Abstract: The present invention relates to a highly concentrated, stable pharmaceutical formulation of a pharmaceutically active anti-HER2 antibody, such as e.g. Trastuzumab (HERCEPTIN™), Pertuzumab or T-DM1, or a mixture of such antibody molecules for subcutaneous injection. In particular, the present invention relates to formulations comprising, in addition to a suitable amount of the anti-HER2 antibody, an effective amount of at least one hyaluronidase enzyme as a combined formulation or for use in form of a co-formulation. The formulations comprise additionally at least one buffering agent, such as e.g. a histidine buffer, a stabilizer or a mixture of two or more stabilizers (e.g. a saccharide, such as e.g. ?,?-trehalose dihydrate or sucrose, and optionally methionine as a second stabilizer), a nonionic surfactant and an effective amount of at least one hyaluronidase enzyme. Methods for preparing such formulations and their uses thereof are also provided.

Abstract: This invention concerns an in situ biodegradable hydrogel drug delivery system in which the components are assembled in a manner that provides a mechanism for the timed cleavage of a particular amide bond in a covalently linked active agent or of the hydrogel structure.

Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.

Abstract: The present invention provides a process for preparing a particulate medicament that has greater homogeneity and a lower adhesion between the particles of the active ingredient and the carrier. The process comprises the steps of: (a) combining a pharmaceutically active ingredient in the form of an agglomerate of primary particles having an agglomerate particle size such that the agglomerate is capable of passing through a sieve having a mesh of 50-3000 ?m with a pharmaceutically acceptable particulate carrier, and (b) mixing the resultant material in a mixer to break up the agglomerate into primary particles dispersed in the pharmaceutically acceptable particulate carrier such that 90% or more of the pharmaceutically active ingredient exists as primary particles having a particle size of 50 ?m or less.

Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.

Abstract: A foamable pharmaceutical composition and a method of treating corticosteroid-responsive dermatoses of the skin are disclosed. The foamable pharmaceutical composition comprises a corticosteroid compound as an active ingredient; a quick-break foaming agent including an aliphatic alcohol, water, a fatty alcohol and a surface active agent; a buffering agent; and a propellant. The foamable composition is disposed within a pressurizable container that comprises an aerosol valve assembly including a dip tube communicating with a valve orifice through which the foamable composition is dispensed and an actuator to start and stop dispensation. The valve assembly dispenses a conically-shaped spray at a rate of about 2 to about 0.3 g/sec and provides a foam having a density of about 0.12 to about 0.25 when sprayed at a distance of about 5 to about 10 cm from the valve orifice onto a glass surface that is at ambient room temperature.

Abstract: A process for preparing particles having a hydrophobic material therein is disclosed. The process comprises providing a multiple emulsion comprising a first emulsion dispersed in a hydrophobic medium, said first emulsion comprising a hydrophobic phase dispersed in a hydrophilic phase, wherein the hydrophobic phase comprises the hydrophobic material and the hydrophilic phase comprises a precursor which is capable of reacting to form a non-fluid matrix and reacting the precursor in the multiple emulsion to form the matrix in the form of the particles having the hydrophobic material therein wherein the precursor is added prior to formation of the multiple emulsion. Also disclosed are particles having a hydrophobic material therein, which may be releasable, as well as particles having a hydrophobic material therein, which may be releasable, made by the process and methods of using the particles.

Abstract: The present invention provides an implantable device having a coating including a slow dissolving polymer or material and the methods of making and using the same.

Abstract: A biodegradable film (4) characterized in that it is prepared from at least one co-product derived from a soya bean-processing process aimed at obtaining soya-based final products by ultrafiltration, said co-product being selected from the group comprising the okara and the permeate. Such a film can be used as a food or pharmaceutical film, in particular for preparing a product for topical administration (1) of a pharmaceutical active ingredient, such as oestrogens.

Abstract: The present invention provides a patch preparation that has an extremely low moisture permeability, has a sufficient ODT effect, is excellent in drug releasability, and has a preferred handleability. The patch preparation of the present invention includes a support; and a pressure-sensitive adhesive layer containing an adherent polymer and a drug on one surface of the support, wherein: the support has a polyester base layer, an inorganic oxide layer, and a polyester nonwoven fabric layer in the stated order; the polyester base layer has a thickness of 1.0 ?m to 16 ?m; and the pressure-sensitive adhesive layer is laminated on the polyester base layer.

Abstract: The present invention provides a pharmaceutical composition for enhancement of adiponectin production, treatment or prevention of hypoadiponectinemia, and the like, comprising as an active ingredient an HMG-CoA reductase inhibitor.

Abstract: The present invention is directed to compositions and methods of delivery of CoQ that is reduced in the presence of lipoic acid and, optionally a fatty acid and/or optionally in a monoterpene. The compositions that include the reduced CoQ can be formulated in soft gel capsules.

Abstract: The invention is directed to a method of treatment of a cancer, in a mammal, the method comprising administering to said mammal in need of such treatment an effective amount of a cell growth inhibitory compound of formula I or a pharmaceutically acceptable salt form thereof.

Abstract: The present invention relates to a composition for the treatment of skin and ear infections in humans and animals such as dogs, cats and horses. In particular, the present invention relates to a topical composition comprising acetic acid, an antibacterial and/or an anti-fungal, and preferably also an anti-inflammatory. More specifically, the composition of the present invention is a bandage, bedding, clothing, conditioner, cream, drape, dressing, film, foam, gauze, gel, lotion, mousse, otic solution, pad, patch, serum, shampoo, solution, spray, or wipe for treatment or prevention of skin infections, wherein the composition comprises about 0.1-10% acetic acid, about 0.1-10% boric acid, about 0.01-20% azole, and optionally about 0.01-20% corticosteroid.

Abstract: Methods for treating the animal central nervous system against the effects of stoke, including associated cognitive, behavioral and physical impairments. Effective amounts of therapeutic agents are administered to the upper third of the stroke patient's nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of a therapeutic agent is the iron chelator deferoxamine (DFO).

Abstract: The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAM-mediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant 1 and ADAM15 variant 2, now identified and isolated.

Abstract: Embodiments described herein are directed to prostanoid (IP) receptor agonist compounds, including cicaprost and certain prodrugs, and methods of preparation and use for the same. Certain embodiments are directed to the use of cicaprost and certain prodrugs in the treatment of topical and ocular conditions.

Abstract: Disclosed are high loading, controlled-release dosage forms for oral administration of magnesium salts. For example, an oral dosage form can comprise from about 80% to about 95% magnesium lactate and one or more components. As another example, an oral dosage form can comprise at least about 50% magnesium salt and exhibit a controlled release dissolution profile. Also disclosed are methods for making controlled release dosage forms for oral administration of a therapeutically effective amount of magnesium salt to a mammal. Also disclosed are methods for treating a disorder characterized by magnesium deficiency and methods for preventing or alleviating low magnesium levels.

Abstract: The present invention relates to compounds comprising the general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms; Y and Z, which may be identical or different, are selected from the group comprising —H, —OH, —COOH, —OR3, —CH(OR3)COOH, in which R3 is selected from H, phenyl, benzyl, —CF3 or —CF2CF3, vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.

Abstract: The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed.

Abstract: Signal Transducer and Activator of Transcription (STAT) proteins have a fundamental role cell signaling, and are activated by a large number of cytokines and growth factors. One member of the STAT family, STAT3, has a critical role in oncogenesis. The present invention relates generally to disruption of the pathway of STAT3 signaling in the treatment of human cancer. STAT3 activation is shown to be present in diverse tumor cell lines and tumors, to promote oncogenesis, to inhibit apoptosis, and to reduce sensitivity to chemotherapeutic agents. Inhibition of STAT3 signaling induces apoptosis specifically in tumor cell lines, and increases sensitivity to chemotherapeutic agents. The invention relates more particularly to methods, compositions, means of administering such compositions, and means for identifying such compositions for the inhibition of STAT3 intracellular signaling in the treatment of human cancers.

Abstract: The present invention relates to a stable oral pharmaceutical composition with improved solubility and bioavailability; comprising a taxoid, a solubilizer, a stabilizing agent, a surfactant(s), a solvent(s), and an oil wherein the concentration of taxoid is in the range of 0.1 to 10%.

Abstract: The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate ?-secretase activity; improve or enhance cognitive ability; and or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.

Abstract: Disclosed is a drug delivery system from which a macrocyclic lactone can be released with a desirable zero order release profile. The system is based on the use of thermoplastic polymers, and particularly of polyethylene vinyl acetate copolymers (EVA). The drug delivery system of the invention comprises a solid non-porous reservoir in which the macrocyclic lactone is contained, preferably in a concentration well above the saturation concentration, and a non-porous skin covering the reservoir not initially loaded with the drug. The system is preferably in the form of a rod, wherein the core and the skin are concentric, and the end surfaces of the rod are not skin-covered.

Abstract: A pharmaceutical composition for anti-viral cancer treatment in mammals, comprising a therapeutically effective amount of Anisomelic acid or salts thereof. The pharmaceutical composition may comprise Anisomelic acid or salt thereof in an oil-in-water emulsion, for example in an isotropic mixture of at least one oil and at least one surfactant or, alternatively, in a hydrophilic solvent and a co-solvents or surfactant or a combination thereof. A method of treating or preventing of cancer in a mammal, wherein the p53 pathway is deregulated by viral oncoproteins, is also provided.

Abstract: The present disclosure relates to methods and compositions for modulating the activity of KCNQ channels as a means for reducing the effects of aberrant KCNQ channel function associated with epilepsy, deafness and arrhythmias including but not limited to, Long-QT syndrome (“LQTS”), and atrial fibrillation. The present disclosure also relates to the discovery of certain regions of KCNQ channels that interact with various channel stimulating molecules such as, ATP, and PIP2, as well as KCNQ channel domains that effect voltage dependant channel activation. The disclosure is also directed to the use of small molecules to modulate KCNQ channel activity in a cell. Moreover, the present disclosure relates to the therapeutic effects of treating a subject with modulators of KCNQ channel activity.

Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an anticonvulsant selected from the group consisting of retigabin, lamotrigine, lacosamide, levetiracetam, carbamazepine, sultiame, phenacemide, felbamate, topiramate, pheneturide, brivaracetam, selectracetam, zonisamide, stiripentol, beclamide, mexiletin, ralfinamide, methylphenobarbital, phenobarbital, primidone, barbexaclone, metharbital, ethotoin, phenyloin, amino(diphenylhydantoin) valeric acid, mephenyloin, fosphenyloin, paramethadione, trimethadione, ethadione, ethosuximide, phensuximide, mesuximide, clonazepam, lorazepam, diazepam, clobazam, oxcarbazepine, eslicarbazepine, rufinamide, valproic acid, valpromide, aminobutyric acid, progabide, tiagabine, and the physiolo

Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.

Abstract: Compositions and methods are provided, comprising at least one beta-lactam compound selected from the group consisting of cefuroxime, a penicillin, ceftriaxone, clavulanic acid, 6-aminopenicillanic acid (6-APA) and tazobactam, for enhancing T cell mediated immune responses in a subject, such as anti-tumor and anti-viral immune responses.

Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.

Abstract: The present invention provides compounds that function as modulators of aldehyde dehydrogenase activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.

Abstract: The present invention relates to a method for enhancing arginase activity in a damaged or injured cell. In other aspects, the invention provides a method for treating a disorder that can be treated by enhancing arginase activity in a human in need thereof, the method comprising administering to the human an effective amount of a compound that enhances arginase activity. Such disorders include ischemia, hypoxia, neurodegenerative disease or condition, stroke or trauma of the nervous system. In yet another aspect, the invention provides methods for promoting regeneration of a neural cell in a human in need thereof.

Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.

Abstract: The present invention provides methods and compositions for treating subjects suffering from a disorder associated with a nicotinic acetylcholine receptor (nAChR), methods for treating a subject having a disorder that would benefit from an increase in neural plasticity, and methods for modulating the plasticity of the primary visual cortex in subjects by modulating the expression, stability, and/or activity of Lynx1.

Abstract: Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with a dermal disorder, a psychological disorder, a mental disorder, a nerve disorder, or a systemic disorder.

Abstract: There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.

Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.

Abstract: The present invention relates to a compositions for and methods of cancer treatment in which compounds of Formula I or Formula II. In some aspects, the treatment of B-cell Lymphoma or other hematopoietic cancers is encompassed. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds of Formula I or Formula II. Combination therapy with, for example, a class of therapeutics known as 26S proteasome inhibitors, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formula I or Formula II. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.

Abstract: This invention pertains to methods of treating systemic lupus erythematosus and Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-xL.

Abstract: The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

Abstract: Germline mutations in the NF1 tumor suppressor gene cause Von Recklinghausen's neurofibromatosis type 1 (NF1), a common genetic disorder of the nervous system characterized by plexiform neurofibroma development. Using adoptive transfer of hematopoietic cells, we establish that NF1 heterozygosity of bone marrow derived cells in the tumor microenvironment is sufficient to allow neurofibroma progression in the context of Schwann cell nullizygosity. Further, genetic or pharmacologic attenuation of the c-kit signaling pathway in hematopoietic cells greatly diminishes neurofibroma initiation and progression. These studies identify haploinsufficient hematopoietic cells and the c-kit receptor as therapeutic targets for preventing plexiform neurofibromas and implicate mast cells as critical mediators of tumor initiation.

Abstract: The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.

Abstract: A process for extracting antioxidants from a plant, including contacting a plant material from a guayusa plant for a first time with a solvent, thereby obtaining a first slurry, filtering said first slurry, thereby obtaining a first extract, contacting said plant material for a second time with said solvent, thereby obtaining a second slurry, filtering said second slurry, thereby obtaining a second extract, combining said first extract and said second extract, thereby generating an third extract containing at least antioxidants, xanthines, and amino acids, and substantially drying said third extract.

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

Abstract: The present invention directs a compound represented by formula (I).

Abstract: Compounds and combinations of them that inhibit phosphatidic phosphohydrolase (PAP) enzymatic activity are formulated into pharmaceuticals useful in cancer treatment. Inhibitors of PAP can be used for blocking the progression of cancers that depend on the epidermal growth factor receptor (EGFR), its oncogenic variants and other members of its ErbB tyrosine kinase receptor family, through induction of their endocytosis, thus making them inaccessible to the extracellular stimuli that promote maintenance and progression of cancer.

Abstract: This invention is directed to a method of treating opioid or opioid-like drug addiction, including acute and post-acute withdrawal symptoms, comprising treating an addicted patient with noribogaine at a dosage that provides an average serum concentration of about 50 ng/mL to about 850 ng/mL (AUC/24 h) under conditions where the QT interval prolongation does not exceed about 50 milliseconds.

Abstract: The present invention relates to solid dispersion compositions of tolvaptan and process for the preparation of oral dosage forms.