Therapeutic nucleosides

Details Therapeutic nucleosides Therapeutic nucleosides

C - Chemistry, Metallurgy

07

H

167/202, 260/229

C07H 19/173 (2006.01) A61K 31/70 (2006.01) C07D 473/00 (2006.01)

Patent

CA 1326237

ABSTRACT This invention relates to 6-substituted 3-2',3'-dideoxypurine nucleosides and pharmaceuti- cally acceptable derivatives thereof and their use in the treatment and prophylaxis of HIV infections, as well as pharmaceutical formulations containing the derivatives and processes for their production; the derivatives are of formula (IA); (I)A Image wherein R1 represents hydrogen or amino; and R2 represents halogen, C1-6 alkoxy, optionally sub- stituted by C3-6 cycloalkyl; C3-8 cycloalkyloxy; aryloxy, aralkyl or aralkyloxy in which the aryl may optionally be substituted with lower alkyl, hydroxy or halogen; C3-6 cycloalkylthio; C1-6 alkylthio; arylthio or aralkylthio in which the aryl may optionally be substituted with lower alkyl hydroxy or halogen; or R2 represents a heterocyclic group containing an oxygen atom or one or two nitrogen atoms, and 3-7 carbon atoms with optional double bonds in the ring optionally containing a sulphur and/or oxygen heteroatom and optionally substituted on the ring by one or more lower alkyl, hydroxy or halogen groups, C3-6 cycloalkylthio, aralkylthio in which the aryl may be substituted with lower alkyl, hydroxy or halogen; or R2 represents an imidazolyl- thio group in which the imidazolyl moiety may be substituted with lower alkyl and/or C-substituted with nitro; or R2 represents an amino group which is mono- di-substituted by C1-6 alkyl, C1-6 alkoxy, hydroxy C1-6, hydroxy C1-6 alkyl, and/or C3-6 cyclo- alkyl, aryl, aralkyl in which the aryl may optionally be substituted with lower alkyl, hydroxy or halogen, allyl optionally substituted with mono- or di-alkyl or alkoxy groups and R3 represents hydrogen or amino; and pharmaceutically acceptable derivatives thereof, other than the compounds of formula (I) in which R1 and R3 represent hydrogen and R2 represents methoxy or methylthio.

563634

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