863566-97-6Relevant academic research and scientific papers
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
Zheng, Xiaofan,Hudyma, Thomas W.,Martin, Scott W.,Bergstrom, Carl,Ding, Min,He, Feng,Romine, Jeffrey,Poss, Michael A.,Kadow, John F.,Chang, Chong-Hwan,Wan, John,Witmer, Mark R.,Morin, Paul,Camac, Daniel M.,Sheriff, Steven,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert,Lemm, Julie,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
, p. 2925 - 2929 (2011/06/26)
Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in conformationally constrained heterocycles
AROMATIC HETEROCYCLIC FUSED INDOLOBENZADIAZEPINE HCV NS5B INHIBITORS
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Page/Page column 27, (2009/10/22)
The disclosure provides compounds of formula (I), including their salts, 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.
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase
Stansfield, Ian,Ercolani, Caterina,Mackay, Angela,Conte, Immacolata,Pompei, Marco,Koch, Uwe,Gennari, Nadia,Giuliano, Claudio,Rowley, Michael,Narjes, Frank
scheme or table, p. 627 - 632 (2009/09/06)
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
TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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Page/Page column 21, (2008/06/13)
The present invention relates to tetracyclic indole derivatives of formula (I): wherein Ar, A, R1, R2, L, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, a
INHIBITORS OF HCV REPLICATION
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Page/Page column 88, (2010/11/28)
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
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
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
, p. 6950 - 6953 (2007/10/03)
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.
FUSED HETEROTETRACYCLIC COMPOUNDS AND USE TEHREOF AS HCV POLYMERASE INHIBITOR
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Example 1-1, (2008/06/13)
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.
Inhibitors of HCV replication
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Page/Page column 32; 51, (2010/10/20)
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.
