Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.

Abstract: Disclosed is a method for producing an ?, ?-unsaturated carboxylic acid from an olefin or an ?, ?-unsaturated aldehyde, while suppressing dissolution of a silica carrier, which is a carrier for a silica-supported noble metal-containing catalyst, in a water-containing solvent. Specifically disclosed is a method for producing an ?, ?-unsaturated carboxylic acid through oxidation of an olefin or an ?, ?-unsaturated aldehyde in a water-containing solvent in the presence of a silica-supported noble metal-containing catalyst in a reactor, in which at least one of silicic acid and ions thereof is supplied into the reactor.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: A method is disclosed for the recovery of an organic acid from a dilute salt solution in which the cation of the salt forms an insoluble carbonate salt. A tertiary amine and CO2 are introduced to the solution to form the insoluble carbonate salt and a complex between the acid and an amine. A water immiscible solvent, such as an alcohol, is added to extract the acid/amine complex from the dilute salt solution to a reaction phase. The reaction phase is continuously dried and a product between the acid and the solvent, such as an ester, is formed.

Abstract: This invention is based upon the unexpected discovery that ethyl lactate can be used as an emulsifying/dispersing excipient for numerous biologically active compounds without destroying the pharmacological activity of the active ingredient. Ethyl lactate proves to be an extremely effective agent for solubilizing biologically active compounds that are difficult to solubilize in conventional excipients. The operability of this invention is predicated on the necessity for the ethyl lactate to be essentially free of peroxide compounds. Such pharmaceutical grade ethyl lactate can be made by reducing the level of peroxide compounds in high purity ethyl lactate by hydrogenation, reduction with a non-catalytic chemical reducing agent, absorption into activated carbon or alumina, or distillation.

Abstract: The present invention relates to the preparation of alicyclic polycarboxylic esters by ring-hydrogenation of the corresponding aromatic polycarboxylic esters on a catalyst which comprises at least one metal from the triad iron, cobalt, nickel, and at least one metal of the IInd, IIIrd, IVth, Vth, and/or VIth transition group of the Periodic Table. An alicyclic carboxylic ester mixture with a proportion above 10 mol % of the trans isomers. The use of the alicyclic polycarboxylic ester mixtures. Mixtures made from plastics and from alicyclic polycarboxylic ester mixtures.

Abstract: A diamine and an epihalohydrin are subjected to ring-opening addition reaction in the presence of water, to thereby produce a tetrahalohydrinamino compound (i.e., halohydrin compound). Thereafter, the halohydrin compound is reacted with an alkali metal hydroxide in the co-presence of a phase-transfer catalyst, to thereby allow cyclization reaction to proceed. An alkali metal halide by-produced during the cyclization reaction is dissolved in water and removed through phase separation. The resultant organic layer is washed with water for phase separation. Then, a crude tetraglycidylamino compound obtained by recovering unreacted epihalohydrin through evaporation is dissolved in an organic solvent and washed with water for phase separation. Subsequently, the organic solvent is recovered through evaporation under reduced pressure with heating, to thereby isolate a tetraglycidylamino compound (i.e., a product of interest).

Abstract: A process for purification of a hydroxycarboxylic acid by distillation, comprising: distilling a hydroxycarboxylic acid solution containing a high-boiling point hydroxy compound comprising at least one species selected from the group consisting of alcohols and phenols having a higher boiling point than the hydroxycarboxylic acid. As a result, a hydroxycarboxylic acid suitable as a starting material for production of a polyhydroxycarboxylic acid can be obtained. The purified hydroxycarboxylic acid is further polycondensed to provide a hydroxycarboxylic acid oligomer, which is de-polymerized to provide a cyclic ester comprising a dimer of the hydroxycarboxylic acid, and the cyclic ester is converted into a polyhydroxycarboxylic acid by ring-opening polymerization thereof.

Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.

Abstract: This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)-(S,S)- or (?)-(R,R)-enantiomer of O,O?-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.

Abstract: A catalyst for producing alkylene oxide including fine metal silver particles dispersed and supported on a carrier, wherein not less than 90% of the fine metal silver particles have silver particle diameters of 2 to 100 nm, is disclosed. The catalyst can be produced by impregnating a carrier with a liquid containing a silver compound or a silver ion; drying the carrier; and then irradiating the carrier with microwave to form fine metal silver particles in dispersed state on the carrier. This catalyst is used for producing olefin oxide by contact gas-phase oxidation of olefin by a molecular-oxygen-containing gas.

Abstract: Disclosed is a method for oxidizing an alcohol in an amide solvent using a mixed reagent containing hydrogen peroxide and a tungsten catalyst.

Abstract: 2,3,3?,4?-biphenyltetracarboxylic acid is heat-dehydrated in a molten state at a temperature not lower than 200° C. in a flow of an inert gas in a reactor 10 having at least one reaction vessel 11 by stirring the molten material to produce 2,3,3?,4?-biphenyltetracarboxylic dianhydride. Thus obtained 2,3,3?,4?-biphenyltetracarboxylic dianhydride in the molten state is subsequently cooled and solidified in an inert gas or dry air, or cooled and solidified in the ambient air at a temperature of 40° C. or lower or 100° C. or higher.

Abstract: There is disclosed an episesamin refining method in which a mixture of sesamin components that contains sesamin, episesamin and the like is brought into contact with an aqueous medium to form a slurried mixture, and thereafter the solids are separated from the mixture or the slurried mixture is dissolved in a suitable aqueous medium under heating and, thereafter, the solution is slowly cooled to recrystallize, thereby yielding an episesamin-enriched composition with an increased relative episesamin content. By the present invention, episesamin can be conveniently and efficiently refined from a mixture of sesamin components that mainly comprises sesamin and episesamin.

Abstract: A process for purifying meloxicam form I from a crude meloxicam, which comprises: i. contacting the crude meloxicam with an amine in a non-aqueous solvent to form a meloxicam salt; ii. isolating the meloxicam salt; iii. dissolving the meloxicam salt in an aqueous solvent to form a salt solution; and iv. adding an acid to the salt solution to precipitate free meloxicam.

Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.

Abstract: There is disclosed a method for producing propylene oxide, which includes: reacting propylene, oxygen, and hydrogen in the presence of a noble metal catalyst and a titanosilicate catalyst in a liquid phase containing a polycyclic compound, which is unsubstituted or substituted with at least one substituent selected from Group B below, wherein the polycyclic compound is composed of two or more identical or different ring compounds selected from Group A below and the ring compounds are fused, directly bonded, or bonded by a linkage group selected from the group consisting of an oxygen atom, carbon chain, and a group composed of oxygen atom(s) and a carbon chain, provided that said polycyclic compound is not a polycyclic compound having hydroxy groups or oxo groups at para or. ortho positions. Group A consisting of benzene, cyclopentadiene, cycloheptatriene, furane, pyrane, cyclopentene, cyclopentane, cyclohexane, cyclohexene, cyclohexadiene, cycloheptane, cycloheptene, and cycloheptadiene.

Abstract: The present invention provides compounds having estrogenic activity selected from the group consisting of RRR-?-tocopherol, hydro-Q9 chromene, coenzyme Q9, cycloartane, 1-Feruloyl glycerol, ?-tocopherol-9, and analogues thereof. The compounds of the present invention activate ER? and ER?, and express high estrogenic activity.

Abstract: A process for producing propylene oxide, which comprises: supplying a solution containing a peroxide selected from the group consisting of hydrogen peroxide and organic hydroperoxide having 2 or more of carbon atoms as a raw material and propylene to an epoxidation step to react the peroxide with propylene, and controlling a concentration of methyl hydroperoxide in the solution to be supplied to the epoxidation step.

Abstract: An object of the present invention is to provide an efficient process for producing an epoxy compound from olefin, oxygen and hydrogen. The process of the present invention is characterized in that an olefin, oxygen and hydrogen are reacted in a liquid phase in the presence of a titanosilicate selected from the group consisting of a crystalline titanosilicate having MEL structure, MTW structure, BEA structure, MWW structure or DON structure, a mesoporous titanosilicate and a lamellar titanosilicate, a noble metal catalyst, and a quinoid compound or a dihydro-form of quinoid compound.