Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.

Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.

Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS. 2 and 4, respectively, and are represented by the formula: Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

Abstract: A compound of the formula wherein R1, R2 and R3 are as defined above, useful as inhibitors of protein kinases, such as the enzyme Janus Kinase 3.

Abstract: The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like] or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.

Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and

Abstract: A pharmaceutical composition comprising an analgesic or analgesic combination and a stool softener is disclosed. The analgesic is selected from morphine, meperidine, fentanyl, hydromorphone, oxymorphone, oxycodone, hydrocodone, methadone, propoxyphene, pentazocine, levorphanol, codeine, acetaminophen and combinations of these analgesics. The composition is formulated for oral administration as a liquid or solid dosage form for immediate, slow, delayed or sustained-release characteristics.

Abstract: The invention relates to new pyridylalkane, alkene, and alkine carboxamides substituted with an imide with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to general formula (I), wherein the residue E is a cyclic imide, methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors, inhibition of abnormal cell growth and control of immune reactions, for example autoimmune diseases.

Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

Abstract: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X? signifies an anion].

Abstract: Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification.

Abstract: Hetero-tetrahydroquinolines can be prepared either by condensing correspondingly substituted hetero-tetrahydroquinoline aldehydes with the desired substituent or by reducing the corresponding keto-substituted hetero-tetrahydroquinolines, followed by introduction of the desired substituent by customary methods. The hetero-tetrahydroquinolines are suitable for use as active compounds in medicaments, in particular in medicaments for treating artheriosclerosis and dyslipidaemias.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1–R7, X1, X2, R, Q, and n are as defined herein.

Abstract: Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal)

Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, (I) R1a is NH(C?W)R5 or (a); W is O or S; R2 and R3 are for example H or F; R1 is for example hydrogen, or halogen; R5 is selected from hydrogen, (2–6C)alkyl (optionally substituted); R6 and R7 are independently selected from hydrogen, and (1–4C)alkyl (optionally substituted); wherein R4 is either a hydroxymethyl substituent on C-4? of the isoxazoline ring; or R4 is a hydroxymethyl substituent on C-5? of the isoxazoline ring and the stereochemistry at C-5? of the isoxazoline ring and at C-5 of the oxazolidinone ring is selected, such that the compound of formula (I) is a single diastereomer; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described

Abstract: Compounds of the formula wherein the substituents are as defined in the specification which are useful for the treatment of pain.

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors.

Abstract: New pyrrolidinium derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.

Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: According to the invention, there is provided a novel 3,4-dihydroxyhydrocinnamic acid derivative, designated DHH105, having blood glucose lowering effects in vivo as a result of the enhancement of glucose transport mediated by the increase of insulin receptor signaling. This invention thus relates to a 3,4-dihydroxyhydrocinnamic acid derivative useful as an anti-diabetic agent, represented by the following formula I: or pharmaceutically acceptable salts thereof, to a method for preparing the compound, and to a composition for treating diabetes comprising the same as an active ingredient.

Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.

Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.

Abstract: The present invention relates to improved methods for filling the skin for cosmetic or medical purposes. Compositions comprising carboxymethyl cellulose (CMC), polyethylene oxide (PEO) and calcium ions can be made and have physical properties that depend on the amounts and types of CMC, PEO, and calcium ions to form ioniclaly cross-linked gels. Compositions can be formed into microspheres, coascervates, gels, or membranes. Gels, microspheres and coascervates can be injected directly into a site for dermal filling. Membranes can be surgically introduced, where they swell to form hydrated gels. After introduction, the dermal filler persists for a period of time and then can disintegrate and be removed from the body.

Abstract: A more controllable acoustic ceiling patch or textured material in the form of a sprayable composition includes a base, a filler, an adhesive binder, an anti-foaming agent, a suspension agent, and rubber particulates or polyethylene particulates forming an aggregate suitable for spraying in the presence of volatile organic compound (VOC) propellants without melting or deterioration. The more controllable acoustic ceiling patch is storable and dispensable from a pressurized dispenser having a delivery nozzle. An aerosol system with a spray nozzle is included on the container for selective discharge of the textured material onto a prepared patch area, which may be on a drywall or support panel so as to match and blend with the surrounding acoustic ceiling surface area in order to provide a continuous and unbroken coextensive surface texture of mechanically and visually matched material.

Abstract: An inorganic compound sol comprises a dispersion medium and, dispersed therein, inorganic compound particulates whose surface has been modified by an organic compound exhibiting a molecular polarizability of from 2×10?40 to 850×10?40C2m2J?2. The inorganic compound sol modified by an organic compound possesses a desirable affinity with the dispersion media, providing excellent dispersion stability in solvents while avoiding aggregation of particulates.

Abstract: This invention is directed to processes (i.e., methods) for making methanol compositions, and to processes (i.e., methods) of using the methanol compositions. The methanol compositions contain ethanol and are particularly suitable for contacting with an olefin forming catalyst to form an olefin stream.

Abstract: The present invention is a process for recycling colored polyester. More specifically, colored polyester for recycling is depolymerized by the addition of glycol to form the monomer BHET. The BHET is contacted with activated carbon to remove some colorant. The remaining colorant is extracted with water, alcohol, or glycol to produce white, purified BHET. The white, purified BHET is separated from the extraction solvent (water, alcohol, or glycol) by filtering, decanting, or centrifuging, for example. The purified BHET monomer can be polymerized to polyethylene terephthalate meeting food contact specifications, using known polymerization processes.

Abstract: The present invention relates to a method of preparing expanded thermoplastic microspheres, comprising charging thermally expandable microspheres into an expansion device comprising rotating feeding means enveloped by a hollow body, and one or more scrapers. The invention further relates to an expansion device for expanding thermoplastic microspheres.

Abstract: The present invention relates to a method for preparing a polyurethane foam, which comprises reacting an organic polyisocyanate and a polyol in the presence of water as a blowing agent, a cell stabilizer, and an acid-blocked tertiary amino alkyl amide catalyst composition. The catalyst composition is represented by the formula I: wherein R1, R2, R3, R4, R5, R6, A, and n are as defined herein and wherein the tertiary amino alkyl amide catalyst of formula I is acid-blocked.

Abstract: A cationically curable composition comprises (a) at least one cationically curable species; (b) at least one cationic photoinitiator; and (c) at least one encapsulated, polymer-bound base.

Abstract: Disclosed are environmentally friendly, substantially all solids coating compositions which are curable using ultraviolet and visible radiation. In addition, the disclosed coating compositions are suitable for coating thermally sensitive objects and/or rusted surfaces. In addition, methods are disclosed for coating surfaces, or at least a portion of the surfaces, and curing of the coated surface to obtain partially or fully cured coated surfaces are also disclosed. Furthermore, articles of manufacture incorporating fully cured coated surfaces are disclosed, including, for example gas tanks such as, barbeque propane tanks. Also disclosed are methods, processes, production lines, articles of manufacture, and factories which incorporate these environmentally friendly, substantially all solids coating compositions curable using ultraviolet and visible radiation.

Abstract: A liquid self-healing coating, incorporating microcapsules filled with tailored repair formulations, repairs itself upon physical compromise after curing. In one embodiment, a commercially available paint primer is mixed with a pre-specified amount of these microcapsules. After the coating has cured on the substrate to which it is applied, any physical compromise of the cured coating results in the microcapsules bursting to release a liquid that fills and seals the compromised volume of the coating. In applications where paint is used to provide corrosion protection, the liquid contains anti-corrosion material as well as suitable diluents and film-forming compounds. In another embodiment, the microcapsules may be provided separately to enhance commercially available products.

Abstract: Disclosed is a method of producing a powdery coating material by using: a curable polyester resin (A) having a hydroxyl group and/or a carboxyl group at the terminals thereof, and further having a number average molecular weight of from 1,000 to 30,000, a glass transition temperature of from 30 to 100° C.; a curing agent (B) which is solid at normal temperature and is capable of being reacted with the hydroxyl group or the carboxyl group of the curable polyester resin (A); and a solvent (C) having a boiling point under normal pressure of from 50 to 130° C.; and comprising a step of kneading the curable polyester resin (A), the curing agent (B) and the solvent (C) under condition in which at 50 to 130° C., not less than 20% by weight of the curing agent (B) is dissolved in the solvent and, then, vapor-removing the solvent (C) under a reduced pressure.

Abstract: Elastomeric polymers are combined with chemical agents in the presence of supercritical fluids such as supercritical carbon dioxide by swelling the polymer with the supercritical fluid, and impregnating the swollen polymer with the chemical agent. The process can be conducted at relatively low temperatures and pressures such that degradation of the polymer or the chemical agent is avoided. The chemical agent is preferably a curing agent which includes functional groups that interact with functional groups on the polymer to create an association therebetween. The process is enhanced by pre-dissolving the chemical agent in a solvent which does not solubilize the polymer to a great extent, but which is itself soluble in the supercritical fluid. In addition, during combining, mechanical mastication is performed to create a free flowing powder.

Abstract: A method and apparatus for manufacturing small batches of solid paint is disclosed, which method includes a first step of providing a component of the solid paint as a liquid in a heated mixing container that has a base and sides and includes a stirrer for stirring the contents of the container. The next step of the method includes controlling, heating and stirring of the contents of the container and progressively adding other components of the solid paint as solids to the container. The liquid acts as a heat transfer medium that transfers heat from the heated container and from the stirrer to the solids. The mix is heated to a temperature of the solid paint and forms a melt that is a uniform liquid. The final step in the method includes discharging the melt from the container and allowing the melt to cool and form the solid paint.

Abstract: A composition for use in making an encapsulant usable in the encapsulation of a semiconductor chip assembled to a substrate with C4 solder interconnections therebetween, which in turn may form part of an electronic package. The composition comprises a resin, a flexibilizing agent and a filler material.

Abstract: A process for producing olefin polymers, which comprises the steps of polymerizing an olefin monomer in a polymerization zone in the presence of a catalyst comprising a transition metal compound to form an olefin polymer, and adding at the end of or downstream from the polymerization zone a composition having a weight averaged molecular weight of at least 100 and containing a group R, a cation Y, an anionic group —C(R1)2—X?, and optionally a group —C(R1)2—X—H, the composition having a relative the composition having a relative mole fraction n of cations Y and a relative mole fraction m of group —C(R1)2—X—H, wherein 0<n?1, 0??m<1, and n+m=1. Use of such m=1. Use of such a composition for rendering inert undesired quantities of acidic compounds or halogen-containing compounds present in an olefin polymer by mixing the olefin polymer intimately with the additive composition.

Abstract: New compositions for use as high refractive index layers are provided. The compositions comprise a polyimide dispersed or dissolved in a solvent system. The polyimide can be prepared from commercially available dianhydrides and diamines. Preferred polymer include recurring monomers selected from the group consisting of The inventive compositions can form strong, thin films and have high refractive indices making them useful in a wide range of optical applications.

Abstract: A golf ball comprising a core and a cover is disclosed. At least a layer of the golf ball is made from an elastomer composition comprising a least one polydiene rubber and at least one moisture scavenger, such as p-toluene sulfonyl isocyanate. The moisture scavenger is generally present in the elastomer composition in an amount of 10 phr or less, and particularly from 0.1 to 5 phr, by weight of the elastomer.

Abstract: A method of producing mass colored beer bottles comprising dyeing mass colored polyester with a dye of formula (1) wherein R1 is a radical of formula or of formula wherein R2 is hydrogen or C1–C4 and R3 is hydrogen or C1–C4alkyl, and a UV absorber.

Abstract: Adherent gels and adherent gel composites which can be made by applying an adherent gel onto one or more selected substrates of foam, plastic, fabric, metal, concrete, wood, wire screen, refractory material, glass, synthetic resin, synthetic fibers, and the like. Such adherent gels and gel composites are useful for protecting articles, the body and skin.

Abstract: A copolymer of a strait chain ?-olefin and a vinyl compound (I) represented by the general formula CH2?CH—R, wherein R is a hydrocarbon group, the steric parameter Es of the substituent R is ?1.64 or less and the steric parameter B1 of the substituent R is 1.53 or more, an adhesive containing the same as an effective ingredient, and an laminate containing the adhesive.

Abstract: There is disclosed a pneumatic tire having a component comprising a vulcanizable rubber composition comprising, based on 100 parts by weight of elastomer (phr), from about 40 to about 90 phr of a solution polymerized styrene-butadiene having a styrene content of greater than 38 percent by weight; from about 10 to about 60 phr of at least one additional elastomer; and from about 10 to about 70 phr of a process oil having a glass transition temperature of from about ?80° C. to about ?40° C. and a polycyclic aromatic content of less than 3 percent by weight as determined by the IP346 method.

Abstract: Aqueous polymer dispersions comprising a) 50–70% by weight of polymer particles composed of at least two different (co)polymers having glass transition temperatures each above 50° C. and synthesized from at least 80% by weight of at least one principal monomer, 0.1–10% by weight of at least one auxiliary monomer, and 0–3% by weight of at least one crosslinker molecule, the difference in the glass transition temperatures (Tg) of the different polymers being at least 10° C., and b) 30–50% by weight of at least one polyfunctional (meth)acrylate, the dispersion a) being subjected to physical and/or chemical deodorization.

Abstract: There is disclosed a process for continuous production of a water-absorbent resin product by which the water-absorbent resin product having high properties can continuously be produced easily and inexpensively with stable constant quality. In addition, there is disclosed a water-absorbent resin product having high properties and being stable in quality.

Abstract: The invention relates to a gelable copolymer composition comprising a copolymer in a solvent. The copolymer has the structure A(B)n, wherein the core (A) is soluble in the solvent, the arms (B) are convertible between soluble and insoluble in the solent depending on an environmental condition, and n>1. The composition forms a gel under environmental conditions in which B is insoluble, through formation of B aggregates. Block copolymers comprising polyethylene glycol (PEG) and poly(N-iso-propylacrylamide) (PNIPAAm) having a liquid form at ambient temperature under aqueous conditions and a gel form at body temperature are disclosed.