C07H11/00

Oligosaccharide Compound for Inhibiting Intrinsic Coagulation Factor X-Enzyme Complex, and Preparation Method Therefor and Uses Thereof

A purified oligosaccharide compound having antithrombotic activity or a mixture of a homologous compound thereof and a pharmaceutically acceptable salt thereof, a preparation method for the mixture, a pharmaceutical composition containing the mixture, and uses thereof serving as an intrinsic factor X-enzyme (Xase) inhibitor in the preparation of drugs for preventing and/or treating thrombotic diseases.

Alpha-selective sialyl donor and its uses for preparation of sialosides
10435425 · 2019-10-08 · ·

Disclosed herein a sialyl donor and its use for the synthesis of gangliosides. The sialyl donor has the structure of, ##STR00001##
wherein, R.sub.1 and R.sub.2 are independently benzoyl, toluenesulfonyl, pivaloyl or acetyl optionally substituted with a halogen; and R.sub.3 is acetyl or (O)CCH.sub.2OH. In one preferred embodiment, in the sialyl donor of formula (I), R is acetyl. Also disclosed herein is a method of synthesizing a sialoside. The method comprises steps of: coupling the sialyl donor of formula (I) with a glycosyl acceptor having a primary hydroxyl group in the presence of N-iodosuccinimide (NIS) and trifluoromethanesulfonic acid (TfOH) under suitable conditions; and isolating the sialoside, which has an -glycosidic linkage. According to preferred embodiments, the coupling is conducted in a solvent selected from the group consisting of, CH.sub.3CN, CH.sub.3Cl, and CH.sub.2Cl.sub.2 at a temperature between 20 C. to 60 C. Additionally or optionally, the coupling is conducted in CH.sub.2Cl.sub.2 with the presence of a powdered molecular sieve at 40 C.

Alpha-selective sialyl donor and its uses for preparation of sialosides
10435425 · 2019-10-08 · ·

Disclosed herein a sialyl donor and its use for the synthesis of gangliosides. The sialyl donor has the structure of, ##STR00001##
wherein, R.sub.1 and R.sub.2 are independently benzoyl, toluenesulfonyl, pivaloyl or acetyl optionally substituted with a halogen; and R.sub.3 is acetyl or (O)CCH.sub.2OH. In one preferred embodiment, in the sialyl donor of formula (I), R is acetyl. Also disclosed herein is a method of synthesizing a sialoside. The method comprises steps of: coupling the sialyl donor of formula (I) with a glycosyl acceptor having a primary hydroxyl group in the presence of N-iodosuccinimide (NIS) and trifluoromethanesulfonic acid (TfOH) under suitable conditions; and isolating the sialoside, which has an -glycosidic linkage. According to preferred embodiments, the coupling is conducted in a solvent selected from the group consisting of, CH.sub.3CN, CH.sub.3Cl, and CH.sub.2Cl.sub.2 at a temperature between 20 C. to 60 C. Additionally or optionally, the coupling is conducted in CH.sub.2Cl.sub.2 with the presence of a powdered molecular sieve at 40 C.

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.

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.

PURE HEPTASULFATED DISACCHARIDES HAVING IMPROVED ORAL BIOAVAILABILITY

Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.

PURE HEPTASULFATED DISACCHARIDES HAVING IMPROVED ORAL BIOAVAILABILITY

Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.

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.