- HEPATITIS B CORE PROTEIN MODULATORS
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The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
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Page/Page column 162
(2018/04/13)
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- CARBOXYL SUBSTITUTED INDOLES FOR USE AS PPAR ALPHA MODULATORS
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There is provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof wherein one of R1 and R2 is H and the other is COOH. The compounds are useful as PPAR modulators.
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Page/Page column 65
(2009/12/28)
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- MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS
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The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, formula (I), wherein R1; R3; and R4 have the meaning defined in the claims. 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 56
(2009/07/25)
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- Compounds for the Treatment of Hepatitis C
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The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 32
(2008/12/07)
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- Compounds for the Treatment of Hepatitis C
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The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 23
(2008/12/06)
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- Compounds for the Treatment of Hepatitis C
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The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 4; 36
(2008/12/07)
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- Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
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The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 1
(2008/06/13)
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- Indolobenzazepine HCV NS5B inhibitors
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The invention encompasses compounds and salts of Formulas I, II, III, and IV as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 174
(2008/06/13)
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- Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
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The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 3; 32
(2008/06/13)
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- INDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS
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Disclosed are compounds having formula I and related compositions and methods thereof. The compounds are useful for treating viral infections caused by the Flaviviridae family of viruses.
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Page/Page column 135
(2008/06/13)
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- Inhibitors of HCV replication
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Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
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Page/Page column 18; 38
(2010/10/20)
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- Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds
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Benzimidazole-based allosteric inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified to a variety of topologically related scaffolds. Replacement of the polar benzimidazole core by lipophilic indoles led to inhibitors with improved potency in the cell-based subgenomic HCV replicon system. Transposing the indole scaffold into a previously described series of benzimidazole-tryptophan amides generated the most potent inhibitors of HCV RNA replication in cell culture reported to date in this series (EC50 ～ 50 nM).
- Beaulieu, Pierre L.,Gillard, James,Bykowski, Darren,Brochu, Christian,Dansereau, Nathalie,Duceppe, Jean-Simon,Hache, Bruno,Jakalian, Araz,Lagace, Lisette,LaPlante, Steven,McKercher, Ginette,Moreau, Elaine,Perreault, Stephane,Stammers, Timothy,Thauvette, Louise,Warrington, Jeff,Kukolj, George
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p. 4987 - 4993
(2007/10/03)
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- INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
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Page/Page column 21
(2010/10/20)
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- Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase
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Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here a novel class of allosteric inhibitor of NS5B that shows potent affinity for the NS5B enzyme and effective inhibition of subgenomic HCV RNA replication in HUH-7 cells. Inhibitors from this class have promising characteristics for further development as anti-HCV agents.
- Harper, Steven,Pacini, Barbara,Avolio, Salvatore,Di Filippo, Marcello,Migliaccio, Giovanni,Laufer, Ralph,De Francesco, Raffaele,Rowley, Michael,Narjes, Frank
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p. 1314 - 1317
(2007/10/03)
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- VIRAL POLYMERASE INHIBITORS
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An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
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- Viral polymerase inhibitors
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An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ---- represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
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