Abstract: The invention belongs to the technical field of drug crystal analysis, and particularly relates to a drug crystal structure landscape analysis system and a landscape analysis method thereof. The drug crystal structure landscape analysis system calls a cloud computing interface to calculate the energy of input crystals through an algorithm deployed in the cloud in advance, and an energy-density space group landscape array diagram of the crystals is generated according to the computation results returned; and analysis is selectively carried out as needed, result reports arc analyzed and summarized as a final report, and the final report is converted into a text document. The drug crystal structure landscape analysis system and the landscape analysis method thereof satisfy the drug crystal structure analysis requirements in the new technology background, and can analyze a large quantity of crystals which are formed by a certain drug molecule and have different structures.

Abstract: Systems, devices, and methods for capturing single source-specific biological material from a multi-source aggregate of biological material are disclosed and discussed. A capture system is generated using reversible chain-blocking to make capture substrates having substrate-linked populations of capture molecules specific for molecules of interest. Incubating such capture substrates in the presence of only a single source of biological material facilitates the association of molecules of interest from the same source. Capture substrate-specific barcode sequences coupled to the capture molecules allow multisource aggregate processing and subsequent grouping to retain the source-specific information following downstream processing.

Abstract: The present invention relates to an improved synthesis of a trisaccharide of the formula, novel intermediates used in the synthesis and the preparation of the intermediates.

Abstract: A modified starch material for biocompatible hemostasis, biocompatible adhesion prevention, tissue healing promotion, absorbable surgical wound sealing and tissue bonding, when applied as a biocompatible modified starch to the tissue of animals. The modified starch material produces hemostasis, reduces bleeding of the wound, extravasation of blood and tissue exudation, preserves the wound surface or the wound in relative wetness or dryness, inhibits the growth of bacteria and inflammatory response, minimizes tissue inflammation, and relieves patient pain. Any excess modified starch not involved in hemostatic activity is readily dissolved and rinsed away through saline irrigation during operation. After treatment of surgical wounds, combat wounds, trauma and emergency wounds, the modified starch hemostatic material is rapidly absorbed by the body without the complications associated with gauze and bandage removal.

Abstract: The present invention relates to polyols and the preparation and use thereof.

Abstract: The present invention concerns compounds of the following formula (I) or a pharmaceutically acceptable salt thereof, a stereoisomer or a mixture of stereoisomers in any proportion, in particular a mixture of enantiomers, and particularly a racemate mixture, in which R represents H, OH or OR19, as well as processes for preparing these compounds and their use as inducer for the transcription of genes under control of the lac promoter.

Abstract: The invention relates to a polyetherester polyol comprising the reaction product of a1) 5 to 63 wt % of one or more polyols or polyamines or mixtures thereof having an average functionality of 2.5 to 8, a2) 2 to 50 wt % of one or more fatty acids, fatty acid monoesters or mixtures thereof, a3) 35 to 70 wt % of one or more alkylene oxides of 2 to 4 carbon atoms.

Abstract: Surface-treated carboxyalkylated polysaccharides comprising a biobased content of at least 82% are described herein. The surface-treated carboxyalkylated polysaccharides comprise a CRC of at least 18 g/g, a FSC of at least 26 g/g, and an AUL at 0.7 psi of at least 14 g/g. Processes for the manufacture of surface-treated carboxyalkylated polysaccharides are also described herein.

Abstract: Described herein is an edible coating for food products in which the coatings comprises a polysaccharide cross-linked with a cross-linking agent solution. Also described herein are methods for coating food products and forming clusters of food products. The use of the edible coating for extending the shelf-life of food products is also described.

Abstract: Glucopyranosyl-substituted benzene derivatives of general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined herein and the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Abstract: The present invention relates to an improved synthesis of a trisaccharide of the formula, novel intermediates used in the synthesis and the preparation of the intermediates.

Abstract: The present invention relates to a sulfated polysaccharide compound and the preparation and use thereof, and in particular to a narrow distribution low molecular weight, highly sulfated pentosan (in this instance a xylan) referred to as glucuronoxylan sulfate (GXS). The invention has been developed primarily for use in the treatment of various clinical conditions. However, it will be appreciated that the invention is not restricted this particular field of use.

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

Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts, to formulations and uses of the compounds of formula (I) in the treatment of metabolic disorders.

Abstract: The present invention relates to derivatized cyclofructan compounds, compositions comprising derivatized cyclofructan compounds, and methods of using compositions comprising derivatized cyclofructan compounds for chromatographic separations of chemical species, including enantiomers. Said compositions may comprise a solid support and/or polymers comprising derivatized cyclofructan compounds.

Abstract: Disclosed is a method of denitrifying a solution including introducing into the solution an amount of a carbon source within a duration and at a frequency so that indigenous heterotrophic bacteria deplete dissolved oxygen in the solution and decompose oxygen from nitrate in the solution to obtain its combined oxygen. Related apparatuses and compounds also are disclosed.

Abstract: The present invention relates to novel methods and novel solid support materials for the tandem synthesis of two or more different oligonucleotides on the same solid support in one synthetic run. The methods involve novel support preparations comprised of two or more types of orthogonally protected anchor groups. Subsequent to the selective removal of the first of the respective protective groups, the first oligonucleotide is assembled on the deblocked anchor groups according to standard methods, preferably via phosphoramidite chemistry. Following the capping of said first oligonucleotide, the anchor groups blocked by a second type of protective group are selectively liberated and serve as the starting point for the assembly of a second oligonucleotide, and so forth. After completion of all the syntheses on the solid support, the oligonucleotides are released from the solid support and deprotected at the nucleobases, using standard methods.

Abstract: A process for chemically bonding an odor-encapsulating agent to textiles includes reacting a cyclodextrin with a cross-linking agent capable of forming ether bonds with the cyclodextrin and with the textile material, and curing the textile material treated with a mixture of the cyclodextrin and cross-linking agent. Preferably, the cross-linking agent is imidazolidone, which forms an ether bond with a hydroxyl group on the cyclodextrin and with a hydroxyl group. In textile materials containing cellulose, imidazolidone forms an ether bond with a hydroxyl group on the cellulose. An active agent can be complexed with the cyclodextrin for release. Textiles formed by such a process can comprise an article of clothing adapted to trap odors emanating from a wearer.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: There is described a process for the synthesis of a sucrose-6-ester comprising: (a) reacting a mixture comprising sucrose and a polar aprotic solvent with an organotin-based acylation promoter, while adding a solvent capable of removing water by co-distillation, and removing water by co-distillation, to afford a first reaction mixture which is substantially free from water, followed by (b) adding a carboxylic anhydride to said first reaction mixture to afford a second reaction mixture, and maintaining said second reaction mixture at a temperature and for a period of time sufficient to produce a sucrose-6-ester, characterised in that step (a) is performed at a temperature of from 85 to 125° C. and at a pressure of from 20 to 80 kPa. In the most preferred embodiment, the polar aprotic solvent is DMF, the solvent capable of removing water by co-distillation is cyclohexane, the organotion-based acylation promoter is a 1,3-diacyloxy-1,1,3,3-tetrabutyldistannoxane, and step (a) is performed at approximately 97° C.

Abstract: The invention relates to a process for the production of perbenzylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents benzyl, n means 2, 3 or 4, X means —COO— or —NH— and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of perbenzylated saccharides with 1-O-functionalized side chains on an industrial scale.

Abstract: A substituted polysaccharide comprising ?1-4 linkages having covalently bonded on the polysaccharide moiety thereof, at least one deposition enhancing group which undergoes a chemical change in water at a use temperature to increase the affinity of the substituted polysaccharide to a substrate, the substituted polysaccharide further comprising one or more independently selected silicone chains.

Abstract: A process for chemically bonding an odor-encapsulating agent to textiles includes reacting a cyclodextrin with a cross-linking agent capable of forming ether bonds with the cyclodextrin and with the textile material, and curing the textile material treated with a mixture of the cyclodextrin and cross-linking agent. Preferably, the cross-linking agent is imidazolidone, which forms an ether bond with a hydroxyl group on the cyclodextrin and with a hydroxyl group. In textile materials containing cellulose, imidazolidone forms an ether bond with a hydroxyl group on the cellulose. An active agent can be complexed with the cyclodextrin for release. Textiles formed by such a process can comprise an article of clothing adapted to trap odors emanating from a wearer.

Abstract: Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.

Abstract: The present invention relates to a low temperature, solvent-free trans-acidolysis process for preparing surface-active carbohydrate fatty-acid esters comprising the steps of: (e) reacting acylated carbohydrate with free fatty acid in the presence of acid catalyst, under reduced pressure, and without adding any solvent; (f) decolorizing and separating the reaction mixture obtained in step (a) into unreacted fatty acid layer and a carbohydrate fatty-ester layer; (g) precipitating out the unreacted acylated carbohydrate; (h) librating the hydroxyl groups by partial hydrolysis in the presence of an acid catalyst; (i) removing the unreacted free fatty acids and unreacted carbohydrate esters of low molecular-weight carboxylic acids during purification, and recycling the removed unreacted free fatty acids and carbohydrate esters to the starting reactant mixture.

Abstract: The present invention is directed toward a novel process for the preparation of pyranosides protected at the 1, 2, 4, and 6 or the 1, 3, 4, and 6 positions.

Abstract: The present invention provides compositions comprising at least one GHB moiety bonded to at least one physiologically compatible carrier molecule. The compositions can enhance the uptake of the drug, deliver effective therapeutic doses in a time-delayed fashion, or can target specific organs.

Abstract: The present invention is to provide means of inhibiting chemical changes in unsaturated compounds by radical reactions through inhibition of radical formation in such an unsaturated compound: The present invention attains such an objective by providing an agent which comprises trehalose as an effective ingredient to form an association product between trehalose and an unsaturated compound.

Abstract: The invention relates to the use of phenolic compounds and derivatives thereof for protection against neurodegenerative diseases, to compositions comprising these compounds, and to some novel phenolic compounds.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1-R13 are as defined herein.

Abstract: The invention concerns a method for preparing Laminaribiose comprising a step for glycoside binding between a donor and an acceptor of glycosyl. The invention is characterized in that the glycosyl donor is in pyranose form and corresponds to formula (II); the glycosyl acceptor is in furanose form and corresponds to formula (III); said binding step is performed in solution in an anhydrous organic solvent, at a temperature ranging between −80° C. and 40° C., for a time interval ranging between 1 minute and 8 hours, in the presence of a suitable promoter.

Abstract: Compositions comprising alkoxylated lipophilic polyol compounds, e.g., ehtoxylated, esterified methyl glucosides, are disclosed wherein at least 5% of the polyol derivatives have about three moles of the lipophilic substituent per mole of polyol. Quite advantageously, the disclosed polyol derivatives can be dissolved into aqueous solutions to provide liquid thickeners suitable for thickening surfactant-containing compositions, e.g., shampoos, at cold processing temperatures.

Abstract: A substituted polysaccharide comprising &bgr;1-4 linkages having covalently bonded on the polysaccharide moiety thereof, at least one deposition enhancing group which undergoes a chemical change in water at a use temperature to increase the affinity of the substituted polysaccharide to a substrate, the substituted polysaccharide further comprising one or more independently selected silicone chains.

Abstract: Process for the preparation of a starch ester, in particular a starch acetate, wherein a starch-based feedstock is reacted with an organic carboxylic acid anhydride in the presence of a catalyst. The reaction of the starch-based feedstock and the anhydride is performed at an excess pressure of about 0.1 to 50 bar in an essentially anhydrous medium containing 10% by weight of water at the most. As catalyst, sodium acetate, sodium hydroxide or sulphuric acid is used, and as the reaction medium, acetic acid or excess acetanhydride is used. By means of the invention, the duration of the esterification reaction can be significantly shortened, the separation of the product can be facilitated, and the recirculation of the waste solutions can be rendered more efficient.

Abstract: A water-soluble, biodegradable hydroxyalkyl cellulose-2-hydroxycarboxylic acid ester is disclosed. The hydroxyalkyl cellulose-2-hydroxycarboxylic acid ester has: (i) a molecular degree of substitution of the hydroxyalkyl group of less than 1.5 (MShydroxyalkyl<1.5); and (ii) a molecular degree of substitution of the 2-hydroxycarboxylic acid group of greater than 0.4 and less than 3 (0.4<MS2-hydroxycarboxylic acid<3). Also described is a method of preparing the hydroxyalkyl cellulose-2-hydroxycarboxylic acid ester, and methods of using it, e.g., as a consistency regulator in at least one of foodstuffs, cosmetics, building materials, paints and strippers.

Abstract: The present invention provides novel &agr;-O-linked glycoconjugates such as &agr;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &agr;-O-linked glycoconjugates.

Abstract: The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.

Abstract: The present invention relates to the use of a compound having general formula (I) as described hereunder wherein R═H (FPA compound) or R═CH3 (FPB compound) for the preparation of compositions with an antioxidant activity for administering to human beings for therapeutic or nutritional purposes. The invention also relates to a process for the preparation of a compound having general formula (I) as defined above characterized in that a cellular culture is obtained from an Ajuga reptans plant, said culture being subsequently subjected to cultivation under aerobic conditions, in a liquid medium containing assimilable carbon and nitrogen sources, and mineral salts.

Abstract: The invention relates to a process for the production of perbenzylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents benzyl, n means 2, 3 or 4, means —O—, —S—, —COO— or —NH— and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of perbenzylated saccharides with 1-O-functionalized side chains on an enlarged scale.

Abstract: The invention is aimed at discovering a new type of anti-cancer compound which can exert an excellent inhibitory activity against the heparanase. A fungal strain Acremonium sp. MT70646 (KCTC 8973P) was isolated from the soil. From the culture of the isolated fungal strain, novel compounds that can inhibit both heparinase and heparanase was purified. Therefore, the present invention regards to provide a newly isolated fungal strain Acremonium sp. MT70646 (KCTC 8973P), its new products, and pharmaceutical agents such as a heparinase inhibitor, a heparanase inhibitor, a metastasis inhibitor and an angeiogenesis inhibitor all of which contain the above new compounds produced by the fungal strain as an active ingredient.

Abstract: Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.

Abstract: The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.

Abstract: Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.

Abstract: An anticancer drug includes a compound represented by Formula (1): 1

Abstract: Compositions comprising alkoxylated lipophilic polyol compounds, e.g., ethoxylated, esterified methyl glucosides, are disclosed wherein at least 5% of the polyol derivatives have about three moles of the lip ophilic substituent per mole of polyol. Quite advantageously, the disclosed polyol derivatives can be dissolved into aqueous solutions to provide liquid thickeners suitable for thickening surfactant-containing compositions, e.g., shampoos, at cold processing temperatures.

Abstract: Disclosed is a synthetic ganglioside comprising a deamino-(2-O-substituted)-sphingosine group.

Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

Abstract: An invention is a chemical process for complete destruction and safe disposition of hazardous organic chemicals carbonaceous chemicals. The invention also comprises the process for production of an inert polymer formed essentially of Carbon and Sulfur, and also comprises the new inert polymer, itself and articles made of the new polymer. This new polymer has many of the properties of refractory materials and is an inert non-inflammable cross-linked polymer that is relatively insoluble in all generally known solvents. In the process of the invention, a carbonaceous chemical and Sulfur is heated, in an atmosphere of Nitrogen at 500.degree. to 1500.degree. C. Waste gases including sulfur and sulfides are condensed, scrubbed and the sulfur recycled. The solids residue when analyzed by a mass spectrometer contains less than one (1) part per million (1 ppm) of unreacted organic chemical.