- Hepatitis C virus inhibitors
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Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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Page/Page column 608; 609
(2017/01/23)
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- 5-Methoxyquinoline derivatives as a new class of EZH2 inhibitors
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A series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also showed good anti-viability activities against two tumor cell lines. Due to the low molecular weight and the fact that no quinoline derivative has been reported as an EZH2 inhibitor, this compound could serve as a lead compound for further optimization.
- Xiang, Pu,Jie, Hui,Zhou, Yang,Yang, Bo,Wang, Hui-Juan,Hu, Jing,Hu, Jian,Yang, Sheng-Yong,Zhao, Ying-Lan
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p. 7620 - 7636
(2015/05/20)
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- Syntheses and fluorescent properties of 6-methoxy-2-oxoquinoline-3,4- dicarbonitriles and 6,7-dimethoxy-2-oxoquinoline-3,4-dicarbonitriles
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4-Chlorocarbostyrils 3, 12, 17, 24, 26 with methoxy substituents in 6, 7, or 6,7-position react with potassium cyanide in a p-toluenesulfinate mediated reaction either to the highly fluorescent and stable 2-oxoquinoline-3,4- dicarbonitriles 6, 27, 29, 30 or at slightly lower temperatures to 4-monocarbonitriles 5, 13, 18. 4-Chlorocarbostyril 3 and lithium p-toluenesulfinate gave pure 4-toluenesulfonylquinolone 4, which reacted with potassium cyanide either to monocarbonitrile 5 or dicarbonitrile 6, depending on the reaction conditions. 4-Trifluoromethylquinolones 9 and 19 were prepared for fluorescence comparison from the appropriate methoxyaniline and 4,4,4-trifluoroacetoacetate. The fluorescence properties such as emission wavelengths and quantum yields of 6-methoxyderivatives 4, 5, 6, 9, 13 were studied and compared with those of 7-methoxy derivatives 18, 19 and 6,7-dimethoxyderivatives 27, 28, 29, 30. 6,7-Dimethoxy derivatives show best results, showing long-waved fluorescence spectra up to 520 nm and acceptable quantum yields up to 0.46 for 3,4-dicyano derivative 27 excited at 440 nm in acetonitrile.
- Enoua, Guy Crépin,Lahm, Günther,Uray, Georg,Stadlbauer, Wolfgang
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p. E263-E275
(2014/11/07)
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- Hepatitis C Virus Inhibitors
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Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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Page/Page column
(2013/05/21)
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- STEREOSELECTIVE METHODS, CATALYSTS AND INTERMEDIATES FOR THE SYNTHESIS OF (-)-NUTLIN-3 AND RELATED COMPOUNDS
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The present invention provides methods and intermediates are provided for the preparation of (?)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use
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Page/Page column 15
(2012/04/18)
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- PROCESS FOR PREPARING BROMO-SUBSTITUTED QUINOLINES
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Disclosed are methods for the preparation of bromo-substituted quinolines of the formula (I) where R is aryl, heteroaryl, alkyl, alkenyl or alkynyl, which are useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections: Formula (I).
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Page/Page column 10-11
(2010/11/18)
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- HCV INHIBITORS
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The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 71-72
(2008/06/13)
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- A convenient synthesis of 8,9,10,11-tetrahydrodibenzo[b,h] [1,6]naphthyridin-6(5H)ones
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Substituted 8,9,10,11-tetrahydrodibenzo[b,h][1,6]naphthyridin-6(5H)ones (5) have been synthesized by the condensation of 4-amino-3-formylquinolin-2(1H)ones (4) with cyclohexanone in presence of acetic acid and sulphuric acid. The precusors have been obtained by the animation of 4-chloro-3-formylquinolin-2(1H)ones (3).
- Arul Prakash,Rajendran
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p. 353 - 358
(2007/10/03)
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- 2,4-Dihalogenoquinolines. Synthesis, Orientation Effects and 1H and 13C NMR Spectral Studies
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Isomer ratios for the syntheses of 2,4-dichloroquinolines from meta-substituted and 3,4-disubstituted anilines are reported, a synthesis of 2,4-dibromoquinoline 1b is also described.The structures of certain bromination products 17 and 1f obtained from 4-hydroxy-2-quinolone have been revised.A thorough study of the 1H and 13C NMR spectra of a series of 2,4-dihalogenoquinolines is presented and the effects of the halogen substituents on JCH couplings are highlighted.
- Osborne, Alan G.,Buley, Jill M.,Clarke, Helen,Dakin, Rachel C. H.,Price, Paul I.
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p. 2747 - 2756
(2007/10/02)
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