Antiviral acyclonucleosides and acyclonucleotides

Details Antiviral acyclonucleosides and acyclonucleotides Antiviral acyclonucleosides and acyclonucleotides

C - Chemistry, Metallurgy

07

D

167/218, 260/251

C07D 473/00 (2006.01) A61K 31/505 (2006.01) C07F 9/6561 (2006.01) C07F 9/6564 (2006.01)

Patent

CA 2009109

217/TGR1 17699 TITLE OF THE INVENTION ANTIVIRAL ACYCLONUCLEOSIDES AND ACYCLONUCLEOTIDES ABSTRACT OF THE INVENTION Disclosed are compounds of the formula: Image wherein B is related to one of the heterocyclic bases found in nucleic acid (DNA, RNA) such as a purine, a substituted purine, a pyrimidine or a substituted pyrimidine wherein the substituents on the purine or pyrimidine are selected from amino, hydroxyl, halogen, thio or alkylthiol wherein the alkyl moiety of the alkylthiol has 1 to 6 carbons; R1 is fluorine, chlorine, hydroxy, alkoxy having 1 to 6 carbons or a phosphate group having the formula: 217/TGRl - i - 17699 Image wherein R4 and R5 are pharmaceutically acceptable cations; R2 and R3 are independently hydroxy, alkoxy having 1 to 6 carbons or a phosphate group having the formula: Image wherein R4 and R5 hydrogen or are pharmaceutically acceptable cations; or two of R1, R2 and R3 taken together form a phosphate group having the formula: Image wherein R4 is hydrogen or a pharmaceutically acceptable cation. The compounds have antiviral activity. They are particularly effective against the herpes group of viruses with special utility against cytomegalovirus (CVM) and varicella-zoster virus (VZV), and against retroviruses such as HTLV-III.

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