Abstract: The invention disclosed relates to methods and models for enhancing stress-induced analgesia through non-opioid mechanisms.

Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.

Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.

Abstract: The disclosure provides that components of a PTEN cell signaling pathway may be utilized as therapeutic targets for treating, preventing, slowing the progression of or delaying the onset of a neurodegenerative disease or disorder. Such components that may be targeted include, phosphatase and tensin homologue (PTEN), glycogen synthase kinase 3 beta (GSK3?), and AKT. The subject matter disclosed herein relates to the therapeutic use of inhibitors of PTEN, inhibitors of GSK3?, or activators of AKT to treat a neurodegenerative disease or disorder in a subject. Compounds are disclosed which may be used in the methods provided.

Abstract: The present invention discloses methods for the diagnosis and treatment of autism. The diagnostic tools provided use analysis of levels of G-protein expression, oxytocin, and vasopressin. Treatment for autism spectrum disorder and symptoms of autism spectrum disorder, especially repetitive behavior, is also provided.

Abstract: The invention relates to compounds of formula I: along with pharmaceutical compositions containing the same and methods of use thereof for the treatment of autoimmune disease.

Abstract: Provided are methods for treatment and prophylaxis of convulsive disorders and seizures, such as epilepsy and febrile seizures, by modulating TRPV1 channel activation.

Abstract: An object of the present invention is to provide a gradual disintegration-type, sustained-release pharmaceutical solid preparation whose pharmacologically active substance release behavior is controlled. The solid pharmaceutical preparation of the present invention is a matrix-type preparation containing: (a) a pharmacologically active substance; (b) calcium polycarbophil; and (c) a specific sugar and/or sugar alcohol.

Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.

Abstract: Formulations of fenoldopam are disclosed for repeated administration or continued slow release administration, over prolonged periods of time or targeted slow and regulated delivery. The formulations include those formulations that increase the bioavailability of fenoldopam after oral intake, particularly lipid based nano dispersions and pronanodispersions and surfactant rich formulations. This may be accomplished by entrapment in nanoparticles or liposomal formulations or conjugation to a polymer or small molecule via a soft bond.

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

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

Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.

Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: The present invention relates to a novel dosage form, to a process for preparing the dosage form and to the use of the dosage form in the treatment of neurological and psychiatric disorders.

Abstract: The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

Abstract: Compounds of the formula (I): where R2, R5, R6 have the meanings as given in the description, and U, V and W, respectively, may be CR2?, CR4? and CR6?, respectively (with the definitions of R2?, R4? and R6? again as in the description), or may be N, were synthesized. They were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.

Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.

Abstract: Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof; and hydrates and other solvates in crystalline form; pharmaceutical formulations; and methods of use are disclosed.

Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.

Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50 wt. % or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.

Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic pain. The present invention further provides methods and compositions that treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic pain without inducing overt sedation. The present invention also contemplates combination therapy using one or more NK antagonists in combination with one or more compounds which decrease or inhibit neuronal excitation in the treatment of pain in association with the treatment of a particular disease condition or pathology.

Abstract: This invention provides novel solid pharmaceutical compositions and processes for the bulk production of said compositions. This invention also provides methods of using the pharmaceutical compositions in the treatment of cancer.

Abstract: The combination of vasopressin V2 receptor antagonists and vasopressin receptor agonists (selective or non-selective) is described, including pharmaceutical compositions, including kits, for administering, and methods and uses of such a combination, e.g. for treatment of critical care diseases and conditions requiring control of arterial blood pressure or for treatment of hypotension.

Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.

Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.

Abstract: The present invention relates to novel 2-phenoxy-6-phenyl- and 2-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.

Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

Abstract: Disclosed are compounds of Formula I: pharmaceutical compositions containing compounds of Formula I, and the use of compounds of Formula I to treat diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety wherein W1-W5, X1-X4, Y, Z1-Z5, m, n, p, and R1-R6 in Formula I are defined in the specification.

Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract: The invention relates to the use of inhibitors of acid sphingomyelinase and/or of inhibitors of products of the reaction catalyzed by this enzyme, for the prophylaxis and/or treatment of infectious diseases and/or diseases which are influenced by infections during the course thereof. The cited products especially include ceramide. Preferrably neutralizing antibodies and/or antidepressants, especially tricyclic and/or tetracyclic antidepressants, are used as inhibitors.

Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.

Abstract: The present invention relates to a compound that is capable of inhibiting the formation of ?-amyloid plaques, of reducing and/or retarding the increase the ?-amyloid plaque load in the brain of an animal, particularly a mammal, but especially a human. In particular, the invention relates to compounds of formula (I) and to metabolites thereof.

Abstract: The present invention relates to methods of reducing cardiotoxicity and/or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration.

Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.

Abstract: In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.

Abstract: Compounds of formula I wherein n, m, p, q, Y, R1 R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.

Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.

Abstract: A guanidine compound having a biaryl skeleton represented by the following formula (1), which is useful as a catalyst for various asymmetric reactions.

Abstract: The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R1-R9 are as defined herein.

Abstract: Compounds of Formula (I): wherein n, m, p, q, Y, R1, R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.

Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.