Abstract: The present invention relates to a purified, easily produced poly-&bgr;-1→4-N-acetylglucosamine (p-GlcNAc) polysaccharide species. The p-GlcNAc of the invention is a polymer of high molecular weight whose constituent monosaccharide sugars are attached in a &bgr;-1→4 conformation, and which is free of proteins, and substantially free of single amino acids, and other organic and inorganic contaminants. In addition, derivatives and reformulations of p-GlcNAc are described. The present invention further relates to methods for the purification of the p-GlcNAc of the invention from microalgae, preferably diatom, starting sources. Still further, the invention relates to methods for the derivatization and reformulation of the p-GlcNAc. Additionally, the present invention relates to the uses of pure p-GlcNAc, its derivatives, and/or its reformulations.

Abstract: 15-Fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: An oligosaccharide derivative, at higher homogeneity than fucose polysaccharide and rhamnose polysaccharide and with greater antiulcer effects, which is represented by the following general formula: Y—OCH(CH2NHR)2 wherein, Y represents an oligofucose or oligorhamnose at a polymerization number of 2 to 20, where the hydroxyl groups may or may not be partially modified in the form of sulfate ester, and R represents phenyl group, a higher alkylphenyl group, a higher alkyl group or —(CH2)n—NHX wherein n is an integer of 1 to 10 and X represents a higher alkanoyl group or an alkylamino group.

Abstract: The present invention provides a method of synthesizing an allyl pentasaccharide having the structure: as well as related oligosaccharide ceramides and other glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefor, and in a method for preventing recurrence of epithelial cancer.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers and nitriles; R2 is hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R3 is selected from the group consisting of hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R4 is of methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; and R5 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxyl, amide and ester. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.

Abstract: A composition is provided for treating diseased, injured or diseased cartilage comprising hyaluronic acid and a growth factor. The composition has a viscosity and biodegradability sufficient to persist at the site for a period of time sufficient to alleviate the symptoms of the disease, injury or abnormality. Preferably hyaluronic acid is used in a composition range of 0.01-4% by weight and the preferred growth factor is IGF-I, present in a concentration range of about 10−6 to 100 mg/ml.

Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2 (C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by—are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

Abstract: The present invention is a compound of general formula (I) or a pharmaceutically acceptable salt of, wherein W represents carbon chain from 9 to 17 which containing double bond or hydroxy group occasionally; X represents carbon chain from 11 to 25 which containing double bond or hydroxy group occasionally; Y represents —(CH2)a—CH═CH—(CH2)a′—, —(CH2)a— (a, a′ denotes an integer of 0-5 and a+a′ is 5 and under.), —S(O)0-2CH2—, —NHCH2—; Z represents —CO—, —SO2—; R represents —CH2OH, CO2H, CH2OCH2CO2SO3H; R0 represents —OH, —NH2, —NHAc.

Abstract: The invention provides pharmaceutical formulation comprising voriconazole, or a pharmaceutically acceptable derivative thereof, and a sulfobutylether &bgr;-cyclodextrin.

Abstract: Compositions comprising ferrous ion and an ascorbate have a synergistic effect on cartilage development. Therapeutic compositions comprising ferrous ion and an ascorbate are therefore useful in the treatment of osteoarthritis. The addition of a glucosamine, such as glucosamine hydrochloride, to the composition has a further enhanced effect on cartilage production. Therapeutic compositions comprising ferrous ion, an ascorbate and a glucosamine derivative are even more useful in the treatment of osteoarthritis.

Abstract: A method and composition for inhibiting human cholesterol absorption comprising ingesting a therapeutic amount of an inhibitor of human cholesterol esterase comprising very high molecular weight sulfated polysaccharide having a sulfate to monomer ratio of from 1.0 to 3.0, containing less than about 5.0 wt. percent of sulfated polysaccharides having a molecular weight less than 75,000 Daltons, and containing less than 0.5 weight percent of inorganic sulfate.

Abstract: The application discloses esters of hyaluronic acid, wherein a first part of the carboxylic functions is esterified with an araliphatic alcohol and a second part is esterified with at least one long-chain, straight aliphatic alcohol with between 10 and 22 carbon atoms. The possible remaining non-esterified carboxylic functions, if present, are salified. The application further discloses biocompatible threads having a multifilament conformation comprising filaments formed by the aforesaid esters, and their use in the fields of medicine and surgery.

Abstract: The present invention relates to a pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina which comprises sucrose and/or maltose, to the use of certain sucrose and/or maltose, in preparing the pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina, in particular to a method for stimulating the growth of gram-positive bacilli and increasing the acidity in the vagina, treating the reduction of gram-positive bacilli and the lowness of acidity in vagina as well as the vaginitis and the disturbance of vaginal bacterioflora accompanying the reduction of gram-positive bacilli, especially bacterial vaginal disease.

Abstract: The present invention relates to dextran whose boron content is reduced to a value less than 0.30 &mgr;g/g (dry basis) calculated on the basis of boron atom, a process for producing the same, and dextran with which a container is filled in a solution state. Dextran of the present invention is obtained by treating a boron-containing dextran with a lower alcohol, and said dextran has such a characteristic that deposition is inhibited or the deposition rate is drastically reduced when using it in the form of a solution. Therefore, an isotonic sodium chloride solution of said dextran is suitably used as substitute plasma or external perfusate in an operation.

Abstract: Methods for chemical modification of hyaluronic acid, formation of amine or aldehyde functionalized hyaluronic acid, and the cross-linking thereof to form hydrogels are provided. Functionalized hyaluronic acid hydrogels of this invention can be polymerized in situ, are biodegradable, and can serve as a tissue adhesive, a tissue separator, a drug delivery system, a matrix for cell cultures, and a temporary scaffold for tissue regeneration.

Abstract: The present invention relates to a purified, easily produced poly-&bgr;-1→4-N-acetylglucosamine (p-GlcNAc) polysaccharide species. The p-GlcNAc of the invention is a polymer of high molecular weight whose constituent monosaccharide sugars are attached in a &bgr;-1→4 conformation, and which is free of proteins, and substantially free of single amino acids, and other organic and inorganic contaminants. In addition, derivatives and reformulations of p-GlcNAc are described. The present invention further relates to methods for the purification of the p-GlcNAc of the invention from microalgae, preferably diatom, starting sources. Still further, the invention relates to methods for the derivatization and reformulation of the p-GlcNAc. Additionally, the present invention relates to the uses of pure p-GlcNAc, its derivatives, and/or its reformulations.

Abstract: The subject matter of the invention is branched maltodextrins, characterised by the fact that they present between 22% and 35%, preferably between 27 and 34%, glucosidic linkages 1→6, a content of reducing sugars lower than 20%, a polymolecularity index lower than 5 and a number average molecular weight Mn at most equal to 4500 g/mole, and the method of obtaining these branched maltodextrins.

Abstract: The present invention provides an anti-thrombogenic and cellular-adhesion coating composition for blood-contacting surfaces. The coating comprises a covalent complex of from 1 to 30 hydrophobic silyl moieties of Formula I: wherein R1 is an C1-18 alkyl or C6-32 aryl group, each R2 is independently selected from the group consisting of C1-18 alkyl and C6-32 aryl, R3 is N or O, n is a number from 1 to 10, directly bound to a heparin molecule via covalent bonding, with an adhesive molecule directly bound to the heparin molecule. In one embodiment, the coating comprises benzyl-(1,2 dimethyl)disilyl heparin, wherein an adhesive molecule, such as fibronectin, is bound to the heparin.

Abstract: Glucosamine salts are effective for the inhibition of neutrophil functions, and hence, are useful for the prevention and/or treatment of diseases, caused as a result of an excessive extracellular release of active oxygen and antibiotic proteins by neutrophils, such as respiratory disease syndrome and adult respiratory disease syndrome. Use of glucosamine salts can, therefore, provide neutrophil function inhibitors, preventives and/or remedies for diseases caused as a result of an excessive extracellular release of active oxygen and antibiotic proteins by neutrophils, and also methods for the prevention and/or treatment of such diseases.

Abstract: The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine n a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins.