Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.

Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.

Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.

Abstract: The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) a mucosal adjuvant, (3) an antihistamine drug and (4) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.

Abstract: The present invention is directed to processes for the preparation of 4-(3-methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of formula (III).

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.

Abstract: This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.

Abstract: This invention relates to novel alkyl substituted piperidine derivatives 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: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.

Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Abstract: A method of treating a mental disorder including administering to a patient in need thereof, an effective amount of a pharmaceutical composition including 1,1-diphenyl-4-piperidine-1-ylbuthan-1-ol or a pharmaceutically acceptable salt thereof. The mental disorder is depression, bipolar disorder, anxiety disorder, impulsive disorder, bulimia, panic disorder, social anxiety disorder, insomnia, attention deficit hyperactivity disorder (ADHD), schizophrenia, dementia, personality disorder, alcoholism, dissociative disorder, sleep apnea syndrome, or fibromyalgia. In a preferred embodiment, the mental disorder as a therapeutic target is fibromyalgia, chronic fatigue syndrome (CFS), or depression with pain, and the administration of the pharmaceutical composition is capable of reducing the pain caused by these diseases.

Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

Abstract: Therapeutic uses of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine and therapeutically acceptable salts thereof are provided.

Abstract: This invention relates to novel piperidine derivatives 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: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The compound 4-[2,3-Difluoro-6-(2-fluoro-4-methyl-phenylsulfanyl)-phenyl]-piperidine according to the structure (formula I), and pharmaceutically acceptable salts thereof are provided for the treatment of CNS related disorders, such as: depressive disorder, dysthymic disorder; mood disorder due to a general medical condition; atypical depression; seasonal affective disorder; melancholia; treatment resistant depression; partial responders; depression associated with bipolar disorder, pain, Alzheimer's disease, psychosis, Parkinson's disease, Lewy body disease, Huntington's disease, multiple sclerosis or anxiety; general anxiety disorder, social anxiety disorder, panic attacks; phobia; social phobia, obsessive compulsive disorder; post traumatic stress disorder, acute stress; ADHD; and pain.

Abstract: Certain substituted sulfonamide derivatives of Formula (I) selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: The present invention relates to methods of treating the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena—. . . ) using compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity. The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and/or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and/or (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The invention provides methods of treating binge eating disorders, obesity resulting from binge eating behavior, and depression. The invention includes methods of treating certain co-morbidities in ADHD and ADD patients; for example the invention includes methods of treating generalized anxiety disorder, obsessional and ruminative thought disorders, and obsessive/compulsive behavior in ADHD and ADD patients. The invention also includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered with one or more other active agents. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.

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: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.

Abstract: The present invention relates to a method for diagnosing neuroendocrine cancers via detecting the presence of N-methyl D-asparate-associated (NMDA) glutamate receptors type 1 and/or type 2. Methods for preventing and treating neuroendocrine cancers are also disclosed.

Abstract: Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds as a pharmacologically active substance, in particular in the treatment of neurodegenerative diseases, cardiovascular diseases, inflammatory diseases; hypercholesterolemia, and diabetes.

Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

Abstract: Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy) phenylmethyl)carbamide including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts.

Abstract: Described herein are injectable compositions containing non-sedating or second and third generation antihistamines such as cetirizine/levocetirizine and methods of use thereof. Specifically, methods of treating acute allergic reactions including anaphylaxis with the compositions are disclosed. In certain embodiments, the injectable compositions are bioequivalent to currently marketed oral dosage forms. In other embodiments, the non-sedating or second and third generation antihistamine injectable formulations are therapeutically equivalent to diphenhydramine injectable formulations and/or are more effective than placebo. In other embodiments, a non-sedating antihistamine injectable composition is delivered by an autoinjector.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

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

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group of formula COR4, or R1 represents a group of formula (A): R2 represents a group of formula NR5R6, or R2 represents a nitrogen-containing heterocyclic group, an aryl group or a heteroaryl group, R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6 inclusive, n represents 0, 1 or 2, their optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating and/or preventing thrombotic events.

Abstract: The present invention is directed to pharmaceutical compositions comprising a plurality of taste-masked high-dose/low-dose drug-containing microparticles, dosage forms comprising such pharmaceutical compositions (such as an orally disintegrating tablet), and methods of making the pharmaceutical compositions and dosage forms of the present invention. Dosage forms comprising the pharmaceutical compositions of the present invention are improved homogeneous blends of high-dose and low-dose drugs which provide for more convenient and palatable administration of drug combinations, for example for treating pain, hyperglycemia, cardiovascular disease, and allergies.

Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of HfnEF, as well as to a method of treating HfnEF, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HFnEF. The invention further relates to a treatment programme for treating HFnEF, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HFnEF or the symptoms thereof.

Abstract: The invention relates to pharmaceutical combinations of retigabine and sodium channel inhibitors for treating, pains which are accompanied by an increase in muscle tone.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: The present disclosure is directed to methods for providing tolperisone having extremely low levels of 4-MMPPO (2-methyl-1-(4-methylphenyl)-propenone), as well as related compositions. The invention further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO, among other features.

Abstract: The present invention relates to methods of treating of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena- . . . ) using compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for. The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and/or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and/or (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: The invention relates to the improvement in the treatment of certain neural disorders/diseases, such as Parkinson's disease and other motor disorders. The invention relates to drug compositions and dosage forms comprising said drug composition; methods of manufacturing the drug compositions and dosage forms; and methods of treatment, comprising administering the drug composition and dosage form to an individual. In certain embodiments, the drug compositions and dosage forms comprise carbidopa and levodopa in a formulation suitable for once-daily administration.

Abstract: Disclosed are methods for alleviating symptoms of neuropsychiatric disorders using tetrahydropyridine derivatives bearing aromatic substituents. The method comprises administering to an individual a tetrahydropyridine derivative bearing aromatic substituents in an amount effective to alleviate symptoms of the neuropsychiatric disorder.

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. wherein R1, R2, and R3 are as defined.

Abstract: Provided are novel tetrahydropyridine derivatives bearing substituents. These compounds can be used for alleviating the symptoms of CNS disorders.

Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.

Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.

Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

Abstract: This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder.