Abstract: The present invention relates to the discovery that acetylsalicylic acid (ASA or aspirin), salicylic acid (SA) and related salicylate esters and their pharmaceutically acceptable salts, when coadministered in effective amounts with a drug or other bioactive agent which typically (in the absence of the salicylate compound) produces significant hepatotoxicity as a secondary indication, will substantially reduce or even eliminate such hepatotoxicity. Favorable therapeutic intervention results from the use of the present invention having the effect of reducing hepatotoxicity associated with the administration of certain drugs and other bioactive agents and in certain instances of allowing the administration of higher doses of a compound which, without the coadministration, would produce hepatotoxicity which limits or even negates the therapeutic value of the compound.

Abstract: The present invention relates to novel 2-phenoxy-6-phenyl- and 2-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.

Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of inflammation and cancer.

Abstract: Disclosed herein are compositions that exhibit viscosities suitable for injectable formulations. The compositions comprise bioactive agent-loaded microparticles and hyaluronic acid or a salt thereof in a suitable liquid pharmaceutical carrier. Also disclosed are methods of making and using the compositions.

Abstract: Isolated polynucleotides encoding novel galectin-8 variants polypeptides are provided. Also provided are methods and kits using same for diagnosing prognosing and treating rheumatoid arthritis (RA) and other joint/chronic inflammatory diseases.

Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).

Abstract: A tablet with an enhanced dissolution profile for a medicinally active ingredient such as aspirin and methods for making the tablet. The tablet comprises a blend of crystals of the medicinally active ingredient and a dissolution aid such as sodium or calcium carbonate or bicarbonate that coats the crystals upon co-milling. The blend is then compressed to form tablets that have an enhanced dissolution profile for the medicinally active ingredient.

Abstract: Methods and formulations for treating inflammatory bowel disease are disclosed. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of 4-aminosalicylic acid and/or 5-aminosalicylic acid, and pharmaceutically acceptable salts and pro-drugs thereof, to affected areas of the intestine, i.e., distal gut. The methods and formulations comprise modified-release elements, providing for drug delivery to the affected or desired area. Diseases and conditions treatable with the present invention include Crohn's disease and ulcerative colitis.

Abstract: The invention relates to freeze-dried molded articles, containing ?50% by wt. of one or more active substances, and >15% by wt. of one or more scaffold-forming agents, with proteins being excepted, as well as optionally one or more auxiliary substances, in each case based on the total composition of the freeze-dried molded article, whose 1% by wt. solution or suspension in water, at 20° C., has a pH value <7. Furthermore, the invention relates to methods for manufacturing these freeze-dried molded articles, the combination of such freeze-dried molded articles in kit-of-parts arrangements together with aqueous solutions, as well as the use of the freeze-dried molded articles and the kit-of-parts combinations for pharmaceutical and cosmetic application.

Abstract: The invention relates to freeze-dried molded articles comprising at least one or more active substances and optionally one or more scaffold-forming agents, optionally one or more auxiliary substances, as well as a coating comprising at least one film-forming agent. Furthermore, the invention relates to methods for manufacturing these freeze-dried molded articles, the combination of such freeze-dried molded articles in kit-of-parts arrangements together with aqueous solutions, as well as the use of the freeze-dried molded articles and the kit-of-parts combinations for pharmaceutical and cosmetic application.

Abstract: Heart diseases such as myocardial infarction and cerebro-vascular diseases remain major causes of death. The underlying disease process involved is usually atherosclerosis. The cause of human atherosclerosis is unknown. At best we know of risk factors. The purpose of the present invention is to act on the risk factors so as to reduce or prevent the development or evolution of atherosclerosis and reduce coronary heart diseases and cerebro-vascular diseases. That treatment is easy to use, effective, safe, and readily available. The present invention describes a pharmaceutical combination of medication for that very purpose. The combination comprises the following ingredients: (1) an angiotensin converting enzyme blocker (ACE), (2) a Beta adrenergic blocker, (3) an antiplatelet agent, (4) a Statin, (5) a calcium channel blocker. Some definitions need to be clarified. Arteriosclerosis is a general term describing any hardening (and loss of elasticity) of medium or large arteries.

Abstract: A method of manufacturing a dosage form is described wherein a liquid solution of a biologically compatible polymer containing a suspension of particulate material that is insoluble in the polymer is supplied to a liquid supply tube (2) having an outlet (2a) and an electrical field is established between the outlet (2a) and a surface (19) spaced from the outlet (2a) to cause liquid issuing from the outlet to form a jet which dries to form a polymer fibre containing particles of the particulate material and which deposits onto the surface (19) to form a dosage which consists of said particulate containing fibre which fibre dissolves or disintegrates in a wet environment such as the mouth.

Abstract: A vehicle to carry a powered medication that addresses the limitations of the prior art. It includes a system and method. A powder delivery system includes a first panel and a second panel coupled together around a periphery of the panels to form a sealed void therebetween, each the panel having a width and length about equal to a standard credit card width and length, respectively; and a powder, disposed in the void, having a quantity at least about equal to an active dose of the powder; wherein a thickness of the panels with the powder disposed therebetween is not greater than about 0.1 inches and more preferably not greater than about 0.03 inches.

Abstract: Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract: A method for delivering a composition for use in treatment and prevention of vascular disease by providing a vehicle for delivery of the composition to an individual, wherein the composition contains a combination of aspirin and resveratrol; administering the vehicle to the mouth of the individual, wherein the vehicle melts at the body temperature of the individual such that the aspirin and resveratrol is absorbed thru the oral mucosa and delivered directly into the inidvidual's bloodstream; and a related melting capsule comprised of a material that has the same melting point as the human body temperature and includes aspirin in the range of 81 to 325 mg and resveratrol in the range of 10 to 300 mg.

Abstract: A method for delivering acetyl salicylic acid to an individual via oral mucosal absorption by providing a melting capsule which includes a therapeutic amount of an acetyl salicylic acid; and administering the capsule sublingually in the patient such that the capsule melts at the individual's body temperature and delivers the acetyl salicylic acid directly into the bloodstream of the individual quickly and without complications; and a melting capsule comprised of a material that has the same melting point as the human body temperature and includes a therapeutic amount of an acetyl salicylic acid liquid or powder having a pH in the range of 2 to 7.

Abstract: Described is a layered or segmented controlled release pharmaceutical tablet adapted for separating one segment from another by breaking through a segment.

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: The present invention relates to a nanowire array (15, 16) for electrically-controlled elution of a therapeutic composition (5) comprising a plurality of nanoscopic-sized wires (12, 12), nanowires, attached to an electrically conducting solid support (7), said nanowires formed from electroactive conjugated polymer (4) containing or doped with said therapeutic composition (5) coated over a plurality of nanoscopic sized electrically conducting protrusions (8). It also relates to a method for preparing a nanowire array and an electrode.

Abstract: A series of substituted oxazole compounds having an alpha keto side chain at the 2 position and an aromatic, heteroaromatic or heterocycle substituent at the 5 position are disclosed. These compounds exhibit inhibition of fatty acid amid hydrolase and arc useful for treatment of malconditions involving that enzyme.

Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.

Abstract: A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump.

Abstract: The invention describes the use of betaine for treating and preventing arterites. The invention also describes an orally administered composition for treating arterites and, in particular, intermittent claudication, said composition containing, as an active ingredient, an active therapeutic quantity of betaine glycine by single dose. The invention particularly describes a medicament provided for treating a patient suffering from an intermittent claudication caused by peripheral circulatory disorders such as arteriosclerosis obliterans or by thromboangiitis obliterans.

Abstract: The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.

Abstract: The present invention relates to a preparation suitable for the prevention and/or treatment of vascular disorders, comprising the following fractions: fraction a) consisting of long chain polyunsaturated fatty acids; fraction b) consisting of phospholipids, which fraction contains at least two different phospholipids selected from the group consisting of phosphatidylserine, phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine. fraction c) consisting of compounds which are a factor in methionine metabolism, which fraction contains at least one member selected from the group consisting of folic acid, vitamin B12, vitamin B6, magnesium and zinc.

Abstract: The present invention describes polymer nanoparticles with a cationic surface potential, in which both hydrophobic and hydrophilic pharmaceutically active substances can be encapsulated. The hydrophilic and thus water-soluble substances are encapsulated in the particle core by co-precipitation through ionic complexing with a charged polymer. Both therapeutic agents and diagnostic agents can be used as pharmaceutically active substances for encapsulation. The cationic particle surface permits stable, electrostatic surface modification with partially oppositely charged compounds, which can contain target-specific ligands for improving passive and active targeting.

Abstract: Oral antidepressant formulation comprising a means for controlling the release of the pharmaceutically acceptable antidepressant active agent selected from the group consisting of SSRI agents, SNRIs (serotonin noradrenaline reuptake inhibitors), CRF antagonists, NK1 antagonists, NK2 antagonists, NK3 antagonists and combinations thereof, with respect to the release of the compound selected from the group consisting of acetylsalicylic acid, salts and esters of acetylsalicylic acid, diaspirin, and mixtures thereof.

Abstract: Disclosed herein are polypeptide multilayer films wherein a therapeutic agent is covalently linked to a first layer polypeptide. An advantage of such attachment is that the linked therapeutic agent can be controllably released from the multilayer film into the environment of the film upon the addition of a suitable stimulus. An advantage of the disclosed films and methods is enablement of environmentally-stimulated release under specific conditions.

Abstract: Provided herein methods for determining whether a subject, particularly a human subject, is at risk of developing, having, or experiencing a complication of cardiovascular disease, and methods of treating subjects who are identified by the current methods of being at risk for cardiovascular disease. In one embodiment, the method comprises determining levels of one or more oxidized apolipoprotein A-I related biomolecules in a bodily sample from the subject. Also, provided are kits and reagents for use in the present methods. Also provided are methods for monitoring the status of cardiovascular disease in a subject or the effects of therapeutic agents on subjects with cardiovascular disease. Such method comprising determining levels of one or more oxidized apolipoprotein A-I related molecules in bodily samples taken from the subject over time or before and after therapy.

Abstract: The present invention relates to new formulations comprising acetylsalicylic acid or its derivatives an oil phase and a cyclodextria in soft capsules, characterized by a high stability.

Abstract: Disclosed herein are ways to solubilize aspirin for parenteral administration containing aspirin and a diluent NNDMA (N,N-Dimethylacetamide) useful in the treatment of acute coronary syndromes as well as other disease states. The solution so constituted is stable at room temperature for prolonged periods without decomposition and avoids significant hydrolysis of the aspirin and thus the loss of the anti-platelet action when stored.

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract: A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulsion for internal, oral, direct or topical administration.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

Abstract: Combination therapy is disclosed herein for the treatment an arthritic condition (e.g. rheumatoid arthritis, osteoarthritis or psoriatic arthritis). The therapies disclosed herein comprise administering tranilast or an analogous compound in combination with a pharmaceutical agent, such as a non-steroidal anti-inflammatory drug, a disease-modifying drug, a COX-2 inhibitor, an antibiotic, an analgesic or combination thereof.

Abstract: Methods are provided for evaluating osteoarthritis (OA), for example for diagnosing OA, to confirm a diagnosis of OA, to assess or prognose progression of OA, determining the severity of a subject who has OA, and determining a subject's risk of developing OA in the future, as are arrays and kits that can be used to practice the methods. In particular examples, the method includes determining an amount of activity (such as an amount of protein present or an amount of expression) of OA risk-related molecules, such as soluble vascular adhesion protein 1 (sVAP-1) or interleukin-15 (IL-15). Also provided are methods of identifying one or more compounds that alter the activity of an OA-related molecule, thereby identifying potential anti-osteoarthritis drugs.

Abstract: The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IGT) in a patient.

Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention relates to new thiazole inhibitors of cyclooxygenase, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The microspheres have many possible applications including smart drug delivery, breaking and damper devices. In one arrangement, a microsphere comprises a shell 120 and a core 110. The core comprises a liquid, which may be a drug, while the shell comprises magnetic particles. The microsphere is deformable in response to to application of an external magnetic field. Also disclose is an arrangement in which a microsphere has a magnetic core and a PDMS shell.

Abstract: The present invention relates to a method for prolonging longevity using and NPC1L1 antagonist. The present invention also provides a method for reducing weight in an individual who consumes a high-fat diet using an NPC1L1 antagonist.

Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: Disclosed herein are novel dietary supplement compositions comprising enriched 3-O-acetyl-11-keto-?-boswellic acid and enriched demethylated curcuminoids, wherein the composition exhibits anti-inflammatory, antiulcerogenic and antioxidant activities. Also disclosed are novel compositions comprising enriched 3-O-acetyl-11-keto-?-boswellic acid, enriched demethylated curcuminoids that have a synergistic effect on specific inhibition of—COX-2 and 5-LOX activity and optionally containing glucosamine, resveratrol, garlic extract, chondroitin, methlysulphonymethane, bromelain, serratiopeptidase, quercitine, gallic acid, caffeic acid, green tea extract, aspirin and ibuprofen.

Abstract: A medical device includes a carrier and an agent. The agent is formulated to control inflammation of biological tissue, such as heart tissue, and is releasably coupled to the carrier. The carrier is configured to be disposed in operative proximity to the biological tissue to be treated by the agent. In one embodiment, the carrier is configured to release the agent or otherwise deliver the agent to the biological tissue, thus controlling inflammation of the tissue. Also, a method to improve healing of biological tissue includes placing a medical device proximate to the heart of a patient, where the medical device has a carrier and an agent configured to control inflammation, the agent is releasably coupled to the carrier. In one embodiment, the method includes causing the agent to be released from the carrier.

Abstract: The invention concerns an improved multiparticulate tablet disintegrating in the mouth in contact with saliva in less than 40 seconds. The invention is characterized in that it is based on particles of coated active principle, said particles having intrinsic compression properties and a mixture of carriers, the proportion of carrier mixture relative to coated active principle particles being 0.4 to 6 parts by weight, the carrier mixture comprising: a disintegrating agent; a diluting soluble agent with binding properties; a lubricant; a permeabilizing agent; and advantageously lubricants, sweeteners, flavoring and coloring agents, the proportion of disintegrating agent and soluble agent relative to the tablet mass being 1 to 15 wt. % for the former and 30 to 90 wt. % for the latter.

Abstract: Methods for increasing plasmin activity in a patient in need thereof are provided, comprising administering to the patient a therapeutic amount of an agent which binds to ?2-antiplasmin at a binding site to increase conversion of cc2-antiplasmin from an inhibitor to a plasmin substrate, thereby increasing plasmin activity in the patient. Also provided are methods for the identification of compounds or molecules that increase plasmin activity, comprising determining whether the compound or molecule binds to a binding site on ?2-antiplasmin which increases the conversion of ?2-antiplasmin from an inhibitor to a plasmin substrate, wherein the compound or molecule is not an antibody, thereby identifying a compound or molecule which increases plasmin activity. Further provided are pharmaceutical compositions and methods of use thereof for the treatment of myocardial infarction, thrombosis, ischemic stroke, and pulmonary embolism.