The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Hepatitis C virus inhibitors

The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase

An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.

Viral Polymerase Inhibitors

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Modulators of atp-binding cassette transporters

The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease

The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infection in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).

Hepatitis C inhibitor peptide analogs

Nature 426, 186–189 (2003). In this Letter, the ‘Competing interests statement’ should be corrected to: ‘The authors declare competing financial interests: R.E.S. was the clinical investigator and received an honorarium from Boehringer Ingelheim. All the other authors are or were employees of Boehringer Ingelheim.

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corrigendum: An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

PROBLEM TO BE SOLVED: To provide a novel inhibitor of HCV NS5B polymerase. SOLUTION: The inhibitor of HCV NS5B polymerase is an isomer of a compound represented by formula (I) (wherein A is O, S, NR 1 or CR 1 ; R 1 is selected from H, a halogen and the like; a dot line is a single bond or a double bond; R 2 is selected from H, a halogen, R 21 , OR 21 , SR 21 , COOR 21 , SO 2 N(R 22 ) 2 , N(R 22 ) 2 and the like; B is NR 3 or CR 3 , provided that one of A and B is CR 1 or CR 3 ; K is N or CR 4 ; L is N or CR 5 ; R 5 has the same definition as R 4 ; M is N or CR 7 ; R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N(R 6a )R 6 or OR 6 ; R 21 , R 22 , R 3 , R 4 , and R 6a are each a 1-6C alkyl or the like; and R 6 is a substituent such as NO 2 and a cyano group), a salt or a derivative thereof. COPYRIGHT: (C)2010,JPO&INPIT

Virus polymerase inhibitor

La presente invention concerne des composes macrocycliques de formule (I), actifs in vitro et dans des analyses cellulaires destinees a detecter la NS3 protease du virus de l'hepatite C. Dans cette formule, W represente CH or N; R21 designe H, halo, alkyle C1-6, cycloalkyle, haloalkyle, alkoxy C1-6, cycloalkoxy, hydroxy, ou N(R23)2, chaque R23 representant independamment H, alkyle C?1-6? ou cycloalkoxy; et R?22? symbolise H, halo, alkyle C?1-6?, cycloalkyle C3-6, haloalkyle C1-6, thioalkyle C1-6, alkoxy C1-6, cycloalkoxy C3-6, alkoxyalkyle C2-7, cycloalkyle C3-6, aryle C6 ou 10 ou Het, qui est un heterocycle sature ou insature a cinq, six, ou sept chainons, contenant un a quatre heteroatomes choisis parmi l'azote, l'oxygene, et le soufre; ce cycloalkyle, aryle ou Het est substitue par R?24?, qui represente H, alkyle C?1-6?, cycloalkyle C3-6, alkoxy C1-6, cycloalkoxy C3-6, NO2, N(R?25)?2, NH-C(O)-R25; ou NH-C(O)-NH-R25; ou chaque R25 designe independamment H, alkyle C?1-6?, ou cycloalkyle C3-6; ou R?24? represente NH-C(O)-OR26, R26 representant alkyle C?1-6? ou cycloalkyle C3-6; R?3? symbolise hydroxy, NH?2?, ou un groupe de formule NH-R?31, R31? designant aryle C?6? ou 10, heteroaryle, -C(O)-R?32?, -C(O)-OR32, ou -C(O)-NHR32, R32 representant alkyle C?1-6? ou cycloalkyle C3-6; D symbolise une chaine alkylene saturee ou insaturee avec 5 a 10 atomes, qui contient eventuellement un a trois heteroatomes independamment choisis parmi: O, S, ou NR?41, R41? designant H, alkyle C?1-6?, cycloalkyle, ou -C(O)-R?42, R42? representant alkyle C?1-6?, cycloalkyle, ou aryle C6 ou 10; R?4? symbolise H ou un a trois substituants sur n'importe quel atome de carbone de ladite chaine D, ce substituant etant choisi independamment dans le groupe compose par: alkyle C?1-6?, haloalkyle C1-6, alkoxy C1-6, hydroxy, halo, amino, oxo, thio, ou thioalkyle C1-6, et A est un amide de formule C(O)-NH-R?5, R5? etant choisi dans le groupe compose par alkyle C?1-8?, cycloalkyle C3-6, aryle C6 ou 10, ou aralkyle C7-16; ou A est un acide carboxylique ou un sel pharmaceutiquement acceptable ou un ester de celui-ci.

Rancourt Jean

Papers

Viral Polymerase Inhibitors

Hepatitis C inhibitor peptide analogs

corrigendum: An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

Virus polymerase inhibitor

Peptides macrocycliques actifs contre le virus de l'hepatite c