Abstract: A cosmetic composition on an external treatment agent containing microcapsules, with an average particle size of 0.1 to 2000 &mgr;m, enclosing a hydrophobic component, wherein the microcapsules are composed of a gelatin film swollen with water.

Abstract: A process for the preparation of nicotinic acid by the direct oxidation of &bgr;-picoline in the gas phase, wherein water and &bgr;-picoline are fed separately to the catalyst bed and the catalyst is based on a titanium dioxide support which has been prepared by the sulfate method and has a high specific surface area and a vanadium oxide content of from 5 to 50 %.

Abstract: Robustaflavone, intermediates and analogues thereof and a method for synthesizing the same are provided. The method involves constructing apigenin ethers containing functionalities at the 6- and 3′-positions which could be cross-coupled using transition metal catalysis. The method also involves development of a regioselective iodination of an apigenin derivative at the 6-position, formation of an apigenin 3′-boronate using a palladium-catalyzed exchange of the corresponding 3′-iodide with a diboron reagent. Finally, Suzuki coupling to form the sterically congested 6-3′″ biaryl bond of robustaflavone provides access to the desired biflavanoid system. Robustaflavone intermediates and analogues may be used to prepare analogues of other biflavanoids such as hinokifavone, rhusflavone and succedaneaflavone.

Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together —CH═CH—CH═CH—; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, —N(R5)2, —N(R5)S(O)2-lower alkyl, —N(R5)C(O)R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, —CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is —C(O)N(R5)—, —(CH2)mO—, —(CH2)mN(R5)—, —N(R5)C(O)—, or —N(R5)(CH2)m—; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof.

Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.

Abstract: This invention relates to a method of improving the catalytic performance of palladium or ruthenium, rhenium-on-carbon hydrogenation catalysts operating in aqueous media where loss of soluble rhenium may result in rapid catalytic failure. A rhenium-containing hydrogenation catalyst comprised of rhenium on a support material is regenerated by first treating the catalyst with aqueous perrhenic acid or potassium perrhenate followed by treating the catalyst under reducing conditions at elevated temperature and pressure. Treatment of the catalyst as described replenishes dispersed fresh finely divided rhenium which enhances the activity of the catalyst while at the same time allowing the operations to be carried out in situ in the hydrogenation reactor or in a side stream reactor with significant savings in reducing reactor down time and precious metal expenses.

Abstract: Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-pyridine-hydrobromide and reacted with 1,3,5-trimethoxyphenyl to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring.

Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: A method for obtaining purified bisbenzylisoquinoline alkaloids from the roots of Stephania Tetrandra involves obtaining, from the roots of Stephania Tetrandra, a precipitate comprising tetrandrine, fangchinoline and compounds which constitute impurities, contacting the precipitate with chloroform to form a chloroform solution in which tetrandrine and fangchinoline is dissolved, separating the chloroform solution containing dissolved tetrandrine and fangchinoline from undissolved impurities, removing chloroform from the chloroform solution to obtain a chloroform extract solid having an enriched tetrandrine and fangchinoline content relative to the precipitate, contacting the chloroform extract solid with cool benzene to form a combination comprising undissolved fangchinoline and a benzene solution in which tetrandrine is dissolved, separating the benzene solution from the undissolved fangchinoline from the first solid, removing benzene from the first benzene solution to form a benzene extract which comprises

Abstract: A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

Abstract: An environmentally friendly process for the preparation of the 4-functionalized N—OR derivatives of 2,2,6,6-tetraalkylpiperidines involves the hydrogen peroxide of the corresponding N—H compound to form the corresponding N-oxyl derivative, reacting two equivalents of the N-oxyl compound with one equivalent of a compound having an allylic hydrogen, a benzylic hydrogen or an activated methine hydrogen to form one equivalent of the corresponding N—OH compound and one equivalent of the corresponding N—OR compound, and recycling the N—OH compound back to the corresponding N-oxyl compound using hydrogen peroxide or air.

Abstract: The present invention provides water-soluble, pyran-based photochromic compounds characterized by improved stability when in an open, excited configuration. The advantages of the present invention are provided, at least in part, by functionalizing a pyran-based photochromic compound with carboxylate functionality in such a way that the carboxylate and/or its counter ion have sufficient mobility to engage in intermolecular and intramolecular interactions. In preferred embodiments, such a mobile carboxylate and/or counter ion provided on one side of an open pyran ring is preferably capable of complexing with functionality on the other side of the open pyran ring, greatly stabilizing the open configuration.

Abstract: A process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them, which comprises the step of reacting a 2-oxazoline compound with a piperidine derivative in the presence of an acid is provided. This process is an industrially excellent process for producing piperidinecarboylic acid amide derivatives useful as serotonin antagonists, antithrombocytic agents or intermediates for them.

Abstract: The invention relates to a single stage method for preparing 2-(quinolylthio)acetic acid and its salts by reacting 2-chloroquinoline and mercaptoacetic acid

Abstract: A process for reacting olefinic compounds, certain carboxylic reactants, and aldehydes or ketones and products prepared by the process. The compositions of the process are useful as intermediates for the preparation of additives for lubricants and fuels.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: The present invention provides compounds of the formula (1): wherein R1 and R2 each independently represent hydrogen, hydroxy, F, Cl, Br, I, CN, 1 to 6 carbon alkyl, 1 to 6 carbon alkoxy, nitro, CF3 and phenyloxy or benzyloxy, in which the aromatic ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; R3 and R4 are each independently a hydrogen, a 1 to 6 carbon alkyl or a CH2Ph in which the phenyl ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; Y is selected from CH2 or CH and, X is selected from a group represented by N, CR3, CHR3, CHCH; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds to treat central nervous system disorders, such as depression, anxiety, drug withdrawal, eating and sexual disorders and other conditions for which serotonin reuptake inhibitors are used.

Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: A method for producing an optically active amino alcohol compound of the formula [3], an enantiomer thereof or a salt thereof, comprising reacting a mesoepoxide compound of the formula [1] with a compound of the formula [2] in the presence of a mixed catalyst comprising a Lewis acid and a proton donor: wherein R1, R2 and R3 are each H, an optionally substituted lower alky, and the like, or R1 and R1 or R2 and R3 may form an optionally substituted ring; and R4 and R5 are each H, an optionally substituted lower alkyl, and the like, or R4 and R5 may form an optionally substituted ring together with the adjacent N, or an imide group or azide group together with the adjacent N, and R6 is H or a silyl group. The present invention enables stereoselective production of a desired intermediate compound, which is an HIV protease inhibitor, extremely efficiently as compared to conventional methods.

Abstract: A process for the manufacture of the racemic compound of the formula (I), its R-enantiomer (formula R-(I)) and its S-enantiomer (formula S-(I)), and pharmaceutically acceptable salts and/or solvates thereof, as well as new intermediates obtained and used in the process.