Abstract: Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries.

Abstract: The invention is directed to a method of detecting a biological substance in the nasal secretion and diagnosing a disease following the detection of the biological substance wherein the biological substance is not related to a respiratory disease. The invention also provides treatment of the diseases following the detection of the biological substance and/or diagnosis of the disease. In some embodiments, the diseases are cancer, hepatitis, smell loss, taste loss, diabetes, and leprosy. The invention also provides a kit for diagnosing a disease. The present invention includes methods of analyzing samples from the nose for the detection of biological substances. In particular, nasal secretion or nasal mucus is collected and analyzed for biological substances. The results of this analysis are then suitable for use in diagnosis, prognosis, and determination of suitability of therapeutic interventions.

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: The present invention provides for a device comprising a scaffold composition, a bioactive composition and a bio-in-hibiting composition, wherein said bioactive and bio-inhibiting compositions are incorporated into or coated onto said scaffold composition, wherein said scaffold composition temporally supports survival and growth of resident follicles, migration and multiplication of stroma cells and spreading and organization of endothelial cells and new vessels wherein said bioactive composition regulates development of a resident follicle, formation of new blood vessels and chemoattraction and proliferation of stroma cells and wherein the bio-inhibiting composition regulates inhibition of the development of a second resident follicle. The presence of the bio-inhibiting composition within the scaffold is involved in the quiescence of the follicles in the primordial stage, which is important to restore fertility.

Abstract: A sustained release pharmaceutical formulation is disclosed. The formulation comprises a water soluble medicament and a polymer mixture comprising a first component of about 80 weight percent polyvinylacetate combined with about 20 weight percent polyvinyl pyrrolidone; of the total weight of the first component, combined with a second component of a cellulose ether polymer.

Abstract: The invention relates to a directly-compressible gastro-resistant spheroid. The spheroid comprises: (i) a core containing one or more active substances; (ii) a flexible, deformable film which directly coats the aforementioned core and which comprises an enteric polymer and a mixture of saturated and/or unsaturated polyglycosylated glycerides, the fatty acids of which include at least 8 carbon atoms; and (iii) an outer water-dispersible layer containing at least one disintegrating agent. The invention further relates to multiparticular tablets comprising said spheroids.

Abstract: The present invention provides a method for treating pain in a subject in need of treatment, by administering to the subject a non-opioid agent in combination with a selective excitatory-opioid-receptor inactivator, in amounts effective to treat pain in the subject. Also disclosed is a method for treating opioid-withdrawal effects in a subject in need of treatment, by the administration to the subject of a non-opioid agent in combination with a selective excitatory-opioid-receptor inactivator, in amounts effective to treat opioid-withdrawal effects in the subject. Finally, the present invention provides a pharmaceutical composition comprising a non-opioid agent and a selective excitatory-opioid-receptor inactivator, and a pharmaceutically-acceptable carrier.

Abstract: Co-crystals comprising at least one nutraceutical compound and at least one co-crystal former with or without impurities. These co-crystals may be included in compositions (optionally also including other components such as pharmaceutically acceptable excipients, other nutritional supplements, etc.) having utility as pharmaceuticals, nutraceuticals, nutritional supplements, and foodstuffs.

Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.

Abstract: The present invention provides various biomarkers of depression. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of depression, methods of determining predisposition to depression, methods of monitoring progression/regression of depression, methods of assessing efficacy of compositions for treating depression, methods of screening compositions for activity in modulating biomarkers of depression, methods of treating depression, as well as other methods based on biomarkers of depression.

Abstract: A mammal undergoing an ablation procedure is treated for symptoms associated with adenosine by administering one or more adenosine receptor antagonists to the mammal prior to or during the procedure.

Abstract: A cocoa extract obtainable by the extraction of non-defatted cocoa beans which have not been fermented or have been allowed to ferment for no more than three days, having a polyphenol content of more than 25% by weight, may be used in the treatment or prophylaxis of a condition selected from dysphoria, depression, anxiety, sleep disorders, gastric motility disorders, sexual dysfunction, brain trauma, memory loss, appetite disorders, bulimia, substance abuse, alcoholism, tobacco addiction, obsessive-compulsive disease, panic disorder, premenstrual syndrome, and migraine.

Abstract: A method for treating migraine comprising administering, as an active ingredient, a xanthine derivative represented by the following formula or a pharmaceutically acceptable salt thereof.

Abstract: A cocoa extract obtainable by the extraction of non-defatted cocoa beans which have not been fermented or have been allowed to ferment for no more than three days, having a polyphenol content of more than 25% by weight, may be used in weight management.

Abstract: The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.

Abstract: Pharmaceutical formulation in the form of agglomerates comprising A) an excipient content composed of a) 60-97% by weight of sugar or sugar alcohols, b) 1-25% by weight of a disintegrant, c) 1-15% by weight of water-insoluble, film-forming polymers d) 0-15% by weight of water-soluble polymers and e) 0-15% by weight of further pharmaceutically customary excipients the total of the components a) to e) being 100% by weight, and B) at least one active ingredient.

Abstract: The present invention concerns the use of an oil-in-water emulsion where the interior of oil droplets exhibit interfaces, between lipophilic domains and hydrophilic or amphiphilic domains, due to the presence of a lipophilic additive solubilized inside the oil droplets and which is used for delayed release of active elements such that the release of at least one active element, which has a octanol/water partitioning coefficient logP higher than ?1, corresponds to a higher Tmax than the Tmax obtained for the simple reference oil-in-water emulsion where no lipophilic additive is used.

Abstract: The instant invention discloses methods of preparing phospholipid delivery systems encapsulating one or more bio-affecting compounds, said methods comprising solubilizing a heterogeneous phospholipid mixture into a suitable organic solvent to form a concentrated formulation of phospholipids, wherein the phospholipids comprise a charged phospholipid species, and mixing the concentrated formulation with an aqueous solution comprising at least one bio-affecting compound. The instant invention also discloses methods of using a phospholipid delivery system encapsulating at least one bio-affecting compound for administration to an individual in need thereof.

Abstract: An object of the present invention is to provide an easily absorbable oral preparation containing a xanthine derivative or a pharmaceutically acceptable salt thereof and a fatty acid or a fatty acid derivative for the purpose of providing an easily absorbable oral preparation containing the xanthine derivative of which absorbability has been enhanced by dissolving the xanthine derivative that shows adenosine A1 receptor antagonistic activity and has diuretic activity, kidney-protecting activity, bronchodilating activity, cerebral function-improving activity, anti-dementia activity or the like in a solvent.

Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial

Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.

Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor.

Abstract: The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor.

Abstract: A cocoa extract obtainable by the extraction of non-defatted cocoa beans which have not been fermented or have been allowed to ferment for no more than three days, having a polyphenol content of more than 25% by weight, may be used in the treatment or alleviation of obesity.

Abstract: The present invention refers to a solid dosage form comprising an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein said inner coating comprises a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of said acid and its salt; wherein said outer coating comprises an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.

Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.

Abstract: The present invention relates to a therapeutically active xanthine derivative compound of formula (I): corresponding pharmaceutical formulations containing, manufacture processes for, methods or uses of such compounds in therapy, in particular for treatment of diseases where under-activation of the HM74A receptor contributes to such diseases or where activation of the HM74A receptor will be beneficial.

Abstract: The present invention includes systems, compositions and methods of making a multilayer modular release system, wherein the layers form a stack of active agent release layers, wherein the stack comprises a body and first and second ends and an impermeable coating surrounding the body of the stack, wherein the active agent is only release from the first, second or both the first and second ends of the stack by diffusion.

Abstract: The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.

Abstract: Described here are compositions and methods for treating side-effects of vasodilator therapy. The compositions may include both a vasodilator and a side-effect alleviating agent in a single dosage form. Alternatively, the vasodilator and side-effect alleviating agent may be formulated separately, each in its own dosage form. The compositions may be packaged as kits for use with various medical conditions.

Abstract: Methods and products for delivering a medicament or agent to an individual are provided as well as methods for producing the product. The product includes a coating having a medicament or agent. The medicament or agent is present within the coating that surrounds a tableted center. The tableted center is defined by compressible excipients. By chewing the product, the medicament or agent is released from the product within the buccal cavity.

Abstract: The present invention relates to the use of the combined oral administration of caffeine with carbohydrate for increasing the rate of muscle glycogen resynthesis after strenuous exercise.

Abstract: The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.

Abstract: The present invention relates to new substituted xanthine-based agents, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This invention relates to methods for multidetector computed tomography myocardial perfusion imaging comprising administering doses of a rate-control agent and one or more adenosine A2A receptor agonists to a mammal.

Abstract: The present invention relates to new xanthine modulators of adenosine A1 receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention includes compositions and methods of making a modified release pharmaceutical formulation and a method of preparation for the embedding of modified release multi-particulates into a polymeric or wax-like matrix. The modified release multi-particulates comprise an effective amount of a therapeutic compound having a known or desired drug-release profile. Modified release multi-particulates may include a polymeric coat or may be incorporated into particle or core material. The polymer matrix comprises a thermoplastic polymer or lipophilic carrier or a mixture thereof that softens or melts at elevated temperature and allows the distribution of the modified release multi-particulates in the polymer matrix during thermal processing. Formulation compounds and processing conditions are selected in a manner to preserve the controlled release characteristics and/or drug-protective properties of the original modified release multi-particulates.

Abstract: The present invention is directed to methods for readily propagating somatic hair follicle stem cells or melanocyte stem cells. The methods comprise enhancing guanine nucleotide (GNP) biosynthesis, thereby expanding guanine nucleotide pools. This in turn conditionally suppresses asymmetric cell kinetics in the explanted cells. The methods of the invention include pharmacological methods and genetic methods. For example, the resulting cultured somatic hair follicle stem cells can be used for a variety of applications including cell replacement therapies such as hair transplants, gene therapies, and tissue engineering applications, such as the generation of artificial skin and skin regeneration strategies including skin grafts.

Abstract: Methods and compositions are disclosed for the treatment of diseases or conditions produced by or associated with low cyclic nucleotide levels. The compositions comprise phosphodiesterase inhibitors and are formulated for intranasal and pulmonary administration.

Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures thereof, and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The present invention relates to the use of paraxanthine for the manufacture of a non-anxiogenic psychoanaleptic drug for the treatment of a neuropsychiatric disorder.

Abstract: Adenosine A2A receptor antagonists are useful for the preparation of medicaments against atrial fibrillation in mammals, including humans. It has been found that the adenosine A2A receptor is present in human atrial cardiomyocytes and participates in the pathological mechanisms underlying atrial fibrillation. An advantage of using A2A antagonists over other agents known in the art is that the A2A antagonists specifically target patients with atrial fibrillation.

Abstract: The invention relates to a method of treatment for muscular dystrophies, including Duchenne, Becker, limb-girdle, facioscapulohumeral, congenital muscular dystrophies and the like using a combination of nitric oxide-releasing and anti-inflammatory compounds.

Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

Abstract: The disclosure herein relates to nuclear hormone receptors including steroid hormone receptors, for example in connection with estrogen, progesterone, and androgen. Embodiments of compositions and methods are disclosed including such relating to compounds, including substituted theophyllines, capable of functioning as inhibitors of estrogen receptor alpha-mediated gene expression and having the ability to modify cancer cells and treat cancer, including breast cancers and resistant breast cancers, particularly those that are resistant to tamoxifen. In embodiments, methods of inhibiting breast cancer cells and resistant breast cancer cells are provided. In embodiments, a useful inhibitor compound includes TPSF/NSC 97998 and other compounds.

Abstract: The invention relates to compositions comprising at least one xanthine compound, preferably further comprising at least one agent which acts on capillary circulation and/or at least one natural moisturizing agent, which can be used to treat, or to reduce and/or minimize the appearance of, defects such as dark circles, bags and/or puffiness around eyes.

Abstract: Methods and compositions are provided for treating vascular depression. The methods involve administering to a subject in need thereof a xanthine derivative in a therapeutically effective amount to treat vascular depression, particularly the xanthine derivatives pentoxifylline or propentofylline. The methods may further include administration of an additional therapeutic agent in combination with the xanthine derivative selected from the group consisting of a selective serotonin reuptake inhibitor (SSRI), a serotonin-norepinephrine reuptake inhibitor (SNRI), and a drug used in the treatment of cerebrovascular disease. Compositions of the invention include pharmaceutical compositions and kits for treating vascular depression in a subject in need thereof that include therapeutically effective amounts of a xanthine derivative and an additional therapeutic agent selected from the group consisting of an SSRI, an SNRI, and a drug used in the treatment of cerebrovascular disease.

Abstract: Described herein are respiratory drug condensation aerosols and methods of making and using them. Kits for delivering condensation aerosols are also described. The respiratory drug aerosols typically comprise respiratory drug condensation aerosol particles. In some variations the respiratory drug compound is selected from the group consisting of ?-adrenergics, methylxanthines, anticholinergics, corticosteroids, mediator-release inhibitors, anti-leukotriene drugs, asthma inhibitors, asthma antagonists, anti-endothelin drugs, prostacyclin drugs, ion channel or pump inhibitors, enhancers, or modulators and pharmaceutically acceptable analogs, derivatives, and mixtures thereof. Methods of treating a respiratory ailment using the described aerosols are also described. In general, the methods typically comprise the step of administering a therapeutically effective amount of respiratory drug condensation aerosol to a person with a respiratory ailment.