Antiviral purine derivatives

Details Antiviral purine derivatives Antiviral purine derivatives

C - Chemistry, Metallurgy

07

F

C07F 9/6561 (2006.01) A61K 31/675 (2006.01)

Patent

CA 2345672

Chemical compounds comprising nucleoside phosphoramidates, their preparation and their therapeutic use in treating viral infections, particularly HIV and HBV are disclosed. The compounds contain a substituted adenine analogue moiety comprising 2-amino-6-(cyclopropylamino)-9H-purin-9-yl. The compounds show both anti-viral activity and acid stability. Salts and esters of the phosphoramidates are included. A representative compound is (1S, 4R), -4-[2- amino-6-(cyclopropylamino)-9H-purin-9-y1]-2-cyclopentene-1-methanol O-[phenyl- (methoxy-L-alaninyl)]-phosphate.

L'invention concerne des composés chimiques comprenant des phosphoramidates de nucleosides, la préparation de ces composés et leur utilisation dans le traitement d'infections virales, notamment de celles par VIH et par VHB. Les composés contiennent un groupe fonctionnel d'analogue d'adénine substitué qui comprend 2-amino-6-(cyclopropylamino)-9H-purin-9-yl. Les composés possèdent une activité antivirale et manifestent une stabilité aux acides. L'invention concerne des sels et des esters des phosphoramidates. Un composé représentatif est (1S, 4R), -4-[2-amino-6-(cyclopropylamino)-9H-purin-9-y1]-2-cyclopentène-1-méthanolO-[phényl-(méthoxy-L-alaninyl)]-phosphate.

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