- Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity
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HCV NS5A inhibitors have demonstrated impressive in vitro potency profiles in HCV replicon assays and robust HCV RNA titer reduction in the clinic making them attractive components for inclusion in an all oral fixed dose combination regimen for the treatment of HCV infection. Herein, we describe research efforts that led to the discovery of a series of fused tricyclic core containing HCV NS5A inhibitors such as 24, 39, 40, 43, and 44 which have pan-genotype activity and are orally bioavailable in the rat.
- Yu, Wensheng,Coburn, Craig A.,Yang, De-Yi,Meinke, Peter T.,Wong, Michael,Rosenblum, Stuart B.,Chen, Kevin X.,Njoroge, George F.,Chen, Lei,Dwyer, Michael P.,Jiang, Yueheng,Nair, Anilkumar G.,Selyutin, Oleg,Tong, Ling,Zeng, Qingbei,Zhong, Bin,Ji, Tao,Hu, Bin,Agrawal, Sony,Xia, Ellen,Zhai, Ying,Liu, Rong,Kong, Rong,Ingravallo, Paul,Asante-Appiah, Ernest,Nomeir, Amin,Fells, James,Kozlowski, Joseph A.
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p. 3158 - 3162
(2016/06/13)
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- FUSED TRICYCLIC COMPOUNDS AND USE THEREOF FOR TREATING VIRAL DISEASES
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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.
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