Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.

Abstract: Provided herein are methods of treating postangiplasty, in-stent restenosis or atherosclerosis in an individual in need of such treatment, comprising the step of administering to said individual an effective dose of morelloflavone with or with a effective dose of one or more of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent. Also provided are pharmaceutical compositions comprising a morelloflavone or pharmaceutical combinations comprising a morelloflavone and one of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent.

Abstract: The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.

Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R3 is —C(?B)C(?O)L or —C(R11R12)C(?O)L; R4 is, inter alia, H, C1-C4 alkyl or C2-C6 alkoxycarbonyl; or R3 and R4 are taken together as —C(?O)C(?O)—, —C(?NR13)C(?O)— or —C(R11R12)C(?O)—. B is O, NR13, NOR13 Or NNR14 R15; L is OH or NR14 R15; and X, R1, R2, R11, R12, R13, R14, R15 and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Hydrolysis of cyanopyridine may be reduced by use of picoline as a predominately non-aqueous quench fluid. The picoline quench fluid may also be a reactant in the manufacture of cyanopyridine.

Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.

Abstract: Methods and compositions are provided for reducing, treating or preventing pain and/or inflammation in a patient in need of such treatment, the methods and compositions comprising administering a therapeutically effective amount of a statin or pharmaceutically acceptable salt thereof to a target tissue site beneath the skin.

Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).

Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.

Abstract: The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years.

Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.

Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.

Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type I1 diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: A compound represented by the general formula 1 as described, a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a radio-labeled analog thereof (i.e. 18F, 124I, 11C, etc), and mixtures of any of the foregoing, for diagnosis or monitoring of a medical condition.

Abstract: The present invention relates to the use of metabotropic glutamate receptor 5 antagonists for the inhibition of transient lower esophageal sphincter relaxations. A further aspect of the invention is directed to the use of metabotropic glutamate receptor 5 antagonists for the treatment of gastroesophageal reflux disease, as well as for the treatment of regurgitation.

Abstract: This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents ?1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1,

Abstract: Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase.

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: There is provided a fluorine-containing organosulfur compound having an excellent control effect on harmful arthropods, which is represented by the formula (I): wherein m represents 0 or 1; n represents 0, 1 or 2; A represents an optionally substituted 6-membered aromatic heterocyclic group; R1 to R4 are the same or different and represent a hydrogen atom, a C1-C4 chain hydrocarbon group optionally substituted with a halogen atom, etc.; and Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom.

Abstract: Mast cell (MC) and peripheral blood basophil (PBB)-associated diseases are treated or prevented, or their symptoms are alleviated by the administration of water soluble fullerenes (buckeyballs) to the individual under conditions sufficient to inhibit MC and PBB responses. MC and PBB responses are associated with, for example, various allergies including Type 1 hypersensitivity initiated by IgE-antigen, arthritis, multiple sclerosis, urticaria, atopic dermatitis, heart disease, etc. The treatment regimen can be enhanced using Chimeric fullerenes that specifically home to and inhibit MC and PBB cells. These molecules, for example, comprise fullerenes to which are attached IgE Fc or stem cell factor (SCF) peptides that bind to receptors specifically on MC and PBB cells. Additional molecules which may be used in the processes include IgE Fc or SCF peptides with several fullerenes covalently attached.

Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.

Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than

Abstract: Disclosed herein are a novel cinnamaldehyde compound represented by Chemical Formula 1 or pharmaceutically acceptable salts thereof. The cinnamaldehyde compound has improved solubility in water and has inhibitory effects on the growth of cancer cells because it induces cell cycle arrest and cell death. Also disclosed are a method of preparing the cinnamaldehyde compound and an anticancer composition including the compound of Chemical Formula 1.

Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.

Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

Abstract: The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: —(CH2)1-4—, (C2-C4)-alkenyl, (C2-C4)alkynyl, —S—(CH2)1-3—#, and —(CH2)1-3—O—#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: —(CH2)2-4—, —S—(CH2)1-3#, and —O—(CH2)1-3—#; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: —OR4. The compounds of formula (I) are useful in the treatment of cancer.

Abstract: A process for the preparation of a pharmaceutical composition comprising a homogeneous or substantially homogeneous mixture of citric acid, magnesium oxide, potassium bicarbonate and sodium picosulphate and, optionally, saccharin sodium and/or orange flavour; products, intermediate products, and uses thereof.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein each W and Y is independently CH2, O, C(?O), S(?O)n, NR8 or a direct bond; R4 is H, halogen, cyano, hydroxy, C1-C2 alkyl, C1-C2 haloalkyl, C2 alkenyl, C2 haloalkenyl or C2 alkynyl; m is an integer selected from 0, 1, 2, 3, 4 and 5; and R1, R2, R3, R5, R8 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The present invention shows that cilostazol, a phosphodiesterase 3 inhibitor has additional beneficial effects to atorvastatin on myocardial remodeling by inducing and preserving eNOS phosphorylation. The present invention demonstrates a cardioprotective effect of Cilostazol indicating the therapeutic potency of this drug. In addition, the present invention demonstrates that the additional effect of Cilostazol and atorvastatin therapy against ischemia injury is due to the augmentation of phosphatodylicositol 3-kinase/AKT (PI3-/AKT), PKA and p-eNOS signaling.

Abstract: The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions.

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.

Abstract: A highly safe and effective prophylactic/ameliorating or therapeutic agent for NACH and the method for using the same are provided. A prophylactic/ameliorating or therapeutic agent for NASH containing a combination of at least one first ingredient selected from the group consisting of an ?3PUFA and pharmaceutically acceptable salts and esters thereof and at least one second ingredient selected from the group consisting of (a) a biguanide hypoglycemic agent, (b) a nonsteroidal anti-inflammatory drug, (c) a 3-hydroxy-3-methyl glutaryl coenzyme A reductase inhibitor, and (d) an angiotensin II receptor blocker as the active ingredients; and its method of use.

Abstract: This invention relates to novel 4-benzhydryl-tetrahydro-pyridine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rband Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A method of colon cleansing that provides superior cleansing. In an embodiment, superior cleansing of the right colon is provided. In an embodiment, a stimulant laxative is consumed at least two days prior to the day for which maximum cleansing is desired, and an osmotic purgative is consumed one day prior to the day for which maximum cleansing is desired. A regimen that administered PICO-SALAX® plus BISACODYL™ was superior in cleansing the right colon compared to PICO-SALAX® alone, and when compared to Oral Sodium Phosphate. Patient tolerability and safety were excellent.

Abstract: Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(=Q1)- (wherein Q1 represents oxygen, sulfur or ?N—R11 (wherein R11 represents hydrogen or C1-6 alkyl)) and nitrogen, etc.; and Z1 represents piperidin-diyl, etc.], salts thereof and hydrates of the foregoing.

Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing a cardiovascular-related disease in subject in need thereof.

Abstract: The present invention provides methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and methods of screening for compounds that modulate A? levels. The invention also provides modulation of A? levels via selective modulation (e.g., inhibition) of ATP-dependent ?-secretase activity. The invention also provides methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a modulator of ?-secretase, including, but not limited to, a selective inhibitor of ATP-dependent ?-secretase activity or an agent that decreases the formation of active (or optimally active) ?-secretase. The invention also provides the use of inhibitors of ATP-dependent ?-secretase activity to prevent, treat or ameliorate the symptoms of Alzheimer's disease.

Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

Abstract: The inventors have found that both the drug dose and drug release profiles are significant factors for the safety and efficacy of drug coated stents. The inventors have identified optimum dosing and release kinetics for drug coated stents. In particular, the inventors have determined dosing and release kinetics that permit the delivery of the lowest effective drug dosage, thus enhancing patient safety and minimizing any side effects from the drug.