The present invention is directed to 4′-substituted nucleoside derivatives of Formula I

##STR00001##

and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

The present invention is directed to 4′-substituted nucleoside derivatives of Formula I

##STR00001##

and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.

The present disclosure provides compounds of Formula (II) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W.sup.1, W.sup.2, W.sup.3, X, Y, and A are as described herein. The disclosed compounds modulate CD73 activity. The present disclosure also provides, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity.

Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base.

Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base.

This disclosure relates to nucleotide and nucleoside therapeutic compounds and uses in treating infectious diseases viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

This disclosure relates to nucleotide and nucleoside therapeutic compounds and uses in treating infectious diseases viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

Provided herein are bridged cyclic phosphates and phosphoramidates (bc-ProTides) of nucleosides, which is a compound, its stereoisomers, isotope-enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, with the following structure: ##STR00001##
These compounds can be used for the treatment of viral infections and/or neoplastic diseases in mammals. By optimizing combinations of Y.sub.2, Y.sub.3, R.sup.0, and M, the cleavability of these compounds as prodrugs can be attuned for different tissue targeting with various functional combinations. Also disclosed are processes and methods for preparation of these compounds.

Provided herein are bridged cyclic phosphates and phosphoramidates (bc-ProTides) of nucleosides, which is a compound, its stereoisomers, isotope-enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, with the following structure: ##STR00001##
These compounds can be used for the treatment of viral infections and/or neoplastic diseases in mammals. By optimizing combinations of Y.sub.2, Y.sub.3, R.sup.0, and M, the cleavability of these compounds as prodrugs can be attuned for different tissue targeting with various functional combinations. Also disclosed are processes and methods for preparation of these compounds.