Patent classifications
C07H19/12
2′-chloro nucleoside analogs for HCV infection
Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2-chloro nucleosides according to Formula 2001: ##STR00001##
or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.
SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
Silylated pyrimidine prodrugs and methods of their use
Silylated-pyrimidine prodrugs, compositions that include the silylated-pyrimidine prodrugs, methods for making the silylated-pyrimidine prodrugs and compositions, and methods for treating cancer using the silylated-pyrimidine prodrugs and compositions.
Silylated pyrimidine prodrugs and methods of their use
Silylated-pyrimidine prodrugs, compositions that include the silylated-pyrimidine prodrugs, methods for making the silylated-pyrimidine prodrugs and compositions, and methods for treating cancer using the silylated-pyrimidine prodrugs and compositions.
A METHOD FOR PREPARING A ß-NUCLEOSIDE COMPOUND
A method for preparing a -nucleoside compound, including the following steps: 1) performing a silylation reaction of a nitrogenous base or an analogue thereof in the presence of TMSOTf to give the nitrogenous base or the analogue thereof being protected by trimethylsilyl; 2) performing a direct glycosylation reaction of the reaction liquid, without being isolated, and a five- or six-membered ring saccharide or a derivative thereof closed by a hydroxyl protecting group to give a closed -nucleoside compound; and 3) performing a deprotection reaction to give the -nucleoside compound. The method uses a one-pot process to prepare the key intermediates of the -nucleoside compound, and the yield of materials in -configuration increases significantly. The method has the benefits of simple operations, being energy conservation and environment protection, and being suitable for industrial applications.
A METHOD FOR PREPARING A ß-NUCLEOSIDE COMPOUND
A method for preparing a -nucleoside compound, including the following steps: 1) performing a silylation reaction of a nitrogenous base or an analogue thereof in the presence of TMSOTf to give the nitrogenous base or the analogue thereof being protected by trimethylsilyl; 2) performing a direct glycosylation reaction of the reaction liquid, without being isolated, and a five- or six-membered ring saccharide or a derivative thereof closed by a hydroxyl protecting group to give a closed -nucleoside compound; and 3) performing a deprotection reaction to give the -nucleoside compound. The method uses a one-pot process to prepare the key intermediates of the -nucleoside compound, and the yield of materials in -configuration increases significantly. The method has the benefits of simple operations, being energy conservation and environment protection, and being suitable for industrial applications.
6-AZA-NUCLEOSIDE PRODRUGS AS ANTIVIRAL AGENTS FOR TREATING VIRUS INFECTIONS
The present disclosure is concerned with 6-aza-nucleoside prodrugs that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, human immunodeficiency virus (HIV), human papillomavirus (HPV), chicken pox, infectious mononucleosis, mumps, measles, rubella, shingles, ebola, viral gastroenteritis, viral hepatitis, viral meningitis, human metapneumovirus, human parainfluenza virus type 1, parainfluenza virus type 2, parainfluenza virus type 3, respiratory syncytial virus, viral pneumonia, yellow fever virus, tick-borne encephalitis virus, Chikungunya virus (CHIKV), Venezuelan equine encephalitis (VEEV), Eastern equine encephalitis (EEEV), Western equine encephalitis (WEEV), dengue (DENV), influenza, West Nile virus (WNV), zika (ZIKV), Middle East Respiratory Syndromes (MERS), Severe Acute Respiratory Syndrome (SARS), and coronavirus disease 2019 (COVID-19), using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
6-AZA-NUCLEOSIDE PRODRUGS AS ANTIVIRAL AGENTS FOR TREATING VIRUS INFECTIONS
The present disclosure is concerned with 6-aza-nucleoside prodrugs that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, human immunodeficiency virus (HIV), human papillomavirus (HPV), chicken pox, infectious mononucleosis, mumps, measles, rubella, shingles, ebola, viral gastroenteritis, viral hepatitis, viral meningitis, human metapneumovirus, human parainfluenza virus type 1, parainfluenza virus type 2, parainfluenza virus type 3, respiratory syncytial virus, viral pneumonia, yellow fever virus, tick-borne encephalitis virus, Chikungunya virus (CHIKV), Venezuelan equine encephalitis (VEEV), Eastern equine encephalitis (EEEV), Western equine encephalitis (WEEV), dengue (DENV), influenza, West Nile virus (WNV), zika (ZIKV), Middle East Respiratory Syndromes (MERS), Severe Acute Respiratory Syndrome (SARS), and coronavirus disease 2019 (COVID-19), using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
ALPHA-D-GALACTOSIDE INHIBITORS OF GALECTINS
The present invention relates to a compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore, the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.