Abstract: The present invention relates to isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, X and n are the same as defined in the specification.

Abstract: Indole derivatives of formula I, their salts and solvates, have valuable pharmacological properties together with good tolerability, as they have actions on the central nervous system: wherein R1 and R3 are as defined herein. The compounds have a strong affinity for 5-HT2A receptors, and furthermore exhibit 5HT2A receptor-antagonistic properties. These are therefore suitable both in veterinary and in human medicine for the treatment of functional disorders of the central nervous system and also of inflammation.

Abstract: Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms.

Abstract: The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.

Abstract: Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.

Abstract: Novel compounds are provided having the formula and salt thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl acyloxymethyl or trialkylsilyl group, or a group —CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is —COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.

Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention provides a percutaneously administrable preparation comprising either an aqueous base comprising 1-menthol, a lower alcohol and an acidic buffer or water, or an oily base comprising 1-menthol, a lower alcohol and isopropyl myristate, and a cerebral function activator, for example, 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine, pharmaceutically acceptable salt or hydrate thereof.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.

Abstract: 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.

Abstract: The present invention is directed to 3-phenylimidazol[4,5-b]pyridine derivatives, that are selective ligands for GABAA receptors. These compounds are useful in the treatment and prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: Substituted isoquinolines, isochromanones and isothiochromanones that inhibit the pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-alpha) and/or interleukin-6 (IL-6) and/or the enzyme cyclooxygenase-2 (COX-2) and/or interleukin-10 (IL-10). Compositions containing such compounds and methods of using such compounds for treatment and/or prevention of inflammation, inflammatory diseases, immunologic diseases and other diseases mediated by TNF-alpha, IL-6, COX-2 and/or IL-10 are also disclosed.

Abstract: The invention discloses methods for the chronic administration of adenosine, which contrary to the acute delivery of the drug by injection or infusion, acts in desensitizing adenosine receptors towards the action of adenosine. The methods and oral compositions of adenosine triphosphate (ATP), which is degraded to adenosine in vivo, can be used in the treatment of disorders and diseases that are therapeutically targeted by agonists or antagonists of adenosine receptors. One example is the stimulation of lipolysis in achieving weight loss in humans and in the treatment of obesity.

Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2 , which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

Abstract: A compound of the formula or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.

Abstract: Compounds of Formula (I) are disclosed. These compounds selected activators of human PPAR delta.

Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.

Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at

Abstract: A compound of the formula wherein W, R1, R2, R3, R4, R5, R6, R7, R8 and R13 are as defined herein, useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss.

Abstract: Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 aklene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 akylene group.

Abstract: Systems and methods for radiographic imaging of tissue using a radio-opaque imaging agent that in one embodiment accumulates intracellularly in tissue in proportion to its functional, or physiological, activity. In one embodiment, the imaging agent is a cell membrane-permeable, radio-opaque, high affinity ligand for an intracellular target. The imaging agent is administered to a patient, and after an accumulation interval, radiographic images are acquired. The imaging agent preferentially accumulates in certain types of tissue and increases its radio-opacity. The tissue being examined is transilluminated by X-ray beams with preselected different mean energy spectra, and a separate radiographic image is acquired during transillumination by each beam. An image processing system may perform a weighted combination of the acquired images to produce a single displayed image. The system and method thus provides a functional image displayed with the anatomical detail and spatial resolution of a radiographic image.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4 R5, R6, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: Method for treating dermal pre-melanoma conditions which include administering an effective amount of a photosensitive agent to a dermal pre-melanoma cell and activating the photosensitive agent, thereby treating a dermal pre-melanoma condition.

Abstract: The present invention relates to crystalline forms of the sodium salt of 5-chloro-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonylphenyl)ethyl)benzamide, processes for their preparation, their use, and pharmaceutical preparations comprising them.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1 )-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-benzyl-N-phenyl aminoalcohols.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.

Abstract: The use of COMT inhibitors in the treatment of control of pain in mammals, for example in animals and humans.

Abstract: A method for topically treating rosacea is disclosed. In this method, an active material having the formula given below is applied to the patient at the site of said rosacea: wherein R1 is selected from —OH and C1-C3 alkyl OH; and R2, R3, R4, R5 and R6 are independently selected from —H, —OH, C1-C6 alkyl, and C3-C6 cycloalkyl. Preferred active materials include 1,2-cyclohexanediol, 1,3-cyclohexanediol, 1,4-cyclohexanediol, and mixtures of those materials. Methods for treating acne vulgaris, as well as colds, flu, sinusitis, and ear infections, using these actives are also disclosed.

Abstract: Unreacted syngas containing CO2 from a Fischer-Tropsch synthesis reactor, a methanol synthesis reactor or a dual functional syngas conversion is scrubbed with an aqueous medium to adsorb at least some of the CO2. At least a portion of the unreacted CO2-depleted syngas is then recycled to the reactor. The aqueous medium containing absorbed CO2 is treated to desorb CO2. A CO2-enriched stream and a CO2-depleted stream are recovered. A portion of the CO2-enriched stream may be recycled to a syngas generator while another portion is dissolved in an aqueous phase and disposed in a marine environment and/or a terrestrial formation. The CO2-depleted stream preferably is used in the scrubber to absorb CO2 from the unreacted syngas. The process reduces the amount of CO2 released into the atmosphere while improving the over-all efficiency of the syngas conversion process.

Abstract: The present invention relates to novel compatible binary and ternary cation-exchanger polymer and anion-exchanger polymer blend membranes.

Abstract: Graft polymeric membranes and methods for making graft polymeric membranes have one or more trifluorovinyl aromatic monomers that are radiation graft polymerized to a polymeric base film. The membranes comprise a polymeric base film to which has been graft polymerized substituted &agr;,&agr;,&bgr;-trifluorostyrene and/or &agr;,&agr;,&bgr;-trifluorovinylnaphthylene monomers, which are activated towards graft polymerization. As ion-exchange membranes, the membranes are suitable for use in electrode apparatus, including membrane electrode assemblies in, for example, fuel cells. The membranes can also be crosslinked.

Abstract: Disclosed is a recycled resin composition having physical properties, a feeding property as well as a moldability which are by no means inferior as compared with the raw material resin composition, even when a ratio of recycled material in recycled resin composition used as molding material is increased. A recycled resin composition obtained by compounding a mixture containing (a) a raw material resin, (b) at least one kind of additives for resin, and (c) a pulverized material of a recovered molded article generated at the time of molding of a raw material resin composition comprising (a) said raw material resin and (b) said at least one kind of additives for resin and/or a recycled resin composition comprising (a) said raw material resin and (b) said at least one kind of additives for resin, is provided.

Abstract: The invention relates to a process for the production of expanded or expandable polyolefin beads by impregnating polyolefin granules with a volatile blowing agent in suspension under pressure. As suspension aid, use is made of a mixture of a water-insoluble inorganic compound and a surfactant, and the impregnation is carried out in the presence of a surface-active polymer carrying carboxyl or carboxylate groups.

Abstract: A method for forming microcellular foams that causes the material to expand uniaxially during the foaming process, and a method for forming objects from the foam. Liquid crystal polymers or polymers having a planar crystalline structure are saturated with a fluid, normally a gas such as carbon dioxide. The ambient conditions are changed such that the fluid is in a supersaturated state, and the material is brought to near its glass transition temperature to induce the formation of nonspherical elongated gas-filled cells. A process for making objects, such as transducer diaphragms, from microcellular foams includes the step of forming the objects prior to the foaming process.

Abstract: There is provided a foamable poly(vinyl chloride) resin composition which can remarkably improve an expansion ratio. There is used a foamable poly(vinyl chloride) resin composition comprising 100 parts by weight of (A) a poly(vinyl chloride) resin, 0.5 to 30 parts by weight of (B) a processing aid, and 0.

Abstract: The present invention provides a new class of materials effective as accelerators for curing anaerobic adhesives. The addition of these materials into anaerobic adhesives as a replacement for conventional curatives, such as APH and/or toluidines, surprisingly provides at higher cure speeds and comparable physical properties for the reaction products formed therefrom.

Abstract: A process for preparing an enlarged latex, which comprises (1) causing (a) an anionic surfactant and (b) at least one surfactant selected from the group consisting of a cationic surfactant and an amphoteric surfactant to exist in a latex, (2) adding, as an aggregating and enlarging agent, at least one selected from the group consisting of (i) an inorganic acid, (ii) an organic acid, (iii) a substance which forms an acid in water, (iv) a combination of at least two substances which are reacted with each other to form an acid, and (v) a substance which forms an acid by exposure to active rays to the latex in the presence of these surfactants, and (3) causing the acid derived from the aggregating and enlarging agent to act on the latex, thereby enlarging the particle diameter of the latex, an enlarged latex obtained by the preparation process, a graft copolymer obtained by polymerizing a polymerizable monomer with the enlarged latex, and a resin composition comprising the graft copolymer and a thermoplastic resi

Abstract: Autodeposition compositions for polymeric coatings of reduced gloss are prepared using resins having at least one hydroxy group and at least one epoxy group per molecule, a low temperature crosslinker and a high temperature crosslinker. The low temperature crosslinker forms a reactive prepolymer that may be subsequently mixed or emulsified with a high temperature crosslinker to form an autodeposition composition. Alternatively, a hybrid crosslinking agent may be utilized which contains both free isocyanate groups reactive at a relatively low temperature with the resin and at least one functional group capable of reacting with the resin only at a relatively elevated temperature. When deposited and cured, the resulting coating has a matte finish that is resistant to surface defects.

Abstract: The present invention relates a method for manufacturing ligneous material, characterized in comprising the steps of acetylating wood elements selected from among wood pieces crushed from lumber, thin wood plates peeled from lumber, and wood fiber obtained by means of defibrating lumber, such that the degree of acetylation (weight percent gain) is 7% or greater, and preferably 7 to 18%; and binding the resultant aceylated wood elements, using a binder containing polyisocyanate. Thereby, it is possible to provide inexpensive ligneous material which exhibits only minor dimensional changes from moisture, wherein only a small amount of formaldehyde is released.

Abstract: The present invention is drawn to colorless toner compositions for overcoating a print having an ink jet ink image printed thereon. The colorless toner can comprise: a toner resin and at least two additives independently selected from the group consisting of ultraviolet absorbers, free radical inhibitors, thermal stabilizers, and combinations thereof, wherein the ratio of toner resin to total additive is from 1:1 to 99:1 by weight. The colorless toner can also be comprised of a charge control agent and/or a low-melt wax.

Abstract: Thermoplastic compositions of polyester/polycarbonate blends have reduced yellowness and improved thermal and melt stability when the polyester is produced with a reduced level of a titanium-containing catalyst in an amount of from about 1 to about 30 ppm elemental titanium, with ppm based on the total weight of the polyester.

Abstract: A process for the production and treatment of a stereoregular propylene polymer such as isotactic polypropylene. The isotactic polypropylene can be produced by catalysis employing a metallocene catalyst or employing a Ziegler-Natta catalyst. A polymerization reactor is operated to provide for the reaction of propylene supplied to the reactor to produce a stereoregular propylene polymer fluff. A product stream containing unreacted propylene and the propylene polymer fluff is withdrawn from the polymerization reactor. The product stream is treated to separate at least a portion of the unreacted propylene from the product stream. The polymer fluff is heated to a temperature sufficient to melt the propylene polymer. Incorporated into the propylene polymer fluff in an amount within the range of 0.01-0.08 wt.

Abstract: A method of producing an organic-inorganic composite material formed from an organic polymer and a metal alkoxide, comprising the steps of polycondensating the metal alkoxide through hydrolysis until the unreacted metal alkoxide is reduced to 3 vol. % or less, and mixing it with the organic polymer to form the organic-inorganic composite material. By laminating such organic-inorganic composite materials, the resulting laminate is provided with a concentration gradation wherein the metal element of the metal alkoxide is increased or decreased from one side to the other side of the laminate.

Abstract: A composition of matter is disclosed wherein the composition comprises a polyurethane elastomer prepared by mixing A) a polyurethane prepolymer, B) a curative, and C) a liquid, non-reactive polydimethylsiloxane, wherein C) is present in a concentration of about 0.5 to about 25% based on the combined weight of A) plus B), and curing the mixture to form the elastomer.

Abstract: The present invention provides a resin composition comprising 100 parts by weight of a methyl methacrylate resin or styrene resin, about 0.1 to about 20 parts by weight of a light diffusing agent, about 0.0005 to about 0.1 parts by weight of an ultraviolet absorber selected from the group consisting of 2-(1-arylalkylidene) malonates and oxalanilides, and about 0.0001 to about 0.01 parts by weight of a phosphor. This resin composition is used as a material of a light diffusing member showing excellent light diffusible transmittance, having excellent durability and manifesting suppressed yellowing of transmitted light. Further, a laminated plate obtained using this resin composition is suitably used as a lighting cover, light diffusing plate for liquid crystal displays, illumination sign board or the like for which light transmittance and light diffusing property are required and durability is desired.

Abstract: A coated transfer sheet comprising a substrate having a first and second surface; optionally at least one barrier layer overlaying said first surface, at least one release layer overlaying said at least one barrier layer or, when the barrier layer is not present, said first surface of the substrate; and an optional image receiving layer comprising an ethylene acrylic acid co-polymer dispersion; wherein the coated transfer sheet exhibits cold peel and hot peel properties when transferred, and may be used in electrostatic printers and copiers or other devices in which toner particles are imagewise applied to a substrate. The addition of elastomeric polymers and polyurethanes help provide enhanced wash stability and chemical stability.