Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst, and subsequent purification of the anhydrosugar alcohol. Very high purities are achieved, without the use of organic solvents in the process.

Abstract: The present invention relates to a low temperature, solvent-free trans-acidolysis process for preparing surface-active carbohydrate fatty-acid esters comprising the steps of: (e) reacting acylated carbohydrate with free fatty acid in the presence of acid catalyst, under reduced pressure, and without adding any solvent; (f) decolorizing and separating the reaction mixture obtained in step (a) into unreacted fatty acid layer and a carbohydrate fatty-ester layer; (g) precipitating out the unreacted acylated carbohydrate; (h) librating the hydroxyl groups by partial hydrolysis in the presence of an acid catalyst; (i) removing the unreacted free fatty acids and unreacted carbohydrate esters of low molecular-weight carboxylic acids during purification, and recycling the removed unreacted free fatty acids and carbohydrate esters to the starting reactant mixture.

Abstract: A method for extracting a hydrophobic group-containing water-soluble organic compound, comprising the step of bringing an aqueous solution containing the hydrophobic group-containing water-soluble organic compound and a saccharide into contact with a polar organic solvent to obtain an aqueous phase and an organic phase, whereby the hydrophobic group-containing water-soluble organic compound is transferred to the organic phase. The saccharide concentration of the aqueous solution may be at least 12 g per 100 ml of the aqueous solution. The aqueous solution may further contain a phase separation assisting agent. The phase separation assisting agent may be selected from the group consisting of sodium chloride, sodium citrate, magnesium sulfate, and ammonium sulfate.

Abstract: Provided are reagents and methods useful for the synthesis of guanidinylated compounds. Also provided are methods for assaying molecules, including guanidinylated molecules that modulate viral infection and replication.

Abstract: The invention relates to a process for the production of peracylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents methyl, ethyl, propyl, isopropyl, tbutyl, phenyl, n means 2, 3 or 4, X means —COO— or —NH—and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of peracylated saccharides with 1-O-functionalized side chains on an enlarged scale.

Abstract: A process for producing aldehydes, and/or carboxylic acids is described, in which a primary alcohol, especially a carbohydrate, is oxidized using a catalytic amount of a nitrosonium compound obtained by oxidizing a nitroxyl compound in the presence of an enzyme compound capable of oxidation. Further described are oxidized carbohydrates containing at least 1 cyclic monosaccharide chain group carrying a carbaldehyde group per 25 monosaccharide units and per molecule.

Abstract: The invention relates to processes for preparing compounds of formula 1 wherein R3 is as defined herein, and to pharmaceutically acceptable salts thereof, as well as intermediates useful in such processes. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing compounds prepared by the processes of the invention and to methods of treating bacterial protozoa infections by administering such compounds.

Abstract: 6-O-Acyl ketolide antibacterials of the formula: wherein R1, R2, R3, R4, W, X, X′, Y, and Y′ are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: Disclosed are pH dependent ion exchange matrices, methods of making, and methods of use.

Abstract: A method of making an arginine silicate-containing complex and its use in the prevention and treatment of atherosclerosis and as a dietary supplement are claimed. The arginine silicate complex is synthesized by combining arginine, potassium silicate and inositol.

Abstract: The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.

Abstract: A versatile methodology to obtain efficient catalytic materials suitable for selective, liquid-phase oxidations of alcohols is described. Solid inorganic membranes were prepared by the sol-gel procedure by adding a solution of stable organic nitroxyl radicals at the onset of the polymerization of silicon alkoxide monomers. In this way, micro- and mesoporous materials can be obtained that axe effective and recyclable catalytic mediators for highly selective oxidations of a vast class of primary and secondary alcohols carried out with several primary oxidants. Delicate substrates such as carbohydrates and allylic alcohols can selectively be oxidized with these novel catalytic materials.

Abstract: The present invention relates to a process for the modification of a material surface comprising the steps of (a1) photochemically fixing one or more different compounds of formula onto the material surface, or (a2) photochemically fixing a compound of formula onto the material surface and subsequently converting the —ZH groups to —Z—X moieties, wherein the variables each have the meanings as given in the claims; and (b) enzymatically attaching one or more further carbohydrates to the X radicals of the modified surface obtained according to stop (a1) or (a2). The materials obtainable by the process of the invention are useful, for example, for the manufacture of biomedical devices including biosensors.

Abstract: Process for preparing a solubilization adjuvant, which comprises placing fusel oils in contact with one or more reducing sugars in the presence of an acid catalyst, at a temperature of between 50° C. and 130° C. and while removing the water from the reaction medium until a solution of alkyl glycosides is obtained, and separating the glycosides from this solution.

Abstract: Anthocyanic colorant made of vegetable primary material and process for its production relate to food, cosmetic, pharmaceutical and textile industry and may be used in production of alcoholic and soft drinks, confectionery, products made of sour milk, in coloring of tablet capsules, dying of children's underwear, toys, etc. According to the invention, pelargonidin glycoside was added to the composition of the natural colorant that contained cyanidin glycosides, peonidin glycosides, organic substance and mineral salts. The components percentage shall be as follows, %: cyanidin glycoside 0.1-8.6; peonidin glycoside 0.08-6.45 pelargonidin glycoside 0.005-4.3; organic substance and mineral salts—the rest. Due to the fact that the colorant solution contains pelergonidin glycoside further to cyanidin and peonidin glycosides, the proposed colorant obtained expanded color spectrum. Combination of these three anthocyans in the proposed colorant provides for the most rich spectrum of red colors.

Abstract: The invention relates to a method of crystallizing maltitol from a maltitol solution by supersaturating the solution in repsect of maltitol and crystallizing the maltitol from the solution. In the process of the invention, the maltitol-containing solution is brought to a supersaturated state, and the solution is subjected to evaporation, until a crystallization mass is obtained which has a crystal yield of 1 to 80% on maltitol, and a dry solids content of over 50%. After bringing the solution to a supersaturated state, the solution is preferably seeded by adding maltitol seed crystals. In one embodiment of the invention, additional feed liquid is added during the crystallization by evaporation.

Abstract: Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.

Abstract: This invention relates to methods of preparing a compound of Formulae 2, 5 and 7, wherein R2-R5, R7, R9, R10 and R15 are defined herein.

Abstract: The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.

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: There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C—O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

Abstract: There are described novel 5-O-mycaminosyltylonide derivatives and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: A simple and easy process for preparing pharmacologically useful flavonoid compound having reductase inhibitory effect, active oxygen extinguishing effect, carcinogenesis promotion inhibitory effect, anti-inflammatory effect, and so on. Particularly, a process for preparing the compound of the formula (I): wherein, R2 is a substituted or un-substituted phenyl group; R7 is a hydrogen atom or a hydroxyl group; and n is an integer of 1 to 4; by bonding a sugar derivative to catechins as the starting compound selectively via O-glycoside bond and then oxidizing the 4-position of flavanoid skeleton of the obtained compound.

Abstract: Azithromycin in the form of a stable monohydrate and processes for the preparation of azithromycin in the form of an, e.g. stable, monohydrate.

Abstract: The invention relates to a production method of &agr;-amylase resistant polysaccharides with high RS content, comprising the following steps: a) producing a paste of water-insoluble poly-(1,4-&agr;-D-glucan) and water; b) heating the paste; c) cooling off and retrogradation of the past at a temperature that is lower than the temperature of the heated paste and d) optionally drying the resulting product.

Abstract: The present invention is directed to nucleoside analogues with as substitute for the sugar part a 1,5-anhydrohexitol moiety, doexygenated and substituted with a nucleobase at the 2-position, of which the hexitorl ring is further substituted with at least one alkoxy substituent at the 3-position or at the 1-position, and to oligonucleotides wherein at least some of the nucleotides are part of the afore mentioned hexitol nucleoside analogues and exhibit sequence-specific hydridization to complementary sequences of nucleic acids, and maintaining or improving the hybridisation strength. The invention further relates to nucleoside analogues with a 1,5-anhydrohexitol moiety as the sugar part, deoxygenated and substituted with a nucleobase at the 2-position, of which the hexitol ring is substituted with a methoxy substituent at the 1-position, having at the same time either a hydroxy or an alkoxy group at the 3-position, or having a 3-deoxygenated position.

Abstract: Compound JK represented by the general formula (1): wherein R is H or —CH3; or a pharmaceutically acceptable salt thereof. Compound JK has an excellent antimicrobial activity even against resistant strains including MRSA and is useful as an anti-microbial agent.

Abstract: The invention relates to a method for recovering high-purity isoquerectin from bioflavonoid pastes, that is from mother-liquor residues which are produced during the recovery of flavonoids, by extraction with a solvent mixture of methyl acetate and water.

Abstract: A method is described for the extraction of products having a pharmacological activity, in particular an immunomodulating activity, from spermatophyte plants. Said products, which are to be used in the pharmaceutical fields, consist of complex mixtures of compounds characterized by one or more stilbene groups, variously hydroxylated and/or glucosidated, and of compounds derived from said group by natural enzymatic biosynthetical processes (stilbenoids). The following compounds are preferred: T-Res, C-Res, glucosidated C-Res, &egr;-viniferine, H-gnetine, r-2-viniferine, r-vinifezine, hopeaphenol, Ampelopepsin A and glucosidated T-Res.

Abstract: The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

Abstract: There are described 11-O-substituted macrolides and their descladinose derivatives and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: There are described novel 11-O-substituted ketolide derivatives of clarithromycin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: The present invention refers to compounds of general formula (I), the pharmaceutically acceptable salts thereof, the processes for their preparation, and the pharmaceutical compositions containing them.

Abstract: The present invention relates to dehydrated dextrose monohydrate having a specific surface area of from 0.20 m2/g to 0.50 m2/g and is reducing the reaction time for preparing chemical compounds selected from the group consisting of alkyl glucoside, alkenyl glucoside, alkyl polyglucosides and alkenyl polyglucosides in a heterogeneous mixture with an alcohol. The present invention further discloses a process for preparing dehydrated dextrose monohydrate and a process for preparing chemical compounds selected from the group consisting of alkyl glucoside, alkenyl glucoside, alkyl polyglucosides and alkenyl polyglucosides by applying dehydrated dextrose monohydrate.

Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract: A hair treatment composition containing: (a) an esterquat; (b) an alkyl and/or alkenyl oligoglycoside; (c) a partial glyceride; and (d) a fatty alcohol ethoxylate.

Abstract: A process for manufacturing morphine-6-glucuronide and related compounds of the general structure of Formula 1: wherein optionally substituted morphine is conjugated with an optionally substituted member of a new class of intermediates, namely, 1-haloglucuronate esters, in the presence of iodine or an iodinium compound. The conjugation may be followed by conversion of R1 of Formula 1 into hydrogen and/or the removal of the ester groups from the glucuronic residue at R2 of Formula 1.

Abstract: A process is described for continuous production of anhydrosugar alcohol by continuous introducing of sugar alcohols and/or monoanhydrosugar alcohols into a reaction vessel and dehydration in the presence of an acid catalyst and solvent in which the resultant reaction product is soluble. Water and the solvent having the dissolved reaction product are each cointinuously removed from the reaction vessel. The reaction product is separated from the removed solvent and the product is optionally purified to a purity of 99.0% the solvent is recycled in the reaction vessel.

Abstract: A single rapid procedure for the quantitative and qualitative analysis of flavonoid glycosides and steroidal glycosides, in natural products, has been developed. The material is extracted with aqueous solutions of polar organic solvents in an ultrasonic bath. Interfering compounds are removed by pre-purification procedures prior to instrumental analysis by High Pressure Liquid Chromatography with Negative Ion Electrospray Mass Spectrometric Detection and on-line Diode Array Ultraviolet-Visible Spectroscopy. The analysis of flavonoid and steroidal glycosidic compounds in HOSTA leaves served as a model system.

Abstract: The present invention relates to a novel 6-O-methylerythromycin A crystal form, a process for preparing the crystal form, and methods for using the crystal form to prepare a 6-O-methylerythromycin A crystal form II.

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.

Abstract: The invention relates to a series of polyglycoside derivatives that contain water-soluble groups introduced into the molecule by reaction with the hydroxyl groups present in the starting polyglycoside molecule, with the chloro material. The preferred products have more than one water-soluble group per molecule and are made with mild reagents to avoid discoloration and mal odor. The most preferred products have between 2 and 3 functional groups per molecule.

Abstract: Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

Abstract: A &bgr;-D-glucofuranose compound which is 1,2,3,5,6-penta-O-propanoyl-&bgr;-D-glucofuranose, preferably in crystalline form, is prepared from D-glucose. The compound is prepared by reacting D-glucose with boric acid, or an equivalent thereof, followed by treatment with a propanoylating reagent, preferably propanoic anhydride. The compound is useful for the preparation of other compounds, such as glucofuranosides.

Abstract: The invention pertains to a process for the regeneration and recovery of periodate from a spent iodate solution, by reacting the iodate with at least an equimolar amount of peroxosulfate. The regenerated periodate is especially suitable for oxidizing carbohydrates to dialdehyde carbohydrates. The oxidation and regeneration can also be carried out in a single stage using a catalytic amount of periodate only.

Abstract: The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether.

Abstract: This method is for preparing salts of amphotericin B methyl ester and other polyene macrolide esters. The steps of the process involve methylation by use of cesium carbonate for converting to methyl ester and significantly reducing side products, which are over methylation products. The free base-Schiff base mixture is converted to amphotericin B methyl ester hydrochloride or some other salt form, by using tetrahydrofuran-water to dissolve the mixture for acid treatment to obtain the salt. The aldehyde liberated during salt formation is removed by centrifuging, as to any precipitated aldehyde, and the aldehyde remaining in solution is removed by eluting the solution through a reverse phase adsorbent to obtain amphotericin B methyl ester hydrochloride as a yellow powder.

Abstract: 6-O-Carbamoyl ketolide antibacterials of the formula: wherein R1, R2, R3, R4, R5, R6, X, X′, Y, and Y′ are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.

Abstract: The invention provides a process to prepare a complex of adsorption charcoal-GM1 stable at different pH values. This process is based on the suspension method, the formulation example being presented. An analytical method to determine non derivatized GM1 in aqueous solutions using the high efficiency liquid chromatography technique is also object of the present invention.

Abstract: An invention is a chemical process for complete destruction and safe disposition of hazardous organic chemicals carbonaceous chemicals. The invention also comprises the process for production of an inert polymer formed essentially of Carbon and Sulfur, and also comprises the new inert polymer, itself and articles made of the new polymer. This new polymer has many of the properties of refractory materials and is an inert non-inflammable cross-linked polymer that is relatively insoluble in all generally known solvents. In the process of the invention, a carbonaceous chemical and Sulfur is heated, in an atmosphere of Nitrogen at 500.degree. to 1500.degree. C. Waste gases including sulfur and sulfides are condensed, scrubbed and the sulfur recycled. The solids residue when analyzed by a mass spectrometer contains less than one (1) part per million (1 ppm) of unreacted organic chemical.