Abstract: Method of localizing hyaluronic acid to the surface of a cell or multi-cellular structure by contacting the cell or multi-cellular structure with a dispersion of a construct of the structure F—S1—S2-L where F—S1 is a polymer or oligomer of hyaluronic acid including a terminal glycamine residue (S1), S2 is —CO(CH2)4CO—, —CO(CH2)5CO— or —CO(CH2)6CO—, and L is a phosphatidylethanolamine.

Abstract: An inventive substrate is provided which includes a substrate compound of formula A-B1-B2-B3-B4: wherein A is a sugar moiety; B1 is a linker moiety allowing the conjugation of moiety A and the remaining structure of the substrate; B2 is a linker moiety with a free reactive amino group so as to be available for reaction with carboxylic acids or detectable tags; B3 contains a permanently charged element such as a quaternary ammonium group so as to increase sensitivity for mass spectrometry analysis; and B4 of various carbon length conferring specificity amongst individual substrates in detection methods. Also provided is a molecule of the formula B1-B2-B3-B4, with similar structural characteristics to an enzymatic product produced by the action of a target enzyme on an inventive substrate. Further provided are methods for using inventive substrates for detecting enzymatic activity.

Abstract: Compounds derived from ?-C-phenyl-N-tert-butylnitrone, a process for the preparation thereof and use thereof for the preparation of medicaments for use in preventing or treating oxidative stress-related diseases.

Abstract: A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective group. This compound may be used an intermediate for making a 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, such as gemcitabine.

Abstract: The present invention provide a compound represented by the following formula (1) wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention and a salt thereof can preferentially induce production of IL-4, which is one kind of cytokines that control action of immunocytes. Therefore, it is useful for the prophylaxis or treatment of autoimmune diseases, infectious diseases and the like, and prophylaxis or treatment of diseases caused by functional promotion of Th1 cells.

Abstract: This invention relates to immunogenic compounds which serve as ligands for NKT (natural killer T) cells and to methods of use thereof in modulating immune responses.

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.

Abstract: The invention relates to conjugates of products of interest and of compounds targeting the cation-independent mannose 6-phosphate receptor with a high affinity. The invention also relates to their applications, for instance in enzyme replacement therapies.

Abstract: The present invention relates to new morphine-6-glucuronide derivatives, to pharmaceutical compositions thereof and uses thereof.

Abstract: Uses of exogenous ganglioside to inhibit the propagation of prostate cancer cells are provided. Gangliosides regulate many cellular processes including cell death. The present disclosure assesses the role of ganglioside in prostate cell growth. Malignant prostate (PC-3) and control (RWPE-1) cells can be cultured with or without ganglioside treatment. Cells can be assayed for differences in cell growth. Supplementation with ganglioside (GD3) can decrease growth of PC-3 cells by 30% compared to controls (p<0.01). Ganglioside can have therapeutic benefit in prostate cancer as demonstrated by decreased growth of malignant PC-3 cells.

Abstract: The present invention generally provides compositions methods and composition relating to the diagnosis and/or treatment of cancers having a cell surface de-N-acetylated sialic acid antigen, e.g., an at least partially de-N-acetylated ganglioside and/or a de-N-acetylated sialic acid-modified cell surface protein.

Abstract: Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.

Abstract: The invention relates to prodrugs of hydroxyl-substituted adamantane compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

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.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating neuronal damage and neurological diseases, and more particularly, to a pharmaceutical composition for preventing or treating neuronal damage and neurological diseases containing, as active ingredients, any one or two or more compounds selected from a group consisting of the compound of chemical formula 1, the compound of chemical formula 2, and the acceptable salts thereof. The pharmaceutical composition repairs nerve tissue damaged by herpes zoster to reduce the acute pain caused by herpes zoster, prevents postherpetic neuralgia, and enables a fundamental treatment through the recovery of nerve tissue in the postherpetic neuralgia.

Abstract: The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.

Abstract: Preparation of synthetic monosaccharides, for use in the preparation of synthetic heparinoids.

Abstract: This invention relates to galactosylceramide compounds.

Abstract: The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.

Abstract: A composition of matter comprising sophorolipids as antimicrobial agents, antifungal agents, biopesticides, for uses as drugs to treat HIV, septic shock, cancer, asthma, dermatological conditions, as spermicidal agents, as anti-inflammatory drugs, as ingredients in cosmetics and building blocks for monomers and polymers and self-assembled templates for further chemical elaboration.

Abstract: A composition for stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells includes a glycolipid antigen and a nanoparticle conjugated with the glycolipid antigen. The glycolipid antigen and the nanoparticle are not antigenic in mouse and human being. The composition can further include covalent or non-covalent connection between the glycolipid antigen and the nanoparticle. The glycolipid antigen is alpha-galactosylceramide or an analog of that. The nanoparticle can be a polymer. A production method of the composition includes preparing a nanoparticle and a glycolipid antigen and loading the glycolipid antigen to the nanoparticle. The glycolipid antigen can be coated onto the surface of the nanoparticle or encapsulated within the nanoparticle. A method of stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells is also provided.

Abstract: This disclosure relates to validamycin A biosynthesis and in particular, to methods of producing validamycin A analogs and uses thereof. In a particular example, a method for making a validamycin A analog includes transforming a host cell with one or more recombinant DNA vectors to produce a valN-inactivated mutant; and culturing the valN-inactivated mutant in a culture medium to produce a validamycin A analog, such as 1,1?-bis-valienamine and validienamycin, and their conversion to valienamine. The present disclosure further relates to compositions including such compounds as well as methods of using the compositions, such as for antifungal agents.

Abstract: Methods for assaying ?-L-iduronidase enzymatic activity and methods for screening newborns for Mucopolysaccharidosis Type-I.

Abstract: The present invention relates to fluorescent enzymatic substrates of saccharidic nature having a self-cleavable spacer arm functionalized by a fluorophore F and by at least one inhibitor of the fluorescence of F, to the use thereof for preparation of a diagnostic reagent for functional imaging in vivo, and to the diagnostic reagent for functional imaging containing at least one such enzymatic substrate.

Abstract: The disclosure relates to derivatives of morphine-6-glucuronide of formula (I) wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics.

Abstract: Described herein are novel cerebroside compounds, designated as Turbostatin 1, Turbostatin 2, Turbostatin 3, and Turbostatin 4. These compounds were extracted and isolated from the marine mollusk Turbo stenogyrus, and their structures elucidated. The new compounds exhibit significant cancer cell growth inhibition activity against a variety of murine and human cancer cell lines, and as such appear will be useful in the treatment of various forms of neoplastic disease.

Abstract: The present invention relates to new adjuvants and the uses in pharmaceutical compositions, like in vaccines. In particular, the present invention provides new compounds useful as adjuvants for prophylactic and/or therapeutic vaccination in the treatment of infectious diseases, inflammatory diseases, autoimmune diseases, tumours, allergies as well as for the control of fertility in human or animal populations. The compounds are particularly useful not only as systemic, but preferably as mucosal adjuvants. In addition, the invention relates to its uses as active ingredients in pharmaceutical compositions.

Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.

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: Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds. Glycolipids having the formula (I): where R3 indicates a substituted or unsubstituted C1 to C7 linear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and R8 indicates a substituted or unsubstituted C1 to C35 alkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.

Abstract: A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even Hemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).

Abstract: A method for detecting a Norwalk-Like Virus (NLV) in a biological sample, comprising the steps of: obtaining a biological sample suspected of containing a NLV; contacting the biological sample with at least one human histo-blood group antigen to allow formation of a complex of the NLV with the antigen; and detecting the antigen-NLV complex. The antigen-NLV complex can be detected by contacting the NLV-antigen complex with a NLV antibody that binds at an epitope of the NLV, and detecting the NLV antibody. The invention also includes a method for identifying compounds, and the compounds, that can inhibit the binding between a Norwalk-Like Virus (NLV) and a histo-blood group antigen.

Abstract: ?-Galactosylceramides and glycosylceramides (“ceramide-like glycolipids”) that modulate NK T cells. The ceramide-like glycolipids vary in the cytokines induced in NK T cells and vary in the antigen-presenting cells that are capable of efficiently presenting the compounds to NK T cells. Pharmaceutical compositions of the ceramide-like glycolipids are provided, as are pharmaceutical compositions of the ceramide-like glycolipids combined with dendritic cells. Methods utilizing the ceramide-like glycolipids in vaccines, to activate NK T cells, to stimulate the immune system, and to treat mammals are also provided. The invention also provides methods of evaluating a compound for its ability to activate an NK T cell in the presence of a cell expressing a CD1d protein.

Abstract: The present invention relates to a diagnostic technique related to a biomarker for a microdomain disease and a method for detecting a microdomain disease of which manipulation is easy and which is inexpensive.

Abstract: The present invention provides novel n-alkenyl glycosides and glycoconjugates, n-alkyl glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycoconjugates as disclosed herein.

Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1 represents a glycosyl group, a phosphate group, or a cyclic phosphate group bound to R2; R2 represents —CH2OH, —CHO, —CH2NH2, —CH2-amino acid residue, or —CH2—OPO2H; and R3 represents hydrogen atom, or —PO3H2, and a composition for cosmetics, medicaments, foodstuffs, and/or feeds containing the aforementioned compound or a salt thereof.

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: A ganglioside or a mixture of gangliosides, isolated from the peripheral and central nervous system of a bird, in particular a parrot, their use for the preparation of a medicament, methods for the diagnosis of Proventricular Dilatation Disease and diagnostic kits thereof, are disclosed.

Abstract: A process for preparing pure monosialoganglioside GM1 in the form of its sodium salt. There is provided a process for the isolation and purification of monosialoganglioside GM1 comprising (a) separation of GM1 from a lipidic mixture containing the monosialoganglioside GM1 as the main ganglioside component by ion exchange column-chromatography using an eluent comprising potassium or caesium ions, (b) recovery of the solute from the eluted solution, (c) diafiltration of an aqueous solution of the recovered solute, and (d) second diafiltration after the addition of 1 M NaCl, and recovering GM1. The purity level of GM1 obtained is higher than 99.0%.

Abstract: A novel compound causing an oral cavity stimulus such as acridness, which is expressed by the following structural formula (I):

Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.

Abstract: Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Abstract: A process for the preparation of compounds having formula (I) is disclosed, wherein: —R1 is a methoxy or methylthio group; —R2 is a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R2=OH and the suitably protected 1-acetyl-glycose.

Abstract: Phytoplankton represent a potential source of bioactive compounds. The present disclosure provides, inter alia, methods for identifying glycerolipids and apoptosis-inducing sphingosine-like lipids from virally-infected phytoplankton.

Abstract: The present invention provides glycorandomized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.

Abstract: The invention relates to the use of certain derivatives of D-mannopyranoside for controlling angiogenesis. These compounds have a pro-angiogenic activity, and can particularly be used for preparing a pharmaceutical composition for treating cardiovascular diseases or for treating muscular atrophy. The invention also relates to certain D-mannopyranoside derivatives, to a pharmaceutical or cosmetic composition containing said derivatives, and to the use of such a cosmetic composition for preventing and/or treating hair loss.

Abstract: The present invention provides compositions of avicins and avicin mixtures that enhance topical, percutaneous, transmucosal, transepithelial, transendothelial or transdermal transport of agents including diagnostic molecules, therapeutic drugs and cosmetic materials.

Abstract: A process for preparing pure monosialoganglioside GM1 in the form of its sodium salt. There is provided a process for the isolation and purification of monosialoganglioside GM1 comprising (a) separation of GM1 from a lipidic mixture containing the monosialoganglioside GM1 as the main ganglioside component by ion exchange column-chromatography using an eluent comprising potassium or caesium ions, (b) recovery of the solute from the eluted solution, (c) diafiltration of an aqueous solution of the recovered solute, and (d) second diafiltration after the addition of 1 M NaCl, and recovering GM1. The purity level of GM1 obtained is higher than 99.0%.

Abstract: The invention provides a glycolipid effective for cancer treatment and the like and a synthetic intermediate therefor, as well as a medicament containing the glycolipid and the like.