1355050-12-2Relevant articles and documents
Application of nucleoside compound, medicine and preparation method thereof
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Paragraph 0072-0076, (2020/01/11)
The invention relates to application of a nucleoside compound to preparation of a medicine for treating feline stomatitis, a medicine and a preparation method thereof. The nucleoside compound has a structure as shown in a formula (1): (please see the spec
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses
Siegel, Dustin,Hui, Hon C.,Doerffler, Edward,Clarke, Michael O.,Chun, Kwon,Zhang, Lijun,Neville, Sean,Carra, Ernest,Lew, Willard,Ross, Bruce,Wang, Queenie,Wolfe, Lydia,Jordan, Robert,Soloveva, Veronica,Knox, John,Perry, Jason,Perron, Michel,Stray, Kirsten M.,Barauskas, Ona,Feng, Joy Y.,Xu, Yili,Lee, Gary,Rheingold, Arnold L.,Ray, Adrian S.,Bannister, Roy,Strickley, Robert,Swaminathan, Swami,Lee, William A.,Bavari, Sina,Cihlar, Tomas,Lo, Michael K.,Warren, Travis K.,Mackman, Richard L.
, p. 1648 - 1661 (2017/03/17)
The recent Ebola virus (EBOV) outbreak in West Africa was the largest recorded in history with over 28,000 cases, resulting in >11,000 deaths including >500 healthcare workers. A focused screening and lead optimization effort identified 4b (GS-5734) with anti-EBOV EC50 = 86 nM in macrophages as the clinical candidate. Structure activity relationships established that the 1′-CN group and C-linked nucleobase were critical for optimal anti-EBOV potency and selectivity against host polymerases. A robust diastereoselective synthesis provided sufficient quantities of 4b to enable preclinical efficacy in a non-human-primate EBOV challenge model. Once-daily 10 mg/kg iv treatment on days 3-14 postinfection had a significant effect on viremia and mortality, resulting in 100% survival of infected treated animals [Nature 2016, 531, 381?385]. A phase 2 study (PREVAIL IV) is currently enrolling and will evaluate the effect of 4b on viral shedding from sanctuary sites in EBOV survivors.
METHODS AND COMPOUNDS FOR TREATING PARAMYXOVIRIDAE VIRUS INFECTIONS
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Page/Page column 128, (2012/02/05)
Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula (I): wherein the 1 ? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections