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Способ получения чистого эпсилон-капролактона

Способ получения -лактона хлоризонитрозопропионовой кислоты

INHIBITING HETEROCYCLIC DERIVATIVES OF DIHIDROOROTATO DESHIDROGENASA, PHARMACEUTICAL COMPOSITIONS CONTAIN THAT THEM, PROCESS TO PREPARE THEM AND USE OF THE SAME FOR THE AUTOIMMUNE TREATMENT OF CANCER AND OTHER UPHEAVALS.

Los compuestos son utiles, por ejemplo, en el tratamiento de trastornos autoinmunes, como, por ejemplo, la esclerosis multiple y, también, en el tratamiento de trastornos de cáncer. Reivindicacion 1: Un compuesto de acuerdo con la formula 1 donde R1 denota COOH, COOA, COA, CF3, acilo, ciano, Het, tetrazoílo, sulfonilo, o si Q es -C=C- o hetarileno, o si Q es un arileno tetrasustituido, R1 también denota CON(R3)2 o CONHA; R2 denota H, Hal, A, O-A, Ar; Ra denota Ar, Het, O-Het, NH-Het, O-Ar, -O-(CH2)m-Het, -NH-(CH2)mHet, NH-Ar, S(O)2Ar, S(O)Ar, -S-Ar, OCF3, Y denota CRf o N, X1, X2 denotan cada uno de manera independiente uno del otro CRcRd, NRc, NRd, y cuando Y denota CRf, también O o S, con la condicion que uno de X1 y X2 sea CRcRd o NRc; Rb y Rc representan juntos un enlace químico; Rf y Re representan juntos un enlace químico, cuando Y es CRf; Re y Rc, en la definicion de X1, representan juntos un enlace químico cuando Y es N, y Rb y Rc, en la definicion de x2, representan juntos un enlace ...

A PROCEDURE FOR THE PREPARATION OF REP THEM POLYMERIC VESICULADAS

Organic semiconductor material and organic thin-film transistor

An organic thin-film transistor comprising a gate electrode, a gate insulator layer, an organic semiconductor layer, a source electrode and a drain electrode wherein the organic semiconductor layer consists of the organic semiconductor material having the structure represented by the general formula (1) shown below, and the organic semiconductor layer has crystallinity: wherein L represents a bivalent linker group having the structure consisting of one group or any combination of two or more groups selected from unsubstituted or fluorinated benzene residue, unsubstituted or fluorinated thiophene residue, unsubstituted or fluorinated thienothophene residue; R 1 represents carbonyl group, cyano group or C 1 -C 6 fluorinated alkyl group; R 2 represents halogen atom, cyano group, carbonyl group or acetyl group.

УСТАНОВКА ДЛЯ ВЫДЕЛЕНИЯ ДИГИДРОКВЕРЦЕТИНА ИЗ ДРЕВЕСИНЫ ЛИСТВЕННИЦЫ

Установка для выделения дигидрокверцетина из древесины лиственницы, содержащая бункер-питатель, узел подачи растворителя, подогреватель, сборник экстракта-растворителя, и по меньшей мере две линии экстракт-растворителей для выделения дигидрокверцетина, каждая из которых содержит подводящие и отводящие вентили, реактор-экстрактор, и пульповый насос, отличающаяся тем, что в нее введен конденсатор паров экстракта-растворителя, а в каждой из линий установлены подогреватель и пульсатор, при этом каждый из экстракторов соединен одним из входов с выходом бункера-питателя, другим входом через первый подводящий вентиль - с узлом подачи экстракта, одним из выходов связан со входом конденсатора, выход которого через вторые подающие вентили также соединен с другим входом каждого из экстракторов, другой выход каждого из которых через последовательно соединенные подогреватель, насос, пульсатор и третий подающий вентиль связан с третьим входом каждого из экстракторов, третьи выходы которых через третий насос и четвертый вентиль соединены со сборником экстракта-растворителя. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 66 199 (13) U1 (51) МПК A61K 36/00 (2006.01) C07D 311/40 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2007116823/22 , 03.05.2007 (24) Дата начала отсчета срока действия патента: 03.05.2007 (45) Опубликовано: 10.09.2007 (73) Патентообладатель(и): ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "ЭЛИОР" (RU), Мальчиков Евгений Леонидович (RU) U 1 6 6 1 9 9 R U Ñòðàíèöà: 1 U 1 Формула полезной модели Установка для выделения дигидрокверцетина из древесины лиственницы, содержащая бункер-питатель, узел подачи растворителя, подогреватель, сборник экстракта-растворителя, и по меньшей мере две линии экстракт-растворителей для выделения дигидрокверцетина, каждая из которых содержит подводящие и отводящие вентили, реактор-экстрактор, и пульповый насос, отличающаяся тем, что в нее введен ...

УСТРОЙСТВО ДЛЯ ЖИДКОФАЗНОГО ТЕРМИЧЕСКОГО ОКИСЛЕНИЯ ФТОРОЛЕФИНОВ

Устройство для проведения жидкофазного термического окисления фторолефинов, включающее стальной реактор с патрубком, электрообогреватель, термопару и приспособление для регулирования температуры, отличающееся тем, что приспособление для регулирования температуры конструктивно выполнено в виде трубчатого змеевика, навитого на верхнюю часть реактора. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 104 870 (13) U1 (51) МПК B01J 10/00 (2006.01) C07D 303/08 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21)(22) Заявка: 2010113819/04, 09.04.2010 (24) Дата начала отсчета срока действия патента: 09.04.2010 (45) Опубликовано: 27.05.2011 1 0 4 8 7 0 R U Формула полезной модели Устройство для проведения жидкофазного термического окисления фторолефинов, включающее стальной реактор с патрубком, электрообогреватель, термопару и приспособление для регулирования температуры, отличающееся тем, что приспособление для регулирования температуры конструктивно выполнено в виде трубчатого змеевика, навитого на верхнюю часть реактора. Ñòðàíèöà: 1 ru CL U 1 U 1 (54) УСТРОЙСТВО ДЛЯ ЖИДКОФАЗНОГО ТЕРМИЧЕСКОГО ОКИСЛЕНИЯ ФТОРОЛЕФИНОВ 1 0 4 8 7 0 Адрес для переписки: 198035, Санкт-Петербург, ул. Гапсальская, 1, ФГП "Ордена Ленина и ордена Трудового Красного Знамени НИИ синтетического каучука имени академика С.В. Лебедева", начальнику ИКЦ П.П. Шпакову (73) Патентообладатель(и): Федеральное государственное унитарное предприятие "Ордена Ленина и ордена Трудового Красного Знамени научноисследовательский институт синтетического каучука имени академика С.В. Лебедева" (RU) R U Приоритет(ы): (22) Дата подачи заявки: 09.04.2010 (72) Автор(ы): Емельянов Геннадий Анатольевич (RU), Родин Виктор Михайлович (RU), Костычева Дарья Михайловна (RU), Кулаченков Сергей Анатольевич (RU) U 1 U 1 1 0 4 8 7 0 1 0 4 8 7 0 R U R U Ñòðàíèöà: 2 RU 5 10 15 20 25 30 35 40 45 50 104 870 U1 Предложение относится к области технологии получения ...

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

Chroman derivatives, medicaments and use in therapy

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

Acetals as perfuming ingredients

Acetal derivatives of 2,2,3,6-tetramethyl-1-cyclohexane/ene-carbaldehyde of formula (I): for use in the perfumery industry as well as the resulting compositions or articles containing one or more of these compounds. In formula (I), one dotted line indicates the presence of a carbon-carbon single or double bond and the other dotted line indicates the presence of a carbon-carbon single bond, R 1 represents a hydrogen atom or a methyl or ethyl group; and each R, taken alone, simultaneously or independently, represents a C 1-3 alkyl or alkenyl group, or the R groups, taken together, represent a C 2-6 hydrocarbon group optionally including an oxygen atom.

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.

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.

Method for preparation of pitavastatin and its pharmaceutical acceptable salts thereof

The present invention discloses a compound, which is alkali or alkaline earth metal salts of pitavastatin, wherein the alkali or earth metal comprise one or more of magnesium, zinc, potassium, strontium and barium.

Process for the production of carnitine from beta-lactones

The invention relates to a method for the production of L-carnitine, wherein a β-lactone, which is a 4-(halomethyl)oxetane-2-one, is converted into carnitine with trimethylamine (TMA), wherein the β-lactone is not subjected to a basic hydrolysis step before being contacted with the trimethylamine. The invention also relates to a carnitine having a unique impurity profile.

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.

Novel Methods for Regeneration of Solvents for Extractive Processes

An improved solvent regeneration system for extractive distillation and liquid-liquid extraction processes capable of effectively removing heavy hydrocarbons and polymeric materials that otherwise develop in a closed solvent loop. The improved process employs a light hydrocarbon displacement agent, which is at least partially soluble in the solvent to squeeze the heavy hydrocarbons and polymeric materials out of the solvent, with virtually no additional energy requirement. It has been demonstrated that the light non-aromatic hydrocarbons in the raffinate stream generated from the extractive distillation or the liquid-liquid extractive process for aromatic hydrocarbons recovery can displace not only the heavy non-aromatic hydrocarbons but also the heavy aromatic hydrocarbons from the extractive solvent, especially when the aromatic hydrocarbons in the solvent are in the C 10+ molecular weight range.

Developers and method of coloring lithographic printing members

A color contrast image in imaged lithographic printing precursors can be obtained by contacting the imaged precursor with a coloration solution containing a colorless form of a photochromic compound. Residual amounts of this compound attached to the oleophilic surface of the imaged precursor can be changed to its colored form when exposed to UV light. The coloration solution can be an alkaline or acidic developer or an alkaline or acidic solution used separately after development. The coloration solution can also be a gum solution.

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.

Bait chemistries in hydrogel particles for serum biomarker analysis

This invention describes the identification of novel organic dye chemistries that can be used as affinity baits to capture proteins and other biomolecules useful in the fields of medical diagnostics, environmental science, toxicology, and infectious disease. Incorporation of unique affinity dye compounds within hydrogel capture particles improves analyte yield and preanalytical precision, and stabilizes the analyte against degradation, while increasing measurement sensitivity. The particles in this invention can be used for routine clinical testing as well as for discovery of low abundance disease biomarkers. Example hydrogel particles containing new high affinity bait chemistries were used to identify a new set of human serum biomarkers.

Novel microbiocides

Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

Process for the preparation of strontium ranelate

The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula III, which is a useful intermediate in the synthesis of strontium ranelate. wherein R 1 and R 2 represents substituted or unsubstituted linear or branched C 1 -C 6 alkyl group or C 3 -C 12 cyclic group.

Process for producing propylene oxide

A multiple liquid phase composition and process for preparing propylene oxide including a reaction mixture of: (a) propylene, (b) at least one peroxide compound, (c) at least one catalyst, such as a titanium silicalite-1 (TS-I) catalyst, and (d) and a predetermined amount of a solvent mixture; wherein the solvent mixture comprises at least (i) at least one alcohol, such as methanol, and (ii) at least one non-reactive co-solvent; wherein the solvents are mixed at a predetermined concentration; wherein the non-reactive co-solvent has a different boiling point than propylene oxide; and wherein the resulting propylene oxide product partitions into a high affinity solvent during the reaction. The process of the present invention advantageously produces a waste stream with little or no significant amount of sodium chloride (NaCl).

Process

The present invention provides a continuous process for the epoxidation of an olefinic compound with an oxidant, which process comprises reaction of an olefinic compound with an oxidant in the presence of a catalyst in an apparatus that comprises a reactive distillation column, which column comprises (i) a reactive section, which comprises the catalyst (ii) a rectifying section situated above the reactive section and adapted to allow separation of reagents and/or by-products from products (ix) a stripping section situated below the reactive section and adapted to allow separation of product from reagents and/or by-products (x) a vessel situated below the stripping section and adapted to provide a source of heat for the column and in which initial vaporisation of one or more of the reagents can occur, wherein the temperature in the reactive section (i) is a temperature at which the reaction between the olefinic compound and the oxidant takes place and the temperature in the stripping section (iii) is higher than the temperature in the rectifying section (ii).

process for the production of an olefin oxide

The invention provides a process for the epoxidation of an olefin, which process comprises reacting a feed comprising an olefin and oxygen in the presence of a catalyst comprising a carrier and silver deposited on the carrier, which carrier comprises at least 85 weight percent α-alumina and has a surface area of at least 1.3 m 2 /g, a median pore diameter of more than 0.8 μm, and a pore size distribution wherein at least 80% of the total pore volume is contained in pores with diameters in the range of from 0.1 to 10 μm and at least 80% of the pore volume contained in the pores with diameters in the range of from 0.1 to 10 μm is contained in pores with diameters in the range of from 0.3 to 10 μm.

Chromene compound

A chromene compound represented by the following formula (1): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.

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.

Process for the working-up of a vitamin e- and vitamin e-acetate-containing mixture or product stream

A rectification column and system for the working-up of a vitamin E (VE)- and/or vitamin E acetate (VEA)-containing product stream includes purification of a vitamin E-containing product stream, acetylation of at least a part of the purified vitamin E and purification of at least a part of the acetylated vitamin E, the purification of vitamin E and vitamin E acetate preferably being effected by distillation, for example rectification.

Methods for producing bis(sulfonyl)imide ammonium salt, bis(sulfonyl)imide and bis(sulfonyl)imide lithium salt

To provide methods for producing a bis(sulfonyl)imide ammonium salt, a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt simply and in good yield. A method for producing a bis(sulfonyl)imide ammonium salt, which comprises reacting a compound of the formula R—CHF—SO 2 X (wherein R is a C 1-4 fluorinated alkyl group which may contain an etheric oxygen atom, or a fluorine atom, and X is a fluorine atom or a chlorine atom) with ammonia in the absence of a catalyst. Further, methods for producing a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt by using the bis(sulfonyl)imide ammonium salt.

Chroman derivatives, medicaments and use in therapy

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

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.

Zinc cluster

Disclosed is a novel zinc cluster compound represented by general formula (1): Zn 4 O (OCOR) 6 (RCOOH) n , wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.

Phosphatidyl oligoglycerols

In order to form liposomes with a longer half-life in blood, use is made of defined compounds with the general formula (A)

Polymerizable composition, color filter, and method of producing the same, solid-state imaging device, and planographic printing plate precursor, and novel compound

Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R 3 and R 4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R 3 and R 4 may form a ring with each other; and X represents OR 5 , SR 6 , or NR 17 R 18 . The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.

Process for preparing episulfide resins

A process for converting epoxy resin to episulfide resin through reactive melt extrusion of a solid epoxy resin with a sulfur donating compound. The resulting resin provides for an application that utilizes the resulting extruded episulfide resin as a low application temperature resin for powder coatings applications.

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.

Anti-influenza agents

The present invention relates to compounds that selectively inhibit influenza A virus group (1) sialidases and are therefore potential anti-influenza agents.

Diuretics

A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

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.

Method for the enhanced recovery of catmint oil

A high yielding method is described for recovery of catmint oil from catmint plants of the genus Nepeta by improved separation of a catmint oil containing phase from the condensed steam distillate of catmint plants. Catmint oil may be obtained in quantitative yields for use in insect repellent compositions.

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.

Bicarbonate precursors, method for preparing same and uses thereof

The present invention concerns a compound of following formula (I): where: R 1 is H or an alkyl group, A 1 is a divalent straight-chain or branched alkylene radical, and A 2 is a —O-A 4 -O— radical, A 4 is a divalent straight-chain or branched alkylene radical.

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.

Processes for making high purity renewable source-based plasticizers and products made therefrom

Presently disclosed are high purity unsaturated fatty acid esters with an ester moiety characterized by having from five to seven members in a ring structure, which esters when epoxidized find particular utility as primary plasticizers in flexible polyvinyl halide applications. Also disclosed are processes for making the high purity esters.

Dendrimer conjugates

The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

Inhibition and treatment of prostate cancer metastasis

The present invention provides compounds and methods of inhibiting and treating metastatic prostate cancer. The compounds include MEK4 inhibitors. In another aspect the invention provides methods of identifying inhibitors of metastatic prostate cancer by screening for inhibitors of MEK4.

Use of rylene derivatives as photosensitizers in solar cells

Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR 1 R 2   (y1) -L-Z—R 3   (y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR 1 R 2 ; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO 3 M; —PO 3 M 2 ; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR 5 ] 4 + ; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R 1 , R 2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R 3 is optionally substituted alkyl, (het)aryl; R′ is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R 5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4, 6 where: n+p=0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

Process of making alpha-aminooxyketone/alpha-aminooxyaldehyde and alpha-hydroxyketone/alpha-hydroxyaldehyde compounds and a process making reaction products from cyclic alpha, beta-unsaturated ketone substrates and nitroso substrates

The present invention is directed to a process of making α-aminooxyketone and α-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein X a -X c represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the α-aminooxyketone compound formed to the α-hydroxyketone compound. The present invention results in α-aminooxyketone and α-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic α,β-unsaturated ketone substrate and a nitroso substrate. This methodology generally involves reacting the cyclic α,β-unsaturated ketone substrate and the nitroso substrate in the presence of a proline-based catalyst, to provide a heterocyclic product.

Process for the preparation of an alkylene carbonate and an alkylene glycol

The invention provides a reaction system for the production of an alkylene carbonate comprising: an epoxidation zone containing an epoxidation catalyst located within an epoxidation reactor; a carboxylation zone containing an bromide-containing carboxylation catalyst located within an alkylene oxide absorber; and one or more purification zones containing a purification absorbent capable of reducing the quantity of bromide-containing impurities in a feed comprising a recycle gas, which purification zones are located upstream from the epoxidation zone; and a process for the production of an alkylene carbonate and an alkylene glycol.

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.

Rodenticidal compounds, composition including same and use thereof for controlling harmful rodents

A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X═H, OH, Cl, Br, F or N0 2 ; R2 is: (IV) or (V) or (VI) with X═H, OH, Cl, Br, F or NO 2 ; R3 is: O or S or (VII) with X═H, OH, Cl, Br, F or N0 2 . Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.

Synthesis of epothilones, intermediates thereto and analogues thereof

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

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 and intermediate compounds useful in the preparation of statins

There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein R a represents an alkyl group, such as a C 1-16 alkyl group, and preferably an isopropyl group; R b represents an aryl group, preferably a 4-fluorophenyl group; R c represents hydrogen, a protecting group or an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO 2 R e group where R e is an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group.

Novel Insect-Repellent Coumarin Derivatives, Syntheses, and Methods of Use

This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.

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.

Supercooling promoting agent

The present invention discloses a supercooling promoting agent comprising a tannin for producing practical water which does not freeze. As the tannin, a hydrolyzable tannin such as 2,3,6-tri-O-galloyl-α,β-D-hamamelose, 1,2,6-tri-O-galloyl-β-D-glucose, and a vitrification liquid, each of which contains the supercooling promoting agent are useful as a solution or the like for storing a biological material at low temperature.

Macrocyclic lactones

The present invention relates to novel macrocyclic lactones, to processes for their preparation and to their use as fragrances and also to products comprising the novel macrocyclic lactones.

Antiprotozoal compound derived from coelenterata

The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R 1 represents R 10 — of formula (4) or R 20 — of formula (5); R 2 represents CHO—, etc.; R 3 represents a hydrogen atom, CH 3 —C(═O)—, etc.; R 4 represents a hydrogen atom, CH 3 —C(═O)—, etc.; each of R 11 and R 12 independently represents each a hydrogen atom, a methyl group, etc.; R 13 represents —CH 2 —, —CH(—OH)— or —C(═O)—; each of R 21 and R 22 independently represents eaeh a hydrogen atom, a methyl group, etc.; R 23 represents —CH 2 —, —CH(—OH)— or —C(═0)—; and R 24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.

Preparation of 2,2-bis (fluoroalkyl) oxirane and preparation of photoacid generator therefrom

A 2,2-bis(fluoroalkyl)oxirane (A) is prepared by reacting a fluorinated alcohol (1) with a chlorinating, brominating or sulfonylating agent under basic conditions to form an oxirane precursor (2) and subjecting the oxirane precursor to ring closure under basic conditions. R 1 and R 2 are fluoroalkyl groups, R 3 and R 4 are hydrogen or monovalent hydrocarbon groups, X is chlorine, bromine or —OSO 2 R 5 group, and R 5 is alkyl or aryl.

Monomers, polymers, photoresist compositions and methods of forming photolithographic patterns

Provided are (meth)acrylate monomers containing acetal moieties, polymers containing a unit formed from such a monomer and photoresist compositions containing such a polymer. The monomers, polymers and photoresist compositions are useful in forming photolithographic patterns. Also provided are substrates coated with the photoresist compositions, methods of forming photolithographic patterns and electronic devices. The compositions, methods and coated substrates find particular applicability in the manufacture of semiconductor devices.

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.

Synthesis of cleistanthin a and derivatives thereof

The present invention provides a method for preparing Cleistanthin A, a diphyllin glycoside, derivatives thereof and intermediates thereto. In particular the present invention provides in one of the aspect a method for synthesis of compound of formula D a key intermediate of diphyllin, which can be carried out in a shorter duration and at an ordinary temperature.

Synthesis and applications of soluble pentacene precursors and related compounds

The present disclosure relates to methods and systems for synthesis of bridged-hydropentacene, hydroanthracene and hydrotetracene from the precursor compounds pentacene derivatives, tetracene derivatives, and anthracene derivatives. The invention further relates to methods and systems for forming thin films for use in electrically conductive assemblies, such as semiconductors or photovoltaic devices.

Lactide Production from Thermal Depolymerization of PLA with applications to Production of PLA or other bioproducts

Methods and systems are disclosed for producing lactide, which can be used for PLA production or other valuable bioproducts. PLA is heated to undergo thermal depolymerization to recover lactide. The lactide can be used for PLA production or other valuable bioproducts.

Novel naphthothiophene compound and organic light-emitting device including the same

The present invention provides a novel naphthothiophene compound having a high lowest excited triplet level (T1).

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.

Aromatic monomers deriving from glycerol units, process for their preparation and use thereof for the preparation of water-soluble conjugated polymers

Monomers having formula (I) and process for their synthesis which comprises the etherification reaction of a halogen-derivative (Z═Cl, Br, I) having formula (III) with the hydroxyl group of the glycerol derivative (IV), according to the following scheme:(Formula III, IV & I) (III) (IV) (I)

Method for preparing a poly(ether sulfonimide or -amide) copolymer using cyclic oligomers

Disclosed is a method for preparing a poly(ethersulfonimide or ethersulfonamide) copolymer using cyclic oligomers, and more particularly, to a method for preparing a poly(ethersulfonimide or ethersulfonamide) copolymer by preparing a cyclic ether sulfone oligomer and a cyclic imide or amide oligomer and subjecting the cyclic ether sulfone oligomer and the cyclic imide or amide oligomer to ring-opening copolymerization in the presence of an alkali metal fluoride catalyst.

Compounds Having Semiconducting Properties and Related Compositions and Devices

Disclosed are new compounds having semiconducting properties. Such compounds can be processed in solution-phase at a temperature of less than about 50° C. into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics.

Fluorescent substrate for detection of enzymatic activity of nitrile-related enzyme

The object of the present invention is to provide a fluorescent substrate for detecting the enzymatic activity of a nitrile-related enzyme. The present invention provides a compound represented by formula (I) and a fluorescent substrate for detecting the enzymatic activity of a nitrile-related enzyme, which comprises the compound.

Method for manufacturing fluorine-containing imide compound

With this method for manufacturing fluorine-containing imide compounds, a method for manufacturing a fluorine-containing imide compound ((Rf 1 SO 2 )(Rf 2 SO 2 )NH) is selected which includes reaction of a fluorine-containing sulfonic acid (Rf 1 SO 3 H) and a fluorine-containing sulfonamide (Rf 2 SO 2 NH) in the presence of thionyl chloride. Wherein, Rf 1 and Rf 2 are fluorine, or straight-chain or branched perfluoroalkyl groups with a carbon number of 1-4.

COMPOUND COMPRISING A FIVE-MEMBERED HETERO RING, AN ORGANIC ELECTRICAL ELEMENT USING THE SAME AND A TERMINAL THEREOF

Disclosed are a compound comprising a five-membered hetero ring, an organic electrical element using the same and a terminal thereof. 2. The compound as claimed in claim 1 , wherein Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand Reach form a substituted or unsubstituted claim 1 , saturated or unsaturated ring together with an adjacent group.5. An organic electrical element comprising one or more organic material layers comprising the compound as claimed in .6. The organic electrical element as claimed in claim 5 , wherein the organic material layers are formed to comprise the compound by a soluble process.7. The organic electrical element as claimed in claim 5 , wherein the organic electrical element comprises an organic light emitting diode (OLED) having a structure in which a first electrode claim 5 , the one or more organic material layers claim 5 , and a second electrode are sequentially laminated.8. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise any one of a hole injection layer claim 7 , a hole transport layer claim 7 , a light emitting layer claim 7 , an electron transport layer claim 7 , and an electron injection layer.9. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise a hole injection layer claim 7 , and the compound is used as a hole transport material in the hole transport layer.10. A terminal comprising a display device claim 7 , which comprises the organic electrical element as claimed in claim 7 , and a control unit for driving the display device.11. The terminal as claimed in claim 10 , wherein the organic electrical element comprises any one of an organic light emitting diode (OLED) claim 10 , an organic solar cell claim 10 , an organic photo conductor (OPC) drum claim 10 , and an organic transistor (organic TFT). The present invention relates to a compound including a five-membered hetero ring, an organic electrical element using the ...

Propynoic Acid Carbamoyl Methyl-Amides and Pharmaceutical Compositions and Methods Based Thereon

This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2. 4. A compound according to claim 1 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.5. A compound according to claim 3 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.7. A pharmaceutical composition comprising any of the compounds of to and a pharmaceutically acceptable carrier.8. A method for treatment a cancer subject claim 3 , comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering to a person in need of said treatment method an effective amount of the pharmaceutical composition according to .'}9. A method of claim 8 , where the cancer is: breast cancer claim 8 , ovarian cancer claim 8 , prostate cancer claim 8 , colon cancer claim 8 , brain cancer claim 8 , pancreatic cancer claim 8 , skin cancer claim 8 , lung cancer claim 8 , and multiple myeloma.10. A method for promoting the release and nuclear localization of the transcription factor Nrf2 comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering an effective amount of the pharmaceutical compositions according to .'}10. A biological or medical diagnostic imaging technique claim 8 , comprising:{'claim-ref': [{'@idref': 'CLM-00004', 'claims 4 ...

TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY

The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. 167-. (canceled)73. The compound of wherein R claim 72 , Rand Rare each independently —OH claim 72 , —SH claim 72 , —NHR claim 72 , —OC(O)NRR claim 72 , —SC(O)NRR claim 72 , —OC(O)R claim 72 , —SC(O)R claim 72 , —OC(O)OR claim 72 , —SC(O)OR claim 72 , —OS(O)R claim 72 , —S(O)OR claim 72 , —SS(O)R claim 72 , —OS(O)OR claim 72 , —SS(O)OR claim 72 , —OC(S)R claim 72 , —SC(S)R claim 72 , —OC(S)OR claim 72 , —SC(S)OR claim 72 , —OC(S)NRR claim 72 , —SC(S)NRR claim 72 , —OC(NR)R claim 72 , —SC(NR)R claim 72 , —OC(NR)OR claim 72 , —SC(NR)OR claim 72 , —OP(O)(OR)or —SP(O)(OR).74. A pharmaceutical composition claim 68 , comprising a pharmaceutically acceptable carrier and a compound of .75. The pharmaceutical composition of claim 74 , further comprising one or more additional therapeutic agents.76. A method of treating cancer in a mammal claim 68 , comprising administering to the mammal an effective amount of a compound of any one of .77. A method of treating cancer in a mammal claim 69 , comprising administering to the mammal an effective amount of a compound of any one of .78. A method of treating cancer in a mammal claim 70 , comprising administering to the mammal an effective amount of a compound of any one of .79. A method of treating cancer in a mammal claim 71 , comprising administering to the mammal an effective amount of a compound of any one of .80. A method of treating cancer in a mammal claim 72 , comprising administering to the mammal an effective amount of a compound of any one of .81. A ...

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 ...

SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1a', '1b', '7, 'Rand Rtaken together with the carbon atom to which they are attached form a partially or fully saturated 4-, 5- or 6-membered ring of carbon atoms optionally including 1-2 heteroatoms selected from O, N, or S, the ring optionally substituted independently with 1-3 substituents of R; and'}{'sup': '1c', 'Ris H.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris a ring selected from phenyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , triazinyl claim 1 , thiophenyl claim 1 , furyl claim 1 , pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , tetrazolyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , isothiazolyl claim 1 , thiadiazolyl claim 1 , oxadiazolyl claim 1 , pyrrolidinyl claim 1 , oxazolinyl claim 1 , isoxazolinyl claim 1 , thiazolinyl claim 1 , pyrazolinyl claim 1 , morpholinyl claim 1 , piperidinyl claim 1 , piperazinyl and pyranyl claim 1 , said ring optionally substituted with 1-5 substituents of R.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '1', 'Ais CH;'}{'sup': 2', '6, 'Ais CR;'}{'sup': 3', '4', '6', '3', '4, 'each of Aand A, independently, is CH or CRor N, provided no more than one of Aand Ais N;'}{'sup': 1a', '7, 'sub': 1-6', '2-6', '2-6', '1-6', '1-3', '1-6', '1-3', '1-6', '2', '1-3', '1-6', '1-3', '1-3', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3, 'Ris C-alkyl, Calkenyl, C-alkynyl, Calkyl-O—C-alkyl-, C-alkyl-S—C-alkyl-, C-alkyl ...

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 ...

THIENOPYRIDINE ESTER DERIVATIVE CONTAINING CYANO GROUP, PREPARATION METHOD, USE AND COMPOSITION THEREOF

A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation. 2. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from one of the following compounds:I-1: 5-(2-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-2: 5-(3-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-3: 5-(4-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate.3. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the pharmaceutically acceptable salt comprises the salt formed by the compound of formula I with an inorganic acid or an organic acid.4. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 3 , wherein the pharmaceutically acceptable salt is selected from hydrochlorides claim 3 , hydrobromides claim 3 , hydriodates claim 3 , sulfates claim 3 , hydrosulfates claim 3 , phosphates claim 3 , hydrophosphates claim 3 , acetates claim 3 , propionates claim 3 , butyrates claim 3 , lactates claim 3 , mesylates claim 3 , tosilates claim 3 , maleates claim 3 , benzoates claim 3 , succinates claim 3 , tartrates claim 3 , citrates claim 3 , fumarates claim 3 , taurates claim 3 , gluconates claim 3 , and amino acid salts of the compound of formula I.5. A method for preparing the compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , ...

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 ...

Process for stereoselective synthesis of 5-fluoro-1-(2r,5s)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine

The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.

18ß-GLYCYRRHETINIC ACID DERIVATIVES AND SYNTHETIC METHOD THEREOF

The present invention provides a chemical compound having the structure being one selected from a group consisting of 2. The method according to further comprising a step of using an isopropylamine solution as the amine solution when Ris CONHCH(CH) claim 1 , and using an aniline solution as the amine solution when Ris CONHCH.3. The method according to further comprising steps of:methylating the 18β-glycyrrhetinic acid to obtain a methylated 18β-glycyrrhetinic acid; andoxidizing the methylated 18β-glycyrrhetinic acid to obtain a second compound.4. The method according to further comprising a step of esterifying the lactone compound to obtain a first derivative of the lactone compound.5. The method according to further comprising a step of cleaving a lactone ring of the lactone compound to obtain a second derivative of the lactone compound.6. The method according to further comprising a step of treating the second derivative with an alcohol solution to obtain a third derivative of the lactone compound.7. The method according to claim 6 , wherein the alcohol solution is one of an isopropyl alcohol solution and a benzyl alcohol solution.8. The method according to further comprising a step of esterifying the second compound with an alcohol solution to obtain a fourth derivative of the lactone compound.9. The method according to further comprising a step of cleaving a lactone ring of the fourth derivative by an acidic solution to obtain a fifth derivative of the lactone compound.13. The method according to claim 12 , wherein the chemical compound with Rbeing one of CONHCH(CH)and CONHCHis obtained by steps of:oxidizing the 18β-glycyrrhetinic acid to form a first compound;treating the first compound with an m-chloroperbenzoic acid to afford a lactone compound; andtreating the lactone compound with an amine solution to obtain the chemical compound being a first derivative of the chemical compound.14. The method according to further comprising a step of using an ...

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 ...

Method for Producing (2R)-2-Fluoro-2-C-Methyl-D-Ribono-y-Lactone Precursor

In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SOF) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is useful as an important intermediate for the synthesis of 2′-deoxy-2′-fluoro-2′-C-methylcytidine with antivirus activity. The present invention relates to a method for producing a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor.There have been reported some methods for production of (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursors. In any of these production methods, the stereoselective introduction of a fluorine atom to 2-position is a significant problem. Ring-opening fluorination of a cyclic sulfuric ester is known as a fluorine atom introduction technique suitable for mass-scale production (see Patent Documents 1 and 2 and Non-Patent Document 1). Using this technique, it is feasible to produce a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor in the form of a ring-opened fluorinated compound in three steps (first step: cyclic sulfurous esterification, second step: oxidation, third step: ring-opening fluorination) from a 1,2-diol substrate (see Scheme 1 where Me is a methyl group; Et is an ethyl group; X is a proton, a protonated organic base, a metal cation, a tetraalkylammonium or a tris(dialkylamino)sulfonium; and Bz is a benzoyl group). There is also reported a modified production method for producing a ring-opened fluorinated compound in two steps (first step: ...

PROCESS AND APPARATUS FOR THE PRODUCTION OF ETHYLENE OXIDE

The invention provides a process and an apparatus for the production of ethylene oxide from ethylene. Ethylene and oxygen are supplied to reactor tubes, wherein the reactor tubes are held by upper and lower tube sheets in a reactor vessel. The reactor vessel has a separation grid, dividing the reactor vessel into an upstream zone and a downstream zone. Coolant is supplied to the upstream zone from an upper coolant circuit and is removed from the upstream zone to the upper coolant circuit. A portion of coolant is removed as vapour from the upper coolant circuit. Coolant is supplied to the downstream zone from a lower coolant circuit and is removed from the downstream zone to the lower coolant circuit. Additional coolant is added to the lower coolant circuit. There is net flow of coolant through the separation grid from the downstream zone to the upstream zone. 1. A process for the production of ethylene oxide from ethylene comprising:a) supplying ethylene and oxygen to a reactor vessel comprising reactor tubes and a separation grid, wherein the reactor tubes are held by upper and lower tube sheets, and wherein the separation grid divides the reactor vessel into an upstream zone and a downstream zone;b) supplying coolant to the upstream zone from an upper coolant circuit, removing coolant from the upstream zone to the upper coolant circuit, and removing a portion of coolant as vapour from the upper coolant circuit; andc) supplying coolant to the downstream zone from a lower coolant circuit, removing coolant from the downstream zone to the lower coolant circuit and adding additional coolant to the lower coolant circuit;wherein there is net flow of coolant through the separation grid from the downstream zone to the upstream zone.2. A process according to wherein the separation grid has an open area that represents from 0.5 to 8% of the cross section of the reactor vessel.3. A process according to wherein the upstream zone represents from 50 to 95% of the reactor vessel ...

COMPOSITIONS AND METHODS USING SAME FOR TREATING AMYLOID-ASSOCIATED DISEASES

Compounds having one or more phenol moieties, derivatives thereof, compositions containing same and uses thereof for the treatment of amyloid-associated diseases are provided. 2. The article-of-manufacture of claim 1 , wherein said compound is selected from the group consisting of phenol red claim 1 , dimethoxy phenol red claim 1 , methoxy phenol red claim 1 , diacetoxy phenol red claim 1 , acetoxy phenol red claim 1 , pyrocatechol violet claim 1 , phenolphthalein claim 1 , hydroxyphenyl claim 1 , tocopherol claim 1 , and bromophenol red.3. The article-of-manufacture of claim 1 , wherein said compound is selected from the group consisting of phenol red and diacetoxy phenol red.4. The article-of-manufacture of claim 3 , wherein said pharmaceutical acceptable carrier comprises a mixture of polyethylene glycol claim 3 , saturated sodium chloride and N claim 3 ,N-Dimethylacetamide.5. The article-of-manufacture of claim 4 , wherein said pharmaceutical composition is formulated for oral administration of said compound.6. The pharmaceutical composition of claim 4 , wherein said pharmaceutical composition is formulated for intravenous administration of said compound.8. The method of claim 7 , wherein said administering is effected orally.9. The method of claim 7 , wherein said compound is selected from the group consisting of phenol red claim 7 , dimethoxy phenol red claim 7 , methoxy phenol red claim 7 , diacetoxy phenol red claim 7 , acetoxy phenol red claim 7 , pyrocatechol violet claim 7 , phenolphthalein claim 7 , hydroxyphenyl claim 7 , tocopherol claim 7 , and bromophenol red.10. The method of claim 7 , wherein said compound is selected from the group consisting of phenol red and diacetoxy phenol red.11. The method of claim 10 , wherein said administering is effected orally.13. The pharmaceutical composition of claim 12 , wherein said compound is selected from the group consisting of phenol red claim 12 , dimethoxy phenol red claim 12 , methoxy phenol red claim 12 , ...

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 , ...

Fused Thiazole Derivatives as Kinase Inhibitors

A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. 2. The compound as claimed in wherein Rrepresents Calkyl.3. The compound as claimed in wherein Rrepresents Calkyl.4. The compound as claimed in wherein T represents N—R.5. The compound as claimed in wherein V is carbon.6. The compound as claimed in wherein W is carbon.7. A compound as claimed in wherein Rrepresents hydrogen claim 1 , cyano claim 1 , carboxy claim 1 , Calkoxycarbonyl claim 1 , di(C)alkylaminocarbonyl claim 1 , [(C)alkyl][cyano(C)alkyl]aminocarbonyl claim 1 , [(C)alkoxy(C)alkyl][(C)alkyl]-aminocarbonyl or azetidinylcarbonyl.8. The compound as claimed in wherein Rrepresents hydrogen.9. The compound as claimed in wherein Rrepresents methyl.10. (canceled)11. The pharmaceutical composition comprising a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , in association with a pharmaceutically acceptable carrier.12. (canceled)13. (canceled)14. (canceled)15. A method for the treatment and/or prevention of a disorder for which the administration of a selective PI3K inhibitor is indicated which comprises administering to a patient in need of such treatment an effective amount of a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof. The present invention relates to a class of fused thiazole derivatives, and to their use in therapy. More particularly, the invention provides a family of 6,7-dihydro-[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety. These compounds are selective ...

THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS

The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer. 2. The compound according to wherein X and Y are independently NHCO or CONH.3. The compound according to wherein X is NHCO.4. The compound according to wherein Y is CONH.5. The compound according to wherein the ar ring is (2-5C)heteroaryl substituted with one or more groups selected from (1-6C)alkyl claim 1 , phenyl claim 1 , (di)[(1-4C)alkyl]amino or pyrrolidinyl.7. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 6 , optionally substituted with one or more CN claim 6 , aminocarbonyl claim 6 , halogen; (1-4C)alkoxy; (di)[(1-4C)alkyl]amino; or (2-5C)heteroaryl.8. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 7 , optionally substituted with one or more CN or halogen.9. The compound according to wherein R7 claim 6 , R9 claim 6 , R10 and R11 are H.10. The compound according to wherein R1 is H; halogen; hydroxy; CN; amino; (1-2C)alkyl; (1-2C)alkylcarbonyl; (1-2C)alkoxy or (di)[(1-2C)alkyl]amino claim 1 , the alkyl group of which is optionally substituted with hydroxy; andR2 is H; halogen; hydroxy; CN; amino; (1-6C)alkyl; (di)[(1-6C)alkyl]amino, the alkyl group of which is optionally substituted with one or more hydroxy, (di)[(1-4C)alkylamino, (1-6C)alkoxy, (2-5C)heterocycloalkyl, (2-5C)heteroaryl or aryl; (1-4C)alkylcarbonyl; (1-4C)alkoxy, optionally substituted with (di)[(1-4C)alkyl]amino; (2-5C)heterocycloalkyl, optionally substituted with one or more groups selected from hydroxy, amino, (1-6C)alkyloxycarbonylamino) or (1-4C)alkyl, the alkyl optionally substituted with hydroxy; (2-5C)heteroaryl, optionally substituted with halogen, CN, (1-4C)alkoxy, (di)[(1-4C)alkyl]amino or (1-4C)alkyl; phenyl optionally substituted with halogen, CN, (1-4C)alkyl, (1-4C)alkoxy or (di)[(1-4C)alkyl]amino; 2-5C)heteroarylamino; phenylamino; or (2-5C) ...

NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA

The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, 2. The compound of formula I according to claim 1 , wherein R is in the para-position of Ring A claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.3. The compound of formula I according to claim 1 , wherein Ring A is selected from the group consisting of phenyl claim 1 , pyridinyl and pyrimidinyl claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.4. The compound of formula I according to claim 2 , wherein Ring A is selected from the group consisting of phenyl claim 2 , pyridinyl and pyrimidinyl claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , or an enantiomer or racemate thereof.7. The compound according to claim 1 , wherein S* is in the R-configuration.8. The compound according to claim 1 , wherein S* is in the S-configuration.9. A crystalline anhydrous compound of formula III according to claim 6 , which shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.62 Å.10. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , and 10.09 Å.11. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , and 3.66 Å.12. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , 10.09 Å claim 6 , 3.93 Å claim 6 , and 4.94 Å.13. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , 3.66 Å claim 6 , 3.73 Å claim 6 , and 18.47 Å.14. A ...

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 ...

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 ...