Abstract: The disclosure relates to broad spectrum, direct acting antiviral agents. Disclosed is a group of novel nucleoside and nucleotide analogs having a 4-substituted imidazol-2-one heterocycle in place of the pyrimidine base of natural nucleic acid components and their prodrug derivatives (see Formula I).

Abstract: The disclosure relates to broad spectrum, direct acting antiviral agents. Disclosed is a group of novel nucleoside and nucleotide analogs having a 4-substituted imidazol-2-one heterocycle in place of the pyrimidine base of natural nucleic acid components and their prodrug derivatives (see Formula I).

Abstract: Multitargeted pyrimidine nucleoside carbamates, substituted with fluorine at both the base and the sugar moieties, are disclosed (see Formula I): where R=linear or branched alkyl (C1-7); R?=H, hydroxy protecting group; R?=H, phosphate ester, amino acid alkyl (C1-7) ester phoshoramidate, or phosphorodiamidate. The disclosed compounds are fluoropyrimidine prodrugs that are characterized by a novel combination of structural components that provide intracellular metabolites capable of 1) inhibiting several cellular enzymes required for the synthesis and proper functioning of DNA, and 2) causing DNA damage by misincorporation into DNA. By acting on multiple targets with different mechanisms of action, compounds of Formula I reduce the likelihood of the emergence of drug resistance, a major drawback of the use of nucleoside-based anticancer and antiviral drugs.

Abstract: Multitargeted pyrimidine nucleoside carbamates, substituted with fluorine at both the base and the sugar moieties, are disclosed (see Formula I): where R=linear or branched alkyl (C1-7); R?=H, hydroxy protecting group; R?=H, phosphate ester, amino acid alkyl (C1-7) ester phoshoramidate, or phosphorodiamidate. The disclosed compounds are fluoropyrimidine prodrugs that are characterized by a novel combination of structural components that provide intracellular metabolites capable of 1) inhibiting several cellular enzymes required for the synthesis and proper functioning of DNA, and 2) causing DNA damage by misincorporation into DNA. By acting on multiple targets with different mechanisms of action, compounds of Formula I reduce the likelihood of the emergence of drug resistance, a major drawback of the use of nucleoside-based anticancer and antiviral drugs.

Abstract: This invention provides new lipophilic dialkylaminomethylene prodrugs, particularly dialkylaminomethylene 2', 3'-dideoxynucleoside compounds and pharmaceutical compositions comprising said compounds which inhibit the replication of viruses.

Abstract: The invention provides new alkylaminomethylene 2',3'-dideoxynucleoside compounds and salts thereof.

Abstract: New compounds having utility for enhancing the activity of antifolates are disclosed of the formula: ##STR1## wherein X is selected from hydrogen ##STR2## and R" ; R' is selected from alkyl, alkenyl, alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heterocyclic aryl; R" is selected from ##STR3## and R'S; M is selected from OR and secondary amine; and R is selected from hydrogen, alkyl, acyloxymethyl, substituted and unsubstituted aryl, substituted and unsubstituted heterocyclic aryl, amino cation and metal cation.

Abstract: New compounds having utility for enhancing the activity of antifolates are disclosed of the formula: ##STR1## wherein X is selected from hydrogen ##STR2## and R"--; R' is selected from alkyl, alkenyl, alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heterocyclic aryl; R" is selected from ##STR3## and R'S; M is selected from OR and secondary amine; and R is selected from hydrogen, alkyl, acyloxymethyl, substituted and unsubstituted aryl, substituted and unsubstituted heterocyclic aryl, amino cation and metal cation.