- MODIFIED OLIGOMERIC COMPOUNDS AND USES THEREOF
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The present disclosure provides oligomeric compounds comprising a modified oligonucleotide having at least one stereo-non-standard nucleoside. An oligomeric compound comprising a modified oligonucleotide consisting of 12-30 linked nucleosides, wherein at least one nucleoside of the modified oligonucleotide is a stereo-non-standard nucleoside; and wherein the oligomeric compound is selected from among an RNAi compound, a modified CRISPR compound, and an artificial mRNA compound.
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Page/Page column 111
(2021/02/19)
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- Novel nucleoside analogues as effective antiviral agents for Zika virus infections
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Previously considered a neglected flavivirus, Zika virus has recently emerged as a public health concern due to its ability to spread rapidly and cause severe neurological disorders, such as microcephaly in newborn babies from infected mothers, and Guilla
- Bassetto, Marcella,Basso, Mattia,Brancale, Andrea,Bugert, Joachim J.,Cima, Cecilia M.,Friese, Daniela,Salerno, Martina,Schwarze, Frank
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- Novel antiviral activity of l-dideoxy bicyclic nucleoside analogues versus vaccinia and measles viruses in vitro
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Dideoxy bicyclic pyrimidine nucleoside analogues (ddBCNAs) with d-chirality have previously been described by us to inhibit replication of human cytomegalovirus. We herein report for the first time that activity against vaccinia virus (VACV) was achieved
- McGuigan, Christopher,Hinsinger, Karen,Farleigh, Laura,Pathirana, Ranjith N.,Bugert, Joachim J.
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p. 1311 - 1322
(2013/03/29)
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- PROCESS FOR PREPARING L-NUCLEIC ACID DERIVATIVES AND INTERMEDIATES THEREOF
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A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now, is possible.
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Page/Page column 4
(2009/01/24)
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- Synthesis of beta-L-2'-deoxy nucleosides
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An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.
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Page/Page column 30-35
(2010/02/11)
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- Synthesis and antiviral activity of C-5 substituted β-D- and β-l-D4T analogues
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A series of β-D-2',3'-didehydro-2',3'-dideoxy-nucleosides bearing a tether attached at the C-5 position and their β-L-counterparts was synthesized. Their inhibitory activities against human immunodeficiency vires (HIV) were investigated and compared to establish relationship(s) between compound structure and their antiviral activity. No significant activity was observed for β-D- and β-L-modified nucleosides respectively 7a-c and 14a-c, but 7d and 14d exhibited a weak activity against HIV-1.
- Delbederi,Fossey,Fontaine,Benzaria,Gavriliu,Ciurea,Lelong,Laduree,Aubertin,Kirn
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p. 1441 - 1461
(2007/10/03)
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- Synthesis of L-analogues of 1-(2',3'-dideoxy-β-D-glycero-pent-2-enofuranosyl)thymine
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β-L(-)-2',3'-Dideoxy-3'-thiacytidine (3TC), its 5-fluoro derivative ((-)-FTC), 2',3'-dideoxycytidine (β-L-ddC), and its 5-fluoro derivative (β-L-FddC) have been reported to have anti-HIV and anti-HBV activity. It was of particular interest therefore to develop a series of β-L-d4T analogues bearing several kinds of amino-linker arms at the C-5 position of the pyrimidine moiety in an attempt to find more potent and less toxic anti-HIV agents. In addition, modification of nucleosides with various functional molecules has been attracting wide interest in biological studies since die primary amino groups could be useful for the attachment of either fluorescent dyes or a non-nucleosidic reverse transcriptase inhibitor. These modified nucleosides were evaluated for antiviral activity against HIV-1(LAI) in CEM-SS cells and HIV-1(IIIB) in MT4 cells. Unfortunately, none of the compounds exhibited significant anti-HIV activity at the doses tested.
- Camara,Ciurea,Delbederi,Fossey,Fontaine,Gavriliu,Jouenne,Laduree,Aubertin,Kirn
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p. 225 - 231
(2007/10/03)
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- A stereospecific synthesis of 2',3'-dideoxy-β-L-cytidine (β-L-ddC). A potent inhibitor against human hepatitis B virus (HBV) and human immunodeficiency virus (HIV)
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2',3'-Dideoxy-β-L-cytidine (β-L-ddC), a potent inhibitor against human hepatitis B virus (HBV) and human immunodeficiency virus (HIV), has been stereospecifically synthesized from L-arabinose in 9 steps.
- Lin,Luo,Liu
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p. 3477 - 3480
(2007/10/02)
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