Abstract: A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m+n is 4 to 10; R4 and R5 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R4 and R5 not more than 4; R6 and R7 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R6 and R7 is not more than 4, and Ar1 is a group selected from (a), (b), (c) and (d).

Abstract: New pharmaceutical combination providing to decrease or eliminate the extrapyramidal side effects of antipsychotic active ingredients by combination of deramciclane with a classic antipsychotic agent (e.g. haloperidol, chloroprozamine or levoprozamin) or an atypical antipsychotic agent (e.g. risperidone, iloperidone or olanzapine).

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: Certain 2-keto-oxazole compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract: The present invention relates to compositions and methods for treatment of ear infections and inflammation. Specifically, the method involves administering to a patient a composition containing an antibacterial, an anti-inflammatory, and an anti-septic that is substantially free of pramoxine to treat the occurrence or negative effects of otic infection and inflammation.

Abstract: L-(?)-moprolol L-(+)-tartrate salt (2:1), method for preparing it and pharmaceutical composition comprising it.

Abstract: The invention relates to a dosage form for controlled release of the active ingredient 3-(2-dimethylaminomethylcyclohexyl)phenol, preferably (1R,2R)-3-(2-dimethylamino-methylcyclohexyl)phenol, or one of the pharmaceutically acceptable salts thereof, which (i) in vivo achieves the peak plasma level of the active ingredient after 2 to 10 h, and/or (ii) in vitro, measured in accordance with the European Pharmacopoeia with a paddle stirrer apparatus in buffer at a pH value of 6.8 (preferably 900 ml), a temperature of 37° C. and 75 rpm releases after 0.5 hours 3.0 to 37 wt. %, after 1 hour 5.0 to 56 wt. %, after 2 hours 10 to 77 wt. %, after 3 hours 15 to 88 wt. %, after 6 hours at least 30 wt. %, after 12 hours at least 50 wt. %, after 18 hours at least 70 wt. % and after 24 hours at least 80 wt. % of the active ingredient originally contained in the dosage form.

Abstract: This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

Abstract: A method and apparatus for administering drugs through a dermal or mucosal layer such that the treatment device may be applied to the mammal for the transdermal or transmucosal administration of various drugs, pharmaceuticals, salts and prodrugs thereof is taught herein. The magnetic device has at least one magnet to provide an effective magnetic sphere of influence of the magnetic field at the desired site of action. The tissue-permeable drug formulation is positioned on the site of action and the magnetic device is positioned adjacent to tissue-permeable drug formulation wherein the magnetic sphere of influence of the magnetic field moves the drug through the dermal or mucosal layer by interaction with the magnetic moment (induced or permanent) of the drug sufficient to increase the movement of the drug beyond the movement caused by diffusion alone.

Abstract: Aspects of the invention include a sustained release dosage form that can be administered to an oral cavity, e.g., the mouth. In certain embodiments, the sustained release dosage form is formulated as a lozenge or gum that may be administered to an oral cavity of a user for the purpose of dissolving over a prolonged period of time and thereby delivering an essential oil component therein. In certain embodiments, the sustained release dosage form includes a beneficial agent and, therefore, not only provides for the prolonged delivery of an essential oil component to an oral cavity, but also provides for the sustained release of a beneficial agent thereto. In certain embodiments, the sustained release dosage form includes a biocompatible, water-insoluble polymer, e.g.

Abstract: The present invention provides new method of treatment of epilepsy with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.

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

Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

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

Abstract: The present application describes deuterium-enriched eplivanserin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Use of Pargyline for the production of a medicament for influencing the metabolism of hair follicles and the modulation of their vital cycle.

Abstract: Methods for treating a demyelinating condition in a subject in need of treatment are provided. In some aspects the methods encompass administering to the subject an amount of a Ca2+-channel blocker effective to treat the demyelinating condition. In other aspects, the methods encompass administering to the subject an amount of a glutamate inhibitor effective to treat the demyelinating condition. In additional aspects, the methods encompass administering to the subject a Ca2+-channel blocker in combination with a glutamate inhibitor, in amounts effective to treat the demyelinating condition. In still other aspects, the methods encompass administering to the subject a Ca2+-channel blocker in combination with a hypertensive agent, in amounts effective to treat the demyelinating condition. Also provided are pharmaceutical compositions having a Ca2+-channel blocker, a glutamate inhibitor, and a pharmaceutically-acceptable carrier.

Abstract: Devices, systems and methods for compressing, cutting, incising, reconfiguring, remodeling, attaching, repositioning, supporting, dislocating or altering the composition of tissues or anatomical structures to alter their positional or force relationship to other tissues or anatomical structures. In some applications, the invention may be used to used to improve patency or fluid flow through a body lumen or cavity (e.g., to limit constriction of the urethra by an enlarged prostate gland).

Abstract: The novel sustained release dosage form comprising an active agent and a combination of a non-swelling pH dependent release retardant and a non swelling pH independent release retardant polymer which provides pH-independent drug release for a considerable period of time after administration.

Abstract: Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT2/5HT3 antagonist and alpha-2 antagonist activity. A second therapeutic agent possesses both serotonin reuptake inhibitory activity and norepinephrine reuptake inhibitory activity or is a reversible inhibitor of monoamine oxidase A (RIMA). In some embodiments, a combination of a first therapeutic agent and a second therapeutic agent results in reduction in one or deleterious side effects associated with the first therapeutic agent, the second therapeutic agent or both. Also provided are methods of treatment employing a first therapeutic agent and a second therapeutic agent. Also provided are kits containing a first therapeutic agent, a second therapeutic agent and instructions for administering the first therapeutic agent and the second therapeutic agent.

Abstract: The present invention concerns a method of administering at least one active pharmaceutical agent to a patient in need thereof, which method comprises the intranasal administration of a composition comprising a therapeutically effective amount of this agent, phospholipids, one or more C2-C4 alcohols and water, wherein the concentrations of the phospholipids and the one or more alcohols in the composition are in the ranges of 0.2 to 10% and 12 to 30% by weight, respectively, with the water content of said composition being not less than 30% by weight, the phospholipids forming vesicles in said composition. Further are disclosed pharmaceutical compositions and combinations suitable for intranasal delivery.

Abstract: The disclosure provides a molecular genetic approach of targeted mutagenesis and heterologous expression, coupled with in vitro and in vivo models of bacterial pathogenesis, to demonstrate that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.

Abstract: The present invention refert to the use of compounds active on the sigma receptor for the treatment of mechanical allodynia.

Abstract: The invention is directed to levalbuterol HCl Form B and methods of making the same.

Abstract: This invention relates to a method of testing agents, such as sigma ligands for their potential use in treating posterior capsule opacification (PCO). The present invention also relates to the use of sigma ligands, such as sigma-1 antagonists in the manufacture of a medicament for preventing posterior capsule opacification (PCO), as well as methods of treating PCO using sigma ligands.

Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Abstract: Disclosed herein are substituted cyclohexanol opioid receptor modulators and/or neurotransmitter reuptake modulators of Formula I or Formula II, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.

Abstract: Provided are processes for the preparation of (R)-SLB.D-DBTA salt and levalbuterol hydrochloride. Also provided are levalbuterol hydrochloride degradation products and processes for preparing them. Pharmaceutical compositions comprising at least one levalbuterol hydrochloride of the invention and at least one pharmaceutically-acceptable excipient are also provided.

Abstract: The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.

Abstract: The present invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, for the treatment of conditions, such as mood disorders, sleep disorders, or attention deficit disorders. In certain embodiments, the compositions useful in the methods of the invention comprise droxidopa and a compound selected from the group consisting of DOPA decarboxylase inhibiting compounds, catechol-O-methyltransferase inhibiting compounds, cholinesterase inhibiting compounds, monoamine oxidase inhibiting compounds, norepinephrine reuptake inhibiting compounds, selective serotonin reuptake inhibiting compounds, tricyclic antidepressant compounds, serotonin norepinephrine reuptake inhibiting compounds, norepinephrine dopamine reuptake inhibiting compound, noradrenergic and specific serotonergic antidepressants, and combinations thereof.

Abstract: A liquid cleansing composition comprising a cleansing surfactant, an adsorbed skin-care agent, adsorptive polymeric particles having an adsorption capacity of at least 2 g of skin care agent per gm of dry polymeric particles, a polymeric thickening agent having a molecular weight in the range of 500,000-10,000,000 Dalton, a water-soluble polymer having a molecular weight in the range of 200-50,000 Dalton, and a hydrophilic liquid, the said cleansing composition having the following features i) the low molecular weight, water-soluble polymer component functions as a foam-boosting and thixotropy-boosting agent; ii) the ratio of the Brookfield viscosity at 1 rpm of spindle speed to the Brookfield viscosity at 100 rpm of spindle speed is at least 10; and iii) the foam-volume is at least 20% higher with the water-soluble, polymeric, foam-boosting component than without it.

Abstract: A drug composition comprising a coated bead is used in the manufacture of immediate release and/or controlled release drug compositions. In a specific embodiment, the bead includes an inert core of a water-soluble or water-swellable material, which has been coated with a seal layer formed from a non-polymeric hydrophobic material. The immediate and/or controlled release beads may be used to form tablets or capsules. A method of making the beads by sequential deposition of multiple layers on the inert cores is also described.

Abstract: Disclosed is a pharmaceutical sustained release tablet for oral administration of a drug which is made of a compressed blend of at least three dry powders including a powder of a drug, a powder of a sustained release matrix for the drug, and a powder of at least one electrolyte. The sustained release matrix consisting of an un-cross-linked high amylose starch wherein the high amylose is substituted by at least one organic substituent comprising at least one carboxyl group. This organic substituent is preferably a carboxyalkyl having 2 to 4 carbon atoms, its salt or mixture thereof. This tablet has the advantage of having an improved integrity.

Abstract: The present invention relates to methods for intradermally delivering one or more biologically active agents such as vaccines and therapeutic agents into the dermis layer of the skin of a subject to obtain systemic delivery or an immune response using a microneedle drug delivery device containing the agent to be delivered. The methods employ a microneedle device with a row of hollow microneedles. The microneedles penetrate the skin of the subject and assume an anchored state in which the microneedles are anchored in the skin and project laterally from the device. A pivotal motion is then performed with the device so that the skin in which the microneedles are engaged is lifted above the initial plane of the surface of the skin while the biologically active agent is delivered. The methods of the invention elicit increased humoral and/or cellular response as compared to conventional vaccine delivery routes, facilitating dose sparing.

Abstract: Disclosed herein are several methods for promoting nerve regeneration. The methods include administering at least one tyrphostin, or a pharmaceutically acceptable salt thereof. In one non-limiting example, the tyrphostin is tyrphostin A9. These methods can be used to promote nerve growth in the central or peripheral nervous system. The methods are of use in treating neurodegenerative diseases, such as Parkinson's disease, or in treating the transaction of a partial or complete transaction of a nerve in the peripheral or central nervous system.

Abstract: There is described a compound selected from the group consisting of tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof, for the treatment or alleviation of depression. There is also described a method of treating a patient suffering from depression.

Abstract: A titration dosing regimen for the administration of controlled release tramadol analgesic to patients. The titration dosing regimen provides a significant reduction in the occurrence of adverse effects from the introduction of controlled released tramadol dosing, thus increasing patient compliance and medication tolerability.

Abstract: A compound of Formula (A), wherein R1 is C1-C5 alkyl, C3-C6 branched alkyl, C4-C7 cycloalkyl, C8-C12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R2 is H or R1; and X is halo, carbonyl carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.

Abstract: The present inventive subject matter relates to amorphous drug beads comprising an amorphous active drug and an organic surfactant having improved solubility, absorption and wettability characteristics. The present inventive subject matter further relates to methods of preparing the amorphous drug beads, wherein molten drug beads are subject to a cooling step with or without shear.

Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.

Abstract: The present invention provides novel honokiol derivatives, as well as pharmaceutical compositions containing the honokiol derivatives. These compounds and pharmaceutical compositions can be used in the prevention and/or treatment of cancer. In particular, honokiol derivatives, pharmaceutical compositions comprising the derivatives, and methods for their use in the treatment of myeloma are provided.

Abstract: Disclosed are topical compositions comprising at least one histone deacetylase (HDAC) inhibitor (HDI) and a carrier comprising petrolatum. Methods for using such compositions to treat or inhibit cancer and various skin diseases are also disclosed.

Abstract: A solid pharmaceutical dosage unit for alleviating the symptoms of rhinorrhea. The dosage unit comprises an anticholinergic agent and an antihistamine and, optionally, a decongestant and, when placed in a basket in 500 ml of 0.01 N HCl of 37° C. which is stirred at 100 rpm, releases at least about 75% of the at least one anticholinergic agent within 45 minutes and releases the at least one antihistamine at a rate of from about 20% to about 60% after 2 hours, from about 45% to about 80% after 4 hours and at least about 75% after 8 hours. This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.

Abstract: In general, this application is directed to medical devices that exhibit antimicrobial activity and to methods for preparing and using the medical devices. The medical devices of the present application include a polymeric portion that has been impregnated with a paraben and an organic dye in a manner whereby the paraben and organic dye exhibiting antibacterial properties. In one form, the paraben is impregnated into the polymeric portion before impregnation thereof with the organic dye. In another form, it is contemplated that the polymeric material may include methyl paraben, propyl paraben, and methylene blue. It is further contemplated that the polymeric material is effective in releasing at least one of the paraben and organic dye to prohibit bacterial growth in surrounding tissue and/or fluid.

Abstract: The present invention relates to compositions to treat CaV2 disorders. The invention also relates to methods treating CaV2 disorders. The invention further relates to kits for treating CaV2 disorders in a subject. The invention further relates to methods of identifying novel treatments for treating Cav2 disorders in a subject.

Abstract: Disclosed herein are substituted cyclohexanone-based NMDA receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Use of 1-phenyl-3-dimethylaminopropane compounds for the production of medicaments for treating neuropathic pain, preferably polyneuropathic pain, also preferably diabetic neuropathic pain, more preferably diabetic peripheral neuropathic pain, and furthermore preferably for treating diabetic peripheral neuropathy.