- C-PURINE NUCLEOSIDE ANALOGS AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE
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The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such C-nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the C-nucleoside compounds of the present invention.
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Page/Page column 41; 42
(2008/06/13)
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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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- Process for the preparation of ribofuranose derivatives
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The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of formula (I): useful in the synthesis of nucleotides.
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- PROCESS FOR THE PREPARATION OF RIBOFURANOSE DERIVATIVES
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The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of Formula (I) useful in the synthesis of nucleotides.
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- Process to ribofuranose sugar derivatives as intermediates to branched-chain nucleosides
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A novel process is provided for the preparation of ribofuranose sugar derivatives which are useful in the synthesis of branched-chain ribonucleoside inhibitors of HCV polymerase for the treatment of HCV infection. Also provided are useful intermediates obtained from the instant process.
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