The present invention relates to novel compounds, compositions and methods for
inhibiting the growth, elaboration and/or replication of HIV in human patients
and to the prevention and treatment of human acquired immunodeficiency syndrome
(AIDS) and other diseases caused by retroviral infection. More particularly, in
preferred aspects, the present invention provides a method for the use of novel
prodrug forms of 9-(2,3-Dideoxy--D-glycero-pent-2-enofuranosyl) guanine
(d4G) for the prevention and treatment of both wild type and drug-resistant Human
Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according
to the present invention are based upon the chemical formula:
##STR1##
where X is OCH3, N3, NHCH3, N(CH3)2
or an aminocyclopropyl group;
- R1 is H or a C1 to C20 acyl or ether
group, a phosphate, diphosphate, triphosphate or phosphodiester group; and
- R2 is H or a C1 to C20 acyl or alkyl group.