Abstract: The present invention is directed to Pak1 agonists and methods of use.

Abstract: The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.

Abstract: The invention relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin thereby treating or prevention various diseases, disorders or conditions. Additionally, the invention relates to treatment of various diseases, disorders or conditions associated with or mediated by oxidative stress since 3DG induces ROS and AGEs, which are associated with the inflammatory response caused by oxidative stress.

Abstract: The present invention comprises cosmetic compositions and methods for retarding hair growth comprising a combination of an ornithine decarboxylase inhibitor, an anti-angiogenic active and an anti-inflammatory.

Abstract: The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. This invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.

Abstract: The present invention features compositions comprising at least one compound of the formula I or formula II: wherein R1, R2, R3, R4, and R5 independently, are selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, or a cosmetically acceptable salt thereof, and the use thereof.

Abstract: Novel wash and carrier solutions ideally suited for topical administration (e.g., as wash solutions and as carrier solutions). The solutions described herein are non-toxic, non-irritating, isotonic, possess non-specific broad-spectrum antimicrobial properties, and have an alkaline pH. Also disclosed are sterile preparations of the solutions and methods of using the same.

Abstract: The present invention provides methods of detecting mutations in a Gnaq gene in a melanocytic neoplasm for diagnostic and prognostic purposes. The invention further provides methods of treating such melanocytic neoplasm by modulating the activity of the mutated Gnaq gene.

Abstract: The present invention features a process for making a lozenge product including the steps of forming a powder blend containing an amorphous carbohydrate polymer into the desired shape of the lozenge product and applying radiofrequency energy to the shape for a sufficient period of time to soften or melt said amorphous carbohydrate polymer to fuse the shape into said lozenge product.

Abstract: The present invention relates to cationic ceramides, their dihydro-analogs and aromatic analogs and their derivatives, comprising a pyridinium group. Also provided are methods for making cationic ceramides comprising a pyridinium group, and their use for treating or preventing diseases associated with cell overproliferation and sphingolipid signal transduction, such as cancer, inflammation, and stenosis. The compounds are also useful as mitochondritropic agents that are localized to mitochondria carrying with them chemical cargoes, such as drugs, or signaling molecules, such as fluorophores for probing organelle structure and functions.

Abstract: Disclosed is a class of compounds which inhibit the enzymatic conversion of fructose-lysine into fructose-lysine-3-phosphate in an ATP dependent reaction in a newly discovered metabolic pathway. According to the normal functioning on this pathway, fructose-lysine-3-phosphate (FL3P) is broken down to form free lysine, inorganic phosphate and 3-deoxyglucosone (3DG), the latter being a reactive protein modifying agent. 3DG can be detoxified by reduction to 3-deoxyfructose (3DF), or it can react with endogenous proteins to form advanced glycation end-product modified proteins (AGE-proteins) Also disclosed are therapeutic methods of using such inhibitors to alleviate deleterious effects of 3DG.

Abstract: The present invention provides new ceramide analogs indicated as the compounds of formula (II). These novel analogs exhibit a significant anti cancerous effect and are therefore provided as a pharmaceutical composition for treating cell proliferative diseases, neurodegenerative disorders, metabolism-associated conditions, infectious diseases, and immune-related disorders. The invention further provides combined compositions and kits combining the novel ceramide analogs of formula (II) with an additional therapeutic agent.

Abstract: The invention provides a process for the production of nanoparticle carriers for drug delivery, said nanoparticles being produced by preparing a double emulsion of water-oil-water including one or more polymer which forms the basis of the nanoparticle carrier, blending the drug to be delivered into one of the emulsion phases, doping either the oil-phase or the outer-water phase with a carbohydrate, and spray drying the emulsion to form nanoparticles of a narrow particle size distribution of 100 nm to 1000 nm, which nanoparticles are substantially spherical.

Abstract: An anti-aging composition is provided that contains high potency retinol along with anti-irritant properties. In particular, an anti-aging composition includes a base, from about 0.001% to 20.0 vol % retinol, at least one anti-irritant agent, at least one antioxidant, at least one anti-inflammatory agent, and a moisturizing complex. In one non-limiting illustration, the anti-aging composition contains about 1.0 vol % retinol, plantago lanceolata, hypericum perforatum leaf extract, phytosphingosine, leontopodium alpinum extract, glycyrriza glabra root extract, sambucus nigra flower extract, nordihydrognaiaretic acid, oleanolic acid, spiraea ulmaria flower extract, evodia rutaecarpa fruit extract, boswellia serrata extract, and additives.

Abstract: The use of bis-amines to enhance the antimicrobial activity of pharmaceutical compositions is described. The bis-amines are particularly useful for enhancing the antimicrobial activity of aqueous ophthalmic compositions, such as artificial tears or ocular lubricants, and solutions for disinfecting contact lenses.

Abstract: The present invention relates to the use of sphingolipids for the preparation of a food item, a food supplement and/or a medicament for the treatment of insulin resistance, diabetes mellitus type 2 and/or metabolic syndrome. In particular, the invention relates to the use of a sphingolipid with the general formula (I): wherein Z is R3 or —CH(OH)—R3; A is sulphate, sulphonate, phosphate, phosphonate or —C(O)O—; R1 is H, hydroxyl, alditol, aldose, an alcohol, C1-C6 alkyl or amino acid; R2 is H or unsaturated or saturated (C1-C30) alkyl chain; R3 is unsaturated or saturated (C1-C30) alkyl chain; Q1 is a primary amine group (—NH2), secondary amine group (—NH—) or an amide group (—NH—CO—); and t is 0 or 1, or a precursor, a derivative or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the prevention and/or treatment of a disorder selected from the group consisting of insulin resistance, diabetes type 2 and metabolic syndrome.

Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Abstract: The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.

Abstract: The invention relates to novel cosmetic uses of phytosphingosine or of one of its cosmetically acceptable salts, particularly its hydrochloride, as a slimming agent and/or as an active agent which stimulates the synthesis of leptin by adipocytes, for preparing a cosmetic composition intended for reducing subcutaneous excess fat. The invention also relates to a method of cosmetic treatment intended for obtaining a slimming effect on the human body according to which a cosmetic composition containing phytosphingosine or one of its cosmetically acceptable salts, particularly its hydrochloride, is applied on the parts of the body to be treated. The invention also relates to novel cosmetic compositions containing phytosphingosine or one of its cosmetically acceptable salts, particularly its hydrochloride, in combination with a lipolytic agent selected from the group consisting of CAMP and its derivatives, adenylate cyclase enzyme activating agents and phosphodiesterase enzyme inhibiting agents.

Abstract: The present invention features compositions comprising at least one compound of the formula I or formula II: wherein R1, R2, R3, R4, and R5 independently, are selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, or a cosmetically acceptable salt thereof, and the use thereof.

Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.

Abstract: Chronic obstructive airway diseases are treated by administering an osmotically active compound such as a salt, sugar, sugar alcohol, or organic osmolyte to the afflicted airway surface. The compound may be administered as a liquid or dry powder aerosol formulation. Diseases that can be treated by the method include cystic fibrosis, chronic bronchitis, and ciliary dyskinesia. The formulations of the invention can also be used in conjunction with other active agents such as bronchodilators, sodium channel blockers, antibiotics, enzymes, or purinoceptor agonists on airway surfaces.

Abstract: The present invention relates to the use of alkoxylated amines to enhance the activity of fungicidal formulations comprising fungicidal triazoles. It also relates to formulations comprising one or more fungicidal triazoles and alkoxylated amines. These formulations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, biodegradable material and textiles against deterioration due to the action of fungi.

Abstract: Described are a method of killing microorganisms in aqueous industrial systems or products for industrial applications based on water by adding from 0.001 to 5% by weight of a water-soluble or water-dispersible polymer containing from 30 to 100 mol % of styrenesulfonic acid, from 0 to 40 mol % of an N-vinyllactam and/or N-vinylamine, and from 0 to 30 mol % of further free-radically polymerizable monomers as biocidal additive, and a method of protecting articles by applying an antimicrobial aqueous composition comprising such an additive.

Abstract: The present invention provides antimicrobial compositions comprising an antibiotic and a sensitizer that enhances the effectiveness or activity of the antibiotic, wherein the sensitizer is preferably a primary amine containing a long alkyl chain. Such compositions are particularly useful for the treatment of infections by drug resistant bacteria.

Abstract: Moisture retention ability of skin is improved and/or skin is protected or treated for another purpose by applying thereto a composition containing at least one of the following compounds: ethanolamine, 2-methoxyethylamine, O-phosphorylethanolamine, 2-ethylaminoethanol, diethanolamine, 2-dimethylaminoethanol, choline, 2-amino-2-hydroxymethyl-1,3-propanediol, noradrenalin, phenethylamine, ethylenediamine, taurine, phosphatidylethanolamine, N-(2-hydroxyethyl)acetoamide, 2-(methylamino)ethanol, 2-anilinoethanol, 2-(benzylamino)ethanol, 3-amino-1-propanol, 2-amino-1-butanol, putrescine, DL-pyroglutamic acid and triethanolamine.

Abstract: The present invention features a method of treating at least one sign of aging on the skin selected from the group consisting of enhancing the elasticity of said skin, enhancing the firmness of said skin, and reducing the appearance of wrinkles or cellulite on the skin, by administering to skin in need of such treatment a composition comprising at least one compound of the formula I or formula II: wherein R1, R2, R3, R4, and R5 independently, are selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, or a cosmetically acceptable salt thereof.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w

Abstract: Method for the treatment or prophylaxis of dry eye disorders by the administration of alkylamino-polyhydroxyalkanes and compositions thereof.

Abstract: The invention relates to the use, as agent for depigmenting and/or whitening the skin, in particular for eliminating pigmentary spots and/or senescence spots, and/or as anti-browning agents, of a compound of formula (I): R1—CHOH—CH(NH—COR2)(CH2OH)??(I) in which R1 denotes a C11 to C21 alkyl radical, and R2 denotes a linear, optionally hydroxylated C11-C19 hydrocarbon-based radical, with the hydroxyl group being in the alpha-position with respect to the carbonyl, which may comprise one or more ethylenic unsaturations, in particular one or two ethylenic unsaturations. The invention also relates to a cosmetic process for depigmenting and/or lightening skin exhibiting pigmentation spots, comprising the application to the skin of a composition comprising, in a physiologically acceptable medium, a compound of formula (I).

Abstract: Provided is a composition for cancer treatment including phytosphingosine or a derivative thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: This invention provides compounds which specifically inhibit TRPA1 but not other members of the thermoTRP ion channel family. Also provided in the invention are methods of using TRPA1-specific inhibitors to treat or alleviate pains mediated by noxious mechanosensation.

Abstract: This invention relates generally to a method of increasing cytosolic Ca2+ levels in mammalian cells comprising contacting P2X receptor Ca2+ entry channels or any and all other Ca2+ entry channels or mechanisms on the cell with an effective amount of a small molecule, and a composition comprising the small molecule in a delivery system. The invention has broad applicability in the pharmaceutical industry as a method of treating airway diseases (such as cystic fibrosis and asthma), ailments of the lung and airways (such as those caused by common cold pathogens or allergens in allergy), kidney diseases and renal hypertensive disorders (such as polycystic kidney disease and salt-sensitive hypertension syndromes), and endocrine disorders (such as diabetes).

Abstract: The invention concerns a pharmaceutical or cosmetic composition, characterised in that it comprises at least a compound for inhibiting Langerhans' cell migration, said active compound being selected in the group consisting of protein kinase C (PKC) inhibiting compounds, matrix metalloprotease (MMP) inhibiting compounds, and combinations thereof, and at least a pharmaceutically or cosmetically acceptable carrier. Said composition enables to inhibit considerably Langerhans' cell migration induced by the presence or an allergenic agent.

Abstract: Disclosed herein are substituted amino alcohol anti-mycobacterial agents and/or chelation therapy agents of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Graft rejection is a serious problem associated with tissue or organ transplantation (e.g., allotransplantation or xenotransplantation), performed to treat various organ failures (e.g., liver, heart, lung, kidney, or pancreas). Described are pharmaceutical compositions for suppressing, treating, or preventing graft rejection comprising a substance having an activity to modulate signal transduction mediated by AILIM, and a pharmaceutically acceptable carrier.

Abstract: The use of bis-amines to enhance the antimicrobial activity of pharmaceutical compositions is described. The bis-amines are particularly useful for enhancing the antimicrobial activity of aqueous ophthalmic compositions, such as artificial tears or ocular lubricants, and solutions for disinfecting contact lenses.

Abstract: The present invention relates generally to a method of modulating hyperglycaemia-induced endothelial cell functioning and agents useful for same. More particularly, the present invention relates to a method of modulating hyperglycaemia-induced vascular endothelial cell functioning by modulating intracellular sphingosine kinase-mediated signalling. The method of the present invention is useful, inter alia, in the treatment and/or prophylaxis of the adverse vascular endothelial cell functioning associated with conditions characterised by hyperglycaemia, and/or diabetes mellitus, per se.

Abstract: The invention relates to a S-(2,3-dihydroxypropyl)-cysteine peptide which has two long-chain fatty acids bonded in the form of esters at the dihydroxypropyl group, and which has the following sequence: DhcGN NDE SNI SFK EK. The invention relates also to a composition comprising the mentioned peptide.

Abstract: The present invention pertains to the use of a S1P receptor agonist in the manufacture of a medicament in the treatment of an ocular disorder.

Abstract: The invention provides A composition for increasing milk production in an animal that includes an active compound chosen from calcium isopropyl cresol, calcium isopropyl-o-cresol, lactic acid, or combinations thereof, and calcium carbonate as a buffering agent. The invention also provides a composition for increasing milk production in an animal that includes about 0.1 wt % to about 15 wt % of the total weight of the composition of active compound, wherein the active compound is chosen from calcium isopropyl cresol, calcium isopropyl-o-cresol, and lactic acid, about 40 wt % to about 75 wt % of the total weight of the composition of calcium carbonate, and about 10 wt % to about 60 wt % of the total weight of the composition of at least one carrier.

Abstract: The present invention relates to specific sphingolipids/sphingolipid derivatives as pharmaceutical compositions as well as their use in the preparation of medicaments for the treatment, prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.

Abstract: The present invention is in the field of prevention and treatment of atherosclerosis and atherosclerosis-related clinical conditions. In particular, the present invention relates to the use of sphingolipids, more preferably phytosphingosine, sphingosine, sphinganine, ceramide, cerebroside lyso-sphingomyelin and/or sphingomyelin for prevention and treatment of inflammatory processes associated with atherosclerosis, psoriasis, colitis or auto-immune diseases in a subject.

Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: A method for treating and preventing diseases associated with neutrophil infiltration, particularly ocular diseases, is provided, which method comprises administering to a subject in need thereof an effective amount of ceramide or a derivative thereof. Also provided is a composition for treating diseases associated with neutrophil infiltration, the composition comprising ceramide or a derivative thereof.

Abstract: The present invention relates to a pharmaceutical composition and the method for the preparation thereof. The composition comprises 1.5˜6.9% (w/v) of one or more substances selected from sodium chloride, sodium bicarbonate, potassium chloride, magnesium sulfate, calcium chloride, calcium gluconate, and the like, and 3˜18% (w/v) of one or more substances selected from hydroxyethylstarch, dextran, carboxymethylstarch, polyvinyl-pyrrolidone, gelatin derivatives, and the like as well as the remainder of conventional injections, as long as sodium chloride is not less than 1.5% (w/v). The pharmaceutical composition of the present invention is used to treat and save the wounded and patients, as well as to treat shock, its advantages include safe and convention use, rapid and good curative effect, long time maintenance, extensive uses and the like.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1—L?—X2—Z or —Z; R1–R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D—Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: The present invention relates to a phytandiol amine derivative represented by the following formula (I) and compositions for treating acne comprising the same: wherein each of Y and Z is OH with the proviso that X is NH2, each of X and Z is zOH with the proviso that Y is NH2, and each of X and Y is OH with the proviso that Z is NH2.

Abstract: Investigation of the activity of extracts of the clam Spisula polynyma has led to antitumor long-chain, straight-chain alkane or alkene compounds which have a 2-amino group and a 3-hydroxy group. The present invention is directed to compositions and methods comprising an isolated and purified long-chain, straight-chain 2-amino-3-hydroxyalkane, or prodrug thereof, and a pharmaceutically acceptable carrier, wherein the carbon chain in the long-chain, straight-chain 2-amino-3-hydroxyalkane is C16–C24.

Abstract: The present invention provides an ophthalmic aqueous pharmaceutical preparation, which is excellent in anti-inflammatory effect, which is less stimulative and which has high safety and excellent storage stability. The ophthalmic aqueous pharmaceutical preparation comprises meloxicam and trometamol.