Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: The present invention provides a transdermal patch having excellent preservation stability and transdermal absorbency of DMAE or its pharmacologically acceptable salt. The patch has a support and a plaster layer integrally laminated on one surface of the support, and the plaster layer includes: 2-amino-1-(2?,5?-dimethoxyphenyl)ethanol or its pharmacologically acceptable salt; 40 to 98% by weight of 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 1 to 30% by weight of saturated aliphatic monohydric alcohol having an alkyl group with a carbon number of 10 to 30.

Abstract: An abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.

Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.

Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of tramadol or a pharmaceutically acceptable salt thereof, the combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of tramadol or a pharmaceutically acceptable salt thereof such that the dosing interval of the meloxicam overlaps with the dosing interval of the tramadol, the combination in an amount sufficient to provide an analgesic effect in a human patient.

Abstract: The present teachings provide compounds of Formulae I and II: and pharmaceutically acceptable salts, hydrates, complexes, esters, and prodrugs thereof, wherein R1, R1?, R2, R2?, R3, R3?, and X are as defined herein. The present teachings also provide methods of making the compounds of formulae I and II, and methods of treating RyR-associated conditions, disorders, and diseases that include administering a therapeutically effective amount of a compound of formula I or II to a subject in need thereof. In addition, the present teachings relate to methods of reducing the open probability of a ryanodine receptor, and methods of reducing Ca2+ release across a ryanodine receptor (e.g., into the cytoplasm of a cell), by contacting a compound of formula I or II with a ryanodine receptor.

Abstract: Use of a polylysine, polyamidoamine or polypropylenimine dendrimer having naphthyl disulphonate terminal groups as a topically applied agent in prophylaxis or treatment of sexually transmitted diseases.

Abstract: The present invention focuses on a process for the hydrogenation of aromatic or heteroaromatic compounds and in particular on the ring hydrogenation of compounds having the formula (I). Aromatic amino acids and amino alcohols can be successfully ring-hydrogenated using a platinum-rhodium mixed catalyst. The products can be used inter alia as mimetics in bioactive peptide active ingredients.

Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial 3 to 6 days of treatment the daily dosage is raised so that in total the R-fold (R being the accumulation factor) standard daily dosage is administered and thereafter continued at the standard daily dosage or at a daily dosage lower than the standard daily dosage.

Abstract: A pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing a pharmacologically active ingredient (A); a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof; a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form; wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).

Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, and when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt, an N-oxide form, a solvate, or a prodrug thereof; and a medicament which includes those. The compound of formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.

Abstract: The present invention relates to the preparation of compositions comprising benzoyl peroxide, with or without other additional active ingredients. The process involves introducing benzoyl peroxide, along with any other active ingredients present, into a fatty substance that contains and protects the ingredients that would otherwise be unstable when in contact with one another. The composition is designed to allow all ingredients to become available for skin contact or skin absorption when the fatty substance softens and/or melts as the composition is applied to the skin. The benzoyl peroxide may be pre-micronized to a particle distribution size of about d90 of 0.1 to 150 microns, preferably d90 of 10 to 15 microns.

Abstract: A pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing a pharmacologically active ingredient (A); an anionic polysaccharide (B) obtainable by introducing anionic functional groups, in protonated form or a physiologically acceptable salt thereof, into a polysaccharide; and a polyalkylene oxide (C); wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the anionic polysaccharide (B) and the polyalkylene oxide (C).

Abstract: The invention relates to pharmaceutical salts comprised of a pharmaceutical active substance and of at least one sugar substitute, to medicaments containing these salts, and to the use of these salts for producing medicaments.

Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.

Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.

Abstract: A pharmaceutical dosage form for controlled release of the active substance 3-(2-dimethylaminomethylcyclohexyl)-phenol, preferably (1R,2R)-3-(2-dimethylaminomethylcyclohexyl)-phenol, or a pharmaceutically acceptable salt thereof, which dosage form (i) in vivo produces a peak plasma level of the active substance after 2 to 10 hours, and/or (ii) in vitro releases 3.0 to 37 percent by weight of the active substance originally contained in the dosage form after one-half hour, 5.0 to 56 percent by weight after one hour, 10 to 77 percent by weight after two hours, 15 to 88 percent by weight after 3 hours, at least 30 percent by weight after six hours, at least 50 percent by weight after 12 hours, at least 70 percent by weight after 18 hours, and at least 80 percent by weight after 24 hours when measured according to the European pharmacopoeia using a blade mixer in preferably 900 ml of a buffer solution at a pH value of 6.9, a temperature of 37° C., and 75 rpm.

Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.

Abstract: A pharmaceutical formulation for prolonged release of the active ingredient 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol or a pharmaceutically acceptable salt thereof in a matrix containing between 1 and 80 wt. % of at least one pharmaceutically acceptable hydrophilic or hydrophobic polymer as a matrix forming agent and exhibiting in vivo the following release rate: 3 to 35% by weight (based on 100% by weight active ingredient) 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 0.

Abstract: Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.

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: The invention provides a method of treating comorbid premature ejaculation and erectile dysfunction. In particular, the method comprises administering an effective amount of a tramadol material and an effective amount of a phosphodiesterase inhibitor. The invention also provides a pharmaceutical composition comprising a pharmaceutically-acceptable carrier, a tramadol material and a phosphodiesterase inhibitor. The invention further provides a kit comprising a tramadol material and a phosphodiesterase inhibitor.

Abstract: The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor.

Abstract: In vitro and in vivo methods for identifying compounds capable of targeting suppressed cancer cells such as micrometastatic cells. The in vitro method includes the steps of comparing the response to a test compound of cancer cells grown on a suppressing cell support matrix which causes suppression of a malignant phenotype in a growing cancer cell and on a non-suppressing cell support matrix. The in vivo method includes a step of co-injecting labeled cancer cells with a malignant-phenotype suppressing matrix into a test animal to produce suppressed micrometastatic cells therein.

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

Abstract: The invention provides methods for detection of medical disorders, associated with cellular oxidative stress, cell degeneration and/or cell death. The invention further relates to compounds comprising a thiol (—SH) group, for detecting cells undergoing oxidative stress, degeneration and/or a death process. The invention further provides methods for utilizing the compounds in medical practice, for diagnostic and therapeutic purposes.

Abstract: Disclosed herein is an oral controlled release pharmaceutical formulation comprising water-soluble drug or pharmaceutically acceptable salts thereof, in a hydrophilic matrix system, further comprising pH independent polymers present in an amount of 5% to 90% w/w in combination with acid insoluble polymer present in an amount of 1% to 70% w/w and/or a diluent, a lubricant and/or a glidant.

Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.

Abstract: The invention provides compositions and methods for reducing one or more symptoms of an autoimmune disease, inflammatory disease, and/or transplant rejection, by the administration to a subject in need thereof a pharmaceutically effective amount of a purified compound of any one of Formulae A-E. The invention's methods are useful for the prevention, amelioration, and treatment of autoimmune disease, inflammatory disease, and/or transplant rejection.

Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.

Abstract: The invention discloses an implant suitable for delivery of at least one drug, the implant comprising a fibrillar collagen matrix having, as measured in Example 1, a viscosity of greater than 100 mPas, optionally greater than 103 mPas, further optionally greater than 106 mPas, still further optionally greater than 109 mPas when a collagen dispersion formed from 140 mg of the fibrillar collagen matrix is dispersed in 25 ml of 2 mM HCl at a pH of less than 3.5 and at a temperature of 30.0+/?0.5° C.

Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.

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 discloses the treatment of dermatological conditions in G6PD-deficient patients with the composition, while avoiding adverse hematologic effects.

Abstract: In one aspect, the invention relates to a method for identifying a drug candidate with activity as a neuroprotective agent. The method includes determining whether a compound reduces ATF4 activity; and identifying the compound that reduces ATF4 activity as a drug candidate.

Abstract: A multiple total daily dose regimen is developed in order to decrease the use by a patient of a tolerance-inducing pharmacological agent. In one example, the method reduces or phases out altogether a patient's chronic use of opioid drugs by use of a successive reduction of the total daily dose of an opioid drug in sub-therapeutic decrements over the course of 3-7 days per therapeutic dose.

Abstract: The present invention provides new tyrphostin derivatives acting as substrate competitive protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.

Abstract: A crystalline salt of 3-[2-(dimethylamino)methyl(cyclohex-1-yl)]phenol and hydrogen chloride, preferably in a 1:1 composition, including various crystalline forms of this salt, processes for preparing the various crystalline forms of this salt, pharmaceutical compositions containing the various crystalline forms of this salt, and the use of this salt as a pharmacologically active agent in a pharmaceutical composition to treat or inhibit pain or other disorders or disease states.

Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.

Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.

Abstract: The present invention features methods of treating a mammalian subject having renal cancer by administration of certain dimethylsulfonate compounds, such as a 4-[bis[2-[(methylsulfonyl)oxy]ethyl]amino]-benzaldehyde. The present invention further features administration protocols and dosing schedules for methods of treating patients having renal cancer and pharmaceutical compositions suitable for use in the treatment methods provided herein.

Abstract: Metabolites of [2-(3-methoxyphenyl)-cyclohexylmethyl]dimethylamine as free bases and/or in the form of physiologically acceptable salts, corresponding medicaments, the use of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for producing a medicament used for treating depression, and related methods of treating depression, pain and urinary incontinence.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same, their uses in pharmaceutical formulations, and for the treatment of various disorders, including pain.

Abstract: Salts and/or co-crystals of (+)-3-[2-(dimethylamino)-methyl-1-hydroxycyclohexyl]-phenol or of (?)-3-[2-(dimethylamino)methyl-1-hydroxy-cyclohexyl]phenol, present in crystalline form, with cinnamic acid, C8- to C10-alkane-monocarboxylic acids, C6- to C10-alkanedicarboxylic acids, C15- to C17-alkane-monocarboxylic acids, fumaric acid, tartaric acid, mandelic acid, hippuric acid and/or embonic acid, a process for their production, and the use of such salts and/or co-crystals as medicaments.

Abstract: The invention provides compositions and methods for treating pulmonary diseases and conditions. The provided compositions and methods utilize either low concentrations of selective ?-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for ?-2 over ?-1 adrenergic receptors or ketamine at specific pH. The compositions preferably comprise brimonidine and/or dexmedetomidine and/or ketamine.

Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

Abstract: The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.

Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.

Abstract: Disclosed is a pharmaceutical composition simultaneously having a rapid acting property and a long-acting property, comprising a sustained-release part coated with a water-insoluble polymer on the surface, comprising a first active pharmaceutical ingredient, at least one release control base selected from the group consisting of water-insoluble polymer, and water-soluble viscous polymer, and a pharmaceutically acceptable carrier; and, an immediate release part comprising a second active pharmaceutical ingredient and a pharmaceutically acceptable carrier.

Abstract: The present invention provides compositions containing one or more antimicrobial peptide sequestering compounds and methods for topical application of such compositions to the skin to treat skin diseases and disorders such as rosacea in humans.

Abstract: A water-dispersible particle is provided that includes organic origin potash in an amount ranging from 5% to 99.9% by weight of the total dry weight of the particle. A binder component is present in an amount from 1% to 95% by weight. The organic origin potash and the binder component on that contact with water causes particle dispersion into more than 100 pieces. A process for making a water-dispersible particle includes mechanical aggregation of the potash into a pellet. A binder component is present in the particle in an amount ranging from 1% to 95% by weight. The potash and the binder component are present in a form such that contact with water causes particle dispersion into more than 100 pieces. The pellet is then dried and ready to be applied.