Abstract: This application describes pharmaceutical compositions, kits, and methods for inhibiting cell proliferative disorders, especially those disorders characterized by overactivity and/or inappropriate activity of a receptor tyrosine kinase, including Her2 related cancers, and methods for imaging an Her-2 expressing tumor.

Abstract: The present invention provides methods and compositions for modifying fertility in a male mammalian subject by contacting the subject's testis cells, germ cells or sperm with a sufficient amount of a composition comprising a ligand that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Also described are methods for screening a test molecule for its effect on fertility by examining changes in male germ cells, testis cells or sperm resulting from contact with a molecule that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Compositions for modifying fertility in a mammalian subject, e.g., contraceptive products, include a ligand that binds, inhibits or activates a TAS2R receptor in a pharmaceutically acceptable carrier.

Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

Abstract: A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the following formula or its salt: wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2? is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2? is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2? and R2? optionally form a condensed ring containing an oxygen atom and (b) at least one other fungicide.

Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.

Abstract: This application describes pharmaceutical compositions, kits, and methods for inhibiting cell proliferative disorders, especially those disorders characterized by overactivity and/or inappropriate activity of a receptor tyrosine kinase, including Her2 related cancers, and methods for imaging an Her-2 expressing tumor.

Abstract: Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.

Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.

Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. Because their mechanism of action does not involve killing of bacteria or inhibiting their growth, the potential for these compounds to induce drug resistance in bacteria is minimized. Through inhibiting bacterial virulence, the present invention provides a novel means of treating bacterial infections.

Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives. In particular, the invention relates to the compounds of the formula I wherein the radicals have meanings described herein, and to their physiologically tolerated salts and to processes for their preparation. The compounds are suitable for example as antidiabetics.

Abstract: Anti-microbial compositions comprising certain imidazolium ionic liquids and non-ionic or anionic surfactants and methods of using said compositions in the preservation of personal care and cosmetic applications are provided.

Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response.

Abstract: Inhibiting the enzymic action of tyrosinase in the melanocyte prior to, during, or after ultraviolet (UV) radiation exposure, including over-exposure causing erythema, or sunburn, prevents the production of melanin and thereby melanoma. Melanoma can be prevented by using a tyrosinase inhibitor agent that inhibits the enzymic action of tyrosinase to prevent damage and/or death of melanocytes. The inhibitor agent can be applied to the skin or ingested.

Abstract: Disclosed is a medicament comprising N-aryl N? morpholino/piperidino thiocarbamide derivatives represented by the following formula 1 for preventing and treating diabetes, diabetic complications, insulin resistance and insulin resistance syndrome, and can be used in drugs, foods, and beverages inducing an effect of preventing and treating diabetes, diabetic complications, insulin resistance and insulin resistance syndrome of modern people who suffer from the increasing development of diabetes resulting from environmental factors, such as intake of westernized foods, obesity, and so on: wherein, X is O or C, and R represents 4-chlorophenyl, 2-methylphenyl, 3-methoxypheny, 3-methylphenyl, or phenyl group.

Abstract: The present application discloses thiourea compounds for use in the treatment of infections. The thiourea compounds have formula (I) wherein X1 and X2 each designate one or more substituents; and Z is —(CHR)—, —(CHR)2—, —O—(CHR)2—, —NH—(CHR)2—, or —S—(CHR)2—; including salts thereof.

Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p

Abstract: The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments.

Abstract: The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.

Abstract: The invention relates to novel specifically trifluoromethyl and halogen substituted 1,3-diphenyl ureas and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects like the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.

Abstract: A method for treating a neurodegenerative condition, in an animal of the mammalian species, including humans, comprising the step of administering to ganglion cells and their axons (optic nerve) of said mammal a pharmaceutical composition which comprises as its active ingredient one or more compounds having activity for blocking a reverse mode of the sodium/calcium exchanger.

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.

Abstract: A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.

Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives. In particular, the invention relates to the compounds of the formula I wherein the radicals have meanings described herein, and to their physiologically tolerated salts and to processes for their preparation. The compounds are suitable for example as antidiabetics.

Abstract: Disclosed herein are compositions and methods used to modulate a NH2-terminal Jun Kinase activity. These compositions and methods can be employed to regulate metabolic disorders associated with, for example, insulin such as diabetes. The reduction in NH2-terminal Jun Kinase activity can lead to the reduction in weight and improve insulin sensitivity.

Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p

Abstract: The present invention is directed to compounds and methods suitable for the treatment of HIV infection.

Abstract: 1-(3-methoxybenzyl)-3-substituted thiourea antioxidant compounds and improved lipids compositions which are supplemented with amounts of such antioxidant compounds effective for augmenting oxidative stability of the base lipid are provided. Also provided are methods for enhancing the oxidative stability of a lipid comprising supplementing a base lipid in need of enhanced oxidative stability with at least one 1-(3-methoxybenzyl)-3-substituted thiourea compound of the present invention.

Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.

Abstract: 1-(3-methoxybenzyl)-3-substituted thiourea antioxidant compounds and improved lipids compositions which are supplemented with amounts of such antioxidant compounds effective for augmenting oxidative stability of the base lipid are provided. Also provided are methods for enhancing the oxidative stability of a lipid comprising supplementing a base lipid in need of enhanced oxidative stability with at least one 1-(3-methoxybenzyl)-3-substituted thiourea compound of the present invention.

Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Abstract: The present invention provides N-aryloxypropanolyl-N?-phenethyl-urea derivatives of formula 3, method for their preparation and use thereof as potent appetite suppressants for treatment of obesity wherein R is selected from the group consisting of H, 2, 3 or 4-trifluoromethyl, 2, 3, or 4-chloro, 2, 3, or 4-bromo, 4-acetyl, 4-propionyl, 4-acetamido, 2,3 or 4 methoxy, 4 nitrile, 2,3 or 4-methyl, and 4 formyl and X is S or O.

Abstract: The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXR? selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXR?-selective antagonist.

Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: Novel antagonists of ∝4&bgr;1 integrin and/or ∝4&bgr;7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.

Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I 1

Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.