- Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase
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We report the evolutionary path from an open-chain series to conformationally constrained tetracyclic indole inhibitors of HCV NS5B-polymerase, where the C2 aromatic is tethered to the indole nitrogen. SAR studies led to the discovery of zwitterionic comp
- Stansfield, Ian,Ercolani, Caterina,Mackay, Angela,Conte, Immacolata,Pompei, Marco,Koch, Uwe,Gennari, Nadia,Giuliano, Claudio,Rowley, Michael,Narjes, Frank
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scheme or table
p. 627 - 632
(2009/09/06)
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- MACROCYCLIC INDOLE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C INFECTIONS
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A class of macrocyclic compounds of formula (I), wherein R7, R9, B, F, M, Q, W, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also p
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Page/Page column 42
(2009/03/07)
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- PENTACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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Page/Page column 29
(2008/06/13)
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- Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
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We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.
- Ikegashira, Kazutaka,Oka, Takahiro,Hirashima, Shintaro,Noji, Satoru,Yamanaka, Hiroshi,Hara, Yoshinori,Adachi, Tsuyoshi,Tsuruha, Jun-Ichiro,Doi, Satoki,Hase, Yasunori,Noguchi, Toru,Ando, Izuru,Ogura, Naoki,Ikeda, Satoru,Hashimoto, Hiromasa
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p. 6950 - 6953
(2007/10/03)
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- FUSED HETEROTETRACYCLIC COMPOUNDS AND USE TEHREOF AS HCV POLYMERASE INHIBITOR
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The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
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