1246471-95-3Relevant academic research and scientific papers
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.
Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742
Yu, Wensheng,Zhou, Guowei,Coburn, Craig A.,Zeng, Qingbei,Tong, Ling,Dwyer, Michael P.,Hu, Bin,Zhong, Bin,Hao, Jinglai,Ji, Tao,Zan, Shuai,Chen, Lei,Mazzola, Robert,Kim, Jae-Hun,Sha, Deyou,Selyutin, Oleg,Rosenblum, Stuart B.,Lavey, Brian,Nair, Anilkumar G.,Heon Kim, Seong,Keertikar, Kerry M.,Rokosz, Laura,Agrawal, Sony,Liu, Rong,Xia, Ellen,Zhai, Ying,Curry, Stephanie,McMonagle, Patricia,Ingravallo, Paul,Asante-Appiah, Ernest,Chen, Shiying,Kozlowski, Joseph A.
, p. 4851 - 4856 (2016/09/13)
As part of an ongoing effort in NS5A inhibition at Merck we now describe our efforts for introducing substitution around the tetracyclic indole core of MK-8742. Fluoro substitution on the core combined with the fluoro substitutions on the proline ring improved the potency against GT1a Y93H significantly. However, no improvement on GT2b potency was achieved. Limiting the fluoro substitution to C-1 of the tetracyclic indole core had a positive impact on the potency against the resistance associated variants, such as GT1a Y93H and GT2b, and the PK profile as well. Compounds, such as 62, with reduced potency shifts between wild type GT1a to GT2b, GT1a Y93H, and GT1a L31V were identified.
TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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, (2012/04/17)
The present invention relates to novel Tetracyclic Indole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprisingat least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing HCV infection in a patient.
TETRACYCLIC INDOLE DERIVATIVES FOR TREATING HEPATITIS C VIRUS INFECTION
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, (2012/04/17)
Tetracyclic indole derivatives of formula (I), pharmaceutically acceptable salts and the pharmaceutical compositions thereof are provided, wherein A, A', G, R1, R15, U, V, V, W, W, X, X', Y, Y' are as defined in the invention. Use of these derivatives for treating hepatitis C virus (HCV) infection is also provided.
INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Page/Page column 147, (2010/11/04)
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.
