Abstract: The present invention describes compounds of Formula I or a pharmaceutically acceptable salts or derivatives thereof. Compositions comprising compounds of Formula I are also described. The present invention further relates to a method of producing non-2-enonate compounds.

Abstract: Phycotoxins are purified from a mixture of phycotoxins produced in a continuous process. Cyanobacteria are produced in a continuous culture, then lyzed, the cells pelleted and extracted, and the extract purified using an organic solvent-aqueous mixture and repeated passage through a diatomaceous earth column. The column is washed with acetic acid, then the neosaxitoxin extracted with an alcohol-water mixture. The eluate is passed through activated charcoal columns, which are washed with distilled water to remove the retained pigments and impurities, the further purified by HPLC. In one embodiment, the process produces only neosaxitoxin and saxitoxin. In another embodiment, the process produces only GTX2/3.

Abstract: The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlab™. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.

Abstract: Disclosed is a process of carrying out a Michael reaction with recovery of the catalyst, where a compound of formula (1): is reacted with a compound of formula (2): in the presence of a catalyst of formula (4): where the compounds of formulae (1) and (2) undergo a Michael reaction.

Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.

Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of antidepressants.

Abstract: A process for preparing a cyclic tertiary amine of the formula I where A is a C4-alkylene group, a C5-alkylene group or a —(CH2)2—B—(CH2)2— group, where B is oxygen (O) or an N—R1 radical and R1 is C1-C5-alkyl, aryl or C5-C7-cycloalkyl, and the radical R2 is a linear or branched C2-C16-alkyl, C5-C7-cycloalkyl or C7-C20-aralkyl, in which (i) an amino alcohol II from the group consisting of 1,4-aminobutanol, 1,5-aminopentanol, aminodiglycol (ADG) and aminoethylethanolamine of the formula IIa where R1 is as defined above or hydrogen (H), in which case R1=R2 in the amine I, is reacted with a primary or secondary alcohol R2OH (III) at a temperature in the range from 150 to 270° C. in the liquid phase in the presence of a copper-comprising heterogeneous catalyst in a reactor.

Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.

Abstract: An organic semiconductor thin film including an organic semiconductor material that is easily synthesized, and is chemically and physically stable, and shows a high carrier mobility, an organic semiconductor device and an organic field effect transistor including the organic semiconductor thin film are provided. An organic semiconductor thin film of the invention includes a compound represented by the following formula 1: wherein, in formula (1), X is oxygen, sulfur or selenium.

Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: A compound having a structure of: wherein X is S, SO, SO2, NR10, O, or Se; R1-R8 are each individually H, amino, alkynyl, substituted alkynyl, halogen, alkyl, aryl, substituted alkyl, substituted aryl, nitro, alkoxy, substituted alkoxy, cyano, thiol, substituted thiol, thioether, hydroxyl, heteroaryl, substituted heteroaryl, cycloalkyl, or substituted cycloalkyl, or R1 and R2 together form an aromatic ring and R5 and R6 together form an aromatic ring; and R10 is selected from H, amino, alkynyl, substituted alkynyl, halogen, alkyl, aryl, substituted alkyl, substituted aryl, nitro, alkoxy, substituted alkoxy, cyano, thiol, substituted thiol, thioether, hydroxyl, heteroaryl, substituted heteroaryl, cycloalkyl, or substituted cycloalkyl.

Abstract: The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.

Abstract: A novel process is described for the synthesis of Sitagliptin, IUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1 2,4-triazolo[4,3-a]pyrazine, of formula (I).

Abstract: Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.

Abstract: A method for producing furfural from lignocellulosic biomass material is provided, comprising (a) contacting the lignocellulosic biomass material with a mixture comprising water and an organic acid at a temperature of at least 100° C. and a pressure of at most 10 bar (absolute) to obtain a first liquid stream comprising hydrolyzed hemicellulose and a second stream comprising lignin and cellulose; (b) maintaining the first liquid stream comprising hydrolyzed hemicellulose at a temperature of at least 130° C. to obtain a second liquid stream comprising furfural; and (c) separating the furfural obtained in step b) from the second liquid stream.

Abstract: The benzo[d]imidazole derivatives of piperidine and piperazine are 5-piperazinyl and 5-piperadinyl-1H-benzo[d]imidazol-2(3H)-ones that exhibit D2 and 5-HT1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: where X is carbon or nitrogen and R is a selected biaryl group, or a pharmaceutically acceptable salt thereof. The piperidinyl compounds are prepared by removal of the Boc group from tert-Butyl-4-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carboxylate. Subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The piperazinyl compounds are prepared by preparation of the intermediate tert-Butyl 4-(3,4-diaminophenyl)piperazine-1-carboxylate.

Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.

Abstract: The present invention provides Crystalline Forms of 4-acetoxy-2?-benzoyloxy-5?-20-epoxy-1-hydroxy-7?,10?-dimethoxy-9-oxotax-11-en-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate, i.e Cabazitaxel. The present invention also discloses methods for the preparation of Crystalline Forms of Cabazitaxel and pharmaceutical compositions thereof.

Abstract: The present invention is directed to an improved process for the preparation of sulfamide derivatives.