Abstract: New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R1 represents an OR3 radical, where R3 represents a radical derived from a saturated hydrocarbon, with a linear or branched chain of 1 to 4 carbon atoms, and R2 represents a phenyl radical substituted at least by one cyan radical (—C?N), or a radical of a heteroaromatic ring of 5 or 6 members substituted at least by one cyan radical (—C?N); and their physiologically acceptable salts, are useful for application in human and/or veterinary therapeutics as sedatives, anticonvulsants, hypnotics and general anaesthetics

Abstract: The present invention relates to novel polymorphs of imatinib mesylate, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.

Abstract: Integrin receptor antagonists whose molecular structure includes a tetrahydropyridimidinylaminoethyloxybenzoyl group on a sulfonylamino-?-alanine nucleus exhibit increased binding affinity for the ?v?3 receptor when further substituted on the sulfonyl moiety with an N-amino alkycarbamyl group or a butyloxycarbonylamino alkylcarbamoyl group or similar groups.

Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.

Abstract: The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their,preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).

Abstract: The invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.

Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2 and R3 are as defined herein; pharmaceutical formulations thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as bipolar disorder, diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.

Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

Abstract: It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein.

Abstract: The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.

Abstract: This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.

Abstract: The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.

Abstract: Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y?C, or substituted diene fused to Y when Y?C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: The present invention discloses a process for preparing a nitrile compound, a carboxylic acid compound or a carboxylic acid ester compound represented by the formula (2): wherein R represents a cyano group, a carboxyl group or an ester group, R1 and R2 each represent a group which does not participate in the reaction, which may have a substituent, and R1 and R2 may be combined to each other to form a ring, which comprises subjecting an acetic acid compound represented by the formula (1): wherein R, R1 and R2 have the same meanings as defined above, to decarboxylation in the presence of a metal catalyst.

Abstract: The present invention provides an antiproliferative compound having a structural formula where X and Y independently are oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers or nitrites; R2 and R3 are hydrogen or R4; R4 is methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide or amine; and R5 is alkenyl; where when Y is nitrogen, said nitrogen is substituted with R6, wherein R6 is hydrogen or methyl. Also provided are methods for treating a cell proliferative disease and for inducing apoptosis in a cell comprising administering this compound is also provided.

Abstract: The invention provides the combined use of an inhibitor of formation or release of ?-amyloid and a nitric oxide releaser for the treatment or prevention of Alzheimer's disease.

Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Abstract: Provided are compositions which are suitable for topical application to human skin for cleansing and anti-microbial properties. In one preferred embodiment, the compositions include a glyceryl monoazelate ester. In another embodiment, the compositions include a glyceryl monoazelate monolaurate ester. It is postulated that bacteria on the skin cleave the ester linkage of a compound according to the invention that is applied to the skin, which causes liberation of the acid moiety from the ester, which acid moiety then inhibits or kills the bacterium. Compositions according to the invention may comprise skin creams, soaps, shampoos and lotions, and are especially effective in treating acne and acne-like skin ebullitions. The glyceryl portion of the molecules is believed to facilitate penetration of the ester into the skin.

Abstract: Ultradispersed ones of primary particles of nanometer-sized carbon are obtained by applying a wet-type milling method and/or a wet dispersion method to an aggregate structure of the primary particles to overcome van der Waals forces, by which forces the primary particles are held together to form the aggregate structure, whereby the ultradispersed primary particles are obtained in a colloidal dispersion on a large-scale basis at low cost without using any additive. In a method of manufacturing the ultradispersed primary particles, the wet-type milling method is carried out in a ball mill, preferably in combination with a high-energy ultrasonic-wave process carried out in a dispersing medium such as pure water, whereby a colloidal solution or slurry with a low-concentration of the primary particles ultradispersed in the dispersing medium is obtained.

Abstract: Fischer-Tropsch process for the conversion of carbon monoxide and hydrogen to C5+ hydrocarbon mixtures in which process use is made of Fischer-Tropsch catalyst particles and particles comprising zeolite Y with a water adsorption capacity (25° C., p/p0=0.20) of at least 16 wt %.

Abstract: A specific relationship must be met in case of: (a) a structural unit derived from propylene is present in 100 to 85 mole %, and a structural unit derived from ethylene and/or alpha-olefin with 4 to 20 carbons is present in 0 to 15 mole %; (b) a content of a position irregularity unit based on 2, 1-insertion of a propylene monomer unit in all propylene insertions, which is measured by 13C-NMR, is 0.5% to 2.0% and a content of a position irregularity unit based on 1,3-insertion of propylene monomer unit in all propylene insertions, which is measured by 13C-NMR, is 0.005% to 0.4%; and (c) a water vapor transmission rate is Y [g/m2/24 hr] as film and a melting point Tm[° C.] shows specific relationship.

Abstract: The present invention relates to polyol compositions which can be used to produce dimensionally stable, low density water-blown rigid foams which have acceptable compressive strengths and acceptable k-factors. In one embodiment of the present invention, the polyol compositions are composed of at least one aromatic amine-initiated polyether polyol and at least one polyether polyol having a functionality greater than or equal to 2.5 in which at least 50% by weight of the polyol composition is aromatic amine-initiated polyether polyol and in which no more than 50% by weight of the polyol composition is polyether polyol having a functionality greater than or equal to 2.5.

Abstract: In one aspect, the present invention provides hydrogels comprising polymer molecules and bridging molecules, wherein substantially all the polymer molecules are cross-linked by hydrogen bonds between polymer molecules and bridging molecules, wherein each bridging molecule is linked to at least two polymer molecules, and wherein there are substantially no covalent linkages between the polymer molecules. In some embodiments, the polymer molecules are poly(vinyl alcohol) (PVA) and the bridging molecules are amino acids. Some embodiments of the invention provide devices comprising hydrogels, and pharmaceutical compositions comprising biologically active molecules within hydrogels. Another aspect provides methods for forming hydrogels of the invention.

Abstract: Hardeners for water-based epoxy resin systems, the hardeners being obtainable by reacting a mixture of: (A) at least one epoxidized polyalkylene oxide selected from the group of epoxidized polyethylene oxides, epoxidized polypropylene oxides and polyethylene propylene oxides, (B) at least one epoxidized aromatic hydroxy compound selected from the group of bisphenol A epoxides and bisphenol F epoxides and (C) at least one aromatic hydroxy compound selected from the group of bisphenol A and bisphenol F, to form an intermediate product and subsequently reacting this intermediate product with a polyamine (E), are disclosed.

Abstract: Carbon black having organic groups, the organic group containing a thiocyanate group. Also described is a process for the production of the carbon black, wherein carbon black is reacted with organic compounds containing a C—C double or triple bond, which is not part of an aromatic system, whose C—C double or triple bond is activated by at least one substituent, and the organic compound contains at least one thiocyanate group. The carbon black according to the invention can be used in rubber compounds.

Abstract: A mixed polymer network made from reacting a carboxyalkyl cellulose and a synthetic water-soluble polymer with a crosslinking agent.

Abstract: A process is described for preparing mixtures of diesters of phthalic acid with decanols and tridecanols by reacting phthalic acid or a reactive derivative of phthalic acid with a mixture made from at least one decanol and at least one tridecanol. Mixtures obtainable in this way are also described, as is their use as plasticizers for molding compositions, and also mixtures of isomeric tridecanols suitable for preparing the mixtures of diesters.

Abstract: Polyester compositions are disclosed that include polyester polymers or copolymers having incorporated therein metallic titanium particles that improve the reheat properties of the compositions. Processes for making such compositions are also disclosed. The titanium particles may be incorporated in the polyester by melt compounding, or may be added at any stage of the polymerization, such as during the melt-phase of the polymerization. A range of particle sizes may be used, as well as a range of particle size distributions. The polyester compositions are suitable for use in packaging made from processes in which a reheat step is desirable.

Abstract: A spin fluid for producing plexifilamentary products made of a polyolefin dissolved in a primary solvent of dicloromethane or 1,2-dichloroethylene with a straight chain hydrofluorocarbon co-solvent.

Abstract: An ink jet recording medium including an ink receiving layer disposed on at least one side of a support, wherein the ink receiving layer is formed by applying an ink receiving layer coating solution. The ink receiving layer coating solution includes a water-soluble resin and a fine silica dispersion that has been prepared by finely dispersing a preliminary silica dispersion. The preliminary silica dispersion includes fumed silica, a cationic polymer having an I/O value of 2.4 or less, and alcohol.

Abstract: A tire tread incorporating an elastomeric composition reinforced by an inorganic filler, based on at least: (i) a diene elastomer; (ii) as reinforcing inorganic filler, more than 80 phr of a silica of low specific surface area having the following characteristics: (a) a BET specific surface area of less than 130 m2/g; (b) an average particle size, dw, of between 30 and 300 nm; (iii) a coupling agent providing the bond between the reinforcing inorganic filler and the diene elastomer; (iv) a vulcanization system comprising sulfur, a vulcanization accelerator and between 0.5 and 1.5 phr of zinc as vulcanization activator. Preferably, this silica furthermore has a disagglomeration rate ? greater than 5×103 ?m?1/min (measured in the ultrasound disagglomeration test).

Abstract: A composition comprises a non-aqueous solvent containing reverse micelle particles formed of block polymers having amphipathic properties. A particle composition and a composition wherein particles are dispersed, which exhibits excellent dispersion properties and can form superbly uniform particles, is provided. Further, display elements, a recording method, and recording apparatus, which employ the composition having excellent dispersion properties and forming superbly uniform particles, are provided.

Abstract: A water-soluble polyimide precursor, which can be suitably applied for aromatic polyimides and exhibits a low reduction in heat resistance and mechanical properties, an aqueous solution of the polyimide precursor and a polyimide obtained from the precursor. A heat-resistant fiber impregnated material and an impregnated sheet-like material are prepared by using the precursor and a laminate is prepared by employing the precursor.

Abstract: A composition comprising expandable cross linked polymeric microparticles having an unexpanded volume average particle size diameter of from about 0.05 to about 10 microns and a cross linking agent content of about 6,000 to less than about 9,000 ppm of labile cross linkers and from 0 to about 300 ppm of non-labile cross linkers, useful for modifying the permeability of subterranean formations and increasing the mobilization and/or recovery rate of hydrocarbon fluids present in the formations.

Abstract: The invention relates to the selection of a natural calcium carbonate crushed to a high degree of fineness, possibly treated with one or more fatty acids or one or more of their salts or mixtures thereof, and its use as a rheology regulator for polymeric compositions. The specific surface area is 14 to 30 m2/g measured according to the BET method to ISO 4652, and the oil absorption is greater than 16 measured according to ISO 787-V (Rub-out method). The conditions of mixing of the constituents and manufacture are improved, as well as the properties of the final product.

Abstract: A flame-retardant polycarbonate resin composition comprising 100 parts by weight of a resin mixture of (A) from 60 to 99% by weight of a polycarbonate resin and (B) from 1 to 40% by weight of a styrenic resin, and from 0.1 to 10 parts by weight of(C) a functional group having silicone compound, and from 0.02 to 5 parts by weight of (D) a fluoro-olefin resin.

Abstract: A method of treating hard substrates by contacting the substrate with a fluorochemical composition comprising: a fluorochemical urethane component and a base component is described. The compositions provide desirable repellency, antisoiling and anti-staining properties to the substrates.

Abstract: This method for preparing an acrylic-modified chlorinated polyolefin resin comprises graft-copolymerizing an acid-modified chlorinated polyolefin resin with a monomer mixture containing a (meth)acrylate ester monomer having one hydroxyl group and another vinyl monomer in the presence of a cyclic ether compound. Also, the cyclic ether compound may be added in an amount of 1 to 100 parts by weight based on 100 parts by weight of the acid-modified chlorinated ployolefin resin, and the cyclic ether compound may be dioxane and/or 1,3-dioxolane.

Abstract: This invention relates to a process for stabilising and at the same time phase compatibilising plastics or plastic compositions by incorporating polymeric compounds obtainable by reacting a compound selected from the group consisting of the sterically hindered phenols, sterically hindered amines, lactones, sulfides, phosphites, benzotriazoles, benzophenones and 2-(2-hydroxyphenyl)-1,3,5-triazines, which compounds contain at least one reactive group, with a compatibilisator.

Abstract: Light-stable and weather-stable coating films contain a powder coating composition, containing from 30 to 98.5% by mass of a binder containing at least one urethane (meth)acrylate having a melting point of from 40 to 130° C.; from 1 to 20% by mass of at least one micronized wax; and from 0.5 to 50% by mass of at least one auxiliary and/or at least one additive, the composition being cross-linked by actinic radiation.

Abstract: A thermoplastic elastomer composition of the invention, formed by dynamically crosslinking a polymer composition including a rubber and an olefinic resin and having an average particle size of rubber particles within a specific range, shows an excellent balance of mechanical properties such as flexibility and elastic recovery, and a moldability. Also an inclusion of a (meth)acrylate resin and a hydrogenated diene polymer provides a composition particularly excellent in scratch resistance. Also an inclusion of a maleimide compound provides a composition particularly excellent in injection fusibility. Also an inclusion of an undenatured organopolysiloxane of a specific viscosity and a denatured organopolysiloxane provides a composition particularly excellent in initial slidability and durable slidability.

Abstract: The present invention includes elastomeric compositions of BIMS elastomers suitable for abrasion resistant, high traction and/or barrier articles. The compositions and articles made from those compositions of the inventions can be described in any number of embodiments. In one embodiment, the composition suitable for an abrasion resistant article includes from 5 to 100 phr of a terpolymer of C4 to C7 isoolefin derived units, p-alkylstyrene derived units and p-bromomehtylstyrene derived units; at least one filler such as carbon black, silica, precipitated silica, clay, or combinations thereof; and from 0.1 to 3 phr of at least one thiourea.

Abstract: A process for producing a modified polyethylene resin, which comprises the step of melt kneading at least: (A) 100 parts by weight of a polyethylene resin, (B) from 0.1 to 20 parts by weight of at least one compound selected from the group consisting of: (B1) a compound having in its molecule (i) at least one carbon-carbon double or triple bond and (ii) at least one polar group, and (B2) a compound having in its molecule (iii) an OR group and (iv) at least two specific functional groups, and (C) from 0.01 to 20 parts by weight of an organic peroxide having a decomposition temperature of from 50 to 115° C., at which temperature a half-life thereof is 1 minute.

Abstract: A polymer composition that has a backbone chain; and a plurality of long chain branches connected to the backbone is described. The polymer composition also has a value of 2g?LCB-1g?LCB that is less than about 0.22, where 1g?LCB is the long chain branching index for a fraction of the composition having a Mw of 100,000 and 2g?LCB is the long chain branching index for a fraction of the composition having a Mw of 500,000.

Abstract: A process for preparing a graft copolymers is provided comprising exposing a polymeric base material to a dose of ionizing radiation, and then contacting the irradiated base material with a microemulsion comprising at least one fluorostyrenic monomer, water and water-miscible solvent. The graft copolymer may be formed into a membrane, including ion exchange membranes.

Abstract: A fluoropolymer having pendant amidoxime groups, pendant amidrazone groups, or combinations thereof is provided. Also provided are methods of making such fluoropolymers, and compositions and articles containing such fluoropolymers.

Abstract: The present invention provides compounds that have an amide linkage and at least two epoxy groups. The compounds are preferably aliphatic.