Abstract: A novel optically pure (−)-1-(Benzofuran-2-yl)-2-propylaminopentane as represented by the following formula, which contains no (+)-isomer, and the pharmaceutically acceptable acid salt thereof. These compounds have excellent CAE effect (catecholaminergic activity enhancer effect) which is the enhancing action of neurotransmitter catecholamine release, and are useful as psychotropic composition, antidepressants, composition for treating Parkinson's disease and/or Alzheimer's disease.

Abstract: The invention relates to a method of producing epoxy resins from hydrocarbons with olefinic double bonds, especially alkenes, by heterogeneous catalyzed oxidation in the gaseous phase. According to said method, and oxidic solid catalyst is released which contains iron as its active component at a concentration of 0.001-1% and alkali and/or alkaline earth elements as the promoters. N2O is used as the oxidizing agent. The granulated oxidic solid catalyst, especially on the basis of SiO2 as the carrier, has a specific surface of greater that 50 m2/g. The ratio of the concentrations of the active components to the promoter components is preferably between 1:100 and 10:1. The partial oxidation of hydrocarbons with olefinic double bonds, especially propene, results in propene selectivities of 10-70% at reaction temperatures of 300-500° C. and conversions of 2-30%.

Abstract: The invention relates to new paclitaxel derivatives showing a comparable cytotoxicity of the parent compound, and their uses in a drug targeting therapy. The present invention also relates to the composition and use of such derivative, composition and conjugates for treating cancer.

Abstract: Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NRa wherein Ra is hydrogen or a C1-8 alkyl group; R1 represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R1 being optionally substituted by one or more R3;groups; P=0 to 3; U, R2, R3 are as defined in the application.

Abstract: A synthesis for preparing asymmetrical 1,4-diketopyrrolo[3,4-c]pyrroles involving: (a) reacting a &bgr;-ketoamide with a strong base; (b) halogenating the same or a different &bgr;-ketoamide; (c) reacting the reaction products of step (a) and (b) to form a succinamide; and (d) heating the succinamide in the presence of a Lewis Acid. Symmetrical 1,4-diketopyrrolo [3,4-c]pyrroles are synthesized by oxidatively dimerizing the reaction product of step (b) to form a succinamide; and heating the succinamide in the presence of a Lewis Acid.

Abstract: Novel 4-methylene-1,3-dioxolanes of the general formula I in which R1 denotes hydrogen or alkyl, X denotes a single bond, C1-C18 alkylene, cycloalkylene, arylalkylene, —CH2(OCH2CH2)n— or —CH2(OCH(CH3)CH2)n—, in which n is an integer from 1 to 100, and Z means a functional group selected from among —OH, —COOR′ or —OCOR′, in which R′ denotes hydrogen or C1-C8 alkyl, are described, as are a process for the production thereof and the intermediates used in this process.

Abstract: An imidazole derivative of formula (I) or a pharmaceutically acceptable salt or derivative thereof. The compounds of formula I exhibit affinity for alpha2 adrenoceptors.

Abstract: Compound represented by the following formula (I): wherein R1 represents a lower alkyl group, R2 represents a phenyl group which may be substituted or a lower alkyl group and R3 represents a phenyl group which may be substituted (e.g., 4-(4-chlorophenyl)-2-phenyl-3-(1,2,4-triazoyl)-butan-2-ol) or salts thereof. The compounds have a specific inhibitory action against the brassinosteroid biosynthesis, and are useful as plant growth regulators.

Abstract: The present invention provides a process for making 3-hydroxyalkanenitriles comprising the steps of reacting an alkenylnitrile, wherein the alkenylnitrile is an alkenyl-2-nitrile or an alkenylnitrile which under reaction conditions isomerizes to form an alkenyl-2-nitrile, in the presence of a base with benzyl alcohol to form a 3-benzyloxyalkanenitrile adduct and then partially hydrogenating the adduct in the presence of a trace amount of HCl to form the 3-hydroxyalkanenitrile or fully hydrogenating the adduct to form a 3-hydroxyaminoalkane.

Abstract: A novel pyrylium compound is represented by the general formula (I): wherein X is oxygen or sulfur, Y− is a monovalent anion, n is an integer of 2 or 3, and M is hydrogen or an alkali metal. This pyrylium compound functions as a labeling agent by intermolecular bonding to nucleic acids, and as a fluorescence label having a chemical bond with the nucleic acids and an excitation wavelength in a visible light region.

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 guanidinium salt or onium salt; and (C) at least one metal co-catalyst.

Abstract: Inhibitor compounds containing a moiety according to this invention are used to inhibit air oxidation and thermal polymerization of furfural or furfural derivatives. A process is provided for use of the inhibitors in the solvent refining of lubricating oils where furfural is used to extract impurities including polycyclic aromatic and oxygen-containing compounds from the lubricating oils. The process provides for combination of the inhibitor with a continuously recirculating furfural stream in the extraction process.

Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.

Abstract: This invention is directed to compounds and intermediates of Formulae 6 and 3, useful in preparing herbicidal sulfonamides of Formula 1, including all geometric and stereoisomers thereof, and agricultural salts thereof. wherein the substituents are defined in the specification.

Abstract: The invention provides improved and simplified methods of synthesizing ligands containing a heteroatom-bearing bridge using a novel intermediate compound. The ligands may be used to form metal complexes that are useful in diagnostic and therapeutic applications.

Abstract: This invention relates to benzocycloheptene derivatives having novel structure. More particularly, it relates to new benzocycloheptene derivatives and pharmaceutically acceptable salts thereof, their production processes, a pharmaceutical composition containing the same and a use thereof for the manufacture of medicaments.

Abstract: An unsaturated fatty acid precursor of a natural 1,3-diol derivative, which precursor is the same as that which is naturally present in a cider apple, is enzymatically converted to the natural 1,3-diol derivative.

Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

Abstract: Disclosed is a method for preparing DL-&agr;-tocopherol with a high yield through the condensation of isophytol or phytol derivatives with trimethylhydroquinone (TMHQ) in the presence of a Zn—Al heterogeneous catalyst system. At 80 to 120° C., the condensation is carried out for 2 to 7 hours in the presence of a Zn(II) ion-coated alumina-silica catalyst in an n-heptane solvent. The synthetic Zn(II) ion-coated silica-alumina synthetic catalyst system can remarkably reduce side-reactions upon the condensation of isophytol or phytol derivatives and TMHQ, thus producing DL-&agr;-tocopherol with a high purity at a high yield. In addition, the catalyst system is greatly convenient to handle and therefore apply for continuous reactions for the preparation of DL-&agr;-tocopherol. With these advantages, the catalyst system can be effectively used in preparing highly pure DL-&agr;-tocopherol at a high yield on a commercial scale.

Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or