Abstract: The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: (I) wherein each of X, Alk, and W are as defined and described herein.

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: The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.

Abstract: An object of the present invention is to provide a novel polysaccharide derivative used for a separating agent for optical isomers. The novel polysaccharide derivative contains a structure in which a hydrogen atom of a hydroxyl group or an amino group at 2-position in a structural unit of the polysaccharide is substituted with a monovalent group represented by the following general formula (1), and a hydrogen atom of a hydroxyl group or an amino group at 3-position in the structural unit is substituted with a monovalent group represented by the following general formula (2): R1—NH—CO—??(1) R2—NH—CO—??(2) where R1 and R2 represent substituted or unsubstituted aryl groups different from each other.

Abstract: Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative.

Abstract: A 7,2?-dehydrate puerarin represented by formula (I) and salt derivatives thereof. The compounds are prepared from puerarin by intramolecular mitsunobu reaction. They are capable of shortening arrhythmia duration and prolonging coagulation time. They can be prepared into oral formulations or injections for treatment of cardiovascular and cerebrovascular diseases including arrhythmia, coronary heart disease, angina pectoris, myocardial infarction, and cerebral infarction.

Abstract: Compounds, compositions and methods are provided for treating cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood. More specifically, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described.

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: A cleaning composition including a poly quaternary functionalized alkyl polyglucoside, a water conditioning agent, an acid source, a solvent, and water. In one embodiment, the cleaning composition is substantially free of alkyl phenol ethoxylates. The cleaning composition is capable of removing soils including up to 20% proteins. The cleaning compositions include a biorenewable, environmentally friendly alternative to nonyl phenol ethoxylates and exhibit superior cleaning of food soils.

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.

Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.

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 a novel process for the chemical synthesis of ?-(1->6)-linked glucosamine disaccharides of the formula (1) and (intermediate) compounds relating to the process. According to further aspects the invention relates to compositions comprising the compounds and the use of the compounds in the synthesis of disaccharides and medicine.

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 relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

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 compound represented by the following formula (1): wherein R1 is an aldopyranose residue wherein the 6-hydroxyl group is optionally alkylated, R2 is a C1-26 hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom or a C1-26 hydrocarbon group optionally having substituent(s), R4 is a C1-21 hydrocarbon group optionally having substituent(s), X is an oxygen atom or —CH2—, and Y is —CH2—, —CH(OH)— or —CH?CH—, or a salt thereof is useful for the prophylaxis or treatment of cancer or infection, since it can preferentially induce production of IFN-? of NKT cells.

Abstract: The present invention encompasses compounds and methods for treating urinary tract infections.

Abstract: Methods and compositions for treating or ameliorating diseases and other conditions, such as infectious diseases, autoimmune diseases and allergies are provided. The methods employ mono- and disaccharide-based compounds for selectively stimulating immune responses in animals and plants.

Abstract: The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs. This invention relates to a method for the production of a broad group of glycosylated drugs, including but not limited to propofol, acetaminophen, and camptothecin carbohydrate derivatives.

Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Huntington's disease (HD) is a neurodegenerative disorder caused by the expansion of a polyglutamine stretch in the protein huntingtin (Htt). HD neurons are dysfunctional at multiple levels and have increased susceptibility to stress and apoptotic stimuli. As described therein there is provided compound(s), composition(s), methods and/or kits for the treatment and/or diagnosis of Huntington's disease.

Abstract: The present invention is directed to the quantitation of GL3 in human urine which can be used for the diagnosis of Fabry disease as well as for the assessment of treatment efficacy thereof.

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: Modified glycolipid compounds are provided. Also disclosed are methods for activating an NKT cell, methods of stimulating an immune response in a subject, and methods suitable for labeling NKT cells.

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

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: Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.

Abstract: Immunogenic compositions, cancer vaccines and methods for treating cancer are provided. Compositions comprising: (a) a glycan such as Globo H or an immunogenic fragment thereof, wherein the glycan is conjugated with a carrier protein by a linker such as para-nitrophenyl; and (b) an adjuvant comprising glycolipid capable of binding CD1d on a dendritic cell, such as an ?-galactosyl-ceramide derivative, wherein the immunogenic composition induces an immune response that induces a higher relative level of IgG isotype antibodies as compared to IgM isotype antibodies, are provided. Immunogenic compositions comprising the carrier protein diphtheria toxin cross-reacting material 197 (DT-CRM197) and the adjuvant C34 are provided. Antibodies generated by immunogenic compositions disclosed herein further neutralize at least one of the antigens Globo H, stage-specific embryonic antigen-3 (SSEA-3) and stage-specific embryonic antigen-4 (SSEA-4).

Abstract: This disclosure provides a composition useful for inhibiting caveolar endocytosis, plasma membrane microdomain formation, virus binding and infection, transmembrane signaling, and integrin function in cells. The composition is composed of non-natural analogs of sphingolipids, and may have applications in the treatment or amelioration of diseases associated with caveolar endocytosis, plasma membrane microdomain formation, transmembrane signaling, and integrin function. Methods for making and using the described composition are also provided.

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: Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.

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: Preparation and use of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.

Abstract: The present invention provides methods and compositions for treating a disorder associated with a deficiency in a gene product of a CLN gene in a subject (e.g., neuronal ceroid lipofuscinosis (NCL)), comprising administering to the subject an effective amount of a sphingolipid (e.g., galactosylceramide, ceramide, lysophosphatidic acid, sulfatide and any combination thereof), thereby treating the disorder in the subject.

Abstract: The invention comprises compounds, methods of making, and methods of using. The compounds may have a backbone and three appended functional groups: one lipid, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. A variety of linkers between the backbone and functional groups may also be selected to optimize performance.

Abstract: The invention comprises compounds, methods of making, and methods of using. The compounds may have a backbone and three appended functional groups: one lipid, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. A variety of linkers between the backbone and functional groups may also be selected to optimize performance.

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: Modified glycolipid compounds are provided. Also disclosed are methods for activating an NKT cell, methods of stimulating an immune response in a subject, and methods suitable for labeling NKT cells.

Abstract: Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of ?-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells.

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: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions of matter that comprise triphosphates of modified 2?-deoxynucleosides and oligonucleotides that are formed when these are appended to the 3?-end of a primer, wherein said modifications comprise NH2 moiety attached to their 3?-hydroxyl group and a fluorescent species in a form of a tag affixed to the nucleobase via a linker that can be cleaved. Such compositions and their associated processes enable and improve the sequencing of oligonucleotides using a strategy of cyclic reversible termination, as outlined in U.S. Pat. No. 6,664,079. Most specifically, the invention concerns compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides carrying detectable tags and oligonucleotides that might be derived from them.

Abstract: The invention relates to selected carbohydrate-lipid constructs and their use as mimics of ligands, for receptors expressed by virus. In particular, the invention relates to the use of selected carbohydrate-lipid constructs in methods of inhibiting virus infection and/or promoting clearance of virus from infected subjects. Carbohydrate-lipid constructs selected for use in these methods where the virus is Human Immunodeficiency Virus (HIV) are provided.

Abstract: This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

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: Tumors can be selectively targeted via compounds provided herein according to the formula, or a pharmaceutically acceptable salt thereof, wherein RA and RB are as defined herein. Tumors can be imaged or targeted for therapeutic treatment using compounds described herein where at least one RA or at least one RB group comprises a imaging agent, a therapeutic agent, or a member of a specific binding pair which can be associated with a secondary imaging agent, such as a microbubble for ultrasonic imaging.

Abstract: There is provided a gallotannic compound, a method of producing a gallotannic compound, a lithographic printing plate coating composition, a lithographic printing plate, a method of producing a lithographic printing plate and a method of printing.

Abstract: Methods and immunogenic compositions for generating an immune response against Marburg virus are provided. The immunogenic composition includes antigens obtained from a Marburg viral strain in combination with an oleanolic acid triterpene adjuvant.

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.