Abstract: The present invention relates to pharmaceuticals, foods and drinks, food additives, animal feeds and feed additives comprising an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof as active ingredients, use of an Nacylated hydroxyproline derivative or a salt thereof for the production of an arthritis preventing or treating agent, and a method for preventing or treating arthritis which comprises administering an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof.

Abstract: The present invention describes a new class of cross-linked derivatives of partially N-deacetylated hyaluronic acid or derivatives thereof, comprising at least one repeating unit of formula (I) hereinafter depicted and a process for the preparation of said cross-linked derivatives, comprising a multicomponent condensation reaction involving the carboxy groups and the amino groups originating from a partial N-deacetylation of hyaluronic acid or derivatives, together with an aldeyde and an isocyanide. The derivatives thus obtained can be used, alone or in association with biologically and/or pharmacologically active substances, for the preparation of pharmaceutical compositions, biomaterials, surgical and healthcare articles, slow release systems and for the coating of biomedical objects.

Abstract: This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: The invention describes new hyaluronan derivatives where the hydroxyl groups are esterified or carbamoylated in amounts ranging from 0.01% to 100% and the carboxyl groups are either totally or partially esterified with alcohols or are in the form of salt.

Abstract: Compounds and methods which are useful for the site-specific delivery and localization of drugs are provided. The compounds can be represented by the formula: A-L-D wherein A is an anchoring moiety; L is a linking group; and D is a drug.

Abstract: Disclosed are methods of conjugating biologically active substances, particularly, alpha-interferon, with a hyaluronan or a mixture of a hyaluronan with at least one other hydrophilic polymer having a functional group capable of reacting with divinyl sulfone. Also disclosed are stable intermediates formed by partially reacting a hyaluronan with divinyl sulfone and stopping the reaction before completion to leave free, or reactive vinyl groups on the hyaluronan molecule available for conjugation with the biologically active substance.

Abstract: The purification of the E.coli K5 polysaccharide by treatment with isopropyl alcohol and elimination of lipophilic substances is described. The purified product can be used to prepare, after N-deacetylation, new N,O-sulfated polysaccharides with high degree of sulfation.

Abstract: The present invention relates to microspheres comprising hyaluronan derivatized with a bifunctional crosslinker to form microspheres. Methods of making such microspheres, comprising mixing hyaluronic acid and a dihydrazide with a crosslinker in an aqueous solution, adding a solvent and an emulsifying agent to form an emulsion, and lowering the pH of the emulsion to allow intramolecular and intermolecular crosslinking to occur, are also disclosed. The invention also provides for pharmaceutical or cosmetic formulations based on the microspheres described herein, further containing one or more active or cosmetic agents, and methods of using such formulations.

Abstract: The present invention relates to polysaccharide conjugates that comprise: a polysaccharide that binds to surface-receptors present on Antigen Presenting Cells, conjugated to one or more compounds having stable carbonyl groups covalently attached, either directly or via a bifunctional linker. The conjugates are useful as immuno-stimulants and adjuvants.

Abstract: The instant invention provides a method of treating or preventing osteoarthritis, joint effusion, joint inflammation and pain, synovitis, lameness, post operative arthroscopic surgery, deterioration of proper joint function including joint mobility, the reduction or inhibition of metabolic activity of chondrocytes, the activity of enzymes that degrade cartilage, the reduction or inhibition of the production of Hyaluronic acid, said method comprising orally administering to a mammalian species a therapeutically effective amount of Hyaluronic Acid or pharmaceutically acceptable salts thereof. Additionally, compositions containing hyaluronic acid; chondroitin sulfate, and glucosamine sulfate in a paste formulation are also disclosed which can be administered on their own or can be used as a feed additive.

Abstract: An immunosuppressive agent comprising, as an effective ingredient, at least one compound selected from the group consisting of compounds represented by general formula (1) below and pharmaceutically acceptable salts thereof: wherein R101 represents an acyl residue of a higher fatty acid, and R102 represents a hydrogen atom or acyl residue of a higher fatty acid.

Abstract: The present invention relates to a process for separating nucleic acid molecules, preferably open circular and supercoiled plasmid DNA and RNA molecules from each other, comprising the steps of providing a solution comprising the molecules; adsorbing the molecules to adsorbing groups on a carrier; and optionally washing the column with a suitable solution. The present process is especially suitable for large-scale isolation of supercoiled ccc DNA to be used in gene therapy.

Abstract: The present invention relates to novel synthetic polysaccharides with antithrombotic activity exhibiting at least one covalent bond with biotin or a biotin derivative and to a process employing avidin or streptavidin which makes it possible to neutralize these polysaccharides.

Abstract: This invention provides prokaryotic glycosyltransferases, including a bifunctional sialyltransferase that has both an &agr;2,3- and an &agr;2,8-activity. A &bgr;1,4-GalNAc transferase and a &bgr;1,3-galactosyltransferase are also provided by the invention, as are other glycosyltransferases and enzymes involved in synthesis of lipooligosaccharide (LOS). The glycosyltransferases can be obtained from, for example, Campylobacter species, including C. jejuni. In additional embodiments, the invention provides nucleic acids that encode the glycosyltransferases, as well as expression vectors and host cells for expressing the glycosyltransferases.

Abstract: This invention involves a type of oligosaccharides and its sulfate derivatives. The backbone of the oligosaccharides consists of 3 to 14 sugar residues, while the side chains contain 0 to 4 sugar residues. There is at least one 1→3&agr; linkage in the backbone. This invention also involves the dendrimers composed of 2 to 3 oligosaccharides that are combined by polyhydroxyl compounds. These oligosaccharides, their sulfates and dendrimers have immune enhancing, antitumor, and antiviral activities. They can be used in immune enhancing, antitumor, and antiviral medicine compounds that would be used as therapeutic treatments.

Abstract: The present invention relates to a new technique formed from polysaccharides of kelp (PK), which has function of anticancer and increasing immunity, and new nanoparticles (NP) and special liposome (SSL), which contained natural anticancer drug their preparation. Also, the present invention is aimed at the overall improvement of therapeutic efficacy of anticancer drugs, including Homoharringtonine (HHT), Curcumol (CUR), Eelemene (ELE) and Camptothecin (CPT) by NP and SSL. NP improves the anticancer therapeutic efficacy of HHT, CUR, ELE and CPT by using PK as polymer. PK can improve the anticancer therapeutic index and decrease side effect of free anticancer drugs. Also, PK has the function of increasing immunity.

Abstract: A method of isolating chondroitin sulfate product from a feedstock comprising connective tissue.

Abstract: A smaller molecule obtainable by allowing a sulfated fucan-digesting enzyme which digests a novel sulfated polysaccharide derived from an alga belonging to Laminariales to act on a sulfated fucan, and a method for producing the same.

Abstract: Glycosaminoglycans derived from the K5 polysaccharide having high anticoagulant and antithrombotic activity obtained by a process comprising the preparation of the K5 polysaccharide from Escherichia coli, N-deacetilation/N-sulfation, C-5 epimerization, supersulfation, selective O-desulfation, selective 6-O sulfation and N-sulfation, wherein said epimerization is carried out using the glucuronosyl C-5 epimerase enzyme in solution or in immobilized form in presence of specific divalent cations.

Abstract: A stabilized aqueous preparation including a shark-derived chondroitin iron sulfate colloid and a trace element. An aqueous preparation of the present invention is pharmaceutically stable, is stable in an infusion such as a high-calorie intravenous nutrition infusion, and can be safely applied in clinical use without worry of bovine spongiform encephalopathy (BSE) infection.

Abstract: Novel sulforhamnosylacylglycerol derivatives represented by General Formula (1): where R101 represents an acyl residue of a higher fatty acid and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid. The derivatives represented by General formula (1) are useful as, a DNA polymerase inhibitor and an anticancer agent.

Abstract: Sulfofucosylacylglycerol derivatives represented by General Formula (1): where R101 represents an acyl residue of a higher fatty acid and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid. The derivatives represented by General formula (1) are useful as a DNA polymerase inhibitor and an anticancer agent.

Abstract: Disclosed are methods of conjugating biologically active substances, particularly, alpha-interferon, with a hyaluronan or a mixture of a hyaluronan with at least one other hydrophilic polymer having a functional group capable of reacting with divinyl sulfone. Also disclosed are stable intermediates formed by partially reacting a hyaluronan with divinyl sulfone and stopping the reaction before completion to leave free, or reactive vinyl groups on the hyaluronan molecule available for conjugation with the biologically active substance.

Abstract: The purification of the E.coli K5 polysaccharide by treatment with isopropyl alcohol and elimination of lipophilic substances is described. The purified product can be used to prepare, after N-deacetylation, new N,O-sulfated polysaccharides with high degree of sulfation.

Abstract: The methods of the present invention prepare carrageenan products from processed seaweed material having a solids content of less than 25% by weight solids, using shear stress treatment. The carrageenan products comprise at least about 60% by weight of carrageenan and at least about 2% by weight of acid insoluble material. The carrageenan products of the present invention are useful as components in food products, such as, dairy products, meats, and dessert gels as well as non-food products, such as, toothpaste formulations, cosmetics, paints, films and delivery capsules.

Abstract: The present invention provides materials and methods for the production of bifunctional enzymes that catalyze the N-deacetylation and N-sulfation of saccharides. The invention also provides conditions and methods for assaying the activity of such enzymes.

Abstract: The present invention refers to the preparation of O-sulphated, N-sulphatated or N-acetylated derivatives, both epimerised or non epimerised, of K5, K4, and optionally defructosilated K4 and K40 polysaccharides and to their use as antiinflammatory agents in chronic and acute inflammations.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1-R13 are as defined herein.

Abstract: A method for purifying high molecular weight hyaluronic acid, comprising the steps of providing one or more raw hyaluronic acid sources; extracting hyaluronic acid from the source; precipitating hyaluronic acid extracts; dissolving extract precipitates in water; extracting enzyme inhibitors from the dissolved precipitates with chloroform, and centrifuging to isolate an aqueous portion; adding one or more protein hydrolyzing enzymes to the aqueous portion in a reactor; adding a solution of CPC and NaCl to the reactor; filtering reactor contents through at least one membrane filter; filtering membrane filtered solution through at least one diafilter having a molecular weight cutoff of about 30 kDa; precipitating the diafiltered solution and isolating purified hyaluronic acid precipitate; and formulating isolated precipitate to about 10 mg/ml hyaluronic acid.

Abstract: A method of making a derivatized aminoglycoside includes reacting an aminoglycoside with at least 2 equivalents of a divalent metal ion in an aprotic solvent to complex two neighboring amino group and hydroxyl group pairs; reacting the non-complexed amino groups with a protecting reagent to provide protecting groups; removing the divalent metal ion to provide two unprotected amino groups; reacting one of the unprotected amino groups with a reactive substance containing an linker, a carrier, or a label; and removing the protecting groups. This method can be used to produce novel compounds and reagents.

Abstract: Three enzymes degrading sulfated glucuronofucan; processes for producing these enzymes; activators for these enzymes; glucuronofucan sulfate and degradation products thereof; and a novel microorganism.

Abstract: The invention relates to novel disaccharides of formula (I), wherein R1 is selected from the group consisting of hydrogen, linear or branched (C1-C4) alkyl, phenylalkyl with less than ten carbon atoms and —COCH3; R2 is selected from the group consisting of hydrogen, —COCH3 and SO3M; R3 is selected from the group consisting of hydrogen, linear or branched (C1-C4) alkyl, phenylalkyl with less than ten carbon atoms, —COCH3 and y —COPh, Ph being phenyl; G is selected from amongst —COOR4 and —COOM, R4 is selected from the group consisting of hydrogen, (C1-C2)-alkyl and arylalkyl with less than sixteen carbon atom; A is selected from the group consisting of hydrogen, —SO3H, —SO3M and —COCH3; B is selected from the group consisting of hydrogen, —SO3H, —SO3M and —COCH3, wherein either A or B are necessarily either —SO3H or —SO3M, M being a an organic or metallic cation.

Abstract: A smaller molecule obtainable by allowing a sulfated fucan-digesting enzyme which digests a novel sulfated polysaccharide derived from an alga belonging to Laminariales to act on a sulfated fucan, and a method for producing the same.

Abstract: The present invention relates to chemical complexes consisting of cysteine or derivatives of cysteine and an aminosugar as well as pharmaceutical compositions and dietary supplements comprising such complexes. The invention further relates to the use of such compositions or complexes for the preparation of a medicament or a dietary supplement in the suppression of hypersensitivity and inflammatory reactions such as rheumatic or dermatological disorders or to a method of treating such diseases by administering such compositions and complexes.

Abstract: A novel chondroitin sulfate which can be produced more economically in a large amount and is expected as being useful for various purposes and processes for producing the same. Namely, a novel chondroitin sulfate which has an intermediate structure between the conventionally known whale-origin chondroitin sulfate and shark-origin chondroitin sulfate and is expected as useful for various purposes in the fields of drugs, cosmetics, food additives, etc. A process for producing the above-described chondroitin sulfate comprises grinding salmon nasal cartilage at a low temperature, defatting the ground matter, then treating it with an alkali and pronase, centrifuging the thus obtained liquid digested matter and then precipitating it from ethanol; and another process wherein the precipitate thus obtained is further treated with a cation exchange resin.

Abstract: The Methods of the present invention prepare carrageenan products from processed seaweed material using shear stress treatment are disclosed. The carrageenan products comprise at least about 65% by weight of carrageenan and at least about 2% by weight of acid insoluble material. The carrageenan products of the present invention preferably have an onset of hydration below about 40*C. and a color of greater than about 74 *L units. The carrageenan products of the present invention are useful as components in food products, such as, dairy products, meats, and dessert gels as well as non-food products, such as, toothpaste formulations, cosmetics, and paints.

Abstract: The present invention relates to pharmaceutical compositions containing as an active ingredient at least one oligosaccharide of formula: to novel oligosaccharides of formula (I), to mixtures thereof and to methods for their preparation.

Abstract: The bioactivity of TNF is inhibited by administering heparin or a derivative thereof along with a soluble TNF receptor. The heparin or derivative thereof can be administered simultaneously with the soluble TNF receptor, either in separate compositions or in compositions containing both heparin or a derivative thereof and at least one soluble TNF receptor. The heparin or derivative may also be administered without the soluble TNF receptor and still effect some amount of inhibition of TNF bioactivity.

Abstract: The present invention provides novel disulfone compounds and methods of preparing and using those compounds to further prepare biologically relevant gem-disulfone analogs of natural enzyme substrates. Methods of using a variety of disulfone compounds as reagents capable of forming symmetrical and non-symmetrical &agr;, &bgr; unsaturated gem-disulfones are also provided. There is also provided a disulfone reagent which reacts with both aromatic and aliphatic aldehydes in good to moderate yield to give exclusively the trans isomer. In accordance with further aspects of the present invention, a methodology for stereospecifically preparing potential gem-disulfone enzyme inhibitors is provided. A synthetic design which allows easy substitution of functional groups so that a number of substrate analogs can be synthesized readily is also provided.

Abstract: A chondroitin polymerase having such properties that it transfers GlcUA and GalNAc alternately to a non-reduced terminal of a sugar chain from a GlcUA donor and a GalNAc donor, respectively, and the like; and a process for producing the chondroitin polymerase.

Abstract: The present invention relates to a chondroitin synthase gene and methods of making and using same. In more particular, but not by way of limitation, the present invention relates to a chondroitin synthase gene from Pasteurella multocida and methods of isolating and using same. Additionally, the present invention relates to the use of unsulfated chondroitin and its preparation, as well as conversion into modified versions such as dermatan sulfate and chondroitin sulfate polymers.

Abstract: The invention provides reagents and methods for conjugating polymers specifically to the &agr;-amine of polypeptides in high yield. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a thioester moiety capable of specifically conjugating to the &agr;-amine of a polypeptide having a cysteine or histidine at the N-terminus. The invention provides active thioester derivatives of PEG that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG and polypeptide. Use of these active esters to prepare PEG-proteins and PEG-peptides is described.

Abstract: New process for the preparation of chondroitin sulfates from the bacterial origin polysaccharide named K4, by defructosilation followed by selective sulfation.

Abstract: The present invention provides a novel compound multiple fluorescent natural dye from a marine organism Holothuria Scabra having a chemical structure of of Si—O—R type wherein silica matrix is an integral part of the compound, taking part in the metabolism of the animal, wherein R being an organic moiety and also provides a composition containing the compound having various applications; also a process of extraction, purification and characterization of the novel multiple fluorescent natural dye compound from a marine organism (Holothuria scabra).

Abstract: Aminoalkyl glucosaminide phosphate (AGP) compounds that are adjuvants and immunoeffectors are described and claimed. The compounds have a 2-deoxy-2-amino glucose in glycosidic linkage with an aminoalkyl (aglycon) group. Compounds are phosphorylated at the 4 or 6 carbon on the glucosaminide ring and comprise three 3- alkanoyloxyalkanoyl residues. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Abstract: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.

Abstract: A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, suitable for use in the treatment of a cyclooxygenase-2 mediated disease is provided.

Abstract: The invention concerns a novel method for preparing by chemical process functionalised &bgr;-(1,3)-glucan derivatives, enabling to obtain free oligosaccharides or comprising specific groups such as, for instance, sulphate, phosphate, methyl, in predetermined positions. Said method consists in reacting a glycosyl donor of formula (Ia) or (Ib) with a glycosyl scavenger of formula (II), as defined in the claims. The invention is useful for preparing biologically active principles for use in the agricultural, cosmetic or pharmaceutical field.

Abstract: Disclosed is a method for preparing a malto-oligosaccharide derived glycoside. Generally, the method comprises providing a malto-oligosaccharide and glycosylating the malto-oligosaccharide with an alcohol or a thiol under conditions suitable to form a malto-oligosaccharide derived glycoside. Also disclosed is a method for preparing a mixture of malto-oligosaccharide derived glycosides by providing a mixture of malto-oligosaccharides and glycosylating the malto-oligosaccharides with an alcohol or a thiol under substantially anhydrous conditions to form a mixture of malto-oligosaccharide derived glycosides.

Abstract: Modified polysaccharides (such as starches, gums, chitosans, celluloses, alginates, sugars, etc.), which are commonly used in the paper industry as strengthening agents, surface sizes, coating binders, emulsifiers and adhesives, can be combined into a single molecule with amphiphilic hydrocarbons (e.g. surface active agents) which are commonly utilized in the paper industry to control absorbency, improve softness, enhance surface feel and function as dispersants. The resulting molecule is a modified polysaccharide having surface active moieties which can provide several potential benefits, depending on the specific combination employed, including: (a) strength aids that do not impart stiffness; (b) softeners that do not reduce strength; (c) wet strength with improved wet/dry strength ratio; (d) debonders with reduced Tinting and sloughing; (e) strength aids with controlled absorbency; and (f) surface sizing agents with improved tactile properties.