Abstract: The present invention provides methods and compositions for sequentially and separately reducing infection and/or inflammation and regenerating tissue at a lesion site, by contacting the lesion site with a biodegradable scaffold that first delivers one or more agents at the lesion site to reduce infection and/or inflammation and then delivers one or more agents to regenerate tissue at the lesion site after inflammation is reduced.

Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention is a system and methods of establishing a Melanocyte Protection Factor (MPF), which indicates the level of protection against DNA damage to a target cell, such as the level of protection a particular sunscreen offers against UVA rays when compared to the unprotected case, i.e., no sunscreen. The present invention determines and records levels of stable melanin radicals (SMR) in a target cell. Light is applied to the target cell forming light-induced melanin radicals (LIR). The levels of SMR and intensity of LIR are measured to determine the amount of incident light reaching the target cell.

Abstract: A compound of general formula (I) wherein A, Y, W, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.

Abstract: The present invention is directed to nanoparticulate compositions comprising statin such as lovastatin or simvastatin. The statin particles of the composition have an effective average particle size of less than about 2000 nm. In another aspect of this invention, novel combinations of statins and other cholesterol lowering agents are described and methods of using same are taught.

Abstract: Compositions containing 5,6,7-trihydroxyheptanoic acid and analogs and their use for treating posterior segment ocular diseases and diseases characterized by cellular hyperproliferation or angiogenesis, are disclosed.

Abstract: Inhibiting the enzymic action of tyrosinase in the melanocyte prior to, during, or after ultraviolet (UV) radiation exposure, including over-exposure causing erythema, or sunburn, prevents the production of melanin and thereby melanoma. Melanoma can be prevented by using a tyrosinase inhibitor agent that inhibits the enzymic action of tyrosinase to prevent damage and/or death of melanocytes. The inhibitor agent can be applied to the skin or ingested.

Abstract: A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier.

Abstract: The present invention provides a process for preparing a redispersible powder of nanoparticles of a water-insoluble organic compound, the process including the steps of: (i) preparing an oil-in-water microemulsion comprising a water-insoluble organic compound, a volatile water-immiscible organic solvent, water, and at least one surfactant; and (ii) removing the volatile water-immiscible organic solvent and the water so as to form the redispersible powder comprising said nanoparticles, wherein the nanoparticle are in a particulate form, and wherein the solubility of the water-insoluble organic compound is at least about 5 times greater than the solubility of the water-insoluble organic compound in unprocessed form. Step (i) can further include the addition of co-solvent or polymer.

Abstract: Methods and formulations for treating metabolic disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.

Abstract: Described herein are microneedle bioactive agent delivery systems, associated apparatus and methods of using such. The microneedles described herein are deliverable using a needle or syringe apparatus that can interface with existing medical devices or the devices can be used as standalone systems. The systems deliver at least one bioactive agent to a tissue in need thereof, for example, the myocardium.

Abstract: Disclosed is a method of treating chronic obstructive disease, said method comprising administering an effective amount of a CXCR2 antagonist and administering an effective amount of at least one drug selected from the group consisting of: angiotensin-converting enzyme inhibitors, Angiotensin II receptor antagonists, cardioselective beta blockers, and lipid regulating drugs. Examples of the CXCR2 antagonist include: (formula 1.0A and 1.0B).

Abstract: The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: A method is provided for treatment of a condition including at least one weakened vertebra or one compression fracture of a vertebra, wherein in at least one embodiment, the vertebra is injected by vertebroplasty or kyphoplasty with particles, grains or granules or a mixture thereof, or an implant suspension including at least one resorbable fluid vehicle and particles, grains or granules or a mixture thereof, wherein the particles, grains or granules individually have a mean length from one side to the opposite side, through a geometrical centre, of up to 5 mm. Moreover, at least one embodiment of the present invention also provides use of the particular or granular material disclosed above, for the manufacture of a medicament for the vertebroplastic treatment or kyphoplastic treatment of a condition including at least one weakened vertebra or one compression fracture of a vertebra.

Abstract: Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided.

Abstract: Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.

Abstract: A pharmaceutical composition for the oral administration of omega polyenoic fatty acids combined with one or more active principles incompatible therewith, is described; also described is a process for preparing said pharmaceutical composition.

Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.

Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.

Abstract: Sulfanyl-tetrahydropyran-based compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment of diseases and disorders such as diabetes and obesity are disclosed.

Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.

Abstract: The present invention relates to novel dihydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: A pharmaceutical or nutraceutical tablet for oral administration comprising at least two fatty acids or derivatives thereof and cyclodextrin. Surprisingly, we have now found that fatty acids or derivatives thereof, especially fatty acid esters, preferably in the form of complexes with cyclodextrins prepared as stable solid materials, can easily be transformed into tablets with very high concentration of the fatty acid compound. The present inventors have realised that ideal dosage forms for these compounds are tablets and these are readily swallowed and are cheap to manufacture. In particular, the inventors have found that tablets containing complexes of fatty acids or derivatives thereof with cyclodextrin can be prepared by direct compression and moreover they can be prepared having a very high concentration of the desired active agent.

Abstract: A gel formulation for use in filling a wound cavity and delivering active ingredient thereto, having a pH range of 6.5 to 7.5, low bioadhesive strength and cohesive integrity and being a PVA borate gel including an active ingredient and a modulator to bind borate and/or PVA in aqueous solution through a mono-diol or di-diol formation and reduces the pH of PVA-borate hydrogels. A suitable modulator is a sugar alcohol such as mannitol and the active ingredient, a medicament suitable for topical application such as a local anaesthetic and/or an antibiotic.

Abstract: The present invention provides the following capsule preparation, which is superior in dissolution property and the like of a pharmaceutically active ingredient and contains liquid and solid pharmaceutically active ingredients: a seamless capsule containing liquid and solid pharmaceutically active ingredients, wherein the liquid pharmaceutically active ingredient is encapsulated in the form of a liquid pharmaceutical composition, and the solid pharmaceutically active ingredient is dispersed in a capsule shell layer.

Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.

Abstract: The present invention relate to the use of a combination of an inhibitor of miR-122 and an inhibitor of VLDL assembly, for the treatment of HCV, hyperlipidemia and hypercholesterolemia.

Abstract: Methods are provided herein to determine if a subject is a candidate for treatment with an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR). The method includes determining the presence of at least one polymorphism in the HMGCR gene in a sample from a subject. The presence of at least one polymorphism indicates that the subject is a candidate for treatment with a statin, for example to decrease risk of or treat cancer, cardiovascular disease, diabetes, obesity, inflammatory disease, or auto-immune disease.

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 incorporating drugs into an implantable medical device. In one variation, water insoluble drugs are used to form crystals within the porous structure of the device. Upon implantation, the drug crystals dissolve slowly and release the drug into the surrounding tissue. In one example, a water insoluble drug is crystallized within the pores of an ePTFE vascular graft.

Abstract: Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from Pseudomonas and/or Erwinia. Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions.

Abstract: Combination therapies comprising a drug metabolized by cytochrome P450 and a growth hormone (GH)-inducing compound (such as a GRF molecule) are described, in which there are no or substantially no drug interactions.

Abstract: A combination therapy is disclosed for treating or inhibiting cardiovascular or metabolic diseases or conditions through a combination of at least one inhibitor of neutral endopeptidase (=NEP), at least one inhibitor of the endogenous endothelin producing system and at least one HMG CoA reductase inhibitor. Pharmaceutical compositions are also described comprising NEP inhibitors, inhibitors of the endogenous endothelin producing system and HMG CoA reductase inhibitors and the use of these pharmaceutical composition in the prophylaxis or treatment of cardiovascular and/or metabolic disorders or diseases in mammals (including humans).

Abstract: Multi-dose active agent packages and methods for using the same for treating a subject for a condition are provided. Aspects of the invention include a multi-dose active agent package containing a plurality of unit dosage forms of an active agent configured to modulate at least a portion of a subject's autonomic nervous system during at least one season of the year. The active agent is present in an amount sufficient to alter the parasympathetic activity/sympathetic activity ratio of the subject in a manner effective to treat the subject for the condition. The subject active agent packages and methods find use in the treatment of a variety of different conditions, including disease conditions that increase in severity and/or occurrence during one or more seasons of the year. Also provided are kits for use in practicing the subject methods.

Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-?) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: Co-therapy of an anti-obesity agent, a statin, is disclosed along with fixed combinations thereof. Atorvastatin and orlistat are preferred as the various components.

Abstract: The present invention relates to a combination therapy for the treatment of cardiovascular disorders. More particularly, the invention relates to compositions combining long-chain optionally substituted amphipatic carboxylates (known as MEDICA drugs) and particularly, M16??, M16?? and M18??, with HMG-CoA reductase inhibitors (known as statins). The compositions of the invention may particularly be used for the treatment of cardiovascular disorders, for elevating HDL-cholesterol levels, decreasing non-HDL-cholesterol and particularly triglycerides, and decreasing insulin resistance in a subject suffering from Metabolic Syndrome or cardiovascular disorders. The invention further provides methods of treatment of such disorders using these combined compositions.

Abstract: The present invention provides a preventive or therapeutic drug for a myeloma tumor and osteoclastic bone loss associating therewith, the drug containing as an active ingredient an osteopontin-production regulator or inhibitor; a screening method for a preventive or therapeutic drug for a myeloma tumor, characterized by determining osteopontin production regulatory or inhibitory effect; as well as a diagnostic kit for a myeloma tumor, characterized by including a reagent for measuring blood osteopontin level, and a diagnostic method.

Abstract: Rosacea is treated with a composition comprising an antimicrobial and at least one of an anti-inflammatory and a non-retinoid inhibitor of at least one of NF-KB, AP-1, MMPs, adhesion molecules, TLRs, and CD14. The composition may further comprise a retinoid.

Abstract: The invention relates to dioxaspiroketal derivatives of formula (I): wherein R, is selected from the group consisting of H, straight or branched chain C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, cycloalkyl, heterocyclyl, phenyl, optionally para-, meta- or ortho-substituted with 0 to 3 substituent selected from halogen, —CN, —NH2, —OH, —NO2, COOR2, wherein R2 is selected from H and C1-C6 alkyl, n is 1 or 2, X is O or S, R1 is selected from H, OH, halogen, C1-C6 alkyl, C1-C6 alkoxy, COOR3, wherein R3 is selected from H and C1-C6 alkyl, or physiologically acceptable salts thereof, process for preparation thereof, their uses in medical field, in particular as anti-tumour medicaments.

Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.

Abstract: Esters of compounds in the leptomycin family, having a structure according to formula I where R, R10, R11, R12, R13, and R14 are as defined herein, exhibit anti-tumor properties.

Abstract: Skin brightening compositions based on esters of 5-hydroxy-2-methyl-4H-pyran-4-one. Also disclosed are methods of making the compositions as well as methods of using the compositions.

Abstract: Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders.

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.