52results about "Aminosugars" patented technology

The application belongs to the technical field of biological medicine, and particularly relates to a galactosamine-doxetaxel conjugate as well as a preparation method and application thereof. First, doxetaxel and 3,3'-diseleno-dipropionic acid are used as raw materials, and after heating reaction, 3,3'-diseleno-dipropionic acid doxetaxel is obtained. Then, the obtained 3,3'-diseleno-dipropionic acid doxetaxel and galactosamine are used as raw materials, and after heating reaction, galactosamine-3,3'-diseleno-dipropionic acid doxetaxel conjugate is obtained through column chromatography separation and purification. The obtained conjugate can be specifically recognized by endogenous lectin receptors (such as asialoglycoprotein receptor ASGPR) which are highly expressed on the surface of hepatoma cells, so as to be taken up by hepatoma cells through a receptor-mediated pathway, and has application prospect in the direction of hepatoma targeted treatment.

The invention relates to a novel chemical cross-linking agent with mass spectrum fragmentable trehalose disaccharide as a skeleton structure and a preparation method thereof. The cross-linking agent disclosed by the invention has the following characteristics: 1) trehalose disaccharide is used as a skeleton structure, so that the cross-linking agent has excellent biocompatibility; 2) the trehalose skeleton has a pair of symmetrical mass spectrum fragmentable glucosidic bonds, so that a cross-linked peptide fragment can be simplified into a conventional peptide fragment modified by a cross-linking agent fragment; 3) the enrichment of the cross-linked peptide fragment can be realized by the trehalose skeleton under the condition of not adding an enrichment handle; and 4) active groups of the cross-linking agent comprise but not limited to a plurality of reactive groups such as succinamide ester, diaziridine, phenylsulfonyl fluoride, hydrazide group, amino group, hydroxylamine group and the like, and chemical cross-linking of a plurality of amino acids except lysine is realized. The trehalose cross-linking agent disclosed by the invention is applied to the field of proteomics, and provides technical support for realizing large-scale analysis of a protein complex in a complex sample, spatial structure analysis of protein and a protein-protein interaction network.

The invention discloses a partial acylated non-natural sugar for metabolic labeling and application, the partial acylated non-natural sugar is a mannose type of a pyranose structure, and 1-hydroxyl and 6-hydroxyl are protected by hydrophobic groups. According to the method, the advantages of existing non-natural sugar are taken into consideration, it is guaranteed that the non-natural sugar can be efficiently utilized by cells, S side reaction of the non-natural sugar and cysteine in protein in the metabolism process is effectively avoided, and meanwhile efficient metabolism marking is achieved. In a cell test, the use concentration of the 1, 6-diacylated non-natural sugar is one order of magnitude lower than that of the non-natural sugar without the protecting group.

The application discloses an enzyme method for synthesizing unnatural sugar and application thereof, and belongs to the technical field of organic chemical synthesis. The unnatural sugar comprises an unnatural sugar obtained by introducing an acyl group into a hydroxyl group at the 6th position of a bare sugar through an acylation reaction; and the bare sugar is obtained by performing derivatization modification on an amide site of a natural sugar. The synthesis method uses a SubC enzyme as a catalyst to realize selective acylation of the hydroxyl group at the 6th position of the bare sugar, and synthesizes the unnatural sugar with an ideal yield. The unnatural sugar can be applied to glycomics metabolic labeling and mass spectrometry analysis as a marker, has excellent biological safety, specificity and labeling efficiency, can avoid non-specific labeling, and has no obvious cytotoxicity.

Methods for chemically modifying bioactive triterpene compounds to increase the bioavailability thereof. The resulting triterpene chemical compounds, having enhanced bioavailability, are useful in pharmaceutical compositions, alone, in combination with, or complexed with therapeutic drugs for the treatment of diseases such as cancers.

The application discloses a full synthesis method of fortimicin B and derivatives thereof, and specifically, the method comprises the following steps: 3-ester group-2-pyrone and N-substituted-2-oxazolone are subjected to asymmetric reverse electron demand Diels-Alder reaction to generate a bridged lactone intermediate, then a series of transformations are performed to obtain an amino cyclic polyol fragment fortimicin B derivative; amino aldehyde and halogenated amino acid ester are subjected to carbon-carbon bond generation reaction mediated by divalent chromium and monovalent cobalt to obtain an amino alcohol intermediate, and subsequent transformation is performed to obtain an amino sugar fragment 6-isomer-erythromycin amine derivative; under the action of a gold catalyst, stereoselective glycosidation reaction occurs between the amino cyclic polyol fragment fortimicin B derivative and the amino sugar fragment 6-isomer-erythromycin amine derivative, ring opening and deprotection steps are performed, and fortimicin B and derivatives thereof are obtained. The synthesis route is short, the operation is simple, raw materials and reagents are easy to obtain, the synthesis route has the advantages of modularity and divergence, and fortimicin B and derivatives thereof which are difficult to synthesize according to the prior art can be synthesized.

The invention relates to a preparation method and application of a sialylated glycan derivative, which comprises the following steps of: uniformly mixing chemically modified sialic acid monosaccharide with a receptor substrate, cytidine triphosphate (CTP), MgCl2, a CMP-sialic acid synthetase preferable mutant and sialyltransferase, transferring a sialic acid derivative to a 3-site or 6-site hydroxyl group on non-reducing end galactose of glycan by a one-pot enzymatic method, and carrying out reaction to obtain the sialylated glycan derivative. And collecting a reaction product to obtain the sialylated glycan derivative. The method is simple and can be used for editing glycans on the surfaces of the immune cells so as to enhance the specificity and cytotoxicity of the immune cells to tumor cells.

The application discloses a kind of glucosamine hydrochloride crude product purification refining process, comprising the following steps: (1) glucosamine hydrochloride crude product is dissolved in water, then add the composite precipitant consisting of sodium chloride and sodium hydroxide, after standing, solid-liquid separation, collected separated liquid phase.(2) after the liquid phase is concentrated, add sodium percarbonate and mix evenly and stand still.After completion, pass in carbon dioxide to convert sodium hydroxide in concentrated solution into sodium carbonate, then continue to add calcium nitrate under stirring condition to make carbonate ion in system complete precipitation, i.e., the liquid to be extracted is obtained.(3) after the liquid to be extracted is cooled, add ethanol for alcohol precipitation, after completion, carry out solid-liquid separation, and the obtained solid product and separated liquid are collected respectively.The solid product is washed with ethanol and dried, and glucosamine hydrochloride finished product is obtained.The above process not only can improve the purity of glucosamine hydrochloride, but also can improve the yield of glucosamine hydrochloride in alcohol precipitation process, thereby reducing waste.

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

The present disclosure belongs to the field for preparation of chitosan oligosaccharide, and particularly relates to a chitosan oligosaccharide sulfate and a preparation method thereof. The method is as follows: adding an equal volume of 1.0%-2.0% by mass of potassium sulfate solution into 2.0%-4.0% by mass of chitosan oligosaccharide hydrochloride solution and evenly mixing to obtain a mixed solution, allowing a molar ratio of amino to sulfate ions in the mixed solution to be 2:1, then adding absolute ethyl alcohol to obtain a chitosan oligosaccharide sulfate suspension, standing, filtering, collecting precipitates, washing, drying and smashing to finally obtain the chitosan oligosaccharide sulfate. This method cleverly utilizes a characteristic that the chitosan oligosaccharide sulfate is difficultly dissolved into 75% ethyl alcohol aqueous solution, while potassium chloride is slightly dissolved into 75% ethyl alcohol aqueous solution, the chitosan oligosaccharide sulfate is obtained using a precipitation method. Moreover, the preparation method used in the present disclosure is simple to operate, economic and environmental-friendly, does not need the use of highly corrosive sulfuric acid, and is friendly to operation staffs, environments and production equipment.

Compounds and compositions are described that have an asialoglycoprotein receptor (ASGPR) binding ligand conjugated to an extracellular protein binding ligand that selectively degrades target extracellular proteins in vivo to treat disorders mediated by the extracellular proteins.

The present invention relates to a process for the synthesis of at least one C-glycoside comprising the following successive steps: (A) the introduction into a first mechanochemical reactor, separately or previously mixed, of at least one sugar in the form of pyranose and / or furanose and of the D and / or L series, said sugar having at least one hydroxyl function at the obligatorily free anomeric position, of a first reagent which is a β-diketone and of a base, in order to form a first initial mixture; (B1) at least a first grinding of said first initial mixture at a temperature greater than or equal to 20°C, in said first mechanochemical reactor, for a residence time less than or equal to 6 hours, so as to form a ketone C-glycoside; (C) the recovery at the outlet of the first mechanochemical reactor of a final mixture.The present invention also relates to the use of the mechanochemical reactor for synthesizing a C-glycoside or a C-glycoside derivative comprising said at least C-glycoside. Figure for the abstract: no figure.

The invention relates to uridine diphosphate-N-difluoroacetyl galactosamine as well as a preparation method and application thereof. The chemical structure of the UDP-GalNDFA is similar to that of a natural substrate UDP-GalNAc, and the core difference is that N-acetyl at the site 2 of the UDP-GalNDFA is replaced by N-difluoroacetyl. The preparation method comprises the following steps: (1) preparing difluoroacetyl galactosamine; and (2) preparing the UDP-GalNDFA by taking the difluoroacetyl galactosamine as a substrate. As a novel artificial donor sugar, the UDP-GalNDFA has the characteristics of high activity, difficulty in hydrolysis and capability of being artificially synthesized. Compared with the existing donor sugar UDP-GalNTFA, the glucose UDP-GalNTFA has higher catalytic activity on glycosyl transferase, has stronger stability, is not easy to hydrolyze, and can be used as a donor substrate for synthesizing a chondroitin oligosaccharide skeleton, a chondroitin oligosaccharide intermediate and a chondroitin oligosaccharide derivative by a chemical enzyme method.

The object of the present invention is to provide novel means that can be used for solubilizing proteins with poor water solubility. Provided is a hydrophilic solubilizing group for proteins or peptides, comprising a sugar chain moiety; and a functional group moiety that is bound to the amino or carboxy group of said sugar chain, and that binds to the amino acid side chain and can be detached from said protein or amino acid side chain in the presence of an acid.

This invention discloses a comprehensive preparation process for vegetarian glucosamine hydrochloride, comprising the following steps: (1) adding hydrochloric acid to a clarified fermentation broth for hydrolysis, followed by neutralization with alkali to obtain a hydrolysate containing glucosamine hydrochloride. Ethanol is added to the hydrolysate for alcohol precipitation, followed by solid-liquid separation, and the resulting ethanol waste liquid and crude glucosamine hydrochloride are collected separately. (2) The crude glucosamine hydrochloride is reconstituted, and a decolorizing agent is added for decolorization under light. After completion, the decolorizing agent is separated, and the resulting decolorized liquid is concentrated and then ethanol is added for further alcohol precipitation, followed by solid-liquid separation, and the resulting ethanol waste liquid and vegetarian glucosamine hydrochloride product are collected separately. This process not only facilitates the recycling of ethanol waste liquid generated during alcohol precipitation but also forms a decolorizing agent that can achieve decolorization and purification of crude glucosamine, thus improving the purity of glucosamine.

There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.

The document describes compounds and novel targeted ligands that can be linked to therapeutic compounds useful for directing the compounds to their in vivo targets. [Solution] The targeted ligands disclosed herein are useful for targeting expression inhibitory oligomeric compounds, such as RNAi agents, to liver cells in order to regulate gene expression. When bound to therapeutic compounds, the targeted ligands disclosed herein can be used in a variety of applications, including therapeutic, diagnostic, target validation, and genome discovery applications. Compositions comprising the targeted ligands disclosed herein, when bound to expression inhibitory oligomeric compounds, can mediate the expression of target nucleic acid sequences in liver cells, such as hepatocytes, and may be useful in treating diseases or disorders that respond to inhibition of gene expression or activity in cells, tissues, or organisms.

The present invention relates to a composition for use in the prevention or treatment of gastrointestinal infections / inflammation in infants or young children. The present invention relates to a nutritional composition comprising at least one fucosylated oligosaccharide and at least one N-acetylated oligosaccharide in specific proportions for use in the prevention and / or treatment of gastrointestinal infections and / or gastroenteritis in infants or young children.

A prebiotic oligosaccharide composition, comprising: (a) at least 8% by weight of Gal-(β1-3)-Gal-(β1-4)-X, based on the total weight of the oligosaccharide compounds present in the composition; a (b) at least 3% by weight of Gal-(β1-3)-Gal-(β1-3)-X b and (c) at least 5% by weight of Gal-(β1-3)-Gal-(β1-2)-X. c wherein X a , X b and X c and (b) are each independently selected from monosaccharides. These compositions contain relatively high amounts of oligosaccharide compounds (a), (b) and (c) and relatively high amounts of β1-3 Gal-Gal linkages compared to known oligosaccharide compositions. These particular characteristics of the compositions are believed to provide benefits to the gut health of consumers, for example, because these compositions provide increased production of butyric acid in the gut of consumers compared to known compositions. Methods for preparing the compositions and uses of the compositions as dietary supplements or medicaments are also disclosed.

The invention discloses a chitosan oligosaccharide zwitterionic corrosion inhibitor containing a long-chain structure, a preparation method and application, belongs to the technical field of preparation of corrosion inhibitors, and solves the technical problem that existing chitosan oligosaccharide is poor in solubility and corrosion inhibition effect. The method comprises the following steps: firstly, dissolving chitosan oligosaccharide with the molecular weight of less than 2000 serving as a raw material to obtain a chitosan oligosaccharide solution; and further modifying the chitosan oligosaccharide zwitterionic corrosion inhibitor with 12-amino dodecanoic acid and 1, 3-propane sultone to obtain the chitosan oligosaccharide zwitterionic corrosion inhibitor which has a long-chain structure and contains a quaternary ammonium cation group and a sulfonic acid anion group. The chitosan oligosaccharide containing a long-chain structure is prepared, the corrosion inhibition effect of the corrosion inhibitor is improved, a physical'electrostatic adsorption 'and'chemical coordination' system is constructed, the raw materials are easy to obtain, and the prepared chitosan oligosaccharide zwitterionic corrosion inhibitor meets the requirements of sustainable and green development and is especially suitable for strong acid working conditions.

Methods for chemically modifying bioactive triterpene compounds to increase the bioavailability thereof. The resulting triterpene chemical compounds, having enhanced bioavailability, are useful in pharmaceutical compositions, alone, in combination with, or complexed with therapeutic drugs for the treatment of diseases such as cancers.

Described herein are bifunctional compounds for removing macrophage migration inhibitory factor (MIF) or immunoglobulin G (IgG). Further described herein are pharmaceutical compositions comprising these bifunctional compounds. Further described herein are methods for treating pathologies and / or conditions with said compounds or compositions. The pathologies and / or conditions are mediated through MIF / IgG or where MIF / IgG is a contributing factor in the development and perpetuation of diseases and / or conditions, such as autoimmune diseases and cancers, among others. TIFF2025509736000504.tif99145

Fibroblast activation protein (FAP) targeting compounds; methods for imaging cancer and fibrosis; and methods for treating fibrosis, inflammatory diseases / disorders and cancer.

The utility model discloses a purification device for chitosan oligosaccharide drug preparation, which comprises a tank body, the bottom of the tank body is fixedly communicated with a conical discharge pipe, the outer wall of the tank body is fixedly communicated with a feed pipe, the top of the tank body is inserted with a movable rod, and the bottom end of the movable rod penetrates through the tank body and is fixedly connected with a mounting block. Scraping assemblies attached to the inner wall of the tank body all the time are connected to the four side walls of the mounting block correspondingly, and the movable rods, the mounting block, the scraping assemblies, the fixing shell, the first driving motor, the mounting frame and the power assembly are arranged and used in cooperation, so that the scraping assemblies can be driven by the first driving motor to rotate; the scraping assembly can be moved from top to bottom along the axial direction of the tank body through the power assembly, so that attachments on the inner wall of the tank body can be comprehensively scraped, the influence of residues on a subsequent purification process is avoided, and the cleanliness and the purification effect of the purification equipment are ensured; meanwhile, material waste is avoided.

The present disclosure relates generally to fluorinated glucosamine analogs and uses thereof, including analogs of N-acetyl glucosamine fluorinated at 4- and / or 6-position(s) and derivatives of xylose at anomeric position for the treatment of a neurological disease, such as multiple sclerosis; inflammation; cancer; central nervous system injury; or conditions associated with up-regulation of an extracellular matrix, such as chondroitin sulfate proteoglycans.

The present invention provides a method for obtaining a dealkoxyphenylated product in high yield from a substrate such as a sugar bonded via an oxygen atom to an alkoxyphenyl group. By reacting a lambda 3 -iodide with a substrate bonded via an oxygen atom to a phenyl group substituted with a C1-C5 alkoxy group in the para or ortho position in a fluorine-containing alcohol and water, a dealkoxyphenylated product can be obtained in high yield under mild conditions.

The invention belongs to an enzyme inhibitor, and particularly relates to a chitin synthetase inhibitor (novel acetylglucosamine thiourea glycoside conjugate) as well as preparation and application thereof. The invention relates to an application of a novel acetylglucosamine thiourea glycoside conjugate as shown in a formula I in serving as a chitin synthetase inhibitor. The glycoside conjugate disclosed by the invention is novel in structure, has good biological safety and chitin synthetase inhibitory activity, and has the potential of becoming a novel chitin synthetase inhibitor.