Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-? by adipose tissue.

Abstract: This invention provides compounds of Formula I having the structure wherein: R1 is hydroxyl, alkoxy of 1-4 carbons or —O(CH2)nX; n is an integer of 1-13; X is CONHR6 or CO2R6; R2 is hydrogen, halogen, hydroxyl, alkyl of 1-4 carbons, alkoxy of 1-4 carbons or acyl of 1-4 carbons; R3, R4 and R5 are each independently, hydrogen, halogen, hydroxyl, alkyl of 1-4 carbons, alkoxy of 1-4 carbons, acyl of 1-4 carbons, CF3, OCF3, SO2NHR6, NR6R7 or CO2R6; R6, and R7 are each independently, hydrogen, alkyl of 1-4 carbons, or alkylaryl where the aryl group is substituted with R2; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: The invention includes selected novel optically active ?-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

Abstract: Compounds having Formula I or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.

Abstract: A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising: a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane-diacetic acid to yield 3,3-pentamethylene glutarimide; b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.

Abstract: The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity.

Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.

Abstract: The present invention relates to a process for preparing (cyclo)aliphatic diisocyanates and triisocyanates corresponding to the formula R—(NCO)n??(I), wherein R represents a (cyclo)aliphatic hydrocarbon group having up to 15 carbon atoms, provided that there are at least two carbon atoms between two nitrogens, n represents the number 2 or 3, by a) separately heating phosgene and a diamine or triamine corresponding to the formula R—(NH2)n??(II), ?to a temperature of 200° C. to 600° C., wherein the amine may optionally be diluted with an inert gas or with the vapors of an inert solvent, b) optionally passing the reactants over torque-producing baffles and c) continuously reacting phosgene and the amine in the gas phase in a reaction chamber without moving parts and with constrictions of the walls in the region of the reaction zone.

Abstract: The compounds of the instant invention are bicyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, and sleep disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.

Abstract: Process for the carbonylation of a conjugated diene by reacting the conjugated diene with carbon monoxide and an hydroxyl group containing compound in the presence of a catalyst system based on: (a) a source of palladium cations, (b) a diphosphine ligand, and (c) a source of anions, wherein the diphosphine ligand is a ligand having the general formula I wherein x1 and x2 represent a cyclic group with at least 5 ring atoms, of which one is a phosphorus atom, and R represents a bivalent aliphatic bridging group, connecting both phosphorus atoms, containing from 2 to 4 atoms in the bridge, which is substituted with at least one substituent or R represents a phenyl group with both phosphorus groups bound to the 1,2-position.

Abstract: A process for producing trimellitic acid which comprises step A for oxidizing pseudocumene, thereby obtaining a reaction mixture comprising dimethyl benzoic acid, dimethyl benzyl alcohol, and dimethyl benzaldehyde, step B for separating dimethyl benzoic acid, dimethyl benzyl alcohol and dimethyl benzaldehyde from the reaction mixture obtained in step A, step C for oxidizing dimethyl benzyl alcohol separated in step B, thereby obtaining dimethyl benzoic acid and dimethyl benzyl aldehyde and then feeding dimethyl benzoic acid and dimethyl benzyl aldehyde thus obtained to step B, and step D for oxidizing dimethyl benzoic acid and/or dimethyl benzaldehyde separated in step B, thereby obtaining trimellitic acid.

Abstract: A natural inexpensive acyclic monoterpene ketone (dihydrotagetone) of formula (4), isolated from the oil of Tagetes sp., was smoothly oxidized with meta-periodate/potassium permanganate into 2,6-dimethyl-4-oxo-heptanoic acid of formula (3), the reduction of 3 with metal hydride such as sodium borohydride or lithium aluminium hydride provided 4-hydroxyacid of formula (2) which on without isolation undergone lactonisation in acidic medium furnished two chiral centered 5-isobutyl-3-methyl-4,5-dihydro-2(3H)-furanone of formula (1) as an analogue of whisky lactone 5-butyl-4-methyl-4,5-dihydro-2(3H)-furanone of formula (1a) responsible for high quality of alcoholic beverage (whisky, wine, brandy and scotch), in addition, coconut flavoured 5-butyl-4-methyl-4,5-dihydro-2(3H)-furanone of formula (1) is also as an analogue of coconut aldehyde (&ggr;-nonalactone, F.E.M.A. No. 2751) of formula (1b) which is responsible for flavouring a wide range of food stuffs including baked goods and confectionery.

Abstract: A novel process for the purification of crude aromatic carboxylic acids, such as, for example, terephthalic acid, orthophthalic acid, trimesic acid, isophthalic acid, 2,6-naphthalenedicarboxylic acid and pyromellitic acid, which are obtained by oxidising the corresponding aromatic precursors is described; the process is based on the subsequent oxidation in heterogeneous phase of the crude product in aqueous solution.

Abstract: The invention relates to a process for the production of isocyanates by reaction of primary amines with phosgene, in which isocyanate is used as solvent, wherein some or all of isocyanate used as solvent is added to the reaction mixture only after the amine and phosgene have been physically combined.

Abstract: A first process for producing an optically active perfluoroalklylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybotanoic aryl ester derivatives.

Abstract: The present invention provides a method for the preparation of carbonaceous materials comprising a plurality of gamma-keto-carboxyl containing functional groups surface bonded thereto, and further provides several surface modified carbonaceous materials resulting therefrom.

Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.

Abstract: The present invention provides alkyl-substituted tetracyclododecenecarboxylic acid esters presented by the general formula (I): wherein R1 is an alkyl group having 1 to 4 carbon atoms and R2 is a hydrocarbon group having 1 to 12 carbon atoms. Further, the represent invention provides (meth)acrylic acid addition products of alkyl-substituted tetracyclododecenecarboxylic acid esters represented by the general formula (II): wherein R1 is an alkyl group having 1 to 4 carbon atoms, R2 is a hydrocarbon group having 1 to 12 carbon atoms, and R3 is a hydrogen atom or a methyl group.

Abstract: The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): The compound according to the present invention is useful for efficient syntheses of 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acids.

Abstract: A method for producing D-allo-isoleucine is provided. The method comprises converting L-isoleucine to the corresponding hydantoin. A mixture containing the hydantoin is contacted with a D-hydantoinase to stereoselectively hydrolyze any D-allo-isoleucine hydantoin in the mixture to the corresponding N-carbamoyl-D-allo-isoleucine. The N-carbamoyl-D-allo-isoleucine is decarbamoylated to produce D-allo-isoleucine. Preferably the contacting of the hydantoin with a D-hydantoinase is carried out under conditions permitting the simultaneous epimerization of the chiral center at C-5 of the hydantoin.