131707-40-9Relevant academic research and scientific papers
COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS AND PHARMACEUTICAL USES THEREOF
-
, (2016/09/26)
The invention provides compounds as hepatitis C virus inhibitors and pharmaceutical uses thereof. Specifically, the invention provides compounds of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a
Discovery of potent macrocyclic HCV NS5A inhibitors
Yu, Wensheng,Vibulbhan, Bancha,Rosenblum, Stuart B.,Martin, Gregory S.,Vellekoop, A. Samuel,Holst, Christian L.,Coburn, Craig A.,Wong, Michael,Selyutin, Oleg,Ji, Tao,Zhong, Bin,Hu, Bin,Chen, Lei,Dwyer, Michael P.,Jiang, Yueheng,Nair, Anilkumar G.,Tong, Ling,Zeng, Qingbei,Agrawal, Sony,Carr, Donna,Rokosz, Laura,Liu, Rong,Curry, Stephanie,McMonagle, Patricia,Ingravallo, Paul,Lahser, Fred,Asante-Appiah, Ernest,Fells, James,Kozlowski, Joseph A.
, p. 3793 - 3799 (2016/07/21)
HCV NS5A inhibitors have demonstrated impressive in vitro virologic 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 (FDC) regimen for the treatment of HCV infection. Merck's effort in this area identified MK-4882 and MK-8325 as early development leads. Herein, we describe the discovery of potent macrocyclic NS5A inhibitors bearing the MK-8325 or MK-4882 core structure.
2,3(1H,4H)quinoxalinedione
-
, (2008/06/13)
2,3(1H,4H)-quinoxalinediones of the formula I STR1 where R1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R3, --CO--O--R3 or --CO--NH--R3, where R3 is hydrogen, C1 -C4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R1 can have up to three of the following substituents: C1 -C4 -alkyl, C1 -C4 -haloalkyl, C1 -C4 -alkoxy, C1 -C4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R3 and --CO--NH--R3 ; R2 is 1-pyrrolyl which can have up to two of the following substituents: C1 -C4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R3, --CO--NH--R3, --CH2 --O--R3, --O--R3 and --CH=NO--R3 R radicals are identical or different and are the following: C1 -C4 -alkyl, C1 -C4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R3 and --CO--NH--R3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' STR2 where R1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
