1208007-67-3Relevant academic research and scientific papers
NOVEL BENZIMIDAZOLE DERIVATIVES
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Paragraph 0184; 0185, (2020/01/22)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
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Paragraph 0368; 0370, (2018/08/20)
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
HEPATITIS C VIRUS INHIBITORS AND USES THEREOF IN PREPARATION OF DRUGS
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Paragraph 0155; 0157, (2017/12/17)
A series of hepatitis C virus (HCV) inhibitors and compositions and applications thereof in the preparation of drugs for treating chronic HCV infection. Especially, a series of compounds that are used as NS5A inhibitors, and compositions and uses thereof in the preparations of drugs.
As hepatitis c inhibitor spiro compound and its use in medicine
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Paragraph 0760; 0788; 0789, (2017/12/28)
The invention provides a spiro compound serving as a hepatitis c inhibitor and application thereof in a medicine. The compound is a compound as shown in a formula (I) or a stereisomer, a geometric isomer, a tautomer, nitric oxide, an aquo-complex, a solvate, a metabolite, pharmaceutically acceptable salt or prodrug of the compound as shown in the formula (I). The invention also provides a pharmaceutical composition containing the compound, application of the compound and the pharmaceutical composition in inhibition of HCV (Hepatitis C Virus) copy and HCV virus protein, as well as the application of the compound and the pharmaceutical composition in prevention, handling, treatment or relieving of HCV infection or hepatitis c disease for a patient. The formula I is as shown in the specification.
9,9,10,10-TETRAFLUORO-9,10-DIHYDROPHENANTHRENE HEPATITIS C VIRUS INHIBITOR AND APPLICATION THEREOF
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Paragraph 0236-0238, (2016/10/31)
The present invention belongs to the field of chemical pharmaceuticals, and specifically relates to compounds represented by formula I having a 9,9,10,10-tetrafluoro-9,10-dihydrophenanthrene structure and being able to inhibit hepatitis C virus activity, or a pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug of said compounds, a pharmaceutical composition containing said compounds, and an application of said compounds or composition in the preparation of a drug. The compounds of the present invention have a good HCV inhibitory effect.
Fused tricyclic hepatitis virus inhibitor and application thereof
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Paragraph 0179; 0180; 0181; 0182, (2016/12/26)
The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
SPIRO COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
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, (2015/11/09)
Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
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Paragraph 0679; 0709; 0710; 0711; 0712, (2015/03/28)
Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
Hepatitis C virus NS5A replication complex inhibitors. Part 6: Discovery of a novel and highly potent biarylimidazole chemotype with inhibitory activity toward genotypes 1a and 1b replicons
Belema, Makonen,Nguyen, Van N.,Romine, Jeffrey L.,St. Laurent, Denis R.,Lopez, Omar D.,Goodrich, Jason T.,Nower, Peter T.,O'Boyle, Donald R.,Lemm, Julie A.,Fridell, Robert A.,Gao, Min,Fang, Hua,Krause, Rudolph G.,Wang, Ying-Kai,Oliver, A. Jayne,Good, Andrew C.,Knipe, Jay O.,Meanwell, Nicholas A.,Snyder, Lawrence B.
, p. 1995 - 2012 (2014/04/03)
A medicinal chemistry campaign that was conducted to address a potential genotoxic liability associated with an aniline-derived scaffold in a series of HCV NS5A inhibitors with dual GT-1a/-1b inhibitory activity is described. Anilides 3b and 3c were used
The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile - Part 1
Tran, Thien Duc,Wakenhut, Florian,Pickford, Chris,Shaw, Stephen,Westby, Mike,Smith-Burchnell, Caroline,Watson, Lesa,Paradowski, Michael,Milbank, Jared,Brimage, Rebecca A.,Halstead, Rebecca,Glen, Rebecca,Wilson, Craig P.,Adam, Fiona,Hay, Duncan,Chiva, Jean-Yves,Nichols, Carly,Blakemore, David C.,Gardner, Iain,Dayal, Satish,Pike, Andrew,Webster, Rob,Pryde, David C.
, p. 1378 - 1386 (2014/07/21)
Nonstructural protein 5A (NS5A) represents a novel target for the treatment of hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol-Myers-Squibb, is a potent NS5A inhibitor currently under investigation in phase 3 clinical trials. While the performance of daclatasvir has been impressive, the emergence of resistance could prove problematic and as such, improved analogues are being sought. By varying the biphenyl-imidazole unit of daclatasvir, novel inhibitors of HCV NS5A were identified with an improved resistance profile against mutant strains of the virus while retaining the picomolar potency of daclatasvir. One compound in particular, methyl ((S)-1-((S)-2-(4-(4-(6-(2-((S)-1-((methoxycarbonyl)-L-valyl)pyrrolidin-2-yl) -1H-imidazol-5-yl)quinoxalin-2-yl)phenyl)-1H-imidazol-2-yl)pyrrolidin-1-yl) -3-methyl-1-oxobutan-2-yl)carbamate (17), exhibited very promising activity and showed good absorption and a long predicted human pharmacokinetic half-life. This compound represents a promising lead that warrants further evaluation. Resisting resistance: An investigation into the anti-hepatitis C virus (HCV) replicon activity of a series of biaryl-linked pyrrolidine NS5A inhibitors explored a diverse range of core structure modifications as key determinants of antiviral activity and susceptibility to common resistance mutations. Further evaluation of several core structure designs identified a compound with excellent pharmacokinetics, suitable for once daily dosing.
