Abstract: Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A nutritional supplement includes elements having been shown to enhance DNA repair or reduce DNA damage by different molecular mechanisms while excluding other bioactive nutrient agents which compete with any of the elements known modes of action. The supplement includes a resveratrol, a carotenoid, a nicotinamide, a dimethylaminoethanol, a zinc source, and a quinic acid analog. The supplement is administered daily in dosages in excess of normal dietary levels. The supplement improves resistance to DNA damage, enhances DNA repair capacity in tissues including skin, and stimulates immune cellular function. This was accomplished by reducing metabolic competition between DNA repair bioactive components that was in turn paralleled by enhancement of thirst quenching properties in aqueous formulations.

Abstract: The disclosure provides compositions and methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure provides compositions and methods based on the use of D-cycloserine in combination with the neurogenic agent, which synergistically stimulates or activates the formation of new nerve cells.

Abstract: The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

Abstract: Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing ?-amyloid production, ?-amyloid deposition, ?-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease ?-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.

Abstract: A modified release dosage product (5) comprises a plurality of minicapsules or minispheres (1, 2) containing nimodipine, and a plurality of minicapsules or minispheres (3), (4) containing tacrolimus. There are uncoated minicapsules or minispheres (1) encapsulating micronized nimodipine for immediate release and a controlled release polymer coated minicapsule or minisphere (2) encapsulating micronized nimodipine for delayed, sustained, controlled or targeted release. There are uncoated seamless minicapsules (3), the core of which comprises tacrolimus lipid-based formulation for immediate release and a controlled release polymer coated seamless minicapsule (4), the core of which comprises tacrolimus lipid-based formulation for delayed, sustained, controlled release or targeted release. The final dosage form may be a hard gelatin capsule (5).

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class I HDACs, which are known to participate in regulation of chromatin structure and gene expression, have generally been considered as pro-hypertrophic in their action. However, the present invention demonstrates that inhibition of certain Class I HDACs should be avoided in the treatment of cardiac hypertrophy, thereby pointing toward selective, and not global, inhibition of Class I HDACs. In particular, the present invention provides for selective inhibition of HDACs 1 and/or 2, and the avoidance of inhibition of HDAC3.

Abstract: The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.

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

Abstract: Niacin drugs are frequently utilized as a therapeutic to treat CVD, increase HDL levels, and/or decrease TG levels. As disclosed herein, it has been found that administration of one or more sPLA2 inhibitors in combination with one or more niacin drugs unexpectedly results in a synergistic increase in HDL levels and a synergistic decrease in TG levels. Therefore, compositions, methods, and kits are provided for treating CVD, increasing HDL levels, decreasing TG levels, and improving HDL/LDL ratios.

Abstract: Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.

Abstract: The present invention relates to novel tablet dosage forms and methods of preparing these forms, which can be used for different classes of pharmaceutical active ingredients posing stability issues in a single unit system. The dosage form includes a first layer, which includes a tablet of one or more active pharmaceutical ingredients, which is inlayed in the first layer along with other pharmaceutically acceptable excipients, and a second layer that includes one or more active pharmaceutical ingredients optionally with other pharmaceutically acceptable excipients.

Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract: A novel encapsulated product is provided and includes: at least one pharmaceutical; at least one compressible material; and at least one tableting material; wherein the encapsulated product is in the form of a caplet having a diameter of from about 1 millimeter to about 7 millimeters and a length from about 1 millimeter to about 7 millimeters. A method for preparing the encapsulated product is also provided.

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.

Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.

Abstract: In accordance with the present invention, it has been discovered that glucose and incretin hormones promote pancreatic islet cell survival via the calcium and cAMP dependent induction, respectively, of the transcription factor CREB. Specifically, a signaling module has been identified which mediates cooperative effects of calcium and cAMP on islet cell gene expression by stimulating the dephosphorylation and nuclear entry of TORC2, a cytoplasmic CREB coactivator. The module comprises a cAMP regulated snfl-like kinase called SIK2 and the calcium regulated phosphatase calcineurin, both of which associate with TORC2 in the cytoplasm. TORC2 is repressed under basal conditions through a phosphorylation dependent interaction with 14-3-3 proteins. cAMP and calcium signals stimulate CREB target gene expression via complementary effects on TORC2 dephosphorylation; cAMP disrupts TORC2-associated activity of SIK2 or related family members, whereas calcium induces TORC2 dephosphorylation via calcineurin.

Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.

Abstract: The invention relates to betulin derivatives, and to the use thereof as agents against protozoa of the genus Leishmania and against leishmaniasis in applications of pharmaceutical industry.

Abstract: A composition comprises a mixture of a silicone and a first solvent, a drug, such as a hydrophilic or lipophilic pharmaceutical agent, a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS), and a second solvent, such as an alcohol. The salt of a dialkyl sulfosuccinate solubilizes the drug. The composition can be topically applied to a substrate, such as skin, for delivering the drug. Drugs with a wide solubility range are soluble and compatible in the composition without separation or crystallization of the drugs occurring.

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.

Abstract: A sustained release composition for oral administration of niacin, comprising niacin; a carrier for sustained release composed of a hydrophilic polymer and a hydrophobic polymer; and a pharmaceutically acceptable additive, the hydrophilic polymer being a polyethylene oxide and a natural gum, is capable of maintaining a constant release rate of niacin.

Abstract: A pharmaceutical composition is provided comprised of a physiologically acceptable source of assimilable copper, a source of salicylic acid or a physiologically acceptable derivative thereof, and vitamin C.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein X, Y, Z, R2a, R2b, R3a, R3b, R8, R9, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The present invention relates to a bilayered tablet comprising: a slow release layer comprising niacin and release retarding agent; and an immediate release layer comprising HMG-CoA reductase inhibitor.

Abstract: The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 ?mol/g of POM. It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.

Abstract: A composition for alleviating symptoms associated with neurotoxicity. The composition may comprise compounds for preventing glutamate mediated neurotoxicity. The composition may include one or more of the following elements: at least one glutamate antagonist, at least one cAMP stimulating agent, at least one antioxidant, vitamin B12, at least one transporter and at least one surfactant. The composition may be used in methods for alleviating tinnitus, Ménière's Disease and/or hearing loss.

Abstract: The invention relates to the use of nicotinic acid alkyl esters, especially myristyl nicotinate, to inhibit side effects associated with retinoic acid therapy. Also a part of the invention is a method for improving skin cell differentiation by administering the nicotinic acid alkyl ester in an amount sufficient to increase expression of caspase 14 and filaggrin. Deficiencies in expression of these molecules can be treated in this way as well.

Abstract: A pharmaceutical composition in the form of a combination tablet is described. The tablet has a rapidly absorbed component that enters the circulation by traversing the buccal mucosa, oral mucosa and combinations thereof, and a more slowly absorbed component that is swallowed. The therapeutic agent in the swallowed portion is absorbed across the gastric mucosa. The combination tablet may be modified, by varying the specific combinations of excipients, fillers, and the like to effect distinct release rates. In addition, the rapid and slow components may have identical or different therapeutic agents depending on the application to a specific medical condition. One embodiment of the combination tablet includes a prostaglandin inhibitor in the rapidly absorbed component in order to mitigate the side effects of immediate release niacin that is in the slow absorbing component.

Abstract: This invention relates to pharmaceutical combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and atorvastatin or a pharmaceutically acceptable salt thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of amlodipine and atorvastatin whereby those synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.

Abstract: Provided herein are ready-to-use premixed pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: The invention is directed to a method and composition suitable for skin color modulation. Particularly, the action of D-dopachrome tautomerase on melanogenesis and/or the transfer of melanin from melanosomes in keratinocytes is reduced, thereby resulting in a change in skin color.

Abstract: This invention relates to a composition containing quercetin, vitamin B3, and vitamin C. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.

Abstract: The present invention provides matrix-forming, sustained-release pharmaceutical formulations comprising four primary components: i) an effective amount of at least one drug substance; ii) at least one pharmaceutically acceptable, water-swellable, pH independent polymer; iii) at least one pharmaceutically-acceptable, anionic, pH dependent polymer; and (iv) a pharmaceutically-acceptable polymer selected from the group consisting of a) at least one pharmaceutically-acceptable cationic polymer; and b) at least one pharmaceutically acceptable hydrocolloid. The present formulations can be used with compounds having a wide range of solubilities as well as compounds characterized as having hydrophobic or hydrophilic characteristics.

Abstract: Methods and compositions for preventing or reducing weight gain associated with drug treatment, which utilize an H1 agonist such as betahistine, betahistine metabolite or a betahistine salt are disclosed.

Abstract: A method is provided for reducing side effects while treating a mammal using indole-3-carbinol, which method includes the steps of administering an effective amount of indole-3-carbinol along with side effect-reducing amounts of a side-effect reducing component. A composition is also provided, as are various combinations of side effect-reducing agents.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of Nicotine, nicotinic acid analogs thereof, their combination with or without other pro-angiogenesis factors, vasodilator, or other therapeutic modalities to promote angiogenesis in the subject. This is composition and combination thereof is applicable to improving wound healing, erectile dysfunction, improving collateral or blood supply in patients with myocardial infarction, stroke, peripheral artery diseases, and other vascular disorders as disclosed.

Abstract: Compositions including topical formulations comprising secreted products obtained from the culture medium of human umbilical cord stem cells and particular combinations of components therefrom are provided for treatment of various dermatological conditions, such as adverse consequences of aging, wrinkling, altered pigmentation, altered viscoelasticity, and altered thickness, among others. Methods for using the compositions and topical formulations for treating adverse or undesirable dermatological conditions are also provided, as well as preventing the appearance of undesirable dermatological conditions.

Abstract: The present invention relates to an extended release tablet formulation comprising niacin and a release retarding agent selected from hydroxypropyl cellulose, polyethylene oxide or mixtures thereof.

Abstract: Pharmaceutical compositions containing an effective amount of a ligand for GPR109 to decrease intracellular cAMP levels of a subject in combination with an effective amount of a DNA methyl transferase inhibito to reduce or inhibit downregulation of GPR109 in the intestinal epithelial cells of the subject relative to a control are provided. It has been discovered that ligands for GPR109 can be used to treat one or more symptoms of cancer, inflammatory disorders, and diarrhea. Representative CPR 109 ligands include, but are not limited to butyrate, ?-hydroxybutyrate, nicotinic acid, acifran, and octanoate. Suitable DNA methyl transferase inhibitors include 5-azacytidine, 5-aza-2?-deoxytidine, 1-?-D-arabinf?mosyl-5-azacytosine and dihydro-5-azacytidine. Typically, the compositions are formulated to achieve a GPR 109 ligand serum blood level of about 1 to about 1000 ?M. The compositions are useful for the treatment of one or more symptoms of cancer.

Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.

Abstract: The present invention is directed to nicotinamide derivatives, and their use in treating lipoprotein abnormalities, alone or in combination with a statin.

Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.

Abstract: Compositions and methods for inhibiting the growth of lens epithelial cells are provided. The compositions provided include a chelating agent in an amount sufficient for inhibiting the growth of lens epithelial cells. The compositions and methods provided may also be used for the treatment of disorders of the eye, especially in the treatment of presbyopia.

Abstract: A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.

Abstract: Microparticles or granules intended for use in the zootechnical field, constituted by a core which contains a substance having a pharmacological action, a food supplement or a diagnostic medium, intimately mixed or adsorbed with a hydrated silicate of magnesium, aluminum, calcium and sodium (smectite, montmorillonite or bentonite); the core is coated with a double fatty layer constituted by two fats or waxes, of which the one having the highest melting point constitutes the inner layer while the one having the lowest melting point is arranged so as to form the outer layer.