C07H19/06

4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

The present invention is directed to 4′-substituted nucleoside derivatives of Formula I

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and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

Methods and devices to generate [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides
11707538 · 2023-07-25 · ·

Described herein are methods and devices that allow the generation of [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides (such as [F-18]tosyl fluoride) in a manner that is suitable for radiosynthesis of F-18 labeled radiopharmaceuticals using currently available synthesis modules.

Methods for the Epigenetic Analysis of DNA, Particularly Cell-Free DNA
20230235380 · 2023-07-27 ·

Methods are provided for the epigenetic analysis of cell-free DNA using organic boranes to convert oxidized 5-methylcytosine residues in the cell-free DNA to dihydrouracil (DHU) residues. Cell-free DNA is contacted with an organic borane selected to successively bring about reduction, deamination, and decarboxylation of oxidized 5-methylcytosine residues such as 5-carboxylcytosine and 5-formylcytosine, resulting in DHU residues in place thereof. Following amplification, the treated cell-free DNA is sequenced, with the DHU residues read as thymine residues. Reaction mixtures, kits and additional methods are also provided, as are related methods for the epigenetic analysis of DNA, including cell-free DNA.

Methods for the Epigenetic Analysis of DNA, Particularly Cell-Free DNA
20230235380 · 2023-07-27 ·

Methods are provided for the epigenetic analysis of cell-free DNA using organic boranes to convert oxidized 5-methylcytosine residues in the cell-free DNA to dihydrouracil (DHU) residues. Cell-free DNA is contacted with an organic borane selected to successively bring about reduction, deamination, and decarboxylation of oxidized 5-methylcytosine residues such as 5-carboxylcytosine and 5-formylcytosine, resulting in DHU residues in place thereof. Following amplification, the treated cell-free DNA is sequenced, with the DHU residues read as thymine residues. Reaction mixtures, kits and additional methods are also provided, as are related methods for the epigenetic analysis of DNA, including cell-free DNA.

ECTONUCLEOTIDASE INHIBITORS AND METHODS OF USE THEREOF
20230002437 · 2023-01-05 ·

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.

ORALLY-BIOAVAILABLE NUCLEOSIDE ANALOGS

Described herein are orally-bioavailable nucleoside analogs and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of coronavirus infections, including SARS-CoV-2 infection.

ORALLY-BIOAVAILABLE NUCLEOSIDE ANALOGS

Described herein are orally-bioavailable nucleoside analogs and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of coronavirus infections, including SARS-CoV-2 infection.

ECTONUCLEOTIDASE INHIBITORS AND METHODS OF USE THEREOF
20230022922 · 2023-01-26 ·

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.

GLYCOSIDE COMPOUND, AMIDITE COMPOUND, AND PRODUCTION METHOD FOR POLYNUCLEOTIDE USING SAID COMPOUNDS

The present invention provides an amidite compound capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound as an intermediate thereof, and a production method for a polynucleotide using the amidite compound. The present invention also provides an amidite compound of formula (1) capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound of formula (10) (in formulae (10) and (1), B.sup.a, R.sup.a, R.sup.b, R.sup.c, G.sup.1, G.sup.2, and G.sup.3 are as defined in the description, and R is represented by the following formulae), and a production method for a polynucleotide using the amidite compound.

GLYCOSIDE COMPOUND, AMIDITE COMPOUND, AND PRODUCTION METHOD FOR POLYNUCLEOTIDE USING SAID COMPOUNDS

The present invention provides an amidite compound capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound as an intermediate thereof, and a production method for a polynucleotide using the amidite compound. The present invention also provides an amidite compound of formula (1) capable of improving a yield and a purity of a polyoligonucleotide, a glycoside compound of formula (10) (in formulae (10) and (1), B.sup.a, R.sup.a, R.sup.b, R.sup.c, G.sup.1, G.sup.2, and G.sup.3 are as defined in the description, and R is represented by the following formulae), and a production method for a polynucleotide using the amidite compound.