1242087-93-9

Usage

Uses

Used in Pharmaceutical Industry:
Ravidasvir, PPI-668 is used as an antiviral agent for the treatment of hepatitis C virus (HCV) infections. It targets the NS5A protein, inhibiting the replication of the virus and leading to high rates of sustained virologic response in patients. This makes it a promising treatment option for those who have failed previous therapies or have difficult-to-treat genotypes.
Used in Virology Research:
In the field of virology, ravidasvir, PPI-668 is used as a research tool to study the mechanisms of HCV replication and the effectiveness of direct-acting antivirals in combating the virus. Its potent activity against various HCV genotypes aids in understanding the genetic diversity of the virus and the development of broad-spectrum antiviral therapies.
Used in Combination Therapies:
Ravidasvir, PPI-668 is used in combination with other antiviral drugs to enhance the treatment of hepatitis C virus infections. The synergistic effect of this combination therapy increases the overall efficacy and helps overcome drug resistance, leading to improved patient outcomes.
Used in Drug Resistance Studies:
Ravidasvir, PPI-668 is utilized in studies focused on drug resistance in HCV, as understanding the development of resistance to this antiviral agent can inform the design of more effective treatment strategies and the development of new drugs to combat resistant strains of the virus.

Upstream product

• 1228552-12-2 methyl (S)-1-((S)-2-(5-(6-bromonaphthalen-2-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-ylcarbamate 
• 1228553-66-9 methyl (S)-3-methyl-1-oxo-1-((S)-2-(5-(6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)naphthalen-2-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)butan-2-ylcarbamate 
• 1228552-45-1 methyl (S)-1-((S)-2-(6-bromo-1H-benzo[d]imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-yl-carbamate 
• 59378-82-4 N-(tert-butoxycarbonyl)pyrrolidine-2-carboxaldehyde 
• 1228633-23-5 C₂₈H₂₈N₆ 
• 111398-44-8 N-methoxycarbonyl-L-valine 
• 181827-47-4 (2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidine-2-carboxylic acid 
• 1228552-50-8 (((S)-3-methyl-1-oxo-1-((S)-2-(6-(4,4,5,5-tetramethyl-1,3,2-dioxolo)ethylpentocycloboran-2-yl)-1H-benzo[d]imidazol-2-yl)pyrrolidin-1-yl)propan-2-yl)carbamate 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 1228552-34-8 C₃₈H₄₄N₆O₄ 
• 1208007-67-3 (S)-tert-butyl 2-(6-bromo-1H-benzo[d]imidazol-2-yl)pyrrolidine-1-carboxylate 
• 1575-37-7 4-Bromo-benzene-1,2-diamine 
• 1228633-23-5 C₂₈H₂₈N₆ 
• 1228552-26-8 (S)-tert-butyl 2-(5-(6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)naphthalen-2-yl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate 

Relevant academic research and scientific papers

NOVEL BENZIMIDAZOLE DERIVATIVES

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.

PROCESS FOR THE SYNTHESIS OF RAVIDASVIR

A process for the synthesis of ravidasvir and intermediates useful in the preparation thereof are disclosed.

Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection

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.

SOLID FORMS COMPRISING INHIBITORS OF HCV NS5A, COMPOSITIONS THEREOF, AND USES THEREWITH

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.

BENZIMIDAZOLE-IMIDAZOLE DERIVATIVES

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.

CHEMICAL COMPOUNDS

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.

NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION

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.

HEPATITIS C VIRUS INHIBITORS

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.