C07H19/167

A PLATFORM FOR SCREENING NAD+ BINDING PROTEINS IN A CELLULAR CONTEXT
20230212213 · 2023-07-06 ·

Provided herein are novel compounds, compositions, that can used as clickable, photo-affinity labeling (PAL) probes methods for use in screening NAD+ binding proteins.

Solid-state forms of Regadenoson, their use and preparation
11535644 · 2022-12-27 · ·

The invention relates to a crystalline methanol or dimethyl sulfoxide solvated form of regadenoson and an anhydrous polymorph of regadenoson. The invention is also directed to the preparation of the methanol or dimethyl sulfoxide solvated and anhydrous solid-state forms of regadenoson. In particular, the invention relates to the preparation of the anhydrous polymorph of regadenoson in a stable form from the dimethyl sulfoxide solvated form of regadenoson, which preparation is purifiable and scalable.

Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers
11518780 · 2022-12-06 ·

Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.

6-HYDRAZINOADENOSINE COMPOUNDS WITH A2A ADENOSINE RECEPTOR AGONIST ACTIVITY
20220380402 · 2022-12-01 ·

The present disclosure provides 6-hydrazinoadenosine represented by the general Formula (I) and its derivatives with A.sub.2A adenosine receptor agonist activity, and pharmaceutical compositions containing them. The compound and composition can be used as A.sub.2A adenosine receptor agonists and used as medicament.

##STR00001##

6-HYDRAZINOADENOSINE COMPOUNDS WITH A2A ADENOSINE RECEPTOR AGONIST ACTIVITY
20220380402 · 2022-12-01 ·

The present disclosure provides 6-hydrazinoadenosine represented by the general Formula (I) and its derivatives with A.sub.2A adenosine receptor agonist activity, and pharmaceutical compositions containing them. The compound and composition can be used as A.sub.2A adenosine receptor agonists and used as medicament.

##STR00001##

2-BENZYLIDENE HYDRAZINOADENOSINE COMPOUNDS HAVING A2A ADENOSINE RECEPTOR AGONISTIC ACTIVITY
20220378816 · 2022-12-01 ·

2-Benzylidene hydrazinoadenosine compounds having A.sub.2A adenosine receptor agonistic activity, represented by a general Formula (I) and pharmaceutical compositions containing the same. The compounds and compositions can act as A.sub.2A adenosine receptor agonist to serve as medicaments.

##STR00001##

CD73 inhibitors and uses thereof

The present disclosure provides compounds of Formula (II) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W.sup.1, W.sup.2, W.sup.3, X, Y, and A are as described herein. The disclosed compounds modulate CD73 activity. The present disclosure also provides, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity.

METHODS AND COMPOSITIONS FOR NUCLEIC ACID SEQUENCING USING PHOTOSWITCHABLE LABELS
20230055284 · 2023-02-23 ·

Embodiments of the present disclosure relate to nucleotides labeled with photoswitchable compounds. Also provided herein are methods and kits of using these labeled nucleotides for sequencing applications.

ECTONUCLEOTIDASE INHIBITORS AND METHODS OF USE THEREOF

The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.

ECTONUCLEOTIDASE INHIBITORS AND METHODS OF USE THEREOF

The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.