C07H19/213

POLYMER LINKED MULTIMERS OF GUANOSINE-3', 5'-CYCLIC MONOPHOSPHATES

Embodiments of the invention are directed to new polymer linked multimeric guanosine-3′, 5′-cyclic monophosphate (cGMP) analogues that modulate the cGMP-signaling system, preferably having activating properties, and more preferably being activators of cGMP dependent protein kinase (PKG), and related monomeric precursors thereof. The invention is also directed to related monomeric compounds, which may also show modulating activity and/or may serve as monomeric precursors of the multimers. The invention further relates to the use of such compounds as reagents for signal transduction research and as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and as ligands for affinity chromatography, for antibody production or for diagnostic applications e.g. on chip surfaces.

CHIRAL PHOSPHORAMIDITE AUXILIARIES AND METHODS OF THEIR USE

Disclosed are P-stereogenic groups that may be used in the synthesis of compounds including stereochemically enriched P-stereogenic phosphorothioates. P-stereogenic groups may be provided in nucleoside phosphoramidites including a sugar bonded to a nucleobase and to a stereochemically enriched phosphoramidite as well as methods of their use and methods of making them.

CHIRAL PHOSPHORAMIDITE AUXILIARIES AND METHODS OF THEIR USE

Disclosed are P-stereogenic groups that may be used in the synthesis of compounds including stereochemically enriched P-stereogenic phosphorothioates. P-stereogenic groups may be provided in nucleoside phosphoramidites including a sugar bonded to a nucleobase and to a stereochemically enriched phosphoramidite as well as methods of their use and methods of making them.

PHOSPHOROUS (V)-BASED REAGENTS, PROCESSES FOR THE PREPARATION THEREOF, AND THEIR USE IN MAKING STEREO-DEFINED ORGANOPHOSHOROUS (V) COMPOUNDS

The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.

3′3′-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator

The present disclosure relates to 3′3′-cyclic dinucleotides having a carbocyclic nucleotide and derivatives that can modulate the activity of the STING adaptor protein.

PYRIDINIUM SALTS AS ACTIVATORS IN THE SYNTHESIS OF STEREODEFINED OLIGONUCLEOTIDES
20210355150 · 2021-11-18 ·

The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.

PYRIDINIUM SALTS AS ACTIVATORS IN THE SYNTHESIS OF STEREODEFINED OLIGONUCLEOTIDES
20210355150 · 2021-11-18 ·

The present invention relates to a method for preparing stereodefined phosphorothioate oligonucleotides, especially locked stereodefined phosphorothioate oligonucleotides with a high yield, using pyridinium acidic salts as a coupling activator.

NEW EQUATORIALLY MODIFIED POLYMER LINKED MULTIMERS OF GUANSINE-3', 5'-CYCLIC MONOPHOSPHATES

Embodiments of the invention are directed to new equatorially modified polymer linked multimers of guanosine-3′, 5′-cyclic monophosphate (cGMP) analogues that inhibit the cGMP-signaling system. The invention is also directed to related monomeric compounds, which may serve as monomeric precursors of the multimers, and/or also show itself inhibitory activity and/or impact the inhibitory activity of the related multimers. The invention further relates to the use of such compounds as reagents for signal transduction research and as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and as ligands for affinity chromatography, for antibody production or for diagnostic applications, e.g., on chip surfaces.

NEW EQUATORIALLY MODIFIED POLYMER LINKED MULTIMERS OF GUANSINE-3', 5'-CYCLIC MONOPHOSPHATES

Embodiments of the invention are directed to new equatorially modified polymer linked multimers of guanosine-3′, 5′-cyclic monophosphate (cGMP) analogues that inhibit the cGMP-signaling system. The invention is also directed to related monomeric compounds, which may serve as monomeric precursors of the multimers, and/or also show itself inhibitory activity and/or impact the inhibitory activity of the related multimers. The invention further relates to the use of such compounds as reagents for signal transduction research and as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and as ligands for affinity chromatography, for antibody production or for diagnostic applications, e.g., on chip surfaces.

Cyclopentane-Based Modulators of STING (Stimulator of Interferon Genes)

Compounds of the general formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.