C07H1/04

PURIFICATION OF TRIPHOSPHORYLATED OLIGONUCLEOTIDES USING CAPTURE TAGS

The present invention relates to a method of preparing triphosphate-modified oligonucleotides using a capture tag. The method allows the synthesis and purification of triphosphate-modified oligonucleotides in high yield and purity suitable for pharmaceutical applications.

TRINUCLEOTIDE CAP ANALOGS AND METHODS OF USE THEREOF

Described herein are novel trinucleotide cap analogs and methods of making and using the same. Also described herein is an RNA molecule comprising a 5-cap, wherein the 5-cap includes a trinucleotide cap analog as described herein. Methods of inducing a therapeutic effect in a 5 subject are also described herein, the methods including a step of administering to the subject an RNA molecule including the trinucleotide cap analog.

TRINUCLEOTIDE CAP ANALOGS AND METHODS OF USE THEREOF

Described herein are novel trinucleotide cap analogs and methods of making and using the same. Also described herein is an RNA molecule comprising a 5-cap, wherein the 5-cap includes a trinucleotide cap analog as described herein. Methods of inducing a therapeutic effect in a 5 subject are also described herein, the methods including a step of administering to the subject an RNA molecule including the trinucleotide cap analog.

C1-Phostphonate Analogue of UDP-GlcNAc for Inhibition of O-GlcNAc Transferase
20170022243 · 2017-01-26 ·

A novel C1-phosphate analogue of uridine-5-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be used as a useful tool in the studies on various vital phenomena in association with the protein modification by O-GlcNAc within cells and furthermore as a candidate substance in the treatment or research of diseases related to the protein modification by O-GlcNAc, such as cancers, diabetes, or degenerative neurological diseases.

Synthesis of 6-azido-6-deoxy-2-n-acetyl-hexosamine-nucleoside diphosphate

The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.

Synthesis of 6-azido-6-deoxy-2-n-acetyl-hexosamine-nucleoside diphosphate

The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.

SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE

The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.

SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE

The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.

Synthesis of an antiviral azasugar triphosphate

Provided are methods of making the active 5-triphosphate form of galidesivir (compound 1) and the active 5-triphosphate form of azasugar nucleoside analogues (compound 2): ##STR00001##
a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively: ##STR00002## ##STR00003##

Synthesis of an antiviral azasugar triphosphate

Provided are methods of making the active 5-triphosphate form of galidesivir (compound 1) and the active 5-triphosphate form of azasugar nucleoside analogues (compound 2): ##STR00001##
a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively: ##STR00002## ##STR00003##