Abstract: The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3? or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3? protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3? protein or GSK-3? protein complexes.

Abstract: The present invention is directed to compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes.

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: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.

Abstract: N,N?-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N?-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods of treatment.

Abstract: Novel compounds useful in the treatment of, prevention of or protection against diseases and/or conditions related to metabolic syndrome and lipid metabolism, especially diseases of fatty acid and cholesterol metabolism, such as those mediated by stearoyl-CoA desaturase, are disclosed along with methods of employing said compounds for such uses.

Abstract: Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2?, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2? are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.

Abstract: Methods are disclosed using trospium, an antimuscarinic smooth muscle relaxant, for the treatment of smooth muscle disorders, while avoiding the concomitant liability of adverse side effects associated with conventional antimuscarinic treatment.

Abstract: A method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, a vanilloid VR-1 antagonist or a pharmaceutically acceptable derivative thereof and an NSAID or a pharmaceutically acceptable derivative thereof, wherein said VR-1 antagonist or said NSAID may optionally be administered as a sub-maximal amount.

Abstract: The present invention relates to pyridoindolone derivatives substituted in the 3-position by a phenyl of general formula (I): to processes for preparing the same and to their use in therapeutics.

Abstract: The compounds of formula I in which R1, R2, R3 and A have the meanings as given in the description are novel effective INOS inhibitors.

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C?O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen.

Abstract: The present invention relates to the use of saredutant and of its pharmaceutically acceptable salts for the preparation of medicinal products that are useful in the treatment or prevention of all mood disorders, adaptation disorders or mixed anxiety-depression disorders.

Abstract: A method is provided for treating diabetes and related diseases, especially Type II diabetes, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract: Substituted oxazolidinone of the formula: wherein R2 is alkyl selected from the group consisting of methyl, ethyl, and isopropyl moieties, are described. The compounds are antibacterial.

Abstract: Cell motility and growth inhibitors, including compounds of the general structural formula and use of the cell motility and cell growth inhibitors, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, as therapeutic agents, are disclosed.

Abstract: A description is given of derivatives of benzoylpyrazoles of the formula (I) and of their use as herbicides. In this formula (I) R1a, R1b, R1c, R2, R3, R4 and R5 stand for various radicals, X for a bridging atom, L for a carbon chain and Y for a chalcogen atom.

Abstract: Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours

Abstract: A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: This invention provides remedies or prophylactics for diseases in association with chemokines such as MIP-1 ? and/or MCP-1. Namely, remedies or prophylactics for diseases in association with the chemokines such as rheumatoid arthritis or nephritis contain, as the active ingredient, cyclic amine derivatives represented by the following formula (I), pharmaceutically acceptable acid addition salts thereof or pharmaceutically acceptable C1-C6 alkyl addition salts thereof.

Abstract: The present invention is directed to tetracyclic steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.

Abstract: The present invention is related to a novel method for oxidizing or splitting nucleic acids at specific points on a complementary nucleic acid segment using a dinuclear copper-based compound of Formula I. Additionally, the present invention is related to a novel treatment of cancer, tumors, and cancer cells using a dinuclear copper-based compound of formula I or a naked ligand of Formula II.

Abstract: The present invention relates to methods of treating ADAMTS-5-associated diseases and particularly osteoarthritis comprising administering an agent capable of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in part, on the discovery that transgenic animals that do not express functional ADAMTS-5 show a reduction in the degree of osteoarthritis after the induction of osteoarthritis as compared to WT animals. Furthermore, the ADAMTS-5 transgenic animals have reduced aggrecanase activity in articular tissue as compared to WT animals. These animals are good models for ADAMTS-5-associated diseases, and for screening of drugs useful in the treatment and/or prevention of these diseases. There are no other animal models in which the deletion of the activity of a single gene is capable of abrogating the course of osteoarthritis.

Abstract: Cyanophenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract: The invention features methods for increasing cell death. The invention also features compounds used to increase cell death. The invention further features methods for identifying compounds that increase cell death.

Abstract: Germicidal compositions containing phenylmalonaldehyde-type compounds, or mixtures of phenylmalonaldehyde-type compounds and phthalaldehydes, and methods of using such compositions for killing bacteria, disinfection, or sterilization, are disclosed. In one aspect, a germicidal composition may include a diluent, and a germicidal compound having the formula: wherein Ar is an aryl group that is selected from the group consisting of phenyl, 4-pyrimidinyl, and 2-(2-nitro-3-formyl-phenyl). In a further aspect, the composition may also include a germicidal efficacy enhancer such as isophthalaldehyde or a combination of isophthalaldehyde and terephthalaldehyde.

Abstract: The present invention is directed to crystalline forms of anhydrous 4-cyclopentyl resorcinol, the Form A and C polymorphs, formulations containing at least one of these crystalline forms and their use to lighten skin.

Abstract: Flame retardant flexible polyurethane foam compositions, methods of flame retarding flexible polyurethane foam compositions, articles made therefrom and flame retardants that comprise blends of (alkyl substituted) triaryl phosphate ester and phosphorus-containing flame retardant having at least about 5 wt. % phosphorus additives. The combined weight of the (alkyl substituted) triaryl phosphate ester and the phosphorus-containing flame retardant comprises about 5 to about 40% by weight of the flexible polyurethane foam compositions or reaction mixtures. The ratio of the (alkyl substituted) triaryl phosphate ester to the phosphorus-containing flame retardant is from about 95:5 to about 50:50 percent by weight.

Abstract: An active ray curable composition, including an epoxy compound which is represented by Formula (A) and an oxetane compound, The active ray curable compound exhibiting a viscosity of 1 to 500 mPa·s at 25° C.

Abstract: Compositions of vinyl halide polymers such as PVC are rendered compostable by a prodegradant system of an organotitanate or zirconate and an organotin. PVC sheets and composites are compostable in landfills.

Abstract: The invention includes pigment compositions for plastics comprising one or more flake-form effect pigments, a carrier material and one or more fluorine-containing polymers, to a process for the preparation of the pigment compositions, and to the use thereof for pigmenting plastics and for the production of masterbatches.

Abstract: An antifouling coating which comprises a varnish comprised of a metal-containing acrylic resin having, in a side chain thereof, at least one group represented by the following formula (1): wherein X represents a group of the formula: n represents 0 or 1; Y represents a hydrocarbon group; M represents a metal; m represents an integer equal to [(the valence number of metal M)?1]; A represents an organic acid residue derived from a monobasic acid, said varnish having a nonvolatile fraction of not less than 40 weight % and a viscosity at 25° C. of not more than 18 poises and said antifouling coating having a volatile organic compound (VOC) content of not more than 400 g/L.

Abstract: The present invention discloses a water dispersible polymer particle stabilized by a hydrophobically capped oligomeric acrylamide dispersant. The present invention also discloses a heterogeneous method for forming polymer particles comprising providing a water immiscible organic phase comprising at least one monomer dispersed in a continuous water phase and a hydrophobically capped oligomeric acrylamide, and polymerizing said organic phase to yield polymer particles stabilized with hydrophobically capped oligomeric acrylamide. Also disclosed in the present invention is a heterogeneous method for forming polymer particles comprising providing a water immiscible organic dispersed in a continuous water phase, polymerizing said organic phase, and adding bydrophobically capped oligomeric acrylamide to yield polymer particles stabilized with hydrophobically capped oligomeric acrylamide.

Abstract: A sealing element is formed from a desirably shaped body of a sealant material formulated from a first polymer, ethylene vinyl acetate (EVA), in a concentration of about 25 percent to about 30 percent, a calcium carbonate inert filler material in a concentration of about 25 percent to about 30 percent, a second ethylene polymer other than EVA in a concentration of about 20 to about 35 percent, and a hydrocarbon resin in a concentration of about 10 percent to about 15 percent. The sealant further comprising an epoxy resin in a concentration of about 2 to about 5 percent and an activator in a concentration of about less than one percent of the sealant. The sealant material, when positioned about a first component is overmolded with a material forming a second component. The sealant material, which is heat activated, forms a seal between the first and second components.

Abstract: Disclosed herein is a process for improving mechanical properties and thermal stability of composites of poly(vinyl chloride) and at least one natural fiber comprising including in said composite an agent comprising a polymer or copolymer comprising at least one alkali metal salt of at least one polymerized ethylenically unsaturated carboxylic acid. Articles of manufacture comprising the stabilized PVC are also disclosed.

Abstract: A composition for the treatment of metal surfaces and for the deposition of metals or metal alloys on plastics surfaces contains a) at least one polymer as component A, composed of the structural element (1) and at least three structural elements selected from the group consisting of b) water or another solvent which is suitable for dissolving, dispersing, suspending or emulsifying the polymer, as component B; c) if required, surface-active compounds, dispersants, suspending media and/or emulsifiers as component C. In a process for the treatment of a metal surface and a process for the deposition of metals or metal alloys on a plastics surface, the metal or plastics surface is brought into contact with a polymer (component A). Furthermore, polymers (component A) are used for the treatment of metal surfaces and for the deposition of metals or metal alloys on a plastics surface, and polymers composed of special components A?a, A?b and A?c.

Abstract: Extrusion processability of non-fluorinated melt-processable polymers is improved by introducing a fluoropolymer process aid by means whereby the weight average particle size of the fluoropolymer is greater than 2 microns as it reaches the extruder die entrance.

Abstract: Resins for powder coatings which are thermally and radiation curable containing both olefinically unsaturated groups and at least one other reactive group in the same molecules selected from epoxide groups and acid groups, a method for their preparation, and the use thereof in powder coating compositions.

Abstract: A thermoplastic elastomer composition comprises a blend of a thermoplastic component with a cured elastomer component characterised in that the elastomer component prior to curing comprises a major proportion of a main elastomer and a minor proportion of a high molecular weight reactive polymer which shows a higher crosslinking efficiency in free-radical induced vulcanisation than the main elastomer. Preferably, the high molecular weight reactive polymer comprises from (3) to (15), and more preferably (4) to (10), parts by weight per one hundred parts of the total elastomer component of the composition. The use of the high molecular weight reactive polymer in the composition improves the low temperature performance of the composition and gives improvements to the processing behaviour, the resistance to stiffening at low temperatures and recovery/relaxation properties. Preferably, the high molecular weight reactive polymer is miscible with the main elastomer in the elastomer component.

Abstract: This invention relates to toughened cyanoacrylate compositions which exhibit improved peel strengths and fixture speeds. The toughened cyanoacrylate compositions include a toughening agent comprising poly(vinychloride-co-vinyl acetate) and poly(methylmethacrytlate).

Abstract: In a multi-piece solid golf ball comprising a solid core, a mantle and a cover, the solid core is made of a rubber composition that includes a base rubber containing a polybutadiene synthesized using a rare-earth catalyst, a small amount of organic peroxide, an unsaturated carboxylic acid and/or a metal salt thereof, an organic sulfur compound and an inorganic filler. The mantle is made of a thermoplastic resin composition. The cover is made primarily of a thermoplastic polyurethane material. This construction provides the golf ball with a combination of outstanding flight performance and soft feel with cover's scuff resistance and coating's abrasion resistance, that is unprecedented.

Abstract: An object of the present invention is to provide a novel solid reagent capable of solving the problems of conventional solid reagents based on resin beads. The present invention relates to a solid reagent comprising an organic polymer base in which a polymer side chain is introduced onto the backbone of the organic polymer base via graft polymerization and a reactive functional group is introduced onto the polymer side chain. The organic polymer base is preferably in the form of a fiber, a woven or nonwoven fabric consisting of an assembly of fibers, a porous membrane or a hollow fiber membrane. The graft polymerization is preferably a radiation-induced graft polymerization. Solid reagents according to the present invention can be used in various organic synthetic reactions.

Abstract: This invention is directed to fluorinated acrylate compositions, which are suitable for use as low shrinkage, low absorbance refractive index matching adhesives for use in “pig-tailing” polymeric integrated waveguides to optical fiber bundles.

Abstract: A new family of concrete admixture additives can be derived from reacting a mixture of olefins/cyclic olefins-maleic anhydride copolymers and methoxy polyethylene glycol amines and/or polyethylene glycol monoalkyl ethers, or a mixture of styrene-maleic anhydride copolymers and methoxy polyethylene glycol amines and/or polyethylene glycol monoalkyl ethers, or a mixture of styrene-olefins/cyclic olefins-maleic anhydride terpolymers and methoxy polyethylene glycol amines and/or polyethylene glycol monoalkyl ethers. These reactions lead to formation of a kind of carboxylic salt containing polymer, which can be used alone in concrete. Only a small amount of this substance is needed to provide excellent water reduction, high concrete flowability and high early strength.

Abstract: Disclosed is a method for making selectively hydrogenated block copolymers of vinyl aromatic hydrocarbons and conjugated dienes comprising: a) anionically polymerizing vinyl aromatic hydrocarbons and conjugated dienes to produce block copolymers with living chain ends; b) terminating the living chain ends; to produce a terminated block copolymer, with a member from the group consisting of an alcohol, hydrogen, and mixtures thereof, to prepare a terminated block copolymer; and c) contacting the terminated block copolymers with hydrogen at a temperature of from 20 to 175° C. in the presence of a catalyst prepared by combining a cobalt carboxylate with an aluminum alkyl, wherein: (i) if the polymer is terminated with an alcohol and the alcohol is a linear alcohol, the linear alcohol is used to terminate the living chain ends in an amount such that the alcohol:living chain end molar ratio is from 0.05 to 1.

Abstract: Crosslinkable polymeric materials are disclosed useful for the temporal stabilization of a poling-induced noncentrosymmetric host lattice containing guest nonlinear optical chromophores. The materials are also suitable as crosslinkable coatings in the absence of chromophores. Also disclosed is a method of crosslinking such polymeric material.