Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.

Abstract: Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide, ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, C(1-6)alkyloxy, cyano, (C?O)R25, (C—O)OR16,

Abstract: The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo [b][1,4]diazepines of formula I wherein R1, R2, R3 and R4 are as defined in the description and claims, which are ?-secretase inhibitors and which may be useful in the treatment of Alzheimer's disease.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.

Abstract: Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

Abstract: There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS.

Abstract: Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein X, Y, Z and R1 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.

Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

Abstract: Triazaspiro Compounds, compositions comprising a Triazaspiro Compound, methods for treating or preventing pain in an animal comprising administering to an animal in need thereof an effective amount of a Triazaspiro Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a Triazaspiro Compound are disclosed.

Abstract: The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.

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: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.

Abstract: The present invention provides to a novel compound having an ACAT inhibiting activity.

Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Abstract: The present invention relates to benzopyran derivatives substituted with secondary amines including tetrazole, method for preparing thereof and pharmaceutical compositions containing them. The compounds of the present invention can be used for protecting neuronal cells and brain damage; antioxidation; inhibiting NO generation; protecting heart; suppressing angiogenesis; protecting preserving organs such as kidney, heart and tissue, and protecting organs in major cardiovascular surgery.

Abstract: Three new alkaloids, Hirsutellones A, B, and C, are produced in cultures of fungus such as Hirsutella nivea strain BCC 2594 and Trichoderma sp. strain BCC 7579. The Hirsutellones exhibited potent growth inhibitory activity against Mycobacterium tuberculosis (H37Ra strain) with an MIC value of 0.78 ?g/ml, while showing weak or no cytotoxicity to mammalian cells. Therefore, Hirsutellones and pharmaceutical compositions containing Hirsutellones may be useful for the treatment of tuberculosis. Also described herein are methods of isolating the Hirsutellones.

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.

Abstract: The present invention provides a method of treating hypertension, liver failure, loss of patency of ductus arteriosus, glaucoma or ocular hypertension in a patient, comprising administering to the patient a therapeutically effective amount of a selective EP4 receptor agonist of Formula I or a prodrug thereof, a pharmaceutically acceptable salt of the selective EP4 receptor agonist or prodrug or a stereoisomer or diastereomeric mixture of the EP4 receptor agonist, prodrug or salt, wherein the variables X, Z, Q, , and R2 are as defined in the specification.

Abstract: There is provided a 5-thio-?-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.

Abstract: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a link, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.

Abstract: Lactones of Formula (I) which are pharmaceutically active in diseases associated with inflammation

Abstract: A composition for lowering internal lipid in a subject which contains a capsinoid substance represented by the following formula wherein n is an integer from 0 to 10. Methods of using the compositions are disclosed and include administering to a subject in need of such treatment.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: Methods are provided for promoting longevity and decreasing the incidence of ageing associated pathologies (e.g. cancer) by the administration of one or more of the following LFFA: linoleic, oleic, and palmitic acid. Secondary LFFA derived from this set, as well as their CoA derivatives and synthetic analogs, are effective also in promoting longevity and delaying the onset of age associated disorders. In addition, interventions including LFFA and CoA LFFA formulations are described which protect the organism from acute physical stress, tissue damage, and hypoxia, either due to trauma or secondary to surgical procedures.

Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.

Abstract: Acyclic compounds containing an ether functionality external to the ring can be used as rhinologically active substances. In the regions of the mouth, the throat and the airways they produce a refreshing and clearing feeling.

Abstract: The polishing pad is suitable for planarizing at least one of semiconductor, optical and magnetic substrates. The polishing pad includes a cast polyurethane polymeric material formed with an isocyanate-terminated reaction product formed from a prepolymer reaction of a prepolymer polyol and a polyfunctional isocyanate. The isocyanate-terminated section product has 4.5 to 8.7 weight percent unreacted NCO; and the isocyanate-terminated reaction product is cured with a curative agent selected from the group comprising curative polyamines, curative polyols, curative alcoholamines and mixtures thereof. The polishing pad contains at least 0.1 volume percent filler or porosity.

Abstract: Radiation-curable compositions, and methods of making the same, for providing a wide variety of substrates with a durable, colored coating or colorant are disclosed. The color is at least in part provided by chromophore molecules that are covalently bonded to other components within the radiation-curable composition. A telecommunication element having a durable color identifying polymeric coating thereon is also disclosed. The telecommunication element comprises an elongated communication transmission medium, such as an optical fiber or an optical fiber ribbon, and a radiation-cured polymeric coating having an identifying color applied on at least a portion of the transmission medium.

Abstract: The present invention relates to a recording liquid comprising at least: a pigment (a); and a polymer (b) having one or more types of bond selected from the group consisting of amide bond, urethane bond and urea bond in the molecule, having a weight-average molecular weight of 5000 to 300000 and having an acid value of free acid of not less than 55 mgKOH/g and less than 150 mgKOH/g, the surface tension of said recording liquid being 25 to 54 dyne/cm.

Abstract: An ink for ink-jet recording contains tripropylene glycol normal butyl ether or dipropylene glycol normal propyl ether, an acrylic polymer, a water-insoluble coloring agent, and water. The ink simultaneously satisfies the straight travel stability of ink droplets during the discharge with an ink-jet recording apparatus, the recovery performance upon introduction into a recording head of the ink-jet recording apparatus, the fixation performance of printed matters, and the drying performance after the printing.

Abstract: A composition which can improve impact resistance of a coating film while maintaining superior weather resistance and gloss of the coating film of a fluororesin powder coating material is provided. A fluororesin powder coating composition containing the following particles (C) in an amount of from 0.1 to 10 parts by mass per 100 parts by mass of a fluororesin. The particles (C) are particles having a core/shell structure and having an average particle size of from 0.01 to 2.5 ?m, wherein the core and/or at least one shell comprises a fluorinated polymer.

Abstract: A coating for wall construction is provided whereby a level 5 finish may be obtained without the need for a finishing coat or final skim coat. The coating may be applied to drywall elements prior to installation and is compatible with jointing materials such that a substantially homogeneous surface may be obtained after the drywall elements are assembled with jointing material and the jointing material is dried. The coating formulation includes a noncellulosic thickener, a binder, a mineral filler and water. A method for the construction of interior walls and a construction assembly for interior walls is further provided.

Abstract: RTV organopolysiloxane compositions comprising (A) a diorganopolysiloxane having hydroxyl or alkoxysilyl groups at both ends, (B) a polyoxypropylene-modified silicone, (C) wet silica, and (D) a silane or siloxane having at least three silicon-bonded hydrolyzable groups have improved sag control and cure at room temperature into products with improved rubber physical properties and durability.

Abstract: The present invention provides a rubber composition, in which reversion when vulcanizing at a high temperature is inhibited without losing rubber properties and which is obtained by efficiently crosslinking with sulfur, and a pneumatic tire using the rubber composition. Specifically, the present invention relates to a rubber composition comprises a rubber component containing diene rubber and fluorinated graphite and a pneumatic tire using the rubber composition. The rubber composition preferably contains 0.1 to 50 parts by weight of fluorinated graphite based on 100 parts by weight of the rubber component containing diene rubber.

Abstract: A method comprising forming and grafting polymers on carbon nanotubes, a functionalized product and product dispersion produced by the method, a method of forming composites from the functionalized carbon nanotubes, and the composites produced therefrom.

Abstract: The present invention is related to methods and compositions for marking and removing turf lines and other markings from artificial and natural turf, including sports fields. The marking compositions include alkali-activatible acrylics, including one or both of alkali-soluble resin and an alkali-swellable thickener to enable removing the dried composition with an alkaline solution.

Abstract: A process for making an insulating glass assembly is disclosed, the process including applying a sealant composition to a surface of a spacer; contacting the sealant composition with a glass pane, and applying pressure on the glass pane to bond the glass pane to the spacer through the sealant composition, the pressure being applied at an ambient temperature of from about 15° C. to about 60° C.

Abstract: A two-component bonding agent composition of an aqueous component having a polyol and an acrylic-styrene polymer, and an isocyanate component having a water dispersible polyisocyanate.

Abstract: Stabilized polyurethane resins and methods for their preparation are disclosed.

Abstract: A second order modified block copolymer which can be obtained by reacting a first order modified block copolymer with a second order modifier, wherein the first order modified block copolymer comprises a base block copolymer and a functional group-containing first order modifier group bonded to the base block co-polymer, wherein the base block copolymer comprises at least one polymer block comprised mainly of vinyl aromatic hydrocarbon monomer units and at least one polymer block comprised mainly of conjugated diene monomer units, and wherein the second order modifier has a specific functional group which is reactive to the functional group of the first order modifier group of the first order modified block copolymer. A second order modified block copolymer containing polymer composition comprising the second order modified block copolymer as well as a thermoplastic resin and/or a rubbery polymer.

Abstract: A rubber composition for an inner liner improving air retention property of a tire, lowering hysteresis loss and further preventing crack growth is provided. A rubber composition for an inner liner comprising 10 to 50 parts by weight of mica having an aspect ratio of at least 50 and an average particle diameter of 40 to 100 ?m, based on 100 parts by weight of a rubber component comprising 30 to 60% by weight of butyl base rubber, 20 to 50% by weight of natural rubber or isoprene rubber and 10 to 40% by weight of butadiene rubber.

Abstract: A solution process for polymerizing one or more ?-olefins of the formula CH2?CHR, where R is H or an alkyl radical C1-C18, to produce a polymer that is soluble in the reaction medium, comprising the steps of: continuously polymerizing in a liquid phase the ?-olefin in the presence of a catalyst system based on a transition metal compound to obtain a solution of polymer in the reaction medium; the polymeric solution obtained from step a) is then mixed in one or more mixing stages with an aqueous mixture comprising one or more organic compounds having at least a hydroxy or epoxy group, said aqueous mixture having a dynamic viscosity at 30° C. higher than 50 cP (centiPoise).