- Monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and preparation method
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The invention discloses a monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and a preparation method. The monoglycosyl-containing heterocyclic compound has a chemical structure represented by a formula I shown in the description. The monoglycosyl-containing heterocyclic compound disclosed by the invention can be used for effectively inhibiting protease of the hepatitis C viruses and treating infection of the hepatitis C viruses (HCV).
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- HEPATITIS C VIRUS INHIBITORS AND USES THEREOF IN PREPARATION OF DRUGS
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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.
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- Synthesis and evaluation of novel HCV replication inhibitors
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Abstract: Direct acting antiviral agents to cure hepatitis C virus (HCV) infection has emerged as the gold standard therapy. Along with protease inhibitors, nucleoside polymerase inhibitors and non-nucleoside polymerase inhibitors, the inhibition of NS5a
- McGowan, David C.,Khamlichi, Mourad D.,De Groot, Alex,Pauwels, Frederik,Delouvroy, Frédéric,Van Emelen, Kristof,Simmen, Kenneth,Raboisson, Pierre
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p. 475 - 481
(2017/05/29)
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- SPIRO COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
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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.
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- Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: From lead to clinical compound
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Rapid clinical progress of hepatitis C virus (HCV) replication inhibitors, including these selecting for resistance in the NS5A region (NS5A inhibitors), promises to revolutionize HCV treatment. Herein, we describe our explorations of diverse spiropyrrolidine motifs in novel NS5A inhibitors and a proposed interaction model. We discovered that the 1,4-dioxa-7-azaspiro[4.4]nonane motif in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genotype 1b L31V and Y93H mutants. Consistent with this, 41H potently suppressed HCV RNA in the 20-day RNA reduction assay. Pharmacokinetic and safety data supported further progression of 41H to the clinic.
- Kazmierski, Wieslaw M.,Maynard, Andrew,Duan, Maosheng,Baskaran, Sam,Botyanszki, Janos,Crosby, Renae,Dickerson, Scott,Tallant, Matthew,Grimes, Rick,Hamatake, Robert,Leivers, Martin,Roberts, Christopher D.,Walker, Jill
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p. 2058 - 2073
(2014/04/03)
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- NOVEL HEPATITIS C VIRUS INHIBITORS
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The invention provides compounds of formula (I): wherein Rings A and A' are independently 5-membered optionally substituted aromatic heterocycles; Q is C(=O)NR1R1' or formula U is C(R4)2, O, S, S(=O)2, C(R4)2C(R4)2, CH2O, OCH2, CH2S, SCH2, CH2S(=O)2, S(=O)CH2 or C=C(Ru )2; X is CH2, CHR12, CR12R12, O, S, S(=O)2 or NRx; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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- Synthesis and evaluation of non-dimeric HCV NS5A inhibitors
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Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000).
- Amblard, Franck,Zhang, Hongwang,Zhou, Longhu,Shi, Junxing,Bobeck, Drew R.,Nettles, James H.,Chavre, Satish,McBrayer, Tamara R.,Tharnish, Philip,Whitaker, Tony,Coats, Steven J.,Schinazi, Raymond F.
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p. 2031 - 2034
(2013/05/09)
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- NOVEL INHIBITORS OF HEPATITIS C VIRUS
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The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
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- SUBSITUTED ALIPHANES, CYCLOPHANES, HETERAPHANES, HETEROPHANES, HETERO-HETERAPHANES AND METALLOCENES USEFUL FOR TREATING HCV INFECTIONS
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The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I [in-line-formulae]D-M-D??(Formula I)[/in-line-formulae] useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/ and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
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Page/Page column 15; 16
(2012/12/13)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of Formula (I) and (II) wherein R1, R2, R3, R6, A and A' are defined herein. The compounds are useful as inhibitors of the function of NS5A protein encoded by HCV for the treatment of hepatitis C viral infection.
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Page/Page column 41-42
(2012/05/04)
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- HEPATITIS C VIRUS INHIBITORS
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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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
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Page/Page column 92
(2011/04/18)
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- HEPATITIS C VIRUS INHIBITORS
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The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
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- FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
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Page/Page column 106-107
(2010/12/17)
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- ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
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The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
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Page/Page column 89
(2010/12/26)
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