Patent classifications
C07H19/207
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.
Phosphoramidate nucleoside derivatives as anticancer agents
This invention relates to derivatives of cladribine of Formula (I). 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. ##STR00001##
Phosphoramidate nucleoside derivatives as anticancer agents
This invention relates to derivatives of cladribine of Formula (I). 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. ##STR00001##
Inhibitors of adenosine 5′-nucleotidase
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.
Inhibitors of adenosine 5′-nucleotidase
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.
METHOD OF SOLID-PHASE NUCLEIC ACID SYNTHESIS AND SOLUTION COMPOSITION FOR SOLID-PHASE NUCLEIC ACID SYNTHESIS
This invention is intended to discover a novel solvent that can be used as an alternative to toluene in the step of deprotection in the method of solid-phase nucleic acid synthesis. With the use of such novel solvent, various problems caused by the use of toluene are dissolved.
This invention is also intended to provide a method of solid-phase nucleic acid synthesis in which protected nucleoside phosphoramidites in which a protective group is bonded to a hydroxyl group at the 5position or the 3 position of a nucleoside are sequentially bound on a solid phase carrier, where a reaction of removing the protecting group from the protected nucleoside phosphoramidite is carried out in a solution comprising an acid with a pKa of 0.2 to 0.8 and acetonitrile.
METHOD OF SOLID-PHASE NUCLEIC ACID SYNTHESIS AND SOLUTION COMPOSITION FOR SOLID-PHASE NUCLEIC ACID SYNTHESIS
This invention is intended to discover a novel solvent that can be used as an alternative to toluene in the step of deprotection in the method of solid-phase nucleic acid synthesis. With the use of such novel solvent, various problems caused by the use of toluene are dissolved.
This invention is also intended to provide a method of solid-phase nucleic acid synthesis in which protected nucleoside phosphoramidites in which a protective group is bonded to a hydroxyl group at the 5position or the 3 position of a nucleoside are sequentially bound on a solid phase carrier, where a reaction of removing the protecting group from the protected nucleoside phosphoramidite is carried out in a solution comprising an acid with a pKa of 0.2 to 0.8 and acetonitrile.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF DISEASE
Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF DISEASE
Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof.
Methods for the use of 5′-adenosine diphosphate ribose (ADPR)
The present invention is directed to methods for the use of 5-adenosine diphosphate ribose (ADPR), and compositions thereof, for treating, managing, or preventing adenovirus-related diseases or conditions, eye disorders, cancer, or diseases or conditions caused by infection, inflammation, or physical, chemical, thermal, or radiation injuries.