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
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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合成参考文献
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