Dihydropyrimidine nucleosides with antiviral properties

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) C07D 405/04 (2006.01)

Patent

CA 2130265

2130265 9414831 PCTABS00032 Pharmaceutical compounds of general formula (I) have been prepared and non-toxic pharmaceutically acceptable salts thereof, wherein R1 is a halogen substituent; R2 is a member selected from the group consisting of alkoxy, hydroxy and azido; and X-Y is a member selected from the group consisting of CH(N3)-CH2, CH(F)-CH2 and CH = CH. Halogen denotes an iodo, bromo, chloro and fluoro atom. Alkoxy denotes a straight or branched chain moiety having 1-16 carbon atoms. Compounds of formula (I) can exist as the (5R, 6R), (5S, 6S), (5R, 6S) and (5S, 6R) diastereomers which differ in configuration at positions C-5 and C-6. These compounds exhibit anti-human immunodeficiency virus activity (anti-HIV) and are useful in the treatment of acquired immunodeficiency syndrom (AIDS) and AIDS-related complex.

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