifically, the present disclosure describes a compound of formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, and methods for synthesis and use of the compound.

专利号:US-9550000-B2
优先权日:2011-09-09
标题 :Compositions, methods, and systems for the synthesis and use of imaging agents
发明人:ROBINSON SIMON P; YU MING
权利人:ROBINSON SIMON P; YU MING; LANTHEUS MEDICAL IMAGING INC
摘要:The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

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-2023346952-A1
优先权日:2015-09-22
标题:Cannabinoid glycoside prodrugs and methods of synthesis
发明人:ZIPP BRANDON J; HARDMAN JANEE’ M; BROOKE ROBERT T; DEUTSCHER TYREL R
权利人:GRAPHIUM BIOSCIENCES INC
摘要:The present invention provides tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs and pharmaceutical compositions comprising these compounds, and their use for the site-specific delivery of tetrahydrocannabinol or cannabidiol. Also provided are processes for the preparation of purified tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs.

专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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主要参考文献


1: Shenasa F, Shenasa M. Dofetilide: Electrophysiologic Effect, Efficacy, and Safety in Patients with Cardiac Arrhythmias. Card Electrophysiol Clin. 2016 Jun;8(2):423-36. doi: 10.1016/j.ccep.2016.02.006. Epub 2016 Mar 23. 23(15):8607. doi: 10.3390/ijms23158607.
3: Mounsey JP, DiMarco JP. Cardiovascular drugs. Dofetilide. Circulation. 2000 Nov 21;102(21):2665-70. doi: 10.1161/01.cir.102.21.2665. 58(6):1043-59. doi: 10.2165/00003495-199958060-00007. 41(4):396-401. doi: 10.1111/pace.13310. Epub 2018 Mar 12. 34(1):44-56. doi: 10.1345/aph.19185. 66(6):640-8. doi: 10.1016/j.ihj.2013.12.021. Epub 2014 Jan 7.
8: Subedi R, Dean RK, Dhamoon AS. Dofetilide-Induced Severe Hepatotoxicity. Am J Ther. 2018 Nov/Dec;25(6):e783-e784. doi: 10.1097/MJT.0000000000000793. 21(15):1204-6. doi: 10.1053/euhj.1999.2049.

合成参考文献


参考文献:10.1007/s10928-005-0048-9
摘要:Dokoumetzidis A, Aarons L. Propagation of Population Pharmacokinetic Information Using a Bayesian Approach: Comparison with Meta-Analysis. Journal of Pharmacokinetics and Pharmacodynamics. 2005 Aug;32(3-4):401–18. doi: 10.1007/s10928-005-0048-9.
参考文献:10.1007/s00210-011-0664-4
摘要:Goegelein H, Gautier P, Roccon A, O'Connor S, Ruetten H. Effects of the novel amiodarone-like compound SAR114646A on cardiac ion channels and ventricular arrhythmias in rats. Naunyn Schmiedebergs Arch Pharmacol. 2011 Sep;384(3):231–44. doi: 10.1007/s00210-011-0664-4.
参考文献:10.2174/092986711796642418
摘要:Szentandrássy N, Nagy D, Ruzsnavszky F, Harmati G, Bányász T, Magyar J, Szentmiklósi AJ, Nánási PP. Powerful technique to test selectivity of agents acting on cardiac ion channels: the action potential voltage-clamp. Curr Med Chem. 2011;18(24):3737–56. doi: 10.2174/092986711796642418.
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