Abstract: The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

Abstract: .alpha.-Glycosyl-L-ascorbic acid exhibiting no direct reducing activity is formed in a solution containing L-ascorbic acid and an .alpha.-glucosyl saccharide when subjected to the action of a saccharide-transferring enzyme. .alpha.-Glycosyl-L-ascorbic acid is superiorly stable, and readily hydrolyzable in vivo to exhibit the activities inherent to L-ascorbic acid. Thus, .alpha.-glycosyl-L-ascorbic acid is favorably useful as a stabilizer, quality-improving agent, antioxidant, physiologically active agent and uv-absorbent in food pharmaceutical and cosmetic industries.

Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.

Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Disclosed are lipid A analogs useful for the treatment of septic shock and LPS-mediated activation of viral infection.

Abstract: Light-colored alkyl oligoglycoside pastes can be obtained by a process in whicha) glycose is reacted with fatty alcohols in the presence of acidic catalysts at elevated temperature to a residual content of glycose of less than 0.1% by weight, based on the starting quantity of glycose,b) water of reaction released is continuously removed from the equilibrium,c) the reaction products are neutralized with a base, the molar ratio of hydrogen ions in the reaction mixture to added base being from 1:1 to 1:1.5,d) unreacted fatty alcohols is separated by distillation,e) the residue is subsequently processed by addition of water to a paste having a solids content of 30 to 70% by weight, based on the paste, the paste is alkalized and, optionally, bleached by methods known per se.

Abstract: A cosmetic composition is provided in the form of a gel exhibiting semi-solid behavior at rest but under slow shear rates fractures ceasing to act as a fluid and becoming a solid. The cosmetic composition achieves this rheology through a combination of an alkyl polyglycoside with a polyether ester.

Abstract: A process for the preparation of 1-(2'-deoxy-2', 2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) from 2-deoxy-2,2-difluoro-.beta.-D-ribo-pentopyranose (I). The process uses a tritylation reaction (Step 3) for preparing 2-deoxy-2,2-difluoro-5-O-triphenylmethyl-ribo-pentofuranose (II) as a key intermediate. The 1-(2'-deoxy-2', 2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) is an antiviral and anti-cancer agent.

Abstract: New sesaminol glucosides, which are glucosides of lignan compounds of a specified structure, are effective in preventing oxidation of lipids in an aqueous solvent. Such sesaminol glucosides are produced substantially in pure form by obtaining an aqueous extract from crushed and defatted sesame seeds, processing the extract with .beta.-glucosidase to obtain a processed sesame product which is itself an effective anti-oxidant, and make separations by liquid chromatography under specified conditions.

Abstract: The present invention relates to novel ester derivatives of antibiotic A 40926 complex and its N-acylaminoglucuronyl aglycone. The compounds of the invention are prepared according to an esterification process involving reaction of an A 40926 substrate with an excess of the selected alkanol in the presence of concentrated mineral acid and are reactive as antibiotics.

Abstract: The present invention relates to a D 25 polysaccharide compound whose lipid has been partially removed and to its derivatives, wherein at least 85% by weight, preferably 90% of the compound, exists in aqueous solution in monomeric form. The 30 kD molecular weight polysaccharide compound extracted from the membrane proteoglycan of the bacterium Klebsiella pneumoniae is mentioned in particular. The amount of palmitic fatty acids which is bound to it in esterified form does not exceed 0.01% by weight of the compound and the amount of palmitic fatty acids which is associated with it in the free form does not exceed 0.1% by weight of the compound.

Abstract: An agent for inducing a phytoalexin comprising a xyloglucan-oligosaccharide as an active ingredient thereof and a method for inducing a phytoalexin in a plant body comprising an application of a xyloglucan-oligosaccharide to the plant. The present invention is useful for promoting growth of a plant and maintaining freshness of a plant while a crop has been grown, or a vegetable or a fruit has been transported and/or stored.

Abstract: Crocetin disaccharide esters represented by the following general formula: ##STR1## wherein R.sub.1 and R.sub.2 are gentiobiose groups or glucose groups and may be the same or different groups from each other, are effective for dose-dependently improving the hippocampal long-term potentiation blocking effect of ethanol and are used as an effective cerebral function-ameliorating agent.

Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis. In the formula,X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms Or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.

Abstract: An antitumor agent is provided by including, as an active ingredient, a polysaccharide-glycan complex obtained by treating a Gram-positive bacteria such as lactic acid bacteria and Bifidobacterium strains with a cell wall lytic enzyme produced by a bacterium belonging to the genus Achromobacter.The polysaccharide-glycan complex has no toxicity and causes no side effect. Being water-soluble, it is easily formulated into any arbitrary dose form, such as an injectable solution. It can easily be prepared from an easily available starting material.

Abstract: Oligosaccharide compounds GlcNAc.beta.1-3Gal.beta.-OMe, GlcNAc.beta.1- 6Gal.alpha.-OMe, GalNAc.beta.1-3Gal.beta.-OMe, GalNAc.alpha.1-3Gal.alpha.-OMe, and Fuc.alpha.1-6Gal.beta.-OMe.

Abstract: The invention relates to the chemical modification of the sphingoid portions of glycosphingolipids. It has been possible by a series of reactions to introduce an amino group in the position of the carbon double-bond in the sphingoid portion after elimination of the long-chain aldehyde. Glycosphingolipids of the formula (2) and (3), where X and Y denote a group capable of coupling, are suitable for coupling to other molecules, preferably proteins. X preferably represents NH.sub.

Abstract: A compound selected from those of formula (I): ##STR1## in which: A either represents --OR.sub.6, and B represents --CH.sub.2 --X,or, together with B and the carbon atom carrying them, forms an oxygen-containing heterocycle selected from oxirane, 2,2-dimethyl[1,3]dioxolane and [1,3]dioxolan-2-one,and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and X are as defined in the description.

Abstract: Polyoxyalkylene polyether polyols suitable for preparation of flexible polyurethane foams are prepared by oxyalkylating an aqueous solution of one or more polyhydric, hydroxyl-functional solid initiators under conditions where both water as well as initiator are oxyalkylated. The polyols have calculated functionalities of between about 2.2 and 4.0 and hydroxyl numbers in the range of 10 to 180. The polyols may be used to prepare soft, high resiliency polyurethane flexible foams at low isocyanate indexes.

Abstract: Oligosacaharide compounds that are substrates and inhibitors of glycosyltransferase and glycosidase enzymes and compositions containing such compounds are disclosed. A method of glycosylation is also disclosed. An E. coli transformed with phagemid CMPSIL-1, which phagemid comprises a gene for a modified CMP-sialic acid synthetase enzyme, which transformed E. coli has the ATCC accession No. 68531 is also provided.

Abstract: 2'-Deoxy-4'-thio-ribonucleosides, intermediates in their production, and their use as antiviral and anticancer agents are disclosed.

Abstract: Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues;R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group;Y is H or lower alkyl (1-4C); andX is H or --CHR.sub.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;the five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.

Abstract: Novel glycolipid derivatives of Formula (I): ##STR1## wherein R is a long chain alkyl, or their salts are disclosed. These compounds act as a ligand for selectin family and exhibit a remarkable inhibitory effect on the binding of selectin family to its native ligand sialyl Lewis.sup.x.

Abstract: Conductive polymer doped by a sulphonated cyclodextrin salt and device for obtaining and/or supplying an active substance incorporating said polymer.The dopant used has the following formula (I): ##STR1## in which n is an integer between 2 and 50, M.sup.+ is Na.sup.+, Li.sup.+, K.sup.+ Mg.sup.+ 1/2 or NH.sub.4.sup.+ and R represents --SO.sub.3.sup.- M.sup.+ or --OH, whereby R can differ from one cycle to the other. The doped conductive polymer can be used as an active electrode material in an electrochemical device.

Abstract: A method for preparing a chloroethylglucopyranose which comprisesa) reacting glucose with from 2 to 10 times the molar amount of chloroethanol at from 100.degree. to 130.degree. C. in the absence of a catalyst, optionally removing water,b) further reacting the product of step (a) at 60.degree. to 90.degree. C. in the presence of an acidic catalyst for from 10 to 600 minutes andc) Separating therefrom the chloroethylglucopyranose.

Abstract: Saponin/antigen conjugates and the use thereof for enhancing immune responses in individuals are disclosed. The saponins may be substantially pure or mixtures of saponins.

Abstract: A method for preparing thiol compounds, comprising: (1) reacting cysteine by a non-enzymatical addition reaction with a compound having the formula (R.sub.1)(R.sub.2)C.dbd.C(R.sub.3)--CO--R.sub.4 via an --S-- bridge to form a cysteine conjugate, wherein the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen or an optionally saturated and/or heterogeneous hydrocarbon group or wherein a combination of two groups selected from the group consisting of R.sub.1, R.sub.3 and R.sub.4, together with the carbon atoms to which the groups are bonded, form an optionally saturated and/or heterogeneous hydrocarbon ring system of five or six members; and (2) reacting the cysteine conjugate so obtained in a concentration of >1 mM conjugate with a microbial .beta.-lyase to form a thiol compound.

Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the formXR-SPACER-REPORTER-BLOCKwherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate,-REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate,-SPACER- is a covalent linkage, andXR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R-).

Abstract: The invention concerns a process for the preparation of sennosides A and B, wherein rheinanthrone-8-glucoside is oxidized with oxygen or an oxygen source to the sennosides A and B. According to the invention, the oxidation is carried out using active carbon as a catalyst, and, if desired, the obtained sennosides A and B are converted to their calcium salts using methanol precipitation from a calcium ion containing aqueous solution.

Abstract: The invention relates to the chemical modification of the sphingoid portions of glycosphingolipids. It has been possible by a series of reactions to introduce an amino group in the position of the carbon double-bond in the sphingoid portion after elimination of the long-chain aldehyde. Glycosphingolipids of the formula (2) and (3), where X and Y denote a group capable of coupling, are suitable for coupling to other molecules, preferably proteins. X preferably represents NH.sub.

Abstract: A method of treating inflammation in a subject by administering a therapeutically effective amount of a compound having the structure: ##STR1## where R.sub.1 to R.sub.4 are the same or different and are each selected from the group consisting of H, an alkylacyl group, an arylacyl group, or a C-1-linked saccharide.

Abstract: Simple lactose or lactosamine related compounds which behave as ligands for the ELAM-1 and related receptors are described. These compounds are useful in the treatment of conditions characterized by excess inflammation. These compounds are of the formula ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, lower alkyl (1-4C), alkylaryl or one or more additional saccharide residues;R.sup.3 and R.sup.4 are each independently H, alkyl(1-6C), aryl or R.sup.3 and R.sup.4, taken together, form a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;wherein said five- or six-membered ring may further be substituted by one or more substituents selected from the group consisting of (CHOR.sup.1).sub.m H wherein m is 1-4, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 ;Y is H, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NCOR.sup.1 or SR.sup.1 ; andX is --CHR.sup.5 (CHOR.sup.1).sub.2 CHR.sup.6 OR.sup.1 wherein R.

Abstract: Synthetic compounds which are useful for suppressing an immune response are disclosed. The synthetic compounds have the formula ##STR1## wherein A is a carbohydrate moiety which corresponds to the carbohydrate moiety of a naturally occurring ganglioside, n is 5 to 20 and m is to 20. Also presented are methods for suppressing an immune response in an animal and compositions of matter employing the compounds as shown above.

Abstract: A composition and process for enhancing the aesthetic and tactile properties of an alkyl polyglycoside involving combining a first alkyl polyglycoside having the general formula I:RO(Z).sub.a (I)wherein R is a monovalent organic radical having from about 8 to about 18 carbon atoms; Z is a saccharide residue having 5 or 6 carbon atoms; and a is a number having a value from about 1 to about 6, with an additive selected from the group consisting of C.sub.6 -C.sub.10 alkyl sulfates, unsaturated aliphatic carboxylic acids including hydroxy-substituted derivatives thereof or their salts, unsaturated aliphatic sorbitan esters, C.sub.8 -C.sub.36 branched aliphatic dicarboxylic acids, C.sub.6 -C.sub.

Abstract: This invention comprises polyanionic benzylglycosides of benzene triacid amides of the general formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium;n is 1 or 2;X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms;Y is carbonyl or sulfonyl;or the pharmaceutically acceptable salts thereof, as well as their use as smooth muscle cell antiproliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation.

Abstract: A production stimulator of nerve growth factor contains a new cyathane derivative of the form ##STR1## where R is either CHO or CH.sub.2 OH.

Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.

Abstract: A process for the preparation of 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) from 2-deoxy-2,2-difluoro-.beta.-D-ribo-pentopyranose (I). The process uses a tritylation reaction (Step 3) for preparing 2-deoxy-2,2-difluoro-5-O-triphenylmethyl-ribo-pentofuranose (II) as a key intermediate. The 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) is an antiviral and anti-cancer agent.

Abstract: Glycoside products having a propensity to discolor and/or to exhibit haze under aqueous alkaline or neutral pH conditions can be stabilized to substantially reduce the extent of discoloration and to essentially eliminate any haze which might also be present by adjusting the pH of an aqueous solution of the alkyl glycoside product to about 7 prior to treatment with a metal borohydride material which at the end of the reaction period is consumed resulting in a stabilized alkyl polyglycoside product which does not exhibit a haze in an aqueous solution at a pH of about 7.

Abstract: The aliphatic primary alcohols are reacted with a glycose, more especially glucose, in the presence of an acidic catalyst in certain process steps so that particularly light-colored and alkali-stable alkyl glucosides are obtained after a subsequent, compulsory bleaching step, which represents an improvement over known direct synthesis processes. The process may be carried out both on a laboratory scale and also on an industrial production scale.

Abstract: A continuous method of bleaching an alkylpolyglycoside, substantially free of alcohol, with peroxy compounds, preferably hydrogen peroxide, which is highly efficient to provide an unexpected high degree of color reduction from a dark brown to a light, white product, from an extinction coefficient color respectively of about 10 to about 15 to about 0.025 to about 0.15. The bleaching is carried out at controlled pH and temperature, under pressure preferably in the presence of Mg or MgO.

Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 comprises a functional group which is chemically similar to that found in the peptide of interest.

Abstract: The present invention relates to a series of silicone containing glycosides prepared by the reaction of a hydroxy containing dimethicone copolyol 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: A composition in dry form which can easily undergo dry blending and milling contains biologically active materials and a solid surfactant composed of a combination of an alkyl polyglycoside and an inert carrier selected from the group consisting of silica, talc, a zeolite, magnesium aluminum silicate, calcium sulfate, magnesium carbonate, magnesium oxide, aluminum oxide.

Abstract: Soil isolates, identified as strains of Bacillus polymyxa, NRRL B-18475 and NRRL B-18476, produce large quantities of a pure and uniform extracellular polysaccharide fructan (levan), in a sucrose medium. The levan consists entirely of fructose and the residues linked by .beta., 2-6 fructofuranoside linkage.

Abstract: Highly concentrated mixtures of surfactants are obtained by a method which comprises adding the acid form of a neutralizable surfactant to an aqueous composition comprised of a base and an alkyl polyglycoside.

Abstract: The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

Abstract: A salt of sucrose-octa-O-sulfonic acid and a tetracycline useful in inhibiting protein synthesis of bacteria.

Abstract: Highly concentrated mixtures of surfactants are obtained by a method which comprises adding the acid form of a neutralizable surfactant to an aqueous composition comprised of a base and an alkyl polyglycoside.

Abstract: The present invention provides novel lipophilic drug derivatives which are capable of being formulated in liposomes or micelles. These drug derivatives are known therapeutic agents which are covalently attached to a fatty acid chain of a phospholipid, glyceride, ceramide or 1,2-diacyloxypropane-3-amine. The linkage between the therapeutic agent and the lipid is one which can be cleaved in vivo, allowing the therapeutic agent to be separated from the micellar or liposomal formulation.