917567-08-9Relevant articles and documents
Synthesis of Benzene and Pyridine 2′-C-Methyl-C-ribonucleosides and -nucleotides
Tokarenko, Anna,Po?tová Slavětínská, Lenka,Klepetá?ová, Blanka,Hocek, Michal
, p. 7962 - 7983 (2015)
A general and modular synthesis of substituted benzene and pyridine 2′-C-methyl-C-ribonucleosides was developed. Benzyl-protected haloaryl-C-nucleoside intermediates were prepared by the addition of bromo(het)aryllithium reagents to a protected lactone, followed by acetylation and reduction. These halogenated intermediates were further transformed by Pd-catalysed cross-couplings, aminations, or hydroxylations. The final deprotection was rather troublesome, and different procedures involving catalytic hydrogenation on Pd/C, or treatment with BCl3, were optimized for each derivative. The final C-nucleosides were also all converted into the corresponding NTPs. None of the C-nucleosides showed any activity in the HCV replicon assay, and none of the NTPs showed any significant inhibition of the HCV polymerase. C-Nucleoside carba-analogues of clinically used antiviral 2′-C-methylribonucleosides were designed and synthesized, but were found to be inactive.
CD73 INHIBITORS
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Paragraph 196, (2020/10/27)
Disclosed are compounds that are inhibitors of CD73 and are useful in treating CD73-associated diseases or conditions, and compositions containing the compounds.
METHODS FOR TREATING HCV
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, (2013/03/28)
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.