Abstract: The invention resides in oligosaccharide derivatives which are obtained by the enzynmatic cleavage of carbohydrates linked to proteins through asparagine groups. The oligosaccharide moieties of the instant invention are 1-amino-1-deoxyoligosaccharide compounds which are cleaved from a glycoprotein with an aminohydrolase enzyme, wherein the amino group of the oligosaccharide is subsequently substituted with a fluorescent reporter compound. The compounds of the instant invention are characterized by the glycosylamine bonds exhibiting less than 10% hydrolysis at 25.degree. C. in aqueous solution over a two days at pH values between 4-10.

Abstract: The present invention relates to compounds of the formula I[CH.sub.3 --(CH.sub.2).sub.29 --O--].sub.m --R (I)whereinif m stands for 1, thenR represents a group derived from a mono- or di- or oligosaccharide by removing the hydrogen atom from the hydroxyl group being in the 1(alpha) or 1(beta) position, or the O-protected, preferably acetylated derivative thereof,if m stands for 2, thenR represents a group derived by removing a hydrogen atom attached to the carbon atom being in position 1 of the reaction product of glucose and mono-, di- or triethylene glycol or the O-protected, preferably O-acetylated derivative thereof.

Abstract: The invention relates to N-deacetyl-lysogangliosides and physiologically acceptable salts thereof, especially those of formula (I): ##STR1## wherein R represents --CH.dbd.CH(CH.sub.2)nCH.sub.3 or --CH.sub.2 CH.sub.2 (CH.sub.2)nCH.sub.3 ;n is 12 or 14;R.sup.1 represents ##STR2## or hydrogen; and R.sup.2 represents hydrogen or acetyl; for use in therapy.The compounds are useful as inhibitors of phospholipases A.sub.2, and of superoxide production, as antiproliferative and immunosuppressant agents in the treatment of autoimmune diseases. The invention also relates to the use of N-deacetyl-lysogangliosides for the manufacture of medicaments for the treatment of the aforementioned conditions.

Abstract: The present invention relates to novel tocopheryl oligosaccharides, acylated tocopheryl oligosaccharides, sulfated tocopheryl oligosaccharides, and antiviral agents including the sulfated tocopheryl oligosaccharides as active ingredients. In the tocopheryl oligosaccharide, the hydrogen atom of the hydroxy group at the 1-position in the terminal sugar moiety of an oligosaccharide which consists of 3.about.20 of identical or different repeating monosaccharide units selected from the group consisting of glucose, galactose, mannose, talose, idose, altrose, allose, glucose, xylose, arabinose, rhamnose, fucose, and fructose, which are glycoside-linked, is substituted by a tocopherol group. In the acylated tocopheryl oligosaccharides, each of any hydroxy group of the sugar moiety, other than the hydroxy group at the 1-position in the terminal sugar moiety of the oligosaccharide described above, is protected by an acyl group.

Abstract: The present invention provides a process for preparing asialo G.sub.M1 characterized in that neuraminidase isozyme L is allowed to act on gangliosides to produce asialo G.sub.M1.

Abstract: An alkylated oligosaccharide and the acetyl derivative of the same, both useful as the raw material for producing lowly toxic surfactants or medicines. The alkylated oligosaccharide is prepared by substituting with an alkyl group having a linear or branched chain the hydrogen atom of the hydroxy group at the 1-position of a terminal sugar moiety of an oligosaccharide in which glucose moieties are .beta.(1.fwdarw.3)-glucoside-linked, or of an oligosaccharide in which galactose is .beta.(1.fwdarw.4)-glycoside-linked at the 4-position in the galactose moiety of lactose and in which galactose moieties are .beta.(1.fwdarw.4)-glycoside-linked in succession to the newly formed terminal galactose moieties. The invention also includes an acetyl derivative of the oligosaccharide, wherein the hydroxy groups excluding the 2-positional hydroxy group adjacent to the alkyl-ether-linking position in the terminal sugar moiety are acetylated, and a mixture thereof.

Abstract: O-glycosylation and O-glycosylation extension inhibitors influence selectin-dependent interactions between cells and between cells and platelets.

Abstract: N-acyl-N,N'-di-lysogangliosides, N'-acyl-N,N'-di-lysogangliosides and N,N'-diacyl-N,N'-di-lysogangliosides, in which the acyl groups are derived from an organic acid of the aliphatic, aromatic, araliphatic, alicyclic or heterocyclic series and in which at least one of the two acyl groups is not aliphatic, and their preparation are disclosed. Also disclosed is the preparation of the esters, inner esters, amides and hydroxy peracylates of these compounds and salts thereof. These compounds are useful in the treatment of pathologies of the central and peripheral nervous systems.

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, Gluc is a glucose molecule, n is 1, 2 or 3 and X is an optically determinable residue.

Abstract: The present invention relates to stabilizing agents for enzymes which comprises an enzyme stabilizing amount of an N-substituted moranoline derivative of the formula (III): ##STR1## wherein R.sup.1 is phenyl lower alkynyl, phenoxy lower alkenyl or phenoxy lower alkynyl, wherein the phenyl moiety is unsubstituted, or a glucose oligomer thereof.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R is a trifluoromethyl radical or a cyano group. The present invention also provides processes for the preparation of these compounds, as well as reagents containing them. The present invention is also concerned with the use of these compounds as .beta.-galactosidase substrates, especially in a CEDIA system.

Abstract: Heptasaccharides containing bivalent receptor determinants for the influenza virus of human isolates which inhibit binding of the virus to host cells as well as other saccharides used in preparation of the heptasaccharides are provided.

Abstract: 5-O-.alpha.-D-Glucopyranosyl-L-ascorbic acid is a novel derivative of L-ascorbic acid which has a direct reducing activity and a satisfiable stability, as well as being readily hydrolyzed in vivo to form L-ascorbic acid. The 5-O-.alpha.-D-glucopyranosyl-L-ascorbic acid is prepared by allowing a saccharide-transferring enzyme together with or without .alpha.-glucosidase to a solution containing an .alpha.-glucosyl saccharide and L-ascorbic acid, and suitably used in food products, agents of anti-susceptive diseases and cosmetics containing thereof.

Abstract: Incubation of 13.beta.-hydroxy ivermectin aglycone with a species of Bacillus subtilis or the incubation of 13-deoxy ivermectin aglycone with a mixed culture of a species of Bacillus subtilis and of Streptomyces griseus results in the production of 13-.beta. ivermectin monoglucopyranoside as the major product and of 5-.beta. ivermectin monoglucopyranoside as the minor product.

Abstract: The invention relates to alkylglycoside sulfosuccinates of the general formula (1) defined herein, useful in cosmetic preparations.

Abstract: Sialic acid- containing glycolipid derivatives represented by the following general formula, their production method, and the particulate carriers that contain as a constituent the sialic acid-containing glycolipid derivative(s). ##STR1## wherein represents the .alpha.- or the .beta.- linkage, R.sup.1, a hydrogen atom or an acetyl group,R.sup.2, a hydrogen atom, a lower alkyl group with 1-4 carbon atoms, an alkaline metal ion, or such,X, an oxygen or sulfur atom or a residue represented by the following formula (II) or (III),--O(CH.sub.2).sub.m NHCO-- (II)where m represents an integer from 1 to 10.--O(CH.sub.2).sub.m CONH-- (III)Y, the formula (IV). ##STR2## where A represents a linear or branched chain acylamino group with 10-40 carbon atoms, or such B, a hydrogen atom, a carboxyl group or such, or the formula (V), and ##STR3## n, an integer of 0 to 3.

Abstract: A process for obtaining polymers with antiviral activity is disclosed. Molecules carrying carbonyl groups and hydroxyl groups in the .alpha. position relative to the carbonyl, and molecules carrying amino and sulfonated groups, react in water or in mixtures of water with water-miscible solvents. The reaction takes place under specific conditions of temperature, time and pH. The first reacting molecule may be a monosaccharide whereas the second reacting molecule may comprise aliphatic aminosulfates. Upon completion of the reaction the polymeric material is purified by conventional processes such that the polymeric material has a molecular weight between 1,500 and 100,000. The polymeric material has antiviral activity, either lacks or has very low toxicity and anticoagulant activity, and is thus suitable for pharmaceutical preparations for use in topical or systemic antiviral therapy in humans or animals.

Abstract: Cyclodextrin derivatives having at least one group selected from among a sulfonic acid group, a sulfonic acid salt group, an ammonium salt group, a phosphoric acid group, a carboxyl group, a carboxylic acid salt group and a hydroxyl group are disclosed. The present invention provides cyclodextrin derivatives having extremely high solubility in water.

Abstract: The metabolism of tumor cells which have .beta.-glucuronidase activity is inhibited by administering to a patient a conjugate of glucuronic acid and a thiocarbamate compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are selected from the group consisting of C.sub.1 -C.sub.6 alkyl and C.sub.1 -C.sub.6 cycloaliphatic, and M is selected from the group consisting of hydrogen, an electropositive, ionically bonded metal, and the radical ##STR2## and R.sup.3 and R.sup.4 are selected from the group consisting of C.sub.1 -C.sub.6 alkyl and C.sub.1 -C.sub.6 cycloaliphatic groups.

Abstract: Sucrosetricarboxylic acid can be prepared by oxidizing sucrose with oxygen, if desired in a mixture with inert gases, by means of a more effective catalyst than platinum/alumina.The product can be used in washing agents or as a food additive.

Abstract: Octyl ethers and octadienyl ethers of glucose, sucrose, are disclosed. Compositions comprised of a mixture of octyl ethers of glucose and sucrose and those containing octadienyl ethers of sugar acids are also disclosed.

Abstract: Polygalactomannans containing a hydroxybutyl ether substituent and a hydrophobic substituent can be used in the fracturing of subterranean formations.

Abstract: An agent for prevention or prophylaxis of general toxic effects or chronic neurotoxic effects which are caused by the administration of antineoplastic agents, which is to be given to patients prior to administration of said antineoplastic agents and which comprises as an active ingredient a mixture of gangliosides GM.sub.1, GD.sub.1a, GD.sub.1b and GT.sub.1b.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO-, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO-, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l 'NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.

Abstract: The present invention relates to non ionic surfactants having the general formula (I): ##STR1## wherein: R.sup.1 is H or CH3R.sup.2 is H or OHR.sup.3 is H or OHR.sup.4 is an alkyl of formula --(CH.sub.2).sub.n --CH.sub.3 wherein n is an integer comprised between 6 and 20It also relates to a process for treatment of proteins containing medium without denaturation of said proteins, using these surfactants.

Abstract: Inclusion complexes of the polyenes apocarotenal and lycopene in a cyclodextrin as well as their manufacture are described. The inclusion complexes are soluble in water, alcohol or water/alcohol mixtures.

Abstract: Heptasaccharides containing bivalent receptor determinants for the influenza virus of human isolates which inhibit binding of the virus to host cells as well as other saccharides used in preparation of the heptasaccharides are provided.

Abstract: Dioxetane compounds reactable with an enzyme to release optically detectable eneregy are disclosed. These compounds have the formula: ##STR1## wherein T is a carboxylic acid or methoxy substituted adamantyl group bound to the ring through a spiro bond, Y is phenoxy or napthyloxy and X is methoxy, ethoxy or propoxy. Z is an enzyme cleavable group such that when cleaved by an enzyme, an electron rich moiety is left bound to the dioxetane ring.

Abstract: 5-(.alpha.-D-glucopyranosyloxymethyl)-furan-2-carboxaldehyde (GMF) is produced from isomaltulose by heating a solution of isomaltulose in a strongly polar aprotic solvent in the presence of an acidic ion-exchanger, either batchwise or by percolation of the solution through a column filled with the ion-exchanger. Novel derivatives of GMF of the formula (I) ##STR1## wherein R' is a hydrogen atom, an acyl group or an alkyl group and X represents --CH.sub.2 OH, --COOH, --C(H).dbd.NOH, --CN, --CH.sub.2 NHR" or --CH.dbd.CR"R'", where R" is a hydrogen atom, an acyl or aryl group or an alkyl group with up to 20 C atoms and R'" is a hydrogen atom, --NO.sub.2, --CN, --COOalkyl or acyl are described, and also their preparation and use for the preparation of surface-active compounds.

Abstract: Lactoneotrehalose, a novel saccharide shown by the formula O-.beta.-D-galactopyranosyl-(1.fwdarw.4)-O-.beta.-D-glucopyranosyl .alpha.-D-glucopyranoside, is prepared by allowing a saccharide-transferring enzyme to act on an aqueous solution containing lactose and amylaceous substance. Lactoneotrehalose is a non-reducing oligosaccharide, extremely stable, readily soluble in water, and substantially free of hygroscopicity, as well as having a satisfiable quality and moderate sweetness. These render lactoneotrehalose very useful in the preparations of orally-administrable products, cosmetics and pharmaceuticals.

Abstract: A process for the preparation of alkyl polyglycosides containing an alkyl group of about 8 to 24 carbon atoms, which comprises glycosylating and transglycosylating one or more saccharides, wherein the glycosylation is carried out in an evaporator at an acid number of about 1 to 10 mg of KOH/g.

Abstract: The present invention provides a dye other than red and purple which is obtained from cultured cells of Euphorbia milli. The present invention also provides cultured cells containing quercetin glucuronide in a large amount, derived from tissues or cells of Euphorbia milli.

Abstract: Antibodies (polyclonal and monoclonal) having specificity for cytokinins having a glycosylated isoprenoid side chain are described. The antibodies simultaneously recognize a purine ring, an isoprenoid side chain, and a 4'-O-glycoside. The antibodies were elicited using a novel hapten, 9-(2-carboxyethyl) cytokinin-O-glycoside. Immunoassay methods for the determination of cytokinins having a glycosylated isoprenoid side chain which utilize the antibodies are also described.

Abstract: The claimed invention relates to a substrate for evaluating glycosidic enzymes comprising a fluorescein derivative of the general formula: ##STR1## wherein GlyX is a carbohydrate bonded to fluorescein by a glycosidic linkage;Y, which may be the same as GlyX or different, is an alkyl ether, an ester, or a glycosidically linked carbohydrate;R is a lipophilic residue containing from 1 to 21 carbon atoms; andL links the R residue to fluorescein.A preferred embodiment of the invention is a non-fluorescent substrate specifically hydrolyzable by a glycosidase inside a cell to yield, after greater than about 2 minutes, a fluorescent detection product excitable at between about 460 nm and 550 nm and with fluorescence observable at an emission wavelength longer than the excitation wavelength, which fluorescent detection product is retained inside a viable cell more than about 2 hours at greater than about 15.degree. C. and which is non-toxic to the cell.

Abstract: Synthetic glycosaminosyl transferase-V acceptors and inhibitors are disclosed. Minimal trisaccharide inhibitors and acceptors specific for GnT-V, which is associated with the ability of cells to metastasize are useful, in diagnosis and treatment of conditions characterized by metastatic cells.

Abstract: Sucrose is treated with an acid catalyst to form an amorphous sucrose anhydrous melt. Heating of the anhydrous melt at 80.degree.-100.degree. C. forms three known kestoses and the novel products, viz. .alpha.-fructosylsucrose anomers of 6-kestose, neokestose, and 1-kestose. Heating of the anhydrous melt at 125.degree.-175.degree. C. produces a fructoglucan sucrose polymer having a molecular weight of about 2,000 to 10,000 Daltons. All of these products are useful as sweeteners, food additives, additives for animal food, and bulking agents.

Abstract: A composition suitable for topical application to human skin comprises, in addition to a suitable vehicle an active ingredient which can control skin barrier functions. The active ingredient is (a) a long chain .omega.-hydroxy fatty acid or a carboxy-substituted derivative, (b) an hydroxy- or epoxy-derivative of an essential fatty acid or an ester formed between (a) and (b). Certain novel compounds of structures (a), (b) and (a)(b) esters are also claimed.

Abstract: There are disclosed processes for the synthesis of substituted and unsubstituted arene diols useful in the further synthesis of sugars, sugar derivatives, chiral synthons or amino acids.

Abstract: Chromogenic merocyanine enzyme substrate compounds of the general formula: ##STR1## where Y is an enzymatically-cleavable group such as a radical of a sugar, carboxylic acid, amino acid, peptide, phosphoric acid, or sulfuric acid; A and B represent residues that complete 5- or 6-membered ring systems; R.sup.1 is substituted or unsubstituted alkyl; R.sup.2 and R.sup.3, independently, are hydrogen or lower alkyl; m, n, and p, which can be different, are integers from 0 through 3 provided that m+n+p must be at least 2; and X is an appropriate counterion (anion).

Abstract: Compounds of the formula (R-COO).sub.n X-OR.sup.1, wherein R.sup.1 is optionally substituted alkyl, phenyl, or alkyl phenyl, n is 1, 2 or 3, X is a carbohydrate moiety, and R is optionally substituted alkyl, have superior effects as additives in detergents. These compounds can be prepared by esterification of glycosides using specific enzymes.

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 usable as a tumoricide.

Abstract: Compounds which are hydrolyzed in vivo to n-butyric acid are esters of butyric acid in which the alcohol group is selected from the group consisting of polyhydric alcohols, cyclic and acyclic aldose or ketose monosaccharides and their acetonides. Of particular interest are O-butanoyl-6-O-ispropylidene-1,2,.alpha. O-glucofuranose, tri-O-butanoyl 3, 5, 6,- isopropylidene-1,2 .alpha.-D-glucofuranose, O-butanoyl-6-di-O-isopropylidene-1,2 : 3,4 .alpha.-D-galactopyranose, and penta-O-butanoyl-1,2,3,4,6 D-galactopyranose and penta-O-butanoyl-1,2,3,4,6.alpha. D-galactopyranose, )-n-butanoyl-1-isopropylidene-2,3 glyceryl, O-butanoyl-3-di-o-palmitoyl-1,2 glyceryl, and di-O-n butanoyl-2,3 O-palmitoyl-1 glyceryl.

Abstract: A sulfate derivative of galactan extracted from Klebsiella mainly comprised of sulfate neutral oses in a proportion of 20 to 90% of hydroxyls and their preparation and method of use.

Abstract: The present invention provides quaternary ammonium-substituted saponin ethers having improved electrostatic and hydrophobic interactive activities, and therefore very useful in hair-care and skin-care products. The product of the invention, particularly, eliminates efficiently the static flyaway of hair and gives excellent conditioning effect to hair when used in hair-care products. The quaternary ammonium-substituted saponin ethers can be prepared by reacting a soya or ginseng saponin or an aglycone thereof with a cationic compound selected from quaternary ammonium halohydrin or quaternary ammonium epoxide.

Abstract: Alkyl (poly)glucoside ether carboxylates of the formula ##STR1## where R is C.sub.1 - to C.sub.24 -alkyl, C.sub.1 - to C.sub.24 -alkylphenyl, hydroxy-C.sub.2 - to C.sub.6 -alkyl, hydroxy-C.sub.1 - to C.sub.24 -alkylphenyl, ##STR2## or H, R.sup.1 is H or methyl,R.sup.2 is ##STR3## X is a hydrogen, alkali metal, ammonium and/or substituted ammonium equivalent,x is from 1 to 10, y is from 0 to 10, z is from 1 to 4,a process for the preparation of the compounds of the formula I and the use of these compounds as an additive to phosphate-free and low-phosphate detergents, are described.

Abstract: A process of making oligoribonucleoside and deoxyribonucleoside boranophosphates and salts thereof is disclosed. The process comprises the steps of condensing a ribonucleotide or deoxyribonucleotide with a nucleoside phosphitylating agent, wherein the phosphitylating agent includes a 5' -OH group protected by an acid-labile protecting group and a moiety bonded to the phosphorus atom therein that is a stronger proton acceptor than the 5'-OH group of the ribonucleotide or deoxyribonucleotide to form a reaction intermediate, then oxidizing the reaction intermediate so formed with a compound comprising a Lewis base and a boron-containing substituent, wherein the Lewis base is a weaker electron donor than the phosphite phosphorus of the reaction intermediate, to form a ribonucleotide or deoxyribonucleotide boranophosphate. These steps are repeated on the nucleotide boranophosphate to form an oligonucleotide boranophosphate.

Abstract: A rapidly hydrating welan gum useful for preparing cementitious products. The gum can be dry blended with cement or other dry component and then added to a preformed cement/water pre-mix, thereby alleviating the need for hydrating the gum prior to addition to a cement/water mixture.

Abstract: Chelating compounds of specified N.sub.2 S.sub.2 N.sub.3 S derived structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable ester orthioester linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.

Abstract: The invention provides liposomes characterized in that the lipid membrane thereof contains a glycolipid resulting from O-glycoside or S-glycoside bonding of a lipid and at least one carbohydrate selected from the group consisting of uronic acids, uronosyl-oligosaccharides, oligosaccharides composed of glucosamine and glucuronic acid, oligosaccharides composed of galactosamine and glucuronic acid, oligosaccharides composed of glucuronic acid and xylose, oligosaccharides composed of glucuronic acid and glucose, oligosaccharides composed of glucuronic acid and galactose, oligosaccharides composed of glucuronic acid and mannose, oligosaccharides composed of galacturonic acid and rhamnose, ketoaldonic acids, 2-acetamido-2-deoxyuronic acids, 2-acetamido-2-deoxyuronic acid-containing oligosaccharides, 6-O-carboxyethyl-.beta.-D-glucose, 6-O-carboxymethyl-.beta.-D-glucose, 6'-O-carboxymethyl-.beta.-D-maltose and 6'-O-carboxyethyl-.beta.-D-maltose.