- NOVEL BENZIMIDAZOLE DERIVATIVES
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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.
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Paragraph 0222-0224; 0241; 0242; 0258; 0259
(2020/01/22)
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- PROCESS FOR THE SYNTHESIS OF RAVIDASVIR
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A process for the synthesis of ravidasvir and intermediates useful in the preparation thereof are disclosed.
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- Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection
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A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification of 39 (ledipasvir, GS-5885). Compound 39 (GT1a replicon EC50 = 31 pM) has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid >3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. 39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.
- Link, John O.,Taylor, James G.,Xu, Lianhong,Mitchell, Michael,Guo, Hongyan,Liu, Hongtao,Kato, Darryl,Kirschberg, Thorsten,Sun, Jianyu,Squires, Neil,Parrish, Jay,Keller, Terry,Yang, Zheng-Yu,Yang, Chris,Matles, Mike,Wang, Yujin,Wang, Kelly,Cheng, Guofeng,Tian, Yang,Mogalian, Erik,Mondou, Elsa,Cornpropst, Melanie,Perry, Jason,Desai, Manoj C.
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p. 2033 - 2046
(2014/04/03)
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- SOLID FORMS COMPRISING INHIBITORS OF HCV NS5A, COMPOSITIONS THEREOF, AND USES THEREWITH
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This invention relates to: -a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) composition comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and composition; (e) method of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
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- BENZIMIDAZOLE-IMIDAZOLE DERIVATIVES
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Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R' are, each independently,-CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
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Page/Page column 51
(2011/06/11)
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- CHEMICAL COMPOUNDS
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Disclosed are compounds of Formula II. Also disclosed are salts of the compounds, pharmaceutical compositions comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
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- NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
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- HEPATITIS C VIRUS INHIBITORS
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The present invention discloses compounds 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.
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Page/Page column 119
(2010/09/17)
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