Abstract: The present invention is directed towards conjugates comprising fragments of the capsular polysaccharide of Type III Group B Streptococcus (GBS). Suitable fragments may be produced synthetically or by depolymerisation of native polysaccharide.

Abstract: The present invention provides a method for reducing a metal of a sugar-alcohol compound, the method including the steps of (A) protecting a hydroxyl group of a sugar-alcohol compound containing metal impurities with a protecting group, (B) removing the metal impurities from the sugar-alcohol compound having the hydroxyl group protected with the protecting group, and (C) eliminating the protecting group of the sugar-alcohol compound from which the metal has been removed. There can be provided a method for reducing a metal of a sugar-alcohol compound that can provide a sugar-alcohol compound with a suitable quality for the semiconductor apparatus manufacturing process.

Abstract: An achemo-enzymatic synthesis of oligosaccharides of formula 1 is presented wherein R is selected from —OH, —N 3 and —OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, —(CH 2) n —NH 2 and —(CH 2) n —N 3 wherein integer n is to 10, preferably 2 or 3, R is selected from sialyl moiety, —SO 3 H and —CH(R)—COOH wherein R is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that at least one of R 3 and R 4 is H, and A is a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.

Abstract: The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.

Abstract: The present invention is directed to processes for preparation of iron sucrose complex and purification of the obtained iron sucrose through diafiltration.

Abstract: Provided herein are oligomeric compounds with conjugate groups targeting apoplipoprotein C-III (ApoCIII). In certain embodiments, the ApoCIII targeting oligomeric compounds are conjugated to N-Acetylgalactosamine. Also disclosed herein are conjugated oligomeric compounds targeting ApoCIII for use in decreasing ApoCIII to treat, prevent, or ameliorate diseases, disorders or conditions related to ApoCIII. Certain diseases, disorders or conditions related to ApoCIII include inflammatory, cardiovascular and/or metabolic diseases, disorders or conditions. The conjugated oligomeric compounds disclosed herein can be used to treat such diseases, disorders or conditions in an individual in need thereof.

Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.

Abstract: Provided herein are oligomeric compounds with conjugate groups targeting apoplipoprotein (a) [apo(a)]. In certain embodiments, the apo(a) targeting oligomeric compounds are conjugated to N-Acetylgalactosamine. Also disclosed herein are conjugated oligomeric compounds targeting apo(a) for use in decreasing apo(a) to treat, prevent, or ameliorate diseases, disorders or conditions related to apo(a) and/or Lp(a). Certain diseases, disorders or conditions related to apo(a) and/or Lp(a) include inflammatory, cardiovascular and/or metabolic diseases, disorders or conditions. The conjugated oligomeric compounds disclosed herein can be used to treat such diseases, disorders or conditions in an individual in need thereof.

Abstract: The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the ALAS1 gene, and methods of using such dsRNA compositions to alter (e.g., inhibit) expression of ALAS1.

Abstract: Essentially pure compounds of the formulas (I) to (XXV) are provided. Compositions and methods for enhancing or stimulating an immune response are also provided. The compounds, provided are advantageous in that the compounds are essentially pure and free from contaminants encountered when such compounds are purified from natural sources.

Abstract: The present invention provides moenomycin-based probe compounds of Formula (I) for use in screening inhibitors of bacterial glycosyltransferases. The present invention also provides bacterial glycosyltransferase screening assays using compounds of Formula (I).

Abstract: The invention provides methods for the synthesis of oligosaccharides comprising an aminooxy group. The invention further provides oligosaccharides comprising an aminooxy group, methods for coupling oligosaccharides comprising an aminooxy group to glycoproteins, and oligosaccharide-protein conjugates. Also provided are methods of treating a lysosomal storage disorder in a mammal by administration of an oligosaccharide-protein conjugate.

Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.

Abstract: The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.

Abstract: Disclosed are fluorine-containing highly water-soluble platinum complexes for tumor treatment and preparation method, said platinum complexes being shown as formula (I); The present fluorine-containing platinum complexes exhibiting superior cytotoxicity and efficacy compare to the clinical drug oxaliplatin, the design strategy of the present platinum complexes is to enhance the solubility and stability favor its clinical use.

Abstract: Disclosed is a pharmaceutical composition containing as an active ingredient a compound represented by formula (I) or a physiologically acceptable salt thereof, and a method for treating cancer, the method including administering the compound represented by formula (I) or the physiologically acceptable salt thereof.

Abstract: A method of localizing reproduction assisting hyaluronic acid to reproductive cell surfaces by covalently linking it to lipids is disclosed.

Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.

Abstract: The present invention provides RNAi agents, e.g., double stranded RNAi agents, that target the transthyretin (TTR) gene and methods of using such RNAi agents for treating or preventing TTR-associated diseases.

Abstract: Aryl boronic esters containing the rhamnose carbamate moiety are prepared in good yield and without cleavage of the carbamate linkage by first contacting p-bromophenyl isocyanate with a tetrahydropyran-2-ol followed by reaction with a diboron compound.

Abstract: Aryl boronic esters and boronic acids containing the rhamnose carbamate moiety are prepared by coupling a boronate substituted phenyl isocyanate with a tetrahydropyran-2-ol in the presence of cesium carbonate.

Abstract: Aryl boronic esters and boronic acids containing the rhamnose carbamate moiety are coupled to a triazole with an appropriate leaving group, generating a 4-triazolylphenyl carbamate in good yield and without cleavage of the carbamate linkage.

Abstract: Conjugates of a saccharide and a biomolecule, covalently linked therebetween via a non-hydrophobic linker and methods of preparing same are disclosed. Also disclosed are medical uses utilizing such conjugates. Glycosylation reagents for use in preparing these conjugates are also disclosed. Glycosylated proteins, characterized by improved performance, are also disclosed.

Abstract: An objective of the present invention is to provide a caged compound that can be photoactivated selectively for specific target cell types and can be used in an individual organism. The objective can be achieved by a compound represented by general formula K-Q-X, which is prepared by binding bioactive substance X, photocleavable protecting group Q, and compound K, which can be an enzyme substrate and is dissociated from Q-X by an enzyme reaction, wherein: Q is a protecting group that is photocleaved by light with a specific wavelength and then dissociated from X, when K is not bound thereto; X is a substance that does not express bioactivity when Q is bound thereto, but expresses bioactivity when Q is dissociated therefrom; and K is dissociated from Q by the above enzyme, so as to form a compound represented by Q-X.

Abstract: Herein is disclosed a method for producing lipopolysaccharide (LPS), comprising: (a) growing a culture of a deep rough mutant bacterial strain in a medium; (b) maintaining the culture in stationary phase for at least about 5 hr; (c) harvesting, cells from the culture; and (d) extracting LPS from the cells. The method allows for the production of an LPS which can be used to produce a 3-O-deacylated monophosphoryl lipid A (3D-MLA) having at least about 20 mol % of the hexaacyl congener group.

Abstract: The present invention provides novel ruthenium compounds of Formula (I): or salts, isomers, hydrates, or solvates thereof, or combinations thereof; wherein E, R1, R2, R3, R4, R5, X1, and X2 are as defined herein, and pharmaceutical compositions thereof. Also provided are methods of use and treatment. Such compounds have been found useful in the treatment of malaria infection. Such compounds may also be useful in the treatment of inflammatory conditions, such as acute lung injury and acute respiratory distress syndrome, which optionally may be associated with a malaria infection.

Abstract: Provided is a polyhedral transition metal complex including a hollow shell, the hollow shell including n1 (where n1 is an integer from 6 to 60) transition metal atoms and 2(n1) bidentate organic ligands, the bidentate organic ligands including a group derived from a polyhydroxy compound via a linking group, and formed so that the group derived from the polyhydroxy compound is oriented toward an inner space of the hollow shell. Also provided are: an ultrafine particle-containing transition metal complex including the polyhedral transition metal complex, and ultrafine particles of a metal oxide, the ultrafine particles being included within the hollow shell of the polyhedral transition metal complex; a method of producing the same.

Abstract: The present invention provides, among other things, phosphorylated and pyrophosphate derivatives of mono-, di- and oligosaccharides, as well as structural derivatives of these compounds. These compounds have a variety of uses including for pharmaceutical applications. Also provided are methods of use in the treatment of disease, including diseases related to oxygen delivery.

Abstract: The present invention relates to a water soluble derivative of camptothecin and preparation method thereof, the derivative having a structure of formula I and being appropriate in water solubility, and having anti-cancer activity and stability of lactonic ring. The present invention also relates to a method for synthesizing the compound and medical use of the compound.

Abstract: Conjugates of a saccharide and a biomolecule, covalently linked therebetween via a non-hydrophobic linker and methods of preparing same are disclosed. Also disclosed are medical uses utilizing such conjugates. Glycosylation reagents for use in preparing these conjugates are also disclosed. Glycosylated proteins, characterized by improved performance, are also disclosed.

Abstract: The present invention provides phosphorylated and pyrophosphate derivatives of polyols, and structural derivatives of these compounds, and provides pharmaceutical compositions comprising the same. The compounds and compositions disclosed herein have various biological activities, including for example, as allosteric effectors of hemoglobin and/or as kinase inhibitors. The present invention further provides methods for therapy in human or mammalian patients, and methods for synthesis of biologically active compounds and their intermediates.

Abstract: The present invention provides solid state forms of Fidaxomycin, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising one or more of the solid state forms of Fidaxomycin, and processes for the preparation of the compositions and formulations. The solid state forms of the present invention exhibit advantageous properties such as improved reliability and reproducibility in manufacturing and processing and stability in formulations.

Abstract: Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.

Abstract: L-Rhamnose antigen-lipid conjugates for recruitment of the immune system to sites of tumor growth for initiating an anti-tumor antigen response. Methods for introducing L-rhamnose antigen-conjugated lipids into cell membranes such that L-rhamnose antigens are displayed on the cell surface. The cells can be tumor cells and more specifically can be melanoma cells. Cells are contacted with one or more L-rhamnose antigen-lipid conjugates such that L-rhamnose antigen-lipid conjugates are inserted into the cell membrane. The cells can be contacted for example by intratumoral injection. Pharmaceutical compositions containing the L-rhamnose antigen-lipid conjugates and therapeutic methods employing the conjugates and compositions.

Abstract: In preparing a glycoside compound from (a) a furanose compound or pyranose compound, and (b) an alcohol compound, a process for preparing a glycoside compound in which glycosidic bond locates selectively trans form relative to C-2 hydroxyl group, the process comprising using a furanose compound wherein the hydroxyl at the 2-position may have a substituent protected with a group A, or a pyranose compound which may have a substituent wherein R2 and R3 are the same or different and are each alkyl having 1 to 4 carbon atoms or aryl having or not having a substituent, or R2 and R3 are combined to form alkylene having 2 to 4 carbon atoms (the alkylene may be substituted with alkyl having 1 to 4 carbon atoms, or may have intervening phenylene), and m and n are each an integer of 0 or 1.

Abstract: The present invention relates to synthetic lipoteicoic acid (LTA) mimetics which are useful as vaccine components for therapy and/or prophylaxis of bacterial infection.

Abstract: The present invention relates to providing compounds of general formula 1 wherein A is glycosyl residue of a mono-, di- or oligosaccharide in protected form and R is selected from optionally substituted aryl or optionally substituted heteroaryl, methods for their preparation and their use in glycosidation reactions.

Abstract: Provided are adenosine analog compounds of the general formula that act as P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.

Abstract: The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative.

Abstract: The present invention is a method for selecting a patient to be given a drug for treating septicemia the mode of action of which is to interrupt toll-like receptor 4-derived intracellular signaling. The provided method comprises a step for measuring sCD14-ST in a blood sample from a subject, a step for comparing the measured value with a cut-off value, and a step for selecting a patient as the patient to be given the drug for the treatment of septicemia when the measured value of the sample of that patient is positive in comparison to the cut-off value. The present invention makes it possible to provide a drug to be given to a specific patient to treat septicemia, the mode of action of which is to interrupt toll-like receptor 4-derived intracellular signaling, and to appropriately select the patient to be given the drug and the administration timing or dose.

Abstract: The present invention relates to dendrimers with a monosaccharide, oligosaccharide or polysaccharide terminal group, to their preparation method and their therapeutic uses, notably anti-inflammatory uses.

Abstract: The efficient synthesis of phosphatidylinositol mono- to hexa-mannoside (PIM1 to PIM6) is reported. The invention relates to these phosphatidylinositol mono- to hexa-mannosides carrying a linker and a reactive functional group, e.g. the sulfhydryl group, a protein, a fluorescent probe, or a solid phase. The invention further relates to vaccines comprising the PIMs linked to a carrier protein or an antigen.

Abstract: A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

Abstract: The present invention relates to a non covalent molecular structure comprising a carbon nanostructure and a porphyrin based glycoconjugate (I) which is linked to the said carbon nanostructure by a non covalent link, the said glycoconjugate (I) having the formula (I): wherein M is a metal selected in the group comprising Fe, Ni, Zn, Cu, Mn, Cr or Co, B is a group which is present on at least one of the four phenyl group (C6H5) represented in (I), n is an integer from 1 to 3, that is to say that one to three B group(s) may be present on each phenyl group, and B is represented by a -A-C group wherein A is selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2)n1 group, n1 being an integer from 1 to 10, C is a group of formula (II). The present invention also relates to an electronic device comprising the said non covalent molecular structure, and to the use of this device for the detection of a lectin involved in bacterial or viral infections.

Abstract: A novel N-acetyl-5-N,4-O-carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and ?-selectivity is disclosed. Methods for making disaccharide building blocks comprising ?(2?3), ?(2?6), ?(2?8), ?(2?8)/?(2?9) alternate, and ?(2?9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutinin (HA) from various strains of influenza are provided.

Abstract: The present invention relates to fluorescent and/or targeting lipophilic compounds having the general formula (R1O)(R2O)P(O)—R3-R4-R5 wherein R1 and R2 are each independently a linear or branched, saturated or unsaturated C2-C24 alkyl, or a linear or branched, saturated or unsaturated C2-C24 monoalkenyl or polyalkenyl, the polyalkenyl having from 2 to 4 double bonds, or a linear or branched, saturated or unsaturated C2-C24 monoalkinyl or polyalkinyl, the polyalkinyl having from 2 to 4 triple bonds; R3 is selected from 0, S, —C(R6)2-, —CH(R7)-, —C(S)—N(R6)-, —CH(SR7)-S—S— or —N(R6)- wherein R6 is a hydrogen atom or a C1-C4 alkyl, and R7 is a C1-C4 alkyl; R4 comprises at least one junction function and at least one linker; and R5 is at least one chemical fluorescent group or at least one targeting group. Methods for preparing said lipophilic compounds are also disclosed.

Abstract: The present invention relates to mannopyranoside-derived compounds and to the use thereof as medicaments, in particular in the treatment of cancer diseases, and also to the method for preparing same and to pharmaceutical compositions comprising such compounds. Medical devices surface-treated with mannopyranoside-derived compounds according to the invention also form part of the invention.

Abstract: The present invention refers to compositions for the treatment or prophylaxis of infectious or inflammatory processes in the oral cavity (cavitas oris) including dental hygiene, the composition comprising lipoteichoic acids and glycerophosphate derivatives, preferably added into a dental hygiene product like toothpastes, toothgels, creams or rinsing fluids, the use of glycerophosphate derivatives as prophylaxis against bacterial infections of the oral cavity like dental caries, or the use of polyglycerophosphates for the production of a medicament for the treatment of or prophylaxis against bacterial infections of the oral cavity, like dental caries.

Abstract: The present invention provides methods for preparing LPS antagonist lipodisaccharide B1287 and stereoisomers thereof, which compounds are useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock. Also provided are synthetic intermediates useful for implementing the inventive methods.

Abstract: The invention features compounds of formula (V) or(XII). In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.