Abstract: Novel sulphur-containing compounds and pharmaceutically acceptable salts thereof are disclosed, which have utility as anti-proliferative agents against mammalian cells. The invention provides a method for synthesizing the sulphur-containing compounds.

Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.

Abstract: Disclosed herein are methods for the treatment of otic diseases or conditions with intratympanic compositions and formulations of multiparticulate auris sensory cell modulating agent administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, Ra, Rb have meanings given in the description.

Abstract: The present invention relates to method(s) of treating a subject afflicted with cancer or a precancerous condition, an inflammatory disease or condition, and/or stroke or other ischemic disease or condition, the method comprising administering to the subject or patient in need a composition comprising a therapeutically effective amount of a substituted cis or trans-stilbene. A method of treating or reducing the likelihood of Alzheimer's disease in a patient is an additional embodiment of the present invention.

Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.

Abstract: The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal.

Abstract: The present invention provides a pharmaceutical carrier system comprising a dermatological composition that is a semi-solid aqueous gel, wherein dapsone is dissolved in the gel such that the dapsone has the capacity to cross the stratum corneum layer of the epidermis, and wherein the composition also contains dapsone in a microparticulate state that does not readily cross the stratum corneum of the epidermis. The present invention also provides methods of treating dermatological conditions in G6PD-deficient patients with the composition, while avoiding adverse hematologic effects.

Abstract: A method of treating peripheral neuropathic pain in humans resulting from a peripheral nerve injury and for treating muscle spasm in humans resulting from a peripheral nerve injury comprises applying a therapeutically effective amount of a drug selected from the group consisting of a dopamine agonist, a skeletal muscle relaxant, and a combination thereof topically to the site of the injury.

Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.

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: The invention relates to the use of an oral dosage form based on microgranules and/or microtablets to reduce the abusive use of at least one active principle contained therein. The aim of the invention is to prevent the diversion of an oral dosage form based on microgranules and/or microtablets containing at least one active principle capable of causing a dependency, a gelling agent, and a gelling activator. The gelling agent and the activator are only brought into contact with each other in the event of diversion by crushing. Said judiciously selected pair of excipients confers a viscosity to the formulation, such that said formulation cannot be administered by injection or does not release the active principle rapidly by forming a gel when it comes into contact with the mucous membrane if nasally administered.

Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.

Abstract: This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic

Abstract: The present invention provides a method of selectively inhibiting PKC? in the presence of PKC?, by administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula I. The present invention also provides a method of inhibiting cytokine synthesis in a T cell, a method of inhibiting T cell proliferation, and a method of inhibiting the replication of and cytokine production by T lymphocytes, while not stimulating or inhibiting the replication of B lymphocytes.

Abstract: The use of malachite green in the form of a tetramethyldiamino-triphenyl-carbinol anhydro-oxalate [(C23H25N2)—(C2HO4)]2—C2H2O4 of the following structural formula as a drug for treating malignant neoplasms administered in a single dose of 1 to 2 g. Malachite green can be used when dissolved in an aqueous solution or in a physiological salt solution or in spirit. In different cases, the malachite green solution is perorally administered before and after a meal or is injected per rectum, or a 1% malachite green solution is intravenously introduced, or the malachite green is applied as a rectal suppository component or as a component of 1-5% ointment. The medicinal agent exhibits an extended range of therapeutic actions with respect to different oncological diseases, is freely available, not expensive, non-toxic, does not generate side effects when used in pharmaceutically acceptable doses, and makes it possible to reduce a treating time and to increase the efficiency of treatment.

Abstract: A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as neurodegenerative diseases and heart failure.

Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.

Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.

Abstract: The present invention provides pharmaceutical compositions for controlled release of pharmaceutically active agents, especially those with a high water solubility, high dose, and/or short half-life. In addition, the present application provides methods for preparing and using such pharmaceutical compositions.

Abstract: The present embodiments relate to topically delivered medication (compounded) for treatment of pain, inflammation, muscle fatigue, spasms, and/or other ailments. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include a salt load of approximately 30% or greater. The transdermal cream may include a unique base composition such that the transdermal cream may be able to remain stable and avoid degradation for six months or more and capable of effective delivery of active ingredient concentrations exceeding approximately 40% or more of the total formulation weight. The active ingredients may include a nerve depressant, NSAID, muscle relaxant, opiate agonist, local anesthetic, NMDA receptor antagonist, and a tricyclic antidepressant. In one embodiment, the transdermal cream may comprise ketamine HCL, gabapentin, clonidine HCL and baclofen.

Abstract: Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.

Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.

Abstract: A method of treating or inhibiting, in particular, pain caused by inflammation in a mammal by administering to the mammal an effective inflammatory pain alleviating amount of a (1R,2R)-3-(2-dimethylaminomethyl-cyclohexyl)-phenol compound or a physiologically acceptable salt thereof, such as the hydrochloride or citrate salt.

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 relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.

Abstract: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.

Abstract: A composition comprises surface-modified nanoparticles of at least one amphoteric metal oxide or oxyhydroxide. The nanoparticles bear, on at least a portion of their surfaces, a surface modification comprising (i) at least one surface modifier selected from lactate, thiolactate, and mixtures thereof, and (ii) at least one surface modifier selected from halide, nitrate, acetate, carbonate, formate, propionate, sulfate, bromate, perchlorate, tribromoacetate, trichloroacetate, trifluoroacetate, carboxylate comprising from one to about four alkyleneoxy moieties, chlorate, and mixtures thereof.

Abstract: In one aspect, the present invention features a tablet including: (i) a first drug layer including naproxen; (ii) a second drug layer including a decongestant (e.g., pseudoephedrine) wherein said second drug layer is a sustained release layer adapted to deliver a therapeutically effective amount of pseudoephedrine for a period of at least twelve hours; and (iii) a barrier layer that does not include naproxen, wherein the barrier layer is in contact with the first drug layer; and (iv) a third drug layer including cetirizine, wherein the third drug layer is in contact with the barrier layer and is not in contact with the first drug layer.

Abstract: Use of a composition for treating Alzheimer's disease, osteoporosis, sleep apnea, erectile dysfunction, McArdle disease, or a carbohydrate metabolism disorder, or for reducing aging or fatigue. The composition includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5?-monophosphate-activated protein kinase activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.

Abstract: Provided are novel compositions which uniquely inhibit sphingosine kinase Type 1 (SphK1) and which are useful in a number of applications including killing or damaging cancer cells, inducing apoptosis, inhibiting growth, metastasis and development of chemoresistance in cancer cells, leukemia, increasing the effectiveness of anti-cancer agents, attenuating immune reactivity, inhibiting survival signaling in cancer cells, and reducing symptoms of multiple sclerosis.

Abstract: The present invention provides a process for preparing a pharmaceutical composition of fingolimod comprising: (i) obtaining a intimate admixture comprising fingolimod or a pharmaceutically acceptable salt thereof, and at least one surfactant (wetting agent), e.g., an intimate admixture of the fingolimod and the at least one surfactant, and (ii) optionally combining the intimate admixture from step (i) with one or more excipients. Also provided are pharmaceutical compositions and dosage forms obtainable by the process, uses of the pharmaceutical compositions and dosage forms, and methods of treating appropriate diseases with the pharmaceutical compositions or dosage forms.

Abstract: The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material; and method of using said tablet to treat pain and other conditions.

Abstract: The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) a plurality of coated particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a physiologically acceptable polymer, preferably a polyalkylene oxide; and form a discontinuous phase within the matrix material; which preferably provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.; and method of using said tablet to treat pain and other conditions.

Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.

Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.

Abstract: The present invention relates to a topical, emulsive composition containing Dapsone or its derivative. The inventive composition incorporates emollients and Dapsone or its derivative in a stable emulsion. The stability is achieved through the use of a combination of certain surfactant mixtures and an enhancer providing solubility of the Dapsone.

Abstract: The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.

Abstract: Methods of inhibiting phagolysosomal fusion in patients infected with a microorganism involve the administration of a 4-hydroxyphenylpyruvate dioxygenase (HPPD)-inhibiting compound, such as 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) to the patient. A HPPD-inhibiting compound administered in an amount effective to enhance phagolysosomal fusion in the macrophages or neutrophils of the patient reduces or treats the infection. Methods for treating bacterial infections by administering a HPPD-inhibiting compound and reducing the production of pyomelanin or melanin in microorganisms are disclosed.

Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.

Abstract: There is disclosed a composition for oral administration of O-desmethyltramadol. There is further disclosed a method for treating disorders modulated by at least opiate receptor activity or monoamine activity, including acute and chronic pain, comprising administering a pharmaceutical formulation comprising O-desmethyltramadol. Compositions and methods are also provided that are effective for overcoming resistance to tramadol in patients.

Abstract: The invention provides compounds of formula I and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.

Abstract: Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.

Abstract: Aerosolized dapsone (or alternatively, an aqueous formulation of dapsone) is used to treat airway inflammation, particularly chronic neutrophil-dominated inflammation. Diseases that may be prevented or treated by the methods include chronic obstructive pulmonary diseases (COPDs), asthma, cystic fibrosis, and others.

Abstract: A method of treating pain, e.g., acute post-operative pain, by administering to a human patient(s) a therapeutically effective dose of tramadol intravenously over a prolonged time period is disclosed. In certain embodiments, the dose is intravenously administered in a time period from about 10 minutes to about 3 hours, preferably from about 10 minutes to about 30 minutes. In other embodiments, intravenous doses are administered at suitable time intervals over a time period from about 3 hours to 48 hours.

Abstract: It is an object of the present invention to provide a substituted propanamide derivative or a pharmacologically acceptable salt thereof that is useful as a prophylactic or therapeutic agent for a bone metabolic disease. The present invention relates to a pharmaceutical composition comprising a compound having General Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; R2 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; and X represents a hydroxyl group or a C1-C6 alkoxy group, for example].

Abstract: The present invention provides a method of treating cancer using benzoic acid derivatives, alone or in combination with standard treatments such as chemotherapy and radiotherapy. Also provided are methods of screening for benzoic derivatives based on their ability to inhibit the enzyme tyrosinase or to bind to and activate PXR/SXR xenobiotic receptors.

Abstract: The invention describes essentially a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I), as defined herein before. Furthermore, it describes the corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin. Thus, the invention describes how and in which form the compounds of the formula (I) or their acid addition salts are used to deter vermin from materials, places or warm-blooded animals.

Abstract: The present invention relates to veterinary compositions in a form of an orally deliverable tablet, and more particularly to a controlled-release composition that provides sufficiently long duration to permit once daily administration.