Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1994-10-27
1995-08-29
Robinson, Douglas W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 2854, A61K 3170, C07H 1909
Patent
active
054460310
ABSTRACT:
The present invention relates to a novel 1-.beta.-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil derivative represented by the following formula (I), whose concentration in blood as XVAU can be kept high for many hours when it is administered orally.
The present invention also relates to an antiviral agent comprising as an active ingredient the compound of the present invention.
Further, the present invention relates to a method for treating viral diseases which comprises administering to a patient with a viral disease a safe and effective amount of the compound of the present invention. ##STR1## wherein X represents a halogen; and R.sup.1, R.sup.2, and R.sup.3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group or an aralkyl group, provided that R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time.
REFERENCES:
patent: 4383990 (1983-05-01), Coe et al.
patent: 4544740 (1985-10-01), Szaboles nee Borbas et al.
Robins et al., "Conversion of Vinylsilanes to Vinyl Halides with Xenon Difuoride and Metal Halides. A Versatile New Route to 5-(2-Halovinyl)pyrimidein Nucleosides," Tett. Lett., 31(39), 5633-5636 (1990).
Ashida et al., "Metabolism of 5'-Ether Prodrugs of 1-.beta.-D-Arabinofuranosyl-E-5-(2-bromoviyl)uracil in Rats," Biochem. Pharmacology, 46(12), 2201-2207 (1993).
Kano et al., "5'-O-Alkyl and Acyl Prodrugs of 1-.beta.-D-Arabinofuranosyl-E-5-(2-bromovinyl)uracil," Antiviral Chem. & Chemotherapy, 5(1), 74-82 (1993).
Ijichi Katsushi
Kano Fumitaka
Machida Haruhiko
Sakata Shinji
Crane L. Eric
Robinson Douglas W.
Yamasa Shuyu Kabushiki Kaisha
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