Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.

Abstract: Compounds of formula (I), in salt or zwitterionic form, wherein J, L, M, R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The subject application provides a method of treating pruritus comprising administering to the skin of a subject afflicted with pruritus an amount of a perfluorocarbon effective to treat the pruritus. The subject application also provides a method of alleviating a symptom of psoriasis comprising administering to the skin of a subject afflicted with psoriasis an amount of a perfluorocarbon effective to alleviate the symptom of psoriasis. The subject application also provides a perfluorocarbon composition for use in treating a subject afflicted with pruritus or psoriasis. The subject application further provides a pharmaceutical composition comprising an amount of a perfluorocarbon for use in treating pruritus or psoriasis.

Abstract: The present invention concerns with a new use of R-Bambuterol or Bambuterol as inhaled medicament for treatment of asthma, COPD and other respiratory disorders, and a new use of R-bambuterol or bambuterol and corticosteroids or other therapeutically active medicament as combined inhaled therapies. The invention also related to a new use of R-bambuterol with reduced drug tollerance and risk of exerbation of asthma associated with bambuterol in treatment of respritroy discorders.

Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided tha

Abstract: The present invention relates to a cosmetic process for treating wrinkled skin, in particular the skin of the face and/or of the forehead, through a dermo-decontracting effect, comprising the topical application to said skin of a composition comprising, in a physiologically acceptable medium, at least one piperidine derivative chosen from the compounds of formula (I): These compounds make it possible to combat expression wrinkles according to a mechanism of dermo-decontraction.

Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.

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

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

Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.

Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.

Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.

Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).

Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against fungal diseases or insect damages, and the corresponding methods of protection by application of the said composition. More precisely, the subject of the present invention is a pesticide composition based on a tetrazolyloxime derivative and a fungicide or an insecticide active substance or compound.

Abstract: There is disclosed a technique for imparting an appropriate rupture strength and high drug-release properties to a jelly formulation comprising pectin. The jelly formulation of the present invention comprises a drug, pectin, and divalent metal ion, and further comprises a component selected from sucrose, maltitol and C3-C4 alditols, and a component selected from C5-C6 alditols in combination.

Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

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: or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: 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 compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract: The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses (6aR,10aR)-?8-tetrahydrocannabinol-11-oic acids (hereinafter referred to as (6aR,10aR)-?8-THC-11-oic acid), as well as pharmaceutical compositions containing the (6aR,10aR)-?8-THC-11-oic acids, for treatment of interstitial cystitis in a mammal. The invention further covers methods of formulating and administering the compounds and pharmaceutical compositions as therapeutic agents in the treatment of interstitial cystitis, with particularly preferred administration routes being oral and via intravesicular instillation.

Abstract: The invention relates to a compound of the following formula (I), or to a pharmaceutically acceptable salt thereof or to a stereoisomer or mixture of stereoisomers at any proportions, where: X1 is a CH2 or C?O group; X2 is a linear saturated or unsaturated carbohydrate chain with 8 to 24 carbon atoms; R1 is a hydrogen atom or an OH or (C1-C6)alkoxy group such as methoxy; and R2 is a CH3 or CH2OR3 group, with R3 being a hydrogen atom or a (C1-C6)alkyl, CO—(C1-C6)alkyl or NH—(C1-C6)alkyl group. The invention also relates to the use of said compound as a drug, in particular for treating neurodegenerative diseases, and to a method for preparing same.

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: The invention relates to a method of treating Attention Deficit Disorder (ADD) and Attention Deficit/Hyperactivity Disorder (ADHD) and compositions for topical application of methylphenidate comprising methylphenidate in a flexible, finite system wherein said composition comprises about 10 to 30 wt % methylphenidate, about 30 to 50 wt % acrylic adhesive, and about 30 to 50 wt % silicone adhesive and wherein said methylphenidate is delivered to a subject in need thereof such that the plasma concentration of methylphenidate increases over a period of about 6-16 hours, and more preferably over a period of about 6-12 hours followed by a steady decrease in plasma concentration of methylphenidate.

Abstract: The present invention provides compositions and methods that are useful for treatment of pain associated with acute herpes zoster. The aqueous compositions are non-stinging and non-irritating.

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: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.

Abstract: The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotome conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

Abstract: Methods and dosage formulations for the safe treatment of cold, cough, flu, and sinus symptoms in children and adolescents by age and nature of symptoms, and adults and the elderly by age, nature of symptoms, and concomitant patient medical conditions. The method of the present invention comprises the formulation of a cold medication which consists essentially of combinations of a nonsedating or minimally sedating antihistamines with pain relievers and the expectorant, guaifenesin.

Abstract: A composition, an infusion solution, a method for treatment, and a kit for intravascular administration for treatment of a brain-dead, heart-beating, respirated, potential organ donor. The composition includes a non-adrenaline and amphetamine or an amphetamine-like substance. The composition may in addition include adrenaline, hydrocortisone, thyroxin, insulin, triiodotyronine, dopamine, a vasopressor agent, such as desmopressin, and methylprednisolone. The composition may be dissolved in pure water, Ringer's acetate solution or physiological sodium chloride solution. The composition is infused in such an amount as to maintain a mean arterial pressure of about 60 mmHg.

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: Provided is a dual-release, dual-adhesiveness flexible thin film dosage form comprising: a quick-release subfilm comprising an admixture of polymer, which comprises predominantly highly water-soluble polymer(s), and a bioactive agent, the polymers and other components of the quick-release subfilm adapted to provide 20 minute or less erodibility for the quick-release subfilm; and laminated against the quick-release subfilm, a sustained-release subfilm comprising an admixture of polymer, which comprises predominantly hydrophilic, bioadhesive polymer(s), and a second bioactive agent, which can be the same as the first, the polymers and other components of the sustained-release subfilm adapted to provide erodibility of 1 hours or more and 20 hours or less for the sustained-release subfilm, the dosage form having a thickness of 30 mil or less, and being more adhesive on the sustained-release side.

Abstract: The present invention provides therapeutic liposomes and methods for producing and using the same. In particular, therapeutic liposomes of the invention comprise phospholipids comprising C16-C22 fatty acid ester moieties. In some embodiments, these therapeutic liposomes are used in assisting delivery of an active compound, e.g., a drug and/or a nutraceutical, to a subject. In some embodiments, compositions of the invention have synergistic therapeutic effect.

Abstract: Novel combinations comprising HMG CoA reductase inhibitors, or statins, with partial fatty acid oxidation inhibitors (pFOXi), and methods for their use, are disclosed. These combinations are useful in preventing or reducing the risk of developing diabetes which results from therapy with a statin.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: A dosage form that provides a controlled release solid dosage form for the oral administration of a central nervous system stimulant, preferably methylphenidate hydrochloride.

Abstract: The invention relates to novel pharmaceutical combinations with improved sodium channel blocking effect. Further, the invention relates to the use of said pharmaceutical combinations in chronic pain, in disturbances of the motor system, in epilepsy, as well as in other therapeutic fields where the use of sodium channel blockers is acceptable.

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: The invention provides a method of treating a pain condition in a mammal utilizing a specific serotonin and norepinephrine reuptake inhibitor (SNRI) and also the combination of the SNRI and an opioid agonist agent. The invention includes methods wherein the opioid agonist agent is administered at a dose that is lower than a dose administered for treating a pain condition when used alone.

Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

Abstract: In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including executive function defects. The methods involve the administration of a composition comprising D-threo methylphenidate that is substantially free of L-threo methylphenidate and of erythro forms of methylphenidate.

Abstract: This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway.

Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e.