- A concise synthesis of 2'-C-methylribonucleosides
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2'-C-methylribonucleosides were synthesized in five steps from commercially available 1,3,5-tri-O-benzoyl-α-D-ribose with good overall yields.
- Wolfe,Harry-O'kuru
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- CYCLIC DINUCLEOTIDES AS STING AGONISTS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein R1A, R1B, R1C, R1D, B1, R2A, R2B, R2C, R2D, and R2E are defined herein and Formula (II), wherein R1H, R1K, R1J, and R2L are defined herein.
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Page/Page column 51; 55
(2018/08/20)
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- SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
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Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a Picornaviridae and/or Flaviviridae viral infections with one or more nucleotide analogs.
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Paragraph 0381
(2018/03/06)
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- METHODS AND COMPOSITIONS FOR TREATING HEPATITIS C VIRUS
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The present invention provides pharmaceutical compositions for the treatment of a hepatitis C infection in a host, comprising an antivirally effective amount of a 2'-C-branched nucleoside or a 2'-C-branched ribofuranosyl nucleoside, or pharmaceutically acceptable salts or esters thereof, in combination with one or more other anti-HCV agent. The present invention further provides the use of a 2'-C-branched nucleoside or a 2'-C-branched ribofuranosyl nucleoside, or pharmaceutically acceptable salts or esters thereof, in the manufacture of a medicament for the treatment of a hepatitis C infection in a host.
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Paragraph 0132; 0133
(2017/03/08)
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- The phosphoramidate ProTide approach greatly enhances the activity of β-2′-C-methylguanosine against hepatitis C virus
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β-2′-C-Methyl purines (1, 2) are known inhibitors of hepatitis C virus (HCV). We herein report the synthesis, biological and enzymatic evaluation of their 5′-phosphoramidate ProTides. Described herein are seven l-alanine phosphoramidate derivatives with v
- McGuigan, Christopher,Perrone, Plinio,Madela, Karolina,Neyts, Johan
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scheme or table
p. 4316 - 4320
(2010/06/19)
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- CHEMICAL COMPOUNDS
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Phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine have enhanced therapeutic potency, in particular, enhanced potency with respect to the prophylaxis or treatment of a viral infection such as hepatitis C vir
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Page/Page column 19-20
(2008/12/05)
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- 2'-C-Methyl analogues of selective adenosine receptor agonists: Synthesis and binding studies
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2'-C-Methyl analogues of selective adenosine receptor agonists such as (R)-PIA, CPA, CCPA, NECA, and IB-MECA were synthesized in order to further investigate the subdomain that binds the ribose moiety. Binding affinities of these new compounds at A1
- Franchetti, Palmarisa,Cappellacci, Loredana,Marchetti, Stefano,Trincavelli, Letizia,Martini, Claudia,Mazzoni, Maria R.,Lucacchini, Antonio,Grifantini, Mario
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p. 1708 - 1715
(2007/10/03)
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- 2′-C-alkylribonucleosides: Design, synthesis, and conformation
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Certain 2′-C-alkylribonucleotides have been designed as potential mechanism-based inactivators of ribonucleotide reductases. A short, flexible route toward the corresponding nucleosides and NMR evidence concerning their preferred solution conformations are discussed. Copyright
- Harry-O'kuru, Rogers E.,Kryjak, Emily A.,Wolfe, Michael S.
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p. 1457 - 1460
(2007/10/03)
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- A short, flexible route toward 2'-C-branched ribonucleosides
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A five-step synthesis of 2'-C-branched ribonucleosides from commercially obtained 1,3,5-tri-O-benzoyl-α-D-ribofuranose (4) is described. The free hydroxyl group of 4 was oxidized in high yield with Dess-Martin periodane reagent. The resultant 2-ketosugar was treated with MeMgBr/TiCl4, CH2=CHMgBr/CeCl3, or TMSC≡CLi/CeCl3, and in each case addition to the ketone proceeded stereoselectively to provide 2-alkylated ribofuranosides. After conversion to the corresponding tetrabenzoyl derivatives, the 2-alkylribofuranosides were coupled to nucleobases under Vorbruggen persilylation conditions, giving the β-nucleosides with high stereoselectivity. Deprotection with methanolic ammonia provided the title compounds in 17-49% overall yields from 4.
- Harry-O'kuru,Smith,Wolfe
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p. 1754 - 1759
(2007/10/03)
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- New 2'-branched-chain sugar nucleoside analogs with potential antiviral or antitumor activity
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The synthesis of 2'-C-hydroxymethyl and 2'-C-methyl nucleoside analogs [1-(3-deoxy-2-hydroxymethyl-D-erythro-pentofuranosyl)thymine (14), the corresponding adenine derivative. 17, 1-(2-methyl-β-D-ribofuranosyl)thymine (20) and 2'-methyladenosine (23)] by
- Wolf,Jarrige,Florent,Grierson,Monneret
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p. 773 - 778
(2007/10/02)
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- NEW SYNTHESES OF 2'-C-METHYLNUCLEOSIDES STARTING FROM D-GLUCOSE AND D-RIBOSE
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Effective general methods have been developed for the synthesis of 2'-C-methylnucleosides starting from D-glucose and D-ribose. 3-O-Benzyl-1,2-O-isopropylidene-3-C-methyl-α-D-allofuranose was prepared in 5 steps from D-glucose and converted into 1,2,3-tri
- Beigelman, Leon N.,Ermolinsky, Boris S.,Gurskaya, Galina V.,Tsapkina, Elena N.,Karpeisky, Marat Ya.,Mikhailov, Sergey N.
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p. 219 - 232
(2007/10/02)
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