C07H19/23

SMALL-MOLECULE COMPOUND HAVING A2A ADENOSINE RECEPTOR ANTAGONISM
20220363710 · 2022-11-17 ·

The present application provides a small-molecule compound, represented by general Formula (I), having A.sub.2A adenosine receptor antagonistic activity and a pharmaceutical composition containing same. The compound and composition can be used as A.sub.2A adenosine receptor antagonistic agents.

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Phosphorous protecting groups and methods of preparation and use thereof

Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.

Phosphorous protecting groups and methods of preparation and use thereof

Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.

Methods of preparing 1′-cyano nucleosides

The present disclosure generally describes methods of preparing 1′-cyano nucleosides, such as a compound of Formula (I). For example, the compound of Formula (I) can be prepared from a compound of Formula (II-a) in a flow reactor.

Methods of preparing 1′-cyano nucleosides

The present disclosure generally describes methods of preparing 1′-cyano nucleosides, such as a compound of Formula (I). For example, the compound of Formula (I) can be prepared from a compound of Formula (II-a) in a flow reactor.

CD73 INHIBITORS

Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

CD73 INHIBITORS

Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Cyclic dinucleotides as sting agonists

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I), wherein R.sub.1, R.sub.1′, X.sub.1, B.sub.1, R.sub.2, R.sub.2′, B.sub.2, X.sub.2, R.sub.3, Z-M-Y, and Y.sub.1-M.sub.1-Z.sub.1 are as defined herein. ##STR00001##

Cyclic dinucleotides as sting agonists

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I), wherein R.sub.1, R.sub.1′, X.sub.1, B.sub.1, R.sub.2, R.sub.2′, B.sub.2, X.sub.2, R.sub.3, Z-M-Y, and Y.sub.1-M.sub.1-Z.sub.1 are as defined herein. ##STR00001##

MODIFIED SHORT INTERFERING NUCLEIC ACID (siNA) MOLECULES AND USES THEREOF

Described are short interfering nucleic acid (siNA) molecules comprising modified nucleotides, compositions, and methods and uses thereof.