863886-03-7Relevant academic research and scientific papers
A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): Application of a one-pot borylation-suzuki coupling reaction
Zhang, Yongda,Lu, Bruce Z.,Li, Guisheng,Rodriguez, Sonia,Tan, Jonathan,Wei, Han-Xun,Liu, Jianxiu,Roschangar, Frank,Ding, Fei,Zhao, Wenyi,Qu, Bo,Reeves, Diana,Grinberg, Nelu,Lee, Heewon,Heckmann, Golo,Niemeier, Oliver,Brenner, Michael,Tsantrizos, Youla,Beaulieu, Pierre L.,Hossain, Azad,Yee, Nathan,Farina, Vittorio,Senanayake, Chris H.
supporting information, p. 4558 - 4561 (2015/03/04)
A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127, 1) was achieved, featuring efficient Pd-catalyzed one-pot borylation-Suzuki coupling where TFP was identified as the unique ligand effective for these transformations.
Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: Discovery of deleobuvir (BI 207127)
LaPlante, Steven R.,B?s, Michael,Brochu, Christian,Chabot, Catherine,Coulombe, René,Gillard, James R.,Jakalian, Araz,Poirier, Martin,Rancourt, Jean,Stammers, Timothy,Thavonekham, Bounkham,Beaulieu, Pierre L.,Kukolj, George,Tsantrizos, Youla S.
supporting information, p. 1845 - 1854 (2014/04/03)
Conformational restrictions of flexible torsion angles were used to guide the identification of new chemotypes of HCV NS5B inhibitors. Sites for rigidification were based on an acquired conformational understanding of compound binding requirements and the roles of substituents in the free and bound states. Chemical bioisosteres of amide bonds were explored to improve cell-based potency. Examples are shown, including the design concept that led to the discovery of the phase III clinical candidate deleobuvir (BI 207127). The structure-based strategies employed have general utility in drug design.
MESYLATE SALT FORMS OF A POTENT HCV INHIBITOR
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Paragraph 0107-0108, (2013/10/08)
This invention relates to novel mesylate salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in methods for the treatment of Hepatitis C Viral (HCV) infection:
ORAL COMBINATION THERAPY FOR TREATING HCV INFECTION IN SPECIFIC PATIENT SUBGENOTYPE POPULATIONS
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Page/Page column 31; 32, (2013/10/21)
The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) Compound (2), or a pharmaceutically acceptable salt thereof, as herein described, and optionally (c) ribavirin, and methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient that has genetic variations located near the IL28B gene, including SNP rs 12979860 with a CC or non-CC genotype and SNP rs 8099917 with a TT or non-TT genotype.
SOLID STATE FORMS OF A POTENT HCV INHIBITOR
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Page/Page column 28-29, (2012/04/17)
This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection.
VIRAL POLYMERASE INHIBITORS
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Page/Page column 85, (2008/06/13)
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particularly those viral polymerases within the Flaviviridae family, more particularly to HCV polymerase.
