Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1991-12-16
1995-09-12
Robinson, Douglas W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 46, 514 47, 514 48, 514 49, 514 50, 514 51, 514934, 536 2612, 536 2613, 536 267, 536 2672, 536 268, 536 2714, 536 276, 536 2781, 536 285, 536 2853, A61K 3170, C07H 1900
Patent
active
054496640
ABSTRACT:
Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine;
X and X' are H, OH or F, provided that at least one is H;
Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H;
Y' and Z together form a cyclic phosphate ester, provided that Y is H; or
Z is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, and
when X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine;
and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.
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Verheyden et al., Ann. N.Y. Acad. Sci. vol. 255, pp. 151-165 (1975).
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"Inhibition of HIV-Induced Cytopathogenicity in vitro by 3'-Azido-2',3'-Dideoxyguanosine", Heinz Hartmann, Gerhard Hunsmann and Fritz Eckstein, The Lancet, Jan. 3, 1987.
"Selective Inhibition of Human Immunodeficiency Virus (HIV) by 3'-Azido-2'-3'-Dideoxyguanosine in vitro", Masanori Baba, Rudi Pauwels, Jan Balzarini, Piet Herdewijn and Erik de Clercq, Biochemical and Biophysical Research Communications, pp. 1080-1086, Jun. 30, 1987.
Maag Hans
Prisbe Ernest J.
Verheyden Julien P. H.
Friedman Susan J.
Krubiner Alan M.
Leitereg Theodore J.
Robinson Douglas W.
Syntex (U.S.A.) Inc.
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