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Generated: September 24, 2017

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Title: Therapeutic nucleosides
Abstract:The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.
Inventor(s): Daluge; Susan M. (Chapel Hill, NC)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Filing Date:Dec 19, 1990
Application Number:07/630,129
Claims:1. Enantiomeric compounds of formula (III) ##STR14## wherein A represents the 2-cyclopentene-1-methanol-4-yl group in either the (1S,4R) or (1R,4S) configuration, R represents a cyclopropylamino or N-cyclopropyl-N-methylamino group, R.sup.2 represents hydrogen or a formyl group and R.sup.3 represents a C.sub.1-6 alkanoyl group, or a salt or ester thereof.

2. Enantiomeric compounds of formula (V) ##STR15## wherein A represents the 2-cyclopentene-1-methanol-4-yl group in either the (1S,4R) or (1R,4S) configuration, Z represents a halo group, R.sup.2 represents hydrogen or a formyl group and R.sup.3 represents a C.sub.1-6 alkanoyl group, or a salt or ester thereof.

3. (1R,4S)-cis-N-[4-Chloro-5-formamido-6-((4 -(hydroxymethyl)-2-cyclopentene-1-yl)amino)-2-pyrimidinyl]isobutyramide substantially free of the corresponding (1S,4R) enantiomer.

4. Compounds of formula (VII) ##STR16## wherein Z represents a halo group, R.sup.2 represents hydrogen or a formyl group, R.sup.3 represents a C.sub.1-6 alkanoyl group and R.sup.4 represents a halo group, or a salt thereof.

5. N-(4,6-Dichloro-5-formamido-2-pyrimidinyl)isobutyramide.

6. Compounds of formula (IX) ##STR17## wherein Z represents a halo group, R.sup.3 represents a C.sub.1-6 alkanoyl group and R.sup.4 represents a halo group or a salt thereof.

7. N-(4,6-Dichloro-5-nitro-2-pyrimidinyl)isobutyramide.

8. Compounds of formula (X) ##STR18## wherein R.sup.3 represents a C.sub.1-6 alkanoyl group and R.sup.4 represents a halo group or a salt thereof.

9. N-(4-Chloro-1,6-dihydro-5-nitro-6-oxo-2-pyrimidinyl)isobutyramide.
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Dow
Chubb

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