C07H19/207

PHOSPHORAMIDATE NUCLEOSIDE DERIVATIVES AS ANTICANCER AGENTS

This invention relates to derivatives of cladribine. The compounds are phosphoramidate derivatives in which the phosphoramidate moiety is situated on the 3′-hydroxyl group of cladribine. The invention also relates to pharmaceutical formulations of the cladribine derivatives and their use in methods of treatment. The compounds are useful in the treatment of cancer.

LABELED NUCLEOTIDE ANALOGS, REACTION MIXTURES, AND METHODS AND SYSTEMS FOR SEQUENCING

Labeled nucleotide analogs comprising at least one avidin protein, at least one dye-labeled compound, and at least one nucleotide compound are provided. The analogs are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The analogs are detectable with high sensitivity at desirable wavelengths. They contain structural components that modulate the interactions of the analogs with DNA polymerase, thus decreasing photodamage and improving the kinetic and other properties of the analogs in sequencing reactions. Also provided are nucleotide and dye-labeled compounds of the subject analogs, as well as intermediates useful in the preparation of the compounds and analogs. Compositions comprising the compounds, methods of synthesis of the intermediates, compounds, and analogs, and mutant DNA polymerases are also provided.

LABELED NUCLEOTIDE ANALOGS, REACTION MIXTURES, AND METHODS AND SYSTEMS FOR SEQUENCING

Labeled nucleotide analogs comprising at least one avidin protein, at least one dye-labeled compound, and at least one nucleotide compound are provided. The analogs are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The analogs are detectable with high sensitivity at desirable wavelengths. They contain structural components that modulate the interactions of the analogs with DNA polymerase, thus decreasing photodamage and improving the kinetic and other properties of the analogs in sequencing reactions. Also provided are nucleotide and dye-labeled compounds of the subject analogs, as well as intermediates useful in the preparation of the compounds and analogs. Compositions comprising the compounds, methods of synthesis of the intermediates, compounds, and analogs, and mutant DNA polymerases are also provided.

IMPROVED PROCESSES FOR THE PREPARATION OF GUADECITABINE AND INTERMEDIATES THEREOF
20210147466 · 2021-05-20 ·

Described are procedures and intermediates for the preparation of guadecitabine, and guadecitabine salts and solid state forms thereof.

IMPROVED PROCESSES FOR THE PREPARATION OF GUADECITABINE AND INTERMEDIATES THEREOF
20210147466 · 2021-05-20 ·

Described are procedures and intermediates for the preparation of guadecitabine, and guadecitabine salts and solid state forms thereof.

CELL INTERNALIZING COMPOUNDS

Provided herein are cell penetrating compounds having the Formula I:

##STR00001##

where, generally, each T is a thiol reactive group (e.g., a phosphorothioate), each L is a linker (e.g., a linear alkyl), and Y is a biologic (e.g., an antibody). Also provided are pharmaceutical compositions including the cell penetrating compounds, and methods of delivering the compound into a cell.

MODIFIED NUCLEOTIDE TRIPHOSPHATES FOR MOLECULAR ELECTRONIC SENSORS
20210139959 · 2021-05-13 ·

In various embodiments, a signal enhancement process for single molecule molecular sensors is disclosed along with new modified dNTPs. In general, the enhancement process comprises providing a molecular electronic sensor comprising a polymerase and providing a nucleotide template and modified dNTPs in appropriate buffers to the polymerase, wherein incorporation of the modified dNTPs during action of the polymerase enzyme provides an enhanced electrical signal or improved signal-to-noise ratio for the incorporation event relative to the performance with corresponding native dNTPs.

MODIFIED NUCLEOTIDE TRIPHOSPHATES FOR MOLECULAR ELECTRONIC SENSORS
20210139959 · 2021-05-13 ·

In various embodiments, a signal enhancement process for single molecule molecular sensors is disclosed along with new modified dNTPs. In general, the enhancement process comprises providing a molecular electronic sensor comprising a polymerase and providing a nucleotide template and modified dNTPs in appropriate buffers to the polymerase, wherein incorporation of the modified dNTPs during action of the polymerase enzyme provides an enhanced electrical signal or improved signal-to-noise ratio for the incorporation event relative to the performance with corresponding native dNTPs.

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.

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.