Abstract: This invention relates to inhibitors of glycogen synthase kinase-3&bgr;, methods of treating diseases characterized by an excess of Th2 cytokines, and to 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives of Formula (I): that are inhibitors of glycogen synthase kinase -3&bgr;, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The invention relates to a process for the cyclizing hydrolysis of an aminonitrile compound into a lactam in the presence of a catalyst. The invention relates more particularly to a process for the cyclizing hydrolysis of an aminonitrile compound in the presence of a macroporous particulate catalyst obtained by deposition/impregnation of an oxygenated compound onto a macroporous support such as alumina. The invention applies in particular to the preparation of &egr;-caprolactam by cyclizing hydrolysis of aminocapronitrile.

Abstract: A process for producing a compound of the formula (II): (wherein R1, R2, R3 and R4 are each independently hydrogen, alkyl, alkoxy or the like, R5 is alkyl or alkoxyalkyl, A is O or S, Ar is aryl or the like, * represents the position of an asymmetric carbon atom and that the compound is the (R) or (S) isomer and Q is an optical resolution reagent) comprising isolating the compound as crystals from a solution or suspension containing the compound of the formula (II) (wherein * represents that the compound is the (R) or (S) isomer or a mixture thereof and the other symbols are the same as the above).

Abstract: A method for continuously producing a dialkyl carbonate and a diol, comprising: (1) continuously feeding a cyclic carbonate and an aliphatic monohydric alcohol to a continuous multi-stage distillation column, and continuously effecting a transesterification between the cyclic carbonate and the aliphatic monohydric alcohol in the presence of a transesterification catalyst in the distillation column, while continuously withdrawing a low boiling point mixture in a gaseous form containing the produced dialkyl carbonate and the unreacted aliphatic monohydric alcohol from an upper portion of the distillation column and continuously withdrawing a high boiling point mixture in a liquid form containing the produced diol and the unreacted cyclic carbonate from a lower portion of the distillation column, and (2) continuously feeding the high boiling point mixture withdrawn from the lower portion of the distillation column to a continuous etherification reactor, to thereby effect a continuous etherification reaction betw

Abstract: The present invention relates to a method of producing paclitaxel from a protected coupled ester compound having a formula: wherein P1 is a hydrogenatable protecting group, comprising the steps of deprotecting the 7-O-position, 3′-N-position and 2′-O-position thereof in the presence of an acid to form a first intermediate compound having a formula: wherein HA is said acid, and benzoylating the first intermediate compound at the 3′-N-position thereby to produce paclitaxel.

Abstract: Oligomeric procyanidins containing 4&agr;-linked epicatechin units are rare in nature and have hitherto not been accessible through stereoselective synthesis. Provided herein is the preparation of the prototypical dimer, epicatechin-4&agr;,8-epicatechin, by reaction of the protected 4-ketones with aryllithium reagents derived by halogen/metal exchange from the aryl bromides. Removal of the 4-hydroxyl group from the resulting tertiary benzylic alcohols is effected by tri-n-butyltin hydride and trifluoroacetic acid in a completely stereoselective manner, resulting in hydride delivery exclusively from the &bgr; face.

Abstract: An object of the present invention is to provide an ammoxidation reaction catalyst composed of an Sb—Re compound oxide with which ammoxidation into an unsaturated nitrile such as methacrylonitrile or the like can be performed in the presence of a molecular oxygen-containing gas and ammonia, and a method for manufacturing an unsaturated nitrile such as methacrylonitrile or the like from an aliphatic hydrocarbon such as isobutylene, isobutane or the like using this ammoxidation reaction catalyst. An unsaturated nitrile such as methacrylonitrile or the like is manufactured by subjecting an aliphatic hydrocarbon such as isobutylene, isobutane or the like to vapor phase contact ammoxidation with ammonia and a molecular oxygen-containing gas in the presence of an ammoxidation reaction catalyst composed of an Sb—Re compound oxide such as SbRe2O6 or the like.

Abstract: Provided herein is a process for producing alkylene carbonates of ultra-high purity. According to the present invention, certain stages of traditional distillation of alkylene carbonate distillation are replaced by carbon treatment. Alkylene carbonates produced according to the invention have a color of less than 25 (Pt-Co), and are suitable for uses requiring ultra-pure alkylene carbonates.

Abstract: A purification method for obtaining high-purity PMDA. The method controls temperatures of cyclone separators in a series to separate PMDA and other by-products of different sublimation temperatures. High-purity PMDA is collected in the first cyclone separator, and no other purification steps are needed.

Abstract: What is disclosed is a process for producing &egr;-caprolactone which comprises removing impurities by distillation from a reaction mixture obtained by co-oxidation of cyclohexanone and aldehyde, wherein &egr;-caprolactone separated from a purifying column is contacted with oxygen containing gas in the presence of cobalt. High boiling point components are removed to give an acid value of lower than 0.15 mgKOH/g. Thereby, a high quality &egr;-caprolactone providing improved polymer appearance is produced advantageously on an industrial scale without repeated purifying distillations or without using expensive stabilizer or adsorbent for the improvement of color.

Abstract: A process for catalytic production of diaryl carbonates by oxidative carbonylation of aromatic hydroxy compounds with carbon monoxide and oxygen achieves water removal during reaction by a process comprising the steps of: removing a liquid stream from an oxidative carbonylation reaction mixture in a reaction vessel, subjecting the liquid stream to reduced pressure, and returning at least a portion of dried liquid stream to the reaction vessel. Typical catalyst systems for oxidative carbonylation contain (A) at least one Group 8, 9, or 10 metal having an atomic number of at least 44 or a compound thereof; (B) at least one alkali metal salt; (C) at least one metal co-catalyst; (D) at least one activating organic solvent; and (E) optionally, at least one base.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions. A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C.

Abstract: A process for preparing a triazolinone includes the step of reacting a triazolinethione with an oxidant at a temperature range of from about 60° C. to about 100° C. in the presence of a base.

Abstract: A compound represented by the following general formula: wherein R1 and R2 represent amino groups present at adjacent positions each other on the phenyl ring; R3, R4, R5 and R6 independently represent a C1-6 alkyl group; R7, R8, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, an allyl group, or a halogen atom; R11 represents a hydrogen atom or a C1-18 alkyl group; and X− represents an anion, and an agent for nitric oxide measurement comprising said compound. The compound efficiently reacts with nitric oxide to give a fluorescent compound that emits strong fluorescence by irradiation with excitation light of a long wavelength. This fluorescent compound is characterized in that said compound is detectable in a fluorescence wavelength range hardly influenced by autofluorescence of cells, and its fluorescence intensity is not attenuated under an acidic condition.

Abstract: Cocoa extracts which include procyanidin monomers and their oligomers are useful in the modulation of inflammatory pathways, in the maintenance of the vascular health of a mammal and as an antibacterial treatment. The liquid or dry cocoa extracts can be included in foods, food supplements and pharmaceuticals for the inhibition of COX activity, the inhibition of LOX activity, the enhancement of nitric oxide production, the modulation of eicosanoids and endothelin, and the modulation of platelet activity.

Abstract: Ethylenically unsaturated organic compounds, for example diolefins, olefinic nitriles and monoolefins, are noncontaminatingly hydrocyanated into corresponding nitriles by (a) reacting such ethylenically unsaturated organic compounds with hydrogen cyanide in the presence of an aqueous solution containing a catalytically effective amount of a catalyst which comprises at least one nickel compound and at least one water-soluble phosphine, (b) thereafter separating the organic phase from the aqueous phase which result, the separated aqueous phase comprising a solid phase formed during hydrocyanation, and (c) thence treating the separated aqueous phase, or a solid phase removed therefrom, with hydrogen cyanide to thus at least partially dissolve said solid phase contained therein or removed therefrom.

Abstract: N-halamine biocidal materials and coatings are provided. Monomeric oxazolidinones or hydantoins are homopolymerized or copolymerized with other monomers so as to produce materials or coatings, which upon exposure to solutions of chlorine or bromine become biocidal. The biocidal materials and coatings are effective at inactivating microorganisms upon surface contact and are regenerable following loss of efficacy upon further exposure to solutions of chlorine or bromine. Surfaces which could be treated with the materials and coatings include, but are not limited to: glass, plastic, metals, fibers, and wood for use in pool and tank liners, food wrappers, catheters, paints, tiles, shower walls, fabrics, sterile bandages, pipes, medical and dental coatings, preservatives, and the like.

Abstract: A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes an effective amount of a Group VIII B metal source; an effective amount of a bromide composition; an effective amount of an activating organic solvent; an effective amount of a combination of inorganic co-catalysts comprising a lead source and a copper source; and an effective amount of a base.