Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.

Abstract: A medicament delivery system is disclosed. The system comprises a descending formulation for delivering the medicament and an ascending formulation to protect a patient being treated with the medicament from the side effects thereof.

Abstract: Embodiments of the invention include determining whether an individual has autism spectrum disorder or is at risk for developing autism spectrum disorder or at risk for regression of or into autism spectrum disorder. Specific embodiments include the determination of indicative levels of carnitine or other metabolites in carnitine biosynthesis and may include assaying for mutations in TMLHE, including in exon 2, for example. In some cases one can assay for mutations in TMLHE in the absence of biochemical analysis of carnitine biosynthesis metabolites. An individual with deficiency in TMLHE and/or carnitine levels may be administered carnitine, acetylcarnitine, butyrobetaine, or a combination thereof, for example.

Abstract: The objective of the present invention is to provide an antimicrobial composition that can be safely used with a broad range of foods and beverages, cosmetics, drugs, and other similar products while showing growth inhibition activity against a wide variety of microorganisms. The present invention relates to the antimicrobial composition comprising at least one cooling agent selected from the group consisting of menthyl 3-hydroxybutanoate, 2-methyl-3-(menthoxy)propane-1,2-diol, 2-(menthoxy)ethanol, 3-menthoxypropan-1-ol, 2-(2-menthoxyethoxy)ethanol, and menthyl glyoxylate.

Abstract: Disclosed are alkoxyalkyl S-prenylthiosalicylates and pharmaceutical compositions containing the same and a pharmaceutically acceptable carrier. Methods for treating a human afflicted with cancer, including solid tumors, or a hematological malignancy by administering to the human in need thereof an effective amount of an alkoxyalkyl S-prenylthiosalicylate are also disclosed.

Abstract: A cooling composition comprising a cooling agent together with a polyethylene glycol (PEG) or a mixture of different PEGs having high molecular weights and an absorbent article comprising the cooling composition. The cooling agent of the composition has a reduced tendency to vaporize and evaporate at room temperature.

Abstract: Provided is a mating disruption method capable of bringing a stable and effective mating disruption result. Specifically provided is a mating disruption method comprising a step of starting to apply a mating disruptant after mating and oviposition of imagoes of the first generation of an insect pest are substantially over and before imagoes of the second generation of the insect pest emerge, the mating disruptant targeting at least one kind of insect pest which contains one or more kinds of acetates as a natural sex pheromone.

Abstract: Disclosed is a method of synthesizing new optically pure heterocyclic compounds using Pd(0) catalyzed intramolecular cyclizations. Analogs of cyclopentanes, like isoxazoline-2-oxide and furan, with similar framework to the cyclopentanes act as anti-HIV and anticancer agents which opens a whole new field for application of these compounds. Starting from a meso-diol, optically pure compounds were prepared without utilizing chiral ligands at any stage of the synthesis. The stereochemical outcome of the product (>99% ee) was influenced by desymmetrization catalyzed by Pseudomonas cepacia lipase and the stereo selective nature of the palladium catalyzed transformations.

Abstract: Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

Abstract: The present disclosure relates to pesticidal compositions and to methods for controlling pests such as insects and other arthropods. More particularly, the disclosure relates to pesticidal compositions containing mineral oil and one or more additional components which, when used in combination, act synergistically to control insect and pest populations.

Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.

Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.

Abstract: The present invention provides a cooling component or sensate component which does not have undesirable stimulus feeling, bitterness and the like and is excellent in the persistence of refresh-feeling and cool-feeling, a sensate composition which comprises the same, and various products that comprise said sensate composition.

Abstract: This invention relates to synergistic combinations of selected microbicides in combination with a second microbicide or formulation ingredient or raw material. The combinations have greater efficacy than would be expected from combinations of the individual components. The combinations include mixtures of (a) 5-Chloro-2-methyl-4-isothiazolin-3-one+2-Methyl-4-isothiazolin-3-one, (b) Methyl-4-isothiazolin-3-one, or (c) 1,2-Benzisothiazolin-3-one with one or more of a variety of other compounds.

Abstract: An aqueous composition for topical application includes at least 60% w/w of a C1-C4 alkyl lactate ester, at least 1% w/w water, having a pH in the range from 1-6, and an effective amount of at least one physically acceptable antioxidant. A method is provided for the preparation, and the use of the composition for the treatment of fungus infections of nails and/or skin, in particular onychomycosis and tinea pedis, and an applicator device for performing such treatment.

Abstract: This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.

Abstract: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.

Abstract: The invention relates to a method of ameliorating multiple sclerosis and/or the symptoms of multiple sclerosis in a mammal, which comprises administering or having self administered to the mammal an effective amount of (a) cetyl myristate or (b) cetyl myristate and cetyl palmitate. In preferred embodiments the mode of administration is oral and both cetyl myristate and cetyl palmitate are administered.

Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Disclosed herein is a device for the application of agricultural active agents, wherein the device is suitable to be brought to the site of action in a manner temporally and spatially separated from the production process, and comprises a dispenser and non-water-soluble nanofibers and/or mesofibers charged with agricultural active agents. The polymers from which the nanofibers and/or mesofibers are made are preferably biodegradable. The agricultural active agents are selected from fungicides, herbicides, batericides, plant growth regulators and plant nutrients. These are preferably pheromones, kairomones and signaling substances. Furthermore, a method for the production of this device is disclosed, wherein the nanofibers and/or mesofibers charged with active agents are produced via electrospinning. The device is suitable to be used to bring agricultural active agents to the site of action in a manner temporally and spatially separated from the production of this device.

Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.

Abstract: The present invention provides microcapsules comprising benzoyl peroxide and topical compositions comprising them, optionally along with other active ingredients, particularly for the treatment of acne.

Abstract: The invention relates to a pharmaceutical composition containing (a) fesoterodine and/or fesoterodine metabolites and (b) fibers, wherein the weight ratio of components (a):(b) is in the range from 1:50 to 1:2; and oral dosage forms containing the pharmaceutical composition. The invention further relates to dry methods of preparing those dosage forms.

Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.

Abstract: By using a composition for preventing onset and/or recurrence of stroke which contains ethyl icosapentate as its effective component, onset and/or recurrence of stroke is prevented, or in particular, the onset and/or recurrence of stroke in a hyperlipidemia patient who has been treated with HMG-CoA RI, or in particular the recurrence of stroke in a patient who is beyond six months after the onset of stroke, is prevented.

Abstract: Polymorphically pure crystalline forms of fesoterodine fumarate and fesoterodine base are described and characterized.

Abstract: The present invention provides compositions comprising peroxy ?-ketocarboxylic acid and methods for using the same. In some particular embodiments, compositions of the invention also include ?-ketoesters.

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: This application discloses a therapeutic composition, a method of preparing a therapeutic composition, and a method for treating skin with a therapeutic composition.

Abstract: Disclosed is a method of synthesizing new optically pure heterocyclic compounds using Pd(0) catalyzed intramolecular cyclizations. Analogs of cyclopentanes, like isoxazoline-2-oxide and furan, with similar framework to the cyclopentanes act as anti-HIV and anticancer agents which opens a whole new field for application of these compounds. Starting from a meso-diol, optically pure compounds were prepared without utilizing chiral ligands at any stage of the synthesis. The stereochemical outcome of the product (>99% ee) was influenced by desymmetrization catalyzed by Pseudomonas cepacia lipase and the stereoselective nature of the palladium catalyzed transformations.

Abstract: The present invention relates to compositions and methods for decreasing the infectivity, morbidity, and rate of mortality associated with a variety of pathogenic organisms and viruses. The present invention also relates to methods and compositions for decontaminating areas colonized or otherwise infected by pathogenic organisms and viruses. Moreover, the present invention relates to methods and compositions for decreasing the infectivity of pathogenic organisms in foodstuffs.

Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: The invention relates to organic compounds having the ability to reduce or suppress the onset of skin irritation induced by extraneous cause selected from the group of 2-heptylcyclopentanone, 2-ethoxynaphthalene; 2-methoxynaphthalene; 1-methoxy-4-(prop-1-enyl)benzene; 1-(cyclopropylmethyl)-4-methoxybenzene; wherein X, Y, and R1 to R11 have the same meaning as given in the description. Furthermore the invention refers to compositions for topical application to the skin comprising them. It further relates to a method of reducing or suppressing the formation of skin irritation.

Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Abstract: Methods and systems for temperature-controlled, on-site generation of peracids, namely peroxycarboxylic acids and peroxycarboxylic acid forming compositions are disclosed. In particular, methods for using an adjustable biocide formulator or generator system overcome the limitations of temperature on the kinetics of the peracid generation and/or peracid decomposition inside an adjustable biocide formulator or generator system. The methods include the controlling of the temperature of at least one raw starting material, namely water, to improve upon methods of on-site generation of peracids. The methods allow for the generation of user-selected chemistry without regard to the ambient temperatures of the raw starting materials and/or the biocide formulator or generator system.

Abstract: The present invention relates to a pharmaceutical composition and method for treating and preventing musculoskeletal and connective tissue diseases of unknown etiology, such as different forms of arthritis and other rheumatic conditions, comprising a combination of therapeutic agents that improve the processes of blood circulation and angiogenesis in the affected tissues, as well as other supporting therapies. Among the components of herein proposed pharmaceutical composition, are: vitamin K, polyunsaturated fatty acids (blood thinner), and niacin (vasodilator and hypolipidemic agent).

Abstract: The invention provides compounds of Formula (I): wherein R1 and R2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Abstract: An acetyl xylan esterase variant having perhydrolytic activity is provided for producing peroxycarboxylic acids from carboxylic acid esters and a source of peroxygen. More specifically, a Thermotoga maritime acetyl xylan esterase gene was modified using error-prone PCR and site-directed mutagenesis to create an enzyme catalyst characterized by an increase in specific activity. The variant acetyl xylan esterase may be used to produce peroxycarboxylic acids suitable for use in a variety of applications such as cleaning, disinfecting, sanitizing, bleaching, wood pulp processing, and paper pulp processing applications.

Abstract: An acetyl xylan esterase variant having perhydrolytic activity is provided for producing peroxycarboxylic acids from carboxylic acid esters and a source of peroxygen. More specifically, a Thermotoga maritima acetyl xylan esterase gene was modified using error-prone PCR and site-directed mutagenesis to create an enzyme catalyst characterized by an increase in specific activity. The variant acetyl xylan esterase may be used to produce peroxycarboxylic acids suitable for use in a variety of applications such as cleaning, disinfecting, sanitizing, bleaching, wood pulp processing, and paper pulp processing applications.

Abstract: The various embodiments of the present invention are directed to methods and compositions for treatment, inhibition or reduction of metastasis in cancers. In particular, the invention is related to compositions and methods affecting connective tissue growth factor (CTGF). An aspect of the present invention comprises a method for interfering with the activity of connective tissue growth factor, comprising, administering to a subject an effective amount of a composition that inhibits production of or activity of connective tissue growth factor (CTGF), wherein the composition interferes with the activity of CTGF or prevents the transcription of CTGF genes or translation of CTGF mRNA. For example, the composition can comprises at least one HMG-CoA reductase inhibitor compound, such as a statin.

Abstract: An acetyl xylan esterase variant having perhydrolytic activity is provided for producing peroxycarboxylic acids from carboxylic acid esters and a source of peroxygen. More specifically, a Thermotoga maritima acetyl xylan esterase gene was modified using error-prone PCR and site-directed mutagenesis to create an enzyme catalyst characterized by an increase in specific activity. The variant acetyl xylan esterase may be used to produce peroxycarboxylic acids suitable for use in a variety of applications such as cleaning, disinfecting, sanitizing, bleaching, wood pulp processing, and paper pulp processing applications.

Abstract: One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.

Abstract: Disclosed is herein a composition comprising hexamidines, derivatives thereof, or pharmaceutically acceptable salts thereof; and retinoids, derivatives thereof, or pharmaceutically acceptable salts thereof, as an active ingredient. The composition of the present invention has effects for preventing, improving or treating acne; controlling sebum; pore-controlling; and preventing, improving or treating skin pigmentation. Also, the composition of the present invention could alleviate skin-irritations caused with retinoids by including ceramides.

Abstract: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having low content in impurities.

Abstract: The present invention discloses the signaling pathway involved in erythroid repression by iron deficiency. Further disclosed is a non-toxic small-molecule compound which potently reverses the erythroid repression caused by iron deficiency. The present invention further encompasses novel compounds for inhibition of red cell production, useful, for example, in the treatment of polycythemia vera, a malignancy causing uncontrolled red cell production. These inhibitory compounds also promote megakaryocytic lineage commitment and may therefore be useful for augmentation of platelet production. The present invention further discloses isocitrate reversal of iron deprivation.

Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract: The present invention relates to 1 or 2 C16-C18 acyl glycerol based compounds which are capable of activating G-protein coupled receptor 119 and thereby stimulate GLP-1 release. Compounds of the present invention are useful in the prophylaxis and/or treatment of metabolic disorders and complications thereof, such as, type 2 diabetes mellitus (T2DM), obesity, insulin resistance, and cardiovascular disease.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating hyperlipidemia, fatty liver, diabetes and obesity comprising a sesquiterpene derivative as an active ingredient. The sesquiterpene derivatives of the present invention leads to decrease in body fat weight, visceral fat weight and total cholesterol levels, triglyceride of plasma and liver tissue, blood glucose and blood insulin levels in a fast state, finally exhibiting efficacies on prevention or treatment of hyperlipidemia, fatty liver, diabetes and obesity.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The invention concerns desfesoterodine in the form of a tartaric acid salt, in particular in the polymorphic “R form”, as well as a process for its production. In a second aspect, the invention concerns the desfesoterodine of the invention in a microencapsulated form.