Abstract: The present invention is an enzyme-decomposable polymer compound having recyclable decomposition products. The polymeric compound is a glycopolymer of a saccharide having only glucopyranose rings and a second component. In addition, the glycopolymer may contain molecular chains having at least one type of repeating unit, which chains are crosslinked by a saccharide having only glucopyranose rings.

Abstract: This invention relates to processes for the production of purified, partially esterified polyol fatty acid polyesters and the compositions derived from those processes. The purified, partially esterified polyol fatty acid polyesters of the present invention are particularly well suited for use in a variety of food, beverage, pharmaceutical, and cosmetic applications and comprise less than about 5% by dry weight of polyol; less than about 5 ppm of residual solvent; less than about 700 ppm of lower alky esters; less than about 5% by dry weight of a soap and free fatty acid mixture; and less than about 3% by dry weight of ash. The compositions have an acid value of less than about 6.

Abstract: The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of formula (I): useful in the synthesis of nucleotides.

Abstract: Finely divided polysacharide derivatives are described. The finely divided polysacharide derivatives are prepared by a process comprising: a) forming an aqueous composition comprising a polysaccharide derivative and water, in which the polysaccharide derivative is soaked or dissolved; b) converting the polysaccharide derivative of the aqueous composition into finely divided solid particles by, (i) contacting the aqueous composition with superheated water vapor in a dryer-pulverizer; or (ii) causing the polysaccharide derivative of the aqueous composition to flocculate; and c) optionally drying the finely divided solid particles of step b). The primary structures of the polysaccharide starting material are largely removed, and the product has a shape factor of less than 5 and greater than or equal to 1.

Abstract: A method of producing a cellueose ether that is predominantly substituted in the C2 position of the anhydroglucose unit of the cellulose is described. The regioselectively substituted saccharide ester produced according to the method of the present invention is selected from the group consisting of oligo-saccharide ester and polysaccharide ester, having a partial average degree of substitution (AS) at the C2 position of its anhydroglucose unit of at least 90% relative to the total AS. Also described is a blood plasma expander comprising the regioselectively substituted ester.

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: Methods for forming structurally defined organosilicon carbohydrates are provided. Additionally, structurally defined organosilicon carbohydrates are provided. The structurally defined organosilicon carbohydrates may be formed by contacting a hydrolase enzyme with an organosilicon reactant and a carbohydrate reactant. The enzyme may catalyze the formation of an ester bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and alcohol functional groups of the carbohydrate or organosilicon reactant. The enzyme may catalyze the formation of an amide bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and amine functional groups of the carbohydrate or organosilicon reactant.

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: The invention relates to an orally administerted agent containing stable, uronic acid-containing polysaccharides cross-linked to each other and in the form of a sponge-like structure which dissolves poorly in water and/or gastrointenstinal liquids or can be poorly resorbed.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.

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 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 invention concerns a method for preparing Laminaribiose comprising a step for glycoside binding between a donor and an acceptor of glycosyl. The invention is characterized in that the glycosyl donor is in pyranose form and corresponds to formula (II); the glycosyl acceptor is in furanose form and corresponds to formula (III); said binding step is performed in solution in an anhydrous organic solvent, at a temperature ranging between −80° C. and 40° C., for a time interval ranging between 1 minute and 8 hours, in the presence of a suitable promoter.

Abstract: A crystal comprising LuxP is obtained, and a binding site for autoinducer-2 (AI-2) identified. The X-ray crystallographic data for LuxP and a LuxP-AI-2 complex is determined and used in a drug discovery method. Pharmaceutical compositions comprising ligands identified by such drug discovery methods are used to treat bacterial infections.

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: Process for the preparation of a starch ester, in particular a starch acetate, wherein a starch-based feedstock is reacted with an organic carboxylic acid anhydride in the presence of a catalyst. The reaction of the starch-based feedstock and the anhydride is performed at an excess pressure of about 0.1 to 50 bar in an essentially anhydrous medium containing 10% by weight of water at the most. As catalyst, sodium acetate, sodium hydroxide or sulphuric acid is used, and as the reaction medium, acetic acid or excess acetanhydride is used. By means of the invention, the duration of the esterification reaction can be significantly shortened, the separation of the product can be facilitated, and the recirculation of the waste solutions can be rendered more efficient.

Abstract: The invention relates to a modified gellan gum in which the total acyl content as well as the ratio of acyl substituent groups to glycerate substituent groups per linear saccharide repeat unit is altered to be higher than 1. The invention further relates to a process for the modification of a gellan gum to alter its acyl content in which the gum is treated with a weak base such as sodium or potassium carbonate or a suitable phosphate. The process enables “tailor made” gums having appropriate setting temperatures and theological properties to be made. Novel compositions containing them are also claimed.

Abstract: The present invention provides novel &agr;-O-linked glycoconjugates such as &agr;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &agr;-O-linked glycoconjugates.

Abstract: Silane-modified biopolymeric, biooligomeric, oxidic or siliceous filler obtainable by reacting at least one biopolymeric, biooligomeric, oxidic or siliceous filler in a compressed gas with at least one silane. The silane-modified biopolymeric, biooligomeric, oxidic or siliceous fillers are used in rubber compounds.

Abstract: Methods of removing a lower alkyl alcohol from a polyester mixture of polyol fatty acid polyester and lower alkyl alcohol comprise (a) contacting the polyester mixture with a stripping mixture comprising an inert stripping gas, up to about 10,000 ppm lower alkyl alcohol and up to about 2000 ppm oxygen, wherein at least a portion of the lower alkyl alcohol is transferred from the polyester mixture to the stripping mixture, thereby increasing the concentration of lower alkyl alcohol in the stripping mixture, and (b) separating the stripping mixture from the polyester mixture.

Abstract: The invention concerns the use as surface-active agent of a fructan N-alkylurethane (I) which is composed of saccharide units of general formula (II) A(O—CO—NH—R)s  (II) wherein A represents a fructosyl unit (F) or a terminal glucosyl unit (G) of said fructan, being a levan or an inulin, with a degree of polymerisation (DP) of minimum 3, (O—CO—NH—R) represents an N-alkylaminocarbonyloxy group replacing a hydroxyl group of the saccharide unit A, wherein R represents a linear or branched, saturated or unsaturated alkyl group containing from 3 to 22 carbon atoms and any mixture thereof, and s represents the number of N-alkylaminocarbonyloxy groups per saccharide unit which is expressed as degree of substitution (DS), and said DS has a value ranging from 0.10 to 2.0. The invention further relates to novel fructan N-alkylurethanes (I), in particular inulin N-alkylurethanes (I), and a method for their manufacture.

Abstract: Product of esterified polysaccharides and the process of making such product. The process can be enzymatic where an enzyme is used as a catalyst for the reaction. The process can also be chemical where no enzyme is used. Novel products are obtained through lipase-catalyzed &bgr;-lactone ring opening alcoholysis of ketene dimers and the process of making such compositions containing products.

Abstract: A compound of formula (I) below, which exhibits excellent macrophage activity inhibitory action, is useful for the treatment or prophylaxis of inflammatory disorders, autoimmune diseases or septicemia. In a preferred embodiment, R1 and R3 each represents a C1-C20 alkanoyl group which may optionally be substituted with one or more substituent groups selected from substituent group A, R2 and R4 each represents a C1-C20 alkyl group which may optionally be substituted with one or more substituent groups selected from substituent group A, R5 is a hydrogen atom, a halogen atom, a hydroxy group, or a C1-C6 alkoxy group, and substituent group A is a halogen atom, a hydroxy group, an oxo group, a C1-C20 alkoxy group, or a C1-C20 alkanoyloxy group.

Abstract: The present invention is drawn to a pharmaceutical composition, comprising a pharmaceutically effective amount of an acidic polysaccharide and/or a derivative thereof, a gaseous vehicle, and a pharmaceutically acceptable carrier or excipient. Said acidic polysaccharide or derivative thereof can be hyaluronic acid, a pharmaceutically acceptable salt of hyaluronic acid, a partial or total ester of hyaluronic acid with an alcohol, a partial or total intermolecular ester of hyaluronic acid, a partial or total intramolecular ester of hyaluronic acid, a cross-linked ester of hyaluronic acid, an alginic acid ester, an ester of carboxymethylcellulose, an ester of carboxymethylchitin, an ester of carboxymethyl starch, a gellan ester, a cross-linked gellan ester, a pectic acid ester, and a pectinic acid ester. The composition can contain one or more topical drugs, and can be in the form of an aerosol or liquid spray, a foam, or a dry spray.

Abstract: A regioselectively substituted member selected from the group consisting of oligo-saccharide ester and polysaccharide ester is disclosed. The ester has a partial average degree of substitution AS at the C2 position of its anhydroglucose unit of at least 90% relative to the total AS. Also disclosed is a method of producing the regioselectively substituted ester. The method entails reacting in the presence of a catalyst a dissolved or a highly swollen oligo-saccharide or polysaccharide with an esterification reagent.

Abstract: Protease enzyme from Bacillus subtilis and Bacillus sp. Catalyzes the acylation of organic solvent-insoluble macromolecules in isooctane solution containing vinyl esters of fatty acids, lactones or lactides as acyl donors. The reaction occurs only when the enzyme is solubilized via ion-pairing with the anionic surfactant dioctylsulfosuccinate, sodium salt (AOT). Enzyme based acylation was demonstrated in macromolecules such as silk proteins. These macromolecules are reactive either as cryogenically milled powder suspended in the organic solvent or as a thin film deposited onto ZnSe slides. This selective acylation approach represents the first attempt at using enzymes to modify organic-insoluble macromolecules in nonaqueous media.

Abstract: Protease enzyme from Bacillus subtilis and Bacillus sp. Catalyzes the acylation of organic solvent-insoluble macromolecules in isooctane solution containing vinyl esters of fatty acids, lactones or lactides as acyl donors. The reaction occurs only when the enzyme is solubilized via ion-pairing with the anionic surfactant dioctylsulfosuccinate, sodium salt (AOT). Enzyme based acylation was demonstrated in macromolecules such as silk proteins. These macromolecules are reactive either as cryogenically milled powder suspended in the organic solvent or as a thin film deposited onto ZnSe slides. This selective acylation approach represents the first attempt at using enzymes to modify organic-insoluble macromolecules in nonaqueous media.

Abstract: Aureobacterium barkerei strain KDO-37-2 (ATCC 49977) and KDO aldolase (EC 4.1.2.23) isolated therefrom are disclosed. The KDO aldolase is further disclosed to have a broad substrate specificity with respect to its reverse reaction, i.e. the condensation of aldoses with pyruvate to form a wide range of 2-keto-3-deoxy-onic acids, including 2-keto-3-deoxy-nonulosonic acid, 2-keto-3-deoxy-octulosonic acid, 2-keto-3-deoxy-heptulosonic acid, and 2-keto-3-deoxy-hexulosonic acid. In particular, 3-deoxy-D-manno-2-octulosonic acid (D-KDO), a vital component of lipopolysaccharides found in the bacterial outer membrane may be synthesized from D-arabinose and pyruvate in 67% yield. Additionally, protected forms of the KDO aldolase products, e.g. hexaacetyl 2-keto-3-deoxy-nonulosonic acid and pentaacetyl 2-keto-3-deoxy-octulosonic acid, may be decarboxylated to form the corresponding 2-deoxy-aldoses, e.g. 2-deoxy-octulose and 2-deoxy-heptulose respectively.

Abstract: It is possible to prepare cationic derivatives of fructans, such as inulin, in which a nitrogen atom having substituents R1, R2 and R3 is bonded to one or more anhydrofructose units via a straight-chain or branched C2-C6 alkylene group, which is optionally preceded by a carbonyl group or interrupted by one or two oxygen atoms or imino or alkylimino groups and optionally substituted by one or two hydroxyl groups or amine groups or a carboxyl or carbamoyl group, the substituents R1, R2 and R3 having the following meaning: R1 and R2 each represent hydrogen, methyl carboxymethyl, phosphonomethyl, ethyl, hydroxyethyl, propyl, isopropyl, allyl, hydroxypropyl or dihydroxypropyl or, together with the nitrogen atom, form a cyclic group, R3 represents hydrogen, C1-C18 alkyl, C3-C18 alkenyl, alkynyl or cycloalkyl, C4-C18 cycloalkyl-alkyl or C7-C18 aralkyl or is bondedvia an alkylene group to an oxygen atom of a subsequent anhydrofructose unit.

Abstract: Acylated cellobiose compounds (CHME) which satisfy the formula; 1

Abstract: A method for the enzymatic synthesis of sucrose ester, comprises introducing, in an adapted reactor and so as to form a reaction medium, predetermined amounts of an organic solvent, a sugar or a sugar derivative, a compound donor of acyl groups and an enzymatic catalyst, the amount of at least one constituent of the reaction mixture being deficient, in controlled addition during the reaction of additional amounts of the deficient constituent(s), and finally purifying the resulting sucrose esters at least by separating the fine enzymatic particles from the solvent.

Abstract: C-glycoside derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment and/or prevention of diabetes and hypoglycemia.

Abstract: The present invention is an enzyme-decomposable polymer compound having recyclable decomposition products. The polymeric compound is a glycopolymer of a saccharide having only glucopyranose rings and a second component. In addition, the glycopolymer may contain molecular chains having at least one type of repeating unit, which chains are crosslinked by a saccharide having only glucopyranose rings.

Abstract: Variant xanthan gums are provided which include a water-soluble polysaccharide polymer comprising repeating pentamer units having a D-glucose:D-mannose:D-glucuronic acid ratio of about 2:2:1, and a water-soluble polysaccharide polymer comprising repeating tetramer units having a D-glucose:D-mannose:D-glucuronic acid ratio of about 2:1:1. The D-glucose moieties are linked in a beta-[1,4] configuration. The inner D-mannose moieties are linked in an alpha-[1,3] configuration, generally to alternate glucose moieties. The D-glucuronic acid moieties are linked in a beta-[1,2] configuration to the inner mannose moieties. The outer mannose moieties are linked to the glucuronic acid moieties in a beta-[1,4] configuration. Processes for preparing the polysaccharide polymers are also provided.

Abstract: Synthetic enantiomeric esters are employed as energy substrates for parenteral or enteral nutritional formulations. The substrates are provided in substantially monoisomeric or anomeric forms readily utilized in patient metabolism.

Abstract: An improved, solvent-free, two-stage transesterification process for preparing, from a polyol and fatty acid esters of an easily removable alcohol highly esterified polyol fatty acid polyesters having reduced levels of difatty ketones and &bgr;-ketoesters is disclosed. These reduced levels of difatty ketones/&bgr;-ketoesters are achieved by controlling the level of generated alcohol in the liquid phase of the reaction mixture and heating the reaction mixture to certain temperatures during the second stage of this improved process. Other optional reaction conditions, such as keeping the molar ratio of fatty acid esters to polyol within a specified range and reducing the level of basic catalyst, can also be used during the second stage reaction to further reduce the level of difatty ketones and/or &bgr;-ketoesters.

Abstract: The present invention embraces methods and compositions which employ antimicrobial compositions which are &agr;-alkylglucosides and esters thereof.

Abstract: A method for preparing a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids, or a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other without the spacer, characterized in that an organic amine salt of the polysaccharide derivative having carboxyl groups is reacted with the drug compound or the spacer bound to the drug compound in a non-aqueous system. The reaction between the polysaccharide derivative having carboxyl groups and the drug compound bound with the spacer or the like can be carried out in high yields, and when a drug compound having a lactone ring is subjected to the reaction, side reactions can be reduced.

Abstract: Sucrose ester and ether products, useful as food or beverage bulking agents, reduced calorie sweeteners, fat replacement agents, stabilizing agents, thickening agents and emulsifying agents; adhesives; biodegradable plastics and films; sizing agents for paper and textiles; ethical pharmaceuticals and new fibers are prepared by using a two-phase reaction system in which sucrose is dissolved in an alkaline, aqueous solution and an acidic reagent such as a bifunctional acid dichloride or epoxide is added to the sucrose in a water-immiscible organic solvent. Several types of products are produced: water-insoluble sucrose ester (ether) copolymers; water-soluble sucrose ester (ether) copolymers; sucrose ester (ether) dimers; and intramolecular, cyclic sucrose esters (ethers). These products can be further varied by using different kinds of acid dichlorides or epoxides that contain different kinds of functional groups.

Abstract: A process for preparing the ignition promoter comprises combining a sugar with selected solvents and heating to form a stable solution, reacting the resulting solution with an oxirane and thereafter reacting the resulting product with nitric acid under nitrating conditions. A fuel for use in compression ignition engines contains a lower alcohol and about 0.15 to 30 wt % of the ignition promoter.

Abstract: An aqueous coating composition comprising hydroxypropyl methyl cellulose trimellitate typically having a mean particle size of up to 10 &mgr;m and a plasticizer is applied to a solid pharmaceutical preparation to form a coating film having acid resistance and solubility at about pH 4. The coated preparation has an improved bioavailability.

Abstract: The invention relates to pharmaceutical compositions of nucleoside dimers containing an L-sugar in at least one of the nucleosides.

Abstract: Methods are disclosed for enhancing the toughness, e.g., resistance to cracking upon flexation, of coatings made from cycloaliphatic epoxide derivatives wherein the cycloaliphatic epoxide derivative is a cycloaliphatic epoxide ester of a hydroxy-functional compound containing at least one branched, 1,2-alkylene oxide unit. Processes for making the cycloaliphatic epoxide derivatives and coating formulations comprising the cycloaliphatic epoxide derivatives are also disclosed.

Abstract: The invention relates to the synthesis of sulfonated sucrose compounds, surfactants and intermediate cyclic sulfates.

Abstract: Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeleci annexin conjugates are also provided.

Abstract: The present application describes total or partial butyric esters of polysaccharides as novel compounds; the number of hydroxyl groups esterified with butyric residues per each glycosidic monomer is preferably higher than 0.001; the application also describes the process of preparation of said esters, their use in therapy as antiproliferative agents, and pharmaceutical compositions containing them.

Abstract: A process for preparing esterified polyol fatty acid polyesters is provided, where the polyol has n hydroxyl groups. The process provides for independent control of the level of fully esterified polyols, on the one hand, and the level of n-3 and lower esters, on the other hand. The process is especially suited for preparing sucrose polyester, wherein the process provides for independent control of the level of octaesters, on the one hand, and penta and lower level esters, on the other hand. The process can be used to reduce the level of undesirable reaction byproducts, such as difatty ketone and beta ketoester.

Abstract: Analogues of RNA and DNA compounds contain a neutral, stereoregular linking group based on replacement of the phosphoryl with a sulfonyl group. Precursors to the analogues are also described, as are methods for preparing the precursors and analogues.

Abstract: A pyruvate compound suitable for cosmetically or dermatologically administering to the skin and for use in treating diabetic ketosis or other medical treatments. The compound includes a pyruvate selected from the group of pyruvate thioester, dihydroxyacetonepyruvate, and an ester of pyruvate and a sugar or a polyol.

Abstract: Fatty acid esters of sucrose wherein the fatty acid groups consist essentially of short chain fatty acid radicals containing from 2 to 10 carbon atoms and long chain fatty acid radicals containing from 20 to 24 carbon atoms in a molar ratio of short chain:long chain radicals of 3:5 to 5:3, the said esters having a degree of esterification of about 7 to 8. The compounds are useful as nondigestible substitutes for solid fats in foods.

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.