2'3'-dideoxy-2',3'-didehydro-7,8-disubstituted guanosines and th

Details 2'3'-dideoxy-2',3'-didehydro-7,8-disubstituted guanosines and th 2'3'-dideoxy-2',3'-didehydro-7,8-disubstituted guanosines and th

1994-05-27

1995-08-15

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 2714, 536 2781, A61K 3170, C07H 19173

Patent

active

054419425

ABSTRACT:
Immunostimulating 7,8-disubstituted guanine derivatives that also contain a .beta.-9,1'-linked-2',3'-dideoxy-2',3'-didehydroribosyl substituent are disclosed whose structures are represented by Formula I ##STR1## wherein X is O or S; R.sup.1 is a hydrocarbyl or substituted hydrocarbyl moiety having a length of about one to about seven carbon atoms; R.sup.2 is hydrogen or C.sub.1 -C.sub.8 acyl; and the pharmaceutically acceptable base addition salts thereof. Also disclosed are compositions containing an immunostimulating guanine derivative and processes for using the same.

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Lien et al., "Physical Factors Contributing to the Partition Coefficients and Retention Time of 2',3'-Dideoxynucleosides Analogues," J. Pharmaceutical Sci., 80(6), 517-521 (1991).
Chu et al. (I), "General Synthesis of 2',3'-Dideoxynucleosides and 2',3'-Didehydro-2',3'-Dideoxynucleosides," J. Organic Chem., 54(9), 2217-2225 (1989).
Balzarini et al., "Estimation of the Lipophilicity of Anti-HIV Nucleoside Analogues by Determination of the Partition Coefficient and Retention Time on a Lichrospher 60 RP-8 HPLC Column," Biochem. Biophys. Res. Comm., 158(2), 413-422 (1989).
Chu et al. (II), "Comparative Activity of 2',3'-Saturated and Unsaturated Pyrimidine and Purine Nucleosides Against Human Immunodeficiency Virus Type 1 in Peripheral Blood Mononuclear Cells," Biochem. Pharmacology, 37(19), 3543-3548 (1988).
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