Abstract: An unusal cytostatic (PS ED.sub.50 4 ug/ml) lignan ester has been isolated from the Central American tree Phyllanthus acuminatus and is herein designated Phyllanthostatin A. Separation of a methanol extract of the root by size exclusion chromatography, high speed countercurrent distribution and semi-preparative hplc afforded glycoside in 0.007% yield. In solution, phyllanthostatin A was slowly transformed into justicidin-B.

Abstract: The present invention provides novel dihydrate crystals of etoposide-2-dimethylamino compound hydrochloride [4'-demethylepipodophillotoxin 9-(4,6-O-ethylidene-2-dimethylamino-2-deoxy-.beta.-D-glucopyranoside hydrochloride] used as a carcinostatic agent and a process for production thereof.

Abstract: Processes for producing antibacterial and antitumor agents designated LL-E33288.epsilon.I and LL-E33288.epsilon.-Br using triphenylphosphine or a sulfhydryl-containing reagent are disclosed. Processes for producing reductively aromatized derivatives of other antibiotics are also disclosed.

Abstract: Glycoside products are successfully prepared directly from aqueous saccharide solutions or syrups, and with acceptably low levels of undesired homopolymerized saccharide by-products, by dissolving same in the desired alcohol reactant or in an alcohol reactant plus glycoside product mixture and contacting the resulting homogeneous aqueous saccharide solution and alcohol-containing reaction medium with an acid catalyst in a fashion such that no separate or distinct, substantially alcohol reactant-free aqueous saccharide solution-containing phase is permitted to come into contact with said acid catalyst material under conditions conductive to homopolymerization of said saccharide reactant.

Abstract: Derivatives of -.alpha.,D-glucofuranose .alpha.,D-allanfuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as psoriasis, atopic dermatitus, rheumatoid arthritis, osterarthritis, scleroderma and systemic lupus erythematosus.

Abstract: The present invention relates to sulfated oligosaccharides or their derivatives such as the following compound and being useful for diagnosing or treating diseases such as immunity-related diseases and mucopolysaccharide diseases. ##STR1## (M is an alkali metal).

Abstract: The present invention relates to sialic acid derivatives. According to the present invention, there is provided sialic acid derivatives having the general formula (I): ##STR1## wherein, R.sup.1 represents hydrogen, an acetyl group, a trityl group, ##STR2## (R.sup.5 represents hydrogen or an acetyl group and R.sup.6 represents hydrogen, sodium or a methyl group).R.sup.2 represents hydrogen or an acetyl group,one of R.sup.3 and R.sup.4 represents ##STR3## (R.sup.7 represents a hydrogen atom or an acetyl group, R.sup.8 represents a hydrogen atom, an acetyl group or a benzyl group, R.sup.9 represents a hydrogen atom, an acetyl group, a benzyl group or ##STR4## wherein R.sup.10 represents a hydrogen atom or a benzoyl group), while the other represents --COOR.sup.11 wherein R.sup.11 represents hydrogen, sodium, or a methyl group.

Abstract: The invention relates to derivatives with a uronic acid structure having substituents selected among a reactive group, a functionalisable group and --OH functions blocked by protective groups. These derivatives are useful for preparing glycosides, particularly enzyme substrates.

Abstract: A process for the ion exchange of polyols for catalyst removal wherein said catalyst is an alkali hydroxide or alkoxide comprising the sequential steps of:(a) mixing the polyether molecule having a molecular weight of 500-10,000 with water,(b) blending into the product of (a) a sufficient amount of a lower aliphatic alcohol to break the emulsion formed in step (a),(c) passing the product of step (b) through a macroporous cation exchange resin to obtain a purified polyether molecule, methanol, and water.The product of (c) may be further subjected to stripping to produce the purified polyether polyols.

Abstract: Compounds having a polyhydroxylated hydrophilic moiety, a highly fluorinated moiety and a functional junction group linking said moieties together, wherein said hydrophilic moiety is derived from a polyol or an aminopolyol, and wherein said highly fluorinated moiety consists of a fluorocarbon group wherein at lest 50% of the atoms bonded to the carbon skeleton are fluorine atoms, the other atoms bonded to the carbon skeleton being hydrogen, chlorine or bromine atoms, said highly fluorinated moiety containing at least 4 fluorine atoms; as well as the internal ethers and ketals thereof; process for their preparation; and a compositions containing said compounds as surfactants, together with non polar compounds, for use as gas carriers.

Abstract: The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have antibacterial and antiviral activity.

Abstract: An external skin care preparation comprising a compound represented by the following general formula (I) or (II), or a salt thereof: ##STR1## wherein R.sup.1 means an aliphatic hydrocarbon group having 9-25 carbon atoms, A and B denote specific groups respectively, R.sup.6 and R.sup.7 are individually an aliphatic hydrocarbon group having 10-26 carbon atoms, and R.sup.8 denotes a group --CH.sub.2 CH.sub.2 OH, --CH.sub.2 COOH or --COCH.sub.3.

Abstract: A process and intermediates useful for the invrsion of 2-deoxy-2,2-difluororibose analogs to provide 2-deoxy-2,2-difluoroxylose analogs is described.

Abstract: Novel mannobiose derivative represented by the general formula [I]: ##STR1## wherein groups of R.sub.1 to R.sub.5 each represents --OH, --OR.sub.6, --NHR.sub.6, (R.sub.6 represents an acyl group) or a group represented by the following formula (a), (b), (c), (d) or (e), provided that one of R.sub.1 to R.sub.5 represents --OR.sub.6 or --NHR.sub.6, one of the other 4 groups of R.sub.1 to R.sub.5 represents one of the groups represented by the formulae (a) to (e), and the remaining 3 groups of R.sub.1 to R.sub.5 represent --OH: ##STR2## wherein represents .alpha. or .beta. bond are provided by the invention.These compounds give liposomes a specific affinity for Kupffer cells of liver, and can be produced industrially.

Abstract: A method of preparing C-5 substituted nucleotides by reacting a C-5 posit mercurated nucleoside with an alkyl or aryl disulfide in the presence of palladium(II) ion. The resulting new method for attaching linker arms to nucleic acids (DNA,RNA) provides a wide ranging reaction far more useful than those heretofore developed, and allows preparation of modified components with linking reactive functionality that allows usefulness as probes, therapeutics, and for DNA sequencing.

Abstract: A second-step virus binding receptor is found in nature on the surface of animal and plant cells. This receptor is thought to be needed for virus penetration into target cells. The second-step receptor has been found to bind a wide variety of viruses belonging to a number of different families. The second-step receptor and natural or synthetic substances which correspond to or are analogous to the binding epitope of the second-step receptor in that they are able to bind to a site on the virus which recognizes the binding epitope of the natural second-step receptor, are therefore indicated for the diagnosis, prophylaxis or treatment of viral infections.

Abstract: A process for the chlorination of sucrose-6-esters to produce 6',4,1'-trichlorosucrose-6-esters which comprises the steps of:(a) adding at least seven molar equivalents of an acid chloride to a reaction mixture containing a sucrose-6-ester and a tertiary amide to form initially a chloroformiminium chloride salt which subsequently forms a complex with the hydroxyl groups of the sucrose-6-ester;(b) subjecting the reaction mixture product of step (a) to an elevated temperature not higher than about 85.degree. C. for a period of time sufficient to produce a mixture of chlorinated sucrose-6-ester products consisting essentially of 6'-chlorosucrose-6-ester, 4,6'-dichlorosucrose-6-ester, and 1',6'-dichlorosucrose-6-ester; and(c) subjecting the reaction mixture product of step (b) to an elevated temperature not higher than about 125.degree. C. for a period of time sufficient to produce a chlorinated product consisting essentially of 1',4,6'-trichlorosucrose-6-ester.

Abstract: The invention disclosed provides a method for preparing spherical-like encapsulated aminoglycosides which may be administered orally to a patient, and which retain antibacterial properties without significant degradation stomachically. The present invention also provides spherical-like encapsulated aminoglycosides and a method for introducing aminoglycosides into a patient by oral ingestion without significant degradation of bactericidal properties.

Abstract: Glucose, and separately a 1:1 mixture of glucose and fructose, were thermally polymerized in the presence of glutamic acid to yield artificial carbohydrates with chemical linkages different from starch, cellulose, or chitin.

Abstract: The compounds of the formula I ##STR1## in which R.sub.1 to R.sub.3 denote, independently of one another, hydrogen or a (C.sub.1 -C.sub.18)-acyl group, and a process for the preparation thereof are described. These compounds have tumor-inhibiting properties.

Abstract: A method for preparing particulate saccharides comprises drying a solution containing at least two kinds of saccharides followed by melting the at least two kinds of saccharides, and cooling and pulverizing the saccharides to obtain the particulate saccharides.

Abstract: A fat substitute food composition containing a polysaccharide fatty acid polyester in place of from about 0.5% to about 95% of the total fat content of the food composition is disclosed. The polysaccharide is a polymer of at least three monosaccharides and has at least four fatty acid ester groups, each fatty acid portion having from 4 to 24 carbon atoms.

Abstract: A new glucan derivative having at least one side chain branch of a compound selected from the group consisting of galactopyranose, L-arabinofuranose and oligomers thereof is disclosed. These glucan derivatives have high tumoricidal activity and are usuable as a tumoricide.

Abstract: Phosphates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These phosphates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the phosphates are also disclosed.

Abstract: A method of preparing a composition comprised of a glycoside having a cationic-substituted glycosyl moiety is provided. A cationic starch derivative is reacted with a monohydric alcohol to form cationic-substituted glycosides. Cationic starch derivatives include the tertiary amino, imino, quaternary ammonium or phosphonium, or tertiary sulfonium starch derivatives. Compounds generally characterized as glycosides having cationic-substituted glycosyl moiety are also claimed.

Abstract: A method for extracting and separating an aglycone which constitutes a glycoside, said method comprises steps of:subjecting a material containing the glycoside to hydrolysis to decompose the glycoside into a sugar moiety and an aglycone;extracting the aglycone from the hydrolyzed material by using a fluid at supercritical or subcritical conditions as an extraction agent; andseparating the extracted aglycone from the extraction agent.

Abstract: A process for producing a condensed polysaccharide, which comprises heat-melting at least one compound selected from the group consisting of glucose, mannose, galactose, xylose and arabinose, which contains from 8 to 180 ppm of hydrogen chloride, followed by dehydration condensation under reduced pressure.

Abstract: An aromatic substituted glycoside is disclosed of the formula ##STR1## wherein the configuration of the substituted --OR on the anomeric carbon is alpha, n is an integer of 0 to 1, and R is a substituted aromatic radical selected from the group ##STR2## where R.sub.1 through R.sub.6 are independently halogen, NO.sub.2, SO.sub.3 H, ##STR3## where R.sub.7 is lower alkyl; and includes its stereoisomers, optical isomers and geometric isomers and mixtures of the foregoing isomers. These substrates are useful as direct substrates for alpha-amylases. A process for the preparation of the substrates and related substances is also described.

Abstract: Novel light producing 1,2-dioxetanes are described of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures. The compounds are produced from novel alkenes.

Abstract: The present invention relates to .beta.-D-phenylthioxyloside compounds selected from the group consisting of:(i) the .beta.-D-phenylthioxylosides of the formula: ##STR1## in which: R.sub.1 and R.sub.2, which can be identical or different, which represent a hydrogen atom or a trifluoromethy or cyano group,A represents CHOH or CO andY represents a hydrogen atom or an acyl group; and(ii) epimers thereof when A is CHOH.The said .beta.-D-phenylthioxyloside compounds are useful in therapy as antithrombotics.

Abstract: 6-C.sub.8 to C.sub.22 acyl-1-C.sub.3 to C.sub.12 alkylglucosides are a new group of surface active compounds useful in particular as emulsifiers in cosmetics, pharmaceutical compositions and foodstuffs. They are prepared by reacting a 1-C.sub.3 to C.sub.12 alkyl glucoside with a C.sub.8 to C.sub.22 fatty acid in the presence of a lipolytic enzyme and in a reaction medium containing at most 30% and preferably 0.01 to 5% water.

Abstract: This invention provides a method of inhibiting osmotic water flow across mammalian cell membranes which involves contacting the water channels of the cell membranes with an effective amount of a glucose transport blocker or of digitonin so as to inhibit osmotic water flow across the membranes.Additionally, this invention provides a method of treating a subject afflicted with a condition associated with abnormal osmotic water flow across cell membranes which comprises administering to the subject an effective amount of a glucose transport blocker or of digitonin so as to contact the water channels of the subject's cell membranes and inhibit osmotic water flow across the membranes.

Abstract: Glycoside products having a propensity to discolor (i.e., darken) under aqueous alkaline conditions are stabilized against discoloration under such conditions by treatment with from about 0.01 to about 2 weight percent (glycoside product dry weight basis) of a borohydride material such as sodium borohydride, potassium borohydride, lithium borohydride, etc.

Abstract: A process is described for extracting a pharmaceutically active polysaccharidic substance from the aloe plant.The pharmaceutically active polysaccharidic substance and its characteristic properties are described.

Abstract: Novel nonionic perfluoroalkylthioglycosides of the formula, R.sub.f -E-S-saccharide are described, wherein R.sub.f is a straight or branched chain perfluoroalkyl of 1 to 18 carbon atoms or said perfluoroalkyl substituted by perfluoroalkoxy of 2 to 6 carbon atoms, E is a connecting group, and the saccharide is a mono-, di-, or higher oligosaccharide, comprising 1 to 30 units of 5, 6 or 7 carbon-membered sugars.

Abstract: A process for preparing gamma inulin comprising the steps of (a) recrystallizing crude inulin from water at a temperature below 37.degree. C. to obtain a suspension, (b) heating the suspension at a temperature of from about 25.degree. to 45.degree. C. for about 1-3 days, (c) further heating the suspension at a temperature of about 40.degree. to 55.degree. C. for about 0.5 to 1.5 hours, and (d) isolating insoluble gamma inulin from the suspension. A composition comprising particles of inulin or an inulin derivative in the gamma polymorphic form is characterized in that the particles have a low rate of solution in aqueous media above 30.degree. C., particularly above 37.degree. C. The composition is effective as the active component of an immunotherapeutic preparation for activation of the alternative pathway of complement, or for antitumor treatment.

Abstract: Chemiluminescent 1,2-dioxetane compounds are disclosed in which the molecule is stabilized at the 3-position on the dioxetane ring against decomposition prior to the molecule's coming in contact with a labile group-removing substance (e.g., an enzyme that will cleave the labile group to cause the molecule to decompose to form at least one light-emitting fluorophore) and substituted at the 4-position on the dioxetane ring with a fused polycyclic ring-containing fluorophore moiety bearing a labile ring substituent whose point of attachment to the fused polycyclic ring, in relation to this ring's point(s) of attachment to the dioxetane ring, is such that the total number of ring atoms separating these points of attachment, including the ring atoms at the points of attachment, is an odd whole number. These odd pattern substituted compounds decompose to emit light of greater intensity and of a different wavelength than that emitted by the corresponding even pattern substituted isomers.

Abstract: Hydrolyzable substrates comprise blocked moieties which, when cleaved from the substrate during hydrolysis, provide electron transfer agents. The released electron transfer agents can be recycled between a reductant and a reducible compound that upon reduction provides a detectable species. Alternatively, they can be recycled between an oxidant and an oxidizable compound that upon oxidation provides a detectable species. These substrates are useful in analytical compositions, elements and methods for the determination of hydrolytic analytes, such as hydrolytic enzymes or biological cells containing such enzymes.

Abstract: A new depressant composition is provided for the enhanced separation into separate value metal concentrates of copper, nickel, zinc, lead present in polymetallic and massive sulphide ores.The depressant is added in an aqueous solution prepared by dissolving first a mixture of quebrachio and dextrin, or quebracho and guar gum. To the solution of modified quebracho a water soluble salt of lignin sulphonate is added. The aqueous polymer of modified quebracho lignin sulphonate is further mixed with one or more of the following inorganic reagents: water soluble cyanide, metal sulphates and water soluble sulphites. The resulting depressant is added together with conventional flotation reagents in conventional mineral separation stages as required.

Abstract: Sucrose is reacted with a 1,3-di(hydrocarbyloxy)-1,1,3,3-tetra(hydrocarbyl)distannoxane to produce a 1,3-di-(6-O-sucrose)-1,1,3,3-tetra(hydrocarbyl)distannoxane, which can be acylated to produce a sucross-6-ester.

Abstract: A process for preparing alkylglycosides by reacting an 8 to 20 carbon atom monohydric alcohol with a monosaccharide in the presence of an acid catalyst, while under partial vacuum, followed by neutralizing the reactant product with an alkaline metal hydroxide in an amount about equal on a molar basis to the amount of catalyst, and removal of the residual unreacted alcohol.

Abstract: Process for the depolymerization and sulfation of polysaccharides by reaction of said polysaccharides with a sulfuric acid/chlorosulfonic acid mixture.

Abstract: Agents and methods for the prevention of metastases of malignant tumors use the monosaccharides which are specific for organ cell lectins and/or glycoconjugates containing these monosaccharides, and more specifically, .beta.-D-galactose and/or glycoconjugates containing terminal .beta.-D-galactose moieties.

Abstract: A glycoside of inositol which has been isolated from a hot-water extract of tea leaves. The glycoside is identified from the analytical results to be 2-O-beta-L-arabinopyranosyl-myo-inositol.

Abstract: Novel processes for synthesizing acid mucopolysaccharide fragments having from 2-12 saccharides and substantially pure products of a single structure produced thereby. Condensation are disclosed between a first protected saccharide and a second protected saccharide to form a protected condensation product having units linked in the manner found in chondroitin sulfate and dermatan sulfate and having protecting groups thereon which allow selective positioning of functional groups, in particular sulfate, at desired positions. Other condensations are disclosed in which a protected condensation product is formed which can be elongated, and has protecting groups thereon which allow selective positioning of functional groups, in particular sulfate, at desired positions. Also disclosed is a process for selectively positioning functional groups on a protected acid mucopolysaccharide having from 2-12 units.

Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## are disclosed.

Abstract: N-demethylefrotomycin, a valuable new antibiotic substance, is produced by the microbial conversion of mocimycin using a novel, efrotomycin-producing, microbial species ATCC 53758.

Abstract: A method for making a water insouble bicompatible gel includes activating HA with an activating agent to form activated HA, and reacting the activated HA with a nucleophile, under conditions producing the water insoluble bicompatible gel. Also, a method for making a water insoluble biocompatible film includes providing a biocompatible gel made according to the above method, and drying the gel or compressing the gel under conditions permitting escape of water from the gel. Also, a water insoluble composition including HA is prepared without the use of any bifunctional or polyfunctional nucleophile.

Abstract: Sialic acid derivatives and process for preparing these compounds. In these compounds, a phenylthio group is stereo-selectively incorporated at the 3-position of the sialic acid. These compounds are useful as intermediates for synthesizing various glycosides such as ganglioside, a blood type determining factor, GQ.sub.1b etc. The present invention also relates to sialic acid-containing oligosaccharide derivatives and process for preparing them.

Abstract: Novel 4'-esters, 4'-carbonates and 4'-carbamates of 4'-demethylepipodophyllotoxin glucosides are disclosed. These agents exhibit antitumor activity in animals.