- CYCLIC DINUCLEOTIDES AS STING AGONISTS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein R1A, R1B, R1C, R1D, B1, R2A, R2B, R2C, R2D, and R2E are defined herein and Formula (II), wherein R1H, R1K, R1J, and R2L are defined herein.
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- SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
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Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a Picornaviridae and/or Flaviviridae viral infections with one or more nucleotide analogs.
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- 6-Hydrazinopurine 2′-methyl ribonucleosides and their 5′-monophosphate prodrugs as potent hepatitis C virus inhibitors
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A series of 6-hydrazinopurine 2′-methyl ribonucleosides was synthesized and tested for its inhibitory activity against the hepatitis C virus (HCV). The lack of antiviral activity of these nucleosides was associated with a poor affinity for adenosine kinase, which prompted us to synthesize several of their 5′-monophosphate prodrugs. Some of these prodrugs exhibited more than 1000-fold improvement in anti-HCV activity when compared to their parent nucleosides (EC50 of 24 nM vs 92 μM for the parent).
- Gunic, Esmir,Chow, Suetying,Rong, Frank,Ramasamy, Kanda,Raney, Anneke,Yunzhi Li, David,Huang, Jingfan,Hamatake, Robert K.,Hong, Zhi,Girardet, Jean-Luc
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p. 2456 - 2458
(2008/02/03)
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- 6-HYDRAZINOPURINE 2'-METHYL RIBONUCLEOSIDES AND NUCLEOTIDES FOR TREATMENT OF HCV
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Compounds of formula I, are provided, which are useful as inhibitors of hepatitis C virus.
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Page/Page column 9-10
(2008/06/13)
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- Synthesis of 9-(2-β-C-methyl-β-d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication
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A series of 9-(2′-β-C-methyl-β-d-ribofuranosyl)-6- substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to
- Ding, Yili,Girardet, Jean-Luc,Hong, Zhi,Lai, Vicky C.H.,An, Haoyun,Koh, Yung-Hyo,Shaw, Stephanie Z.,Zhong, Weidong
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p. 709 - 713
(2007/10/03)
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- Practical synthesis of a potent hepatitis C virus RNA replication inhibitor
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A practical, efficient synthesis of 1, a hepatitis C virus RNA replication inhibitor, is described. Starting with the inexpensive diacetone glucose, the 12-step synthesis features a novel stereoselective rearrangement to prepare the key crystalline furanose diol intermediate. This is followed by a highly selective glycosidation to couple the C-2 branched furanose epoxide with deazapurine.
- Bio, Matthew M.,Xu, Feng,Waters, Marjorie,Williams, J. Michael,Savary, Kimberly A.,Cowden, Cameron J.,Yang, Chunhua,Buck, Elizabeth,Song, Zhiguo J.,Tschaen, David M.,Volante,Reamer, Robert A.,Grabowski, Edward J. J.
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p. 6257 - 6266
(2007/10/03)
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- 2'-C-Methyl analogues of selective adenosine receptor agonists: Synthesis and binding studies
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2'-C-Methyl analogues of selective adenosine receptor agonists such as (R)-PIA, CPA, CCPA, NECA, and IB-MECA were synthesized in order to further investigate the subdomain that binds the ribose moiety. Binding affinities of these new compounds at A1
- Franchetti, Palmarisa,Cappellacci, Loredana,Marchetti, Stefano,Trincavelli, Letizia,Martini, Claudia,Mazzoni, Maria R.,Lucacchini, Antonio,Grifantini, Mario
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p. 1708 - 1715
(2007/10/03)
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