749928-75-4Relevant academic research and scientific papers
Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5, 7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5, 6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor
Li, Hui,Tatlock, John,Linton, Angelica,Gonzalez, Javier,Jewell, Tanya,Patel, Leena,Ludlum, Sarah,Drowns, Matthew,Rahavendran, Sadayappan V.,Skor, Heather,Hunter, Robert,Shi, Stephanie T.,Herlihy, Koleen J.,Parge, Hans,Hickey, Michael,Yu, Xiu,Chau, Fannie,Nonomiya, Jim,Lewis, Cristina
supporting information; experimental part, p. 1255 - 1258 (2009/12/26)
The HCV RNA-dependent RNA polymerase has emerged as one of the key targets for novel anti-HCV therapy development. Herein, we report the optimization of the dihydropyrone series inhibitors to improve compound aqueous solubility and reduce CYP2D6 inhibitio
Allosteric inhibitors of hepatitis C polymerase: Discovery of potent and orally bioavailable carbon-linked dihydropyrones
Li, Hui,Linton, Angelica,Tatlock, John,Gonzalez, Javier,Borchardt, Allen,Abreo, Mel,Jewell, Tanya,Patel, Leena,Drowns, Matthew,Ludlum, Sarah,Goble, Mike,Yang, Michele,Blazel, Julie,Rahavendran, Ravi,Skor, Heather,Shi, Stephanie,Lewis, Cristina,Fuhrman, Sheila
, p. 3969 - 3972 (2008/02/11)
The discovery and optimization of a novel class of carbon-linked dihydropyrones as allosteric HCV NS5B polymerase inhibitors are presented. Replacement of the sulfur linker atom with carbon reduced compound acidity and greatly increased cell permeation. F
INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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Page/Page column 173, (2008/06/13)
The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
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Page/Page column 57, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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Page 106, (2008/06/13)
The invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula (I), and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula (I). The invention also relates to methods of preparing the compounds of formula (I).
