Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.

Abstract: Compositions comprising glucopyranosyl lipid adjuvant (GLA) and methods for reducing or preventing the formation of cancer metastasis utilizing same are provided. The compositions may be formulated for local-regional delivery. The compositions may be substantially devoid of a cancer antigen. The treatment with GLA may be combined with treatment with a COX2 inhibitor and a beta-adrenergic blocker.

Abstract: Provided are effective and highly safe agents, medicaments and the like for ameliorating various disorders caused by brain hypofunction. Also provided is a preventing or ameliorating agent for brain hypofunction containing N-acetyl-D-mannosamine, a pharmaceutical composition for preventing, ameliorating or treating disorders due to brain hypofunction, containing an effective amount of N-acetyl-D-mannosamine and a pharmaceutically acceptable carrier, and a food comprising N-acetyl-D-mannosamine added thereto.

Abstract: Hyaluronic acid particles and their use in biomedical applications are provided. In one embodiment, an HA particle comprising a plurality of free polymer chains extending from a surface of the particle such that the polymer chains are capable of association with polymers or with polymer chains on a surface of other particles is provided.

Abstract: The present invention is related to a compound conjugating a drug with a glycosaminoglycan, such as hyaluronic acid (HA), where the drug is useful for the treatment of diseases such as inflammation, auto-immune disease, allergy, infection and preferably cancer. The conjugated compound of the present invention can increase the concentration of drug at the specific site of disease by an interaction of the glycosaminoglycan used as target drug delivery carrier and the CD44 cell surface receptor, then enhancing the therapeutic efficacy and reducing the systemic side effect of the site-delivered drug.

Abstract: An injectable monophase hydrogel is provided and is made of a reaction mixture of a high molecular weight hyaluronic acid and a low molecular weight hyaluronic acid.

Abstract: The present invention provides a modified polyuronic acid represented by formula (1) or a salt thereof which is excellent in surface activity: wherein R1 is a hydrogen atom, a hydrocarbon group having 1 to 40 carbon atoms or the like; X is an oxygen atom, a sulfur atom or a —NH— group, with the proviso that a ratio value of [m/(m+n)] is from 0.3 to 1.0, and a plurality of the R1 groups being present in a molecule of the modified polyuronic acid or the salt thereof may be the same or different from each other but all of the R1 groups are not hydrogen atoms at the same time.

Abstract: A compound having a structure expressed by the following General Formula (1) or a salt thereof where “R” denotes a hydrogen atom or an alkyl group.

Abstract: The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.

Abstract: Disclosed are CEST paramagnetic agents comprising a substrate (SH) containing mobile protons bonded to a paramagnetic chelate (SR) containing a metal selected from iron (11) (high-spin configuration), iron (111), cobalt (11), rhodium (11), copper (11), nickel (11), cerium (111), praseodymium (111), neodymium (111), dysprosium (111), erbium (111), terbium (111), holmium (111), thulium (III), ytterbium (III) and europium (111).

Abstract: The present invention relates to a conjugate of acetylated biocompatible polysaccharide and phthalocyanine-based compound for photodynamic diagnosis or therapy in which biocompatible polysaccharide is acetylated and a phthalocyanine-based compound is bound to the acetylated polysaccharide. The conjugate for photodynamic diagnosis or therapy according to the present invention is characterized in that the polysaccharide is acetylated to improve solubility in a solvent and thus enable various chemical modifications, and the conjugate may specifically target tumor cells, has superior cancer cell selecting and accumulating capacity, and has excellent effects of killing cancer cells when near infrared ray is irradiated. The conjugate of the present invention may not show cytotoxicity for cells other than cancer cells even when near infrared ray is irradiated, and thus exhibits superior in vivo stability, and therefore, may be valuably used in disease diagnosis or therapy using photodynamics.

Abstract: Biologically compatible polymers carry an imide and can be used as an adhesive, a hydrogel or both. A second biologically compatible polymer reactive with the imidated polymer can be used therewith to seal openings.

Abstract: The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.

Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.

Abstract: Disclosed are chemically modified hyaluronic acid (HA) derivatives containing hydrazido groups directly linked to the glucuronic acid residues of HA. Said hydrazido groups are used to obtain crosslinked and labeled HA derivatives. The invention further relates to methods of preparation of said HA derivatives.

Abstract: This invention provides compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a polymer; and n is a number from 1 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond.

Abstract: It relates to a process for the preparation of partially depolymerized glycosaminoglycan metal salts, wherein the metal is gold or silver, which comprises the steps of: a) depolymerization of a high molecular weight glycosaminoglycan metal salt; wherein the metal is different from gold or silver with a depolymerizing agent selected from the group consisting of potassium permanganate, sodium hydroxide; and hydrogen peroxide; b) bleaching with hydrogen peroxide; and c) metal ion exchange. It also relates to the partially depolymerized glycosaminoglycan gold or silver salts obtainable by said process, to their oral or topical pharmaceutical or cosmetic compositions, to their pharmaceutical uses for the treatment and/or prevention of wounds, scars, burns, microbial infections and inflammatory processes of the skin; and to their cosmetic uses for skin care.

Abstract: An organic material including a hydrophilic polymer and an organic moiety having a hydroxyl substituted C6-C14 aromatic functional group, the organic moiety binding to an end or a side of the hydrophilic polymer.

Abstract: The invention relates to a new hyaluronan derivative according to the general formula (I), the method of preparation thereof, a hydrogel based on the new derivative, method of preparation of the hydrogel and the use of the hydrogel in tissue engineering, cosmetics, medicine or regenerative medicine, especially in the form of scaffolds for the treatment of articular cartilage or bone tissue defects.

Abstract: Provided is a novel hyaluronan synthase (HAS2), isolated nucleic acids encoding it, and expression vectors which express the novel HAS2. Also provided are cell cultures which contain cells which harbor the expression vectors, methods of using the cell cultures to produce high molecular weight hyaluronic acid, and cell culture media that contains the high molecular weight hyaluronic acid.

Abstract: Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.

Abstract: The invention provides a method for producing an orexin neuron by culturing a pluripotent stem cell or a neural progenitor cell in the presence of N-acetyl-D-mannosamine and optionally in the presence of at least one inhibitor selected from the group consisting of a Sirtuin 1 inhibitor and an O-linked ?-N-acetylglucosamine transferase inhibitor. The invention also provides a therapeutic agent for narcolepsy or eating disorders, such as anorexia, containing N-acetyl-D-mannosamine, which is based on the induction of orexin neuron in vivo.

Abstract: Provided a method of producing a purified hyaluronic acid type which comprises adding a water-soluble organic medium to a solution which comprises a hyaluronic acid type having an average molecular weight of 400 to 100,000 and has a pH of 3 or less to obtain a suspension, and adjusting a pH of the suspension in a range of 3.5 to 8 to precipitate a purified hyaluronic acid type.

Abstract: The invention provides methods, compositions and kits relating to hyaluronan based matrices using oxidized glutathione as a crosslinking agent.

Abstract: Disclosed are novel ?-galactosylceramide derivatives, pharmaceutically acceptable salts thereof, preparation methods thereof, and pharmaceutical compositions for use in an immune adjuvant containing the same as an active ingredient. The derivatives, in which the amide moiety of ?-GalCer is bioisosterically replaced with a triazole moiety, direct cytokine secretion toward IL-4 rather than IFN-?and thus can be used as a therapeutic for autoimmune diseases regulated by IL-4, such as type 1 diabetes and multiple sclerosis.

Abstract: In one aspect, the present disclosure provides compounds of formulae (I) and (II). In another aspect, a compound of formula (I) or (II) is formulated into compositions with an antigen, optionally with a vesicle. In some embodiments, compositions are administered intramuscularly.

Abstract: The present invention generally relates to the field of sialic acids, in particular to the field of sialic acid enriched food products and their uses. One embodiment of the present invention relates to a food product enriched with food-grade sialic acid producing bacteria and/or a fraction thereof containing sialic acid.

Abstract: The present disclosure generally relates to protein binding agents, such as protein kinase binding agents of general Formula (I). The protein binding agents may be provided attached to a solid support and may be used, for example, to detect the presence of a broad range of proteins in a sample. Methods of synthesizing the protein binding agents, and kits comprising the protein binding agents, are also disclosed.

Abstract: The present invention discloses a process for the production of chondroitin sulphate with an average molecular weight (Mw) of 10-30 kDa by chemical sulphation starting from an unsulphated chondroitin backbone, obtained in turn by acid hydrolysis of capsular polysaccharide K4 made directly from E. coli strain O5:K4:H4, or directly produced from a genetically modified strain of E. coli. Sulphation of the N-acetyl-D-galactosamine residue at position 4 or 6 takes place simultaneously in the same polysaccharide chain, simulating the sulphation pattern observed in natural chondroitin sulphate, unlike the sulphation obtained with the synthesis methods described to date.

Abstract: The invention provides a family of fluorescent compounds. The compounds are substituted silaxanthenium compounds that can be chemically linked to one or more biomolecules, such as a protein, nucleic acid, and therapeutic small molecule. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications. The dyes are particularly useful for in vitro, in vivo and ex vivo imaging applications.

Abstract: The invention relates to providing isolactosamine (Gal?1-3GlcNH2, formula 1) and salts thereof in the form of either anomer or mixture thereof, as well as hydrates or solvates of the free base and salts thereof. The synthesis of isolactosamine and its use in the synthesis of lacto-N-biose containing oligosaccharides are also disclosed.

Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: The invention relates to the field of recombinant DNA technology for the production of chondroitin, including the production of chondroitin sulfate via a combination of recombinant bacterial fermentation and post-fermentation sulfation.

Abstract: Functionalized chondroitin sulfate, cross-linked polymer matrices comprising functionalized chondroitin sulfate, and methods of making and using the same are provided. Such polymer matrices may be used for tissue engineering, reconstructing cartilage, and the like. Kits are also provided for detection of cartilage degrading enzymes.

Abstract: The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.

Abstract: Uses of depolymerized hyaluronan (e.g., prepared by sonicating high molecular weight hyaluronan such as naturally-occurring hyaluronan) or anti-Hyal-2 antibody in cancer treatment. Also described herein are methods for preparing depolymerized and crosslinked hyaluronan by sonication and the hyaluronan composition thus obtained.

Abstract: The present disclosure relates to hyaluronic acid derivatives, and in particular, derivatives in which the N-acetyl group of hyaluronic acid has been substituted, and methods and uses thereof.

Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Abstract: A hydrogel is provided which is obtained by reacting an azide group and a cyclooctyne group in the absence of a catalyst, especially in the absence of a copper catalyst. The hydrogel has: (a) a first polymer moiety composed of hyaluronic acid, carboxymethyl dextran or the like; (b) a second polymer moiety composed of hyaluronic acid, carboxymethyl dextran or the like, said second polymer moiety being of a kind that is same as or different from the kind of the moiety (a) and is composed of a molecule different from the moiety (a); and (c) a triazole ring group or a derivative group thereof.

Abstract: Provided a method of producing a purified hyaluronic acid type which comprises adding a water-soluble organic medium to a solution which comprises a hyaluronic acid type having an average molecular weight of 400 to 100,000 and has a pH of 3 or less to obtain a suspension, and adjusting a pH of the suspension in a range of 3.5 to 8 to precipitate a purified hyaluronic acid type.

Abstract: A highly stable crystal of (1S)-1,5-anhydro-1-[5-(4-{(1E)-4-[(1-{[2-(dimethylamino)ethyl]amino}-2-methyl-1-oxopropan-2-yl)amino]-3,3-dimethyl-4-oxobut-1-en-1-yl}benzyl)-2-methoxy-4-(propan-2-yl)phenyl]-D-glucitol, and a process for producing the crystal are provided. Specifically, an ethanolate having the following physical properties, and a plurality of other crystal forms transformed from the ethanolate are provided: (a) Having peaks at 2?=5.9 degrees, 17.1 degrees, 17.6 degrees and 21.5 degrees in X-ray powder diffraction (Cu—K?); (b) Showing characteristic absorption bands at 3538 cm?1, 3357 cm?1, 2964 cm?1, 1673 cm?1, 1634 cm?1 and 1505 cm?1 in an infrared absorption spectrum; and (c) Having a melting point in a vicinity of 111° C.

Abstract: Reagents comprising MS active, fluorescent molecules with an activated functionality for reaction with amines useful in tagging biomolecules such as N-glycans and uses thereof are taught and described.

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

Abstract: The present invention provides a one-pot multi-enzyme method for preparing UDP-sugars from simple sugar starting materials. The invention also provides a one-pot multi-enzyme method for preparing oligosaccharides from simple sugar starting materials.

Abstract: Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3?), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3? is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.

Abstract: The invention provides D02S derivatives conjugated to monosaccharide ligands directly or through a linker and optionally chelated to a metal, wherein the D02S derivatives having the following structure: wherein R1?, R2? are each independently —OH or —O-alkyl; R1 is a hydrogen, a linker, or a ligand; R3 is a linker and/or a ligand; and n is an integer from 1 to 10; the linker is an amino acid, a peptide, an amino alcohol, a polyethylylene glycol, an alkyl, an alkenyl, an alkynyl, an azide, an aromatic compound, a carboxylic acid, or an ester, the alkyl, alkenyl, or alkynyl is optionally substituted with an alkyl, a halogen, a nitro group, a hydroxyl group, an amino group, or a carboxyl group; the ligand is a GLUT1 targeting moiety.

Abstract: Hyaluronic acid (HA) conjugates or crosslinked HAs compositions for coating an implantable device are provided. The implantable device can be used for treating a disorder such as atherosclerosis, thrombosis, restenosis, high cholesterol, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, and combinations thereof.

Abstract: This application concerns a method for preparing glucan from Aspergillus niger, characterised in that it comprises (i) the at least partial deacetylation of the mycelium of A. niger; (ii) acid treatment of the (partially) deacetylated mycelium, preferably following purification and/or washing, to obtain insoluble glucan and soluble chitosane, which acid treatment comprises placing the deacetylated mycelium in contact with an acidic solution; (iii) the separation of the soluble chitosan on the one hand, and the insoluble glucan on the other; (iv) alkaline treatment of the glucan comprising placing the glucan in contact with an alkaline solution to cause the glucans to flocculate; and (v) drying the flocculated glucans to obtain glucan powder. This invention further concerns the glucans thus obtained, compositions comprising them, and their uses. The glucans of the invention may be used as immunostimulants.

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: To develop glucosamine (GlcN) pro-drugs with properties superior to the presently available GlcN products, we have synthesized derivatives with improved pharmaceutical properties. The synthesized derivatives include peptide-GlcN ester and amide conjugates where the peptide portion consists of one or more amino acids. One such compound is (5-amino-3,4,6-trihydroxyoxan-2-yl)methyl 2-(2-aminoacetamido)-3-methylbutanoate or glycine-valine-COO-GlcN (GV-GlcN).7.