Abstract: This invention provides a method of treating a subject suffering from a dermatologic condition, including, inter alia, psoriasis, contact dermatitis, and seboreic dermatitis, the method includes the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from a dermatologic condition.

Abstract: Compositions and methods for treatment of disease with acetylated disaccharides and analogs thereof are provided.

Abstract: The invention provides compounds of Formula (Ia) or pharmaceutically acceptable salts thereof, as well as the preparation, compositions and uses thereof, where R1, R2, R3, and m are defined as described above.

Abstract: The present invention relates to the discovery of polypeptide biomarkers excreted into the blood stream (serum or plasma) and/or urine from adipocytes and their use to determine the existence of metabolic syndrome (prediabetic) and/or diabetic conditions (including type 2 diabetes) including insulin resistance and/or glucose intolerance, their use to monitor the state of metabolic syndrome or diabetes toward a state of control and/or cure of the disease state or condition and their use to monitor the long-term health of the patient by determining the existence of metabolic syndrome (prediabetic conditions insulin resistance and/or glucose intolerance) or the existence of type 2 diabetes and to identify potential antidiabetes agents. Methods of identifying potential agents to be used in the treatment of metabolic syndrome and/or type2 diabetes and assays for assisting in the diagnosis of metabolic syndrome and/or type 2 diabetes are additional aspects of the invention.

Abstract: The present invention provides methods of producing libraries of compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides a library of neoglycoside digitoxin analogs that includes compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.

Abstract: The present invention provides 5?-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5?-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.

Abstract: The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.

Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.

Abstract: The invention is based on the discovery that specific dosages of pyrimidine compositions, such as uridine compositions, can be used to treat patients diagnosed with bipolar disorder.

Abstract: The present invention relates to new compositions of (active) solid lipidic particles (SLP), e.g. for inhalation, and their use as carriers or as fillers in pharmaceutical compositions. It also relates new formulations obtained by mixing a SLP composition of the invention and a (micronized) active compound. It further relates to a method for fabricating said compositions of (active) solid lipidic particles.

Abstract: The invention is directed to 5-amino-3-(3?-deoxy-?-D-ribofuranosyl)-thiazolo[4,5-d]pyrimidin-2,7-dione prodrugs, whose metabolized parent compound has immunomodulatory activity. The invention also relates to the therapeutic use of such prodrugs and pharmaceutical compositions thereof in treating disease states associated with abnormal cell growth, such as cancer.

Abstract: Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.

Abstract: A complex consisting of galectin-3 and chondroitin oligosaccharide and methods for seperating and detecting the chondroitin oligosaccharide in a sample using the immobilized complex.

Abstract: The present invention provides a method for increasing the efficacy of antifolates which act via inhibition of dihydrofolate reductase (DHFR). The method comprises the steps of administration of 5-amino-4-imidazolecarboxamide riboside (Z) or its base with the antifolate such that the targeted cells are exposed to both the antifolate and Z simultaneously. This results in increased influx of the antifolate. For MTX, accumulation of the more biologically active polyglutamate forms is also potentiated. This potentiation appears to be mediated by an effect on the RFC.

Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with fluorine, method for producing the same, drugs containing said compounds and use thereof.

Abstract: The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5?-methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.

Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.

Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives with improved properties, method for producing the same, drugs containing said compounds and use thereof.

Abstract: The present invention relates to novel sequences for use in diagnosis and treatment of carcinomas, especially breast cancers. In addition, the present invention describes the use of novel compositions for use in screening methods. The invention provides compositions and methods associated with altered expression of PRLR in cancer.

Abstract: The present invention relates to compounds of Formula I, II or III, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a ?-galactosidase inhibitor or a glycolipid metabolic disorder treating agent. Wherein each of R1 and R2 independently represents H, an alkyl group, an acyl group, an aryl group or an aralkyl group, with the proviso that both are not H at the same time, and each of R3, R4, R5 and R6 independently represents a hydroxyl group or hydroxyl group having a substituent. Also, R7 represents an alkyl group, and each of R8, R9, R10 and R11 independently represents a hydroxyl group or a hydroxyl group having a substituent.

Abstract: The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts.

Abstract: In one embodiment, the invention provides a method of suppressing, inhibiting, preventing, or treating conjunctivitis in a subject, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound via an ester or amide bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof to a subject with conjunctivitis.

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

Abstract: The present invention provides methods for identifying target genes whose partial or complete functional inactivation potentiates the activity of an antibiotic agent, e.g., a quinolone antibiotic. The invention further provides methods for identifying agents that modulate expression of target genes or that modulate activity of expression products of target genes. Agents identified according to various methods of the invention potentiate the activity of antibiotics such as quinolones, aminoglycosides, peptide antibiotics and ?-lactams. Also provided are agents that suppress and/or retard resistance to antibiotics. The inventive methods provide potentiating agents and compositions comprising potentiating agents and antibiotics. Such agents and compositions can be used for inhibiting growth or survival of a microbial cell or of treating a subject suffering from or susceptible to a microbial infection.

Abstract: The invention provides methods for treating or suppressing tobacco or nicotine usage or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.

Abstract: The present invention provides pharmaceutical compositions comprising: (a) a modulator of hepatic parasympathetic tone, (b) at least one diabetes drug, and (c) a pharmaceutically acceptable carrier. The present invention includes methods for the treatment and/or prevention of insulin resistance, type 2 diabetes, impaired glucose intolerance, and other associated disorders with pharmaceutical compositions described herein. The invention also provides for a kit comprising a pharmaceutical composition and instructions for its use.

Abstract: Physical forms of beta-L-2?-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2?-deoxythymidine can be used in the manufacture of other forms of beta-L-2?-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.

Abstract: The 3?-L-valine ester of ?-D-2?-C-methyl-ribofuranosyl cytidine provides superior results against flaviviruses and pestiviruses, including hepatitis C virus. Based on this discovery, compounds, compositions, methods and uses are provided for the treatment of flaviviridae, including HCV, that include the administration of an effective amount of val-mCyd or its salt, ester, prodrug or derivative, optionally in a pharmaceutically acceptable carrier. In an alternative embodiment, val-mCyd is used to treat any virus that replicates through an RNA-dependent RNA polymerase.

Abstract: The invention provides carbohydrate based compounds, methods of preparation, and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a carbohydrate based compound of the invention having a core structure comprising of one or more sugar moieties. The carbohydrate based compounds are useful for inhibiting immune stimulation involving TLR ligands, especially TLR4 and TLR2. The compounds also are suitable for inhibition of inflammatory conditions resulting from infections. The compounds have use in the treatment of inflammation, autoimmunity, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

Abstract: The present invention relates to fluorine-containing monosaccharides that are useful for forming extracellular fluorinated glycoconjugates. Methods of forming extracellular fluorinated glycoconjugates comprise the steps of contacting a cell with a fluorine-containing monosaccharide, and incubating the cell under conditions whereby the cell internalizes the fluorine-containing monosaccharide, or a derivative thereof, on the surface of the cell. The present invention also relates to the use of a fluorine-containing monosaccharide in cellular imaging using fluorine NMR. The invention additionally relates to the use of fluorine containing monosaccharides in the treatment of cancer and inflammatory disease.

Abstract: This invention relates to anticancer therapy and more precisely to the immunological control of cancer. Specifically this invention relates to pharmaceutical compositions incorporating as the active ingredient at least one immuno-stimulating agent with charged or central groups of general formula I wherein X, Y, A, B, R1 and R2 are as defined in the specification together with a radiotherapy method suitable to fight cancer or together with a known antineoplastic chemotherapeutic agent selected from the group consisting of alkylating agents, anti-metabolic agents, agents acting on tubules and tyrosine Kinase inhibitors in conjunction or admixture with an inert non toxic pharmaceutically acceptable diluent or carrier. This invention also relates to the salts of a compound of general formula I with a mineral or organic base, namely a pharmaceutically-acceptable base.

Abstract: An antimicrobial additive composition is provided which economically and efficiently imparts antimicrobial characteristics to acrylic polymers, and particularly thermoformable acrylic sheets made from such polymers. The antimicrobial composition comprises an alkyl dimethyl ammonium saccharinate, an oxathiazine, an azole, an isothiazoline, a chlorothalonil, and/or mixtures thereof, among others.

Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described herein.

Abstract: The invention relates to peptide nucleic acid (PNA) conjugates which can be used for treating diseases correlated with HIV, wherein the peptide nucleic acid (PNA) inhibits the gene expression of HIV. The conjugates comprise the following components: (a) a transport mediator for the cell membrane, (b) an address protein or peptide for the import into the cell nucleus, and (c) a peptide nucleic acid (PNA) which is to be transported and can be hybridized with an HIV gene and can inhibit the expression of the HIV gene.

Abstract: The present invention provides methods of treating gastrointestinal inflammation, methods of treating inflammatory bowel disease, methods of treating Crohn's Disease, and methods of treating ulcerative colitis in an individual. The methods generally involve administering an effective amount of an agent that increases the level of a Type I interferon and/or that activates a Type I interferon signaling pathway in the individual.

Abstract: Disclosed are compositions and methods for modulating odor sensitivity, as well as screening methods for detecting compounds that modulate odor sensitivity.

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: The present invention provides 5?-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5?-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.

Abstract: The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R4 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention is directed to carbonate and carbamate prodrugs of thiazolo[4,5-d]pyrimidine compounds, whose metabolized parent compound has immunomodulatory activity. The invention also relates to the therapeutic use of such prodrugs and pharmaceutical compositions thereof in treating disease states associated with abnormal cell growth, such as cancer.

Abstract: Described herein are methods for the noninvasive immunization of a subject that involve alkyl glycosides. Also described herein are compositions, kits, and devices for the noninvasive immunization of a subject.

Abstract: The present invention provides methods for treating infections, in a host, by viruses belonging to the Flaviviridae family, such as HCV, comprising administering an Ara-C homologue to the host.

Abstract: A compound of the formula: wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl grou

Abstract: The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compounds—Free-B-ring flavonoids and flavans—for use in the prevention and treatment of diseases and conditions mediated by the COX-2 and 5-LO pathways. The present invention further provides a novel method for simultaneously inhibiting the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) enzymes, and reducing cox-2 mRNA production. Finally, the present invention includes a method for weight loss and blood glucose control. The methods of this invention are comprised of administering to a host in need thereof an effective amount of the composition of this invention together with a pharmaceutically acceptable carrier.

Abstract: The present invention provides methods of producing libraries of compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides a library of neoglycoside digitoxin analogs that includes compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.

Abstract: This invention provides compounds and methods of use thereof in suppressing, inhibiting, preventing, or treating a pathogenic effect on a cell, including, inter alia, infection with intracellular pathogens. Also provided are compounds and methods of use thereof in suppressing, inhibiting, preventing, or treating an infection in a subject.

Abstract: Disclosed are novel methods of treatment for retinal diseases and conditions including age-related macular degeneration, genetic-based retinal degenerations and retinal detachment. A novel glycan binding protein thought to be a cell surface receptor has been discovered in the retina. The retinal glycan binding receptor is shown to play an important role in promoting assembly of outer segment (OS) membranes by the photoreceptor cells of the eye, a process that is essential for vision. Based on the finding that certain sugars can bind with very high affinity to the retinal glycan receptor and stimulate its function, the invention provides novel therapeutic agents for treatment of retinal diseases that are multivalent N-linked glycans. Preferred pharmaceutical compositions in accordance with the present invention comprise active agents having the general formula: (Gal-GlcNAc)n-Man3-GlcNAc2, where n is 1-4.

Abstract: The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening/diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPAR?2, LPL and ?P2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual.