Abstract: A novel process for preparing the compounds of the formula I where: n is 0, 1 or 2; R1, R2 are C1-C6-alkyl; R3, R4, R5 are hydrogen or C1-C6-alkyl, or R4 and R5 together form a bond; R6 is Cl, Br, which comprises a synthesis sequence starting from 1,2-dialkylbenzenes of the formula II with subsequent halogenation to give 3,6-dihalo-1,2-dialkylbenzenes, haloalkylation to give benzyl bromides, oxidation to give benzaldehydes, oximation, reaction with alkenes to give isoxazoles, conversion into thioethers and, if appropriate, oxidation to give sulfenyl or sulfonyl derivatives of the formula I.

Abstract: The invention is directed to substituted thieno[2,3-b]pyrrolidin-5-ones. The compounds are useful as inhibitors of cellular production of tumor necrosis factor (TNF-&agr;) and as antiproliferative agents. These compounds are useful in the treatment or control of neuro-degenerative diseases, cardiovascular diseases, cancer or inflammatory diseases.

Abstract: There is provided a process for the production of a compound of formula I, which process comprises reaction of a compound of formula II, with a compound of formula III, wherein R1, R2, n and R3 have meanings given in the description.

Abstract: The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) to a process for their preparation and to their use as pesticides and herbicides.

Abstract: Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.

Abstract: The present invention relates to a process for preparing a colour-stable, aqueous dimethylaminoacetonitrile solution from a formaldehyde source, dimethylamine and hydrocyanic acid, wherein the reaction mixture contains 2,4-diamino-6-phenyl-1,3,5-triazine(benzoguanamine) in a concentration of from 0.001 to 5% by weight, based on formaldehyde, prior to the reaction and the starting substances are used stoichiometrically or in a ratio of 0.98-1.02 mol of formaldehyde and 0.95-1.10 mol of dimethylamine per mol of hydrocyanic acid. The resulting product remains colour-stable without a further purification step even after prolonged storage.

Abstract: Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one hetero atom selected from the group O, S and NR, or ferrocenyl; R is H or C1-C4alkyl; each R4 individually or both R4 together are a hydrocarbon radical having from 1 to 20 carbon atoms; and R01 and R02 are each independently of the other a hydrogen atom or a hydrocarbon radical having from 1 to 20 carbon atoms, are chiral ligands for metal complexes with metals of sub-groups I and VII, which are catalysts for asymmetric addition reactions, for example of hydrogen, to prochiral unsaturated organic compounds.

Abstract: This invention provides a convenient process for manufacturing 1,3-dialkyl-2-imidazolidinones in a direct one-step reaction from industrially available alkylene carbonate, N-alkylethanolamine or 1,2-diol, which can minimize forming solid materials and be readily conducted in an industrial large-scale production with a higher yield and less byproducts. The process is characterized in that alkylene carbonate, N-alkylethanolamine or 1,2-diol is reacted with monoalkylamine and carbon dioxide, alkylcarbamate alkylamine salt, and/or 1,3-dialkylurea, by heating them at 50° C. or higher in a reactor whose area in contact with at least part of the reactants and/or products is made of a metal comprising titanium or zirconium and/or an oxide thereof or inorganic glass.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: The isomerization of an alkylated phenol composition that contains an ortho-alkyl substituted phenol component to isomerize and reduce the level of ortho-alkyl substituted phenol component therein can be accomplished by heating that composition in the presence of a catalytically effective amount of a solid acid catalyst to carry out such isomerization and reduction in the level of ortho-alkyl substituted phenol. Examples of suitable solid acid catalysts can be selected from the H-form zeolites, the supported sulfonic acids, and the heteropoly acids. The resulting isomerized product can be subsequently phosphorylated.

Abstract: Processes for the preparation of haloalkylamines and tertiary aminoalkylorganometallic compounds are disclosed. The haloalkylamines can be prepared by direct reaction of an amine with an &agr;, &ohgr;-dihaloalkane or an &agr;, &ohgr;-dihaloalkene. Tertiary aminoalkylorganometallic compounds can be prepared by reacting selected tertiary haloalkylamines with an alkali metal at a temperature greater than 45° C. in hydrocarbon solvents.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—═CH—, —S— or —O—.

Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral amine oxazolinyl ligands and related ligands. Specially, a direct asymmetric hydrogenation system based on Ru-Ambox catalyst was discovered.

Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in indications associated with the androgen receptor, such as cell hyperplasia dependent on androgens, hirsutism, acne and androgenetic alopecia.

Abstract: Novel phosphine oxazoline ligands of formula (I) wherein m is 1, 2, 3 or 4; n, p, q, r are independently zero or 1 provided that at least one of n, p, q and r is 1; X is O, S, Se, CH2, NH; Y is N, P, As, S; R is H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; ferrocenyl; a thioalkyl group; a thioaryl group; or R is part of a polymeric structure, for example polyacrylic acid; R1 to R13 are independently selected from H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; a process for the preparation thereof,

Abstract: A process for the preparation of a stabilizer mixture containing a low amount of chloride comprising a) 50-80% by weight of tetrakis(2,4-di-tert-butylphenyl)biphenylene diphosphonite and its isomers, b) 5-25% by weight of bis(2,4-di-tert-butylphenyl)biphenylene monophosphonite and its isomers, and c) 5-25% by weight of a tris(2,4-di-tert-butylphenyl) phosphite, and where the sum of components (a), (b) and (c) is not greater than 100% by weight, by reacting biphenyl under Friedel-Crafts condition with phosphorus trichloride and aluminium trichloride and by reacting the product mixture with 2,4-di-tert-butyl-phenol in the presence of a tertiary amine or an aromatic amine and a solvent, separating the formed two layers, which process comprises treating the solvent layer with water, a base and a desiccant, separating the precipitate from the solution containing the stabilizer mixture and evaporating the solvent.

Abstract: An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl group using Raney Nickel or Magnesium in alcohol having 1 to 4 carbon atoms or mixtures thereof, if desired reesterifying using sufphuric acid at a temperature in the range of 0° C. to 60° C. to obtain a compound of formula (3′) wherein R is as defined above, hydrolyzing the compound of formula (3′) wherein R is as defined above, by conventional methods to obtain the acid of formula (4), condensing the acid of formula (4) with N-methyl anthranilamide directly without any preactivation of the acid to produce the compound of formula (1) and if desired, converting the compound of formula (1) to pharmaceutically acceptable salts thereof by conventional methods.

Abstract: A method of preparing vicinal difluoro aromatic compounds in high yield from hydroxy aromatic compounds and a method of preparing intermediates thereof. The hydroxy aromatic compound can be a mono-, bi- or tricyclic aromatic in which the rings are separate or fused. One or more of the rings can contain heteroatoms, such as oxygen, nitrogen, or sulfur, and can contain one or more substitutions, in addition to the hydroxy substitution.

Abstract: A high purity N,N-Carbonyl diimidazole (I) is obtained by the reaction of Imidazole, general formula-II, and bis (trichloromethyl) carbonate.

Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.