Achiral amino acid acyl esters of ganciclovir and its derivative

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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544276, 544277, A61K 3152, C07D47332, C07D47318

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active

055434142

ABSTRACT:
Compounds of the Formula I ##STR1## wherein X is hydrogen, chloro, amino or hydroxy; R.sup.1 is an achiral amino acid acyl residue with a tertiary .alpha.-carbon atom. Preferred achiral amino acid acyl residues have the formula ##STR2## wherein each R.sup.2 is alkyl with 1 to 6 carbon atoms, cycloalkyl with 3 to 5 carbon atoms, or benzyl; or the two R.sup.2 groups link together to form a polymethylene group with 3 to 9 carbon atoms, and pharmaceutically acceptable salts thereof are antiviral agents with improved absorption. Intermediates for the preparation of the compounds of Formula I are also described.

REFERENCES:
patent: 4355032 (1982-10-01), Verheyden et al.
patent: 5043339 (1991-08-01), Beauchamp
E. Jensen et. al., Acta Pharm. Nord. 3(4) 243-247 (1991).
John C. Martin et. al., J. Pharm. Sci. 76(2), pp. 180-184 (1987).
P. C. Maudgal et. al., Arch. Ophthalmol. 1984; 102: 140-142.
Leon Colla et. al., J. Med. Chem. 98, 3, 26, 602-604 (1983).
L. M. Beauchamp et. al., Antiviral Chemistry & Chemotherapy (1992), 3 (3), 157-164.
Derwent for JP 05-097887 (Apr. 1993).

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