1241377-74-1Relevant articles and documents
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)
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.
Industrial preparation method of 6-bromonaphthalene-1, 2-diamine
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Paragraph 0004-0005; 0016, (2021/04/21)
The invention discloses an industrial preparation method of 6-bromonaphthalene-1, 2-diamine. The method comprises the following steps of: S1, making a compound III react with acetic anhydride in the presence of alkali and a catalyst to obtain a compound IV; S2, in the presence of acetic anhydride and nitric acid, taking acetic acid as a reaction solvent, performing reacting and purifying on the compound IV obtained in the step S1 to generate a compound V; S3, adding the compound V obtained in the above step into a solvent for dissolving the compound V, then adding a metal reducing agent and an ammonium chloride solution, heating to carry out a reaction for 6h, performing centrifugal filtering after finishing the reaction to obtain a filtrate, washing the filtrate with a sodium chloride solution, and performing concentrating to obtain a compound VI; and S4, adding the compound VI obtained in the previous step into a methanol solution, dropwise adding strong acid, replacing the solvent after finishing the reaction, performing crystallizing and filtering to obtain a compound 8. According to the method, the process is optimized, large-scale production can be achieved, applied materials are all commercial reagents, the cost is reduced, and the operation convenience is improved.
COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS AND PHARMACEUTICAL USES THEREOF
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Paragraph 00248; 00252, (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
PESTICIDE COMPOUNDS
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Page/Page column 270, (2015/02/02)
The present invention relates to novel compounds of the formula I and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein C1 is C or CH; C2 is C or CH; A1 is N or C; A2 is N, C(R2), N(R3), O, S or C(R4,R5); and A3 is N, O, S, N(R6), C(R7) or C(R8,R9); where one or two non-adjacent bonds in the 5-membered ring formed by C1, C2, A1, A2 and A3 are double bonds, while the others are single bonds, provided that the bond between A1 and A2 or the bond between A1 and C1 or the bond between A2 and A3 or the bond between C1 and C2 or the bond between A3 and C2 is a double bond further provided that at least one of A1, A2 and A3 is N, N(R3) or N(R6), and where Ar, R1, R2, R3, R4,R5, R6, R7, R8, R9 and (R)k are as defined in the claims and in the description, which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
FUSED TRICYCLIC SILYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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Paragraph 0336; 0337, (2015/12/08)
no abstract published
HEPATITIS C VIRUS INHIBITORS
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Page/Page column 156, (2012/02/15)
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
FUSED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 76, (2011/08/04)
The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
FUSED TRICYCLIC COMPOUNDS AND DERIVATIVES THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 109-110, (2011/06/23)
The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
2,3(1H,4H)quinoxalinedione
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, (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.