C07H19/14

Functionalized N-acetylgalactosamine nucleosides

Embodiments of the present application relate to N-acetylgalactosamine-conjugated nucleosides. In particular, the N-acetylgalactosamine is installed on the nucleobase of the nucleosides through a wide variety of linkers. Methods of making N-acetylgalactosamine-conjugated nucleosides are also disclosed herein. N-acetylgalactosamine is a well-defined liver-targeted moiety and N-acetylgalactosamine-conjugated nucleosides may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

Functionalized N-acetylgalactosamine nucleosides

Embodiments of the present application relate to N-acetylgalactosamine-conjugated nucleosides. In particular, the N-acetylgalactosamine is installed on the nucleobase of the nucleosides through a wide variety of linkers. Methods of making N-acetylgalactosamine-conjugated nucleosides are also disclosed herein. N-acetylgalactosamine is a well-defined liver-targeted moiety and N-acetylgalactosamine-conjugated nucleosides may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

NUCLEOTIDE ANALOGUES

Disclosed herein, interalia, are compounds, compositions, and methods of using the same for the sequencing of a nucleic acid.

NUCLEOTIDE ANALOGUES

Disclosed herein, interalia, are compounds, compositions, and methods of using the same for the sequencing of a nucleic acid.

5′-substituted nucleoside compounds

The present invention relates to novel 5′-substituted nucleoside compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer, in particular glioblastomas, melanoma, sarcomas, gastric cancer, pancreatic cancer, cholangiocarcinoma, bladder cancer, breast cancer, non-small cell lung cancer, leukemias including acute myeloid leukemia, and lymphomas.

5′-substituted nucleoside compounds

The present invention relates to novel 5′-substituted nucleoside compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer, in particular glioblastomas, melanoma, sarcomas, gastric cancer, pancreatic cancer, cholangiocarcinoma, bladder cancer, breast cancer, non-small cell lung cancer, leukemias including acute myeloid leukemia, and lymphomas.

Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides
09828409 · 2017-11-28 ·

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.

Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides
09828409 · 2017-11-28 ·

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.

ANALOGS OF ADENOSINE MONOPHOSPHATE (AMP) AS INHIBITORS OF UBIQUITIN-LIKE MODIFIER-ACTIVATING ENZYME ATG7
20170312284 · 2017-11-02 · ·

Disclosed are analogs of adenosine monophosphate (AMP) as inhibitors of ubiquitin-like modifier-activing enzyme ATG7. The AMP analogs may be formulated as pharmaceutical compositions for treating diseases or disorders that depend on ATG7 activity and/or autophagy such as cell proliferative diseases and disorders.

Modulators of 5′-nucleotidase, ecto and the use thereof

Compounds that modulate the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided.