- MACROCYCLIC INHIBITORS OF HEPATITIS C PROTEASE
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The invention provides compounds inhibitory to the Hepatitis C viral protease, compositions and combinations including the compounds, methods of treatment of conditions wherein inhibition of the Hepatitis C viral protease is medically indicated, and metho
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Page/Page column 54-55
(2009/10/09)
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- MACROCYCLIC HEPATITIS C PROTEASE INHIBITORS
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The present invention provides novel macrocyclic compounds that mimic peptide substrates of the hepatitis C viral protease and inhibit the viral protease, more particularly as inhibitors of the NS3 serine protease from hepatitis C virus. Methods for synthesis of the compounds are also provided. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
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Page/Page column 47
(2008/12/07)
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- Synthesis of BILN 2061, an HCV NS3 protease inhibitor with proven antiviral effect in humans
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(Equation Presented) The synthesis of BILN 2061, an NS3 protease inhibitor with proven antiviral effect in humans, was accomplished in a convergent manner from four building blocks. The procedure described here was suitable for the preparation of multigra
- Faucher, Anne-Marie,Bailey, Murray D.,Beaulieu, Pierre L.,Brochu, Christian,Duceppe, Jean-Simon,Ferland, Jean-Marie,Ghiro, Elise,Gorys, Vida,Halmos, Ted,Kawai, Stephen H.,Poirier, Martin,Simoneau, Bruno,Tsantrizos, Youla S.,Llinas-Brunet, Montse
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p. 2901 - 2904
(2007/10/03)
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- Macrocyclic peptides active against the hepatitis C virus
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The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R21, R22, R3, R4, D and A are as defined herein, or a pharmaceutically acceptable salts or ester thereof.
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- Macrocyclic peptides active against the hepatitis C virus
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Compounds of formula I: wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O(C1-6)alkyl, amido, amino or phenyl; R2 is (C5-6)cycloalkyl and R3 is cyclopentyl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.
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