Patent classifications
C07H19/04
CD73 inhibitors and therapeutic uses thereof
This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers. ##STR00001##
CD73 inhibitors and therapeutic uses thereof
This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers. ##STR00001##
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.
SYNTHESES, ACTIVITIES, AND METHODS OF USE OF DIHYDRONICOTINAMIDE RIBOSIDE DERIVATIVES
Disclosed is a compound of formula (I):
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, and are as defined herein. Also disclosed are methods for increasing mammalian cell NAD.sup.+ production and improving mitochondrial cell densities comprising administering to a cell the compound or a salt thereof.
SYNTHESES, ACTIVITIES, AND METHODS OF USE OF DIHYDRONICOTINAMIDE RIBOSIDE DERIVATIVES
Disclosed is a compound of formula (I):
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, and are as defined herein. Also disclosed are methods for increasing mammalian cell NAD.sup.+ production and improving mitochondrial cell densities comprising administering to a cell the compound or a salt thereof.
EFFICIENT AND SCALABLE SYNTHESES OF NICOTINOYL RIBOSIDES AND REDUCED NICOTINOYL RIBOSIDES, MODIFIED DERIVATIVES THEREOF, PHOSPHORYLATED ANALOGS THEREOF, ADENYLYL DINUCLEOTIDE CONJUGATES THEREOF, AND NOVEL CRYSTALLINE FORMS THEREOF
The present disclosure provides methods of making nicotinoyl riboside compounds or derivatives of formula (I):
##STR00001##
wherein X.sup.−, Z.sup.1, Z.sup.2, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are described herein, reduced analogs thereof, modified derivatives thereof, phosphorylated analogs thereof, and adenylyl dinucleotide conjugates thereof, or salts, solvates, or prodrugs thereof; and novel crystalline forms thereof.
Efficient and scalable syntheses of nicotinoyl ribosides and reduced nicotinoyl ribosides, modified derivatives thereof, phosphorylated analogs thereof, adenylyl dinucleotide conjugates thereof, and novel crystalline forms thereof
The present disclosure provides methods of making nicotinoyl riboside compounds or derivatives of formula (I): ##STR00001##
wherein X.sup.−, Z.sup.1, Z.sup.2, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are described herein, reduced analogs thereof, modified derivatives thereof, phosphorylated analogs thereof, and adenylyl dinucleotide conjugates thereof, or salts, solvates, or prodrugs thereof; and novel crystalline forms thereof.
CRYSTAL FORM, PREPARATION METHOD, AND APPLICATION OF 4′-SUBSTITUTED NUCLEOSIDE
The present invention discloses a crystal form, a preparation method and an application of a 4′-substituted nucleoside compound I having the following structure, including salts, prodrugs, and compositions thereof. Animal pharmacokinetic studies demonstrated that the effective drug concentrations of Compound Ia and Compound Ig in HIV target cells, peripheral blood mononuclear cells (PBMC), were effective in inhibiting HIV replication after 7 and 5 days, respectively. Therefore, Compound I can be used as a long-acting drug for preventing and treating AIDS. R is selected from ethynyl, azide, and cyano groups, X is selected from hydrogen and fluorine, and B is selected from B1 and B2.
SPHERICAL NUCLEIC ACIDS WITH DENDRITIC LIGANDS
The present disclosure is directed to spherical nucleic acids (SNAs) comprising a nanoparticle core and an oligonucleotide dendron attached thereto. The disclosure also provides methods of using the SNAs for, for example, gene regulation and immune regulation.
SPHERICAL NUCLEIC ACIDS WITH DENDRITIC LIGANDS
The present disclosure is directed to spherical nucleic acids (SNAs) comprising a nanoparticle core and an oligonucleotide dendron attached thereto. The disclosure also provides methods of using the SNAs for, for example, gene regulation and immune regulation.