Abstract: The present invention relates to a method of treating anti-bacterial infections which method comprises the separate, simultaneous or sequential administration to a patient in need thereof, of an effective amount of gemifloxacin or a salt thereof and a ?-lactam antibiotic.

Abstract: A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.

Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia–If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Polyarylcarboxamide compounds of formula I) are useful as lipid lowering agents.

Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.

Abstract: The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole·n?H2O (wherein n? is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-benzimidazole·nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.

Abstract: Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0–10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: The present invention provides novel N-substituted fluorooxindoles having the general Formula I wherein the wavy bond represents the racemate, the (R)-enantiomer or the (S)-enantiomer and m, n, p, q, A, B, D, Q, X, and Z are as defined below, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R?3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R?10 is alkyl, X is sulphur, oxygen, NR10, or N+(R?10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.

Abstract: Captopril nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment or prophylaxis of cardiovascular, inflammatory and renal diseases.

Abstract: Compounds which are 1-(2?-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1–C6alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2–5, b is 1–4, c is 1–2, d is 1–2, e is 1–3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1–C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2–4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p— where p is 3 or 4; R3 is selected from H, C1–C6 alkyl and phenyl; R4 is selected from H, C1–C6 alkyl, benzy

Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein the dashed line represents the presence or absence of a double bond; J is C?O or CHOH; A is —(CH2)6—, or cis —CH2CH?CH—(CH2)3—, wherein 1 or 2 carbons may be substituted with S or O; B is CO2H, or CO2R, CONR2, CONHCH2CH2OH, CON(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl; D is —(CH2)n—, —X(CH2)n, or —(CH2)nX—, wherein n is from 0 to 3 and X is S or O; and E is an aromatic or heteroaromatic moiety having from 0 to 4 substituents, said substituents each comprising from 1 to 6 non-hydrogen atoms is disclosed herein. Methods, compositions, and medicaments related thereto, as well as experimental results showing prostaglandin EP4 selective agonist activity for certain compounds disclosed herein, are also disclosed.

Abstract: Formula (I) compounds are described, where the groups are defined in the description, as well as processes for their preparation and their use as medicaments, particularly as selective phosphodiesterase IV inhibitors.

Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.

Abstract: The present invention releates to certain novel guanidine or amidine acid derivatives and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to a composition for topical use for treating and improving the aesthetic conditions of the skin, which comprises, as an active ingredient, a mixture of ethyllinoleate and triethylcitrate. This composition is active in the treatment of seborrhea and acne.

Abstract: Injectable compositions containing gabapentin and processes for preparing sterile injectable compositions containing gabapentin are discussed. The process includes subjecting the compositions to heat. Heating results in increased production of gabapentin lactam, which has previously been shown to be toxic. Surprisingly, heated injectable compositions containing gabapentin are found to be non-toxic when administered intrathecally. Thus, heating for the purposes of sterilization or to assure sterility provides a viable option in the production of injectable compositions containing gabapentin.

Abstract: A drug based on a metabolite of fenretinide, or N-(4hydroxyphenyl) retinamide (4-HPR), specifically 4-oxo-N-(4-hydroxyphenyl) retinamide (4-oxo-4-HPR), is used in the treatment of different kinds of tumors, in particular in the treatment of ovarian carcinoma, breast tumor and neuroblastoma. The drug is more potent than fenretinide alone, and enhances the effects of fenretinide when administered together with fenretinide.

Abstract: Transport reagents and conjugates of therapeutic agents linked to transport reagents are described. In particular, the transport reagents have a plurality of guanidinium moieties that are either contiguous or spaced along a backbone, but are sufficiently removed from the backbone via tethers, to allow their interaction with a cell or tissue surface, leading to uptake of the therapeutic agent.

Abstract: 1-(3-methoxybenzyl)-3-substituted thiourea antioxidant compounds and improved lipids compositions which are supplemented with amounts of such antioxidant compounds effective for augmenting oxidative stability of the base lipid are provided. Also provided are methods for enhancing the oxidative stability of a lipid comprising supplementing a base lipid in need of enhanced oxidative stability with at least one 1-(3-methoxybenzyl)-3-substituted thiourea compound of the present invention.

Abstract: Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.

Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.

Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.

Abstract: A pharmaceutical composition for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent capable of dispersing or solubilizing the retinide. The solvent comprises an alcohol, such as ethanol, in combination with an alkoxylated castor oil, such as CREMOPHOR® EL, or comprising a retinide, such as fenretinide, in an emulsion composed of a lipoid dispersed in an aqueous phase, a stabilizing amount of a non-ionic surfactant, optionally a solvent, and optionally an isotonic agent. In addition, a method of use in the treatment of hyperproliferative disorders, such as cancers is described.

Abstract: The invention concerns a colloidal dispersion of a phosphate of a rare earth and a process for its preparation. The dispersion is characterized in that it comprises anisotropic and disaggregated or disaggregatable particles of a phosphate of at least one rare earth and an anion of a monobasic acid, soluble in water and with a pKa of at least 2.5. It is prepared by a process in which a solution of a salt of at least one rare earth is mixed with phosphate ions while controlling the pH of the reaction medium to a value in the range 4 to 9 and in the presence of a monobasic acid, soluble in water and with a pKa of at least 2.5; the mixture obtained optionally undergoes a maturing step; the precipitate is then separated from the reaction medium; and said precipitate is then dispersed in water.

Abstract: The present invention relates to a process and apparatus for processing agricultural waste to make alcohol and/or biodiesel. The agricultural wastes are subjected to anaerobic digestion which produces a biogas stream containing methane, which is subsequently reformed to a syngas containing carbon monoxide and hydrogen. The syngas is converted to an alcohol which may be stored, sold, used, or fed directly to a reactor for production of biodiesel. The solids effluent from the anaerobic digester can be further utilized as slow release, organic certified fertilizer. Additionally, the wastewater from the process is acceptable for immediate reuse in agricultural operations.

Abstract: A polymeric actuator of simple structure, capable of being easily miniaturized, showing quick response and capable of generating large displacement. The polymeric actuator includes an ion-exchange resin product and metal electrodes. The ion-exchange resin product contains an alkylammonium. The metal electrodes are formed on the surface of the ion-exchange resin product and are insulated from each other. The polymeric actuator operates as an actuator by applying a potential difference between the metal electrodes when the ion-exchange resin product is in water-containing state to allow the ion-exchange resin product to undergo bending or deformation.

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 a tertiary amine amide catalyst composition represented by formula (I): wherein A, R1–R6, and n are defined herein and wherein the tertiary amino amide catalyst of formula I is acid-blocked.

Abstract: Process for preparing flexible polyurethane foam by reacting an MDI-based polyisocyanate and a polyether polyol with a high oxyethylene content in a mold.

Abstract: Self-photoinitiating liquid oligomeric compositions are disclosed. The oligomeric compositions are formed from multifunctional mercaptans and Michael addition polyacrylate resins, synthesized from multifunctional acrylates and ?-dicarbonyl Michael donors, specifically ?-keto esters, ?-diketones, ?-ketoamides or ?-ketoanilides or combinations thereof The oligomeric compositions are provided along with uses thereof and methods of fabricating.

Abstract: Optical fiber coating compositions which comprise at least one ethylenically unsaturated polymerizable compound and a photoinitiator blend, wherein the blend comprises (a) bis(2,4,6-trimethylbenzoyl)phenylphosphine oxide and (b) 2,4,6,-trimethylbenzoylethoxyphenylphosphine oxide in an (a):(b) weight:weight ratio of between about 1:10 and about 1:8; or (c) bis(2,4,6-trimethylbenzoyl)phenylphosphine oxide, (d) 2,4,6,-trimethylbenzoylethoxyphenylphosphine oxide and (e) 2-hydroxy-2-methyl-1-phenyl-1-propanone in a (c):(d):(e) weight:weight:weight ratio between about 3:1:14 and about 4:1:16; or (f) bis(2,4,6-trimethylbenzoyl)phenylphosphine oxide and (g) 2-hydroxy-2-methyl-1-phenyl-1-propanone in a (f):(g) weight:weight ratio of between about 1:3 and about 1:5 exhibit fast photospeed, very low color and fast photobleaching. The photoinitiator blends have low volatility, high shelf life stability and high compatibility with resins and monomers. The photoinitiator blends are for example liquid and easy to use.

Abstract: A process for producing polypropylene having increased melt strength, the process comprising irradiating polypropylene which has been polymerised using a Ziegler-Natta catalyst with an electron beam having an energy of at least 5 MeV and a radiation dose of at least 10 kGray and mechanically processing the irradiated polypropylene to form long chain branches on the polypropylene molecules, whereby the polypropylene has a melt flow index (MFI) of at least 25 dg/min.

Abstract: The invention relates to a method of manufacturing a replica, which method comprises the provision of a polymerizable resin composition between a front mold having a pre-shaped surface and a back mold having a pre-shaped surface, carrying out a curing treatment and removing the replica thus manufactured from the molds. The invention further relates to a replica obtained by carrying out a UV light-initiated cationic polymerization.

Abstract: The present invention provides (meth)acrylate compounds bearing a specific maleimide group and resin compositions containing said compounds that can be cured by irradiation of light in a practical dose even when a photoinitiator is not used or used in a smaller amount than that of the prior art, and cured articles of the resin compositions.

Abstract: A tire sealant composition for use in pneumatic tires is provided. The tire sealant composition primarily serves to seal the tire around the wheel rim and particularly in the tread area of the tire against punctures. The composition includes a naturally derived viscous carrier fluid and at least one fibrous material, polymeric material or combination of both, wherein the composition remains fluid in use. The naturally derived viscous carrier fluid is preferably desugared molasses (less than 30% by weight sucrose) and is able to sustain a temperature of ?30° F. (?34.4° C. and below) without freezing. The tire sealant composition is fire-retardant, non-toxic, non-corrosive and non-abrasive and is environmentally friendly.

Abstract: The invention relates to a pavement marking composition comprising ceramic fibers. The ceramic fibers are preferably randomly dispersed within a polymeric material. The polymeric material preferably comprises a substantially non-crosslinked elastomer. The pavement marking composition is preferably formed into a sheet material such as a tape.

Abstract: Surface-modified nanoparticles whose surface is covered completely or near-completely with (A) modifying groups which are attached covalently to the surface via linking functional groups (a) and contain inert spacer groups (b) and contain reactive functional groups (c) which are connected via the groups (b) to the groups (a) and are inert toward the reactive functional groups of the surface to be modified, (B) modifying groups which are attached covalently to the surface via linking functional groups (a) and contain inert groups (d) having a smaller hydrodynamic volume VH than the inert spacer groups (Ab), and (C) modifying groups which are attached to the surface via linking functional groups (a) which contain at least one silicon atom, contain inert groups (e), and have a smaller hydrodynamic volume VH than the modifying groups (A); dispersions comprising the nanoparticles, processes for preparing them, and their use.

Abstract: A liquid epoxy resin composition comprising (A) a liquid epoxy resin, (B) an aromatic amine curing agent comprising 5–100% by weight of a specific aromatic amine compound having a purity of at least 99%, (C) an inorganic filler, and (D) an ester organic solvent having a boiling point of 130–250° C. is useful for semiconductor encapsulation. The composition has an infiltration ability, adhesion to silicon chips, resistance to deterioration under hot humid conditions, and resistance to thermal shocks.

Abstract: A composition containing transparent thermoplastic polymers and a surface modified oxide particles is disclosed. The size of the particles is less than 200 nm and the composition is suitable for the preparation of products wherever diathermancy is undesirable.

Abstract: A stabilizer mixture containing (A) a sterically hindered amine compound, and (B) two different compounds selected from the group consisting of an organic salt of Zn, an inorganic salt of Zn, an organic salt of Mg and an inorganic salt of Mg; the weight ratio of the two different compounds being 1:10 to 10:1; with the provisos that (1) the stabilizer mixture is essentially free of perchloric acid, and (2) the two compounds in component (B) are different from the combination ZnO and Zn stearate and the combination ZnO and hydrotalcite; is useful for stabilizing an organic material, in particular a polyolefin, against degradation induced by light, heat or oxidation.

Abstract: A flame retardant comprising a phosphazene compound, a polyphenylene oxide-series resin, and if necessary a styrenic resin and/or a nitrogen-containing compound imparts flame retardancy to a polyalkylene arylate-series resin. The phosphazene compound comprises at least a crosslinked phenoxyphosphazene compound. The obtained polyalkylene arylate-series resin composition shows high flame-retardancy.

Abstract: A flame retardant resin composition comprising: (A) 100 parts by weight of a resin component (component a) containing at least 50% by weight of a high impact polystyrene, and (B) 1 to 50 parts by weight of a phosphorous-containing compound (component b) represented by the following general formula (I): wherein A and A? are the same or different and represent —OR or -Q wherein R and Q represent an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 5 to 10 carbon atoms, an aralkyl group having 7 to 20 carbon atoms or an aryl group having 6 to 15 carbon atoms. According to the present invention, there are provided a polystyrene resin composition containing substantially no halogen and having heat resistance, particularly a high heat distortion temperature under load, and an article from the composition.

Abstract: The invention relates to thermoplastic moulding materials containing A) between 20 and 97 wt. % of a thermoplastic polyester; B) between 1 and 40 wt. % of a phosphinic acid salt and/or a diphosphinic acid salt and/or the polymers thereof, constituent B) having an average particle size (value d50) which is smaller than 10 ?m; C) between 1 and 30 wt. % of a nitrogenated flameproofing agent; D) between 0 and 5 wt. % of at least one ester or amide of saturated or unsaturated aliphatic carboxylic acids having between 10 and 40 C atoms and aliphatic saturated alcohols or amines having between 2 and 40 C atoms; and E) between 0 and 60 wt. % of other additives. The total weight percent of constituents A) to E) amounts to 100%.

Abstract: An acrylic rubber composition in which the base material is an acrylic rubber comprising monomer units of ethyl acrylate, n-butyl acrylate, and cure site monomer, with a ratio (B/A) of the amount of n-butyl acrylate (B) with respect to ethyl acrylate (A) of 1.0 or less by weight. A heat-resistant hose having a layer of this acrylic rubber composition as the innermost layer. The above constitution of the invention provides the acrylic rubber composition effective for preventing aluminum fixing while retaining the material properties of acrylic rubber and its excellent characteristics. The present invention also provides a heat-resistant hose using this acrylic rubber composition at the surface which is to be fitted with an aluminum member.

Abstract: In a process for the manufacture of aqueous floor covering adhesives without the addition of solvents, high-boiling solvents, or plasticizers and with the use of a non-carboxylated styrene/butadiene (SBR) dispersion and of an agent providing initial adhesion, a melt of the agent providing initial adhesion, for example a resin with a melting point of 45 to 98° C., is added to the SBR dispersion under high shear forces for the purpose of obtaining a durably stable emulsion which provides not only high initial adhesion, but also high final strength.

Abstract: A curable aqueous polyurethane dispersion substantially comprises a) at least one compound having two free isocyanate groups, at least one allophanate group and at least one C?C double bond capable of free radical polymerization, a carbonyl group or an oxygen atom in the form of an ether function being bonded directly to the double bond, b) at least one compound having at least one group reactive toward isocyanate groups and having a C?C double bond capable of free-radical polymerization, c) if required, at least one compound having at least two groups reactive towards isocyanate groups and selected from hydroxyl, mercapto, primary and/or secondary amino groups, d) at least one compound having at least one group reactive towards isocyanate groups and having at least one acid group, e) at least one basic compound for neutralizing or partially neutralizing the acid groups of the compounds d), and a thermal initiator and is used for coating substrates.