Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of Formula III, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

Abstract: The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.

Abstract: Specific fractions of Vitreoscilla filiformis comprising its Lipid A are useful for stimulating the synthesis of anti-microbial peptides of the skin.

Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a) a lipid fraction comprising at least one of docosahexaneoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b) a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c) a mineral fraction comprising at least one of manganese and molybdene, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.

Abstract: The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.

Abstract: The invention relates to methods of producing, and compositions comprising, an isolated alpha (2?8) or (2?9) oligosialic acid derivative bearing a non-reducing end enriched for one or more de-N-acetyl residues and resistant to degradation by exoneuraminidase. A representative production method involves: (i) treating an alpha (2?8) or (2?9) oligosialic acid precursor having a reducing end and a non-reducing end with sodium borohydride under conditions for de-N-acetylating the non-reducing end; and (ii) isolating alpha (2?8) or (2?9) oligosialic acid derivative having one or more de-N-acetylated residues and a non-reducing end that is resistant to degradation by exoneuraminidase. Isolated alpha (2?8) or (2?9) oligosialic acid derivatives that comprise a non-reducing end de-N-acetyl residue are provided, as well as antibodies specific for the derivatives, compositions comprising the derivatives, kits, and methods of use including protection against and detection of E. coli K1 and N.

Abstract: Compounds, compositions and methods for treating conditions characterized by leukocyte rolling are described. The compounds contain glycosulfopeptide structures comprising sulfated tyrosines and sialyated, fucosylated N-acetyllactosamino glycans. The glycosulfopeptides may be conjugated or complexed to other compounds for enhancing serum half-life or for controlled release, for example. Examples of conditions treated include inflammation, ischemia-reperfusion injury, rheumatoid arthritis, atherosclerosis, leukocyte-mediated lung injury, restenosis, and thrombosis.

Abstract: The invention encompasses nucleoside compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: The present invention relates to a combination of organic compounds which comprises at least two antidiabetic agents, preferably with different modes of action, in which the active ingredients are in each case present in free form or in the form of a pharmaceutically acceptable salt and, optionally, at least on pharmaceutically acceptable carrier, for simultaneous, separate or sequential use.

Abstract: The application relates to 4?-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such compounds, to methods and intermediates useful for preparing such compounds, and to therapeutic methods comprising administering such compounds to animals in need thereof.

Abstract: Described herein is a method for reducing levels of the harmful metabolic waste product of S-adenosylmethionine (SAMe), homocysteine, and provide vitamin and other nutritional co-factors that reduce the production of homocysteine and either re-methylate homocysteine back to S-adenosylmethionine, or facilitate its conversion downstream to cystathione. The method of the invention may be achieved by administering 5-methyl tetrahydrofolate, methylcobalamin, and one or more compounds selected from the group consisting of betaine, pyridoxal-5-phosphate, N-acetyl-cysteine, and other cofactors.

Abstract: A cosmetic combination product, wherein the product comprises at least two components selected from (a) one or more dietary supplements, (b) one or more cosmetic preparations for topical application to human skin, and (c) one or more patches for adhesion to human skin. Each of the selected components (a) to (c) comprises at least one cosmetically active substance which is also comprised in the other selected component(s). This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.

Abstract: There is provided a 5-thio-?-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.

Abstract: An O-GlcNAcase-specific inhibitor and substrate are engineered by the extension of the N-Acetyl Moiety of O-(2-acet-amido-2-deoxy-D-glucopyranosylidene)amino-N-phenylcarbamate (PUGNAc). The reagent substrate includes a fluorophor and the inhibitor. This reagent substrate is for high-throughput analysis of O-GlcNAcase within cellular assays and imaging agent for the in vivo analysis of O-GlcNAcase.

Abstract: Compositions and methods for treating various diseases and disorders, such as for a myeldoysplastic syndrome are provided. The methods include administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising at least one of an esterificated azacytidine, an acetylated azacitidine, an esterificated decitabine, and an acetylated decitabine, such as 2?,3?,5?-triacetyl-5-azacytidine.

Abstract: The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.

Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a Flaviviridae family virus, such as hepatitis C virus.

Abstract: The present invention relates to methods of preventing or inhibiting the growth of Helicobacter through the use of a composition that comprises a glucosinolate, an isothiocyanate or a derivative or metabolite thereof. The present invention also relates to methods of preventing or treating persistent chronic gastritis, ulcers and/or stomach cancer in subjects at risk for, or in need of treatment thereof.

Abstract: The present invention relates to the polymorphic crystalline hydrochloride salts of a nucleoside valinate ester according to formula Ib, methods of treating diseases mediated by Hepatitis C Virus and pharmaceutical composition containing Ib

Abstract: The invention relates to relatively short peptides (termed ?-conotoxins herein), about 10-25 residues in length, which are naturally available in minute amounts in the venom of the cone snails or analogous to the naturally available peptides, and which preferably include two disulfide bonds.

Abstract: The invention involves methods of regulating cell growth and division to control disease processes by manipulating mitochondrial metabolism and the expression of cell surface immune proteins. The invention also involves related compositions and screening assays.

Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.

Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.

Abstract: Carbonyl compounds generated and accumulated in the peritoneal dialysate can be inactivated or eliminated by a carbonyl compound-trapping agent such as aminoguanidine. Carbonyl compounds generated during sterilization and storage of the peritoneal dialysate can be eliminated by pre-contacting with the trapping agent. Further, it is possible to eliminate carbonyl compounds transferred from the blood to the peritoneal cavity of the patient during peritoneal dialysis treatment, by adding the trapping agent to the peritoneal dialysate or by circulating the fluid through a carbonyl compound-trapping cartridge. Intraperitoneal protein modification by carbonyl compounds is inhibited by the present invention, thereby sufficiently reducing peritoneal disorders associated with peritoneal dialysis treatment.

Abstract: Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted aromatic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and process for their preparation. The compounds are suitable for example as antidiabetics.

Abstract: The invention relates to a method for treating infectious diseases which are elicited by viruses which are pathogenic to humans comprising the step of administering an amphiphilic nucleoside-phosphonoformic acid derivative having an esterified or unesterified carboxyl group, preferably of a nucleoside-glycerol-(hydroxycarbonyl)-phosphonate, as an active compound.

Abstract: The present invention relates to improved methods for delivering bioadhesive, bioresorbable, anti-adhesion compositions. Antiadhesion compositions can be made of intermacromolecular complexes of carboxyl-containing polysaccharides, polyethers, polyacids, polyalkylene oxides, multivalent cations and/or polycations. The polymers are associated with each other, and are then used as fluids, gels or foams. By providing a product bag, the compositions can be delivered as gels or as sprays. By dissolving propellant gases in the compositions, the materials can be delivered as foams, which have decreased density, and therefore can adhere to surfaces that previously have been difficult to coat with antiadhesion gels. Delivery systems can also provide mechanisms for expelling more product, and for directing the flow of materials leaving the delivery system. Bioresorbable, bioadhesive, anti-adhesion, and/or hemostatic compositions are useful in surgery to prevent the formation and reformation of post-surgical adhesions.

Abstract: The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.

Abstract: In accordance with the present invention there is provided a pharmaceutical composition useful for the treatment or prophylaxis of viral infections comprising tipranavir and at least one antiviral active compound of formula (I) wherein Base is selected from the group consisting of thymine, cytosine, adenine, guanine, inosine, uracil, 5-ethyluracil and 2,6-diaminopurine, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: A new class of synthetic glycosulfopeptides (GSPs) which have one or more sulfated tyrosine residues and a glycan linked to the peptide, the glycan preferably including a sialyl Lewisx group or a sialyl Lewisa group. In a preferred version the GSPs have an O-glycan comprising a ?1,6 linkage to a GalNAc. The present invention further contemplates in vitro methods of the synthesis of these GSPs without the use of the cells and methods of their use in vivo as powerful anti-inflammatory antithrombotic, or anti-metastatic compounds. The invention also contemplates a method of synthesizing oligosaccharides by cleaving the glycan from the GSP.

Abstract: The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula: Wherein substitutions at R1, R2, R3—R12, and Y are set forth in the specification.

Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.

Abstract: Compounds, compositions and methods for treating conditions characterized by leukocyte rolling are described. The compounds contain glycosulfopeptide structures comprising sulfated tyrosines and sialyated, fucosylated N-acetyllactosamino glycans. The glycosulfopeptides may be conjugated or complexed to other compounds for enhancing serum half-life or for controlled release, for example. Examples of conditions treated include inflammation, ischemia-reperfusion injury, rheumatoid arthritis, atherosclerosis, leukocyte-mediated lung injury, restenosis, and thrombosis.

Abstract: A stimuli-responsive, hybrid hydrogel wherein the bulk of the polymer is made up of relatively inexpensive water soluble polymer strands crosslinked by protein domains. The responsiveness of the gel is controlled or modulated by the protein component. The physical and biological properties of the hydrogel are determined by specifically designed or engineered protein domains. The crosslinking of the protein domains to the water soluble polymers is by means of non-covalent bonding such as chelation or coordination bonding, biotin-avidin bonding, protein—protein interaction and protein-ligand interaction, or by means of covalent bonding. Methods of making and using the polymer-protein hydrogels are disclosed in this application.

Abstract: The invention provides compounds having increased or reduced immunostimulatory effect, said compounds comprising a CpG dinucleotide and an immunomodulatory moiety wherein the increased or reduced immunomodulatory effect is relative to a similar compound lacking the immunomodulatorv moiety.

Abstract: Compositions and methods are provided for prevention and clinical treatment of various forms of graft-versus-host disease (GVHD) by using inhibitors of adenosine deaminase (ADA). In particular, various formulations and dosing regimens of ADA inhibitors such as pentostatin are provided for the treatment of all forms of GVHD, especially steroid-refractory acute and chronic GVHD.

Abstract: Novel amino-modified polysaccharides are provided. The amino-modified polysaccharides have one or more amino groups, each being linked to one or more arginine residues.

Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.

Abstract: A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising niacin-bound chromium that prevents or reduces the symptoms. Compositions incorporating niacin-bound chromium and additional compounds also are disclosed that are particularly effective in synergistically preventing or reducing these symptoms.

Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: Pharmaceutical formulations, kits and vessels are provided for delivering decitabine to a patient suffering from a disease in need of treatment with decitabine. The pharmaceutical formulation comprises decitabine solvated in a non-aqueous solvent that comprises glycerin, propylene glycol, polyethylene glycol, or combinations. Such formulations are more chemically stable than conventional liquid formulations of decitabine containing more than 40% water in volume. The pharmaceutical formulations can be used for any disease that is sensitive to the treatment with decitabine, such as hematological disorders and cancer.

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: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4?-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: A synthetic oligonucleotide comprising a C-5 methylcytosine and which recognizes and binds an allosteric site on DNA methyltransferase thereby inhibiting DNA methyltransferase activity is disclosed. Also disclosed is a composition comprising a synthetic oligonucleotide of the invention. The composition is useful for inhibiting DNA methyltransferase activity, thereby inhibiting the methylation of DNA. The composition can be a pharmaceutical composition useful for treating disorders associated with methylation defects, such as cancer and certain developmental disorders. Also disclosed is a method of inhibiting methylation of DNA. The method involves contacting a DCMTase with a synthetic oligonucleotide of the invention in the presence of the DNA, thereby resulting in an enzyme/synthetic oligonucleotide complex. The presence of the complex prevents catalysis, thereby inhibiting DNA methyltransferase activity.

Abstract: Pharmaceutical formulations, kits and vessels are provided for delivering decitabine to a patient suffering from a disease in need of treatment with decitabine. The pharmaceutical formulation comprises decitabine solvated in a non-aqueous solvent that comprises glycerin, propylene glycol, polyethylene glycol, or combinations. Such formulations are more chemically stable than conventional liquid formulations of decitabine containing more than 40% water in volume. The pharmaceutical formulations can be used for any disease that is sensitive to the treatment with decitabine, such as hematological disorders and cancer.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure

Abstract: This invention provides compounds having excellent antitumor activity, which are represented by the following formulae in which R1, R2, R3, m, n and R4 have the significations as given in the specification.

Abstract: A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising niacin-bound chromium that prevents or reduces the symptoms. Compositions incorporating niacin-bound chromium and additional compounds also are disclosed that are particularly effective in synergistically preventing or reducing these symptoms.

Abstract: The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.

Abstract: The present invention relates to a combination comprising (a) an adenosine A2a receptor agonist as define herein and (b) an adrenergic ?2 receptor agonist, for simultaneous, sequential or separate administration by the inhaled route in the treatment of an obstructive airways or other inflammatory disease.