Abstract: Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.

Abstract: The preparation of a carboxylic ester by direct reaction of a carboxylic acid and an alcohol catalyzed by a sulphonic acid R—SO3H is carried out in the presence of a solid comprising tertiary amine functions.

Abstract: Granular product of parahydroxybenzoic acid or its ester which exhibits well suppressed dusting and caking tendency and a process for preparing the product are provided. The granular product of parahydroxybenzoic acid or its ester according to the instant invention has an average particle size of equal to or more than 150 &mgr;m and a hardness of 10-3000 g. The granular product of the invention can be prepared by dry compressing powdery parahydroxybenzoic acid or its ester to give compressed material, pulverizing and classifying the material.

Abstract: This invention encompasses the Form V polymorph of Compound A of structural formula: which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.

Abstract: The invention relates to novel arylalkyl- or aryloxyalkyl-substituted oxiranecarboxylic acids of the general formula I: in which Ar, R3, Y and n are as defined in the description, and also to medicaments comprising them and to their use for the treatment and prophylaxis of the disorders mentioned in claim 4 which are caused by disturbances of glucose and/or lipid metabolism, such as, for example, diabetes type 2 and other insulin-resistant conditions.

Abstract: A process for recovering a desired organic acid from a solution includes the steps of: providing an aqueous solution including at least one desired organic acid or its acid anion; adjusting the proton concentration in the aqueous solution to a desired level, with the desired proton concentration being selected, at least in part, by the amount of available protons needed to associate with the acid anions of the desired organic acid(s) to be recovered and/or acid anions that are weaker than the desired organic acids; and recovering at least a portion of the at least one desired organic acid from the aqueous phase. The desired proton concentration can be based on the amount of available protons being greater than, less than or substantially equal, to the amount of protons needed to associate with the anion of the desired organic acid(s) and acid anions that are weaker than the desired organic acid(s).

Abstract: The present invention provides methods for making N-methylpyrrolidine and analogous compounds via hydrogenation. Novel catalysts for this process, and novel conditions/yields are also described. Other process improvements may include extraction and hydrolysis steps. Some preferred reactions take place in the aqueous phase. Starting materials for making N-methylpyrrolidine may include succinic acid, N-methylsuccinimide, and their analogs.

Abstract: This invention provides amino acid N-carboxyanhydrides, each of which has an N-acyl substituent on its nitrogen atom, is represented by the following formula (1): readily reacts with nucleophilic reagents such as free amino acids, alcohols, anions or the like, and are intermediates useful for the high-yield production of amino acid derivatives, optically active compounds, peptides, polypeptides and the like useful in many fields lead by the fields of pharmaceuticals and agrochemicals, and also provides a process for the production of the amino acid N-carboxyanhydrides. Further, the present invention also provides a process for the production of diamides, which uses the compounds of the formula (1) and amine derivatives represented by the following formula (7): These diamides can also be suitably used for the production of amino acid derivatives, optically active compounds, peptides, polypeptides and the like.

Abstract: Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.

Abstract: An ester compound of the following formula (1) is provided. R1 is H, methyl or CH2CO2R3, R2 is H, methyl or CO2R3, R3 is C1-C15 alkyl, R4 is branched or cyclic, tertiary C5-C20 alkyl group, Z is a divalent C1-C10 hydrocarbon group, and k is 0 or 1. A resist composition comprising as the base resin a polymer resulting from the ester compound is sensitive to high-energy radiation, has excellent sensitivity, resolution, and etching resistance, and is suited for micropatterning using electron beams or deep-UV.

Abstract: A method for the absorption of (meth)acrylic acid and/or (meth)acrolein and an apparatus thereof which, in an absorption column adapted to cause an (meth)acrylic acid and/or (meth)acrolein-containing gas obtained in consequence of catalytic gas phase oxidation to come into countercurrent contact with a solvent, contemplate using a packing of relatively high efficiency in absorption disposed on the upstream side of the flow of a liquid containing the solvent and a packing and/or trays of relatively low performance of forming polymerization disposed on the downstream side thereof, in the column.

Abstract: The invention provides a process for producing lactic acid from a medium containing an alkaline earth-metal salt of lactic acid, comprising (a) reacting a conjugated base of an alkali metal from a subsequent step with the medium to form a water soluble alkali metal lactate salt and a basic compound of the alkaline earth metal; (b) separating the water soluble alkali metal lactate salt and the basic compound of the alkaline earth-metal; (c) splitting the water soluble alkali metal lactate to form a conjugated alkali metal base and a lactic acid product, which product is selected from the group consisting of lactic acid; and (d) separating the conjugated alkali metal base and the lactic acid product; (e) reusing the separated conjugated alkali metal base or the product in the step (a); and (f) reusing the basic compound of the alkaline earth metal, separated in step (b) to form an alkaline earth metal salt of lactic acid.

Abstract: Non-steroidal compounds and compositions which are agonists, partial agonists, and antagonists for androgen receptors and methods of preparation for the non-steroidal compounds and compositions.

Abstract: A method and system is provided for producing acetic acid by the catalytic carbonylation of methanol with carbon monoxide to obtain a reaction product stream comprising acetic acid and a minor amount of acetaldehyde. The acetaldehyde content in the reaction product stream is reduced by oxidation to convert at least a portion of the acetaldehyde in the stream to acetic acid or further to CO2 and H2O. The oxidized stream may then be directed to the purification section, the reaction section, or both whereby the deleterious effects of acetaldehyde are reduced. Advantage of the present invention over conventional processes is the reduced need to dispose of acetaldehyde as waste and improved overall system efficiency in the production of acetic acid.

Abstract: Non steroidal mimetics or analogues of brassinosteroids such as brassinolide include two bicyclic subunits each having a vicinal diol group and a polar unit and linked by a linking moiety such that the vicinal diol groups and polar unit are closely superimposable on corresponding functional groups in the brassinosteroid.

Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.

Abstract: A method for inhibiting polymerization during transportation, storage and/or production of (meth)acrylic acid or an ester thereof includes adding an N-oxyl compound and water to a vinyl compound; or dissolving an N-oxyl compound in water and adding the solution to a vinyl compound in a process of recovering, purifying, and/or synthesizing of the vinyl compound. The method can effectively inhibit polymerization of the vinyl compound.

Abstract: An adhesive composition is provided which is suitable for the bonding of polymeric materials, in whole or in part, such as composite resins, or methacrylate-containing glass-ionomer filling materials, to tooth enamel, or tooth dentin, or to other hand tissues of the human body, such as bone. The composition comprises an unsaturated carboxylic acid ester, an unsaturated phosphate ester and other crosslinking agents. The especially preferred phosphates (which are provided as new compounds) are those of formula (I) in which: R1 is a hydrogen atom, alkyl C1-C4, or CN; R is an aliphatic, cycloaliphatic or aryl radical containing from 1 to 10 carbon atoms and having a valence of n+1; n is an integer from 1 to 5, preferably from 3 to 5.

Abstract: A process for producing an ester comprises the steps of: (a) feeding to a first vessel a feed that comprises organic acid, alcohol, and water, whereby organic acid and alcohol react to form monomeric ester and water, and whereby a first liquid effluent is produced that comprises as its components at least some ester, alcohol, and water, the components of the first liquid effluent being substantially in reaction equilibrium; and (b) feeding the first liquid effluent to a second vessel, whereby a vapor product stream and a second liquid effluent stream are produced, the vapor stream comprising ester, alcohol, and water, wherein the second vessel is maintained substantially at vapor-liquid equilibrium but not substantially at reaction equilibrium.

Abstract: Use of (+)-(11R,2′S)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol or a pharmaceutically acceptable salt thereof substantially free of its (−)-enantiomer in the manufacture of a medicament having reduced side-effect compared to the racemic (±)-(R*,S*)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol for treating or preventing malaria in a subject. A method of treating or preventing malaria with reduced side-effects comprising administration of (+)-(11R,2′S)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol or a pharmaceutically acceptable salt thereof substantially free of its (−)-enantiomer.