CAS: 1216941-48-8; (2R,6S,13As,14Ar,16As,Z)-N-(Cyclopropylsulfonyl)-6-(5-Methylpyrazine-2-Carboxamido)-5,16-Dioxo-2-(Phenanthridin-6-Yloxy)-1,2,3,6,7,8,9,10,11,13A,14,15,16,16A-Tetradecahydrocyclopropa[e]Pyrrolo[1,2-A][1,4]Diazacyclopentadecine-14A(5H)-Carboxamide

5-甲基吡嗪-2-羧酸,Paritaprevir Metabolite M25置于n,N-二异丙基乙胺体系中,用 乙腈 用作溶剂,以11.15 Kg的收率获得帕利普韦
参考文献:一种原料药帕利普韦的制备方法
标题:一种原料药帕利普韦的制备方法
摘要:本发明公开了一种原料药帕利普韦的制备方法,包括中间体1‑(4‑(叔丁基苯基)‑2,5‑双(4‑硝基苯基))吡咯烷中双硝基的还原反应s1,双氨基的脯氨酸肽耦合反应s2和吡咯烷氨基的脱保护反应s3以及吡咯烷氨基的缬氨酸肽耦合反应s4.本发明原料药帕利普韦的制备方法中采用中间体ⅰ作为原料,经闭环,氨基脱保护和酰胺化制得帕利普韦,步骤简单,反应条件温和,中间产物稳定性高,中间体分离收率高,反应体系溶剂均可实现回收再利用,上述因素均有利于工业化大规模生产.

专利信息

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-12404246-B1
优先权日:2024-10-01
标 题:2-aminomethylimidazole mimics of NS4A and their effect thereof on hepatitis C virus NS3 protease
发明人：BARADWAN MOHAMMED A; OMAR ABDELSATTAR M; ELFAKY MAHMOUD A; EL-ARABY MOUSTAFA E; SOROR SAMEH H
权利人:BARADWAN MOHAMMED A; OMAR ABDELSATTAR M; ELFAKY MAHMOUD A; EL ARABY MOUSTAFA E; SOROR SAMEH H; UNIV KING ABDULAZIZ
摘要:Chronic hepatitis C is a global health problem affecting large number of people and leads to mortalities and morbidities. In this invention, new compounds belonging to 2-substituted-1H-imidazole-4-carboxamide derivatives (Formula I) intended for use in the treatment of hepatitis C are disclosed. The compounds interfere with the important viral peptide NS4A co-enzyme function. The described art includes chemical synthesis, spectral confirmation and binding assays with NS3 protein.

专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人：WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.