A method of isolating ginkgolides from the leaves of the ginkgo tree and purifying them

УСТРОЙСТВО ДЛЯ ПОЛУЧЕНИЯ ТЕРМИЧЕСКИ НЕСТАБИЛЬНЫХ АНГИДРИДОВ ОРГАНИЧЕСКИХ КИСЛОТ

Устройство для получения термически нестабильных ангидридов органических кислот, характеризующееся тем, что оно содержит реактор термолиза с аксиальной линией подачи органической кислоты из бункера-дозатора и радиальной линией подачи в его верхнюю часть подогретого газа-носителя из нагревателя, вход которого подсоединен к узлу подачи газа-носителя, холодильник с линией подвода хладоагента, сепаратор, контур регулирования температуры нагревателя, состоящий из последовательно соединенных датчика температуры на выходе нагревателя, регулятора расхода теплоносителя и исполнительного клапана на линии подачи теплоносителя в нагреватель, контур регулирования соотношения расходов органической кислоты и газа-носителя в реактор, состоящий из последовательно соединенных датчика температуры на выходе реактора, регулятора расхода газа-носителя в нагреватель и исполнительного клапана на линии подачи газа-носителя в нагреватель, и контур регулирования температуры холодильника, состоящий из последовательно соединенных датчика температуры на выходе холодильника, регулятора расхода хладоагента и исполнительного клапана, при этом выход реактора подключен к холодильнику, линия отвода охлажденных продуктов реакции которого подсоединена к входу сепаратора с линиями отвода газовой фазы продукта, жидкой водной фазы продукта и жидкой неводной фазы целевого продукта. И 1 138568 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ ВУ” 138 568” 44 ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ИЗВЕЩЕНИЯ К ПАТЕНТУ НА ПОЛЕЗНУЮ МОДЕЛЬ ММ9К Досрочное прекращение действия патента из-за неуплаты в установленный срок пошлины за поддержание патента в силе Дата прекращения действия патента: 24.10.2018 Дата внесения записи в Государственный реестр: 01.08.2019 Дата публикации и номер бюллетеня: 01.08.2019 Бюл. №22 Стр.: 1 па 8 9948$ ЕП

Pest controlling composition

The present invention provides a pest controlling composition comprising, as active ingredients, an amide compound of the formula (I) and a pyrethroid compound; and so on.

Method and apparatus for preparing hydroxymethylfurfural

In an embodiment of the invention, an apparatus for preparing hydroxymethylfurfural (HMF) is provided. The apparatus includes a reaction area including a first organic layer including sugar and a solvent and a second organic layer including a solvent mixture with azeotropy and extractability, a boiling area including a mixing solution formed by the hydroxymethylfurfural and the solvent mixture, connected with the reaction area, and a distilling area including water and a liquid layer including the solvent mixture, connected to the reaction area. In another embodiment of the invention, a method for preparing hydroxymethylfurfural (HMF) is provided.

Hydrogenation process for the preparation of tetrahydrofuran and alkylated derivatives thereof

A process is provided for the synthesis of tetrahydrofuran and related compounds by hydrogenation of furan and derivatives, using a sponge nickel catalyst that has been promoted with iron and chromium.

Methods of making lubiprostone and intermediates thereof

There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)

Method for the synthesis of 5-alkoxymethyl furfural ethers and their use

Method for the manufacture of 5-alkoxymethylfurfural derivatives by reacting a fructose and/or glucose-containing starting material with an alcohol in the presence of a catalytic or sub-stoechiometric amount of heterogeneous acid catalyst. The catalysts may be employed in a continuous flow fixed bed or catalytic distillation reactor. The ethers can be applied as a fuel or fuel additive.

Combined use of two insecticides

The present disclosure relates to the combined use of two pesticides. A first pesticide composition provides an initial contact kill, and may form a barrier when applied to greasy surfaces. A second pesticide composition provides residual pesticidal activity on the surface. Methods of making and using the pesticide compositions are also provided.

Novel 3.2.1-bicyclo-octane compounds

The present invention relates to novel compounds and their use in fragrance compositions. Novel 3.2.1-bicyclo-octane compounds of the present invention are represented by formula: wherein R is selected from the group consisting of carbonyl and [1,3]dioxolane; R′ is selected from the group consisting of hydrogen and allyl; or R and R′ taken together represent

Organic Compounds Having Cooling Properties

Provided are compounds of formula (I) wherein m is 0, 1 or 2; R I is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R 2 is selected from hydrogen, methyl and ethyl; I) R 3 is hydrogen, methyl, or ethyl; and R 4 and R 5 are independently selected from ethyl and isopropyl; and R 3 , R 4 and R 5 together have at least 6 carbon atoms: or II) any two or all of R 3 , R 4 and R 5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.

Light-emitting device material and light-emitting device

Embodiments provide a light emitting device material characterized by containing an anthracene compound represented by the following general formula. where R 19 to R 37 are a hydrogen atom, alkyl group, cycloalkyl group, heterocyclic group or the like; n is 1 or 2; and A is a heteroarylene group or arylene group. Any one of the R 19 to R 27 and any one of the R 28 to R 37 are used for linking with A. The present teachings allow a light emitting device having high luminous efficiency and excellent durability.

Method for synthesis of secondary alcohols

A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.

Ruthenium (ii) catalysts for use in stereoselective cyclopropanations

Chiral ruthenium catalysts comprising salen and alkenyl ligands are provided for stereoselective cyclopropanation, and methods of cyclopropanation are provided. The chiral ruthenium catalyst is prepared in situ by combining an alkenyl ligand, a deprotonated chiral salen ligand, and a ruthenium (II) metal. A preferred catalyst is prepared in situ by combining 2,3-dihydro-4-venylbenzofuran, deprotonated 1,2-cyclohexanediamino-N,N′-bis(3,5-di-t-butyl-salicylidene) and RuCl 2 (p-cymene)] 2 .

(e)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine and process for producing the same and process for producing (e,z)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine

The present invention provides a process for producing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine represented by Formula (1); wherein R is a C 1-4 alkyl, the method comprising the steps of: maintaining a solution containing (Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine dissolved therein at 25° C. or below to deposit crystals and separating crystals having a particle diameter of 100 μm or less from the deposited crystals; and a process for producing (E,Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine comprising the steps of: reacting an alkali metal salt of β-oxo-β-(2-thienyl)propanal with a monoalkylamine compound; adding a water-insoluble organic solvent to the resulting reaction mixture; adding seed crystals containing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine to an organic layer obtained by conducting separation; and keeping the resulting mixture at 25° C. or below.

Second-order nonlinear optical compound and nonlinear optical element comprising the same

Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a π-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.

Stilbene Compound, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

An object is to provide a novel stilbene compound suitable for an organic EL light-emitting material. Provided is a novel stilbene compound represented by a general formula (G1) below. In the formula, Q 1 and Q 2 separately represent an oxygen atom or a sulfur atom; R 1 to R 9 and R 11 to R 17 separately represent any one of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, and a substituted or unsubstituted biphenyl group; α 1 to α 6 separately represent a substituted or unsubstituted phenylene group; Ar 1 and Ar 2 separately represent any one of a substituted or unsubstituted aryl group having 6 to 12 carbon atoms forming a ring, a substituted or unsubstituted dibenzothiophen-2-yl group, and a substituted or unsubstituted dibenzofuran-2-yl group; and j, k, m, n, p, and q separately represent 0 or 1.

Processes for the production of hydrogenated products

A process for making a hydrogenated product includes providing a clarified DAS-containing fermentation broth, distilling the broth to form an overhead that includes water and ammonia, and a liquid bottoms that includes MAS, at least some DAS, and at least about 20 wt % water, cooling and/or evaporating the bottoms, and optionally adding an antisolvent to the bottoms, to attain a temperature and composition sufficient to cause the bottoms to separate into a DAS-containing liquid portion and a MAS-containing solid portion that is substantially free of DAS, separating the solid portion from the liquid portion, recovering the solid portion, hydrogenating the second solid portion in the presence of at least one hydrogenation catalyst to produce the hydrogenated product comprising at least one of THF, GBL or BDO, and recovering the hydrogenated product.

Aryloxyanilide imaging agents

The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.

Processes for the synthesis of bazedoxifene acetate and intermediates thereof

Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.

Insecticidal Compositions Suitable for Use in Preparation of Insecticidal Granular Fertilizer and Insecticidal Formulations

Insecticidal compositions suitable for use in preparation of insecticidal granular fertilizer and insecticidal formulations comprising a pyrethroid and a glycol present in a concentration of from 40.0% by weight to 99.0% by weight based upon the total weight of all components in the composition is disclosed.

Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.

Production of liquid fuels (sylvan-liquid-fuels) from 2-methylfuran

The present invention describes a procedure for the production of liquid fuel having a content high in alkanes and low in oxygenated compounds, comprising as a minimum: —a first step of alkylation of 2-methylfuran (commonly denominated Sylvan) with a furan alcohol 2 having the formula: (2), wherein R 1 is H or an aliphatic or aromatic or heteroaromatic moiety, R 2 is H or an aliphatic or aromatic or heteroaromatic moiety, and R 3 is H, hydroxymethyl or an aliphatic or aromatic or heteroaromatic moiety, in the presence of a catalyst, —a second step of hydrogenation and dehydration of the compound obtained in step 1 in the presence of hydrogen, utilising suitable hydrogenation and dehydration catalysts.

Process for the preparation of dronedarone

The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.

Bis-phosphate compound and asymmetric reaction using the same

A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds. Thus, the invention enables an industrially feasible method for the production of optically active amidoaldehydes, optically active β-amino acid derivatives, optically active diamine compounds, optically active pyrrolidine derivatives and optically active dihydropyran derivatives which are useful as products such as medicines, agricultural chemicals and chemical products as well as synthesis intermediates for such products.

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

METHODS AND COMPOSITIONS FOR CONTROL OF GYPSY MOTH, Lymantria dispar

The invention provides in part dialkoxybenzene and eugenol compounds for controlling infestation by a Lymantria dispar , and methods thereof. The compounds include a compound of Formula I: where R1 may be methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; R2 may be at positions 2, 3 or 4 and may be H, methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; and R3 may be optionally present at positions 2, 3 and 4, and is allyl; with the provisos that when R2 is at position 2, R3 if present is at position 3, or when R2 is at position 3, R3 if present is at positions 2 or 4, or when R2 is at position 4, R3 if present is at position 2; or of Formula II: where R1 may be methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; or mixtures thereof.

COMPOUNDS FOR TREATING PROTEIN FOLDING DISORDERS

The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis. 112-. (canceled)1427-. (canceled)28. The method of claim 13 , wherein Dis N(R) and wherein each Ris independently selected from the group consisting of hydrogen and optionally substituted C-Calkyl.2932-. (canceled)33. The method of claim 28 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.34. The method of claim 33 , wherein Gis benzothiazolyl claim 33 , benzoxazolyl claim 33 , benzimidazolyl claim 33 , benzothiophenyl claim 33 , and benzofuranyl claim 33 , each optionally substituted.3646-. (canceled)47. The method of claim 35 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.48. The method of claim 47 , wherein Gis benzothiazolyl claim 47 , benzoxazolyl claim 47 , benzimidazolyl claim 47 , benzothiophenyl claim 47 , and benzofuranyl claim 47 , each optionally substituted.5065-. (canceled)70. The method of claim 13 , wherein the condition is associated with a dysfunction in the proteostasis of a protein selected from the group consisting of hexosamine A claim 13 , cystic fibrosis transmembrane conductance regulator claim 13 , aspartylglucsaminidase claim 13 , a-galactosidase A claim 13 , cysteine transporter claim 13 , acid ceremidase claim 13 , acid α-L-fucosidase claim 13 , protective protein claim 13 , cathepsin A claim 13 , acid β-glucosidase claim 13 , acid β-galactosidase claim 13 , iduronate 2-sulfatase claim 13 , α-L-iduronidase claim 13 , galactocerebrosidase claim 13 , acid α-mannosidase claim 13 , acid β-mannosidase claim 13 , arylsulfatase B claim 13 , arylsulfatase A claim 13 , N-acetylgalactosamine-6-sulfate sulfatase claim 13 , acid β-galactosidase claim 13 , N-acetylglucosamine-1-phosphotransferase claim 13 , acid sphingmyelinase ...

2-PHENYL BENZOYLAMIDES

Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein. 2. A compound according to wherein Ris —C(O)—N—RRand q is 0.5. A compound according to wherein p is 0 and Ris hydrogen or (C-C)alkyl.6. A compound according to wherein Ris —C(O)—O—(C-C)alkyl.7. A compound according to wherein m and n are each independently 0 or 1 and Rand Rare each independently (C-C)alkyl claim 6 , (C-C)alkoxy or trifluoromethyl.8. The compound:Ethyl (1R)-1-({2-[3-(Dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 1-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate:Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[5-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[6-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxy-5-methylbiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl ...

CRYSTALLINE HYDROCHLORIDE SALT OF DARUNAVIR

The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it. 1. A crystalline hydrochloride salt of darunavir.2. The crystalline hydrochloride salt of darunavir according to claim 1 , which is characterized by peaks in the powder x-ray diffraction spectrum having 2θ angle positions at about 6.7 claim 1 , 8.0 claim 1 , 13.1 claim 1 , 13.9 claim 1 , 14.9 claim 1 , 19.6 claim 1 , 19.9 claim 1 , 24.5 and 27.9±0.2 degrees.3. The crystalline hydrochloride salt of darunavir according to claim 1 , which is characterized by an x-ray powder diffractogram as shown in .4. A process for the preparation of crystalline hydrochloride salt of darunavir as defined in claim 1 , which comprises:a. providing a solution of darunavir in a solvent;b. adding hydrochloric acid to the solution obtained in step (a);c. slurrying the reaction mass obtained in step (b) at below 40° C.; andd. isolating crystalline hydrochloride salt of darunavir.5. The process according to claim 4 , wherein the solvent used in step (a) is a solvent or mixture of solvents selected from the group consisting of water; a halogenated hydrocarbon solvents are dichloromethane claim 4 , chloroform claim 4 , carbontetrachloride and ethylene dichloride; an ester solvents are ethyl acetate claim 4 , methyl acetate claim 4 , isopropyl acetate claim 4 , tert-butyl methyl acetate and ethyl formate; a ketonic solvents are acetone claim 4 , methyl ethyl ketone claim 4 , methyl isobutyl ketone and diethyl ketone; an ether solvents are tetrahydrofuran claim 4 , 1 claim 4 ,4-dioxane claim 4 , methyl tert-butyl ether claim 4 , diisopropyl ether and diethyl ether.6. The process according to claim 5 , wherein the solvent is water claim 5 , dichloromethane claim 5 , ethyl acetate claim 5 , methyl ...

PROSTAGLANDIN SYNTHESIS AND INTERMEDIATES FOR USE THEREIN

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: 2. Compound A according to wherein R represents a substituted phenyl group.3. Compound A according to wherein R represents p-methoxyphenyl5. Compound B according to wherein R′ represents p-methoxybenzyl. This invention relates to prostaglandin analogs and their synthesis. More particularly, it relates to a novel, simplified synthesis of prostaglandin analogs, and novel chemical compounds useful as intermediates in such synthesis.Prostaglandins (PGs) are organic carboxylic acids, namely cyclopentanes carrying two side chain substituents, typically linear C6-C8 side chains, bonded to adjacent positions on the cyclopentane nucleus. One of the side chains, the α-side chain, carries a terminal carboxylic acid group. Many are natural products found in mammalian organs and tissues (primary PGs), and exhibit a variety of physiological activities. Primary PGs generally have a prostanoic acid skeleton, which forms the basis of the nomenclature:A significant number of synthetic PG analogs have been made and found to have useful pharmacological properties. These may have modified skeletons, and substituted and unsaturated side chains. PGs are characterized by a hydroxyl (or ketone) substituent on the cyclopentane nucleus, position 9.Prostaglandin analogs are difficult to synthesize. Complications arise because of the requirements of the end products to have several functional groups and two side chains of significant size and complexity. Stereospecificity is commonly required, for substituent groups and for bonds in the core. Since the products are intended for pharmaceutical use, the range of industrially acceptable reagents, solvents, catalysts, etc. which can be used in their synthesis is limited to those having pharmaceutical industry acceptability.A common starting material for PG analog ...

PREPARATION PROCESS OF DRONEDARONE AND ITS SALTS

A process is provided for preparing dronedarone or pharmaceutically acceptable salts thereof. The process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran (compound A) with methanesulfonyl chloride without any catalyst to provide crude dronedarone hydrochloride, which is purified to afford highly pure product. Then, the dronedarone hydrochloride can be converted to highly pure dronedarone through treatment with an alkaline solvent, the dronedarone can be further converted to other pharmaceutically acceptable salts of dronedarone. In this process, acylation between compound A and methanesulfonyl chloride is carried out successfully and the formation of the dimethylsulfonyl by-product is inhibited. 1. A process for preparing dronedarone hydrochloride , wherein the process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran with methanesulfonyl chloride to provide dronedarone hydrochloride , wherein no catalyst is added to the reaction.2. The process according to claim 1 , wherein the reaction between 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran and methanesulfonyl chloride is carried out in one solvent or a mixture of multiple solvents.3. The process according to claim 2 , wherein the solvents are selected from the group consisting of a nitrile claim 2 , ketone claim 2 , halogenated hydrocarbon claim 2 , ether and aromatic hydrocarbon.4. The process according to claim 2 , wherein the mixture comprises two or more solvents of the same or different kinds selected from the group consisting of a nitrile claim 2 , ketone claim 2 , halogenated hydrocarbon claim 2 , ether and aromatic hydrocarbon.5. The process according to claim 3 , wherein the nitrile is selected from the group consisting of C2˜C6 aliphatic nitriles.6. The process according to claim 3 , wherein the ketone is selected from the group consisting of C3˜C6 aliphatic ketones.7. The process according to claim 3 , wherein the ...

NEURO-PROTECTIVE EFFECTS OF ADELOSTEMMA GRACILLIMUM AND ITS ISOLATED COMPOUNDS

Isolated compounds from refined fractions and compositions containing the compounds are provided by the present invention. refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention. 10. The compound of claim 9 , wherein Ris H.11. The compound of claim 9 , wherein{'sup': '1', 'Ris H;'}{'sup': 2', '3, 'each of Rand Rare Me; and'}subscript n is 10.1514. A pharmaceutical composition for treating a neurodegenerative disease or neuropathological condition in a subject claims 1 , the composition comprising a compound of any one of - and a pharmaceutically acceptable carrier or excipient.16Adelostemma gracillimum. A method of preparing a refined fraction claims 1 , the method comprising:{'i': 'Adelostemma gracillimum', 'contacting herb with an alcohol selected from the group consisting of methanol and ethanol, to form an alcohol extract;'}contacting the alcohol extract with an organic solvent to form an organic solvent fraction; and{'i': 'Adelostemma gracillimum', 'contacting the organic solvent fraction with a petroleum ether to form the refined fraction.'}17. The method of claim 16 , further comprising:{'i': 'Adelostemma gracillimum', 'eluting a first fraction of the refined fraction from a resin column with a solution of about 30% ethanol in water;'}eluting a second fraction from the resin column with a solution of about 60% ethanol in water; andeluting a third fraction from the resin column with a solution of about 96% ethanol in water.18Adelostemma gracillimum. An refined fraction prepared by the method of .19Adelostemma gracillimum. An refined fraction prepared by the method of .20Adelostemma gracillimum. A method of improving memory in a subject claim 17 , ...

ETOMIDATE ANALOGUES THAT DO NOT INHIBIT ADRENOCORTICAL STEROID SYNTHESIS

The invention is directed to compounds according to formula (I): where Ris LC(O)OT or LC(O)OLC(O)OT; Ris a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, or R; n is an integer from 0 to 5; each Ris independently halogen or R; Rand Rare independently H, halogen, CN or CF; Land Lare each independently a bond, a substituted or unsubstituted C-Calkylene, C-Calkenylene, or C-Calkynylene; and T is H, a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition. 2. The compound of claim 1 , wherein said compound is present in the form of a pure enantiomer.3. The compound of claim 2 , wherein said enantiomer is the R enantiomer.4. The compound of claim 1 , wherein Ris LC(O)OT.5. The compound of claim 1 , wherein Ris LC(O)OLC(O)OT.6. The compound of claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCHand CHCHCH.7. The compound of claim 1 , wherein T is selected from the group consisting of H claim 1 , CH claim 1 , CHCH claim 1 , CHCH(OH)CH claim 1 , and CHCHCH.8. The compound of claim 1 , wherein n is 0 or 1.9. The compound of claim 1 , wherein Ris CH claim 1 , n is 0 claim 1 , Lis a bond claim 1 , and T is H claim 1 , CH claim 1 , CHCH claim 1 , or CHCH(OH)CH.10. The compound of claim 1 , wherein both Rand Rare H.11. The compound of claim 1 , wherein at least one of Rand Ris H and the other is Br or CN.12. The compound of claim 11 , wherein Ris H and Ris Br or CN.13. The compound of claim 11 , wherein Ris Br or CN and Ris H.15. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of and a pharmaceutically acceptable carrier.16. A method for providing anesthesia to a subject comprising administering to said ...

PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES

An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture. 15-. (canceled)61. A process for producing crystals of (S)—N-[2-(1 ,6 ,7 ,8-tetrahydro-2H-indeno[5 ,4-b]furan-8-yl)ethyl]propionamide , comprising step (a): a step for propionylating the amino group of (S)—N-[2-(1 ,6 ,7 ,8-tetrahydro-2H-indeno[5 ,4-b]furan-8-yl)ethylamine or a salt thereof obtained in the process according to claim , and step (b): a step for crystallizing by adding aqueous solvent to the reaction solution obtained in step (a).9. The crystals according to or , wherein the content of the compound represented by formula (I) is 0.10% by weight or less.13. The crystals according to or the composition according to , which is prepared on a commercial scale.14. A process for producing 1 ,2 ,6 ,7-tetrahydro-8H-indeno[5 ,4-b]furan-8-one , comprising a step for reducing 4 ,5-dibromo-1 ,2 ,6 ,7-tetrahydro-8H-indeno[5 ,4-b]furan-8-one with Pd—C catalyst under the condition:hydrogen pressure (MPa)>−0.02×gas-liquid overall mass transfer volume coefficient (1/hr)+0.43.15. Use of the crystals according to for the manufacture of a preventive or therapeutic agent for sleep disorder.16. The composition according to which is a preventive or therapeutic agent for sleep disorder.17. A method for the prevention or treatment of sleep disorder claim 10 , comprising administering the crystals according to or the composition according to . The present invention relates to a process for production of an optically active amine derivative having high purity, ...

Complexes of Ruthenium, Method of Production Thereof And Use Thereof As (Pre)Catalysts of the Metathesis Reaction

The present invention provides ruthenium complexes of the formula 111-. (canceled)13. The complex of claim 12 , wherein X and X′ are chlorine.14. The complex of claim 12 , wherein Ris hydrogen.15. The complex of claim 12 , wherein A is nitrogen.16. The complex of claim 12 , wherein A is carbon with an Rgroup.17. The method for preparing the ruthenium complex of which comprises reacting 8-ethenylquinoline with a Ru carbene catalyst.19. The method of claim 17 , wherein the Ru carbene catalyst comprises an indenylidene residue claim 17 ,20. The method according to claim 17 , wherein the reaction is conducted in the presence of a copper(I) salt.21. The method according to claim 20 , wherein the copper(I) salt is copper(I) chloride.22. The method according to claim 17 , wherein the reaction is performed in a chlorinated solvent claim 17 , an aliphatic solvent claim 17 , a cycloaliphatic solvent or an aromatic hydrocarbon solvent claim 17 , or mixtures thereof.24. An improved process for ring closing metathesis (RCM) claim 12 , wherein the improvement comprise the use of the ruthenium complex of as an initiator or (pre)catalyst.25. An improved process for ring-opening metathesis polymerization (ROMP) claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst.26. An improved process for metathesis of “alkene-alkyne” (ene-yne) type claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst. This application is a continuation application of U.S. patent application Ser. No. 12/303,615, filed Apr. 3, 2009, which in turn is a national stage application of PCT Application No. EP2007/004901, filed Jun. 1, 2007. The disclosures of the above-referenced applications are hereby incorporated by reference into the present disclosure.The invention relates to novel metal complexes with formula 1, whereCompounds of formula 1 occur as two isomers: with formula 1a, in which atoms X ...

PESTICIDAL MIXTURES CONTAINING ISOXAZOLINE DERIVATIVES AND INSECTICIDE OR NEMATOICIDAL BIOLOGICAL AGENT

The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A, A, R, R, R, Rand Rare as defined in claim and one of Yand Yis S, SO or SOand the other is CHand component B is an insecticide or nematicidal biological agent as defined in claim . The present invention also relates to methods of using said mixtures for the control of pests. 2. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis S and the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.3. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis SO and the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.4. A pesticidal mixture according to claim 3 , wherein the molar proportion of the cis SO compounds of formula I compared to the total amount of cis SO and trans SO compounds of formula I is greater than 50%.5. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis SOand the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.6. A pesticidal mixture according to claim 1 , wherein when L is a direct bond Yis CHand Yis S claim 1 , SO or SO claim 1 , and wherein when L is methylene Yis S claim 1 , SO or SOand Yis CH.8. A pesticidal mixture according to claim 1 , wherein component B is a compound selected froma) a pyrethroid selected from the group consisting of permethrin, cypermethrin, fenvalerate, esfenvalerate, deltamethrin, cyhalothrin, lambda-cyhalothrin, gamma-cyhalothrin, bifenthrin, fenpropathrin, cyfluthrin, tefluthrin, ethofenprox, ...

HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS

Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed. 1. A process for the selective bromination of a (2−)Calkylbenzofuran to form 3-bromo-2-alkylbenzofuran in high purity , said process comprising contacting a (2−)(Calkyl)-benzofuran with less than 1.2 equivalents of bromine in a non-halogenated , polar , aprotic solvent at a temperature greater than −5° C. , and recovering the brominated reaction product.2. The process of conducted at a temperature from 0 to 20° C.3. The process of wherein the solvent comprises an alkyl ester of an aliphatic or aromatic carboxylic acid having a total of up to 12 carbons.4. The process of wherein the solvent is ethyl acetate. This application is a divisional application of the U.S. patent application Ser. No. 12/299,519, filed on Nov. 4, 2008, entitled “HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS,” and which is a 371 national phase of PCT application number PCT/US07/07882, filed on Mar. 29, 2007, which claims the benefit of U.S. Provisional Patent Application No. 60/798,108, filed on May 5, 2006, the teachings of which are incorporated by reference herein, as if reproduced in full hereinbelow.This invention is directed to certain hafnium complexes, to catalyst compositions comprising the same, and to addition polymerization processes, especially olefin polymerization processes, using such hafnium complexes as one component of a coordination polymerization catalyst composition.Advances in polymerization and catalysis have resulted in the capability to produce many new polymers having improved physical and chemical properties useful in a wide variety of superior products and applications. With the development of new catalysts the choice of polymerization-type (solution, slurry, high pressure or gas phase) for producing a particular polymer ...

Method for the manufacture of furan compounds for renewable primary products

Method for the manufacture of furan compounds by using a heterogeneous catalyst in aqueous solution.

ESTER COMPOUND AND USE THEREOF

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

PYRETHRINOID-TYPE ESTERS AS PESTICIDES

An ester compound represented by formula (1): wherein Rrepresents Rrepresents 2-propenyl or 2-propynyl; Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of ...

Biguanide Compositions and Methods of Treating Metabolic Disorders

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 2. A composition according to claim 1 , wherein{'sub': 2', '3', '4', '5', '6', '7, 'R, R, R, R, Rand Rare independently selected from H, methyl, ethyl, propyl or isopropyl; and'}{'sub': '1', 'Ris selected fromH,{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkenyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkynyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 3', '7', '2', '6, 'Cto Ccycloalkyl, Cto Cheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N,'}{'sub': 4', '12, 'Cto Calkylcycloalkyl,'}{'sub': 3', '11, 'Cto Calkylheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N and wherein N is present in the heterocyclic ring, the nitrogen atom may be in the form of an amide, carbamate or urea,'}phenyl, substituted phenyl, naphthyl, substituted naphthyl,alkylphenyl, alkylsubstituted phenyl, alkylnaphthyl, alkylsubstituted naphthyl,pyridyl, furanyl, thiophenyl, pyrrollyl, oxazolyl, isoxazolyl, thiazolyl, diazolyl, pyrazolyl ...

THIOETHER PRODRUG COMPOSITIONS AS ANTI-HIV AND ANTI-RETROVIRAL AGENTS

Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus. 2. The compound or salt of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently selected from hydrogen claim 1 , halogen claim 1 , CF claim 1 , optionally substituted alkyl claim 1 , optionally substituted alkoxy claim 1 , optionally substituted aryl claim 1 , NO claim 1 , optionally substituted acylamino claim 1 , optionally substituted arylamino claim 1 , optionally substituted acyl claim 1 , optionally substituted acyloxy claim 1 , or any of Rand Rtaken together claim 1 , Rand Rtaken together claim 1 , or Rand Rtaken together form a 5- or 6-membered saturated or unsaturated ring.34.-. (canceled)5. The compound or salt of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently selected from halogen claim 1 , CF claim 1 , optionally substituted alkyl claim 1 , optionally substituted alkoxy claim 1 , optionally substituted aryl claim 1 , NO claim 1 , optionally substituted acylamino claim 1 , optionally substituted arylamino claim 1 , optionally substituted acyl claim 1 , optionally substituted acyloxy claim 1 , or any of Rand Rtaken together claim 1 , Rand Rtaken together claim 1 , or Rand Rtaken together form a 5- or 6-membered saturated or unsaturated ring.67.-. (canceled)8. The compound or salt of claim 1 , wherein Ris selected from hydrogen claim 1 , optionally substituted acyl claim 1 , optionally substituted acyloxy claim 1 , optionally substituted alkoxyacyl claim 1 , optionally substituted aryloxyacyl claim 1 , optionally substituted alkyl claim 1 , optionally substituted aryl claim 1 , ...

ACTIVATORS OF CLASS I HISTONE DEACETLYASES (HDACS) AND USES THEREOF

The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D). 35.-. (canceled)6. The compound of claim 1 , wherein{'sup': A1', 'A3, 'Xand Xare oxygen;'}{'sup': 'A2', 'Xis sulfur; and'}{'sup': A1', 'A2, 'Rand Rare hydrogen.'}7. The compound of claim 1 , wherein Ar is optionally substituted aryl.11. The compound of claim 1 , wherein Ar is optionally substituted heteroaryl.15. The compound of claim 14 , wherein{'sup': A1', 'A3, 'Xand Xare oxygen;'}{'sup': 'A2', 'Xis sulfur; and'}{'sup': A1', 'A2, 'Rand Rare hydrogen.'}1934-. (canceled)3146-. (canceled)4857-. (canceled)58. A pharmaceutical composition comprising a compound of any claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and optionally a pharmaceutically acceptable excipient.59. (canceled)60. A method for treating or preventing a neurological disorder in a subject claim 1 , the method comprising administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of an HDAC (histone deacetylase) activator of to treat the neurological disorder.61. The method in claim 60 , wherein the HDAC activator is a class I HDAC activator.62. The method in claim 61 , wherein the class I HDAC activator is an HDAC1 (histone deacetylase 1) activator.64. The method of claim 60 , wherein the neurological disorder is Alzheimer's disease claim 60 , Parkinson's disease claim 60 , Huntington's ...

Compounds and Methods for Altering Lifespan of Eukaryotic Organisms

Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation. 11.) The compound of claim 1 , wherein the compound is selected from the following: 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[4-(N claim 1 ,N-dimethylamino)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-methylphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-(1-methylethyl)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-chlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-isobutyryl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2-chloro-6-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[naphth-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2 claim 1 ,4-dichlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[2 claim 1 ,4 claim 1 ,5-trimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopropanecarbonyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2- ...

NOVEL MIXTURE AND COMPOUNDS FROM MYCELIA OF ANTRODIA CAMPHORATA AND USE THEREOF

The present invention relates to a compound derived from mycelium of . The present invention also relates to the composition or mycelium comprising the compounds of the invention. The composition of the invention decreases systolic blood pressure and increases high density lipoprotein. 2. The compound of claim 1 , wherein Ris Calkenyloxy or Calkynyloxy.3. The compound of claim 2 , wherein Calkenyloxy is substituted with Calkyl.4. The compound of claim 1 , wherein Ris isobutyl.5. The compound of claim 1 , which is 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]furan-2 claim 1 ,5-dione. This application is a Continue-in-part Application of U.S. patent application Ser. No. 12/840,655, filed Jul. 21, 2010, which is a Continue-in-part Application of U.S. patent application Ser. No. 12/078,985, filed Apr. 9, 2008, which is a Divisional Application of U.S. application Ser. No. 11/312,480, filed Dec. 21, 2005, which is currently pending, the entire contents of which are incorporated herein by reference, which is a Divisional Application of U.S. application Ser. No. 10/793,820, filed Mar. 8, 2004, now U.S. Pat. No. 7,109,232, issued Sep. 19, 2006, the entire contents of which are incorporated herein by reference.Although incorporated by reference in its entirety, no arguments or disclaimers made in the parent application apply to this Continuation-in-part application. Any disclaimer that may have occurred during the prosecution of the above-referenced application(s) is hereby expressly rescinded. Consequently, the Patent Office is asked to review the new set of claims in view of the entire prior art of record and any search that the Office deems appropriate.The present invention relates to novel mixture and compounds from mycelium of and the use thereof. The present invention relates to the composition or mycelium comprising the compounds of the invention.The fruiting body of (Polyporaceae, Aphyllophorales) is well known in Taiwan as a traditional Chinese medicine. It grows ...

Process for preparing optically active antrocin

The present invention relates to a process of preparation of optically active antrocin. At first, to introduce the correct configuration of trans-decalone, alkyl aluminum/TMSCN was used to react with decalenone. The resulting racemic nitrile-decalone was resolved with chiral diol by ketalization to produce two chromatography separable diasteromers. After a simple column chromatography, optically pure compounds were obtained. Formylation was a critical step for the lactone formation. The rest of the synthesis is straight forward through oxidation and olefination. Accordingly, the total synthesis was completed in 10 steps with 7% overall yield from commercially available 6-methoxy-2-tetralone.

SUBSTITUTED BIARYL ALKYL AMIDES

Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds. 2. The compound of claim 1 , wherein n is selected from the group consisting of 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , and 5.3. The compound of claim 2 , wherein n is 2.4. The compound of claim 1 , wherein each Ris halo.5. The compound of claim 4 , wherein each Ris chloro.6. The compound of claim 1 , wherein Z claim 1 , Z claim 1 , Zand Zare each —CH—.7. The compound of claim 1 , wherein Ris (Calkoxy)Calkyl.8. The compound of claim 7 , wherein Ris methoxymethyl or ethoxymethyl.9. The compound of claim 1 , wherein Ris (aryloxy)Calkyl.10. The compound of claim 9 , wherein Ris phenoxymethyl.11. The compound of claim 1 , wherein Ris Cheterocyclyl.12. The compound of claim 11 , wherein Ris selected from optionally substituted tetrahydrofuranyl or optionally substituted pyrrolidinyl.13. The compound of claim 12 , wherein the nitrogen atom in pyrrolidinyl is protected with a t-butyloxycarbonyl (Boc) protecting group.14. The compound of claim 1 , wherein Ris Ccycloalkyl.15. The compound of claim 14 , wherein Ris cyclopentyl.16. The compound of claim 1 , wherein Ris haloalkyl.17. The compound of claim 16 , wherein Ris selected from the group consisting of —CHCl claim 16 , —CHBr claim 16 , —CHCHCl claim 16 , —CHCHBr claim 16 , —CH(Cl)CHand —CH(Br)CH.18. The compound of claim 1 , wherein Ris optionally substituted aminoalkyl.19. The compound of claim 18 , wherein Ris selected from the group consisting of —CHNH claim 18 , —CHNH(Boc) claim 18 , —CH(NH)CH claim 18 , and —CH(Boc-NH)CH.20. The compound of claim 1 , wherein Ris —OH.22. The compound of claim 21 , wherein Ris —OH.23. The compound of claim 1 , wherein Ris selected from the group consisting of —OH claim 1 , —NHR claim 1 , an optionally substituted Calkoxy claim 1 , and an optionally ...

HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS

Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed. 2. The process of wherein the isopropyl boronate cyclic ester is isopropyl pinacolato boronate.3. The process of wherein the alkyllithium is t-butyllithium claim 1 , s-butyllithium or n-butyllithium.4. The process of wherein the isopropyl pinacolato boronate is added to a diethyl ether solution of the metallated 3-bromo-2-ethylbenzofuran at a temperature from −75 to −100° C.6. The process of wherein the 2-ethylbenzofuran-3-yl cyclicboronate ester is recovered by extraction with ethyl acetate. This application is a divisional application of the U.S. patent application Ser. No. 12/299,519, filed on Nov. 4, 2008, entitled “HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS,” and which is a 371 national phase of PCT application number PCT/US07/07882, filed on Mar. 29, 2007, which claims the benefit of U.S. Provisional Patent Application No. 60/798,108, filed on May 5, 2006, the teachings of which are incorporated by reference herein, as if reproduced in full hereinbelow.This invention is directed to certain hafnium complexes, to catalyst compositions comprising the same, and to addition polymerization processes, especially olefin polymerization processes, using such hafnium complexes as one component of a coordination polymerization catalyst composition.Advances in polymerization and catalysis have resulted in the capability to produce many new polymers having improved physical and chemical properties useful in a wide variety of superior products and applications. With the development of new catalysts the choice of polymerization-type (solution, slurry, high pressure or gas phase) for producing a particular polymer has been greatly expanded. Also, advances in polymerization technology have provided more efficient, highly productive ...

ANTIMICROBIAL AGENTS

The invention provides a compound of formula I:or a salt thereof, wherein R-Rand X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents. 2. The compound of wherein:{'sup': 1', 'y', 'y, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 2', 'z', 'x, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 4', '5', '6', '7', 'd', '4', '5', '6', '7', 'p', 'p', 'p', 'g', 'h', 'g', 'h', 'a', '4', '5', '6', '7', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'at least one of RRRand Ris aryl or heteroaryl wherein each aryl or heteroaryl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and the remainder of RRRand Rare each independently H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, heteroaryloxy, (C-C)alkylthio, —S(O)R, —S(O)R, —S(O)R, —S(O)NRR, and —NRR; wherein any alkyl and any alkyl or alkanoyl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and wherein any aryl, heteroaryl, or any aryl or heteroaryl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl of RRRand Ris optionally substituted with one or more (e.g. 1, 2, 3, or 4) R;'}{'sup': 8', 'p', 'p', 'p', 'g', 'h', 'g', 'h', '8', 'a', '8', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2, 'Ris H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, ...

PHARMACEUTICAL COMPOSITION

Provided are compositions comprising aqueous solutions of valsartan suitable for oral administration, preferably in pediatric and geriatric populations. Methods for making such compositions and methods for their stabilization are provided. 1. A liquid oral dosage formulation comprising water , and valsartan , wherein the pH of said formulation is between about 4.5 and about 7.0.2. The liquid oral dosage formulation of claim 1 , further comprising a wetting agent.3. The liquid oral dosage formulation of claim 2 , wherein said wetting agent is a member selected from the group consisting of polysorbate 80 claim 2 , poloxamers claim 2 , polyethoxylated castor oil claim 2 , polyethoxylated hydrogenated castor oil claim 2 , polyoxyl 40 stearate claim 2 , propylene glycol claim 2 , and mixtures thereof.4. The liquid oral dosage formulation of claim 1 , wherein the pH of said formulation is between about 5.5 and about 6.2.5. The liquid oral formulation of claim 4 , wherein the pH of said formulation is about 5.96. The liquid oral formulation of comprising a buffer system.7. The liquid oral formulation of wherein said buffer system comprises a member selected from the group consisting of alkaline metal citrate salts with citric acid claim 6 , alkaline metal acetate salts with acetic acid claim 6 , alkaline metal succinate salts with succinic acid claim 6 , and mixtures thereof.8. The liquid oral formulation of claim 7 , further comprising an antifoaming agent.9. The liquid oral formulation of claim 7 , further comprising a preservative.10. The liquid oral formulation of claim 9 , wherein said preservative is a member selected from the group consisting of benzoic acid claim 9 , sorbic acid claim 9 , butylparaben claim 9 , ethylparaben claim 9 , methylparaben claim 9 , propylparaben claim 9 , sodium benzoate claim 9 , sodium propionate claim 9 , and mixtures or salts thereof.11. A method for preparing a liquid oral solution comprising valsartan claim 9 , comprising:admixing ...

MICHELIOLIDE DERIVATIVES, MEDICINAL COMPOSITION, PRODUCING METHOD AND USAGE THEREOF

The present invention provides a compound of formula (I) 2. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises any of cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl claim 1 , heteroaryl.3. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises amino acid fragment and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid.4. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises —NRR claim 1 , and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid;{'sub': 7', '8, 'Wherein, Rand Rare any of hydrogen, alkyl, cycloalkyl, alkyl substituted by hydroxyl, alkenyl, alkynyl, aryl, alkyaryl, arylakyl, arylalkenyl, arylalkynyl, heterocyclic, trifluoromethyl, perfluoroalkyl, cyano, cyanomethyl, carboxyl, cabamate, sulfonyl, sulfonamide or aryloxyalkyl respectively.'}5. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises —NRR claim 1 , and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid;{'sub': 7', '8', '7', '8, 'Wherein, Rand Rtogether with N form a ring, and Rand Rare any of hydrogen, alkyl with 1 to 8 carbon atoms, any cycloalkyl respectively.'}6. A compound of claim 5 , wherein claim 5 , the ring comprises one or more than one substituent.7. A compound of claim 6 , wherein claim 6 , the one or more than one substituent is any of hydrogen claim 6 , alkyl claim 6 , cycloalkyl claim 6 , alkenyl claim 6 , alkynyl claim 6 , aryl claim 6 , alkyaryl claim 6 , arylakyl claim 6 , arylalkenyl claim 6 , arylalkynyl and heterocyclic.8. A compound of claim 5 , wherein claim 5 , the number of the ring is three to nine.9. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises quaternary ammonium salts formed by amino acid fragment or —NRRwith RZ;Wherein, Z is any of fluorine, chlorine, bromine, iodine, tosylate, ...

NOVEL ARYLAMIDE DERIVATIVES HAVING ANTIANDROGENIC PROPERTIES

The invention relates to novel arylamide derivatives having formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, where R1-R11, R′, R″, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation. 2. Arylamide derivative according to claim 1 , where R4 and R5 are H and R1 is H claim 1 , alkyl or halogen.3. Arylamide derivative according to claim 1 , where R1 claim 1 , R4 and R5 are H; R2 is selected from the group consisting of halogen and trifluoromethyl; R3 is selected from the group consisting of NO claim 1 , CONHand CN; R6 claim 1 , R7 and R10 are H; R8 and R9 are selected from the group consisting of H claim 1 , halogen and trifluoromethyl claim 1 , provided that at least one of R8 and R9 is other than H; X is selected from the group consisting of O and SO; and R11 is selected from the group consisting of alkyl containing up to 6 carbon atoms claim 1 , phenyl optionally substituted with 1 or 2 halogen atoms or with 1 halogen atom and a further substituent selected from the group consisting of CN claim 1 , NO claim 1 , CONHR claim 1 , NHCOR claim 1 , NHSOR claim 1 , where R is as defined in claim 1 , and alkylsulfonyl; and furyl.4. Arylamide derivative according to claim 3 , where R1 claim 3 , R4 and R5 are H; R2 is trifluoromethyl; R3 is CN; R6 claim 3 , R7 and R10 are H; R8 is trifluoromethyl; R9 is H; X is SO; and R11 is alkyl containing up to 4 carbon atoms.5. Arylamide derivative according to claim 3 , where R1 claim 3 , R4 and R5 are H; R2 is chloro; R3 is CN; R6 claim 3 , R7 and R10 are H; R8 is trifluoromethyl; R9 is H; X is SO; and R11 is 4-fluorophenyl.6. Arylamide derivative according to claim 1 , where R8 and R9 are both halogens or one of R8 and R9 is halogen and the other is selected from the group consisting of CN claim 1 ...

Furan based resin, process for the preparation thereof, and use of the compound

The present invention relates to the polymeric reaction product of compounds according to Formula (I) and Formulae (II) or (III). Formula (I) has the following structure: where R 1 , R 2 , R 3 and R 4 are independently H, OH, optionally substituted C 1-12 alkyl, optionally substituted C 1-12 alkenyl, C 1-12 aldehyde, C 3-12 acetals, C 2-12 ether, and/or C 2-12 ester; where optionally at least one of R 1 , R 2 , R 3 and R 4 is H. Formulae (II) and (III) have the following structure: where X is H or C 1-4 alkyl; Y is OH or OR 5 where R 5 is C 1-12 alkyl, C 3-12 aryl, C 4-12 aralkyl or C 3-12 cycloalkyl; and Z is an electron-withdrawing group.

Process for the Preparation of Dronedarone

This disclosure relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)-propoxy]-benzoyl}-1-benzofuran-5-yl]-methane-sulfonamide of formula I 2. The process as defined in claim 1 , further comprising carrying out the reaction in an organic solvent or in a mixture of organic solvents.3. The process as defined in claim 1 , wherein the reaction is carried out in the presence of alkali alcoholate.5. The process according to claim 4 , comprising performing reaction step b) in the presence of a Lewis acid.6. The process according to claim 4 , comprising carrying out reaction step b) in an inert organic solvent or in a mixture of inert organic solvents.7. The process according to claim 4 , comprising carrying out reaction step b) at a temperature between 20-100° C.8. The process according to claim 4 , comprising carrying out reaction step c) at a temperature around the boiling point of the applied solvent or solvent mixture.9. The process according to claim 4 , comprising carrying out reaction step c) in an inert organic solvent or in a mixture of inert organic solvents.10. The process according to claim 4 , comprising carrying out reaction step c) in the presence of an acid binder of basic character.12. The process according to claim 4 , comprising using iron(III) chloride or aluminium(III) chloride in reaction step a) as the Lewis acid.13. The process according to claim 5 , comprising using iron(III) chloride or aluminium(III) chloride in reaction step a) as the Lewis acid.14. The process according to claim 11 , comprising using iron(III) chloride or aluminium(III) chloride in reaction step a) as the Lewis acid.15. The process according to claim 4 , comprising carrying out reaction step a) in an inert organic solvent or in a mixture of inert organic solvents.16. The process according to claim 12 , comprising carrying out reaction step a) in an inert organic solvent or in the mixture of inert organic solvents. This application is a continuation of ...

Method for producing biobased chemicals from woody biomass

A method for utilizing woody biomass components, namely cellulose, hemicellose, and lignin, and converting them to value-added biobased chemical products is described herein. The present method provides treatments to obtain a plurality of component streams from woody biomass for producing derivative products while minimizing waste products.

INHIBITORS OF HIF AND ANGIOGENESIS

Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided. 2. The compound of claim 1 , wherein A is —CRR—.3. The compound of claim 1 , wherein X is N claim 1 , Y is CR claim 1 , and Z is CR.4. The compound of claim 1 , wherein Y is N claim 1 , X is CR claim 1 , and Z is CR.5. The compound of claim 1 , wherein Z is N claim 1 , X is CR claim 1 , and Y is CR.6. The compound of claim 1 , wherein Ris a cyclopropyl claim 1 , cyclobutyl or cyclopentyl.7. The compound of claim 1 , wherein Rand Rare alkyl.8. The compound of claim 1 , wherein Ris alkyl other than methyl.9. The compound of claim 1 , wherein is a double bond claim 1 , E is CR claim 1 , and A is —CR═CR—.10. The compound of claim 1 , wherein Ris 4-methoxyphenyl claim 1 , 3 claim 1 ,4-dimethoxyphenyl claim 1 , or 3 claim 1 ,5-dimethylphenyl.11. The compound of selected from the group:N-cyclopentyl-N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-4-methoxy-N-phenylbenzenesulfonamide;N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,5-dimethyl-N-phenylbenzenesulfonamide;N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxy-N-phenylbenzenesulfonamide;N-cyclopentyl-N-((2,2-dimethyl-2H-pyrano[3,2-b]pyridin-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-cyclobutyl-N-((2,2-dimethyl-2H-pyrano[3,2-b]pyridin-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-butyl-N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxybenzenesulfonamide; andN-cyclopentyl-N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxybenzenesulfonamide or salts thereof.12. A pharmaceutical compositions comprising a compound as provided in or pharmaceutically acceptable salt and a pharmaceutically acceptable excipient.13. A method of treatment ...

FURANYL COMPOUNDS AND THE USE THEREOF

Provided herein are substituted furanyl compounds of formula (I), pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate eIF4E activity. In one embodiment, the compounds provided herein modulate the Hedgehog pathway activity. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders. 2. The compound of claim 1 , wherein L is S(O).3. The compound of claim 1 , wherein L is C(O).8. A pharmaceutical composition comprising a compound of claim 1 , or an enantiomer claim 1 , a mixture of enantiomers claim 1 , or a mixture of two or more diastereomers thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , hydrate claim 1 , or prodrug thereof claim 1 , and at least one pharmaceutically acceptable excipient or carrier.9. The pharmaceutical composition of claim 8 , further comprising one or more additional active agents.10. A method of treating claim 1 , preventing claim 1 , or ameliorating one or more symptoms of a disorder mediated by cap-dependent protein translation claim 1 , comprising administering a compound of claim 1 , or an enantiomer claim 1 , a mixture of enantiomers claim 1 , or a mixture of two or more diastereomers thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , hydrate claim 1 , or prodrug thereof.11. A method of treating claim 1 , preventing claim 1 , or ameliorating one or more symptoms of a disorder mediated by eIF4E claim 1 , comprising administering a compound of claim 1 , or an enantiomer claim 1 , a mixture of enantiomers claim ...

Styryl-based compound, composition containing styryl-based compound, and organic light emitting diode including styryl-based compound

A styryl-based compound represented by Formula 1, a composition containing the styryl-based compound, and an organic light-emitting diode (OLED) including the styryl-based compound: The styryl-based compound may exhibit high heat resistance and thus an OLED including the same may have low driving voltage, high brightness, high efficiency, and long lifetime.

RADIATION-SENSITIVE RESIN COMPOSITION, METHOD FOR FORMING RESIST PATTERN, AND POLYMER AND COMPOUND

A radiation-sensitive resin composition that provides a resist coating film in a liquid immersion lithography process is provided, the radiation-sensitive resin composition being capable of exhibiting a great dynamic contact angle during exposure, whereby the surface of the resist coating film can exhibit a superior water draining property, and the radiation-sensitive resin composition being capable of leading to a significant decrease in the dynamic contact angle during development, whereby generation of development defects can be inhibited, and further shortening of a time period required for change in a dynamic contact angle is enabled. A radiation-sensitive resin composition including (A) a fluorine-containing polymer having a structural unit (I) that includes a group represented by the following formula (1), and (B) a radiation-sensitive acid generator. 8. The radiation-sensitive resin composition according to claim 7 , wherein Rin the above formula (1-5) represents a trifluoromethyl group.10. The radiation-sensitive resin composition according to claim 1 , wherein the content of the structural unit (I) in the polymer (A) is no less than 30 mol % and no greater than 100 mol %.12. The radiation-sensitive resin composition according to claim 1 , further comprising (C) a polymer having an acid-dissociable group and having a content of fluorine atoms less than that of the polymer (A).13. The radiation-sensitive resin composition according to claim 12 , wherein the content of the polymer (A) is no less than 0.1 parts by mass and no greater than 10 parts by mass with respect to 100 parts by mass of the polymer (C).14. A method for forming a resist pattern comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'forming a photoresist film on a substrate using the radiation-sensitive resin composition according to ;'}subjecting the photoresist film to liquid immersion lithography; andforming a resist pattern by developing the photoresist film subjected to the ...

MODULATORS OF CENTRAL NERVOUS SYSTEM NEUROTRANSMITTERS

Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents. 3. A compound of claim 2 , wherein G is hydrogen or combined with Rto form a 5-6 membered heterocylcoalkyl containing 1-2 heteroatoms each independently selected from the group consisting of N and 0; and subscript b is 1-3.4. A compound of claim 3 , wherein D is a member selected from the group consisting of optionally substituted phenyl claim 3 , optionally substituted naphthyl and optionally substituted bi-phenyl; and subscript a is 0-3.5. A compound of claim 3 , selected from the group consisting of:2-(aminomethyl)-5-phenyltetrahydrofuran,2-(aminomethyl)-5-(4′-chlorophenyl)tetrahydrofuran,2-(aminomethyl)-5-(4-bromophenyl)tetrahydrofuran,2-(aminomethyl)-5-(4-methoxyphenyl)tetrahydrofuran,2-(aminomethyl)-5-(4′-t-butylphenyl)tetrahydrofuran,trans-2-(aminomethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,cis-2-(aminomethyl)-5-(2′-methoxy-5-fluorophenyl)tetrahydrofuran,2-(aminomethyl)-5-(3′-fluoro-4′-methylphenyl)tetrahydrofuran,2-(aminomethyl)-5-cyclohexyltetrahydrofuran,2-(aminomethyl)-5-(1′-naphthyl)tetrahydrofuran,2-(aminomethyl)-5-(2′-naphthyl)tetrahydrofuran,2-(aminomethyl)-5-(2′-naphthyl)tetrahydrofuran,2-(aminoethyl)-5-phenyltetrahydrofuran,2-(aminoethyl)-5-(4′-fluorophenyl)tetrahydrofuran,2-(aminoethyl)-5-(4′-bromophenyl)tetrahydrofuran,2-(aminoethyl)-5-(4′-t-butylphenyl)tetrahydrofuran,trans-7 aminoethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,cis-2-(aminoethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,2-(aminoethyl)-5-cyclohexyltetrahydrofuran,2-(aminoethyl)-5-(2′-furyl)tetrahydrofuran,2-(aminomethyl)-5-benzyltetrahydrofuran,2-(aminoethyl)-5-benzyltetrahydrofuran,trans-2-(aminomethyl)-5-(2′-methoxy-5′-fluorobenzyl) ...

TREATMENT OF A PATHOLOGY LINKED TO AN EXCESSIVE EFFECT OF TNF WITH A BENZENE SULPHONAMIDE COMPOUND

A benzene sulphonamide compound of formula I 2. A sulphonated compound as defined in for its use in a method for treating a non-cancer pathology linked to an excessive effect of TNF-alpha chosen from the inflammatory diseases of the intestine claim 1 , inflammation claim 1 , chronic inflammatory diseases claim 1 , rheumatoid arthritis claim 1 , juvenile rheumatoid arthritis claim 1 , psoriatic arthritis claim 1 , arthrosis claim 1 , refractory rheumatoid arthritis claim 1 , non-rheumatoid chronic arthritis claim 1 , bone resorption/osteoporosis claim 1 , Crohn's disease claim 1 , haemorrhagic rectocolitis claim 1 , septic shock claim 1 , endotoxin shock claim 1 , atherosclerosis claim 1 , ischaemia-reperfusion lesions claim 1 , coronary heart disease claim 1 , vasculitis claim 1 , amydoloidosis claim 1 , multiple sclerosis claim 1 , septicaemia claim 1 , chronic recurrent uveitis claim 1 , hepatitis C virus claim 1 , malaria claim 1 , ulcerative colitis claim 1 , cachexia claim 1 , psoriasis claim 1 , endometriosis claim 1 , Behçet's disease claim 1 , Wegener's granulomatosis claim 1 , meningitis claim 1 , AIDS claim 1 , HIV infections claim 1 , auto-immune diseases claim 1 , immunodeficiency claim 1 , common variable immunodeficiency (CVID) claim 1 , chronic graft-versus-host diseases claim 1 , trauma and graft rejections claim 1 , respiratory distress syndrome claim 1 , pulmonary fibrosis claim 1 , diabetes claim 1 , juvenile diabetes claim 1 , ankylosing spondylitis claim 1 , and skin disorders due to delayed-type hypersensitivity reactions claim 1 , Alzheimer's disease claim 1 , disseminated lupus erythematosus claim 1 , and allergic asthma and more generally the inflammatory diseases for which the anti-TNF biotherapies (monoclonal antibodies claim 1 , soluble receptors) are effective.3. A sulphonated compound according to or claim 1 , characterized in that R4 represents a hydrogen atom or a C1-C5 alkyl and', {'claim-ref': {'@idref': 'CLM-00001', 'claims 1'}, ' ...

MICROWAVE ASSISTED SYNTHESIS OF DEHYDRATED SUGAR DERIVATIVES HYDROXYMETHYLFURFURAL, LEVULINIC ACID, ANHYDROSUGAR ALCOHOLS, AND ETHERS THEREOF

Methods for the production of dehydrated sugars and derivatives of dehydrated sugars using microwave (MW) irradiation and methods of purifying the same are described. The dehydrated sugars derivatives include 5-hydroxymethyl-2-furfural (HMF) and anhydrosugar alcohols such as sorbitans and isosorbide. The derivatives include HMF ethers, levulinic acid esters, and ether derivatives of the anhydrosugar alcohols. The described methods require lower reaction temperatures and shorter reaction times than similar non microwave mediated reactions known in the art. Typical reaction conditions are 120-210° C., and typical reaction times are 30 minutes or less. 1. A method of producing a dehydrated sugar derivative comprising ,a. forming a reaction mixture comprising a solvent and a reactant selected from the group consisting of a hexose, a sugar alcohol, and an anhydrosugar alcohol; andb. contacting the reaction mixture with microwave radiation to achieve a temperature of between 130° C. and 210° C. for a time sufficient to convert at least 40% of the reactant into at least one desired dehydrated sugar derivative product.2. The method of wherein the reactant is a fructose and the desired dehydrated sugar derivative is HMF.3. The method of wherein the reactant is a sugar alcohol and the desired dehydrated sugar derivative is an anhydrosugar alcohol.4. The method of wherein the reaction mixture further contains an acidic catalyst selected from the group consisting of a heterogeneous solid acid substrate and a homogeneous acid.5. The method of where in the reaction mixture contains a R-alcohol that is miscible in the reaction mixture claim 4 , where R is an alkyl claim 4 , allyl claim 4 , cycloalkyl claim 4 , or aryl group claim 4 , and the desired dehydrated sugar derivative is selected from the group consisting of an R-ether or R-ester of the desired dehydrated sugar derivative.6. The method of wherein the he R-alcohol is the solvent of the reaction mixture.7. The method of ...

Pesticidal Mixtures

The present invention, comprising: [(3S,4R,4aR,6S,6aS,12R,12a5,12b5)-3-(cyclopropanecarbonyloxy)-6,12-dihy-droxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,2,3,4,4a,5,6,6a,12a,12b-decahydro-11H,12H-benzo[f]pyrano[4,3-b]chromen-4-yl]methyl cydopropanecarboxylate (compound II) and a pesticidal compound II; in synergistic effective amounts. 130-. (canceled)32. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of alpha-cypermethrin claim 31 , bifenthrin claim 31 , cypermethrin claim 31 , deltamethrin claim 31 , flucythrinate claim 31 , lambda-cyhalothrin claim 31 , tefluthrin and permethrin.33. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of nitenpyram claim 31 , spinosad claim 31 , spinetoram and thiacloprid.34. The mixture according to claim 31 , wherein the pesticidal compound II is ethiprole.35. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of abamectin claim 31 , emamectin benzoate claim 31 , milbemectin and lepimectin.36. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of chloranthraniliprole and cyantraniliprole.37Bacillus firmus. The mixture according to claim 31 , wherein the pesticidal compound II is CNCM 1-1582.38. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of chloranthraniliprole claim 31 , spinosad and abamectin.39. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of abamectin claim 31 , bifenthrin claim 31 , alpha-cypermethrin claim 31 , metaflumizone claim 31 , pymetrozine claim 31 , chloranthraniliprole claim 31 , cyanantraniliprole claim 31 , sulfloxaflor claim 31 , spinosad and 4-{[(6-chloropyrid-3-yl)methyl](2 claim 31 ,2-difluoroethyl)amino}furan-2(5H)-on.40. The mixture according ...

ETHER COMPOUND, ELECTROLYTE COMPOSITION FOR NON-AQUEOUS BATTERY, BINDER COMPOSITION FOR NON-AQUEOUS BATTERY ELECTRODE, SLURRY COMPOSITION FOR NON-AQUEOUS BATTERY ELECTRODE, ELECTRODE FOR NON-AQUEOUS BATTERY AND NON-AQUEOUS BATTERY

An ether compound represented by the following formula and its use: 4. An electrolyte solution composition for a non-aqueous battery claim 1 , comprising an organic solvent claim 1 , an electrolyte dissolved in the organic solvent claim 1 , and the ether compound according to .5. A binder composition for a non-aqueous battery electrode claim 1 , comprising an acrylic-based polymer and the ether compound according to .6. A slurry composition for a non-aqueous battery electrode claim 5 , containing an electrode active material and the binder composition for a non-aqueous battery electrode according to .7. An electrode for a non-aqueous battery claim 5 , comprising a current collector and an electrode active material layer provided on a surface of the current collector claim 5 ,{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'wherein the electrode active material layer is obtained by applying and drying the slurry composition for a non-aqueous battery electrode according to .'}8. A non-aqueous battery claim 5 , comprising a positive electrode claim 5 , a negative electrode claim 5 , and a non-aqueous electrolyte solution claim 5 ,{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'wherein the non-aqueous electrolyte solution is the electrolyte solution composition for a non-aqueous battery according to .'}9. A non-aqueous battery claim 5 , comprising a positive electrode claim 5 , a negative electrode claim 5 , and a non-aqueous electrolyte solution claim 5 ,{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'wherein one or both of the positive electrode and the negative electrode is the electrode for a non-aqueous battery according to .'} The present invention relates to a novel ether compound as well as an electrolyte solution composition for a non-aqueous battery, a binder composition for a non-aqueous battery electrode, a slurry composition for a non-aqueous battery electrode, an electrode for a non-aqueous battery, and a non-aqueous battery, each of which uses the ...

Production of renewable aromatic compounds

The invention provides a process for producing a variety renewable aromatic compounds such as benzene, toluene, xylenes, and cumene, as well as compounds derived from these including, for example, aniline, benzoic acid, cresol, cyclohexane, cyclohexanone, phenol and bisphenol A, toluene di-isocyanate, isophthalic acid, phthalic anhydride, terephthalic acid and dimethyl terephthalate. The invention also provides for renewable forms of these aromatic compounds.

PEST CONTROL COMPOSITION

A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q, Q, Q, Q, R, R, R, Rand m have the same meanings described in the specification) and an ester compound shown by formula (2) below (in the formula, X, Xand Xhave the same meanings described in the specification) and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and the ester compound represented by formula (II) is applied to a pest or a pest habitat. 2. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , G is a group shown by G-1 claim 1 , Yis an oxygen atom claim 1 , Ris a trifluoromethyl group claim 1 , each of Q claim 1 , Q claim 1 , and Qis a CH group claim 1 , Qis a CRgroup claim 1 , Ris the group defined above claim 1 , (R)is a substituent at 3- and 5-positions claim 1 , m is 2 claim 1 , and Ris a chlorine atom.3. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom.4. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom or a methyl group.5. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a halogen atom.6. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a chlorine atom.7. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group claim 1 , a C1 to C6 haloalkyl group claim 1 , a C3 to C6 cycloalkyl group claim 1 , or a (C1 to C6 alkoxy) C1 to C6 alkyl group.8. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group.9. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C1 to C6 haloalkyl group.10. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C3 to C6 ...

NOVEL FORMS OF [R-(R*,R*)]-2-(4-FLUOROPHENYL)-b,d-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID MAGNESIUM

Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described. 1. (canceled)2. (canceled)3. A Form B atorvastatin magnesium having an X-ray powder diffraction containing the following 2θ values measured using CuKradiation: 6.1 , 8.0 , 10.9 , 19.8 , and 23.0.4. A Form B atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:{'sup': '13', 'A) a C shift containing values: 118.3, 125.4, 126.8, 132.2, and 133.8 ppm; and'}{'sup': '19', 'B) an F shift containing value: −115.7 ppm.'}5. A Form C atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKradiation: 5.2 , 6.6 , and 12.3.6. A Form C atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:{'sup': '13', 'A) a C shift containing the values: 129.2, 133.3, and 139.1 ppm; and'}{'sup': '19', 'B) an F shift containing the values: −109.6, and −113.0 ppm.'}7. A Form D atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKradiation: 7.7 , 20.5 , and 24.2.8. A Form D atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:{'sup': '13', 'A) a C shift containing the values: 132.6, 134.4, 136.9, and 138.6 ppm; and'}{'sup': '19', 'B) an F shift containing the values: −110.0, −111.7, −114.7, and −119.8 ppm.'}9. (canceled)10. (canceled)11. A Form F atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKradiation: 8.7 , 10.1 , 11.7 , and 16.1.12. A Form F atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:{'sup': '13', 'A) a C shift ...

Vitamin C Composition for Use in the Prevention and Treatment of Stretch Marks, Radiation Dermatitis, and Other Skin Conditions and Methods of Using the Same

A formulation for a stable ascorbic acid composition which, in a simplified form, is comprised of ascorbic acid in solution with a hygroscopic compound (i.e., a substance with the ability to attract water molecules from the surrounding environment through either absorption or adsorption). Also disclosed herein are methods for the production of such compounds and methods of using such compounds in the prevention, inhibition and treatment of striae gravidarum, radiation dermatitis, rhytids, lentigoes, dyschromia, sun-damage induced hyperpigmentation, cellulite, scars and purpura, among other skin diseases or conditions. 1. A method of stimulating collagen synthesis comprising:forming a composition of ascorbic acid in solution with a hygroscopic compound; andapplying said composition topically to a patient's skin.2. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of striae gravidarum.3. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of radiation dermatitis.4. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of rhytids.5. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of lentigoes.6. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of dyschromia.7. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of sun-damage induced hyperpigmentation.8. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of cellulite.9. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of scars.10. The method of claim 1 , wherein the composition is topically applied to the patient for the treatment of pupura. This application is a Divisional of U.S. Utility patent application Ser. No. ...

GPR120 RECEPTOR AGONISTS AND USES THEREOF

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. 125.-. (canceled)28. The compound of wherein Ris independently selected from the group consisting of F claim 27 , Cl claim 27 , —CH claim 27 , —CFand —OCH.29. The compound of claim 28 , wherein each Ris independently selected from the group consisting of F claim 28 , Cl claim 28 , —CH claim 28 , —CHand —CF.30. The compound of claim 29 , wherein Z is H or alkyl.31. The compound of claim 30 , wherein Z is H.32. The compound of claim 31 , wherein q is 2.33. The compound of claim 32 , wherein each of Rand Ris H. This application claims the benefit under 35 U.S.C. 119(e) of U.S. Provisional Application No. 61/138,923, filed Dec. 18, 2008, which is incorporated by reference in its entirety into this application.Diabetes mellitus can be divided into two clinical syndromes, Type I and Type II diabetes mellitus. Type I diabetes, or insulin-dependent diabetes mellitus, is a chronic autoimmune disease characterized by the extensive loss of beta cells in the pancreatic islets of Langerhans (hereinafter referred to as “pancreatic islet cells” or “islet cells”), which produce insulin. As these cells are progressively destroyed, the amount of secreted insulin decreases, eventually leading to hyperglycemia (abnormally high level of glucose in the blood) when the amount secreted drops below the level required for euglycemia (normal blood glucose level). Although the exact trigger for this immune response is not known, patients with Type I diabetes have high levels of antibodies against pancreatic beta cells (hereinafter “beta cells”). However, not all patients with high levels of these antibodies develop Type I diabetes.Type II diabetes, or non-insulin-dependent diabetes mellitus, develops when muscle, fat and liver cells fail to respond normally to insulin. This failure to respond (called insulin resistance) ...

Novel Process for the Preparation of Dronedarone

The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: 2. The process according to claim 1 , comprising carrying out the reaction in an alcoholic organic solvent or in a mixture of alcoholic organic solvents.3. The process according to claim 1 , comprising carrying out the reaction in the presence of an alkali alcoholate.4. The process according to claim 1 , comprising carrying out the reaction in the presence of an alkali metal- or alkali earth metal hydroxide.5. The process according to claim 1 , comprising carrying out the reaction in the presence of an inorganic acid.6. The process according to claim 1 , comprising carrying out the reaction at a temperature between 20° C. and the boiling point of the applied solvent or solvent mixture.8. The process according to claim 7 , comprising carrying out the reaction in step a) in an inert organic solvent or in a mixture of inert organic solvents.9. The process according to claim 7 , comprising carrying out the reaction in step a) in the presence of an acid binder.10. The process according to claim 7 , comprising carrying out the reaction in step b) in an inert organic solvent or in a mixture of inert organic solvents.12. The process according to claim 11 , comprising carrying out the reaction in step a) in an inert organic solvent or in a mixture of inert organic solvents.13. The process according to claim 11 , comprising carrying out the reaction in step a) in the presence of an acid binder.14. The process according to claim 11 , comprising carrying out the reaction in step b) an inert organic solvent or in a mixture of inert organic solvents. This application is a continuation of International Application No. PCT/HU2011//000067, filed Jul. 13, 2011, which is incorporated herein by reference, and which claims the benefit of priority of Hungarian Application No. P1000386, filed Jul. 22, 2010.This ...

Hydrogenating Acetic Acid to Produce Ethyl Acetate and Reducing Ethyl Acetate to Ethanol

Disclosed herein are processes for alcohol production by reducing an ethyl acetate produced by hydrogenating acetic acid in the presence of a suitable catalyst. The ethyl acetate is reduced with hydrogen in the presence of a catalyst to obtain a crude reaction mixture comprising the alcohol, in particular ethanol, which may be separated from the crude reaction mixture. Thus, ethanol may be produced from acetic acid through an ethyl acetate intermediate without an esterification step. This may reduce the recycle of ethanol in the hydrogenolysis process and improve ethanol productivity. 1. A method of producing ethanol comprising:hydrogenating acetic acid in a first reactor in the presence of a first catalyst to form a hydrogenation product comprising ethyl acetate, water, and acetic acid;recovering an ester feed stream from the hydrogenation product; andreducing the ester feed stream in a second reactor in the presence of a second catalyst to form ethanol.2. The method of claim 1 , wherein the ester feed stream is recovered in the absence of an esterification process.3. The method of claim 1 , wherein none of the ethanol formed by reducing the ester feed stream is recycled to the first reactor.4. The method of claim 1 , wherein the hydrogenation product comprises from 20 to 95 wt. % ethyl acetate claim 1 , from 5 to 40 wt. % water and from 0.01 to 90 wt. % acetic acid.5. The method of claim 1 , wherein the hydrogenation product further comprises from 0.1 to 30 wt. % ethanol.6. The method of claim 1 , wherein the hydrogenation product is fed to a distillation column to yield a distillate comprising ethyl acetate claim 1 , ethanol claim 1 , and water claim 1 , wherein the ester feed stream comprises the distillate; and a residue comprising acetic acid claim 1 , and wherein the residue is returned to the first reactor.7. The method of claim 6 , wherein the distillate is further condensed and biphasically separated into an organic phase and an aqueous phase claim 6 , and ...

SUB-MICRON COMPOSITIONS

The invention relates to sub-micron compositions, and methods of preparing such compositions, in particular for the treatment of substrates against biological degradation biological pests. 1. A method of preparing a composition comprising sub-micron particles , containing or coated with an active agent(s) , the method comprising at least the steps of:a) (i) dispersing sub-micron particles in a solvent(s);(ii) adding to the dispersion, a formulation containing the active agent(s) dissolved in a suitable solvent in a manner sufficient to achieve substantial uniformity of the mixture (or vice versa); orb) dispersing sub-micron particles in a solvent(s) whilst concurrently or sequentially dissolving an active agent in said solvent in a manner sufficient to achieve substantial uniformity of the mixture; andc) altering the physicochemical environment within the dispersion to cause the active agent to fall out of solution as a sub-micron layer in or on the sub-micron particles.2. The method according to claim 1 , wherein the active agent is a biocide claim 1 , colouring agent or a water repellent agent or a mixture thereof.3. The method according to claim 1 , wherein the alteration in the physicochemical environment can be by one or more of; change in pH claim 1 , introduction of another moiety which reacts with the active agent to cause precipitation claim 1 , heating which can change the isoelectric point claim 1 , heating which can remove sufficient solvent such that the solubility product of the active agent is exceeded claim 1 , addition of a non-solvent of the active agent to cause precipitation or addition of a solute which causes precipitation of the active agent.4. The method according to claim 1 , wherein the physicochemical environment is altered while agitating the result of step (a) (ii) or (b) such that the active agent precipitates as a sub-micron layer on the sub-micron particles and/or within any porosity in the sub-micron particles.5. The method according ...

PROCESS FOR THE SYNTHESIS OF 2,5-FURANDICARBOXYLIC ACID

Process for the synthesis of 2,5-furandicarboxylic acid through the oxidation of -hydroxymethylfurfural in a flow of oxygenor a compound containing oxygen, catalysed by a supported catalyst containing a metal of the platinum group, carried out in aqueous solution in which the pH is maintained higher than 7 and lower than 12 through the addition of a weak base. 114-. (canceled)15. Process for the synthesis of 2 ,5-furandicarboxylic acid through the oxidation of 5-hydroxymethylfurfural by an oxidising substance which is oxygen or a compound containing oxygen , catalysed by a supported catalyst containing a metal of the platinum group , carried out in aqueous solution whose pH is maintained higher than 7 and lower than 12 through the addition of a weak base.16. Process according to wherein the oxidation of 5-hydroxymethylfurfural is carried out by a flow of oxygen.17. Process according to wherein the weak base is added before starting the 5-hydroxymethylfurfural oxidation reaction claim 15 , wherein the pH value of the aqueous solution containing 5-hydroxymethylfurfural and said weak base is higher than or equal to 8 and lower than 12 claim 15 , and the pH value of the aqueous solution at the end of the oxidation reaction is higher than 7 and lower than 11.18. Process according to wherein part of the weak base is added to the reaction mixture before starting the 5-hydroxymethylfurfural oxidation reaction and part is gradually added after said reaction has started claim 15 , and wherein the pH of the aqueous solution is maintained higher than 7 and lower than 11.19. Process according to in which the said weak base is selected from: sodium bicarbonate claim 15 , potassium bicarbonate claim 15 , sodium carbonate claim 15 , potassium carbonate claim 15 , calcium carbonate claim 15 , magnesium carbonate claim 15 , calcium hydroxide claim 15 , magnesium hydroxide claim 15 , dibasic and tribasic phosphate buffer solutions and their mixtures.20. Process according to in which ...

BENZOHETEROCYCLIC ANTI-BACTERIAL AGENTS

Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria. 2. A method of treating a drug-resistant bacterial strain , comprising:{'i': 'Staphylococcus aureus', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering a compound to an individual infected with or suspected of being infected with a methicillin-resistant strain, a vancomycin-resistant strain, or a linezolid-resistant strain, a compound of .'} This application is a continuation of U.S. patent application Ser. No. 12/995,437, filed Nov. 30, 2010, which is a continuation of International Application No. PCT/US2009/045737, filed May 29, 2009, which claims priority to U.S. Provisional Patent Application No. 61/057,282, filed May 30, 2008, the entire disclosures of which are hereby incorporated by reference in their entirety.This invention was made with government support under Grant No. R01 AI 054193 awarded by the National Institutes of Health. The United States Government has certain rights in the invention.Embodiments herein relate to anti-bacterial agents, and, more specifically, to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.In 2004, the IDSA (Infectious Disease Society of America) reported that each year 90,000 of the 2 million people who acquire a hospital bacterial infection will die. That is a 4.5% mortality rate arising from just being within the hospital. Multi-drug resistance bacterial strains are a major problem and one that has been increasing very rapidly every year during the last few decades. In brief, from its discovery in 1968 multi-drug resistant (MRSA) had already accounted for greater than 50% of patient isolates by 1999 in ICUs (intensive care units) within ...

NOVEL SEROTONIN REUPTAKE INHIBITORS AS DRUGS HAVING PERIPHERAL-SYSTEM-RESTRICTED ACTIVITY

Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation. 1. A serotonin reuptake inhibitor (SRI) compound , being modified so as to comprise at least one positively charged group , said at least one positively charged group being selected such that the modified SRI compound retains its charge at physiological pH , while substantially retaining its SRI activity.2. The SRI compound of claim 1 , wherein said positively charged group is a quaternary ammonium group.3. The SRI compound of claim 2 , wherein said quaternary ammonium group has the formula:{'br': None, 'sub': 1', '2', '3, 'sup': +', '−, '—(NRRR)Z'}wherein:Z is an organic or inorganic anion; and{'sub': 1', '2', '3, 'R, Rand Rare each independently selected from the group consisting of alkyl, aryl and cycloalkyl.'}4. The SRI compound of claim 3 , wherein R claim 3 , Rand Rare each independently an alkyl having from 1 to 4 carbon atoms.5. The SRI compound of claim 4 , wherein said alkyl is methyl.6. The SRI compound of claim 1 , wherein said positively charged group is a tertiary sulfonium group.7. The SRI compound of claim 1 , being derived from a compound selected from the group consisting of a selective serotonin reuptake inhibitor (SSRI) claim 1 , a serotonin-norepinephrine reuptake inhibitor (SNRI) and a serotonin-noradrenaline-dopamine reuptake inhibitor (SNDRI).8. The SRI compound of claim 7 , wherein said SSRI is selected from the group consisting of citalopram claim 7 , alaproclate claim 7 , dapoxetine claim 7 , etoperidone claim 7 , fluoxetine claim 7 , fluvoxamine claim 7 , paroxetine claim 7 , sertraline claim 7 , venlafaxine and zimelidine ...

CO-GASIFICATION OF AQUATIC BIOMASS AND COAL

The invention also relates to co-gasification processes for forming syngas from aquatic biomass and a fossil fuel. In one aspect, the invention is to a process for producing syngas, comprising: introducing aquatic biomass, a fossil fuel, water and oxygen to a gasifier and forming syngas comprising hydrogen, carbon monoxide and carbon dioxide; and feeding aquatic biomass with carbon dioxide derived from the syngas. In other aspects, the invention relates to integrated processes for producing industrial chemicals, such as alcohols, carboxylic acids, esters, aldehydes, olefins and polymers from such syngas. 1. A process for producing syngas , comprising:(a) introducing aquatic biomass, a fossil fuel, water and oxygen to a gasifier and forming syngas comprising hydrogen, carbon monoxide and carbon dioxide; and(b) feeding aquatic biomass with carbon dioxide derived from the syngas.2. The process of claim 1 , wherein the aquatic biomass that is introduced into the gasifier comprises the aquatic biomass that is fed in step (b).3. The process of claim 1 , wherein the aquatic biomass is selected from the group consisting of microalgae claim 1 , macroalgae claim 1 , microplants claim 1 , duckweed claim 1 , water hyacinth claim 1 , cattails claim 1 , banana tree stem claim 1 , kelp claim 1 , and green algae.4. The process of claim 1 , wherein the gasifier is an entrained flow slagging gasifier.5. The process of claim 4 , wherein the gasifier is operated at a pressure greater than 30 bar.6. The process of claim 4 , wherein runoff from the gasifier provides nutrients for the aquatic biomass that is fed with carbon dioxide.7. The process of claim 4 , wherein the aquatic biomass and fossil fuel are introduced to the gasifier at a weight ratio from 1:99 to 40:60.8. The process of claim 4 , wherein the aquatic biomass is formed from microalgae having an average size less than 15 μm.9. The process of claim 4 , wherein the aquatic biomass is formed from macroalgae having an average ...

Hyperpolarized agents for mri characterization of redox systems in vivo

The present invention provides a MRI probe of use in detecting and characterizing redox systems in vivo. Also provided are methods of using the probe in MR imaging experiments for diagnosis of disease in a subject, for drug discovery and for probing the redox states of biological systems in vitro.

NAPHTHOQUINONES FOR DISEASE THERAPIES

The present invention discloses novel naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones and methods of making and using the same. The present invention also discloses pharmaceutical compositions comprising novel naphtho[2,3-b]furan-4,9-dione or naphtho[2,3-b]thiophene-4,9-diones for the treatment of various indications including proliferative diseases. 2. The compound of claim 1 , wherein n is 0.3. The compound of claim 1 , wherein n is 1.4. The compound of claim 1 , wherein m is 0.5. The compound of claim 1 , wherein m is 1.6. The compound of claim 1 , wherein m is 2.7. The compound of claim 1 , wherein Ris halogen.8. The compound of claim 1 , wherein Ris hydrogen.9. The compound of claim 1 , wherein Ris optionally substituted amine.10. The compound of claim 1 , wherein Ris hydrogen.11. The compound of claim 1 , wherein Ris hydroxyl.12. The compound of claim 1 , wherein Ris hydrogen.13. The compound of claim 1 , wherein R′ is —S(O)R.14. The compound of claim 1 , wherein R′ is —S(O)R.15. The compound of claim 1 , wherein R′ is —NO.16. The compound of or claim 1 , wherein Ris optionally substituted Caliphatic.17. The compound of claim 16 , wherein Ris methyl.18. The compound of claim 16 , wherein Ris —CF.19. The compound of or claim 16 , wherein Ris optionally substituted phenyl.20. The compound of claim 1 , wherein X is O.21. The compound of claim 1 , wherein X is S.2524. A pharmaceutical composition comprising a compound as claimed in any one of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , and a pharmaceutically acceptable excipient claims 1 , carrier claims 1 , or diluent.2624. A method of treating a subject suffering from or susceptible to a disease claims 1 , disorder claims 1 , or condition claims 1 , the method comprising administering to the subject a therapeutically effective amount of a compound of any one of - or a composition thereof.27. The method of claim 26 , wherein the disease claim 26 , disorder claim 26 ...

PROCESS FOR RECOVERY OF MALEIC ANHYDRIDE BY USING ORGANIC SOLVENT

A process for the recovery of maleic anhydride from the gas produced by the catalytic oxidation of hydrocarbon, n-butane or benzene, is characterized by: 115-. (canceled)16. A process for recovering maleic anhydride from a gaseous reaction mixture , said process comprising the following steps:{'b': 1', '21', '1', '2, '(a) Feeding the reaction gas mixture () at temperature between 120 to 200° C. to an high efficiency absorption column (), wherein the absorber includes a feed zone (F), an absorption section (C, C, Am, Af) disposed above the feed zone (F) and a stripping section (S) disposed below the feed zone (F);'}{'b': '21', 'claim-text': [{'b': 1', '23', '8, '(i) a first gas cooling section comprising a packing section (C) where the sensible and the absorption heat is removed through the cooling of a recirculation solvent stream, withdrawn from a chimney tray located above the feed zone, cooled in an external heat exchanger () by cooling water at controlled temperature and recycled back () above said packing section;'}, {'b': 2', '1', '2', '7', '22, '(ii) a second gas cooling section (C) above the first one, for removing from 10 to 30% of the total heat removed from the two cooling sections (C, C), through a recirculation solvent stream () cooled in a heat exchanger () using cooling water at controlled temperature);'}, {'b': '3', '(iii) a main absorption section (Am), consisting in fractionation trays, where the reaction gas at temperature below 90° C. are contacted with a stream () of organic solvent stripped under vacuum, but still containing a small amount of maleic anhydride, fed under controlled conditions of flow-rate and temperature, to an intermediate tray near to the top of the absorption column,'}, {'b': '2', '(iv) a final absorption section, (Af) consisting in one or more suitable trays, where the reaction gas, at this point containing a very small amount of maleic anhydride, are further washed by a small stream () of organic solvent, typically from 10 ...

PRODUCTION OF 5 HYDROXYMETHYULFURFURAL (HMF) FROM HEXOSE SOLUTIONS IN THE PRESENCE OF STEAM

Method for producing 5-hydroxymethylfurfural (HMF), wherein 114-. (canceled)15. A method for producing 5-hydroxymethylfurfural (HMF) , comprising a hexose and', 'a high-boiling component which comprises an organic solvent with a boiling point greater than 200° C. (at standard pressure), to a reaction vessel,, 'a) feeding a starting solution which comprises'}b) in the reaction vessel, converting the hexose to HMF in the presence of steam with the simultaneous distillative removal of the HMF andc) obtaining a distillate comprising an aqueous, HMF-comprising solution.16. The method according to claim 15 , wherein the hexose is fructose claim 15 , glucose or mixtures of fructose and glucose.17. The method according to claim 15 , wherein the high-boiling component is a polyether.18. The method according to claim 17 , wherein the polyether is a poly-C2- to C4-alkylene glycol claim 17 , the terminal hydroxyl groups of which are optionally etherified with C1-C4 alkyl groups.19. The method according to claim 15 , wherein the starting solution comprises the high-boiling component in amounts of from 5 to 90% by weight.20. The method according to claim 15 , wherein the starting solution is an aqueous solution.21. The method according to claim 15 , wherein the reaction to give HMF takes place in the presence of an acid which is soluble in the starting solution.22. The method according to claim 15 , wherein the reaction to give HMF takes place at 100° C. to 200° C.23. The method according to claim 15 , wherein the reaction to give HMF takes place at a pressure of from 1 to 300 mbar.24. The method according to claim 15 , wherein the method is carried out continuously claim 15 , where the starting solution and steam are fed to the evaporator continuously and the product solution is drawn off continuously.25. The method according to claim 15 , wherein the reaction vessel is a thin-film evaporator.26. The method according to claim 15 , wherein the steam is fed countercurrently to the ...

PREPARATION OF 5-HYDROXYMETHYLFURFURAL (HMF) FROM SACCHARIDE SOLUTIONS IN THE PRESENCE OF A SOLVENT HAVING A BOILING POINT GREATER THAN 60ºC AND LESS THAN 200ºC (AT STANDARD PRESSURE, CALLED LOW BOILER FOR SHORT)

A process for preparing 5-hydroxymethylfurfural (HMF), which comprises 116-. (canceled)17. A process for preparing 5-hydroxymethylfurfural (HMF) , which comprises at least one saccharide and', 'a high boiler comprising an organic solvent having a boiling point greater than 200° C. (at standard pressure) and', 'water,, 'a) feeding a starting solution comprising'}and low boiler comprising a solvent having a boiling point greater than 60° C. and less than 200° C. (at standard pressure) to a reaction vessel,b) converting hexose to HMF in the reaction vessel in the presence of water vapor with simultaneous distillative removal of the HMF andc) obtaining, as a distillate, an aqueous, HMF-comprising solution.18. The process according to claim 17 , wherein the at least one saccharide is fructose claim 17 , glucose or mixtures of fructose and glucose.19. The process according to claim 17 , wherein the high boiler is a polyether or an ionic liquid.20. The process according to claim 19 , wherein the ionic liquid comprises imidazolium chlorides or imidazolium methanesulfonates.21. The process according to claim 17 , wherein the starting solution is prepared by the following steps:A1) the saccharide and water are present in a reaction vessel,A2) a further reaction vessel is initially charged with the high boiler and preferably a catalyst,A3) immediately prior to process step b), the components are mixed, preferably in a mixing chamber,the solutions of steps A1 and A2 being preheated to a temperature between 150 and 200° C. in the two reaction vessels separated from one another prior to the mixing.22. The process according to claim 17 , wherein the low boiler is water vapor claim 17 , methanol or 2-butanol.23. The process according to claim 17 , wherein the starting solution comprises the high boiler in amounts of 5 to 90% by weight.24. The process according to claim 17 , wherein the starting solution comprises a metal chloride or metal nitrate of the formula MXn where M is a ...

METHODS FOR TREATING OR PREVENTING CANCER AND NEURODEGENERATIVE DISEASES

Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: 218-. (canceled)21. (canceled)23. The method of claim 20 , wherein each Ris H.24. (canceled)25. The method of claim 20 , wherein v is 1 and X is in the 5-position of the thiopheno group.26. The method of claim 20 , wherein p is 1 and Ris in the 4-position of the phenyl group.2830-. (canceled)34. The method of claim 31 , wherein each Ris H.35. The method of claim 31 , wherein Ris H or methyl.36. The method of claim 31 , wherein Ris methyl.37. The method of claim 31 , wherein q is 0.38. The method of claim 31 , wherein v is 1 and X is in the 5-position of the thiopheno group.41. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease claim 31 , Parkinson's disease claim 31 , ALS claim 31 , or MS.42. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease. This application claims priority to U.S. Provisional Patent Application Ser. No. 61/139,751, filed Dec. 22, 2008, the entire content of which is incorporated herein by reference.The invention relates to methods of treatment or prevention of cancer and neurodegenerative diseases comprising administering an effective amount of a Sulfonamide-Based Compound to a subject.Alzheimer's disease (AD) is the most prevalent form of dementia. It is a neurodegenerative disorder, clinically characterized by progressive loss of memory and general cognitive function, and pathologically characterized by the deposition of extracellular proteinaceous plaques in the cortical and associative brain regions of sufferers. These plaques mainly comprise fibrillar aggregates of beta-amyloid peptide (Aβ). Aβ is formed from amyloid precursor protein (APP). APP is a ubiquitous membrane-spanning (type 1) glycoprotein, of which three major isoforms (APP695, APP751, and APP770) are known, that ...

METHODS OF MANAGING BLOOD SUGAR LEVELS AND COMPOSITIONS RELATED THERETO

The disclosure relates to methods of managing blood sugar levels and compositions related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diabetes, insulin resistance, or hyperglycemia comprising administering to a subject diagnosed with, at risk of or exhibiting symptoms of diabetes, insulin resistance, or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I. 2. The compound of claim 1 , wherein Rand Rare hydroxy substituted with formyl claim 1 , wherein formyl is substituted with R.3. The compound of claim 1 , wherein Ris a halogen.4. The compound of claim 1 , wherein Ris halogen.5. The compound of selected from:5,8-diacetyloxy-2,3-dichloro-1,4-naphthoquinone;5-acetyloxy-2,3-dichloro-1,4-naphthoquinone;2-((4-chlorophenyl)amino)naphtho[2,3-d]thiazole-4,9-dione, and2-((2,4-dichlorophenyl)amino)naphtho[2,3-d]thiazole-4,9-dione.6. A method of treating or preventing diabetes claim 1 , insulin resistance claim 1 , or hyperglycemia comprising administering to a subject diagnosed with claim 1 , at risk of claim 1 , or exhibiting symptoms of diabetes claim 1 , insulin resistance claim 1 , or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I claim 1 , as provide in .7. The use of a compound as provided in in the production of a medicament for the treatment of diabetes claim 1 , insulin resistance claim 1 , or hyperglycemia.8. A pharmaceutical composition comprising a compound of formula I a provided in .10. The method of claim 9 , wherein X is NH.11. The method of claim 9 , wherein Ris carbocyclyl claim 9 , aryl claim 9 , or heterocyclyl optionally substituted R.12. The method of claim 9 , wherein Ris a halogen.13. The method of claim 9 , wherein Rand Rare not hydroxy or alkoxy.14. The method of claim 9 , wherein Rand Rare hydrogen.15. The method of claim 9 , wherein the subject is diagnosed with Type 1 or Type 2 diabetes. This application claims priority to U.S ...

TREATMENT OF HYPERTENSION AND/OR PREVENTION OR TREATMENT OF HEART FAILURE IN A MAMMAL RECEIVING ANTI-COAGULANT THERAPY

The invention relates to methods and pharmaceutical compositions for treating hypertension and/or preventing or treating heart failure in a mammal receiving anti-coagulant therapy using compound(s) which are therapeutically effective but do not impact the pharmacokinetic or the pharmacodynamic effect(s) of the anti-coagulant, such as warfarin. 114-. (canceled)15. A method of treating hypertension and/or preventing or treating heart failure in a mammal receiving anti-coagulant therapy comprising administering to said mammal: {'br': None, 'sub': 1', '2', 'y', '2, '[(A)(A)](C)·x HO \u2003\u2003(I)'}, 'a) a pharmaceutical composition comprising a therapeutically effective amount of the compound of the formula [{'sub': '1', 'Ais S—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form;'}, {'sub': '2', 'Ais (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form;'}, '(Cat) is a cation;', 'y is 1 to 3; and', 'x is 0 to 3;, 'wherein'}or (i) valsartan or a pharmaceutically acceptable salt thereof; and', '(ii) N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methylbutanoic acid ethyl ester or (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionyl amino)-2-methyl-pentanoic acid or a pharmaceutically acceptable salt thereof., 'b) a pharmaceutical composition comprising a therapeutically effective amount of'}16. The method of wherein the mammal is a human.17. The method of wherein the compound of formula (I) is trisodium [3-((1S claim 15 ,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate.18. The method of wherein the anticoagulant treatment comprises administration of warfarin or a pharmaceutically acceptable salt thereof.19. The method of wherein the heart failure is congestive heart failure claim 15 , left heart failure claim 15 , right heart failure claim 15 , ...

GPR 17 Agonists and Screening Assay

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I. 17.-. (canceled)9. The method according to claim 8 , wherein the GPR17 mediated disease is multiple sclerosis.11. The screening assay according to further comprising means for determining the GPR17 activity claim 10 ,wherein, optionally, said means for determining the GPR17 activity is selected from one or more of the group consisting of:a. means for determining the release of calcium from intracellular calcium stores associated with GPR17 activation, said means optionally comprising a cell membrane permeable indicator which binds to calcium released within the cell thereby providing a measurable signal, preferably fluorescence or luminescence;{'sub': Y', 'Y, 'sup': '35', 'b. means for determining GTPS binding to heterotrimeric G proteins, wherein said heterotrimeric G protein is optionally SGTPS;'}c. means for determining the inhibition of cAMP formation or its increase associated with GPR17 activation, said means optionally comprising a stimulator of the adenylyl cyclase and a suitable cAMP indicator system;d. means for determining the increase in inositolphosphates (IP), quantified as IP1, said means optionally comprising a suitable IP 1 detector system; ande. means for determining the recruitment of cytoplasmic β-arrestin proteins, optionally by detection of the B-arrestin translocation to the receptor using fluorescence or bioluminescence resonance energy transfer.12. The screening assay according to (c) wherein said stimulator of the adenylyl cyclase is forskolin claim 11 , and wherein said cAMP indicator system is a competitive immunoassay claim 11 , optionally providing a fluorescence signal.13. (canceled)14. A compound selected from3-(2- ...

Novel flavonoids and uses thereof

The present invention provides novel flavonoids extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the flavonoid and a method for treating inflammation in a subject, which method comprises administering to said subject an effective amount of the flavonoid and a pharmaceutically acceptable carrier or excipient.

CHEMICAL TRANSFORMATION OF LIGNOCELLULOSIC BIOMASS INTO FUELS AND CHEMICALS

A method for converting a carbohydrate to a furan in a polar aprotic solvent in the presence of a chloride, bromide, or iodide salt or a mixture thereof and optionally in the presence of an acid catalyst, a metal halide catalyst and/or an ionic liquid (up to 40 wt %). The method can be employed in particular to produce furfural or 5-hydroxymethylfurfural. 1. A method for converting a carbohydrate to a furan which comprises the steps of:(a) preparing a mixture of the carbohydrate in a polar aprotic solvent containing a chloride, bromide, or iodide salt;(b) heating the mixture to obtain a furan.2. The method of wherein the reaction is carried out to produce greater than 30 wt % of the furan product in the reaction mixture.3. The method of wherein the concentration of the salt ranges from 0.5 wt % to 15 wt %.4. (canceled)5. (canceled)6. (canceled)7. The method of wherein the furan is HMF or furfural.8. (canceled)9. (canceled)10. (canceled)11. The method of wherein the carbohydrate is or comprises cellulose.12. The method of wherein the carbohydrate is a lignocellulosic feedstock.13. The method of wherein the solvent is DMA.14. (canceled)15. The method of further comprising adding a metal catalyst to the solvent before or after adding the carbohydrate.16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. The method of wherein the ionic liquid is selected an alkylimidazolium ionic liquid claim 39 , an alkylimidazolium halide ionic liquid claim 39 , an alkylimidazolium chloride ionic liquid claim 39 , an alkylpyridinium ionic liquid claim 39 , an alkylpyridinium halide ionic liquid claim 39 , an an alkylpyridinium chloride ionic liquid or a combination thereof.21. The method of wherein the ionic liquid is selected from [EMIM]Cl claim 20 , [BMIM]Cl claim 20 , [EMIM]Br claim 20 , 1-ethyl-2 claim 20 ,3-dimethylimidazolium chloride claim 20 , 1-ethylpyridinium chloride claim 20 , 1-butyl-4-methylpyridinium chloride claim 20 , or a mixture thereof.22. (canceled)23. A ...

RUTHENIUM-DIAMINE COMPLEXES AND METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUNDS

Provided is a catalyst for asymmetric reduction, which can be produced by a convenient and safe production method, has a strong catalytic activity, and has excellent stereoselectivity. The present invention relates to a ruthenium complex represented by the following formula (1): wherein Rrepresents an alkyl group or the like; Y represents a hydrogen atom; X represents a halogen atom or the like; j and k each represent 0 or 1; Rand Reach represent an alkyl group or the like; Rto Reach represent a hydrogen atom, an alkyl group or the like; Z represents oxygen or sulfur; nrepresents 1 or 2; and nrepresents an integer from 1 to 3, a method for producing the ruthenium complex, a catalyst for asymmetric reduction formed from the ruthenium complex, and methods for selectively producing an optically active alcohol and an optically active amine using the catalyst for asymmetric reduction. 4. A method for producing a reduction product by reducing an organic compound in the presence of the ruthenium complex as set forth in and a hydrogen donor.5. A method for producing an optically active alcohol claim 1 , the method comprising reducing a carbonyl group of a carbonyl compound in the presence of the ruthenium complex according to and a hydrogen donor.6. A method for producing an optically active amine claim 1 , the method comprising reducing an imino group of an imine compound in the presence of the ruthenium complex according to and a hydrogen donor.7. The method according to claim 4 , wherein the hydrogen donor is selected from formic acid claim 4 , a formic acid alkali metal salt claim 4 , and an alcohol having a hydrogen atom on the α-position carbon atom substituted with a hydroxyl group.8. The method according to claim 4 , wherein the hydrogen donor is hydrogen.9. A catalyst for reduction claim 4 , comprising the ruthenium complex according to .10. The catalyst according to claim 9 , wherein the catalyst is a catalyst for asymmetric reduction. The present invention ...

BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Compounds of the formula I: 2. The compound of claim 1 , wherein R claim 1 , Rand Rare hydrogen.3. The compound of claim 2 , wherein Ris phenyl substituted at the 4-position with methyl or halo and optionally substituted at the 2-position with halo.4. The compound of claim 2 , wherein Ris 4-methyl-phenyl.5. The compound of claim 2 , wherein Ris pyridin 2-yl substituted with methyl or halo at the 5-position.6. The compound of claim 2 , wherein Ris 5-methyl-pyridin-2-yl.8. The compound of claim 7 , wherein Ris hydrogen.9. The compound of claim 7 , wherein Ris methyl.10. The compound of claim 7 , wherein Ris: Calkyl; Calkyloxy-Calkyl; hydroxy-Calkyl; Calkylsulfanyl-Calkyl; Calkylsulfonyl-Calkyl; amino-Calkyl; N—Calkyl-amino-Calkyl; N claim 7 ,N-di-Calkyl-amino-Calkyl; Ccycloalkyl; optionally substituted phenyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.11. The compound of claim 7 , wherein Ris: Calkyloxy-Calkyl; hydroxy-Calkyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.12. The compound of claim 7 , wherein Ris methoxymethyl.13. The compound of claim 7 , wherein Ris hydroxymethyl.14. The compound of claim 7 , wherein Ris heteroaryl selected from pyridinyl claim 7 , pyrimidinyl claim 7 , or pyrazinyl claim 7 , each of which may be optionally substituted once or twice with methyl.15. The compound of claim 7 , wherein Ris hydroxymethyl claim 7 , methoxymethyl claim 7 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.16. The compound of claim 7 , wherein Ris Calkyl claim 7 , Ccycloalkyl or Ccycloalkyl-Calkyl.17. The compound of claim 7 , wherein Ris isopropyl claim 7 , isobutyl or tert butyl.18. The compound of claim 1 , wherein said compound is selected from:4-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;5-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Furan-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Thiophene-2- ...

Antiviral Drugs for Treatment of Arenavirus Infection

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 167-. (canceled)68. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and a pharmaceutically effective amount of a compound or a pharmaceutically-acceptable salt thereof , selected from the group consisting of2-Phenyl-cyclopropanecarboxylic acid [1-(4-amino-phenyl)-eth-(E)-ylidene]-hydrazide;Cyclopropanecarboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(2,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-p-tolyl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-biphenyl-4-yl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(3,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;Furan-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2,4-Dichloro-N-(4-[1-[(2-Phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-benzamide;2-Phenyl-cyclopropanecarboxylic acid [1-(2-hydroxy-phenyl)-eth-(E)-ylidene]-hydrazide;Thiophene-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-dimethylamino-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-methoxy- ...

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

SUCCINIC ANHYDRIDE FROM ETHYLENE OXIDE

Continuous flow systems and methods produce succinic anhydride by a double carbonylation of ethylene oxide with carbon monoxide and at least one catalyst. In some embodiments, the double carbonylation occurs using a single catalyst. In other embodiments, a first catalyst is used to promote the first carbonylation, and a second catalyst different from the first catalyst is used to promote the second carbonylation. The succinic anhydride is isolated from the product stream by crystallization and the catalyst is recycled to the reaction stream. 1. A method of synthesizing an acid anhydride comprising the steps of:a) feeding a reaction stream comprising an epoxide, at least one catalyst, at least one solvent, and carbon monoxide to a reaction vessel under reaction conditions to promote a double carbonylation of the epoxide to form a dissolved acid anhydride in the reaction vessel, which exits the reaction vessel in a reaction product stream in a continuous flow process;b) treating the reaction product stream containing dissolved acid anhydride to conditions that cause the acid anhydride to crystallize such that the reaction product stream comprises crystallized acid anhydride and a liquid phase comprising dissolved catalyst and solvent;c) separating the crystallized acid anhydride from the liquid phase; andd) recycling the liquid phase comprising dissolved catalyst and solvent to the reaction stream comprising the epoxide.2. The method of claim 1 , wherein step b) occurs in an adiabatic evaporative cooling crystallizer.3. The method of claim 1 , wherein step c) occurs in a rotary drum filter.4. The method of claim 1 , wherein step d) comprises feeding the liquid phase comprising dissolved catalyst and solvent to a recovery flash drum to separate volatiles prior to returning it to the reaction stream.5. The method of claim 4 , further comprising treating the liquid phase by performing at least one step selected from the group consisting of: drying; heating or cooling; ...

OXIDATION CATALYST FOR MALEIC ANHYDRIDE PRODUCTION

A process for preparing a catalyst by selecting an active catalyst and contacting the active catalyst with one or more fluids containing an organic solvent or mixture of organic solvents. In one embodiment, each organic solvent has a dielectric constant within a range of about 5 to about 55 when measured at a temperature of 20° C. to 25° C. The catalyst thus prepared may be used in a process for preparing maleic anhydride. 1. A process for preparing a VPO catalyst comprising the steps of:{'sub': 2', '2', '7, '(i) selecting an active VPO catalyst comprising at least 90% by weight (VO)PObased on the weight of the catalyst; and'}(ii) contacting the active VPO catalyst with one or more fluids comprising an organic solvent.2. The process according to wherein the organic solvent has a dielectric constant within a range of about 5 to about 55 when measured at a temperature of 20° C. to 25° C.3. The process according to wherein the organic solvent has a dielectric constant within a range of about 10 to about 50 when measured at a temperature of 20° C. to 25° C.4. The process according to wherein the organic solvent is selected from the group consisting of methanol claim 1 , ethanol claim 1 , n-propanol claim 1 , n-butanol claim 1 , isopropanol claim 1 , isobutanol claim 1 , acetonitrile claim 1 , acetone claim 1 , methyl ethyl ketone claim 1 , DMF claim 1 , dimethyly sulfoxide claim 1 , tetrafuran claim 1 , ethylene glycol claim 1 , propylene glycol claim 1 , diethylene glycol claim 1 , dipropylene glycol claim 1 , 1 claim 1 ,4-butanediol claim 1 , glycerin and a mixture thereof.5. The process according to wherein contacting the active VPO catalyst with one or more fluids comprising an organic solvent comprises diffusing the organic solvent into the active VPO catalyst.6. The process according to wherein the active VPO catalyst further comprises a promoter.7. The process according to wherein contacting is carried out at a temperature within a range from room temperature to ...

METHOD FOR PREPARING 3-KETO-BENZOFURANE DERIVATIVES

The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, Ris hydrogen or an alkyl or aryl group, and Ris a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO—NHin the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand. 2. The method as claimed in claim 1 , wherein:{'sub': 1', '1', '8, 'R or Rrepresents a linear or branched C-Calkyl group or a phenyl group that is substituted or unsubstituted,'}{'sub': 2', '1', '8', '1', '8', '1', '8', '1', '8, 'Rrepresents a linear or branched C-Calkyl group or a phenyl group of formula II in which Y represents chlorine, bromine or iodine or a linear or branched C-Calkoxy group or a dialkylaminoalkoxy group in which each linear or branched alkyl group is a C-Cand the linear or branched alkoxy group is a C-C.'}3. The method as claimed in claim 2 , wherein:{'sub': 1', '1', '4, 'R or Rrepresents a linear or branched C-Calkyl group,'}{'sub': 2', '1', '4', '1', '4', '1', '4', '1', '4, 'Rrepresents a linear or branched C-Calkyl group or a phenyl group of formula II in which Y represents a C-Calkoxy group or a dialkylaminoalkoxy group in which each linear or branched alkyl group is a C-Cand the linear or branched alkoxy group is a C-C.'}4. The method as claimed in one of to claim 2 , wherein R represents methyl claim 2 , Rrepresents n-butyl and Rrepresents 4-[3-(di-n-butylamino)-propoxy]-phenyl.5. The method as claimed in claim 1 , the palladium compound is bis(dibenzylideneacetone)palladium(0).6. The method as claimed in claim 1 , wherein the palladium compound is tris(dibenzylideneacetone)-dipalladium(0).7. The method as claimed in claim 1 , wherein the ligand is 2-(di-tert-butylphosphino)-2′ claim 1 ,4′ ...

PROCESS FOR PREPARING BENZOFURAN DERIVATIVES SUBSTITUTED AT POSITION 5

The disclosure relates to a process for preparing benzofuran derivatives of general formula I: 2. The process as claimed in claim 1 , in which R represents an ester —COOR′ in which R′ represents an alkyl group; Rrepresents an alkyl group; and Rrepresents hydrogen or a hydroxyl claim 1 , haloalkyl claim 1 , dialkylaminoalkoxy or dialkylaminoalkyl group.3. The process as claimed in claim 1 , wherein the acid is a weak acid optionally combined with a strong acid.4. The process as claimed in claim 3 , wherein the weak acid is acetic acid.5. The process as claimed in claim 1 , wherein the oxime is cyclized in the medium in which it is formed.6. The process as claimed in claim 1 , in which:{'sub': 1', '1', '8, 'Rrepresents a linear or branched C-Calkyl group; and'}{'sub': 2', '1', '8', '1', '8', '1', '8', '1', '8, 'Rrepresents a linear or branched C-Calkyl group, a linear or branched C-Calkoxy group or a dialkylaminoalkoxy group in which each alkyl group is of C-C, and the linear or branched alkoxy group is of C-C.'}7. The process as claimed in claim 6 , in which:{'sub': 1', '1', '4, 'Rrepresents a linear or branched C-Calkyl group; and'}{'sub': 2', '1', '4', '1', '4', '1', '4', '1', '4, 'Rrepresents a linear or branched C-Calkyl group, a linear or branched C-Calkoxy group or a dialkylaminoalkoxy group in which each alkyl group is of C-C, and the linear or branched alkoxy group is of C-C.'}8. The process as claimed in claim 6 , in which Rrepresents n-butyl and Rrepresents 3-(di-n-butylamino)propoxy.9. The process as claimed in claim 6 , in which Rrepresents n-butyl and Rrepresents 3-(di-n-butylamino)propoxy.15. The benzoyloxy derivative as claimed in claim 14 , in which Y represents the group of formula XIX or the group of formula XX in which R′ represents n-butyl.16. The benzoyloxy derivative as claimed in claim 14 , in which R′ represents 3-(di-n-butylamino)propyl.17. The benzoyloxy derivative as claimed in claim 14 , in which R′ represents 3-(di-n-butylamino)propyl ...

PROCESS FOR PREPARING AMINOBENZOYLBENZOFURAN DERIVATIVES

The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: 3. The process according to or , wherein:{'sub': 1', '1', '8, 'Rrepresents a linear or branched C-Calkyl group;'}{'sub': 2', '1', '8', '1', '8', '1', '8', '1', '8, 'Rrepresents a linear or branched C-Calkyl group, a linear or branched C-Calkoxy group or a dialkylaminoalkoxy group in which each linear or branched alkyl group is a C-Calkyl group and the linear or branched alkoxy group is a C-Calkoxy group; and'}{'sub': 3', '1', '8, 'Rrepresents a linear or branched C-Calkyl group.'}4. The process as claimed in or , wherein:{'sub': 1', '1', '4, 'Rrepresents a linear or branched C-Calkyl group;'}{'sub': 2', '1', '4', '1', '4', '1', '4', '1', '4, 'Rrepresents a linear or branched C-Calkyl group, a linear or branched C-Calkoxy group or a dialkylaminoalkoxy group in which each linear or branched alkyl group is a C-Cgroup and the linear or branched alkoxy group is a C-Cgroup; and'}{'sub': 3', '1', '4, 'Rrepresents a linear or branched C-Calkyl group.'}5. The process as claimed in or , wherein Rrepresents n-butyl; Rrepresents 3-[di(n-butyl)amino]propoxy; and Rrepresents methyl.6. The process as claimed in or , wherein the hydrogen-transfer agent is a formate or a phosphinate.7. The process as claimed in claim 6 , wherein the formate is ammonium formate and the phosphinate is sodium phosphinate.8. The process as claimed in or claim 6 , wherein the hydrogen-transfer agent is used in excess with respect to the compound of formula II.9. The process as claimed in claim 8 , wherein the hydrogen-transfer agent is used in a proportion of 5 equivalents per equivalent of compound of formula II.10. The process as claimed in or claim 8 , wherein the ether is a dialkyl ether claim 8 , a cyclic ether or a mixture of these.11. The process as claimed in claim 10 , wherein the dialkyl ether is methyl tert-butyl ether and the cyclic ether is tetrahydrofuran.12. The process as claimed in or ...

PROCESS FOR THE PRODUCTION OF FURFURAL

Furfural is produced in one step at both high yield and high conversion from a feedstock comprising solid biomass and/or insoluble polysaccharide, in a high boiling, water-miscible solvent containing a soluble acid catalyst, and water. Furfural product and water can be distilled off, leaving non-volatile solvent behind. Because furfural contact with the acidic medium is minimized, degradation is kept to a minimum. The feedstock does not have to be pretreated. Because the biomass undergoes near complete dissolution, the residual material is flowable and easier to handle than residual solids reported from other processes. Further, certain by-products (e.g., humins, lignins) solubilized in the reaction solvent can be precipitated by addition of water or aqueous solution and then removed from the reaction mixture. 1. A process comprising:(d) providing a reactor comprising a distillation column disposed on top of a reaction vessel, wherein the reaction vessel contains a biomass feedstock, water, a soluble acid catalyst and a water-miscible organic solvent having boiling point of at least 100° C., wherein the biomass feedstock comprises solid biomass, insoluble polysaccharide or a mixture thereof;(e) adding water to the reaction vessel and bringing the contents of the reaction vessel to a temperature in the range of 100-250° C. and a pressure in the range of 0.0001-0.21 MPa to form a reaction mixture for a residence time sufficient to produce a mixture of water and furfural; and(f) removing the mixture of water and furfural from the top of the distillation column.2. The process according to further comprising recovering at least one of formic acid or acetic acid from the distillation column in step (c).3. The process according to claim 1 , wherein the process is a continuous process further comprising:(d) distilling at least a portion of the contents of the reaction vessel to remove distillates including levulinic acid, that have boiling points between that of furfural/ ...

2-Alkyl-Cycloalk(en)yl-Carboxamides

Novel -alkylcycloalk(en)ylcarboxamides of the formula (I) 3. Composition for controlling unwanted microorganisms claim 1 , characterized in that it comprises at least one 2-alkylcycloalk(en)ylcarboxamide of the formula (I) according to claim 1 , in addition to extenders and/or surfactants.4. Use of 2-alkylcycloalk(en)ylcarboxamides of the formula (I) according to for controlling unwanted microorganisms.5. Method for controlling unwanted microorganisms claim 1 , characterized in that 2-alkyl-cycloalk(en)ylcarboxamides of the formula (I) according to are applied to the microorganisms and/or their habitat.6. Process for preparing compositions for controlling unwanted microorganisms claim 1 , characterized in that 2-alkylcycloalk(en)ylcarboxamides of the formula (I) according to are mixed with extenders and/or surfactants. The present invention relates to novel 2-alkylcycloalk(en)ylcarboxamides, to a plurality of processes for their preparation and to their use for controlling unwanted microorganisms.It is already known that numerous carboxamides have fungicidal properties (cf., for example, WO 98/03495, WO 98/03486 and EP-A 0 589 313). Thus, some 2-alkylcycloalkylcarboxamides are already known, such as, for example, N-(2-sec-butylcyclohexyl)-2-methyl-4,5-dihydrofuran-3-carboxamide from WO 98/03495, N-[2(2-ethylbutyl)cyclohexyl]-5-fluoro-1,3-dimethyl-1H-pyrazole-4-carboxamide from WO 98/03486 and N-2-sec-butylcyclohexyl)-2-methyl-4-(trifluoromethyl)-1,3-thiazole-5-carboxamide from EP-A 0 589 313. The activity of these compounds is good; however, in some cases, for example at low application rates, it is unsatisfactory.This invention now provides novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I)in whichRrepresents hydrogen, halogen, hydroxyl, cyano, C-C-alkyl, C-C-haloalkyl, C-C-haloalkoxy or C-C-haloalkylthio having in each case 1 to 5 halogen atoms,Furthermore, it has been found that 2-alkylcycloalk(en)ylcarboxamides of the formula (I) are obtained whenR—X  ( ...

Haloalkyl-Substituted Amides as Insecticides and Acaricides

The present invention relates to halogen-substituted amide derivatives of the general formula (I) 4. A compound of formula (I) and the diastereomers claim 1 , enantiomers claim 1 , E/Z isomers and salts thereof according to claim 1 , where{'sup': '1', 'Ris hydrogen, nitro, cyano, fluorine, chlorine, bromine, iodine, methyl, ethyl, n- or i-propyl, fluoromethyl, chloromethyl, trichloromethyl, difluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, trifluoromethyl, fluoroethyl, chloroethyl, difluoroethyl, dichloroethyl, trifluoroethyl, chlorofluoroethyl, chlorodifluoroethyl, dichlorofluoroethyl, tetrafluoroethyl, pentafluoroethyl, chlorotetrafluoroethyl, trichloroethyl, heptafluoro-n-propyl, heptafluoroisopropyl, methoxy, ethoxy, n- or i-propoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, methylthio, ethylthio, difluoromethylthio, trifluoromethylthio, chlorodifluoromethylthio, methylsulphinyl, trifluoromethylsulphinyl, trifluoromethylsulphonyl, methylsulphonyl, ethylsulphonyl, acetyl, propionyl, methoxycarbonyl, ethoxycarbonyl, methylaminocarbonyl, dimethylaminocarbonyl or ethylaminocarbonyl,'}n is 1, 2 or 3,{'sup': '2', 'Ris hydrogen, methyl or ethyl,'}{'sup': '3', 'Ris hydrogen, methyl, ethyl, 2-ethynyl, 2-propenyl, methoxymethyl, ethoxymethyl, methylcarbonyl, ethylcarbonyl, methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, i-propoxycarbonyl, n-butoxycarbonyl, t-butoxycarbonyl or phenoxycarbonyl,'}{'sup': 8', '4, 'V is —O— or —N(R)—, and is bonded to Qvia a single bond, where'}{'sup': '8', 'Ris hydrogen, methyl, ethyl, methylcarbonyl, ethylcarbonyl, methoxymethyl, ethoxymethyl, cyanomethyl, cyanoeth-2-yl, propyl, phenylmethyl, prop-2-en-1-yl, prop-2-yn-1-yl, benzyloxy, methoxycarbonyl, ethoxycarbonyl, methoxycarbonylmethyl, ethoxycarbonylmethyl, methoxycarbonyleth-2-yl, ethoxycarbonyleth-2-yl, amidomethyl, amidoethyl or amidoprop-3-yl,'}{'sup': '5', 'Ris hydrogen,'}{'sup': '6', 'Ris hydrogen, nitro, cyano, fluorine, chlorine, bromine, iodine, methyl, ...

PROCESS FOR PRODUCING A RINGLIKE OXIDIC SHAPED BODY

A process for producing a ringlike oxidic shaped body by mechanically compacting a pulverulent aggregate introduced into the fill chamber of a die, wherein the outer face of the resulting compact corresponds to that of a frustocone. 1. A ringlike oxidic shaped body obtained by a process comprising the mechanical compaction of a pulverulent aggregate which has been introduced into the fill chamber of a die and is composed of constituents which comprise at least one metal compound which can be converted to a metal oxide by thermal treatment at a temperature of ≧100° C. , or at least one metal oxide , or at least one metal oxide and at least one such metal compound , to give a ringlike shaped precursor body , in which the fill chamber is disposed in a die bore conducted through the die material from the top downward with a vertical bore axis B and is delimited bythe inner wall of the die bore,the upper end face of a lower punch introduced from below along the bore axis B into the die bore so as to be liftable and lowerable, on which the pulverulent aggregate introduced into the fill chamber rests,the lower end face, disposed along the bore axis B at an axial starting distance A above the upper end face of the lower punch, of an upper punch mounted so as to be liftable and lowerable along the bore axis B, whose lower end face is in contact with the pulverulent aggregate introduced into the fill chamber from above, andthe outer face of a center pin MF conducted from the bottom upward in the die bore along the bore axis B from the geometric center of the upper end face of the lower punch, said center pin MF extending at least up to the geometric center of the lower end face of the upper punch,the process comprising reducing the axial starting distance A of the two end faces along the bore axis B to an axial end distance E predefined for the compaction by lowering the upper punch while maintaining the position of the lower punch or additionally lifting the lower punch, ...