Abstract: Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.

Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.

Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.

Abstract: Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder.

Abstract: The present invention provides a composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1) and ethaboxam.

Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B??(I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: Stable pharmaceutical compositions of famotidine and ibuprofen in a single unit dosage form are disclosed herein. The compositions comprise a famotidine core having a reduced or minimal surface area surrounded by a layer of ibuprofen. In some embodiments, the ibuprofen is in direct physical contact with the famotidine.

Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.

Abstract: Stable pharmaceutical compositions of famotidine and ibuprofen in a single unit dosage form are disclosed herein. The compositions comprise a famotidine core having a reduced or minimal surface area surrounded by a layer of ibuprofen. In some embodiments, the ibuprofen is in direct physical contact with the famotidine.

Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract: The present invention provides: a composition for controlling plant diseases comprising, as active ingredients, 4-oxo-4-[(2-phenylethyl)amino]-butyric acid and ethaboxam; a method for controlling plant diseases which comprises applying effective amounts of 4-oxo-4-[(2-phenylethyl)amino]-butyric acid and ethaboxam to a plant or soil for growing plant; and so on.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: An inexpensive, easily available, and convenient method of treating or preventing a virus infection is provided. The present invention relates to a method for the treatment or prevention of virus infections using polybiguanide-based compounds administering a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof The invention relies on the unique biochemical reaction in which polybiguanide-based compounds interfere with the spread of virus within or between organisms. The compositions and formulations described in the present invention are effective means to reduce the infectivity of the human immunodeficiency virus type 1 (HIV-1), and human herpes simplex viruses, and also to kill the causative organisms of many other sexually transmitted diseases (STDs).

Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.

Abstract: Compositions and methods are provided for predicting inhibitors of protein targets related to treatment of infectious disease, for example, bacterial, viral, or parasitic diseases. Methods are provided for predicting inhibitors of protein targets related to treatment infectious disease, for example, microbial disease, utilizing a docking with dynamics protocol to identify inhibitors, or utilizing a protein structure energy function to identify peptide or peptidomimetic inhibitors.

Abstract: A trilayer osmotic tablet is described. The tablet includes a core, a semi-permeable membrane disposed generally around the core, and an orifice in the semi-permeable membrane in fluid communication with the core. The core includes first, second, and third layers. The first layer is in fluid communication with the orifice. The second layer includes a therapeutically effective dose of a drug and is located adjacent to the first layer. The third layer is located adjacent the second layer. The tablet may include a coating having therapeutically effective doses of at least one additional drug disposed in the coating that generally surrounds the semi-permeable membrane. The at least one additional drug in the coating may be the same or different from the drug in the trilayer core. Methods for treating epilepsy, psychiatric disorders, asthma, and peptic ulcer disease by administering these compositions are also described.

Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

Abstract: The present invention is directed to, inter alia, methods of treating or ameliorating an effect of a polycystic disease. This method include administering to a patient in need thereof an amount of a modulator of a histone deacetylase (HDAC) path-way, which is sufficient to treat or ameliorate an effect of a polycystic disease, particularly a polycystic kidney disease.

Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.

Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.

Abstract: An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and/or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage for in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract: Methods of treating a subject having, or at risk of having, a myeloproliferative disorder are provided according to embodiments of the present invention which include administering a therapeutically effective amount of an arachidonate 5-lipoxygenase (5-LO) inhibitor to the subject. Combinations of therapeutic agents are administered according to embodiments of the present invention. In some embodiments, two or more 5-LO inhibitors are administered to a subject to treat a myeloproliferative disorder. In further embodiments, at least one 5-LO inhibitor and at least one additional therapeutic agent are administered to a subject to treat a myeloproliferative disorder. Methods of inhibiting leukemia stem cells are provided according to embodiments of the present invention which include contacting leukemia stem cells with an effective amount of an arachidonate 5-lipoxygenase inhibitor.

Abstract: The invention provides a process for preparing non-crystalline organic compositions and non-crystalline, co-amorphous blends of organic compounds.

Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.

Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds 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. These infectious diseases include viral infections, particularly HCV infections.

Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention generally relates to aqueous seed treatment formulations comprising a pesticidal agent, a polyvinyl alcohol (PVA), a graft copolymer, and a plasticizer. In one embodiment of the invention, PVA-compatible polymer emulsions are employed. The present invention also relates to uses of the disclosed compositions for protecting seeds from pests.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, of Formula (I) wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment of type II diabetes.

Abstract: The present invention relates to novel thiazole-based compounds and T-type calcium channel inhibitors containing the compound. The T-type calcium channel inhibitor of the present invention is useful as a treating agent for disease associated with overexpression of T-type calcium channel.

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a maximum blood drug concentration (Cmax) when administered in a fasted state is 400 ng/mL or less, is disclosed.

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).

Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.

Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.

Abstract: The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: The invention concerns a composition for the treatment of varroa mite infestations in honeybee colonies, comprising a base layer and an active layer, wherein the active layer comprises an effective amount of an acaricidal compound.