Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (?-GalCer) analogs, and their use as immunotherapies. In one aspect. a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1: or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.

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: 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: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in N?-benzyloxycarbonyl-N?-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

Abstract: Pharmaceutical formulations containing (i) an amphiphilic drug and (ii) a short-chain sphingolipid are described and provided herein along with methods of making and using same.

Abstract: Disclosed herein are compounds useful as two-photon tracers. Also, methods are provided for visualizing intracellular glucose uptake, screening anticancer agents, and diagnosing cancer using the compounds. They exhibit preferential uptake by cancer cells, penetrability sufficient to allow bright section images, high water solubility, high pH resistance and low toxicity in addition to applicability to living cells in deep tissues over a long period of time.

Abstract: This invention relates with the gambogic acid glycoside derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted glycosyl, optionally substituted multi-hydroxyl, optional substituent oxy, optional substituent containing carbon, oxygen, sulfur, nitrogen or phosphorus element. Compounds of the present invention are useful as therapeutically effective agents of anti-cancer, anti-virus and anti-bacterial. This invention also relates with their preparative methods and applications.

Abstract: The present invention relates to novel aminoglycoside antibiotics, a process for producing the same, and pharmaceutical use thereof. More specifically, the present invention relates to compounds represented by formula (I), a process for producing the same, and use of the same as antimicrobial agents. wherein R represents amino or hydroxyl.

Abstract: The invention provides analogs of alpha-galactosyl ceramide that increase the immune response elicited by various antigens. It also provides methods of using such compounds to increase the effectiveness of vaccines.

Abstract: The invention relates to ?-galactoceramide analogs, their methods of manufacture, intermediate compounds useful in these methods. It also relates to pharmaceutical compositions containing the ?-galactoceramide analogs. The methods of manufacture of the invention involve the use of unsaturated intermediate compounds which enable to synthesize ?-galactoceramide analogs by a mere metathesis reaction. The ?-galactoceramide analogs of the invention are useful as active ingredients of pharmaceutical compositions, particularly in pharmaceutical compositions having anti-cancerous properties.

Abstract: 13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines to 13-deoxyanthrcyclines wherein the reduction reaction is maintained at temperatures of about 55° C. to 64° C. without stirring or agitation. The reaction is completed with the addition of aqueous bicarbonate which forms the 13-deoxyanthracycline and precipitates. The precipitates are filtered and the precipitate and filtrate are extracted separately with organic solvents. The crude 13-deoxy anthracycline can be converted to 5-imino-13-deoxy anthracycline by reaction with methanolic ammonia. The reaction can also be performed with an acidic pyridinium salt instead of a strong acid so that neutralization of the reaction or extraction of the product is not necessary, thereby facilitating purification.

Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Abstract: The present invention provides a lyophilized preparation of amrubicin, which contains L-cysteine or a salt thereof and has a water content of 0 to about 4% by weight within the preparation, and is stable even in a long-term storage, and further provides a method for production of said preparation. Said preparation is useful as a chemotherapeutic agent for cancers.

Abstract: The invention provides a compound (which can act as an adjuvant) of Formula I or Formula (II), wherein R1 R4 R5 R6 and R7 are each independently selected from hydrogen, acetyl, hydrocarbyl, a lipid moiety and a lipid acyl moiety; R2 is a hydroxyl, a hydrocarbyl, a lipid moiety, a lipid acyl moiety; or an amino hydrocarbyl group optionally substituted with a hydrocarbyl, a lipid moiety or a lipid acyl moiety; R3 and R8 are each independently selected from acetyl, a hydrocarbyl, a lipid moiety and a lipid acyl moiety; X is a peptide chain; The above normuramylglycopeptide compounds can be located in liposomes and micelles and can function as immunomodulators, along with a desired antigen (or DNA encloding the antigen), in (e.g. DNA) vaccines.

Abstract: Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described.

Abstract: Compositions comprising the compound of formula are provided herein. Also provided are methods of enhancing an immune response of a subject to an antigen by administering the antigen and the composition. The enhanced immune response may be an humoral immune response, a CD4+T cell response, a CD8+T cell response or result in activation of antigen presenting cells. Methods of enhancing the immune response by intramuscular administration of an antigen and the composition including the compound of formula I are also provided.

Abstract: Disclosed are novel compositions and methods for the treatment of Multiple Sclerosis (MS), and in particular immunostimulatory compositions comprising muramyl dipeptide microparticles for use, e.g., in the treatment of MS.

Abstract: The invention provides formulations and methods for mediating inflammation, in particular an inflammatory bowel disorder such as necrotizing enterocolitis, and for. Further, the formulations are effective in lowering blood cholesterol and decreasing blood cholesterol absorption. The formulations comprise at least one ganglioside, which may be selected from the group consisting of: GD3, GM1, GM2, GM3, and GD1b. The invention provides a method of treating or preventing inflammatory diseases, such as necrotizing enterocolitis by delivery of at least one ganglioside to a subject in need thereof. Supplementation of foods or liquids with gangliosides, fore example infant formula or infant foods, can be employed according to the invention.

Abstract: The invention relates to a ganglioside mixture, consisting of gangliosides, of the following general formula: (sugar)-OCH2—CH(—NH—CO—R1)—CH(OH)—CH?CH—R2, wherein (sugar) represents a sugar radical, the group —CO—R1 represents an acyl-fatty acid which is bonded to the radical of the molecule in the form of an amide, R1 represents a straight saturated alkyl radical having at least 10 C-atoms and R2 represents a straight, saturated alkyl radical having at least 10 C-atoms or a straight alkenyl radical having at least 10 C-atoms and one, two or three double bond(s). Said mixture is characterised in that at least 10 wt. % of the gangliosides of the general formula I are of the group —CO—R1 and the acyl-fatty acids are a C20:0 fatty acid. Said mixtures exhibit an improved biological activity.

Abstract: The invention provides amphiphilic compounds and methods for manipulating membrane proteins. Compounds of the invention, for example, the compounds of Formulas I-XIX, can be prepared from readily available starting materials. The amphiphilic compounds can manipulate membrane protein at relatively low concentrations compared to many known detergents. The compounds can be used to aid the isolation of membrane proteins, for example, to aid their solubilization and/or purification. The compounds can also be used to aid the functional and structural determination of membrane proteins, including their stabilization and crystallization.

Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.

Abstract: Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.

Abstract: To provide a pharmaceutical composition comprising a ceramide-related substance having little adverse side effects as an active ingredient by using a raw material that is highly safe to a human body and is inexpensive. A pharmaceutical composition comprising at least one sphingoglycolipid derivative that is produced from a beer waste and is represented by the formula below as an active ingredient: wherein R3 represents H or OH; R4 is as defined by (a) or (b): (a) when R3 is H, R4 represents (CH2)13CH3 or (CH2)6CH?CHCH2CH?CH(CH2)4CH3; and (b) when R3 is OH, R4 represents (CH2)yCH3 (where Y represents an integer of 13 to 21) or (CH2)z1CH?CH(CH2)Z2CH3 (where Z1 and Z2 independently represent 0 or a natural number, provided that Z1+Z2=19).

Abstract: The invention provides formulations for mediating inflammation and for lowering blood cholesterol. For example, inflammation of the intestine, retina or neural tissues, may be mediated. Further the formulations are effective in decreasing blood cholesterol absorption. The formulations comprise at least one ganglioside, which may be selected from the group consisting of: GD3, GM1, GM2, GM3, GD1b, NANA, and sialic acid. The invention further provides a method of treating or preventing inflammatory diseases by delivery of at least one ganglioside to a subject in need thereof, and a method of reducing blood cholesterol in a subject be delivery of a ganglioside-containing formulation. The formulation of the invention may be used to supplement foods or liquids, and may for example be used in preparation of infant formula or foods.

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 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: ?-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: 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: Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein.

Abstract: A sophorolid produced by a method involving reacting a compound of formula I with a compound of formula II wherein R1 and R2 are H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, phenyl, or C1 through C18 acyl or alkoxycarbonyl, R1 and R2 are not both acyl, R3 is H, CH3, CH2-phenyl, CH2—C6H4—OH, CH2CO2H, CH2CH2CO2H, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2OH, CH(CH3)OH, CH2CH2CH2CH2NH2, CH2CH2CONH2, CH2CONH2, CH2—C3N2H3(histidine), CH2CH2CH2NHC(NH)NH2, CH2CH2SCH3, R2 and R3 may be joined in a ring, R4 is H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, or phenyl, n is 0-6, R5 and R6 are H, C1-C18 alkyl, C3-C18 alkenyl, C3-C10 cycloalkyl, or phenyl, and X is C1-C18 alkyl or C1-C18 alkenyl; optionally followed by acidolytic (treating with an acid) or hydrogenolytic deprotection (treating with a hydrogenolysis catalyst) which removes one of the groups R1 or R2 and replaces it with hydrogen.

Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds of this invention can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases, for example, bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection or psoriasis. The present invention also relates to pharmacological compositions containing these monosaccharide derivatives, as well as methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, and other inflammatory and/or auto immune disorders.

Abstract: The present invention relates to a fluorescent dye-labeled glucose analog, and a synthesis method and usage of the same, and more particularly, to novel glucose ? and ? anomers in which a fluorescent dye is labeled by O-1-glycosylation, an asymmetric synthesis method of the anomers, a molecular bioimaging method of the anomers, and a screening method of curing or preventing drugs for diseases related to glucose metabolism.

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 present invention relates to colchicine derivatives, in particular to the 3-demethyl and 3-demethylthio-colchicine of the general formula (I) in which X is oxygen or sulfur, a method for the preparation thereof and pharmaceutical compositions containing them. The compounds of formula (I) have muscle relaxing, anti-inflammatory and anti-gout activity.

Abstract: The invention provides a pseudoglycolipid effective for cancer treatment and the like and a novel synthesis intermediate therefor, as well as a medicament containing the pseudoglycolipid and the like. The inventive compound is represented by the formula (1), or a salt thereof, wherein each symbol is as defined in the specification.

Abstract: The present invention is in the field of Fabry disease and concerns a pathogenic factor allowing diagnosis of Fabry disease. In particular lyso-ceramide trihexosamide (lyso-CTH) has been found to function as a diagnostic marker for Fabry disease.

Abstract: Novel compounds, derivatives of ?-C-phenyl N-tert-butyl nitrone, a method for production and use thereof for the preparation of medicaments for the prevention of treatment of diseases related to oxidative stress.

Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (?-GalCer) analogs, and their use as immunotherapies. In one aspect. a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1: or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.

Abstract: One aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one ligand tethered to an altered or non-natural nucleobase. In certain embodiments, the non-natural nucleobase is difluorotolyl, nitropyrrolyl, or nitroimidazolyl. In certain embodiments, the ligand is a steroid or aromatic compound. In certain embodiments, only one of the two oligonucleotide strands comprising the double-stranded oligonucleotide contains a ligand tethered to an altered or non-natural nucleobase. In certain embodiments, both of the oligonucleotide strands comprising the double-stranded oligonucleotide independently contain a ligand tethered to an altered or non-natural nucleobase. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one ligand tethered to an altered or non-natural nucleobase.

Abstract: Compounds having the formula (I): wherein A represents a group such as a cyclic group, R1 and R2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.

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: 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 object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine. The present invention relates to a galactose derivative represented by the following general formula (I) a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, an oligo nucleic acid). wherein, R1 represents hydrogen, an alkyl having 1 to 10 carbons which may be substituted or 1-(D)-deoxylactito-1-yl; R2 represents a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms.

Abstract: [Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against Hemophilus influenzae, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.

Abstract: The invention relates to high affinity Siglec ligands that are useful for isolating cells that express Siglecs and for delivering agents to cells that express Siglecs. In one embodiment, the invention provides a method for treating cancer in a mammal that involves administering a Siglec ligand of the invention to the mammal, where the Siglec ligand is linked to a therapeutic agent.

Abstract: There are disclosed compound of formula I, in which R1 represents a hydrophobic moiety adapted to occupy the C? channel of human CDId, R2 represents a hydrophobic moiety adapted to occupy the A? channel of human CDId, such that R1 fills at least at least 30% of the occupied volume of the C? channel compared to the volume occupied by the terminal nC14H29 of the sphingosine chain of ?-galactosylceramide when bound to human CDId and R2 fills at least 30% of the occupied volume of the A? channel compared to the volume occupied by the terminal nC25H51 of the acyl chain of ?-galactosylceramide when bound to human CDId R3 represents hydrogen or OH, Ra and Rb each represent hydrogen and in addition, when R3 represents hydrogen, Ra and Rb together may form a single bond, X represents or —CHA(CHOH)nY or —P(?0)(0?)0CH2(CH0H)mY, in which Y represents CHB1B2, n represents an integer from 1 to 4, m represents 0 or 1, A årepresents hydrogen, one of B1 and B2 represents H, OH or phenyl, and the other represents hydrogen or o

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

Abstract: A method is provided in which the recognition specificity of a virus for a receptor sugar chain can be easily determined with a simple instrument or apparatus. This method for determining the recognition specificity of a virus for a receptor sugar chain or for determining the change in a host infected in accordance with the mutation of virus includes the steps of bringing a sample of the virus into contact with a support having a polymer with sialo-oligosaccharide immobilized on the surface thereof; and assaying the degree of binding therein to determine the recognition specificity of the virus for the receptor sugar chain and to determine the change in a host range. The method is suitable for the surveillance of a virus.

Abstract: A (co)polycarbonate the molecular structure of which contains units derived from bisphenols conforming to formulae (1a1) and (1b1) in which R1 independently of one another represents hydrogen or a C1-C10-alkyl and R2 represents C1-C10-alkyl, or phenyl or benzyl in each case unsubstituted or substituted by at least one member selected from the group consisting of hydrogen and C1-C10-alkyl radical. The (co)polycarbonate exhibits relatively high glass transition temperature and improved adhesion to metals.

Abstract: The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a hydrogen atom or a group forming a prodrug; R1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.