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.
Anti-norovirus activity of C7-modified 4-amino-pyrrolo[2,1-f][1,2,4]triazine C-nucleosides
Groaz, Elisabetta,Herdewijn, Piet,Li, Qingfeng,Neyts, Johan,Rocha-Pereira, Joana
, (2020/04/15)
Synthetic nucleoside analogues characterized by a C–C anomeric linkage form a family of promising therapeutics against infectious and malignant diseases. Herein, C-nucleosides comprising structural variations at the sugar and nucleobase moieties were exam
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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, (2013/10/22)
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.
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.
METHODS FOR THE PREPARATION OF DIASTEROMERICALLY PURE PHOSPHORAMIDATE PRODRUGS
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, (2012/02/05)
Provided are methods and intermediates for preparing diastereomerically pure phosphoramidate prodrugs of nucleosides of Formulas (la) and (lb): The compounds of Formula la and lb are useful for the treatment Hepatitis C infections.
1'-SUBSTITUTED-CARBA-NUCLEOSIDE PRODRUGS FOR ANTIVIRAL TREATMENT
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, (2011/12/14)
Provided are prodrugs of pyrrolo[l,2-f][l,2,4]triazin-7-yl nucleoside phosphates wherein the 1 '' position of the nucleoside sugar is substituted with CN. The compounds, compositions, and methods provided are useful for the treatment Hepatitis C infections.
PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 1'-SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS
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Page/Page column 72, (2011/04/19)
Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,2-f][1,2,4]triazinyl heterocycles of Formula I.
CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT
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Page/Page column 136-137, (2010/09/03)
Provided are thieno[3,4-d]pyrimidin-7-yI and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.
CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT
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Page/Page column 103, (2009/12/05)
Provided are imidazol [1,5-f] [1,2.4]triazinyl, imidazol [1,2,4]triazinyl, and [1,2,4] triazolo [4,3-f] [1,2,4] triazinyl nucleosides of formula I nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections. Wherein X1 or X2 is indepently C-R10 or N and wherein at least one of X1 or X2 is N.