Abstract: Disclosed are aminocoumarin compounds, pharmaceutical compositions containing aminocoumarin compounds, and methods of their use, e.g., in the treatment of a Gram-negative bacterial infection.

Abstract: An antitumor pharmaceutical combination includes (i) a compound ABX196 and (ii) at least one chemotherapeutic agent and/or at least one immunotherapeutic agent, for use in the treatment of cancer.

Abstract: Compounds, compositions, and methods for the diagnosis and/or treatment of medical conditions involving infections with and colonization by Pseudomonas bacteria including, for example, Pseudomonas aeruginosa in the lungs of patients with cystic fibrosis are described.

Abstract: The present invention relates to a method of preparation of ?-galactosyl ceramides compounds of formula (I): comprising a step a) of glycosylation of a compound of formula (II): with a compound of formula (III):

Abstract: Provided herein are genetically modified yeast cells capable of producing one or more human milk oligosaccharides. The yeast cells include one or more heterologous nucleic acids that encode enzymes of a human milk oligosaccharide biosynthetic pathway. The yeast cells do not include a heterologous nucleic acid encoding a fucokinase. Also provided are fermentation compositions including the disclosed genetically modified yeast cells, and related methods of producing and recovering human milk oligosaccharides generated by the yeast cells.

Abstract: The present invention provides a method for preparing a 6-aminohexyl lactoside-NOTA conjugate. The preparation method comprises brominating perbenzoylated lactose with hydrobromic acid; glycosylating 6-azidohexanol to obtain 6-azidohexyl perbenzoyl lactoside; and deprotecting this precursor in two steps to obtain 6-aminohexyl lactoside and conjugating 6-aminohexyl lactoside to NCS-benzyl-NODA GA (i.e. 2,2?-(7-(1-carboxy-4-((4-isothiocyanate benzyl) amino)-4-oxobutyl)-1,4,7-triazonane-1,4-diyl) diacetic acid) in triethyl amine as an alkaline solvent, to obtain a 6-aminohexyl lactoside-NCS-benzyl-NODA GA conjugate. In this novel preparation method, no deglycosylated side product is produced, such that the yield is considerably increased to 46%. Therefore, the method is suitable for future massive production since the requirement for repeated preparations for massive production is reduced, and the impurities produced in the previously scaled-up preparation process are not present.

Abstract: Compounds of the formulas: wherein: R1-R4, X1, Y1, and A are as defined herein are provided. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds are are useful for the treatment of a disease or disorder. In some embodiments, the disease or disorder is a proliferative disease such as cancer.

Abstract: There is provided a method of glycosylating an aminocoumarin compound comprising conjugating a sugar to the 4?-OH position of the core of the aminocoumarin compound. Also provided is an aminocoumarin compound glycosylated at the 4?-OH position of the core of the aminocoumarin compound. Further aspects of this invention provide this compound for use in therapy, more particularly for use as an antibiotic, or in anticancer treatment.

Abstract: The present invention relates to enterococcal cell wall polymers and their uses in the prevention and therapy of bacterial infection.

Abstract: The present invention relates to a bone regeneration or bone formation promoting pharmaceutical composition comprising muramyl dipeptide, an analogue thereof, a derivative thereof or a pharmaceutically acceptable salt thereof. In contrast to existing passive therapeutic agents which center on bone absorption suppression based on mechanisms for reducing osteoclast functionality, the composition comprising muramyl dipeptide of the present invention promotes the differentiation of osteoblasts, which are bone forming cells, and can advantageously be used in various diseases where bone formation is required as an active therapeutic agent that does not affect osteoclast.

Abstract: The application discloses a method for producing anomerically protected glycosidic oligosaccharide derivatives comprising the step of culturing, in a culture medium containing an anomerically protected lactose acceptor, a genetically modified cell having a recombinant gene that encodes a glycosyl transferase that can transfer a glycosyl residue of an activated sugar nucleotide to said lactose acceptor. The application further discloses a method for producing an oligosaccharide comprising the steps of: (a) culturing, in a culture medium containing an anomerically protected lactose acceptor, a genetically modified cell having a recombinant gene that encodes a glycosyl transferase that can transfer a glycosyl residue of an activated sugar nucleotide to said lactose acceptor to produce an anomerically protected glycosidic oligosaccharide derivative, then (b) removing/deprotecting the anomeric protective group.

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

Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.

Abstract: Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.

Abstract: This invention provides nucleoside triphosphate analogues having the structure: wherein B is a base and is adenine, guanine, cytosine, uracil or thymine, wherein R? is an OH or an H, and wherein R? is azidomethyl, a hydrocarbyl, or a substituted hydrocarbyl, and which has a Raman spectroscopy peak with wavenumber from 2000 cm?1 to 2300 cm?1 or a Fourier transform-infrared spectroscopy spectroscopy peak with wavenumber from 2000 cm?1 to 2300 cm?1, and also to methods of DNA sequencing and SNP detection.

Abstract: Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.

Abstract: Glycosphingolipids (GSLs) bearing ?-glucose (?-Glc) that preferentially stimulate human invariant NKT (iNKT) cells are provided. GSLs with ?-glucose (?-Glc) that exhibit stronger induction in humans (but weaker in mice) of cytokines and chemokines and expansion and/or activation of immune cells than those with ?-galactose (?-Gal) are disclosed. GSLs bearing ?-glucose (?-Glc) and derivatives of ?-Glc with F at the 4 and/or 6 positions are provided. Methods for iNKT-independent induction of chemokines by the GSL with ?-Glc and derivatives thereof are disclosed. Methods for immune stimulation in humans using GSLs with ?-Glc and derivatives thereof are provided.

Abstract: Proton mopping is a new anti-cancer therapeutic approach that disrupts cancer's immunologic balance. It results in the alteration of the pHi/pHe ratio (intracellular-extracellular) of the cancer cell, leading cancer to either normalcy or apoptosis. This technology deploys a chemical compound that has two parts, a glucose part to guide the molecule to the cancer site and a proton neutralizer to mop up the protons. Proof of the validity of this therapeutic approach came after using an existing chemical compound 2-[2(2-Aminoethoxy)ethoxy]ethyl a-D-mannopyranoside, C12H25NO8, which has the above mentioned properties. This compound is of the class of functionalized PEGylated glycosides, which are ligands for conjugation to biological molecules.

Abstract: Hsp90 C-terminal inhibitors and pharmaceutical compositions containing such compounds are provided. The compounds of the disclosure are useful for the treatment and/or prevention of neurodegenerative disorders such as diabetic peripheral neuropathy.

Abstract: A 18F-labeled monomeric galactose derivative is provided as a tomography probe. The derivative is a positron emission tomography (PET) probe. The derivative has high affinity and good stability in animal's body. The derivative can be an alternative glucose metabolism imaging agent used in clinic examination and quantification.

Abstract: Provided herein are water-soluble carbohydrate polymers which are monoderivatized at their reducing terminus, such that the carbohydrate polymers can be selectively conjugated at a single location. Also provided are methods of preparation and conjugation of the monoderivatized carbohydrate polymers.

Abstract: Disclosed are water-soluble platinum complexes for tumor treatment and preparation method, said platinum complexes being shown as formula (I); The present 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: The present invention relates to a use of at least one glycosylated tetrafunctional amphiphilic block copolymer, as immune adjuvant.

Abstract: The present invention relates to a novel alkaloid and novel bioactive alkaloid fractions derivable from Ribes preferably selected among Ribes Rubrum and Ribes nigrum; methods of manufacturing such bioactive Ribes alkaloid fractions and their use for the inhibition of IKK-?, PDE4 and/or PDE5 and in addition their promoting effect on mitochondrial biogenesis and function; their therapeutic or non-therapeutic applications as nutritive or medicinal products in the management of conditions associated with impaired mitochondrial function or IKK-?, PDE4 and/or PDE5 activity, such as inflammation, neurodegeneration, dyslipidemia, type 2 diabetes mellitus, impaired wound healing, sarcopenia and other conditions associated with muscle dysfunction or tiredness and fatigue, or where optimization of muscular or cognitive function is desired; extracts, juices or concentrates of Ribes comprising such alkaloids; compostions comprising such alkaloids, including pharmaceutical compositions, nutritive product such as functional

Abstract: Processes for the synthesis of the Factor Xa anticoagulent Fondaparinux, and related compounds are described. Also described are protected pentasaccharide intermediates as well as efficient and scalable processes for the industrial scale production of Fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions.

Abstract: Provided herein are sphingolipid compounds that are useful for activating natural killer T cells. Also provided are methods for treating or preventing a disease or disorder that is treatable by activating the immune system by stimulating natural killer T cells. The compounds are therefore useful for treating or reducing the likelihood of occurrence of an immune diseases and disorders, such as autoimmune diseases or disorders. The compounds may also be used for treating or reducing the likelihood of occurrence of a microbial infection or for treating or reducing the likelihood of occurrence of a cancer in a subject by administering the sphingolipid compounds described herein.

Abstract: The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.

Abstract: A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5? position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

Abstract: ?-mannosylceramides or salts or solvates thereof in a pharmaceutically acceptable carrier, for use as a Type I NKT cell agonist in conjunction with a therapeutically effective amount of ?-galactosylceramide or a salt or a solvate thereof, and/or at least one or more T-cell co-stimulatory molecules, disclosed. Compositions comprising ?-mannosylceramide, as well as methods of treatment of tumors are also provided.

Abstract: The present invention relates to new anti-infectious compounds consisting of (i) a polar head having from one to three mannose, dimannose or trimannose moieties, which is coupled through an appropriate linker to (ii) a single lipid chain of at least 17 carbon atoms of length. Pharmaceutical compositions and therapeutic uses thereof are also provided.

Abstract: A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5? position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

Abstract: Disclosed are novel ?-galactosylceramide derivatives, pharmaceutically acceptable salts thereof, preparation methods thereof, and pharmaceutical compositions for use in an immune adjuvant containing the same as an active ingredient. The derivatives, in which the amide moiety of ?-GalCer is bioisosterically replaced with a triazole moiety, direct cytokine secretion toward IL-4 rather than IFN-?and thus can be used as a therapeutic for autoimmune diseases regulated by IL-4, such as type 1 diabetes and multiple sclerosis.

Abstract: The invention provides amphiphiles for manipulating membrane proteins. The amphiphiles can feature carbohydrate-derived hydrophilic groups and branchpoints in the hydrophilic moiety and/or in a lipophilic moiety. Such amphiphiles are useful as detergents for solubilization and stabilization of membrane proteins, including photosynthetic protein superassemblies obtained from bacterial membranes.

Abstract: A method of treating or preventing a retinopathy such as glaucoma in a human patient in need thereof comprising administering one or more gangliosides to the patient.

Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.

Abstract: Disclosed is a method for selective synthesis of 1,2-cis-?-linked glycosides which does not require the use of the specialized protecting group patterns normally employed to control diastereoselectivity. Thioglycoside acceptors can be used, permitting iterative oligosaccharide synthesis. The approach eliminates the need for lengthy syntheses of monosaccharides possessing highly specialized and unconventional protecting group patterns.

Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.

Abstract: Substrates are provided that include compounds suitable for detecting the activity of an enzyme such as a lysosomal storage enzyme where the substrates include: a sugar moiety; a linker moiety allowing the conjugation of sugar moiety with the remaining structure of the substrate; and two or more fatty acid chains or derivatives thereof at least one of which is sufficiently structured to provide improved solubility in aqueous or organic solvent systems. Also provided are methods for using substrates for detecting enzymatic activity using the inventive substrates.

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

Abstract: ?-mannosylceramides or salts or solvates thereof in a pharmaceutically acceptable carrier, for use as a Type I NKT cell agonist in conjunction with a therapeutically effective amount of ?-galactosylceramide or a salt or a solvate thereof, and/or at least one or more T-cell co-stimulatory molecules, disclosed. Compositions comprising ?-mannosylceramide, as well as methods of treatment of tumors are also provided.

Abstract: A compound represented by the following Structural Formula (A) or a salt thereof. The compound or the salt thereof is suitably produced from a microorganism belonging to the genus Saccharothrix and can be suitably used as a prostaglandin production inhibitor.

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: In a first embodiment the present invention relates to a sorbent comprising a porous inorganic solid support material having on its surface a film of a crosslinked polyvinylamine comprising derivatized amine groups and amine groups binding to the surface of the support material via electron donor/acceptor interactions. In a second embodiment the present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbents according to the invention for the purification of organic molecules, in particular pharmaceutical active compounds, preferably in chromatographic applications.

Abstract: The present invention provides a hapten derivative and conjugate of a natural high intensity sweetener containing hydroxyl groups. The conjugate can be used to produce antibodies specific against the natural high intensity sweetener. The present invention further provides a kit and method for detecting and quantifying the natural high intensity sweetener in a sample.

Abstract: The present invention relates to the total chemical synthesis of the monosaccharide 35# (R??H), the disaccharide 36# (R??H; R??H), the trisaccharide 37# (R??H; R??H; R???H) and the tetrasaccharide 1# (R??H; R??H; R???H) of the following general formula wherein R represents —Y—NH2Y represents a linker R? is H or R? is H or R?? is H or of the lipopolysaccharide from Neisseria meningitidis, as well as to the trisaccharide 37# and the tetrasaccharide 1#, to vaccines containing at least one of the saccharides 1#, 35#, 36#, and 37# and to the use of such vaccine for immunization against diseases caused by infection with bacteria containing the tetrasaccharide ?-GlcNAc-(1?2)-?-Hep-(1?3)-?-Hep-(1?5)-?-Kdo or the trisaccharide ?-Hep-(1?3)-?-Hep-(1?5)-?-Kdo or ?-GlcNAc-(1?2)-?-Hep-(1?3)-?-Hep, especially for immunization against meningitis, septicaemia, pneumonia and nasopharyngitis caused by Neisseria meningitidis.

Abstract: A composition in the form of an injectable aqueous solution, the pH of which is from 6.6 to 7.8, comprises at least: a) a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and b) an anionic compound bearing carboxylate charges and hydrophobic radicals. The composition may also include a prandial insulin.

Abstract: The invention is directed to compositions and methods related to proteins that are physically associated with ceramide-like glycolipids for use as activators of NKT cells. The compositions and methods of the present invention are useful for the prevention and treatment of diseases.

Abstract: Herein are disclosed novel compounds according to Formula (I) and aggregates comprising such compounds. These aggregates are useful to treat and prevent ocular infections caused by a vims, which virus binds to terminal sialic residues present on the cell surface of the cell to be infected by the virus.

Abstract: The present invention provides a one-pot method of preparing an unprotected ?-O-glycolipid. The first step involves contacting a protected ?-iodo sugar with a catalyst and a lipid comprising a hydroxy group, under conditions sufficient to prepare a protected ?-O-glycolipid. The second step involves deprotecting the protected ?-O-glycolipid under conditions sufficient to prepare the unprotected ?-O-glycolipid, wherein the contacting and deprotecting steps are performed in a single vessel. The present invention also provides a one-pot method of preparing an unprotected ?-O-glycolipid following the steps for the preparation of the unprotected ?-O-glycolipid.

Abstract: Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.