1240893-76-8Relevant articles and documents
INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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, (2019/05/15)
The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
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, (2018/08/20)
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
9,9,10,10-TETRAFLUORO-9,10-DIHYDROPHENANTHRENE HEPATITIS C VIRUS INHIBITOR AND APPLICATION THEREOF
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, (2016/10/31)
The present invention belongs to the field of chemical pharmaceuticals, and specifically relates to compounds represented by formula I having a 9,9,10,10-tetrafluoro-9,10-dihydrophenanthrene structure and being able to inhibit hepatitis C virus activity, or a pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug of said compounds, a pharmaceutical composition containing said compounds, and an application of said compounds or composition in the preparation of a drug. The compounds of the present invention have a good HCV inhibitory effect.
Fused tricyclic hepatitis virus inhibitor and application thereof
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, (2016/12/26)
The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers
Giroux, Simon,Bilimoria, Darius,Cadilhac, Caroline,Cottrell, Kevin M.,Denis, Francois,Dietrich, Evelyne,Ewing, Nigel,Henderson, James A.,L'Heureux, Lucille,Mani, Nagraj,Morris, Mark,Nicolas, Olivier,Reddy, T. Jagadeeswar,Selliah, Subajini,Shawgo, Rebecca S.,Xu, Jinwang,Chauret, Nathalie,Berlioz-Seux, Francoise,Chan, Laval C.,Das, Sanjoy K.,Grillot, Anne-Laure,Bennani, Youssef L.,Maxwell, John P.
, p. 936 - 939 (2015/02/19)
The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the aromatic character of the linker to achieve high genotype 1a potency.
FUSED TRICYCLIC SILYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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, (2015/12/08)
no abstract published
Discovery of MK-8742: An HCV NS5A inhibitor with broad genotype activity
Coburn, Craig A.,Meinke, Peter T.,Chang, Wei,Fandozzi, Christine M.,Graham, Donald J.,Hu, Bin,Huang, Qian,Kargman, Stacia,Kozlowski, Joseph,Liu, Rong,McCauley, John A.,Nomeir, Amin A.,Soll, Richard M.,Vacca, Joseph P.,Wang, Dahai,Wu, Hao,Zhong, Bin,Olsen, David B.,Ludmerer, Steven W.
, p. 1930 - 1940 (2014/01/06)
The NS5A protein plays a critical role in the replication of HCV and has been the focus of numerous research efforts over the past few years. NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays, making them attractive components for inclusion in all oral combination regimens. Early work in the NS5A arena led to the discovery of our first clinical candidate, MK-4882 [2-((S)-pyrrolidin-2-yl)-5-(2-(4-(5-((S)-pyrrolidin- 2-yl)-1H-imidazol-2-yl)phenyl)benzofuran-5-yl)-1H-imidazole]. While preclinical proof-of-concept studies in HCV-infected chimpanzees harboring chronic genotype 1 infections resulted in significant decreases in viral load after both single- and multiple-dose treatments, viral breakthrough proved to be a concern, thus necessitating the development of compounds with increased potency against a number of genotypes and NS5A resistance mutations. Modification of the MK-4882 core scaffold by introduction of a cyclic constraint afforded a series of tetracyclic inhibitors, which showed improved virologic profiles. Herein we describe the research efforts that led to the discovery of MK-8742, a tetracyclic indole-based NS5A inhibitor, which is currently in phase 2b clinical trials as part of an all-oral, interferon-free regimen for the treatment of HCV infection. Effective treatment of chronic hepatitis C with direct-acting antivirals will require combination therapy with multiple agents that target different steps in the viral replication cycle and impose a high barrier to resistance. MK-8742 is a potent inhibitor of hepatitis C virus non-structural protein 5A (HCV NS5A) that is being developed as a component of an once-daily, all-oral, interferon-free regimen for the treatment of chronic HCV infection. Copyright
FUSED TRICYCLIC COMPOUNDS AND USE THEREOF FOR TREATING VIRAL DISEASES
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Example 3, (2012/02/01)
Fused tricyclic compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein X1, X2, X3, X4, Y1, Y2, M1, M2, Ra, Rb, R1, R2 and R6 are as defined in the description. Compositions comprising at least one fused tricyclic compound and methods of using the fused tricyclic compounds for treating or preventing HCV infection in a patient are also disclosed.
TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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Page/Page column 55-56, (2012/10/07)
The present invention discloses tetracyclic xanthene derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b, and R2 are as defined herein. The present invention also discloses compositions comprising at least one tetracyclic xanthene derivative, and methods of using the tetracyclic xanthene derivatives for treating or preventing HCV infection in a patient.
FUSED TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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, (2012/04/17)
The present invention discloses novel Fused Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', W, W', X, X', Y and Y' are as defined herein. The present invention also discloses compositions comprising at least one Fused Tetracyclic Heterocycle Compound, and methods of using the Fused Tetracyclic Heterocycle Compounds for treating or preventing HCV infection in a patient.