C07H19/207

PRODRUGS OF 4'-C-SUBSTITUTED-2-HALO-2'-DEOXYADENOSINE NUCLEOSIDES AND METHODS OF MAKING AND USING THE SAME

The present disclosure provides prodrugs of 4′-C-substituted-2-halo-2′-deoxyadenoside nucleosides, and compositions, methods, and kits thereof. Such compounds can be useful for treating viral infections including, but not limited to, human immunodeficiency virus.

Substituted nucleosides, nucleotides and analogs thereof

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Substituted nucleosides, nucleotides and analogs thereof

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

HIGHLY ACTIVE COMPOUNDS AGAINST COVID-19

The present invention is the use of purine nucleotide phosphoramidates or pharmaceutically acceptable salts thereof administered in an effective amount for the treatment or prevention of COVID-19, an infection caused by the SARS CoV-2 virus in a host, for example a human, in need thereof.

METHOD FOR MANUFACTURING PHOSPHONATE ESTERS AND METHOD FOR MANUFACTURING PHOSPHATE ESTERS
20230130333 · 2023-04-27 ·

The present invention provides a method for efficiently manufacturing a phosphonate ester by phosphonylating an alcohol under mild conditions, and a method for manufacturing a phosphate ester. In the method for manufacturing a phosphonate ester of the present invention, a compound represented by the formula (1) is reacted with a compound represented by the formula (2) in the presence of a zinc catalyst to obtain a compound represented by the formula (3).

##STR00001##

X represents an organic group. R.sup.1 represents an alkyl group. R.sup.2 represents an organic group.

METHOD FOR MANUFACTURING PHOSPHONATE ESTERS AND METHOD FOR MANUFACTURING PHOSPHATE ESTERS
20230130333 · 2023-04-27 ·

The present invention provides a method for efficiently manufacturing a phosphonate ester by phosphonylating an alcohol under mild conditions, and a method for manufacturing a phosphate ester. In the method for manufacturing a phosphonate ester of the present invention, a compound represented by the formula (1) is reacted with a compound represented by the formula (2) in the presence of a zinc catalyst to obtain a compound represented by the formula (3).

##STR00001##

X represents an organic group. R.sup.1 represents an alkyl group. R.sup.2 represents an organic group.

β-modified phosphoric acid compound precursor, β-modified phosphoric acid compound, reaction inhibitor and medicine containing the same, and method for inhibiting reaction

A β-modified phosphoric acid compound precursor that inhibits the progress of a phosphorylation reaction having a partial structure represented by ##STR00001##
where A.sub.1 represents —SR.sub.1, —S—S—R.sub.1, —SeR.sub.1, or —X, where X is a halogen selected from fluoro, chloro, bromo, and iodo; R.sub.1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.2 represents an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.1 and L.sub.2 may be linked to each other to form a 4 to 6-membered ring structure; L.sub.1 and L.sub.2 may each have a substituent; and the symbol * represents a bond to be bonded to a phosphate group by phosphorylation. Further, provided are a reaction inhibitor and a medicine, each of which includes the β-modified phosphoric acid compound precursor.

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##

3′ end caps, 5′ end caps and combinations thereof for therapeutic RNA

The disclosure relates to nucleic acids that contain modifications at the 5′-end, 3′-end or 5′-end and 3′-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.