Abstract: Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress N—CoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death.

Abstract: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.

Abstract: Methods of using dronedarone or a pharmaceutically acceptable salt thereof for the treatment of patients with arrhythmia, said patients having an increase of creatinine level due to dronedarone administration, said creatinine level increasing following dronedarone treatment initiation, said creatinine level increase reaching a plateau and being used as a new baseline, said creatinine level increase being reversible after dronedarone discontinuation.

Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: The present invention relates to modulators of metalloproteinase activity.

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: A novel compound, a novel ?1 adrenergic receptor antagonistic agent, and a novel composition are provided which are capable of exerting a therapeutic effect on treatment of hypertension as well as treatment of prostatic hypertrophy and the like.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: A plaster including a backing layer and a drug layer laminated on the backing layer, where the drug layer contains an adhesive base and at least one compound selected from the group consisting of citalopram and pharmaceutically acceptable salts thereof, an abundance ratio of the S form being greater than an abundance ratio of the R form.

Abstract: It is intended to clarify a transportation system participating in the uric acid uptake in vascular smooth muscle cells (VSMCs) and provide a novel remedy, a preventive or a treating agent for vascular disorders, hypertension and renal disorders with the use of a drug participating in this transportation system. It is also intended to provide a novel screening system for a remedy, a preventive or a treating agent for vascular disorders, hypertension and renal disorders with the use of such a transportation system.

Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.

Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.

Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.

Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, A, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.

Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders

Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, compositions containing such compounds and the uses of such compounds as antiparasitic agents.

Abstract: The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I): wherein the radicals and symbols have the meanings as defined in the specification, for the preparation of a medicament for the treatment of lymphoproliferative diseases, in particular, cutaneous T-cell lymphomas.

Abstract: Antifungal compounds having a benzofuran structure. Antifungals exhibit much less toxicity to human cells than amiodarone. These compounds are useful alone or in combination with other compounds having antifungal activity. Compounds of this invention exhibit synergistic antifungal activity in combination with antifungal amiodarone compounds. The invention provides pharmaceutical compositions useful for treating fungal infections, methods for treating fungal infections and compounds useful in such compositions for treating fungal infections. Compounds of this invention are further useful as antifungal agents for the prevention and or treatment of fungal infections in plants. The invention includes agriculturally useful compositions comprising one or more compounds of this invention which exhibit fungistatic or fungicidal function against one or more plant pathogen is a fungus.

Abstract: Described herein are compositions and methods for treating a subject suffering from a non-localized inflammatory condition (or any symptoms associated with such inflammation), including systemic inflammation, and inflammatory conditions affecting the large portions of or the whole body, or sepsis by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor. Also described herein are methods for decreasing iNOS and cytokine expression by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor.

Abstract: The present invention relates to a method of treating a central nervous system disorder, such as a mood disorder (e.g., major depressive disorder) or an anxiety disorder (e.g., general anxiety disorder, social anxiety disorder, post traumatic stress disorder, and panic disorder) with a low dose combination of escitalopram and bupropion.

Abstract: A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g.

Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: Soybean volatile compounds, soybean aphid-induced volatile compounds and soybean aphid sex pheromones are semiochemicals of the invention used to suppress soybean aphid population. Methyl salicylate is an embodiment of a soybean aphid-induced volatile compound useful in the invention. Benzaldehyde is an embodiment of a soybean host plant volatile compound useful in the invention. Also useful as sex pheromones are nepetalactol and nepetalactone. The compounds may be blended in a preferred embodiment.

Abstract: This invention relates to lithospermate B (‘LAB’ hereinafter) that inhibits proliferation and migration of vascular smooth muscle cells (‘VSMC’ hereinafter). More specifically, this invention relates to a pharmaceutical composition comprising LAB isolated from Salviae miltiorrhiza as an active ingredient for treating atherosclerosis.

Abstract: Certain novel (dihalopropenyl)phenylalkyl substituted benzodioxolane and benzodioxane derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: where R through R10, inclusively, x, A, B, y, D, E, G and M are fully described herein. Preferred compounds of the present invention are those wherein the benzofused ring moiety is attached to the remainder of the molecule at the positions designated as 1- or 2-. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.

Abstract: This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O?X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.

Abstract: Disclosed are methods of treating cancer comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound of Formula VI. The animal is a mammal, preferably a human or a rodent.

Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: A method of treating depression comprising administering a melatonin agonist.

Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Abstract: Cell growth is inhibited and/or cell death is induced in a cell by administering an RXR agonist and an inhibitor of casein kinase 1?. A cell or a tissue can be screened for enhanced susceptibility to cell death or interference with cell growth. Conditions characterized by uncontrolled cell growth or proliferation, such as a cancer, can be treated with inhibitors of casein kinase 1?.

Abstract: The present invention relates to a method of treating a central nervous system disorder, such as a mood disorder (e.g., major depressive disorder) or an anxiety disorder (e.g., general anxiety disorder, social anxiety disorder, post traumatic stress disorder, and panic disorder) with a low dose combination of escitalopram and bupropion.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse.

Abstract: A chemotherapeutic composition can be configured for subcutaneous administration for preferential intralymphatic accumulation while also providing a therapeutic systemic concentration that is not toxic. The composition can include a pharmaceutically acceptable carrier, and a nanoconjugate configured for preferential intralymphatic accumulation after subcutaneous administration. The nanoconjugate can include a nanocarrier configured for preferential intralymphatic accumulation after subcutaneous or interstitial administration, and a plurality of chemotherapeutic agents coupled to the nanocarrier. The nanoconjugate can have a dimension of about 10 nm to about 50 nm. Also, the nanoconjugate can be loaded with the chemotherapeutic agents from about 10% to about 50% w/w. The nanocarrier can be a hyaluronan polymer of about 3 kDa to about 50 kDa. Alternatively, the nanocarrier can be a dendrimer.

Abstract: An insecticidal and fungicidal composition capable of controlling crop diseases and insect pests at the same time by combining an insecticidal active ingredient and a fungicidal active ingredient is provided. The insecticidal and fungicidal composition is characterized by comprising as active ingredients a compound represented by the general formula (1) or (2) and a compound represented by the general formula (3) or (4). wherein, in the formula, A1, A2, A3, and A4 independently represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom; G1 and G2 independently represent an oxygen atom or a sulfur atom; R1 and R2 independently a hydrogen atom or a C1-C4 alkyl group; Xs may be the same or different and represent a hydrogen atom, a halogen atom or a trifluoromethyl group; Q1 represents substituents such as a phenyl group, a heterocyclic group or the like; and Q2 represents substituents such as a phenyl group, a heterocyclic group or the like.

Abstract: The formulation provides a method of treating headaches, neck, joint and inflammatory-type pain in a mammalian subject by administering to the subject a therapeutically effective amount of a nitrate-containing compound and a therapeutically effective amount of a selenium-containing compound. The formulation also provides kits and systems for practicing the subject methods.

Abstract: The invention relates to an orally administrable mucoadhesive film which comprises one or more bioactive ingredients and, as a major film-forming polymer, at least one alginate which is capable of forming a low viscosity aqueous solution. Also provided is a process for preparing such films.

Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.

Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.

Abstract: The present invention is directed to the use of EP2 and/or EP4 agonists as therapeutics for the treatment of diseases associated with influenza A viruses, such as for example H5N1 and mutations thereof.

Abstract: A method for determining the appropriate medication for a patient suffering from depression. A patient will take a questionnaire wherein the patient answers a number of questions with scaled responses concerning the degree to which the patient's mental state is affected by at least one or both of impaired modulation and impaired activation. Next, the patient's answers will be processed to arrive at scores for the at least one impaired modulation and impaired activation. Depending upon the patient's scores for demodulation and deactivation, at least one medication which affects the at least one impaired modulation and impaired activation is recommended.

Abstract: The invention relates to a combination comprising (a) a compound selected from the class of prostaglandins and (b) a compound selected from the class of tubulin/microtubule interfering agents and/or (c) a compound selected from the class of cyclooxygenase inhibitors.

Abstract: The present invention relates to pesticidal compositions comprising 2,3-dihydro-2,2-dimethylbenzofuran-7-yl(dibutylaminothio)methylcarbamate, namely benzofuranyl methylcarbamate, commonly known as carbosulfane, of structural formula (I). The present invention deals more particularly with compositions comprising this active compound at a high concentration, which makes it the most economical product for sale, more stable during storage and more effective in small quantities, and it may be further combined with one or more inerts. The present invention further discloses a process for preparing said compositions and a process for controlling insects/mites/nematode. The applications for these formulations include the treatment of seeds and leaves. In the latter case, in addition to the diluting agent, a mixture of anionic and non-ionic surfactants have been included in the formulation, so that the solution will become self-emulsifying upon being added to water.

Abstract: The invention provides compounds of formula (I) wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.