Abstract: The present invention provides a transdermal patch having excellent preservation stability and transdermal absorbency of DMAEs. The patch has a support and a plaster layer integrally laminated on one surface of the support, and the plaster layer includes: DMAEs; an acrylic adhesive prepared by copolymerizing monomers respectively containing 30 to 99% by weight of alkyl methacrylate having an alkyl group with a carbon number of 6 to 22 and 1 to 70% by weight of alkyl acrylate having an alkyl group with a carbon number of 2 to 20; and fatty acid ester prepared by dehydro-condensing saturated fatty acid having an alkyl group with a carbon number of 10 to 20 and saturated aliphatic monohydric alcohol having an alkyl group with a carbon number of 2 to 20, wherein solubility of the DMAEs is 0.05 to 5 g at 25° C. with respect to the fatty acid ester.

Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.

Abstract: The present invention relates to a compound of formula A, wherein R is alkyl. Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.

Abstract: This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding ?2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.

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. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.

Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.

Abstract: Methods for treating Alzheimer's Disease (AD) using modulators of lysosomal activity are described herein. More particularly, methods described herein relate to the use and application of compounds or agents that enhance lysosomal activity for the treatment of AD. In a particular aspect, the method relates to the use and application of compounds or agents that increase the pH of the lysosome and/or increase the overall activity of lysosomal proteases for the treatment of AD. Also described herein are methods and assays for screening to identify compounds or agents that increase the pH of the lysosome and/or increase the overall activity of lysosomal proteases for the treatment of AD.

Abstract: 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: A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R3 is independently selected from the group consisting of alkyl and cyclo-alkyl; and n is independently selected from 0 to 6. The compounds have lower immunosuppressive side effects as a result of not being phosphorylated by sphingosine kinase 2.

Abstract: An inhaler includes a first body member and a second body member fit closely together to form an inhaler body, and an outlet. The first body member has a medicament chamber containing a unit dose of powdered medicament. A seal such as a foil strip seals the medicament chamber and extends outwardly of the inhaler body. In use, one end of the seal can be grasped by a user and withdrawn, fully or partially, from the inhaler body, to release the powdered medicament from the medicament chamber. The second body member includes a medicament collection well in which the medicament is collected upon its release from the medicament chamber. The medicament collection well forms part of an airway connecting into the outlet. In use, air can be drawn by inhalation at the outlet to entrain the powder medicament in the collection well for inhalation by a user.

Abstract: A compound for therapeutic use, of the formula (I), wherein R1 is aryl or heteroaryl optionally substituted with R5; R2 is H, alkyl or CH2OH or forms part of a ring with R4; R3 is H, alkyl or CH2OH or forms part of a ring with R4; R4 is H, alkyl or (when forming part of a ring with R2 or R3) CH2; and R5 is alkyl, CF3, OH, Oalkyl, OCOalkyl, CONH2, CN, halogen, NH2, NO2, NHCHO, NHCONH2, NHSO2Me, CONH2, or SOMe; or a salt thereof.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: A stabilised composition comprising at least one adrenergic compound and at least one antioxidant selected from the group consisting of a bisulfite, a metabisulfite and a sulfite compound.

Abstract: The present invention relates to methods and feed compositions for increasing or maintaining the reproductive performance of sows. More particularly, the present invention relates to methods of increasing or maintaining the reproductive performance of sows by administering a biologically active compound during lactation, and food compositions comprising said biologically active compound for the purposes of increasing or maintaining the reproductive performance of sows. The present invention also relates to a method of increasing or maintaining ovarian function in sows.

Abstract: Memantine compositions and methods of use are described herein. In some embodiments, the compositions comprise memantine and an absorption enhancer, or memantine and an elimination enhancer, or memantine and an absorption enhancer and an elimination enhancer.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present disclosure relates to systems, methods, and formulations for the pulmonary administration of one or more therapeutic agents, in dry powder form, in a single, large dose quantity. These formulations, methods, and systems are useful in the treatment of patients suffering from toxic or harmful gas exposure, such as nerve gas exposure, as well as in the treatment of patients suffering from diseases of the pulmonary system, including tuberculosis, cystic fibrosis, and chronic obstructive pulmonary disease (COPD).

Abstract: A dry powder suitable for inhalation n a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period of time that is less than 60 minutes.

Abstract: A pH dependent drug delivery system comprising a pH sensitive graft copolymer, a therapeutically active agent and other pharmaceutically acceptable ingredients. More specifically, a composition which is capable of suppressing the drug release in the acidic pH prevalent in the stomach and releasing the drug over an extended period of time at pH prevalent in the intestinal region.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.

Abstract: A device for drug delivery to an orifice of a subject, comprising a shell which is elastically stressed by an active pharmaceutical ingredient, said shell containing and being substantially impermeable to said active pharmaceutical ingredient, wherein said shell has at least one hole sized for in-vivo release of said active pharmaceutical ingredient as a result of elastic stressing.

Abstract: Ocular and cerebral blood flow are enhanced by the administration of (?) erythro isomer of ?-methyl epinephrine, a C1 to C8 aliphatic ester of ?-methyl epinephrine, ?-methyl norepinephrine, a C1 to C8 aliphatic ester of ?-methyl norepinephrine, or a pharmacologically acceptable acid addition salt thereof.

Abstract: This invention relates to a layered pharmaceutical composition comprising a combination of an antihistamine and a decongestant.

Abstract: Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.

Abstract: A method of treating a reactive airway disease in a subject comprising administering at least one peroxidase inhibitor in association with administration of at least one ?-agonist.

Abstract: A method for delivering an agent to the pulmonary system, in a single, breath-activated step or a single breath, comprises administering from a receptacle enclosing a mass of particles, to a subject's respiratory tract, particles which have a tap density of less than 0.4 g/cm3 and deliver at least about 50% of the mass of particles. The particles are capable of carrying agents. The agent is (1) part of the spray-drying pre-mixture and thereby incorporated into the particles, (2) added to separately-prepared particles so that the agent is in chemical association with the particles or (3) blended so that the agent is mixed with, and co-delivered with the particles. Respirable compositions comprising carrier particles having a tap density of less than 0.4 g/cm3 and a composition comprising an agent are also disclosed. Methods of delivering these respirable compositions are also included.

Abstract: There is disclosed the topical dermal use of vasocontrictor substances for regulating body temperature to treat, prevent or delay the onset of anesthetic induced hypothermia. Kits containing appropriate materials and instructions, and other embodiments, are also disclosed.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: Pharmaceutical formulations comprising desvenlafaxine, processes for preparing formulations comprising desvenlafaxine, and therapeutic uses and methods of treatment employing formulations comprising desvenlafaxine.

Abstract: Process for preparing sterile suspensions for inhalation comprising an active ingredient insoluble in water and wherein at least 80% of the particles of said active ingredient have a diameter between 3 and 5 ?m, comprising the following stages: dissolving the active ingredient in the minimum quantity of an alcoholic solvent, optionally in the presence of a polyol and adding at least one surfactant, filtering the solution obtained in the previous stage through a sterilizing filter, adding the solution from stage (b) to sterile water under sonication to directly obtain a suspension wherein the particles have a reduced diameter.

Abstract: Methods of treating a lysosomal storage disorder and methods of increasing cellular uptake of a lysosomal enzyme using ?2 agonists or therapeutic agents that increase expression of receptors for a lysosomal enzyme.

Abstract: Provided herein are compositions and methods for the treatment of soft tissue injury, sports-related injury, physical overuse of muscles, ligaments or joints, and trauma, traumatic stress or sudden jolts on bones and tissues in an individual. Described herein are pharmaceutical compositions comprising a vasoconstrictor and, optionally, a topical analgesic and methods of using said compositions for the treatment of a variety of soft tissue injuries.

Abstract: The present invention relates to a pharmaceutical composition for inhalation. The invention is further directed to a method for setting the performance characteristics of such a pharmaceutical composition and the use of such a composition in the treatment of asthma, COPD, allergies, infectious diseases and diseases of the cardiovascular system.

Abstract: The present invention relates to an improved process for the preparation of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine which is an intermediate for the preparation of the analgesic tapentadol.

Abstract: A method of promoting or improving the feed efficiency and the muscle to fat ratio in animals by administering to the animals a therapeutically effective amount of a pure or substantially pure RR-isomer of ractopamine is disclosed. Also disclosed are animal feed preparations and compositions and pharmaceutical preparations capable of increasing lean meat deposition in an animal or decreasing body fat, or promoting or improving the growth of an animal or improving the feed efficiency of an animal.

Abstract: A modified-release oral pharmaceutical composition in capsules with microspheres contains loratadine, phenylephrine and pharmaceutically acceptable excipients. The composition has immediate bioavailability, with plasmatic concentration values within the therapeutic window with a uniform, continuous release. A method for the production of the composition and a method for treatment as a nasal decongestant and an antihistamine are included.

Abstract: A buccal and/or sublingual formulation comprising one or more active compounds; and a buccal matrix which releases the active compounds at a predetermined rate for transport across the buccal and/or sublingual membranes, wherein the rate of release of the active compounds is either (A) the same or substantially the same rate at which the active compounds are transported across the buccal and/or sublingual membranes; or (B) a rate which releases the active compounds over an extended period as required by the therapeutic affect or treatment window for those active compounds.

Abstract: Provided herein are pharmaceutical formulations, methods, and systems for treating regional fat deposits and fat-related conditions and indications. Methods comprise administering a pharmaceutical formulation consisting essentially of a long-acting beta-2 adrenergic receptor agonist, for example, salmeterol, suitable for subcutaneous administration. Methods further comprise administering a pharmaceutical formulation that is suitable for subcutaneous injection comprising: (a) a lipophilic long-acting selective beta-2 adrenergic receptor agonist and/or glucocorticosteroid, or a salt, optical isomer, racemate, solvate, or polymorph thereof; and (b) at least one subcutaneously acceptable inactive ingredient.

Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Provided are electrokinetically-altered fluids (e.g., electrokinetically-altered gas-enriched fluids and solutions) comprising an ionic aqueous solution of charge-stabilized oxygen-containing nanostructures in an amount sufficient for treating an inflammatory neurodegenerative condition or disease (e.g., a taupathy) or at least one symptom thereof. The electrokinetically-altered fluids or therapeutic compositions and methods include electrokinetically-altered ionic aqueous fluids optionally in combination with other therapeutic agents. Particular aspects provide for modulating phosphorylation of tau protein. Particular aspects provide for regulating or modulating intracellular signal transduction associated with said inflammatory responses by modulation of at least one of cellular membrane potential and/or conductance, membrane proteins such as membrane receptors, including but not limited to G-Protein Coupled Receptors (GPCR), and intercellular junctions (e.g.

Abstract: The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.

Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: Compositions and methods are provided for obtaining stabilized quinol compositions, such as catecholamine drugs (e.g., epinephrine solutions), and also for obtaining stable pharmaceutical formulations that comprise a stabilized quinol composition and a second pharmacologically active component such as a local anesthetic or other active drug ingredient having a reversibly protonated amine group. Stability is achieved through the inclusion of an appropriately selected pH buffer and a thiol agent, based on redox and pH buffering principles including pKa of the buffer and of the reversibly protonated amine group.

Abstract: The invention provides nanostructures or products of manufacture for use as ex vivo or in vivo composition (e.g., a drug, or a therapeutic, diagnostic or imaging reagent) delivery vehicles. In one aspect, the invention provides nanoparticles comprising several compartments which in unison function as a composite nanostructure. In one embodiment, the nanoparticles of the invention comprise a combination of polymer core/lipid bilayer interface which incorporate covalently attached lipid-vascular targeting ligands. These composite nanoparticles can deliver highly effective and selective payloads for diagnostic, prophylactic or therapeutic applications.

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: The invention features topical formulations comprising an osmotically active agent and/or a vasoconstrictor and/or an astringent agent for the treatment and prevention of eyelid swelling, and methods of use thereof.

Abstract: Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.