Abstract: The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of ?-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the ?-enriched anomer of gemcitabine hydrochloride of formula (IIb) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

Abstract: Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. In particular, the compounds are based on the 1,6 linkage of a sugar residue and a cyclitol.

Abstract: Processes for purifying oligosaccharides including contacting a basic oligosaccharide solution with a basic boronate resin to bind monosaccharides to the basic boronate resin and obtain a purified oligosaccharide solution. The basic boronate resin can bind about 50% of the monosaccharides and about 10% of oligosaccharides in the basic oligosaccharide solution, by weight of total carbohydrates therein.

Abstract: The present invention relates to a method for making an indolopyrrolocarbazole of the general formula [I], where the method includes the step of reacting a bisindolylmaleimide compound with an oxidizing agent in the presence of an oxygen containing gas at a temperature and for a time sufficient to yield the indolopyrrolocarbazole compound of the general formula [I].

Abstract: Disclosed are glycosides, orthoester glycosides and glycuronamides of fluoxetine and analogs thereof to treat conditions and diseases such as depression.

Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.

Abstract: The present invention describes the use of polysaccharide derivatives for the preparation of biocompatible and biodegradable biomaterials with absorbent properties for body fluids and physical hemostatic activity, to be used in both venous and arterial vascular anastomoses to create a physical hemostatic barrier and to prevent scar tissue formation and formation of post-surgical adherence of the vessels to the surrounding tissues.

Abstract: The invention relates to nucleic acid molecules which code for the tumor rejection antigen precursor MAGE-4 and 41. Also disclosed are vectors, cell lines, and so forth, which utilize the nucleic acid molecule, and optionally, molecules coding for human leukocyte antigen HLA-A1. Use of these materials in therapeutic and diagnostic contexts are also a part of the invention.

Abstract: Methods for chemical modification of hyaluronic acid, formation of amine or aldehyde functionalized hyaluronic acid, and the cross-linking thereof to form hydrogels are provided. Functionalized hyaluronic acid hydrogels of this invention can be polymerized in situ, are biodegradable, and can serve as a tissue adhesive, a tissue separator, a drug delivery system, a matrix for cell cultures, and a temporary scaffold for tissue regeneration.

Abstract: A gelatinizer having gel-forming capability in both organic solvents and water, is provided. The hydrogelatinizer is represented by: (where, A is a sugar residue, and R is an alkyl group).

Abstract: Galactosylceramide analogues represented by the following formula (1) or (2). (wherein X and Y each represent S or O, R1 and R2 each represent an alkyl group or an alkenyl group each having 9 to 35 carbon atoms. R3 represents an alkyl group or an alkenyl group each having 2 to 30 carbon atoms.) It is provided a ?-glucocerebrosidase activator which is easily available, and external skin preparations and a method of activating ?-glucocerebrosidase, in which improvement in formation of horny layer transmission barrier is expected by activating ?-glucocerebrosidase so that an improved effect in rough skin is also expected.

Abstract: Therapeutic 5-aminosalicylic acid derivative compositions having general formula (I), wherein R is a 1-deoxy sugar residue or a poly(ethylene glycol) chain-containing residue, are provided. The compositions enable topical delivery of 5-aminosalicylic acid to the gastrointestinal tract following oral administration in pharmaceutical preparations.

Abstract: The present invention provides a separating agent for enantiomeric isomers, which has an excellent ability to identify asymmetry. That is, the present invention relates to a separating agent for enantiomeric isomers which includes as an effective component a polysaccharide derivative having a bicyclic or more structure having an aromatic, alicyclic, or heterocyclic ring.

Abstract: The present invention relates to pharmaceuticals, foods and drinks, food additives, animal feeds and feed additives comprising an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof as active ingredients, use of an Nacylated hydroxyproline derivative or a salt thereof for the production of an arthritis preventing or treating agent, and a method for preventing or treating arthritis which comprises administering an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof.

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: This invention provides compounds containing a 2-deoxy-2-amino-?-D-glucopyranose (glucosamine) glycosidically linked to a cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.

Abstract: Compositions containing purified nucleic acid wherein the nucleic acid acts as an antioxidant. Such compositions also include materials subject to oxidative damage such as antioxidants, vitamins, lipids, foods and pharmaceuticals. The invention also includes methods for preparing such compositions. These methods include dissolving the nucleic acid and a hydrophilic material in an aqueous solution, which may later be dried or further processed. Additionally, nucleic acid may be coupled with a molecule having hydrophobic and hydrophilic regions and then solubilized in a hydrophobic material. It may also be shaped into small aggregates and added to a hydrophobic material.

Abstract: The invention describes methods for inhibiting angiogenesis in a tissue by administering an antagonist that specifically binds to a proteolyzed or denatured collagen but not to native triple helical forms of the collagen. Antagonists of the invention can target, for example, denatured collagens type-I, type-II, type-III, type-IV, type-V and combinations thereof. Methods utilizing such antagonists for therapeutic treatment of tumor growth, tumor metastasis or of restenosis also are described, as are methods to use such antagonists as diagnostic markers of angiogenesis in normal or diseased tissues both in vivo and ex vivo. Antagonists include monoclonal antibodies referred to as HUI77, HUIV26, and XL313.

Abstract: The present invention relates to anti-tumor compounds, compositions and methods.

Abstract: A set of contiguous and partially overlapping RNA sequences and polypeptides encoded thereby, designated as PS190 and transcribed from prostate tissue is described. These sequences are useful for the detecting, diagnosing, staging, monitoring, prognosticating, preventing or treating, or determining the predisposition of an individual to diseases and conditions of the prostate, such as prostate cancer. Also provided are antibodies which specifically bind to PS190-encoded polypeptide or protein, and agonists or inhibitors which prevent action of the tissue-specific PS190 polypeptide, which molecules are useful for the therapeutic treatment of prostate diseases, tumors or metastases.

Abstract: Disclosed are compounds having the formula wherein R2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula R is a lower alkylene, R? is selected from the group consisting of moieties having the formula where X=0 or 1, Y=0 or 1, R1 is hydrogen or a pharmacologically active drug residue, R8 a pharmacologically active drug residue, R4, R5, and R6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R7 is hydroxyl or hydroxyalkyl.

Abstract: Development of colorectal neoplasia in a patient subject or predisposed to colorectal neoplasia is reduced by the steps of (a) determining a patient is subject or predisposed to colorectal neoplasia; and (b) enterically delivering into the gut of the person an effective amount of an aminoglycoside antibiotic having poor gut absorption, whereby the development of the colorectal neoplasia is reduced as compared with otherwise similar non-treated patients.

Abstract: The present invention relates to compositions comprising semi-crystalline ?-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and/or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and/or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a ?-1-4 conformation.

Abstract: There are provided a novel microorganism Enterobacter sp. B20 strain which produces (E)-4-(2-isocyanovinyl)phenyl ?-rhamnopyranoside having a favorable effect of inhibiting melanogenesis and ?-L-rhamnopyranoside produced thereby. This novel microorganism is a gram-negative bacillus isolated from soil and shows motility owing to polar flagellum. The ?-L-rhamnopyranoside, which is produced by culturing the microorganism under aerobic conditions at a culture temperature of 10 to 37° C. and at a medium pH of about 5 to 9 usually for about 1 to 7 days, is useful as a highly safe and stable whitening agent.

Abstract: Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.

Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3 —(CH2)n—SR3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an interger ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.

Abstract: The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels.

Abstract: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.

Abstract: In accordance with the present invention there is provided a new composition and method for chemically modifying chitosan, including N-substituting or N-cross-linking, under homogeneous conditions by providing neutral aqueous chitosan solutions with enhanced reactivity. The method comprises the steps of i) preparing a clear aqueous solution of chitosan, said solution comprising 0.1 to 10% by weight of a chitosan, and 0.1 to 20% by weight of at least one buffering agent having a pKa between 6.0 and 7.6, said solution having a pH ranging from 6.8 to 7.2; and ii) dissolving homogeneously at least one reagent into the solution of step a), said reagent being reactive toward amine groups of chitosan; and said reagent being at a concentration from 0.01 to 10% by weight. The chitosan in the aqueous solution is chemically modified or cross-linked by a selective substitution on the amino group of chitosan.

Abstract: This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: Proteinase inhibitors comprising a Kunitz domain are disclosed. The Kunitz domain comprises a sequence of amino acid residues as shown in SEQ ID NO:3, wherein the sequence is at least 80% identical to residues 6 through 56 of SEQ ID NO:2. Also disclosed are methods for making the proteinase inhibitors, and expression vectors and cultured cells that are useful within the methods. The proteinase inhibitors may be used as components of cell culture media, in protein purification, and in certain therapeutic and diagnostic applications.

Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3 —(CH2)n—SR3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an interger ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.

Abstract: Targeted molecular bar codes and methods for using the same are provided. The subject targeted molecular bar codes include a molecular bar code and a member of a specific binding pair, where the specific binding pair member is generally bonded to the bar code through a linking group. The subject molecular bar code may be read during translocation through a single nano-meter scale pore. The subject targeted molecular bar codes find use in a variety of different applications involving analyte detection, such as screening and diagnostic applications.

Abstract: The invention relates to the use of the disaccharide derivatives 3?-aminosucrose, sucrose-C6-acid and palatinose-C6?-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.

Abstract: The present invention relates to compositions comprising semi-crystalline ?-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and/or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and/or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a ?-1-4 conformation.

Abstract: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: The invention provides novel methods for treating disease based upon the medicinal use of lipids and phospholipids covalently bound to physiologically acceptable monomers or polymers. Phosphatidylethanolamine moieties conjugated to physiologically acceptable monomers and polymers (PE conjugates) manifest an unexpectedly wide range of pharmacological effects, including stabilizing cell membranes; limiting oxidative damage to cell and blood components; limiting cell proliferation, cell extravasation and (tumor) cell migratory behavior; suppressing immune responses; and attenuating physiological reactions to stress, as expressed in elevated chemokine levels.

Abstract: The present invention relates to a newly identified human aminopeptidase. The invention also relates to polynucleotides encoding the aminopeptidase. The invention further relates to methods using the aminopeptidase polypeptides and polynucleotides as a target for diagnosis and treatment in aminopeptidase-related disorders. The invention further relates to drug-screening methods using the aminopeptidase polypeptides and polynucleotides to identify agonists and antagonists for diagnosis and treatment. The invention further encompasses agonists and antagonists based on the aminopeptidase polypeptides and polynucleotides. The invention further relates to procedures for producing the aminopeptidase polypeptides and polynucleotides.

Abstract: Compounds and methods which are useful for the site-specific delivery and localization of drugs are provided. The compounds can be represented by the formula: A-L-D wherein A is an anchoring moiety; L is a linking group; and D is a drug.

Abstract: The invention described herein relates to: the use of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in the manufacture of a composition for the treatment of rumen acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase to a ruminant; a formulation suitable for the treatment of rumen acidosis in an animal which comprises an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial ?-amylase and/or ?-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacte

Abstract: A composition containing an alk(en)yl oligoglycoside betaine esterquat corresponding to formula I: R1O(G)nOCOCR2R3NR4R5R6??(I) wherein R1 is an alk(en)yl group having from about 4 to about 22 carbon atoms, G is a sugar unit containing 5 or 6 carbon atoms and n is a number from 1 to about 10, R2 is H or a CH3 group, R3 is H or a linear and/or branched alk(en)yl group having from 1 to about 6 carbon atoms, R4, R5 and R6, independently of one another, represent a linear and/or branched alk(en)yl group having from 1 to about 24 carbon atoms or a linear and/or branched hydroxyalk(en)yl group having from 1 to about 24 carbon atoms.

Abstract: The use of carbohydrate-based surfactant compounds having the general formula (I): wherein Y1 and Y2, which may be the same or different, are carbohydrate groups; R1 and R2, which may be the same or different, are selected from: a) hydrogen; b) C(1-24) alkyl group; c) C(1-24) alkyl carboxy group; or d) a carbon chain of 2 to 24 carbon atoms having one or more carbon/carbon double bonds, and n is from 1 to 10; for facilitating the transfer of DNA or RNA polynucleotides, or analogs thereof, into a eukaryotic or prokaryotic cell in vivo or in vitro. New carbohydrate-based surfactant compounds are also disclosed.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: The present invention provides a new class of compounds presenting a high compatibility with tissues and organic fluids. Such new compounds are polysaccharides essentially formed of units of uronic acid and/or hexosamine, containing nitro groups —ONO2 covalently bonded to the saccharide structure. Preferably, the polysaccharides according to the invention are prevalently formed of disaccharide repeating units formed of uronic acid and hexosamine. These compounds, in psychological conditions, selectively release NO, allowing a reduction in the amount of NO needed to achieve a determined therapeutical effect. This result has been achieved by functionalizing polysaccharides essentially formed of units of uronic acid and/or hexosamine, with subsituents containing a ONO2 ? group.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: The invention describes SAGE (sdph3.10) and sdp3.5 tumor associated nucleic acids, including fragments and biologically functional variants thereof. Also included are polypeptides and fragments thereof encoded by such nucleic acid molecules, and antibodies relating thereto. Methods and products also are provided for diagnosing and treating conditions characterized by expression of a sdph3.10 and/or sdp3.5 gene product.

Abstract: The invention provides a formulation for treatment or prevention of a parasitic infection such as a protozoan or helminths infection, for example: Giardia. The formulation comprises at least one ganglioside, which may be selected from the group consisting of: GD3, GM1, GM2, GM3, GD1b, NANA, and sialic acid. The formulation may be used to supplement foods or liquids, for example: infant formula, baby food, baby cereal, juice, dehydrated camping food, or bottled water.

Abstract: The present invention is directed to novel aminooxy-cyclodextrin derivatives of the formula (1): CD—(X—Y—ONH2)n, wherein CD is mono- or polydeoxy ?-, ?-, or ?-cyclodextrin, carrying in its 6-, 3- and/or 2-position a group containing the aminooxy group, and optionally carrying substituents different from (X—Y—ONH2). Y is a linker group between the aminooxy group and the mono- or polydeoxy-CD group, X is a functional group or an atom necessary to connect the linker Y and the deoxy CD group, or Y is a direct bond when X is a direct bond, and n is ?1, but ?24, 21 and 18 for ?-, ?- or ?-cyclodextrin, respectively, the protected aminooxy derivatives thereof, as well the methods for their preparation and use.

Abstract: The present invention provides certain cationic lipids containing stigmasterol, ergosterol and cholic acid groups. Compounds of the invention are useful, either alone or in combination with other lipid aggregate-forming components (e.g., DOPE, DOSPA, DOTMA or cholesterol) for formulation into liposomes or other lipid aggregates. Such aggregates are cationic, and able to form stable complexes with anionic macromolecules, such as nucleic acids. The cationic lipids of the invention are useful in methods of transfecting cells, particularly to introduce nucleic acids into cells. The invention also related to kits for the preparation of lipid aggregates and to lipid aggregates and compositions for transfection of cells.