Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Pyridylene Compound”); compositions comprising an effective amount of a Pyridylene Compound; and methods for treating or preventing pain or other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Pyridylene Compound.

Abstract: The use of azaxanthones for treating diseases associated with tumor cells which express one or more protein of S100 family, and in treating patients that have malignancies consisting of tumors of an epithelial or mesenchymel nature, where these compounds are effective in retarding the progression and/or metastasis of these tumors.

Abstract: The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.

Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract: An agent for the treatment of allergic eye disease containing a 3-anilino-2-cycloalkenone derivative having the formula (I): wherein R1 is an unsubstituted or substituted C1 to C8 alkyl group provided that an unsubstituted methyl group is excluded, a C3 to C7 cycloalkyl group, a C6 to C10 bicycloalkyl group or an indanyl group, etc., R2 is a C1 to C4 alkyl group, R3 is a hydrogen atom, a C1 to C5 alkyl group, a C3 to C7 cycloalkyl group, etc., R4 is a hydrogen atom, an unsubstituted or substituted C1 to C5 alkyl group, a halogen atom, etc., R5, R6, R7 and R8 are independently a hydrogen atom, a C1 to C5 alkyl group, etc., X is —(CR11R12)n— or NR13—, wherein n is 0 to 2, R11, R12 and R13 are independently a hydrogen atom, a C1 to C5 alkyl group, etc.

Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Abstract: This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.

Abstract: The disclosure relates to a compound of formula (I): in which: R1, R2, R3 and R4 are as described in the specification, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these compounds and to certain intermediate products.

Abstract: The present invention relates to substituted benzoylguanidines of the formula I: in which R1 to R8 and X and Y are as described in the specification, and their pharmaceutically acceptable salts are substituted acylguanidines as inhibitors of the cellular sodium-proton antiporter (Na+/H+ exchanger, NHE).

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.

Abstract: The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.

Abstract: Novel compounds of the formula I in which R, X and n are as defined herein, are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: There are provided compounds according to formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention. Other embodiments are also disclosed.

Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.

Abstract: The invention relates to the compounds of formula (I): or a pharmaceutically acceptable salt and solvate thereof, wherein R1 is F or H and to processes for the preparation of, intermediates used in the preparation of, compositions containing the uses of, such compounds. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular allergic and respiratory diseases, disorders and conditions.

Abstract: The invention relates to a bicycloazaheterocyclyl carboxylic acid sulfonamide derivative of formula I herein, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use.

Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.

Abstract: The present invention provides a pharmaceutical composition for enhancement of glucose uptake into warm-blooded animal cells, treatment of diabetes, treatment or prevention of diabetes complications etc., treatment or prevention of diabetes or diabetes complications caused by insulin resistance syndrome, and the like, comprising as an active ingredient an HMG-CoA reductase inhibitor.

Abstract: A stable pharmaceutical composition for oral administration comprising atorvastatin and an amount of a pharmaceutically acceptable organic alkalizing compound capable of establishing a microenvironment for atorvastatin having a pH of at least about 5, for example 2-amino-2-(hydroxymethyl)-1,3-propanediol (trometamol).

Abstract: Pharmaceutical formulations comprising docetaxel, solubilizer, and ?-lipoic acid, wherein the formulation is substantially free of polysorbates and polyethoxylated castor oil. The solubilizer may comprise glycofurol, acetic acid, benzyl alcohol, or ethanol. The ?-lipoic acid, at certain concentrations, may impart stability and prevent degradation of docetaxel while the formulations are in storage. The formulations may be combined with a diluent, which comprises one or more hydrotropes such as tocopherol polyethylene glycol succinate and polyethylene glycol. The formulations combined with the diluent also exhibit stability after storage. Methods of administering docetaxel comprise preparing the formulation comprising docetaxel, solubilizer, and ?-lipoic acid; mixing the formulation with a diluent; diluting the resulting formulation in saline, water for injection, or the like; and then injecting the formulations into patients in need thereof.

Abstract: Therapeutic compositions of doxepin and having a preponderance of the cis doxepin isomer over the trans doxepin isomer provide therapeutic effects for affective, painful, or allergic disorders without the sedative effects commonly experienced with compositions having a preponderance of the trans doxepin isomer.

Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.

Abstract: The invention provides novel omega-3 oil formulations comprising fenofibrate and a statin. These formulations are effective in small volumes. Related methods of treatment are also described.

Abstract: The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione.

Abstract: A vegetable butter based dietary supplement of cetyl myristoleate is disclosed for use in the treatment of osteoarthritis and other joint inflammatory diseases of the musculoskeletal system in animals, especially equines. In its preferred form, the cetyl myristoleate is a vegetable butter-based and is administered in doses of about 4000 to about 4500 mg. The dosage may also include 3000 mg methylsulfonylmethane, 3000 mg glucosamine HCL and 1000 mg of Vitamin C.

Abstract: The present invention provides crystals of L-ornithine and a process for producing the crystals of L-ornithine including the steps of (i) exposing L-ornithine or a salt thereof, a composition comprising L-ornithine or a salt thereof, or a solution containing L-ornithine, a salt thereof, or the composition to a cation exchange resin to adsorb L-ornithine onto the cation exchange resin; (ii) eluting L-ornithine from the cation exchange resin on which L-ornithine is adsorbed with an aqueous alkaline solution, and removing an alkaline component from the resulting eluate to prepare an aqueous L-ornithine solution; and (iii) mixing the aqueous L-ornithine solution with a hydrophilic organic solvent, and crystallizing L-ornithine from the resulting mixed solution.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: An inexpensive, easily available, and convenient method of treating or preventing a virus infection is provided. The present invention relates to a method for the treatment or prevention of virus infections using polybiguanide-based compounds administering a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof. The invention relies on the unique biochemical reaction in which polybiguanide-based compounds interfere with the spread of virus within or between organisms. The compositions and formulations described in the present invention are effective means to reduce the infectivity of the human immunodeficiency virus type 1 (HIV-1), and human herpes simplex viruses, and also to kill the causative organisms of many other sexually transmitted diseases (STDs).

Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.

Abstract: The present invention relates to a copolymer, which is the reaction product of (a) a first prepolymer, comprising a bioactive moiety and at least one radically polymerizable group, and (b) a second prepolymer which is a polyvinyl alcohol having a weight average molecular weight of at least about 2000 that, based on the number of hydroxy groups of the polyvinyl alcohol, comprises from 0.5 to 80% structural units of formula (I) wherein: R is alkylene having up to 8 carbon atoms, R1 is hydrogen or alkyl having up to seven carbon atoms, and R2 is an olefinically unsaturated, electron-attracting copolymerizable radical.

Abstract: A process and apparatus for rapidly producing an emulsion and microcapsules in a simple manner is provided wherein a dispersion phase is ejected from a dispersion phase-feeding port toward a continuous phase flowing in a microchannel in such a manner that flows of the dispersion phase and the continuous phase cross each other, thereby obtaining microdroplets, formed by the shear force of the continuous phase, having a size smaller than the width of the channel for feeding the dispersion phase.

Abstract: The invention provides a composition that is a dispersion made from a Group III nitride, a solvent system, and a dispersant. The dispersion can be used to prepare Group III nitride thin films on a wide range of substrates, for example, glass, silicon, silicon dioxide, silicon nitride, silicon carbide, aluminum nitride, sapphire, and organic polymers. The particle size of the Group III nitride used for producing the thin films can be controlled by adjusting centrifugation of the dispersion and selecting a desired layer of supernatant. The dispersant can be removed from the thin films by calcination. The Group III nitride can contain a dopant. Doped Group III nitride thin films can emit visible light upon irradiation. Green, red, and yellow light emissions result from irradiating erbium-, europium-, and cerium-doped gallium nitride, respectively.

Abstract: Prior colloidal crystal preparation means requires much workmanship to obtain colloidal crystals, relying much on the expertise of an operator. To utilize colloidal crystals in various fields and develop them from now on, it is in demand to establish preparation means capable of preparing colloidal crystals with good reproducibility. The object of the invention is to meet such demand. A gas compressed in a compressor (1) is controlled by a gas pulse controller (3) to generate compressed air pulses, and the pulses are then guided to a colloidal crystal preparation vessel (6) having a flat plate type capillary portion to produce a pressure fluctuation, which is in turn used as driving power, thereby giving a flow and hard-stopping motion to a colloidal solution in the flat plate type capillary for formation of colloidal crystals of good single crystallinity.

Abstract: A method to prepare multi-phobic effects nanosized-structure film and its application are described, which features nanosized silica, titanium oxide and zinc oxide compounded materials of previous size 3-100 nm are in-situ combined with substrate through fluorocarbon surfactants and perfluoro alkyl filming substance under specific conditions to form a nanosized-structure film. The reaction between fluorocarbon surfactants and hydroxyl groups on surfaces of nanosized particles renders the modified nanosized particle and nanosized film having extremely high chemical stability, resistance, and the capacity to repel and disperse water, oil, bacteria, organic dust, gas, electricity, magnetism and light (i.e., multi-phobic effects). This technology may be widely used in surface modification of fabric, chemical fiber, cotton, wool, glass product, brick-stone concrete and wood wall.

Abstract: A process for producing liquid and, optionally, gaseous products from gaseous reactants includes feeding at a low level a gaseous reactants feed comprising at least CO and H2 into an expanded slurry bed of solid non-shifting hydrocarbon synthesis catalyst particles suspended in a suspension liquid, the expanded slurry bed having an aspect ratio of less than 5. The gaseous reactants and any recycled gas are allowed to react with a per pass CO plus H2 conversion of at least 60% as they pass upwardly through the slurry bed at a gas velocity of at least 35 cm/s, thereby to form liquid and, optionally, gaseous products, and with the gaseous reactants and any recycled gas and any gaseous product assisting in maintaining the solid catalyst particles in suspension in the suspension liquid, and with the liquid product forming together with the suspension liquid, a liquid phase of the slurry bed.

Abstract: A method of producing synthesis gas for methanol synthesis that comprises the steps of: (a) obtaining a hydrogen stream that has greater than 5 mol % methane from an external process; (b) feeding into a reforming reactor: (i) a feed gas that comprises methane, (ii) water in a specified amount, (iii) oxygen in a specified amount, and (iv) the hydrogen stream in a specified amount; (c) reacting the feed gas, water, oxygen and the hydrogen stream in the reactor; and (d) withdrawing from the reactor the synthesis gas that is at a specific temperature, has less than 3 mol % methane, and has a stoichiometric number of from 1.9 to 2.3.

Abstract: An improved process for the hydrolysis of nylon polymer is herein disclosed using ionic liquids and optionally one equivalent of sulfuric acid per amide residue of the polymer. The process provides for a simplified means for separation of the hydrolyzed polyamide constituent monomers.

Abstract: A method for forming a fire resistant material is disclosed. The method comprises providing a plurality of expandable beads of a polymeric material. The beads are coated with an exfoliable graphite. The exfoliable graphite is adhered to the beads with a resin having a solubility parameter of the polymeric material. The beads are thereafter caused or allowed to expand and fuse.

Abstract: To provide a resin composition excellent in conformability to special shapes and in holding power without the need of containing a low molecular softener such as a plasticizer, other than a polysiloxane, and a cured product and a sheet using it. A resin composition characterized by comprising (a) an acrylic rubber, (b) a compound containing at least two mercapto groups per molecule, (c) a compound containing at least two acryloyl and/or methacryloyl groups per molecule, (d) an acrylate and/or methacrylate having a C2-12 alkyl group, and (e) acrylic acid or methacrylic acid. The above resin composition which contains a thermally conductive filler. A cured product and sheet using it.

Abstract: The present invention provides novel antimicrobial polyurethane compositions having excellent mechanical and biocompatibility properties, and methods to prepare them. The antimicrobial polyurethane compositions include a homogenous distribution of silver ions by incorporating this antimicrobial agent into the composition prior to the complete polymerization of the polyurethane. In preferred embodiments, the silver ion is associated with a carrier, such as zirconium phosphate or soluble glass powder. The present invention also includes components made from the antimicrobial polyurethane compositions, such as medical devices.

Abstract: A method for making an optical element comprises polymerizing a first monomer to form a first polymer, the first polymer having a spatially varying degree of cure that provides a predetermined refractive index profile; and polymerizing a second monomer in the presence of the first polymer to form a second polymer intermixed with the first polymer, the second polymer stabilizing the first polymer and the refractive index profile.

Abstract: Ink jet recording is carried out using an ink set including a clear ink composition that contains polymer fine particles and does not contain a colorant, a yellow ink composition, a magenta ink composition, a cyan ink composition, a red ink composition, a violet ink composition, and a black ink composition, whereby a high-quality recorded article having excellent recorded image coloration and glossiness can be obtained.

Abstract: A method for forming polyolefin/clay composites by olefin polymerization which can be used as flame retardants in which at least one filler is combined with an early or late transition metal first catalyst component that becomes activated for olefin polymerization when in contact with the treated filler. An olefin is contacted by the activated catalyst-filler combination either (a) in the absence of an alkylaluminum second catalyst component or (b) in the presence an alkylaluminum second catalyst component when the first catalyst component is an early transition metal catalyst, whereby to form an clay-polyolefin composite incorporating platelets of said filler. The filler is preferably clay, exemplified by montmorillonite and chlorite. The first catalyst component is preferably a non-metallocene catalyst. A predetermined amount of one or more olefinic polymers can also be blended with a masterbatch to obtain a composite having a desired amount of loading.

Abstract: A polymeric composition consisting of water-soluble or water-swellable copolymers containing sulfo groups and nonionic polysaccharide derivatives, such as methylcellulose (MC), hydroxyethylcellulose (HEC), hydroxypropylcellulose (HPC), methylhydroxyethylcellulose (MHEC), methylhydroxypropylcellulose (MHPC) and welan gum or diutan gum, and the use thereof as an additive in aqueous construction systems based on hydraulic binders, such as cement, lime, gypsum or anhydrite, is described. The composition can also be used in water-based paint and coating systems. The composition according to the invention exhibits a synergistic improvement of the properties and, when used in relatively small amounts, constitutes highly effective water retention agents in such construction and paint systems, which also achieve outstanding air pore stability and tack.