Abstract: A process for producing a polysaccharide sponge comprises the steps of (A) freezing a photoreactive polysaccharide solution, and (B) irradiating the frozen photoreactive polysaccharide solution with light to crosslink the photoreactive polysaccharide, thereby obtaining the polysaccharide sponge. The process includes simplified steps requiring no removal of solvent, and has such an advantage that impurities are easily removed therefrom.

Abstract: The present invention for the stereoselective preparation of 2-deoxy-?-D-adenine nucleosides wherein a blocked 2-deoxy-?-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.

Abstract: Glycopeptide having at least one asparagine-linked oligosaccharide at a desired position of the peptide chain which is obtained by: (1) esterifying hydroxyl of a resin and carboxyl of an amino acid having amino group nitrogen protected with a fat-soluble protective group (AGFPG), (2) removing the protective group to form a free amino group, (3) amidating the free amino group and carboxyl of an amino acid having AGFPG, (4) removing the protective group, (5) repeating the steps (3) and (4), (6) amidating the free amino group and carboxyl of the asparagine portion of an asparagine-linked oligosaccharide having AGFPG, (7) removing the protective group, (8) amidating the free amino group and carboxyl of an amino acid having AGFPG, (9) repeating steps (7) and (8), (10) removing the protective group, and (11) cutting off the resin with an acid; glycopeptide obtained by transferring sialic acid or a derivative thereof to the above glycopeptide.

Abstract: The invention relates to a long-acting formulation of biopharmaceutical, more specifically an aptamer therapeutics. A branched PEGylated aptamer or a hyaluronic acid (HA) derivative of which degradation in vivo is regulated is linked by the bioconjugation with biopharmaceutical to produce the long-action formulation.

Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.

Abstract: A process for preparing a sterile ready-to-use aqueous pharmaceutical formulation comprises a high molecular weight hyaluronic acid salt (HA) at a specified concentration, comprising the steps of: providing an aqueous formulation comprising high molecular weight HA at a concentration of less than the specified final concentration; passing said aqueous formulation through a filter having a pore sizeless than 0.45 pm; concentrating said aqueous formulation by applying a vacuum and boiling off water until said specified concentration is reached.

Abstract: The invention provides a tobramycin formulation for delivery by aerosolization in the form of additive-free, isotonic solution whose pH has been optimised to ensure adequate shelf-life at room temperature. Said formulation can be advantageously used for the treatment and prophylaxis of acute and chronic endobronchial infections, in particular those caused by the bacterium Pseudomonas aeruginosa associated to lung diseases such as cystic fibrosis.

Abstract: A method of preparing a sugar chain sample, for reducing unreacted labeling reagent in a sample solution containing a labeled sugar chain, includes (process 1) a process of bringing the sample solution containing the labeled sugar chain into contact with monolithic silica, so as to allow the monolithic silica to adsorb a sugar chain component; (process 2) a process of washing the monolithic silica with a washing liquid; and (process 3) a process of bringing the monolithic silica into contact with an eluant, so as to elute the adsorbed sugar chain.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: The present invention relates to a method of labeling a sugar chain, used for labeling a sugar chain contained in a biological sample, aimed at simplifying a process of isolating a sugar chain from a biological sample and labeling it, which includes (a) trapping a sugar chain in a sugar-trapping substance, which is a substance for specifically trapping a sugar chain from a biological sample; (b) washing the sugar-trapping substance having the sugar chains trapped thereon; (c) releasing the sugar chain from the sugar-trapping substance; and (d) labeling the released sugar chain, wherein the processes (a), (b), (c) and (d) are conducted sequentially in a single reaction vessel.

Abstract: A process for producing a polysaccharide sponge comprises the steps of (A) freezing a photoreactive polysaccharide solution, and (B) irradiating the frozen photoreactive polysaccharide solution with light to crosslink the photoreactive polysaccharide, thereby obtaining the polysaccharide sponge. The process includes simplified steps requiring no removal of solvent, and has such an advantage that impurities are easily removed therefrom.

Abstract: It is an object of the present invention to provide an extraction method for a sialic acid-containing compound from a natural raw material, which has no risk of contamination with pathogens affecting animals, can achieve mass production, and does not require the use of an organic solvent harmful to the environment and human body. Provided is an extraction method for a water-soluble sialic acid-containing compound, the method comprising: crudely extracting a water-soluble component with water, polyol, or water containing either an acid or an alkali or polyol from a plant body or a processed product of the plant body, in particular, seeds of cereal or seeds of bean; and separating and recovering the water-soluble sialic acid-containing compound from the resultant crude extract solution with a column packed with a serotonin affinity support.

Abstract: “Locked-ring” C-glycoside derivatives may be prepared wherein the ring of the sugar molecule remains intact without the need for any protecting groups. These C-glycoside derivatives may be produced by first reacting an aldose reducing sugar, which may be a hexose or a pentose, with a ?-diketone to form a C-glycoside ketone. The C-glycoside ketone is then reacted with a ketone reactive compound, such as a hydrazine or hydroxylamine, optionally linked to a detectable label, to form a C-glycoside derivative wherein the ketone reactive compound is conjugated to the C-glycoside at the site of the ketone. The aldose reducing sugar used in the first reaction may a simple pentose or hexose monosaccharide, or it may be optionally substituted.

Abstract: The invention provides isolated peptide-methionine sulfoxide reductase nucleic acids and their encoded proteins. The present invention provides methods and compositions relating to altering peptide-methionine sulfoxide reductase levels in plants. The invention further provides recombinant expression cassettes, host cells, transgenic plants, and antibody compositions.

Abstract: Novel ester derivatives of ascorbic acid and 2-keto-acid saccharides are provided wherein the ester is introduced by ester bond formation between at least one hydroxy-functionality on the ascorbic acid or 2-keto-acid saccharide and a carboxy-functional organosiloxane, or between a 2-keto-gulonic acid and a hydroxy-functional organosiloxane, as well as methods for their synthesis. Treatment, cosmetic, and personal care formulations comprising the novel esters are also provided, including controlled release forms thereof.

Abstract: A process is described for the continuous preparation and/or workup of polysaccharide derivatives by reaction and/or conditioning in a suspension with liquid reaction partners, in which, in accordance with FIG. 1, a) a preferably pumpable suspension stream of solids SE and liquid phase LE, if appropriate preheated to 185° C.

Abstract: Various methods for altering surface characteristics of a microsphere are provided. One method includes coupling an enolic acid to the microsphere to modify the surface characteristics of the microsphere. The surface characteristics may include charge density and/or pKa. A reagent can be coupled to the microsphere via the enolic acid. The reagent may include a biomolecule. The modified surface characteristics may increase a stability of the reagent when the reagent is coupled to the microsphere. The modified surface characteristics may also improve performance of an assay carried out with the microsphere. Another embodiment relates to a microsphere that includes an enolic acid coupled to a polymer core of the microsphere such that the enolic acid modifies surface characteristics of the microsphere. A reagent can be coupled to the microsphere via the enolic acid.

Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

Abstract: A new method is described for the oversulfation of epiK-N sulfate to obtain an epiK5-amine-O-oversulfate with very high sulfation degree which, by subsequent N-sulfation, provides new epiK5-N,O-oversulfate-derivatives with a sulfation degree of at least 4, basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are new low molecular weight epiK5-N-sulfates useful as intermediates in the preparation of the corresponding LMW-epiK5-N,O-oversulfate-derivatives.

Abstract: The present invention relates to esters of hyaluronic acid with rhein, more particularly to a compound based on hyaluronic acid, wherein alcohol groups of hyaluronic acid are esterified with rhein, to a process for preparing said ester and to a pharmaceutical composition comprising said ester.

Abstract: Glucosamine suitable for human or animal consumption is disclosed. The glucosamine is derived from fungal biomass containing chitin. Various methods of producing glucosamine by acid hydrolysis of fermented fungal biomass are also disclosed.

Abstract: The invention relates to a long-acting formulation of biopharmaceutical, more specifically an aptamer therapeutics. A branched PEGylated aptamer or a hyaluronic acid (HA) derivative of which degradation in vivo is regulated is linked by the bioconjugation with biopharmaceutical to produce the long-action formulation.

Abstract: Novel depolymerized-LMWepiK5-N,O-sulfates obtainable starting from a LMW-epiK5-N-sulfate prepared by nitrous depolymerization of an epiK5-N-sulfate or by C5-epimerization of a LMW-K5-N-sulfate obtained by nitrous depolymerization of a K5-N-sulfate. A process consists of submitting the starting depolymerized-LMW-epiK5-N-sulfate to four steps: a O-oversulfation, a partila O-desulfation, a 6-O-sulfation and a N-sulfation. The new depolymerized-LMWepiK5-N,O-sulfates present a di- or trisulfated 2,5-anhydromannitol unit at the reducing end of the majority of its chains, have a content of iduronic acid of 40-60%, a sulfation degree of from 2.3 to 2.9 and a mean molecular weight of from about 1,500 to about 12,000. They exhibit a good antithrombotic activity with a low pro-hemorrhagic risk.

Abstract: Partially desulfated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives exhibit antiangiogenic activity and are devoid of anticoagulant activity.

Abstract: A process is provided for the preparation of a key intermediate in the preparation of 2?-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-1,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-1,5-lactone and optionally into a 2-deoxy-2-halo-2-C-disubstituted ribono-1,4-lactone.

Abstract: Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.

Abstract: The invention provides methods of using beta glucans to treat conditions associated with bone loss or low bone density as well as methods for promoting bone growth in situations where enhanced bone growth is desirable. In the invention methods beta glucans are administered so as to enhance the development of osteoblasts and the inhibition of the development and recruitment of osteoclasts. The inhibition of the recruitment and development of osteoclasts, coupled with the enhancement of osteoblast maturation by beta glucans leads to decreased bone resorption and increased bone formation, making beta glucans ideal agents for the treatment of osteoporosis and other bone resorption diseases.

Abstract: A salt of a glucosamine base having a purity of at least about 99 wt. % and a maximum halide content of about 0.01 wt. %, and an organic acid. The organic acid that is saltified with the glucosamine base is preferably a hydroxyacid or a ketoacid. Preferably, the salt is stabilized by coating the salt with at least one pharmaceutically acceptable polymer comprising a water-soluble, water-immiscible and/or water-swellable homopolymer and/or copolymer. Suitable polymers include carboxypolymethylene homopolymers and copolymers; polyethylene glycol homopolymers and copolymers; polypropylene glycol homopolymers and copolymers; ethylcellulose; povidone homopolymers and copolymers; polyacrylic acid homopolymers and copolymers; polyacrylamide homopolymers and copolymers; polysaccharides; and mixtures of two or more of the foregoing polymers. The resultant coated salt composition will be stable at ambient temperatures and upon exposure to the atmosphere.

Abstract: A novel compound, 2?/3?-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2? and 3? regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2?-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2?/3?-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2?/3?-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2?/3?-O-acetyl-ADP-ribose are also provided.

Abstract: A method of storing and dispensing a fluid includes providing a vessel configured for selective dispensing of the fluid therefrom. A polymerized polymeric material is provided within the vessel. The fluid is contacted with the polymerized polymeric material for take-up of the fluid by the polymerized polymeric material. The fluid is released from the polymerized polymeric material and dispensed from the vessel.

Abstract: Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.

Abstract: The invention includes a method of treating a solid acid catalyst. After exposing the catalyst to a mixture containing a sugar alcohol, the catalyst is washed with an organic solvent and is then exposed to a second reaction mixture. The invention includes a process for production of anhydrosugar alcohol. A solid acid catalyst is provided to convert sugar alcohol in a first sample to an anhydrosugar alcohol. The catalyst is then washed with an organic solvent and is subsequently utilized to expose a second sample. The invention includes a method for selective production of an anhydrosugar. A solid acid catalyst is provided within a reactor and anhydrosugar alcohol is formed by flowing a starting sugar alcohol into the reactor. The acid catalyst is then exposed to an organic solvent which allows a greater amount of additional anhydrosugar to be produced than would occur without exposing the acid catalyst to the organic solvent.

Abstract: The invention provides for the use of sulfur nucleophiles in analyzing methylated DNA and novel sulfur nucleophiles suitable for such us.

Abstract: A method for preparing amino linker oligonucleotides is provided, wherein an amino protecting group is efficiently removed from the amino linker oligonucleotides protected by the protecting group, and thereby achieving a high yield of the amino linker oligonucleotides.

Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.

Abstract: The invention provides a tobramycin formulation for delivery by aerosolization in the form of additive-free, isotonic solution whose pH has been optimised to ensure adequate shelf-life at room temperature. Said formulation can be advantageously used for the treatment and prophylaxis of acute and chronic endobronchial infections, in particular those caused by the bacterium Pseudomonas aeruginosa associated to lung diseases such as cystic fibrosis.

Abstract: The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.

Abstract: The present inventors identified RSIS, and succeeded in suppressing the expression of a target gene by linking RSIS between the region from the promoter to mRNA 5? end sequence of a target gene and a terminator sequence including the 3?UTR after the stop codon. Furthermore, the inventors demonstrated that the expression of two different genes could be suppressed at the same time in cells where a promoter was active, by using the promoter and terminator derived from different genes, and a portion of the mRNA of each gene.

Abstract: A stabilized glucosamine base composition comprising a glucosamine base having a purity level of at least 99.0 wt. % and a maximum halide content of about 0.01 wt. % coated with at least one pharmaceutically acceptable polymer comprising a water-soluble, water-immiscible and/or water-swellable homopolymer and/or copolymer. The resultant coated glucosamine base composition will be stable at ambient temperatures and upon exposure to the atmosphere. Suitable polymers include carboxypolymethylene homopolymers and copolymers; polyethylene glycol homopolymers and copolymers; polypropylene glycol homopolymers and copolymers; ethylcellulose; povidone homopolymers and copolymers; polyacrylic acid homopolymers and copolymers; polyacrylamide homopolymers and copolymers; polysaccharides; and mixtures of two or more of the foregoing polymers.

Abstract: The present invention relates to percarboxylated polysaccharide selected from the group consisting of gellan, carboxymethylcellulose, pectic acid, pectin and hyaluronic acid derivatives; the process for their preparation and their use in the pharmaceutical, biomedical, surgical and healthcare fields.

Abstract: A linker polynucleotide for attaching a nanomaterial to a polynucleotidic platform and related nanoassemblies, arrangements, structures, methods and systems.

Abstract: A method for extracting a nucleic acid, which comprises: (a) preparing a biomaterial containing a solution by a following step (i) or (ii): (i) a step in which a biomaterial containing a phosphate buffer solution or a Bis-Tris (N,N-bis(2-hydroxyethyl)iminotris(hydroxymethyl)methane) buffer solution is prepared; or (ii) a step in which a buffer solution contained in a biomaterial is replaced with a Bis-Tris buffer solution; (b) dissolving the biomaterial with a lysis solution, and eluting a nucleic acid contained in the biomaterial; (c) preparing a lysate solution by adding a water-soluble organic solvent to the nucleic acid-eluted solution obtained in the step (b); (d) allowing the nucleic acid contained in the lysate solution to be adsorbed by a solid material; (e) washing impurities remaining in the solid material and the lysis solution; and (f) desorbing the absorbed nucleic acid from the solid material by a recovering solution.

Abstract: The invention provides supramolecular metal complexes as DNA cleaving agents. In the complexes, charge is transferred from one light absorbing metal (e.g. Ru or Os) to an electron accepting metal (e.g. Rh) via a bridging ?-acceptor ligand. A bioactive metal-to-metal charge transfer state capable of cleaving DNA is thus generated. The complexes function when irradiated with low energy visible light with or without molecular oxygen.

Abstract: A compound which can be attached to a solid support and used as a reagent for methods of solid phase synthesis has the following structure: (I) where Ri is selected from hydrogen and C1-C6 alkyl; R2 is selected from hydrogen, hydroxy, and C1-C6 alkoxy, or together R1 and R2 form a single bond; R3, R4, R5 and R6 are the same or different from each other and each represents hydrogen, C1-C6 alkyl, and halogen, or together R3 and R4 with R5 and R6 form an aromatic ring, further wherein the aromatic ring is substituted with one or more X; X is selected from halogen, nitro, amino, and aminocarbonyl; s is 0, 1, 2, or 3, t is 0, 1, 2, or 3, wherein s+t?1; R7 and R8 are the same or different from each other and each represents hydroxy, halogen, hydrogen, C1-C6 alkoxy, oxyacyl, or together R7 and R8 form a carbonyl; Y is selected from a methylene or substituted methylene, nucleoside, nucleotide, protected nucleoside, protected nucleotide, C1-C6 aryl, arylalkyl, heteroalkyl, heterocycle, and heteroaryl; n is 1, 2, 3, 4,

Abstract: The invention includes methods of producing dianhydrosugars. A polyol is reacted in the presence of a first catalyst to form a monocyclic sugar. The monocyclic sugar is transferred to a second reactor where it is converted to a dianhydrosugar alcohol in the presence of a second catalyst. The invention includes a process of forming isosorbide. An initial reaction is conducted at a first temperature in the presence of a solid acid catalyst. The initial reaction involves reacting sorbitol to produce 1,4-sorbitan, 3,6-sorbitan, 2,5-mannitan and 2,5-iditan. Utilizing a second temperature, the 1,4-sorbitan and 3,6-sorbitan are converted to isosorbide. The invention includes a method of purifying isosorbide from a mixture containing isosorbide and at least one additional component. A first distillation removes a first portion of the isosorbide from the mixture. A second distillation is then conducted at a higher temperature to remove a second portion of isosorbide from the mixture.

Abstract: Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to an active agent.

Abstract: This invention relates to a process for preparing bioabsorbable oxidized cellulose comprising combining cellulose material, with nitrogen dioxide and a nonaqueous solvent chosen from the class of perfluorinated tertiary amines. This invention also relates to a method of oxidizing cellulose material comprising introducing a solvent into the vessel, circulating the solvent through the cellulose material, adding nitrogen dioxide to said vessel containing the solvent and cellulose in the required amounts, circulating the solution for 7 to 24 hours while controlling the reaction temperature, and isolating the oxidized material. Preferably, isolation of the oxidized product is followed by first washing the oxidized cellulose material with cold water, then washing the oxidized cellulose material with an aqueous alcohol solution several times, then washing the material with 100% alcohol several times, and finally drying the oxidized material.

Abstract: The present invention relates to method for the preparation of glycosaminoglycan compositions, isolated glycosaminoglycan compositions obtainable therefrom, glycosaminoglycan compositions, kits and use thereof. More specifically, the present invention provides a method for isolating glycosaminoglycan compositions of the invention from human follicular fluid. The compositions, related methods and uses according to the present invention are useful in the treatment and/or prevention of thrombotic diseases, cell proliferation disorders, proteolysis and inflammation mediated cell invasion and infertility.

Abstract: The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing.

Abstract: The invention provides hydrolases, polynucleotides encoding them, and methods of making and using these polynucleotides and polypeptides. In one aspect, the invention is directed to polypeptides, e.g., enzymes, having a hydrolase activity, e.g., an esterase, acylase, lipase, phospholipase (e.g., phospholipase A, B, C and D activity, patatin activity, lipid acyl hydrolase (LAH) activity) or protease activity, including thermostable and thermotolerant hydrolase activity, and polynucleotides encoding these enzymes, and making and using these polynucleotides and polypeptides. The hydrolase activities of the polypeptides and peptides of the invention include esterase activity, lipase activity (hydrolysis of lipids), acidolysis reactions (to replace an esterified fatty acid with a free fatty acid), transesterification reactions (exchange of fatty acids between triglycerides), ester synthesis, ester interchange reactions, phospholipase activity and protease activity (hydrolysis of peptide bonds).