Abstract: The present invention relates to pharmaceutical compositions and combinations for treating cancer, comprising a diaryl urea compound and an PI3K/AKT signaling pathway inhibitor. Useful combinations include e.g. BAY-43-9006 as a diaryl urea compound.

Abstract: Compositions, methods, and apparatuses for treatment of subcutaneous fat tissue for the purpose of fat tissue reduction or other alterations of the subcutaneous fat tissue which affect the appearance of the overlying skin layer.

Abstract: Disclosed is a novel food product characterized by a low glucose or glucose free content, a balanced functional fat content, and a proactive agent aimed for the diabetic and diabetic-prone populations. The food product of the invention is a functional food which may be used clinically to lower the lipid level in people suffering from an imbalanced lipid profile and which may progress towards diabetes complications and coronary vascular disorders. In particular embodiments the proactive agent can be any of a naturally occurring lipid, a synthetic or mimetic lipid which is not digestible by humans and interferes with body weight gain/loss, plant extracts and substances derived therefrom, antioxidants, animal-derived substances, minerals and pharmaceuticals, and any mixture thereof.

Abstract: Procedure for the obtaining a concentrate of the total fixed lipids of the kernels of the family Sapotaceae, genus Calocarpum, Chrysophyllum and Lucuma. The kernels (seeds removed of the endocarp), are squeezed by means of mechanical techniques that use pressure and heat, without using extractive liquids, getting a concentrate of lipidic juices (virgin) in a dry way and with their characteristic aroma. This concentrate of total fixed lipids can be fractioned in its main constituents by means of a process that consist of the emulsification of the lipids, followed by centrifugation or sedimentation, giving place to the stratification of the main constituents and their consequent separations. The main constituent consist of oils, of phospholipids and of residues glucosidic triterpenes plus of sterols fractions.

Abstract: Pharmaceutical composition which comprises squalene or its pharmaceutically acceptable derivatives; at least one phospholipid, its salts or pharmaceutically acceptable derivatives; and at least one omega-3 fatty acid, its salts or pharmaceutically acceptable derivatives. Use of the composition in the preparation of a drug designed for the prophylaxis, treatment and/or improvement of cancer symptoms in mammals. The invention also relates to a fodder for animals such as dogs and cats which comprises the composition.

Abstract: A method including advancing a delivery device through a lumen of a blood vessel to a particular region in the blood vessel; and introducing a composition including a sustained-release carrier and an apolipoprotein A-I (apo A-I) synthetic mimetic peptide into a wall of the blood vessel at the particular region or a perivascular site, wherein the peptide has a property that renders the peptide effective in reverse cholesterol transport. A composition including an apolipoprotein A-I (apo A-I) synthetic peptide, or combination of an apo A-I synthetic mimetic peptide and an Acyl CoA cholesterol: acyltransferase (ACAT) inhibitor in a form suitable for delivery into a blood vessel, the peptide including an amino acid sequence in an order reverse to an order of various apo A-I mimetic peptides, or endogenous apo A-I analogs, or a chimera of helix 1 and helix 9 of endogenous apo A-I.

Abstract: A method including advancing a delivery device through a lumen of a blood vessel to a particular region in the blood vessel; and introducing a composition including a sustained-release carrier and an apolipoprotein A-I (apo A-I) synthetic mimetic peptide into a wall of the blood vessel at the particular region or a perivascular site, wherein the peptide has a property that renders the peptide effective in reverse cholesterol transport. A composition including an apolipoprotein A-I (apo A-I) synthetic peptide, or combination of an apo A-I synthetic mimetic peptide and an Acyl CoA cholesterol: acyltransferase (ACAT) inhibitor in a form suitable for delivery into a blood vessel, the peptide including an amino acid sequence in an order reverse to an order of various apo A-I mimetic peptides, or endogenous apo A-I analogs, or a chimera of helix 1 and helix 9 of endogenous apo A-I.

Abstract: The invention discloses a method and a composition for smoking cessation or for promoting smoking cessation in individual smokers. The compositions described contain phosphatidic acid as the active ingredient.

Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.

Abstract: A composition that has an activity of ameliorating reduced higher brain functions resulting from organic brain lesions, said composition comprising arachidonic acid and/or a compound having arachidonic acid as a constituent fatty acid as well as docosahexaenoic acid and/or a compound having docosahexaenoic acid as a constituent fatty acid.

Abstract: A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as saturated and unsaturated phosphatidyl cholines, hydrophobic substances, cholesterol, cholesterol derivatives, antioxidant and hydrophilic polymer-modified lipids such as MPEG-DSPE.

Abstract: The present invention relates to novel use of a ligand specific to a FEX-2 polypeptide. More specifically, the present invention relates to methods for modulating the secretion of an inflammation-associated cytokine and for treating or preventing an inflammatory disease using the FEX-2-specific ligand. The ligand specific to the FEX-2 polypeptide can bind to FEX-2 expressed on the surface of phagocytes so that it can stimulate the secretion of anti-inflammatory cytokine and inhibit the secretion of inflammatory cytokine, so as to treat or prevent inflammatory diseases.

Abstract: The invention provides synthetic methods for PEGylated cardiolipins with varying linkers. The methods can be employed to prepare PEGylated cardiolipin with different fatty acid and/or alkyl chain length with or without unsaturation. The PEGylated cardiolipin, prepared by the present methods, can be incorporated into liposomes that can also include active agents such as hydrophilic or hydrophobic drugs for the treatment of human and animal diseases. In addition, the PEGylated cardiolipin can be incorporated into liposomes that include compounds for therapeutic and diagnostic imaging. The use of such liposomes with PEGylated cardiolipin prolongs the period of liposomal circulation without disrupting the lipid bilayer.

Abstract: This invention discloses new krill oil compositions characterized by having high amounts of phospholipids, astaxanthin esters and/or omega-3 contents. The krill oils are obtained from krill meal using supercritical fluid extraction in a two stage process. Stage 1 removes the neutral lipid by extracting with neat supercritical CO2 or CO2 plus approximately 5% of a co-solvent. Stage 2 extracts the actual krill oils by using supercritical CO2 in combination with approximately 20% ethanol. The krill oil materials obtained are compared with commercially available krill oil and found to be more bioeffective in a number of areas such as anti-inflammation, anti-oxidant effects, improving insulin resistances and improving blood lipid profile.

Abstract: The invention provides a pharmaceutical composition comprising a synthetic or naturally occurring charged phospholipid, which is formulated into a dosage form for administration to a subject or which is administered as a food additive. Negatively charged phospholipid composition increase the net negative charge on intravascular lipoproteins, enhance the clearance of cholesterol and regulate the function of lipolytic enzymes, retard prothrombin formation and aid in the clearance of virus and bacterial particles. Negatively charged lipid compositions can therefore be administered to humans and animals for the treatment of hyperlipidemia and blood coagulation disorders and to reduce the levels of virus, bacteria, and endotoxins in the blood stream. Positively charged lipid compositions can be administered to delay lipoprotein clearance from the plasma compartment and give longer duration of activity for drugs which are associated with lipoproteins.

Abstract: The present invention is directed to a method of inhibiting CDld activation by administering a composition containing a moiety that blocks CDld activation. Compositions of the invention are useful for the attenuation of CDld-restricted immune responses, including treatment of skin disorders due to hyperactive immune responses (e.g., contact hypersensitivity), for systemic administration to attenuate ongoing immune responses, and to provide hypoallergenic cosmetic products including pharmaceutical, cosmetic, and skin care compositions. Preferably, these compositions are in a form intended for topical administration.

Abstract: Described herein are combination methods, compositions and therapies for treating ophthalmic conditions or diseases arising from, associated with or leading to the overproduction of waste products in the visual cycle. Agents included within these combinations are 13-cis-retinyl derivatives; other agents included within these combinations are selected from vitamins, antioxidants, minerals, inducers of nitric oxide production, anti-inflammatory agents, and negatively-charged phospholipids. Such combination methods may be used as single or multiple administration therapies, or in combination with other agents or therapies.

Abstract: Embodiments of the invention are directed to methods and compositions for inhibiting activation of cSrc by human actin filament associated protein (AFAP). Libraries and methods of screening compositions for inhibitive activity are also provided. Also provided are methods of treating cancer. Cancer may be, for example, but is not limited to ovarian cancer, breast cancer, and gastrointestinal cancer. Also provided are methods of decreasing resistance to chemotherapy.

Abstract: The invention is directed to the use of Ginkgo complexed with phosphatidylserine for the manufacture of a medicament or a dietary supplement for the enhancement of cognitive function and mental fatigue, i.e. to improve the factors related therewith such as to improve the speed of memory and memory quality, to increase accuracy and attention in activities in normal, healthy subjects, to prevent deterioration of the speed and quality of memory in people with decreased cognitive functions and to counteract cognitive fatigue, having also an influence on the mood, particularly in healthy children, young adults, middle-aged and/or old people. It is further provided the use of the Ginkgo phosphatidylserine complex for the treatment and prevention of a disease related with a decrease of the cognitive function and mental fatigue such as Dementia, e.g. Alzheimer's Disease.

Abstract: Described herein are synthetically modified fullerene molecules, wherein the fullerene is preferably ellipsoid in shape with an equatorial band and two opposing poles, comprising an adduct at one or both poles, at least one adduct being a hydrophobic chemical moiety capable of anchoring the fullerene on or in a lipid membrane.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: An in-vitro model apparatus of a human spine and methods for detecting and analyzing substance distribution patterns therein. In one embodiment, the model apparatus includes a column body defining a passageway that substantially mimics the size, shape, and structure of an adult human spinal canal. Also included is a cord structure that may be located and anchored within the passageway. The cord structure substantially mimics the size, shape, and structure of an adult human spinal cord. For example, the cord structure may include connecting elements that resemble nerve roots, dentate ligaments, and the septum posticum of a human spine. The passageway of the model apparatus may be filled with a first fluid that simulates cerebro-spinal fluid (CSF), and a second fluid containing a drug (or simulated drug) may be introduced into the passageway, after which the drug's distribution within the passageway may be analyzed.

Abstract: This invention relates to three-dimensional synthetic and semi-synthetic compositions having biological activity, and to the uses thereof in the treatment and/or prophylaxis of various disorders in mammalian patients. More particularly it relates to preparations and uses of synthetic and semi-synthetic bodies, such as liposomes, which after introduction into the body of a patient, produce beneficial anti-inflammatory, organ protective and immune regulatory effects. The invention also relates to treatments and compositions for alleviating inflammatory and autoimmune diseases and their symptoms.

Abstract: Synthetic and semisynthetic bodies having a three-dimensional structure, sized and shaped to resemble apoptotic cells and apoptotic bodies, and having phosphatidyl serine (PS) molecules on the surface thereof, are administered to a patient, to alleviate a variety of disorders such as T-cell mediated disorders (autoimmune conditions). The bodies are believed to trigger an apoptosis-like mechanism in the patient.

Abstract: The instant invention provides reagents and methods for diagnosis, detection and treatment of cancers (for example, prostate cancers). In particular, the invention provides methods to generate various functionalized PSMA ligands, and their uses in diagnosis, detection, imaging, and treatment of prostate cancers, especially those overexpressing PSMA.

Abstract: The present invention relates to methods for regulating the release of TGF-&bgr; from living cells in vitro or in vivo, comprising bringing the cells into contact with an effective amount of a NAALADase inhibitor. Such methods are believed to be useful for affecting neuroregeneration, cell proliferation, cell differentiation, extracellular matrix formation, myelination, inflammation, immune function, liver function, pancreatic function, angiogenesis, or wound healing; and/or for preventing or treating diabetes.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.

Abstract: Methods for modulating apoptosis by administering a phosphatidic acid compound are described.

Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.

Abstract: The present invention provides a hair-growing agent comprising, as an active ingredient, a phosphatidic acid represented by formula (I): (wherein R1 represents straight-chain alkyl having an odd number of carbon atoms, straight-chain alkenyl having an odd number of carbon atoms, or straight-chain alkynyl having an odd number of carbon atoms).

Abstract: A pharmaceutical composition adapted for use as a spermicide, the composition comprising a gel-microemulsion comprising an oil-in-water microemulsion and a polymeric hydrogel. The gel-microemulsion can be used in a spermicidal method.

Abstract: An insect pest eradication system comprised of a non-lethal knockout agent and an insecticide. The present invention also relates to a method of eradicating insects, particularly those found in earthen colonies, by treating the insects with a non-lethal knockout agent, such as trans-dichloroethylene, in combination with a suitable insecticide for the targeted insects.

Abstract: Negatively charged phospholipids, as well as compositions including negatively charged phospholipids and possibly carotenoids and/or antioxidants, for treating the eye are disclosed. In a preferred embodiment, a composition comprising at least one negatively charged phospholipid except cardiolipin is used to treat age-related macular degeneration. Methods for producing the negatively charged phospholipids, as well as methods for producing the compositions including negatively charged phospholipids and possibly carotenoids and/or antioxidants for treating age-related macular degeneration, are also disclosed.

Abstract: This invention provides novel methods of inhibiting one or more symptoms of atherosclerosis. Also provided are assays for compounds that will inhibit the progression and/or ameliorate one or more symptoms of atherosclerosis. The methods and assays are based, in part, on the discovery that oxidized LDL or components thereof induce strong upregulation of MAP kinase phosphatase-1 which, in turn, is associated with an “inflammatory response” characteristic of atherosclerotic plaque formation. Inhibition of MKP-1 inhibits one or more symptoms of this response, e.g. monocyte adhesion, monocyte chemotaxis, differentiation into macrophages, etc. Inhibition of MKP-1 thus provides an effective method of inhibiting symptoms of atherosclerosis.

Abstract: A multi-layer wood pest barrier having a prolonged lifetime that can be as long as the life of a building or structure to be protected. The lifetime protection is achieved by binding at least one pesticide within a continuous or discontinuous polymer matrix layer thereby substantially reducing release of the pesticide from the matrix. The release rate of the pesticide from the matrix can be controlled by the use of a carrier such as carbon black. The release of the pesticide from the barrier can be further controlled by inclusion of additional layers which can make the barrier substantially non-releasing.

Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative, antibiotic, antimycotic, antiviral and antineoplastic drugs, in particular in combination with a multiplicity of other emollients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of such agents through the epidermis for treatment of skin diseases and other disorders.

Abstract: Novel compositions for the treatment of IRDS and ARDS are indicated which contain N-(3,5-dichloro-pyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide and/or its pharmacologically tolerable salts and lung surfactant.

Abstract: The present invention relates to methods of using NAALADase inhibitors to regulate TGF-&bgr; and to treat neurodegenerative disorders, extracellular matrix formation disorders, cell-growth related diseases, infectious diseases, immune related diseases, epithelial tissue scarring, collagen vascular diseases, fibroproliferative disorders, connective tissue disorders, inflammatory diseases, respiratory distress syndrome and infertility.

Abstract: A composition and various formulations comprise preventative or therapeutic amounts of an epiandrosterone, analogs thereof or salt thereof, and/or a ubiquinone or salt thereof, and a pharmaceutically or veterinarily acceptable carrier or diluent. The composition and formulations are useful for treating bronchoconstriction, respiratory tract inflammation and allergies, asthma, and cancer. A method of treating diseases associated with low adenosine levels or adenosine depletion comprises administering folinic acid or a pharmaceutically acceptable salt hereof in a preventative or therapeutic amount, or an amount effective to treat adenosine depletion.

Abstract: Pesticidal formulations of cadusafos are provided. An aqueous capsule suspension is provided, containing from about 150 to about 360 grams of cadusafos per liter of formulation and having lower mammalian toxicity than aqueous cadusafos microemulsion formulations is prepared by interfacial polymerization of a first polyfunctional compound, such as a polymethylene polyphenyl isocyanate, with a second polyfunctional compound, such as a polyfunctional amine or mixtures of polyfunctional amines, in an aqueous phase optionally containing from about 0.05 to about 0.50 xanthan gum viscosity modifier/stabilizer. A granular form of the microencapsulated cadusafos is also provided. Several such formulations and the method of their preparation are described.

Abstract: The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.

Abstract: An anti-depressant, mental & emotional stress suppressor and mood improver having a prominent action for decreasing blood cortisol level and serotonin reuptake and has an effect of alleviating symptoms associated with depression and mental & emotional stress of a subject administered with the improver. The improver contains as the effective ingredient a combination of phosphatidy-L-serine and phosphatidic acid, or the salts thereof, comprising at least 20% (w/w) phosphatidy-L-serine and typically within the range of about 20%-40% of phosphatidy-L-serine, out of the total phospholipid content of the composition and at least 3% (w/w) of phosphatidic acid, preferably above about 10% and typically within the range of about 20%-40% of phosphatidic acid, out of the total phospholipid content of the composition.

Abstract: The present disclosure relates to a method of inhibiting angiogenesis comprising administering a N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitor to a patient in need thereof, and a pharmaceutical composition comprising an anti-angiogenic effective amount of a NAALADase inhibitor and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to prodrugs of NAALADase inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat glutamate abnormalities and prostate diseases.

Abstract: The present invention relates to pharmaceutical compositions and methods of using NAALADase inhibitors for treating glutamate-mediated diseases, disorders and conditions selected from the group consisting of anxiety, anxiety disorders and memory impairment.

Abstract: Compounds having utility in achieving the foregoing objects of the invention are prepared by reacting a 2,2-bis-(disubstituted-phosphoryl)-ethylsulfanyl-acetic acid compound with a pharmaceutically active chemical entity effective to treat the underlying disease state or with non-pharmaceutical entities such as pesticides, insecticides, fungicides or poisons for vermin.

Abstract: A method to inhibit inflammation in a mammal is disclosed. The method includes administering to the mammal a composition comprising a phospholipid, which can be lysophosphatidic acid. The administration of a phospholipid is believed to down regulate expression of adhesion molecules on the surface of vascular endothelial cells and circulating leukocytes of the mammal.

Abstract: Pulmonary function may be increased and pulmonary disorders treated by administering pharmaceutical formulations consisting essentially of phosphatidyl glycerol (PG) and a pharmaceutically acceptable carrier. Pulmonary disorders that may be treated by these methods and formulations include respiratory distress syndrome, asthma, and chronic bronchitis.

Abstract: A method of preparing a rapid acting bait composition which is water based and contains a water-sensitive insecticide as an active ingredient is described. The composition is easily applied into cracks and crevices and voids or other pest harborage areas to rapidly kill insect pests, particularly cockroaches. A kit is also described for preparation of the composition.

Abstract: A method of treating an individual with an immune system with decreased activity by administering an effective amount of a lipid preparation derived from a natural source and enriched to contain at least 10% (w/w) phosphatidic acid (PA) is disclosed.