Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers.

Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseas

Abstract: The present invention relates to a combination of the anti-diabetic drug metformin and the MTP (microsomal triglyceride transfer protein) inhibitor (+)-phenyl-(4-{4-[(4?-trifluoromethyl-biphenyl-2-carbonyl)-amino]-phenyl}-piperidin-1-yl)-acetic acid methyl ester and the use thereof for combined administration in the treatment or prevention of diabetes mellitus type 2 conditions. The invention further relates to products containing as first active ingredient metformin and as second active ingredient the MTP inhibitor (+)-phenyl-(4-{4-[(4?-trifluoromethyl-biphenyl-2-carbonyl)-amino]-phenyl}-piperidin-1-yl)-acetic acid methyl ester, as combined preparations for simultaneous or sequential use in the treatment or prevention of diabetes mellitus type 2; and to related pharmaceutical compositions and uses.

Abstract: A compound having the general formula (I) wherein R1 represents C1-C6 alkyl, etc., R2 represents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R4—(CH2)l—, etc., R3 represents C6-C10 aryl, etc., X1, X2, X3, X4 and X5 each independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. They have excellent inhibition of platelet activation, etc. and are useful as a prophylactic or therapeutic agents for diseases related to thrombus or embolus formation.

Abstract: The present invention provides a pharmaceutical composition for use in a dosage form for oral administration to a patient. The composition expands upon contact with gastric fluid and promotes retention of the dosage form in the patient's stomach for a prolonged period of time. The present invention further provides pharmaceutical dosage forms containing an active ingredient, and the pharmaceutical composition. The forms are adapted for immediate or controlled release of the active ingredient. The dosage forms may be used advantageously in the treatment of Parkinson's disease with levodopa and hyperactivity and attention deficit disorder with methylphenidate.

Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.

Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

Abstract: The present invention relates to pharmaceutical formulation containing tolperisone or its pharmaceutically acceptable salts or tolperisone combined with a non-steroidal anti-inflammatory drug or their salts, gel forming macromolecule, solvent, and if required thickening agent, penetration enhancer and pH adjuvant or the mixture thereof. The invention also relates to the manufacturing process of the above mentioned pharmaceutical compositions, further the use of these formulations and the containers suitable for the dosage, which are dual compartment containers consisting of two separated chambers.

Abstract: Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions.

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: The present invention provides piperidine derivatives of formula (I): salts and optical isomers thereof and cosmetic compositions containing them.

Abstract: A pharmaceutical suspension having a therapeutically effective amount of phenylephrine and a therapeutically effective amount of a first active agent consisting essentially of a first substantially water insoluble active agent having an average particle size of between about 10 and about 100 microns, an effective amount of non-reducing sweetener; an effective amount of water; and an effective amount of a suspending system; wherein the pharmaceutical suspension has a pH of from about 4 to about 6 and is substantially free of a reducing sugar and related methods.

Abstract: A therapeutic method is provided to treat neutrophil-associated pulmonary diseases, such as chronic obstructive pulmonary disease, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

Abstract: The invention relates to a solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.

Abstract: The invention relates to compounds corresponding to general formula (I) below: to the compositions containing same, to methods for the preparation thereof and to the use thereof in pharmaceutical compositions for use in human or veterinary medicine, or else in cosmetic compositions.

Abstract: Controlled release oral dosage forms suitable for administration of methylphenidate are provided. Abuse-resistant controlled release oral dosage forms suitable for administration of methylphenidate are also provided. Methods of treating ADD and ADHD using the oral dosage forms are also provided.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.

Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.

Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.

Abstract: A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: formula (II), (III) and (IV); or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: (V) and (VI); wherein R1 and R2 together represent an oxo group, or R1 and R2 each represent hydrogen, methoxy or ethoxy, or R1 and R2 together with the interjacent carbon atom represent a 1,3-dioxolane or 1,3-dioxane ring, attached via the 2 position and optionally bearing one or more methyl or ethyl groups; or a salt thereof, is suitable for the treatment of anxiety and depression.

Abstract: The present invention relates to the cosmetic use, as an agent for combating wrinkles, especially expression wrinkles, and/or for dencontracting the skin and/or relaxing the features, of at least one piperidine derivative chosen from the compounds of formula (I): and the salts and optical isomers thereof. The invention also relates to novel piperidine derivatives and also to cosmetic compositions containing them.

Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.

Abstract: The present invention relates to the prediction of QT prolongation following administration of a compound capable of increasing an individual's QT interval based on the individual's genotype at one or more single nucleotide polymorphism (SNP) loci and to the treatment of a patient based on such prediction.

Abstract: A composition comprising an antacid, and a local, topical anesthetic. The composition is used to relieve pain or discomfort associated with a sore throat, and therefore, the invention is also directed to a method of alleviating the pain or discomfort associated with a sore throat comprising instructing a human to orally administer the composition.

Abstract: Provided are combinations of inhibitors of dipeptidyl peptidase IV (DP IV) and of enzymes having the same substrate specificity (DP IV-analogous enzymatic activity) and inhibitors of alanyl aminopeptidase (aminopeptidase N, APN) and of enzymes having the same substrate specificity (APN-analogous enzymatic activity) and use of the same to obtain a more than additive to superadditive inhibition for the treatment of arteriosclerosis, for the treatment of allergic reactions of the type I according to the Gell and Coombs classification and for the treatment of dermatological diseases with follicular and epidermal hyperkeratoses and an enhanced proliferation of keratinocytes.

Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to a quickly decomposing oral drug preparation, for the application of active ingredient combinations for smoking withdrawal, which contains nicotine, a nicotine salt, a nicotine derivative, or a substance that reacts to nicotine, in combination with another active ingredient, and the use of such a drug preparation for the treatment of smoking withdrawal, and the use of nicotine, and/or nicotine salts or derivatives, for the production of medications for the treatment of smoking withdrawal. The active ingredient that is to be administered, in combination, for this purpose is a centrally active ingredient, preferably an antidepressant for the fighting of psychic dependency in terms of a smoking withdrawal therapy. The administration of the active ingredient combination to the patient should be handled in a simple and reliable way and should exclude side effects to a large extent.

Abstract: This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the azaspiro-head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.

Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.

Abstract: A piperidine derivative of the formula (I) is found to bind specifically with the NR1/NR2B receptor and usable as an analgesic (pain treatment drug). wherein X is OH or lower alkylsulfonyloxy; Ar is optionally substituted aryl or optionally substituted heteroaryl; n is an integer of 1 to 4; m is an integer of 0 to 1; R1 is hydrogen; R2 is OH or R1 and R2 taken together may form a single bond; excluding that 1) n is 2; m is 0; R1 and R2 taken together may form a single bond; and Ar is optionally substituted phenyl and 2) n is 3; m is 0; R1 and R2 taken together may form a single bond; and Ar is phenyl.

Abstract: The present invention relates to dihydrospiroindene modulators of muscarinic receptors. The present invention also provides compositions comprising such dihydrospiroindene modulators, and methods therewith for treating muscarinic receptor mediated diseases.

Abstract: An adhesive patch for percutaneous fentanyl administration which is easily produced, has long-term continuity, and is excellent in adhesion and conformability to the skin. The adhesive patch comprises a backing layer and a pressure-sensitive adhesive layer formed on one side thereof, wherein the pressure-sensitive adhesive layer comprises fentanyl as an active ingredient, a pressure-sensitive adhesive base, and a tackifier resin, the pressure-sensitive adhesive base comprising polyisobutylene and a styrene/isoprene/styrene block copolymer, the proportion of the polyisobutylene in the adhesive base being, 8 to 15 wt. %, and the ratio of the concentration of the polyisobutylene to that of the styrene/isoprene/styrene block copolymer being from 2:3 to 3:2.

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of Formula (I) wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.

Abstract: The invention relates to novel crystalline forms of fexofenadine base, a process for the preparation thereof and the use thereof in therapy.

Abstract: A composition for control of diseases on useful plants or on propagation material thereof caused by phytopathogens, comprising (A) a compound of formula (I) or a tautomer of such a compound; and component (B) and component (C) are pesticides as described in claim 1.

Abstract: A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump.

Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.

Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.

Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.

Abstract: 4-substituted 1-amidomethylcarbonyl-piperidine compounds having motilin-agonistic properties and their acid addition salts, pharmaceutical compositions containing these compounds, processes and intermediate products for the preparation of these compounds, and methods of treatment utilizing these compounds.

Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.

Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.