Abstract: There is disclosed a process for recovering sucralose-6-ester from a feed mixture of 6-O-acyl-4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose in a reaction medium comprising a tertiary amide (such as N,N-dimethylformamide), wherein said process comprises removing a major proportion of said tertiary amide by steam distillation. In preferred aspects of the invention, the steam distillation is followed by extraction and then purification by crystallization or crystal aging to recover sucralose-6-ester in good yield.

Abstract: Graphic laminar sheet material in which a barrier layer separates a base layer and an eradicable layer of color contrasting with the base layer.

Abstract: Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypocholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate, 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.

Abstract: Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.

Abstract: There are provided novel compounds of the formulae I and II: ##STR1## and their physiologically acceptable salts. The compounds according to the present invention and their physiologically acceptable salts exhibit an antiallergic activity and are useful for treating allergic diseases.

Abstract: A method of treating hyperandrogenism in warm-blooded animals comprising administering to warm-blooded animals an antiandro genically effective amount of oenotheine B and a process for the preparation of oenotheine B.

Abstract: The present invention provides N- and O-substituted aminophenol derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, G and L are as hereinbefore defined. The present invention also provides intermediates for the preparation of these aminophenol derivatives of general formula (I), as well as the use of the aminophenol derivatives of general formula (I) for the determination of hydrolases, as well as for the preparation of agents for carrying out determinations of hydrolysis.

Abstract: N-acyl-N,N'-di-lysogangliosides, N'-acyl-N,N'-di-lysogangliosides and N,N'-diacyl-N,N'-di-lysogangliosides, wherein the acyl groups are derived from an aliphatic acid having from 1 to 24 carbon atoms, substituted by one or more polar groups are disclosed. The acyl-di-lysogangliosides of the invention exhibit an inhibiting action on protein kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system. Pharmaceutical compositions and therapeutic utilities for the lysoganglioside derivatives are also disclosed.

Abstract: Ascosteroside, obtainable by cultivation of a strain of Ascotricha amphitricha A.T.C.C. No. 74237, analogs thereof and salts and prodrugs of these compounds. The compounds have antifungal activity for use in a method for treating and preventing a fungal infection. Further, the compounds are useful in a method for inhibiting fungal growth.

Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.

Abstract: 1'-Deoxy-5-ethyl-4'-thio-.beta.-uridine as a compound including its physiologically functional derivatives, pharmaceutical compositions containing it and methods of treating herpes virus infections are described.

Abstract: Foaming shampoo compositions which contain no anionic surfactant and are mild to the skin and eyes are comprised of alkyl polyglycosides, betaines, and polymeric slip agents.

Abstract: Thio linked glycosyl compounds are disclosed and synthesized. The synthesis employs a blocked carbohydrate donor and a blocked glycosyl acceptor. The carbohydrate donor includes an acid labile phosphite leaving group attached to the anomeric carbon. The blocked glycosyl acceptor includes an unprotected thio group susceptible to electrophilic attack. The reaction is initiated by the addition of a Lewis acid so as to activate the acid labile phosphite leaving group on the carbohydrate donor. The substitution reaction may be conducted at -78.degree. C. in a solvent such as Et.sub.3 N which favors the formation of thio linked glycosylation products.

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)-Gal-.beta.(1)-(--X--).sub.m -(--Y--).sub.n -).sub.p -ZwhereinX=a chemical bond or a group capable of linking the 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.(2-3)-Gal-.beta.(1)-AwhereinA=a group capable of bonding to the galactose;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C.

Abstract: This invention relates to a pharmaceutical laxative composition in unit dosage form, for peroral administration of sennosides to a human or other animal subject, comprising a safe and effective amount of sennosides in a rapidly dissolving matrix; and a proximal colonic delivery carrier which effects release of said sennosides substantially near the junction between the small intestine and the colon or within the colon of said subject. This invention also involves methods for providing laxation for humans and other animals in need thereof by peroral administration of such compositions.

Abstract: The invention relates to 3-deoxy oligosaccharides of formula I: ##STR1## in which X represents an --OSO.sub.3.sup.- radical, a radical of formula R--O, a radical of formula: ##STR2## or a radical of formula: ##STR3## Y represents a radical of formula: ##STR4## R represents an alkyl radical, R.sub.1, R.sub.3, R.sub.5, R.sub.7, R.sub.8, R.sub.10, R.sub.12 and R.sub.13 represent a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical,R.sub.2, R.sub.4, R.sub.6, R.sub.9 and R.sub.11 represent a hydrogen atom, a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical, with the proviso that at least R.sub.2 or R.sub.4 or R.sub.6 or R.sub.9 or R.sub.11 represents a hydrogen atom,and their pharmaceutically acceptable salts with a base.

Abstract: Cereal grains are ground, slurried in water below the starch gelatinization temperature. Bran, starch granules and protein are removed. .beta.-Glucan is precipitated and dehydrated with alcohol, screened and ground to become a white-colored product with a neutral flavor. The method recovers from 33 to 75 percent of the total natural occurring .beta.-glucan in cereal grains. The .beta.-glucan product is water soluble with purity ranging from 60-90 percent and exhibiting molecular weight of .beta.-glucan ranging from 4.times.10.sup.5 daltons to 2.times.10.sup.6 daltons.

Abstract: The present invention relates to compounds represented by the following formula (I) ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent a hydrogen atom or an acetyl or benzyl group, R.sup.6 represents a hydrogen atom, a hydroxyl, acetoxy, or benzyloxy group, R.sup.7 represents a hydrogen atom, or R.sup.6 and R.sup.7 together my represent another direct bond, and R.sup.8 represents a carboxyl, methoxycarbonyl, hydroxymethyl, or acetoxymethyl group) or salts thereof and a process for the preparation thereof, as well as their utilities in a method for culture, a method for the growth inhibition of moyashi roots, and a method for the growth promotion of moyashi hypocotyls.

Abstract: This invention relates to sulfonates of .beta.-cyclodextrin polymer having a sulfur content of 10% or more, which inhibit propagation of smooth muscle cells.

Abstract: Functionalized monomers are presented which can be used in the fabrication of molecular films for controlling adhesion, detection of receptor-ligand binding and enzymatic reactions; new coatings for lithography; and for semiconductor materials. The monomers are a combination of a ligand, a linker, optionally including a polymerizable group, and a surface attachment group. The processes and an apparatus for making films from these monomers, as well as methods of using the films are also provided.

Abstract: A chiral, bidentate organophosphorus ligand containing a dideoxysaccharide used along with zero valent nickel as a catalyst for enantioselective hydrocyanation. The preferred organophosphorus ligand species is phenyl 2,3-bis-O-(3,5-bis(trifluoromethyl)phenyl)phosphine-4,6-O-benzylidene-B-D- glucopyranoside.

Abstract: The present invention relates to methods for the treatment of prevention of osteoporosis by the administration of a vitamin D glycoside or vitamin D orthoester glycoside, or an analog thereof.

Abstract: 2-O-.alpha.-D-Glucopyranosyl-L-ascrobic acid is crystallizable in its supersaturated solution. Crystalline 2-O-.alpha.-D-glucopyranosyl-L-ascorbic acid is substantially nonhygroscopic, free flowing, free of deliquescence, consolidation and direct reducing activity, but is readily soluble in water. Because of these characteristics, crystalline 2-O-.alpha.-D-glucopyranosyl-L-ascorbic acid is handleable with an ease, and superiorly high in stability and physiological activities. Thus, crystalline 2-O-.alpha.-D-glucopyranosyl-L-acorbic acid is favorably useful in vitamin C-enriching agents, foodstuffs, pharmaceuticals and cosmetics.

Abstract: Stable parenteral antitumor formulations contain elsamitrucin salt, a stabilizer and a buffer. The formations are optionally stored in sealed containers under air or nitrogen headspace.

Abstract: Diterpenes of the formula I ##STR1## in which R.sup.1 is --CH.sub.2 --C(CH.sub.3).dbd.CH--R.sup.3 or --CH.sub.2 --CH(CH.sub.3)--CH.sub.2 --R.sup.3,R.sup.3 is --CH.sub.2 OH, --CHO, --COOH or --COOR.sup.4,R.sup.4 is alkyl having 1 to 5 C atoms,A is ##STR2## and R.sup.2 is H, pentoses, hexoses, di-/oligosaccharides or amino sugars,are suitable for production of medicaments having immunomodulatory action, in particular stimulating T-cells.

Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.

Abstract: The present invention relates to a series of silicone containing glycosides prepared by the reaction of a silanol with a reducing saccharide, or a source of reducing saccharide, in the presence of a suitable catalyst. The invention also relates to the application of these novel compounds in personal care compositions for use on hair and skin.

Abstract: There is disclosed a process for producing sucralose from sucralose-6-ester whereby the sucralose-6-ester is deacylated directly either prior to or after removal of the tertiary amide reaction vehicle from the neutralized chlorination reaction mixture, to produce an aqueous solution of sucralose plus salts and impurities, from which sucralose is recovered by extraction and is then preferably purified by crystallization.

Abstract: Oligosaccharide aromatic glycoside sulfates and physiologically acceptable salts thereof, are disclosed. Further, antiviral agents having these sulfate compounds as the active components, and particularly an antiviral agent, wherein the virus is one which causes AIDS (Acquired Immune Deficiency Syndrome), are disclosed. The active components or the glycoside sulfates, and the salts thereof, are characterized by an oligosaccharide aromatic glycoside sulfate in which the hydrogen of the position-1 hydroxyl group of the terminal sugar of an oligosaccharide is substituted with a specified formula having an alkyl group consisting of 1 to 18 carbons, an oxygen or no oxygen, and an allylene group. The number of constituent monosaccharides in the oligosaccharide portion is preferably within a range of 2 to 20. Further, 10% or more of the remaining hydroxyl groups of the sugar subunits are subjected to sulfated esterification.

Abstract: A polysaccharide substance having the following formula is provided: ##STR1## Also provided is a method of producing the polysaccharide substance in which an oligosaccharide having a degree of polymerization from 3 to 10 is chemically bonded to a silane agent at the reducing terminal of the resultant oligosaccharide, the oligosaccharide compound is then polymerized to an average degree of polymerization from 11 to 500 in the presence of an enzyme. Another method for producing the polysaccharide substance is provided in which an aldehyde group at the reducing terminal of an oligosaccharide having a degree of polymerization from 3 to 10 is oxidized with an oxidizing agent, and the saccharide chain of the oxidized product is polymerized to a degree of polymerization from 11 to 500 in the presence of an enzyme, followed by the addition of an acid. The polysaccharide substance has excellent solvent resistance and is useful as a separating agent for chromatography, especially for the separation of chiral compounds.

Abstract: Hair treatment compositions containing (a) an alkyl polyglycoside of the formula IR.sup.1 O--[G].sub.p (I)wherein R.sup.1 is an alkyl or alkenyl radical having from 6 to 22 carbon atoms, G is a sugar unit having 5 or 6 carbon atoms and p is a number from 1 to 10; (b) a protein hydrolyzate having an average molecular weight in the range from 500 to 10,000 and, (c) a monomeric cationic surfactant provide hair with hold, body, stylability, strength and bounce.

Abstract: A process for differentially determining .alpha.-amylase isoenzyme activities by the inhibitor method, in which 6.sup.3 -deoxymaltotriose (DOG3) represented by the formula ##STR1## is used as an inhibitor.

Abstract: Shaped hydrogel articles such as soft contact lenses are prepared by the steps of:(1) molding or casting a polymerization mixture comprising:(a) a monomer mixture comprising a major proportion of one or more hydrophilic monomers such as 2-hydroxyethyl methacrylate, and one or more cross-linking monomers; and(b) an inert, displaceable diluent selected from the group consisting of:(i) ethoxylated alkyl glucoside;(ii) ethoxylated bisphenol A;(iii) polyethylene glycol;(iv) mixture of propoxylated and ethoxylated alkyl glucoside;(v) single phase mixture of ethoxylated or propoxylated alkyl glucoside and C.sub.2-12 dihydric alcohol;(vi) adduct of .epsilon.-caprolactone and C.sub.2-6 alkanediols and triols;(vii) ethoxylated C.sub.3-6 alkanetriol; and(viii) mixtures of one or more of (i) through (vii),under conditions to polymerize said monomer mixture to produce a shaped gel of a copolymer of said monomers and said diluent; and(2) thereafter replacing said diluent with water.

Abstract: Sulfated oligosaccharides which bind to L-selectin receptors and act as agonists are formulated into pharmaceutical formulations and administered by injection to treat inflammation. Compounds which act as metabolic inhibitors of carbohydrate sulfation and inhibit the sulfation of naturally occurring ligands for L-selectin receptors are administered locally by injection to alleviate and/or prevent inflammation. The sulfated oligosaccharides can be administered in combination with the chlorates and sulfatases in order to obtain a combined effect which is useful in preventing and/or alleviating inflammation. A preferred group of ligands are obtained by the hydrolysis of GlyCAM-1 by separation procedures including high pH anion exchange chromatography. The invention describes compounds that have the recognition determinants for L-selectin on GlyCAM-1 as Galactose-6-sulfate and/or N-acetylglucosamine-6-sulfate, in concert with sialic acid and fucose.

Abstract: N-acyl-N,N'-dilysogangliosides, wherein the acyl groups are derived from unsubstituted aliphatic acids having from 1 to 11 carbon atoms, and N'-acyl-N,N'-dilysogangliosides and N,N'-di-acyl-N,N'-dilysogangliosides, in which the acyl groups are derived from unsubstituted aliphatic acids having from 1 to 24 carbon atoms (with the exception of certain acetyl and diacetyl derivatives). The compounds of the invention exhibit an inhibiting action on protein kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system. Pharmaceutical compositions and therapeutic utilities for the lysoganglioside derivatives are also disclosed.

Abstract: A composition for the enantioselective hydrocyanation of aromatic vinyl compounds comprising zero valent nickel and a chiral, nonracemic, bidentate organophosphorus ligand. The preferred organophosphorus ligand species is phenyl 2,3-bis-O-(3,5-bis(tri-fluoromethyl)phenyl)phosphino-4,6,0-benzilidene-B-D -glucopy-anoside as shown below.

Abstract: Alkyl and/or alkenyl oligoglycosides can be obtained in short reaction times and high yields by a process in which glycose is reacted with fatty alcohols at elevated temperature in the presence of sulfomonocarboxylic acids containing 2 to 8 carbon atoms, carboxylic anhydrides thereof and/or mixed cyclic sulfonic/carboxylic anhydrides thereof as acidic catalysts, the water of reaction is removed and the reaction products are worked up.

Abstract: The invention relates to a process for the removal of alcohols containing up to 30 and, more particularly, between 8 and 18 carbon atoms by distillation from a mixture of alkyl glycosides and alcohols remaining unreacted in the production of these alkyl glycosides, the alcohols being removed in two stages, a falling-film evaporator being used in the first stage and a thin-layer evaporator being used in the second stage.

Abstract: Certain new phenone derivatives of the formula (I) ##STR1## in which R.sup.1 =CH.sub.3,R.sup.2 =H, Cl, Br, I, methyl, hydroxy, methoxy, propoxy, propoxy or ethoxy;R.sup.3 =H or .beta.-D-glykosyl;R.sup.4 =H, Cl, Br, I, methyl, hydroxy, methoxy, propoxy, iso-propoxy or ethoxy;R.sup.5 =H or hydroxy,and the pharmaceutically acceptable salts, ethers and esters thereof, with the exception of the compounds 4-hydroxyacetophenone, 4-hydroxy-3-methoxy-acetophenone, 4-glucopyranosyloxy-acetophenone, 4-glucopyranosyloxy-3-methoxyacetophenone, 4-galactopyranosyloxy-3-methoxy-acetophenone, 4-glucopyranosyloxy-3,5-dimethoxy-acetophenone and galactopyranosyloxy-3,5-dimethoxy-acetophenone and a method for manufacturing them and pharmaceutical preparations containing them. The invention also concerns pharmaceutical preparations containing at least one compound of the formula (II) ##STR2## in which R.sup.1 denotes H, OH, alkoxy or C.sub.1-8 alkyl;R.sup.2 denotes H or C.sub.1-4 alkoxy;R.sup.3 denotes OH or a .beta.

Abstract: There are disclosed novel compounds which are derived from 22,23-dihydro avermectin B1 aglycone. The compounds are both isomers of the 27-hydroxy adduct of the substrate avermectin compound that have been glycosylated at the 4" position to yield 4"-O-glucosyl 27-OH avermectin compounds. The compounds and the intermediates used to make them are highly potent antiparasitic, insecticidal and anthelmintic avermectin agents.

Abstract: A method for orally inducing and enhancing the absorption of calcium into mammalian bone tissue comprises the administration of an effective dose of a flavonol aglycone glycoside in combination with nutritional calcium. Various herbal sources are shown. Potassium gluconate may be added to the system as an adjuvant.

Abstract: A substantially purified arabinogalactan, its degradative products and selected modifications thereof have been found to act as carriers for delivering therapeutic agent to cell receptors capable of receptor mediated endocytosis (RME). The arabinogalactan and its degrative products once derivatived are capable of forming a complex between the therapeutic agent and the polysaccharide such that the complex retains the ability to recognize and bind to the RME receptor.

Abstract: Light-colored alkyl or alkenyl oligoglucosides are obtained by a process in which glucose or aqueous starch degradation products are reacted with fatty alcohols in the presence of acidic catalysts which are obtained by partial sulfation of C.sub.4-22 fatty alcohols.

Abstract: This invention provides a novel chromanol glycoside which is a water soluble antioxidant excellent in heat and pH stability and production method thereof. It is a chromanol glycoside represented by the general formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 independently are a hydrogen atom or a lower alkyl group, R.sup.5 is a hydrogen atom, a lower alkyl group, or a lower acyl group, X is a monosaccharide residue or an oligosaccharide residue, providing the hydrogen atom of the hydroxyl group of saccharide residue may be substituted by a lower alkyl group or a lower acyl group, n is an integer in the range of 0 to 4, and m is an integer in the range of 1 to 6.

Abstract: 2',3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X.dbd.H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases. The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose is useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides. Other intermediates include the 4-thio-2,3-dideoxyribofuranose having different hydroxyl protecting groups and leaving groups.

Abstract: The present invention relates to a method of protecting the hemiacetal or acetal group at the anomeric carbon of a saccharide molecule comprising forming a 4-alkenyl glycoside or 4-alkenoyl glycosyl ester. The invention also relates to use of 4-alkenyl glycosides and 4-alkenoyl glycosyl esters in carbohydrate chemistry, including in the synthesis of oligosaccharides.

Abstract: An immunoactive composition comprising particles containing inulin or an inulin derivative in the gamma polymorphic form, an antigen-binding carrier material and optionally an immune modulator such as an antigenic materials or a cytokine. The compositions provide methods for enhancing immune responses. A process for preparation of the compositions is also considered.

Abstract: Tumor coils which have both saccharidase and tyrosinase activity are selectively treated by administration of a conjugate of a cytotoxic compound which is a substrate for tyrosinase and at least one saccharide or a pharmaceutically acceptable salt or ester thereof. Among the cytotoxic phenolic compounds which are substrates for tyrosinase which can be used are 4-hydroxyanisole, butylated hydroxyanisole, L-3,4-dihydrophenylalanine, dopamine, tertbutylcatechol, hydroquinone, resorcinol, 6-hydroxydopa, and methyl gallate. The efficacy of the treatment is enhanced by also administering a compound that inhibits the action of glutathione reductase.

Abstract: The present invention provides a process for the specific determination of pancreatic .alpha.-amylase in the presence of salivary .alpha.-amylase in body fluids by reaction with a system for the detection of .alpha.-amylase with the use of an inhibitor for salivary .alpha.-amylase, wherein, as substrate, there is used a compound of the general formula:-- ##STR1## in which R.sub.1 is a straight-chained or branched alkyl or alkoyl radical containing up to 6 carbon atoms, a cycloalkyl or cycloalkoxyl radical containing 3 to 6 carbon atoms or a benzoyl, benzyl or phenyl radical which is optionally hydrophilically substituted, R.sub.2 is a hydrogen atom or in which R.sub.1 and R.sub.2 together form a methylene bridge, the hydrogen atoms of which, independently of one another, can each be substituted by an alkyl radical containing up to 5 carbon atoms or a phenyl radical, n is 1, 2 or 3 and X is an optically determinable residue.

Abstract: An oligosaccharide lipid is provided which has 2 to 20 saccharide units, and has a hydrophobic group linked by an ether linkage to an anomer carbon on a reducing end group. A stabilizer for a phospholipid vesicle is also provided which comprises an oligosaccharide derivative having 2 to 20 saccharide units, and having a hydrophobic group linked by an amide linkage or an ether linkage to an anomer carbon on a reducing end group constituted of an aldose.