Patent classifications
C07H11/00
Disaccharide intermediate and synthesis method thereof
The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.
Methods for treating Filoviridae virus infections
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: ##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Methods for treating Filoviridae virus infections
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: ##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
NON-ANIMAL CHONDROITIN SULFATE OLIGOSACCHARIDE AND PREPARATION METHOD THEREOF
The invention provides a non-animal chondroitin sulfate oligosaccharide and a preparation method thereof. The method includes a one-step chemical procedure and an enzyme catalysis procedure that are orderly carried out, including: extracting Escherichia coli K4 polysaccharide, chemically removing the fructosyl group therefrom, and degrading with a chondroitin sulfate degrading enzyme to obtain a chondroitin oligosaccharide mixture; preparing chondroitin disaccharide to octasaccharide by separation by separation by a centrifugal ultrafiltration tube, Bio-Gel P-2 gel exclusion chromatography, and high performance liquid chromatography (HPLC); and enzymatically modifying the obtained products by 4-O-sulfation and 6-O-sulfation, to obtain chondroitin sulfate CS-A and CS-C oligosaccharides respectively. The raw materials are from non-animal sources, the pollution risk is low, the reaction conditions are mild and efficient, and the structures and molecular weights of the prepared chondroitin sulfate disaccharide to octasaccharide are definite, providing possibility for the research of chondroitin sulfate oligosaccharides with single degrees of polymerization.
NON-ANIMAL CHONDROITIN SULFATE OLIGOSACCHARIDE AND PREPARATION METHOD THEREOF
The invention provides a non-animal chondroitin sulfate oligosaccharide and a preparation method thereof. The method includes a one-step chemical procedure and an enzyme catalysis procedure that are orderly carried out, including: extracting Escherichia coli K4 polysaccharide, chemically removing the fructosyl group therefrom, and degrading with a chondroitin sulfate degrading enzyme to obtain a chondroitin oligosaccharide mixture; preparing chondroitin disaccharide to octasaccharide by separation by separation by a centrifugal ultrafiltration tube, Bio-Gel P-2 gel exclusion chromatography, and high performance liquid chromatography (HPLC); and enzymatically modifying the obtained products by 4-O-sulfation and 6-O-sulfation, to obtain chondroitin sulfate CS-A and CS-C oligosaccharides respectively. The raw materials are from non-animal sources, the pollution risk is low, the reaction conditions are mild and efficient, and the structures and molecular weights of the prepared chondroitin sulfate disaccharide to octasaccharide are definite, providing possibility for the research of chondroitin sulfate oligosaccharides with single degrees of polymerization.
Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. 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 disclosure.
Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. 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 disclosure.
METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV:
##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV:
##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
ENZYMATIC SYNTHESIS OF HOMOGENEOUS CHONDROITIN SULFATE OLIGOSACCHARIDES
Methods of synthesizing chondroitin sulfate oligosaccharides are provided. Enzymatic schematic approaches to synthesizing structurally defined homogenous chondroitin sulfate oligosaccharides at high yields are provided. Synthetic chondroitin sulfate oligosaccharides ranging from 3-mers to 15-mers are provided.