Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.

Abstract: A process for producing a compacted rumen-protected nutrient pellet and the resultant pellet. The process includes the steps of (i) blending a C4-24 fatty acid and a biologically active ingredient to form solid central core particles, (ii) compacting the core particles to form pellets, and (iii) sequentially coating the pellets with an organic solvent and a fatty acid alkali metal or alkaline earth metal salt.

Abstract: Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.

Abstract: Provided herein are methods and compositions for modulating the activity or level of a sirtuin, thereby treating or preventing obesity or an insulin resistance disorder, such as diabetes in a subject. Exemplary methods comprise contacting a cell with a sirtuin activating compound or an inhibitory compound to thereby increase or decrease fat accumulation, respectively.

Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention generally relates to methods of modulating Cav1.2 channels and Cav1.2 channel activators.

Abstract: A cosmetic composition suitable for topical application is provided. In some examples, the cosmetic composition can include glycerin, hexyldecanol, a vitamin B compound, and one or more materials selected from the group consisting of 1,2-pentanediol, 1,4-pentanediol, 2,4-pentanediol, 1,5-pentanediol, 1,2-butanediol, 1,3-butanediol, 1,4-butanediol, 2,3-butanediol, 1,2-hexanediol, 1,5-hexanediol, 1,6-hexanediol, 2,5-hexanediol, hexylene glycol, and combinations thereof.

Abstract: The described invention provides a biodegradable, biocompatible delivery system of flowable sustained release microparticulate composition of a substantially pure crystalline form of a bioactive agent such as, for example, nimodipine, a process of preparing a therapeutic form of a substantially pure crystalline form of the bioactive agent and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.

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: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.

Abstract: The described invention provides a biodegradable, biocompatible delivery system of flowable sustained release microparticulate composition of a substantially pure crystalline form of a bioactive agent such as, for example, nimodipine, a process of preparing a therapeutic form of a substantially pure crystalline form of the bioactive agent and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.

Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.

Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection.

Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.

Abstract: The present invention relates to a hard capsule composite formulation comprising a capsule having a hemispherical closure at each end and an interior space; and one or more tablets encapsulated in the capsule, wherein the tablet or the tablets as a whole have a shape conforming to the internal space of the capsule. The hard capsule composite formulation can efficiently charge pharmaceutical compositions inside the limited interior space of the capsule, and hence, it allows packing a high-dose of pharmaceutical composition in a relatively small-sized capsule, which increases productivity and patient compliance. Also, the composite formulation exhibits good dissolution rate because pharmaceutically active ingredients contained in the capsule are separated from one another, and thus, the ingredients are less affected by the dissolution rate of one another, allowing good storage stability which can optimize the therapeutic effects.

Abstract: A process for the manufacture of compositions containing niacin, the process including a first compaction step of niacin or a pharmaceutically acceptable salt thereof, then a second compaction step of a dry blend comprising niacin and microcrystalline cellulose and a further compression step into tablets. Stable tablet compositions including niacin are capable of extended release of niacin.

Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures. One disclosed composition comprises ketoprofen and nifedipine in a liquid irrigation carrier, and includes a solubilizing agent, stabilizing agents and a buffering agent.

Abstract: The invention relates to formulations useful in treating hair disorders, improving the health of hair, increasing hair growth, and in increasing the niacin content of hair follicles. Nicotinic acid alkyl esters having a straight chain alkyl group of from 1 to 22 methylene units, preferably from 6 to 16 methylene units, and most preferably from 8 to 14 methyl units, may be used, alone or in combinations for treating these conditions.

Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.

Abstract: The invention relates to a pharmaceutical combination of 2-aminoethanesulfonic acid with a pharmaceutical agent such as an antihypertensive agent and the use of 2-aminoethanesulfonic acid in a method to lower the bilirubin level in the blood.

Abstract: A single layer pharmaceutical composition comprising active agent(s) amlodipine or a pharmaceutically acceptable salt thereof and valsartan or a pharmaceutically acceptable salt thereof wherein the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to human subject, under the bioequivalence parameters of a 90% Confidence Interval for AUC which is between 80% and 125%, and a 90% Confidence Interval for Cmax, which is between 80% and 125%.

Abstract: Disclosure of methods and compositions related to chemical conjugations to nanoparticles of polysaccharides cross-linked to poloxamers as well as nano-sized colloids comprised of polysaccharides and poloxamers. The nanoparticles may be produced by various methods including inverse miniemulsion polymerization processes which create nanogels of desired size, shape, and stability for controlled therapeutic drug delivery, imaging, and theragnostic applications.

Abstract: The present invention relates to liquid application for skin rejuvenation created from specific amino acids, lipids, nucleic acids and vitamins. This collection of molecules delivers precisely the factors necessary to a specific site requiring healing; a direct intervention system to most expeditiously remodel skin with building blocks. This delivery is a transdermal topical delivery and healing is via specific molecules that engender a false autocoid reaction rapidly followed by an incremental healing-anti-inflammatory response augmented by very specific GRAS ingredients in the invention and also recruited from the body to this needy site. Energy is brought to site by transdermally delivered protons and enhanced by the local vascular flow initiated by transdermal molecules. This delivery system bypasses digestion and dilution. Key is a lipophilic carrier with nuclear and mitochondrial ligands that rapidly penetrate and permeate all membranes and truncates the inflammatory site quickly manifesting curation.

Abstract: This invention relates to the use of niacin and/or trigonelline compounds to increase muscle weight during periods of activity or to inhibit muscle loss during periods of inactivity.

Abstract: A botanical antioxidant composition includes a botanical antioxidant extract blend including a first antioxidant botanical extract including at least one hydroxycinnamic acid, and at least one additional antioxidant botanical extracts including at least one antioxidant selected from the group consisting of vitamins, stilbenoids, curcumininoids, tannins, flavones, flavonols, flavan-3-ols, flavanones, anthocyanidins, anthocyanins, isoflavones, flavanonols, proanthocyanidins, dihydroxybenzoic acids, and pyridine alkaloids.

Abstract: A transdermal delivery kit that enhances the efficacy of a topical drug includes at least one drug dispensing device, a lipophilic base, a hydrophilic base, a lipid-soluble active ingredient, a water-soluble active ingredient, a first container for mixing the lipophilic base with the lipid-soluble active ingredient to form a first compound, a second container for mixing the hydrophilic base with the water-soluble active ingredient to form a second compound, a mixing member, and instructions for compounding the lipophilic base with the lipid-soluble active ingredient to form the first compound, compounding the hydrophilic base with the water-soluble active ingredient to form the second compound, and mixing the first compound and the second compound to form a transdermal pharmaceutical delivery system capable of delivering a drug to the dermal layer of the skin.

Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.

Abstract: This invention pertains to methods and compositions for the diagnosis and treatment of cardiovascular conditions. More specifically, the invention relates to isolated molecules that can be used to diagnose and/or treat cardiovascular conditions including cardiac hypertrophy, myocardial infarction, stroke, arteriosclerosis, and heart failure.

Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment (particularly for reducing the risk of venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection.

Abstract: A device for drug delivery to an orifice of a subject, comprising a shell which is elastically stressed by an active pharmaceutical ingredient, said shell containing and being substantially impermeable to said active pharmaceutical ingredient, wherein said shell has at least one hole sized for in-vivo release of said active pharmaceutical ingredient as a result of elastic stressing.

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: The present invention relates to oral dosage formulations consisting of at least one active ingredient contained in a plurality of hydrophobic carriers dispersed in an aqueous medium comprising a hydrocolloid. The active ingredients include various energy supplements, such as caffeine and vitamins. The formulations may further include emulsifiers, permeation enhancers, and vasodilators. The invention further relates to methods of making the oral dosage formulations.

Abstract: Methods for controlling, maintaining, or reducing blood pressure, and/or for treating, preventing, or alleviating symptoms such as dyspnea, in a patient suffering from or susceptible to acute heart failure. The methods involve the administration of an effective amount of a pharmaceutical composition comprising a short acting dihydropyridine compound such as clevidipine. The pharmaceutical composition may be administered at an initial dose, and if blood pressure is not controlled or maintained within a target blood pressure range or reduced to within a target blood pressure range, the initial dose may be titrated to achieve a blood pressure within the target blood pressure range. The patient may have a systolic blood pressure of about 120 mmHg or above.

Abstract: Provided are materials and methods for the prevention and treatment of Juvenile Neuronal Ceroid Lipofuscinosis comprising administration of an effective amount of at least one of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor. In some embodiments, the methods comprise administration of an effective amount of each of a hemi-channel inhibitor and a phosphodiesterase-4 inhibitor. Also provided are pharmaceutical compositions comprising a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor, as well as kits comprising at least one effective dose of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor or a combination of both.

Abstract: Methods for treating hyperlipidemia with intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, without causing drug-induced hepatotoxicity to a level which would require discontinuation of the therapy, are disclosed. According to the methods of the present invention, the intermediate nicotinic acid formulations are administered as a single dose once-a-day during the evening or at night. While the methods of the present invention contemplate administering the intermediate release nicotinic acid formulations at any time during a 24 hour period, it is preferable to administer them as a single dose during the evening or at night between about 6:00 pm. and 12:00 a.m., preferably between about 8:00 p.m. and 12:00 a.m., and most preferably between about 8:00 p.m. and 10:00 p.m.

Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.

Abstract: The present invention relates to a pharmaceutical composition having dopaminergic activity and other related pharmaceutical activities comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s), optionally along with excipients(s); a process of preparing a pharmaceutical composition comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s), optionally along with excipients(s), wherein the process comprising steps of: (a) extracting a clear solution containing trigonelline and 4-hydroxyisoleucine from plant source; and (b) optionally precipitating derivative(s) of trigonelline and 4-hydroxyisoleucine from the clear solution and obtaining said composition; and an in-vitro method to increase levels of dopamine or to inhibit prolactin by allowing composition comprising trigonelline or its derivative(s) and 4-hydroxyisoleucine or its derivative(s) to bind to cell receptors.

Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.

Abstract: The present invention provides a patch preparation containing a support and an adhesive layer on at least one surface of the support, wherein the adhesive layer contains a drug, amine oxide, a low-polar liquid component based on an organic compound having an angle of 0-19° as calculated by the formula (I): angle(°)=arctan(inorganic value/organic value)×(180/?) and using an inorganic value and an organic value on an organic conceptual diagram, and an adhesive base, and the adhesive layer has an amine oxide content of 0.1-5 wt % and a low-polar liquid component content of 30-50 wt %.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Abstract: The invention provides compositions and methods for visualizing particular tissues and delivering one or more therapeutics to that tissue using single-walled carbon nanotubes (SWNTs), which are taken up and delivered to target tissues by specific monocytes in the body. The delivery of SWNT to target tissues allows the visualization of the affected tissue for diagnostics and therapy in diseases where the specific monocyte is implicated in the disease pathogenesis. These nanotubes can be conjugated to a peptide, such as RGD, which helps direct the SWNT-containing monocytes to the vascular endothelium.

Abstract: The present invention relates to a solid pharmaceutical composition for preventing or treating cardiovascular disorders comprising granular forms of amlodipine and losartan which are separated from each other, and a stabilizing agent, which has improved storage stability due to minimized interaction between amlodipine and losartan.

Abstract: The present invention relates to a solid pharmaceutical composition for preventing or treating cardiovascular disorders comprising amlodipine and losartan as active ingredients, and a disintegrant which is a mixture of at least two components selected from the group consisting of sodium starch glycolate, crosscarmellose sodium, and crosspovidone, which exhibits a high and stable level of amlodipine and losartan dissolution rates.

Abstract: A transdermal delivery kit that enhances the efficacy of a topical drug includes at least one drug dispensing device, a lipophilic base, a hydrophilic base, a lipid-soluble active ingredient, a water-soluble active ingredient, a first container for mixing the lipophilic base with the lipid-soluble active ingredient to form a first compound, a second container for mixing the hydrophilic base with the water-soluble active ingredient to form a second compound, a mixing member, and instructions for compounding the lipophilic base with the lipid-soluble active ingredient to form the first compound, compounding the hydrophilic base with the water-soluble active ingredient to form the second compound, and mixing the first compound and the second compound to form a transdermal pharmaceutical delivery system capable of delivering a drug to the dermal layer of the skin.

Abstract: Pharmaceutical formulations comprising clevidipine in an oil-in-water formulation that is resistant to microbial growth and stable against the formation of impurities.

Abstract: A pharmaceutical tablet containing olmesartan medoxomil and amlodipine besylate, which has improved dissolvability. The composition contains (A) olmesartan medoxomil and (B) amlodipine besylate as active ingredients and (C) a calcium-containing additive. A method for treating or preventing hypertension by administering the pharmaceutical tablet to a patient.