Abstract: Disclosed is a method of chlorinating a carbohydrate or derivative thereof, for example, a sucrose-6-ester at the 4,1?, and 6? positions, with irreversible removal of HCl formed during the reaction to form the chlorinated carbohydrate or derivative thereof, for example, a 4,1?,6?-trichloro-4,1?,6?-trideoxy-6-O-ester of galactosucrose (TGS-6E). The irreversible removal of HCl can be carried out by an irreversible physical process and/or an irreversible chemical process. Sucralose, an artificial sweetener, can be prepared by deesterification of the TGS-6E. The chlorination reaction takes place at low temperatures and the desired chlorinated product is obtained in high yields and in high purities.

Abstract: The invention provides methods and compositions for the inhibition of fucosylation of proteins, including antibodies, in vivo by administration of a fucose analog.

Abstract: There is provided an improved method for the recovery of residual, unseparated ?-ACF from reaction mixtures remaining from an initial synthesis of ACF, which is in particular usable on a large industrial scale, more particularly in the production of capecitabine.

Abstract: The invention provides novel compounds and formulations of turmeric oil, fish oil, aspirin and anti-cancer drugs (paclitaxel) having anti-inflammatory, analgesic and/or anti-cancer activity.

Abstract: A dendritic emulsifier for forming an oil-in-water emulsion includes an anhydride-modified phytoglycogen or glycogen-type material. A method of preparing an oil-in-water emulsion includes: (a) combining oil, water, and a dendritic emulsifier; and (b) mixing a combination of the oil, water, and dendritic emulsifier. A method of preparing a dendritic emulsifier includes reacting an anhydride with a phytoglycogen or glycogen-type material in solution, thereby forming an anhydride-modified phytoglycogen or glycogen-type material.

Abstract: The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.

Abstract: The present invention discloses a supercooling promoting agent comprising a tannin for producing practical water which does not freeze. As the tannin, a hydrolyzable tannin such as 2,3,6-tri-O-galloyl-?,?-D-hamamelose, 1,2,6-tri-O-galloyl-?-D-glucose, and a vitrification liquid, each of which contains the supercooling promoting agent are useful as a solution or the like for storing a biological material at low temperature.

Abstract: The present invention is related to methods for lowering peroxide levels in sucrose acetate isobutyrate formulations and to composition used in and formed by such methods.

Abstract: A process for the production of an ester of a non-reducing sugar or sugar derivative comprises reacting the non-reducing sugar or sugar derivative with a triglyceride of a fatty acid or a fatty acid ester of a monohydric alcohol in air, substantially in the absence of a solvent and under heterogeneous reaction conditions in which the sucrose and alkyl ester or triglyceride are present as separate phases, at a temperature in the range of from 110° C. to 140° C., wherein the reaction is conducted in the presence of a potassium soap but in the absence of an alkaline component. The process enables esters of sugars and sugar derivatives to be produced at lower temperatures than hitherto and in a much simpler process.

Abstract: The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs. This invention relates to a method for the production of a broad group of glycosylated drugs, including but not limited to propofol, acetaminophen, and camptothecin carbohydrate derivatives.

Abstract: The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

Abstract: A method of removing a carboxylic acid from a liquid including a tertiary amide solvent includes: A) forming an extraction medium including an acid-extracting tin species and an extraction solvent that is immiscible with the tertiary amide solvent; B) subsequently contacting the liquid with the extraction medium, forming a phase including a de-acidified tertiary amide solvent and a phase including the extraction solvent; and C) removing the phase including the extraction solvent, to afford a liquid including the de-acidified tertiary amide solvent. The acid-extracting tin species is one or more tin species obtainable by reaction of a di(hydrocarbyl)tin oxide with less than one equivalent of a carboxylic acid, tin species obtainable by reaction of a 1,3-diacyloxy-1,1,3,3-tetra-(hydrocarbyl)distannoxane with an aqueous base.

Abstract: The invention provides a method of extracting and isolating certain compounds from tobacco. The resulting isolate can include more than 90% by weight of a given compound and can be used as a flavor component for tobacco material used in smoking articles and smokeless tobacco compositions. Exemplary compounds that may be present in the isolate according to the invention include, but are not limited to, solanone, neophytadiene, megastigmatrienone, ?-damascenone, norsolanadione, cis-abienol, ?-cembratrienediol, ?-cembratrienediol, sucrose esters, and lutein.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of glycolysis, inhibitors of protein glycosylation, anti-virals, and down-regulators of insulin receptor and IGF-1 receptor for the treatment or prevention of inflammatory dermatological diseases or proliferative dermatological diseases.

Abstract: The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.

Abstract: Sugar-acrylic monomers are synthesized to have a carbohydrate moiety linked to an acrylate group. The sugar-acrylic monomers may be polymerized to form polymers, adhesives, hydrogels, and the like. The sugar-acrylic monomers and polymers may be used in tissue engineering, adhesives and sealers, wound healing, and the like.

Abstract: A method for producing an active esterified polysaccharide, the method including: subjecting a carboxy group of a carboxy group-containing polysaccharide and an agent for introducing an electrophilic group, to an esterification reaction, wherein an active esterified polysaccharide is formed; bringing the active esterified polysaccharide into contact with a polyvalent carboxylic acid; and after the active esterified polysaccharide is brought into contact with the polyvalent carboxylic acid, precipitating and collecting the resulting active esterified polysaccharide.

Abstract: The present invention relates to a process for preparing a chemically modified polysaccharide, preferably starch, by using a microdevice. It further relates to the use of a microdevice for the chemical reactions of polysaccharides in heterogeneous mixtures. Examples of chemical modifications are acetylation, oxidation, hydroxypropylation and the like.

Abstract: A novel ketogenic compound is provided having general formula (R(OCH(CH3)CH2C(O))nO)m-A wherein n is a integer between I and 10, m is an integer of 1 to 200,000, A is a monosaccharide, polysaccharide or oligosaccharide residue and R is selected from the group consisting of H, C1-C6 alkyl and acetoacetyl-

Abstract: Ionic liquids and cellulose ester compositions and processes for producing ionic liquids and cellulose esters. Cellulose esters can be produced by esterifying cellulose in a reaction medium comprising one or more ionic liquids. Cellulose esters prepared via the methods of the present invention can be contacted with at least one bleaching agent to produce bleached cellulose esters having a ?E value of less than 30.

Abstract: The invention relates to a vaccine for the treatment of disease caused by Neisseria, the vaccine including one or more immunogenic components for Neisseria serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating Neisseria infections. The immunogens are based on elements of the inner core lipopolysaccharide.

Abstract: The object of the present invention is to provide a novel trehalose compound having a high affinity for an adenosine A3 receptor. The trehalose compound of the present invention is represented by General Formula (1): wherein X and X? represent a hydrogen atom, and the like; Y and Y? independently represent an oxygen atom, and the like; R1 and R2 independently represent a C1-C6 alkyl group; and R3 and R4 independently represent a C3-C6 alkyl group. The trehalose compound of the present invention has a remarkably high affinity for an adenosine A3 receptor.

Abstract: Ionic liquids and cellulose ester compositions and processes for producing ionic liquids and cellulose esters. Cellulose esters can be produced by esterifying cellulose in a reaction medium comprising one or more halide ionic liquids and at least one binary component. Cellulose esters prepared via the methods of the present invention can have a degree of substitution (“DS”) of at least 1.5 and can comprise a plurality of ester substituents, where at least 50 percent of the ester substituents comprise alkyl esters having a carbon chain length of at least 6 carbons.

Abstract: A method of preparing a compound of formula (III): wherein x is from 1 to 6, y is from 1 to 12, z is from 0 to 10, each M and each M? is independently a mycolic acid residue including a ?-hydroxy acid moiety and each S is a monosaccharide unit; the method comprising reacting one or more mycolic acids with one or more saccharide units wherein the hydroxyl group of each ?-hydroxy acid moiety is protected prior to reaction with the one or more saccharide units.

Abstract: A powder of reversed vesicles, which comprises one or more non-ionic surfactants and optionally a lipophilic stabilising factor and a bio-active agent, is provided. The product is prepared by making a dispersion of reversed vesicles in a suitable apolar vehicle, which vehicle is subsequently removed. In admixture with one or more excipients the product can be incorporated in compositions.

Abstract: Disclosed is a novel compound contained in blue rose. This novel compound, which is contained in blue rose, has a chemical structure represented by general formula (I): [wherein R1 is a group as set forth in claim 1; and R2 represents —OH, or R1 and R2 together form —O—]. Also disclosed are a rose plant containing the aforesaid compound, and a part of the same.

Abstract: The invention relates to formulations for the washing and care of human or animal body parts, said formulations containing sorbitan carboxylic acid esters and characterized in that the carboxylic acid part of the sorbitain carboxylic acid ester is derived from a carboxylic acid containing between 6 and 10 carbon atoms and the sorbitan carboxylic acid esters have a hydroxyl count (OH count) of higher than 350. The invention also relates to the use of sorbitan carboxylic acid ester in washing or care formulations.

Abstract: The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

Abstract: The present invention relates to fatty acid esters of polyols or sulfonated fatty acid esters or sulfonated fatty acid amides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)t— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.

Abstract: The present invention relates to esterified polysaccharide osmotics, use of same, processes for synthesis of same as well as compositions containing same.

Abstract: Suggested is an improved process for making polyol esters with improved colour quality by transesterification of polyols or their alkoxylation products with fatty acid alkyl esters, which is characterised in that the reaction is carried out in the presence of a reducing mineral or organic acid as a catalyst selected from the group consisting of (i) sulphuric or sulphonic acids with an oxidation value of sulphur of less than 6 or their salts, and/or (ii) phosphoric or phosphonic acids with an oxidation value of phosphor of less than 5 or their salts.

Abstract: The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.

Abstract: A trehalose compound having high immunopotentiating activity and low toxicity is represented by formula (1). (In the formula, X and X? each represents a phenyl, a naphthyl, R1—CHR1— (wherein R1 and R2 each represents a C7-C21 alkyl group or the like) or the like; and n and n? each independently represents an integer of 0-3). The compound exhibits a high activating effect on macrophages and neutrophils.

Abstract: This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.

Abstract: Method for preparing the disaccharide [?-D-Gldp(1?3)]-?-L-Rhap-YR wherein Y is selected from —O— and —S— and R is selected from the group consisting of: C1-C6 alkyl, C1-C6 alkenyl, aryl, allyl, —CO-alkyl (C1-C6), —CO-alkenyl (C1-C6), —CO-aryl comprising the step of using a mutant of a wild type glycoside hydrolase.

Abstract: Methods for the production of pectin hydrolysis products, the pectin hydrolysis products produced in this manner, as well as their use are described.

Abstract: Provided is a pigment dispersant having excellent pigment dispersibility thus allowing a larger amount of pigments to be blended in various cosmetics, and capability of imparting good sense of use, make-up lasting, odor, and stability over time to the cosmetic. A trehalose fatty acid ester composition prepared by esterifying trehalose with a fatty acid having 8 to 22 carbon atoms, which has a hydroxyl value of 20 to 500, and the total amount of a diester, a triester, a tetraester and a pentaester in the trehalose fatty acid esters of 10 to 100% by area; and a cosmetic including the trehalose fatty acid ester composition.

Abstract: The present invention provides an ophthalmic pharmaceutical composition containing acetylated hyaluronic acid and a pharmacologically acceptable carrier. Preferably, the average molecular weight of the acetylated hyaluronic acid is 10,000 to 1,000,000, and the acetyl group substitution number is from 2.0 to 4.0. In a preferred embodiment, this ophthalmic pharmaceutical composition is used in the treatment or prevention of dry eye, and in an even more preferred embodiment it is a dry-eye instillation.

Abstract: Polysaccharide including carboxyl functional groups. The polysaccharide being chosen from the group of anionic synthetic polysaccharides including 1,6 bonds obtained from neutral polysaccharides of which at least one of a carboxyl functional groups is esterified by a hydrophobic alcohol (-Ah) (residue of a hydrophobic alcohol). The hydrophobic alcohol (Ah) being grafted or bonded to the anionic polysaccharide by a function F (ester function), which results from coupling between the carboxylate function of the anionic polysaccharide and hydroxyl function of the hydrophobic alcohol. Carboxyl functions of anionic polysaccharide, which are not substituted, are in the form of carboxylate of a cation. The polysaccharide including carboxyl functional groups are amphiphilic at neutral pH. It also relates to its use for the preparation of pharmaceutical compositions and the pharmaceutical compositions comprising a polysaccharide and at least one active principle.

Abstract: A process for the production of sucrose-6-ester is disclosed. The process includes, in order, the steps of: (a) providing a first reaction mixture including sucrose, a reaction vehicle, and an organotin-based acylation promoter; (b) removing water from the first reaction mixture to afford a second reaction mixture that is substantially free from water; and (c) adding a carboxylic acid anhydride to the second reaction mixture to afford a third reaction mixture, thereby producing a sucrose-6-ester; wherein: during step (b), the removing of water includes distillation of water with the reaction vehicle using an apparatus supplying a heat flux of from 500 to 25,000 BTU/hrft2 (1577 to 78865 W/m2) selected from the group consisting of wiped film evaporators, agitated thin film evaporators, falling film evaporators and rising film evaporators.

Abstract: A method for the preparation of a sucrose-6-ester is disclosed. In a first step of the method, sucrose in a polar aprotic solvent is reacted with an organotin-based acylation promoter. The water of reaction is removed at a temperature that does not exceed about 80° C. In one aspect, the water is removed by distillation of part of the polar aprotic solvent at reduced pressure. In a second step, a carboxylic acid anhydride is added. In one aspect, the resulting reaction mixture is maintained at a temperature of 10° C. or less for a period of time sufficient to produce a sucrose-6-ester. The sucrose-6-ester can be converted to sucralose.

Abstract: A method is described for providing acute symptomatic relief to a subject with Parkinson's Disease (PD) or other CNS disorders resulting from dopamine deficiency in the brain comprising administering to said subject an amount of a ketogenic material sufficient to produce a ketosis in the subject sufficient to provide therapeutic benefit in such neurological disorders. Preferred materials produce a ketosis is such that the total concentration of acetoacetate and (R)-3-hydroxybutyrate in the blood of the subject is raised to between 0.1 and 30 mM.

Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.

Abstract: A process for preparing a bioabsorbable sheet preparation holding thrombin is provided. A process for preparing a bioabsorbable sheet preparation holding thrombin which comprises immersing a bioabsorbable sheet consisting of polyglycolic acid in a thrombin solution containing thrombin as an active ingredient, glycerol as a softening agent, Tween 80 as a permeating agent, and optionally histidine and trehalose as a stabilizing agent followed by drying to hold thrombin on said bioabsorbable sheet, and a bioabsorbable sheet preparation holding thrombin prepared by said process.

Abstract: Novel ester derivatives of ascorbic acid and 2-keto-acid saccharides are provided wherein the ester is introduced by ester bond formation between at least one hydroxy-functionality on the ascorbic acid or 2-keto-acid saccharide and a carboxy-functional organosiloxane, or between a 2-keto-gulonic acid and a hydroxy-functional organosiloxane, as well as methods for their synthesis. Treatment, cosmetic, and personal care formulations comprising the novel esters are also provided, including controlled release forms thereof.

Abstract: A highly pure asiaticoside and a pharmaceutical grade asiatic acid can be prepared, along with salts of asiatic acid, for use in formulating therapeutic compositions that are suitable for treating arthritis, psoriasis and other inflammatory diseases, as well as pulmonary fibrosis, diabetic nephropathy, and other fibrotic diseases.

Abstract: Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): —OX—Y (Ia) or —O—R1 (Ib) wherein X is C(O), S(O) or SO2; Y is NR1R2 or R3; R1 is C1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R2 is H or C1-6 alkyl; and R3 is C1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.

Abstract: To provide safe and easy means for preventing or treating diseases of birds and mammals, in particular, livestock. In particular, to provide means for preventing or treating an infectious disease caused by a Gram-positive bacterium. In addition, to improve fermentation in the rumen of a ruminant animal, to contribute to suppression of the generation of greenhouse gas, and to increase the feed efficiency. Mannosylerythritol lipids (MEL) and/or rhamnolipids are given to birds or mammals.

Abstract: An O-acyl product derived from glucose which may be obtained by partial or total esterification of glucose and of vitamin F, comprising a mixture of esters, for example, monoesters, of glucose and of at least one acid chosen from linoleic acid, oleic acid, palmitic acid and stearic acid, compositions, for example, cosmetic and pharmaceutical compositions, comprising this novel derivative, and their use for improving the condition of head hair and/or other hairs, and, for example, for reducing and/or impeding the loss of head hair and/or other hairs, and/or for inducing and/or stimulating hair growth, as well as a process for preparing O-acyl derivatives mainly in position 6 of glucose, comprising preparing a mixed anhydride by reacting a carboxylic acid with a trimethylacetyl halide, followed by reacting said mixed anhydride formed with glucose.

Abstract: Preparation of chlorinating reagent or chlorination reaction itself for use in a reaction such as production of high intensity sweetener trichlorogalactosucrose (TGS) from partially protected sucrose, comprising reaction of dimethylformamide (DMF) with thionyl chloride or another sulphur containing inorganic acid chlorides including sulphuryl chloride is faced with a problem of prolific release of gaseous by-products, that at times may lead to violent explosion also. This problem is solved by innovative addition of solid powder inert to the constituents of the chlorination reaction mixture to the reaction, or by adding DMF to acid chloride solution in that order. The invention also leads to use of isolated solid Vilsmeier reagent being used for chlorination in a solvent other than DMF making it possible to avoid altogether problems arising from use of DMF which include irrecoverable loss in alkaline as well as acid conditions, interference in crystallization of TGS and the like.