Abstract: Galactosylhydroxylysine is a terminal degradation product of the bone matrix which thus serves as biochemical marker of bone resorption. A method of synthesizing galactosylhydroxylysine is provided. Antibodies against this synthetically prepared galactosylhydroxylysine conjugated to protein carriers were raised to establish methods to measure galactosylhydroxylysine in biological fluids. The antibodies of the invention recognize native galactosylhydroxylysine and are, for example, useful in the measurement of galactosylhydroxylysine as a biochemical marker of bone resorption in biological fluids. Testing of human serum or adolescent urine resulted in dose-dependent increases in signal intensity using the method of the invention.

Abstract: Compounds of the formulae I and II ##STR1## are suitable for the suppression of tumor growth and of tumor metastasis.

Abstract: A novel saponin component having a molecular weight of about 956 daltons, a process for isolating the saponin component from the bark of Quillaja saponaria Molina, a vaccine formulation comprising the saponin component as an immune adjuvant, a method for increasing the immune response to an antigen by employing an adjuvant composition comprising saponin component and a second adjuvant.

Abstract: This present invention provides a method and compounds for priming the incorporation of cellular glucose into an oligosaccharide in a cell comprising administering to the cell a priming amount of a membrane-permeating nontoxic glycoside having a suitable hydrophobic organic group joined by a linkage to a suitable hydrophilic saccharide, wherein the hydrophilic saccharide has a nonreducing terminal sugar residue selected from the group consisting of glucose or xylose, thereby priming the incorporation of cellular glucose onto the glycoside to form an oligosaccharide. Also disclosed are methods wherein the administration of the glycoside is sufficient to treat diabetes mellitus and glycogen storage disease.

Abstract: The present invention provides a novel purine 4'-thioarabinonucleoside represented by the following formula ?1!: ##STR1## wherein B represents a purine base other than adenine. Also disclosed are a method for preparing the purine 4'-thioarabinonucleoside and pharmaceutical compositions containing the purine 4'-thioarabinonucleoside.

Abstract: A cosmetic composition is provided comprising:A) a cosmetically acceptable carrier; andB) 0.05 to 3.0% by weight, based on the weight of the total composition, of a .beta.-1,3-glucan having a mean molecular weight of 10.sup.5 to 25.10.sup.6.

Abstract: The present invention relates to 2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides having excellent antitumor activity, represented by formula ?I!: ##STR1## wherein B represents a pyrimidine or purine base, R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, a cyano group or alkyl group, and R.sub.3 represents hydrogen or a phosphoric acid residue, and a method for producing the same, and a use of the same.

Abstract: The invention relates to multiply fucosylated dicarboxylic acid derivatives possessing antiadhesive properties, to a process for preparing them, to their use, and to pharmaceuticals and diagnostic agents which are prepared from these derivatives. These multiply fucosylated dicarboxylic acid derivatives are suitable for preparing pharmaceuticals or diagnostic agents for diseases which are associated with an excessive, selectin receptor-mediated cell adhesion in the tissue which is affected by the disease.

Abstract: Disclosed is a 5-O-pyrimidyl-2,3-dideoxy-1-thio-D-furanoside derivative represented by the following formula (I) or an L-form isomer thereof: ##STR1## wherein X represents a hydrogen atom, a fluorine atom or an azido group; R.sup.1 represents a C.sub.1-4 alkyl group; R.sup.2 represents a hydrogen atom, a methyl group or a fluorine atom or a trifluoromethyl group; R.sup.3 represents a C.sub.1-10 alkyl group or a C.sub.6-15 aryl group which is unsubstituted or substituted with at least one substituent selected from the group consisting of a chlorine atom, a bromine atom, a methyl group, an ethyl group and a nitro group. When this derivative is reacted with a sulfonium ion-generating reagent to thereby effect an intramolecular N-glycosylation of the derivative, a .beta.-2',3'-dideoxynucleoside derivative which is useful as a precursor of an antiviral agent, such as AZT, DDC or FLT, can be produced with an extremely high stereoselectivity for the .beta.-anomer and in high yield while very little or none of the .

Abstract: A sialyl Lewis X derivative represented by the general formula: ##STR1## in which a hydroxyl group at the 2 position of fucose is replaced with a fluorine atom, and a synthetic intermediate therefor are provided.

Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier.

Abstract: The invention describes 7-O-carbamoyl heptose derivatives of general formula (I) in which R is the substituent R.sup.1 or a group of general formula (II) in which R.sup.1 is a hydrogen atom, a methyl group or a suitable linker substituent suitable for a covalent coupling, a process for their production and their use in producing reagents and compositions for the diagnosis and therapy of pseudomona infections in humans and animals, and a screening process for their detection in Gram-negative bacteria.

Abstract: Semisynthetic analogues of gangliosides selected from the group consisting of N-sulfo-, N-hydrocarbyl-sulfonyl- and N-hydrocarbyloxy-sulfonyl-N,N'-dilyso-gangliosides and the N'-acyl derivatives thereof, N'-sulfo-, N'-hydrocarbylsulfonyl- and N'-hydrocarbyloxy-sulfonyl-N,N'-dilyso-gangliosides and the N-acyl derivatives thereof, N,N'-di or polysulfo-N,N'-di- or poly-lyso-gangliosides, N,N'-di- or polyhydrocarbylsulfonyl-N,N'-di- or poly-lyso-gangliosides and N,N'-di- or polyhydrocarbyloxy-N,N'-di- or poly-lyso-gangliosides, and functional derivatives thereof, and salts of these compounds, have protective activity against neurotoxicity induced by excitatory amino acids and are foreseen to be used in therapy in the nervous system and in modulating of the expression of determinants such as CD.sub.4 on the surface of human cells in the immune system.

Abstract: The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.

Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##

Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinamide, and a process for their manufacture.

Abstract: The invention relates to 1-C-perfluoroalkyl glucosides consisting essentially of a monosaccharide having an anomeric carbon directly linked to a perfluoroalkyl radical and a hydroxyl group. These glycosides are prepared by a process comprising: (a) reacting an aldonolactone with a hydroxyl protecting group; (b) reacting the product of step (a) with a compound of formula R.sub.F -M in which R.sub.F represents a linear or branched perfluoroalkyl radical containing from 2 to 12 carbon atoms, and M represents Li or MgX, X being a halogen; and (c) liberating the hydroxyl group. The 1-C-perfluoroalkyl glycosides may be used as surfactants and as flame retardants.

Abstract: A composition and process for enhancing the aesthetic and tactile properties of an alkyl polyglycoside involving combining an alkyl polyglycoside having the general formula I:RO(Z).sub.a (I)wherein R is a monovalent organic radical having from about 8 to about 18 carbon atoms; Z is a saccharide residue having 5 or 6 carbon atoms; and a is a number having a value from about 1 to about 6, with an aliphatic alcohol having from 1 to about 20 carbon atoms.

Abstract: Sulfated disaccharides characterized by the ability to inhibit the binding of selectin to its physiologically-relevant ligand are disclosed. Included are efficient and inexpensive methods for producing the sulfated disaccharides, and methods for their therapeutic use and in in vivo and in vitro assays.

Abstract: The present invention relates to a method for making a compound of the structure: ##STR1## comprising the steps: (a) adding 6-deoxy-.alpha.-L-mannopyranosyl bromide, 2,3,4-tri-O-benzoate; DMSO; a base, selected from the group including tertiary amines, amidines, bicarbonates, carbonates, heteroaryl amine, and a solvent, hydrocarbons, esters, and ethers, in a slurry heated to 50.degree.-150.degree. C.;(b) stirring the reaction mixture at 50.degree.-150.degree. C. for 5 minutes to 30 minutes,(c) pouring the reaction mixture over ice water; and(d) extracting the product with a solvent selected from the group consisting of chlorinated solvents, aromatic hydrocarbons, esters, ethers, and evaporating said layer to give a solid.

Abstract: A method for screening a compound as a potential anti-obesity agent by determining whether the compound stimulates micro motion of cells in vitro is described

Abstract: The in vivo oxidation of lipids and lipid-containing molecules has been discovered to be initiated by the concurrent reaction of such lipid materials with reducing sugars such as glucose, advanced glycosylation endproducts such as ME-peptides, or a compound which forms advanced glycosylation endproducts, to form materials or particles known as AGE-lipids. AGE-lipids have been implicated in the aging process, the abnormal formation of lipofuscin and in various disease states such as diabetes and atherosclerosis. Diagnostic methods are contemplated, extending in utility from the detection of the onset and course of conditions in which variations in lipid oxidation, AGE-lipid levels, LDL levels, apolipoprotein levels, apolipoprotein receptor binding the like, may be measured, to drug discovery assays.

Abstract: The invention relates to water-soluble sugar retinoids (I) and to their preparation and the use thereof as medicaments and in the cosmetic sector, wherein X is a sugar radical attached at an oxygen atom, i.e. a mono-, di- or oligosaccharide, provided that X is not a glucose or galactose sugar residue attached at the oxygen atom in the respective 1-positions of the glucose or galactose residues.

Abstract: Disclosed are methods for synthesizing very large collections of diverse thiosaccaride derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccaride derviatives.

Abstract: Disclosed is carboxymethyl inulin having a degree of substitution (DS) ranging from 0,15 to 2,5, preferably from 0,5 to 1,5, a process for the preparation of said carboxymethyl inulin by reacting inulin at a concentration of at least 100 g/l, preferably at least 200 g/l, at elevated temperature with an aqueous alkaline solution of monochloroacetic acid, followed by working up the reaction mixture according to a method known in the chemical art, and the use of said carboxymethyl inulin as inhibitor for the crystallization of calcium carbonate.

Abstract: A cationic sugar surfactant made by a process involving: (a) reacting an alkyl or alkenyl oligoglycoside of the formula (I):R.sup.1 O--?G!.sub.p (I)wherein R.sup.1 is an alkyl or an alkenyl radical having from 4 to 22 carbon atoms, G is sugar unit having 5 or 6 carbon atoms and p is a number from 1 to 10, with either a chloroacetic acid, chloroacetic anhydride or chloroacetic acid methyl ester; and (b) reacting the product from step (a) with a tertiary amine of the formula (II): ##STR1## wherein each of R.sup.2 and R.sup.3 is an alkyl or alkenyl radical having from 1 to 22 carbon atoms.

Abstract: Disclosed is a process of enzymatically preparing .alpha.-glucoside esters. First, .alpha.-glucosides are produced by placing an acyclic alcohol or a mixture of acyclic alcohols having a water solubility of at least 2.7% v/v at 20.degree. C. in contact with starch, maltodextrins or maltose, in the presence of a purified enzymatic preparation having .alpha.-transglucosylation activity, wherein the enzymatic preparation is free of .beta.-glucosidase activity. Then, the .alpha.-glucosides are contacted with at least one fatty acid and a preparation having lipase activity to produce the .alpha.-glucoside esters, which may then be recovered. The preparation having .alpha.-transglucosylation activity may originate from a fungus such as Talaromyces duponti, Aspergillus niger, Aspergillus oryzae or Aspergillus batatae.

Abstract: This disclosure describes a method for constructing targeting agent drug conjugates from the family of methyltrithio antibacterial and antitumor agents.

Abstract: The present invention relates to fractions of sea cucumbers (Phylum Echinodermata, Class Holothuroidea), particularly those derived from the epithelial layers and the flower portion, that markedly inhibit inflammation in laboratory animals and show significant subjective benefit in humans with inflammation disorders such as arthritis, and methods for preparing the same.

Abstract: Regioselective acetylation of the 9-hydroxyl group on N-acetylneuraminic acid is achieved enzymatically for producing oligosaccharides which contain a terminal N-acetylneuraminic acid moiety. This method provides access to O-acylated disialogangliosides as well as other N-acetyl-neuraminic acid oligosaccharides. These compounds are biologically and medicinally important and are difficult to obtain from nature or by chemical acylations. The methodology affords simple reaction conditions and minimal purification steps. In addition, the process affords good yields and the enzymes and reagents employed are commercially available with high stability and low costs.

Abstract: A propiophenone derivative the formula ?I!: ##STR1## wherein R' is a lower alkanoyl group and R" is a hydrogen atom, or R' is a hydrogen atom and R" is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Abstract: Antibody-mediated xenograft rejection is attenuated by parenterally administering a xenoantibody-inhibiting amount of an identified carbohydrate xenoantigen to the recipient shortly before graft revascularization and thereafter.

Abstract: .alpha.-Glycosyl-L-ascorbic acid exhibiting no direct reducing activity is formed in a solution containing L-ascorbic acid and an .alpha.-glucosyl saccharide when subjected to the action of a saccharide-transferring enzyme. .alpha.-Glycosyl-L-ascorbic acid is superiorly stable, and readily hydrolyzable in vivo to exhibit the activities inherent to L-ascorbic acid. Thus, .alpha.-glycosyl-L-ascorbic acid is favorably useful as a stabilizer, quality-improving agent, antioxidant, physiologically active agent and uv-absorbent in food pharmaceutical and cosmetic industries.

Abstract: Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system;G.sup.1, G.sup.2 and G.sup.3 each independently signify a residue of a glycopyranoside, a glycopyranose or a derivative thereof, with at least one hydroxy group of residue G.sup.1, G.sup.2 or G.sup.3 being esterified with sulfuric acid, and pharmaceutically usable salts thereof, are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.

Abstract: The extraction of proteins from selected naturally occurring membranes without any harmful, adverse, or other deleterious effect(s). In one preferred embodiment the detergent is prepared from the reaction of a cycloalkyl aliphatic alcohol and a saccharide.

Abstract: A Lewis-associated compound, represented by general formula (I), a process for producing the same, and an anti-inflammatory, wherein R.sup.1 and R.sup.3 represent each hydrogen, m SO.sub.3 H or CH.sub.2 COOH; R.sup.2 represents hydrogen, SO.sub.3 H, CH.sub.2 COOH or N-acetyl-neutraminic acid residue; R.sup.4 represents hydrogen; R.sup.5 represents O-lower alkyl, O-lower alkenyl, O-ceramide residue, O-mannose residue, O-galactose residue or O-lactose residue; R.sup.6 represents acetylamine; and R.sup.7 and R.sup.8 represent each hydrogen.

Abstract: Novel oligosaccharide antibiotics of formula I and I' are disclosed, together with a method for their preparation.

Abstract: A method of adhering a denture, having a biocontact surface, to a gum or a roof of a mouth, containing the steps of: (1) Treating the biocontact surface of the denture with a denture adhesive composition containing a chemical substance derived from an aloe leaf to obtain a treated denture; and (2) placing the treated denture in close proximity to a gum or the roof of the mouth thereby engaging the treated denture with the gum or the roof of the mouth. A method of preparing a denture adhesive composition containing a chemical substance derived from an aloe leaf.

Abstract: According to the present invention, a substrate for cytochrome p450 which, after oxidation by cytochrome p450, reacts with thiol groups is conjugated to a saccharide to provide a tumor-specific compound which has low toxicity to normal cells. In one embodiment of the present invention, the saccharide conjugate of the cytochrome p450 substrate is administered in conjunction with a saccharide conjugate of a cytotoxic phenol, which provides a synergistic effect in destroying tumors.

Abstract: Light-colored alkyl and/or alkenyl oligoglycosides corresponding to formula (I)R.sup.1 O--?G!.sub.p (I)which R.sup.1 is an alkyl and/or alkenyl radical containing 4 to 22 carbon atoms, G is a sugar unit containing 5 or 6 carbon atoms and p is a number of 1 to 10, can be produced by a process in which sugars are subjected to acid-catalyzed acetalization with a large excess of primary alcohols, the reaction mixture is neutralized in the presence of reducing agents and is then bleached in known manner. At the same time, the quality of the excess fatty alcohol to be separated off is considerably improved.

Abstract: The present invention relates to a process for preparing alkylpolyglycoside compositions. Specifically the process is a direct synthesis producing compositions of highly polymerized alkylpolyglycosides in high yield. The invention further relates to alkylpolyglycoside compositions having enhanced surfactant properties. The invention also relates to mixtures of alkylpolyglycosides of preselected average alkyl chain length and controlled average degree of polymerization (DP).

Abstract: The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in those processes.

Abstract: A method for treating and/or inhibiting gastric and duodenal ulcers, comprising administering a pharmaceutical composition comprising an oligosaccharide of Formula I(NeuAc-.alpha.(2-3)-pGal-.beta.(1)--(--X--).sub.m --(--Y--).sub.n --).sub.p --ZwhereinX=a chemical bond or a group capable of linking the p galactose to either the linking group Y or the multivalent support Z;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C;Y=a linking group;Z=a multivalent support;m=0 or 1;n=0 or 1; andp=an integer of 2-1,000 is described. Also described is a method for treating and/or inhibiting gastric and duodenal ulcers, comprising administering a pharmaceutical composition comprising an oligosaccharide of Formula IINeuAc-.alpha.(214 3)-pGal-.beta.(1)-AwhereinA=a group capable of bonding to the p galactose;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C.

Abstract: A solid hard-surface cleaning composition contains from about 20 to about 40% by weight of a fatty acid component; from about 10 to about 25% by weight of a polyol component; from about 2 to about 6% by weight of a base component; from about 2 to about 15% by weight of a foaming agent; and remainder, water, all weights being based on the total weight of the composition. The cleaning composition is particularly useful in combination with an abrasive substrate such as in abrasive scouring pads, providing lubricity, sudsing and improved detergency over untreated pads.

Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.

Abstract: Compounds that are synthetically inexpensive to make relative to the naturally occurring selectin ligands and that retain selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs or derivatives of these groups, such that sialic acid and fucose are separated by a non-carbohydrate linker that permits binding between those groups and the selectins, such compounds being represented by the following general structure formula I(a): ##STR1## wherein m and n are independently an integer of from 1 to 5, Y and Z are independently a connecting moiety selected from the group consisting of --CH.sub.

Abstract: A process for obtaining pharmacologically active compounds from complex mixtures of substancesFree organic acids, hydroxy acids, fatty alcohols, sugars and hydroxy-substituted steroids are obtained from complex mixtures of substances by mixing the material to be extracted with a polar solvent, drying the resulting mixture, subsequently silylating, esterifying or acylating, and extracting the resulting material with a supercritical fluid under a pressure of more than 200 bar.

Abstract: The present invention relates to the area of pharmacology; its objective is to solve the technical problem of inflammation, pain, pruritus and local hyperthermia in human beings and animal species. The composition and the subcompositions thereof are obtained from plants of the family Cactaceae, the main methodological steps being a set of processes: production, purification, physicochemical quantification, biotherapeutic evaluation, biopharmaceutical formulation and molecular identification. From the molecular identification a set of molecules is recognized, comprising carbohydrates and an aromatic amine, the general formulae of which are:C.sub.5 H.sub.10 O.sub.5 (RIBOSE),C.sub.6 H.sub.12 O.sub.5 (FUCOSE),C.sub.6 H.sub.12 O.sub.6 (GALACTOSE; MANNOSE; GLUCOSE),C.sub.8 H.sub.11 O.sub.2 N (1-HYDROXY-1-(4-HYDROXYPHENYL)-2-AMINOETHANE),C.sub.10 H.sub.18 O.sub.9 (RIBOFURANOSYLRIBOSE).

Abstract: The use of ginsenoside R.sub.0 or a plant extract containing same to prepare a cosmetic or pharmaceutical composition, particularly a skin care composition, for promoting collagen synthesis, particularly collagen I and/or collagen III synthesis. Said cosmetic or pharmaceutical composition is administered to a mammal, particularly a human being, in order to promote collagen synthesis. A method for promoting collagen synthesis in fibroblast growth media is also disclosed.