CAS: 1370468-36-2; Dimethyl ((2S,2'S)-((2S,2'S)-2,2'-(5,5'-((S)-6-Phenyl-6H-Benzo[5,6][1,3]Oxazino[3,4-A]Indole-3,10-Diyl)Bis(1H-Imidazole-5,2-Diyl))Bis(Pyrrolidine-2,1-Diyl))Bis(3-Methyl-1-Oxobutane-2,1-Diyl))Dicarbamate

该化合物是主要用于治疗丙型肝炎病毒(HCV)感染的抗病毒药物,它作为NS5A抑制剂,针对的是病毒复制和组装所必需的特定蛋白质.Elbasvir经常与其他抗病毒剂结合,以提高其功效,扩大各种HCV基因型的治疗范围.该物质的特点在于它对NS5A蛋白具有高度的威力和选择性,有助于有效抑制病毒负荷.在化学特性方面,Elbasvir具有复杂的分子结构,包括多种功能组,有助于其药理活动.它通常通过口服,在胃肠道中被吸收.药物的安全特征一般是有利的,具有常见的副作用,包括疲劳和头痛,但监测潜在的药物相互作用至关重要,特别是在混合疗法中使用时.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    专利信息


    专利号:US-9790207-B2
    优先权日:2015-09-04
    标题 :Pan-genomic inhibitors of NS5A protein encoded by HCV, pharmaceutical compositions, intermediates for inhibitor synthesis, and their synthesis and application methods
    发明人:IVACHTCHENKO ALEXANDRE VASILIEVICH; MITKIN OLEG DMITRIEVICH
    权利人:IVACHTCHENKO ALEXANDRE VASILIEVICH; IVASHCHENKO ANDREY ALEXANDROVICH; SAVCHUK NIKOLAY FILIPPOVICH; ALLA CHEM LLC
    摘要:Compound represented by formula 1: n nor a pharmaceutically acceptable salt, a hydrate, a crystalline form, or a stereoisomer thereof, wherein:n nR1 is hydrogen, tert-butoxycarbonyl,n n nwhere R11 is an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 3 -C 6 cycloalkyl, or an optionally substituted C 1 -C 6 alkyloxy, and arrows (â†?) indicate the position of substituents attachment;n nR2 is hydrogen, halogen, or C 1 -C 4 alkyl;n nR3 is an optionally substituted aryl, an optionally substituted aryloxy, an optionally substituted arylsulfanyl, an optionally substituted arylamino, or an optionally substituted nitrogen hetaryl;n n n n n n n n n n n n n where R41 is an optionally substituted C 1 -C 6 alkyl, an optionally substituted C 3 -C 6 cycloalkyl, or an optionally substituted C 1 -C 6 alkyloxy; X is buta-1,3-diynylene or 1,4-phenylene; arrows (â†?) indicate the position of substituents attacment.

    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:CN-107021968-A
    优先权日:2017-05-25
    标题:A method for the synthesis of indole compounds by oxidative dehydrogenation of indoline compounds catalyzed by multi-substituted BODIPY organic photocatalysts

    专利号:CN-107021968-B
    优先权日:2017-05-25
    标题 :A method for the synthesis of indole compounds by oxidative dehydrogenation of indoline compounds catalyzed by multi-substituted BODIPY organic photocatalysts

    专利号:EA-034084-B1
    优先权日:2015-09-04
    标 题:Pan-Genomic Protein Inhibitors of NS5A Hepatitis C Virus, Pharmaceutical Compositions, Intermediate Products for the Synthesis of Inhibitors and Methods for Their Production and Use

    专利号:RU-2669919-C1
    优先权日:2015-09-04
    标题 :Pan-genomic inhibitors of the hepatitis c virus protein ns5a, pharmaceutical compositions, intermediates for the synthesis of inhibitors, and methods for their preparation and use
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    主要参考文献


    1: Morikawa K, Nakamura A, Shimazaki T, Sakamoto N. Safety and efficacy of elbasvir/grazoprevir for the treatment of chronic hepatitis C: current evidence. Drug Des Devel Ther. 2018 Sep 5;12:2749-2756. doi: 10.2147/DDDT.S133697. eCollection 2018. Review.
    2: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500816/ doi: 10.2147/HMER.S130103. eCollection 2018. Review.
    4: Ahmed H, Abushouk AI, Menshawy A, Attia A, Mohamed A, Negida A, Abdel-Daim MM. Meta-Analysis of Grazoprevir plus Elbasvir for Treatment of Hepatitis C Virus Genotype 1 Infection. Ann Hepatol. 2018 January-February;17(1):18-32. doi: 10.5604/01.3001.0010.7532. Review. doi: 10.2146/ajhp160558. Review. doi: 10.1007/s40265-017-0739-8. Review. doi: 10.1177/1756283X16671293. Epub 2016 Oct 17. Review.

    合成参考文献


    摘要:Goetzke#, F. W.; Modicom#, F.; Fletcher, S. P., Science of Synthesis, (2022) , 364.
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