Invention Grant
- Patent Title: Methods for the preparation of ribosides
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Application No.: US14926063Application Date: 2015-10-29
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Publication No.: US11344565B2Publication Date: 2022-05-31
- Inventor: Steven Donald Axt , Pavel Robertovich Badalov , Katrien Brak , Silvio Campagna , Andrei Chtchemelinine , Edward Doerffler , Morin Mae Frick , Detian Gao , Lars V. Heumann , Brittanie Hoang , Willard Lew , Robert Ronald Milburn , Sean Timothy Neville , Bruce Ross , Erik Rueden , Robert William Scott , Dustin Siegel , Andrew C. Stevens , Clarissa Tadeus , Tiago Vieira , Andrew W. Waltman , Xianghong Wang , Mark Charles Whitcomb , Lydia Wolfe , Chia-Yun Yu
- Applicant: Gilead Sciences, Inc.
- Applicant Address: US CA Foster City
- Assignee: Gilead Sciences, Inc.
- Current Assignee: Gilead Sciences, Inc.
- Current Assignee Address: US CA Foster City
- Agency: Fish & Richardson P.C.
- Main IPC: C07H5/06
- IPC: C07H5/06 ; C07H7/06 ; A61K31/685 ; A61K31/706 ; A61K31/7056 ; A61K31/53 ; C07H1/00 ; C07H1/02 ; C07H11/00 ; C07H15/18 ; A61K31/6615 ; A61K31/665 ; A61K31/683 ; C07D487/04 ; C07D519/00 ; C07F9/24 ; C07F9/6561 ; A61K31/675 ; A61K45/06 ; A61K31/00

Abstract:
Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl3-2LiCl, LaCl3, CeCl3, NdCl3, or YCl3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Public/Granted literature
- US20160122356A1 METHODS FOR THE PREPARATION OF RIBOSIDES Public/Granted day:2016-05-05
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