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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3358. Отображено 100.
27-12-2012 дата публикации

Conjugated aromatic compound, optical material, and optical element

Номер: US20120330052A1
Автор: Terunobu Saitoh
Принадлежит: Canon Inc

The present invention relates to a conjugated aromatic compound represented by the Formula (1) in claim 1 (in the formula, Ar 1 represents a hydrogen atom or an aryl group optionally having a substituent; Ar 2 and Ar 3 each represent a hydrogen atom or an aryl group optionally having a substituent but at least one of Ar 2 and Ar 3 represents an aryl group optionally having a substituent; and A represents an aromatic hydrocarbon group) and relates to an optical material containing the conjugated aromatic compound. The conjugated aromatic compound and the optical material have characteristics of a high chromatic aberration correction function, high refractive-index dispersion characteristics (Abbe number (vd)) and high secondary dispersion characteristics (θg,F) (anomalous dispersion characteristics).

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Номер записи: 1
30-05-2013 дата публикации

Photo-Responsive Microencapsulation Materials, Compositions and Methods of Use Thereof

Номер: US20130137625A1
Автор: STOWELL Michael H.B.
Принадлежит: SOLARBRE, INC.

Photoactivatable prepolymers and methods of use thereof are disclosed for microencapsulation of a substantially water-insoluble material within a nonporous shell. As provided herein, the microencapsulated material is released with no more than a slow release rate. Upon exposure of the nonporous shell to light, the nonporous shell is converted into a porous shell having an increased release rate for the microencapsulated material. 118.-. (canceled)19. A method for producing microcapsules comprising a substantially water-insoluble liquid material within a non-porous , light-sensitive shell , wherein the non-porous shell is characterized by a release rate of the liquid material in the absence of light of less than lppm/minute , wherein exposure to light converts the nonporous shell into a porous shell characterized by a release rate of the liquid material of from 1 to at least 100 ppm/minute , the method comprising the steps of:(a) providing an organic solution comprising said liquid material and an etherified photoactivatable-based prepolymer or mixture of photoactivatable and nonphotoactive-based prepolymers dissolved therein;(b) creating an emulsion of said organic solution in a continuous phase aqueous solution comprising water and a surface-active agent, wherein said emulsion comprises discrete droplets of said organic solution dispersed in said continuous phase aqueous solution, there being formed thereby an interface between the discrete droplets of organic solution and the surrounding continuous phase aqueous solution; and(c) causing in situ self-condensation and curing of said prepolymers in the organic phase of said discrete droplets adjacent to said interface by catalysis using heat, pH, or a chemical or free radical initiator for a time sufficient to allow substantial completion of in situ condensation of said prepolymers, thereby converting the liquid droplets of said organic solution to microcapsules comprising a solid nonpermeable polymer shell that ...

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Номер записи: 2
30-05-2013 дата публикации

NEW COMPOUNDS FOR THE PREVENTION AND/OR TREATMENT OF OSTEOARTHROSIS

Номер: US20130137761A1
Автор: Prehm Peter, Stracke Dennis
Принадлежит: UNIVERSITAETSKLINIKUM MUEUENSTER

The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged. 4. The compound method according to claim 1 , wherein the compound is comprised in foodstuff.5. The method of claim 4 , wherein said foodstuff is a beverage.6. The method according to claim 1 , wherein said disease is osteoarthritis.8. The method according to wherein the disease is osteoarthritis.10. The method according to wherein the disease is osteoarthritis. The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged.Hyaluronan is the major water binding component of the extracellular matrix. It is a very large glycosaminoglycan that is exported into the extracellular matrix by fibroblasts or epithelial ...

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Номер записи: 3
11-07-2013 дата публикации

MONOTERPENE DERIVATIVES OF CHALCONE OR DIHYDROCHALCONE AND THEIR USE AS DEPIGMENTING AGENTS

Номер: US20130177515A1
Автор: Belaubre Françoise, Mandeau Anne, Poigny Stéphane
Принадлежит: PIERRE FABRE DERMO-COSMETIQUE

The present invention relates to new monoterpene derivatives of chalcone or dihydrochalcone and their use as a depigmenting agent. 2. The extract according to comprising one or more molecules of the formula I in an amount of between 0.1 and 30 g per 100 g of dried material.3. A process for preparing an extract according to any of to comprising the following series of steps:{'i': Helichrysum gymnocephalum', 'Stenocline gymnocephala, 'harvesting, drying and grinding aerial parts of (DC) Humbert (Asteraceae, syn. ),'}extracting the ground material obtained from the previous step with an organic solvent at a plant/solvent ratio of between about 1/1 and about 1/20subjecting to a solid/liquid separation for example by filtration or centrifugation.6Helichrysum, Piper, LinderaMitrellaHelichrysum gymnocephalumPiper hostmannianum, P. aduncum, P. hispidum, Lindera aggregata, L. glauca, L. umbellatta, Mitrella mesnyi, M. kentii.. The use according to characterized in that the extract of plant origin enriched with one or more molecules of the formula (I) is an extract of plants belonging to the genus or claim 4 , including: (DC) Humbert claim 4 ,7. The use according to any of to characterized in that{'img': {'@id': 'CUSTOM-CHARACTER-00023', '@he': '3.13mm', '@wi': '0.68mm', '@file': 'US20130177515A1-20130711-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'is a double bond'}R1=H; andR2=OH.8. The use according to any of to characterized in that{'img': {'@id': 'CUSTOM-CHARACTER-00024', '@he': '3.13mm', '@wi': '0.68mm', '@file': 'US20130177515A1-20130711-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'is a single bond'}R1=H; andR2=H.9. The use according to claim 4 , for bleaching and/or lightening the skin and/or bristles and/or hair.10. The use according to claim 4 , for reducing and/or removing age spots on the skin.11. The use according to claim 4 , for reducing and/or removing brownish ...

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Номер записи: 4
15-08-2013 дата публикации

COUMARIN-CHALCONES AS ANTICANCER AGENTS

Номер: US20130210909A1
Автор: Kumar Abdhesh, Kumar Manoj, Sarkar Jayanta, Sashidhara Koneni Venkata, Sinha Sudhir Kumar
Принадлежит: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

The present invention relates to certain coumarin/chalcone compounds or a pharmaceutically acceptable salt thereof. The present invention particularly relates to the coumarin/chalcone compounds as anticancer agents useful for the treatment of cancer. The present invention also relates to the process of preparation of the said compounds. 2. The compound as claimed in wherein pharmaceutically acceptable salt is selected from a group consisting of solvates claim 1 , amides claim 1 , esters claim 1 , ethers claim 1 , chemically protected forms claim 1 , and prodrugs of compound of formula VI.3. The compound of formula (VI) as claimed in claim 1 , useful as an anticancer agent for the treatment or prevention of cervical carcinoma claim 1 , oral squamous cell carcinoma or lung or prostate carcinoma or brain tumor.4. The compound as claimed in wherein the compound has a ICvalue ranging between 1.53 to 146.82 μM.5. The compound as claimed in wherein the representative compounds comprising:I. Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxylate (S-009-0131)II. Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-phenylprop-1-enyl)-2H-chromene-3-carboxylate (S-009-0132)III. Methyl 8-sec-butyl-2-oxo-6-(3-oxo-3-phenylprop-1-enyl)-2H-chromene-3-carboxylate (S009-0133)IV. Ethyl 8-sec-butyl-6-(3-(4-chlorophenyl)-3-oxoprop-1-enyl)-2-oxo-2H-chromene-3-carboxylate (S-009-0135)V. Methyl 8-sec-butyl-6-(3-(4-chlorophenyl)-3-oxoprop-1-enyl)-2-oxo-2H-chromene-3-carboxylate (S-009-0136)VI. (E)-8-tert-Butyl-N,N-diethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1992)VII. (E)-8-sec-Butyl-N-methyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1994)VIII. (E)-8-sec-Butyl-N-ethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1995)IX. (E)-8-sec-Butyl-N,N-diethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1996)X. (E)-Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-(3,4,5-trimethoxyphenyl)prop-1-enyl)-2H- ...

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Номер записи: 5
05-09-2013 дата публикации

AROMATIC PERFLUOROALKANE MONOMER

Номер: US20130231405A1
Автор: Fedurco Milan
Принадлежит:

An aromatic perfluoroalkane monomer is provided that can be used for the manufacture of a polymer membrane for a PEM-type fuel cell. The perfluoroalkane monomer has a structure corresponding to a formula (I): 110-. (canceled)12. The monomer according to claim 11 , wherein n is in a range from 2 to 20.13. The monomer according to claim 11 , wherein n is in a range from 2 to 8.14. The monomer according to claim 11 , wherein Zand Z claim 11 , which are identical or different claim 11 , are chosen from a group that includes: halogens claim 11 , hydroxyl claim 11 , alkoxyls claim 11 , thiol claim 11 , carboxyl claim 11 , carboxylates claim 11 , amino claim 11 , sulphonamido claim 11 , acyl chloride claim 11 , sulphonyl chloride claim 11 , sulphonyl fluoride claim 11 , isocyanate claim 11 , and combinations thereof.15. The monomer according to claim 14 , wherein the monomer corresponds to a formula (I-2):{'br': None, 'sub': 3', '1', '2', 'n', '2', '4, 'F—Ar—CO—Ar—(CF)—Ar—CO—Ar—F.\u2003\u2003(I-2)'}16. The monomer according to claim 14 , wherein the monomer corresponds to a formula (I-3):{'br': None, 'sub': 3', '1', '2', 'n', '2', '4, 'HO—Ar—CO—Ar—(CF)—Ar—CO—Ar—OH.\u2003\u2003(I-3)'}17. The monomer according to claim 11 , wherein n is equal to 4.18. The monomer according to claim 12 , wherein n is equal to 4.19. The monomer according to claim 13 , wherein n is equal to 4.20. The monomer according to claim 14 , wherein n is equal to 4.21. The monomer according to claim 15 , wherein n is equal to 4.22. The monomer according to claim 16 , wherein n is equal to 4.23. The monomer according to claim 11 , wherein the monomer is a sulphonic monomer carrying a sulphonic (—SOH) group or a sulphonate (—SOM) group claim 11 , in which M represents an alkali metal cation.24. The monomer according to claim 23 , wherein the sulphonic (—SOH) group or the sulphonate (—SOM) group is carried by a phenyl group or a phenylene group claim 23 , or by a substituent thereof. The present invention ...

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Номер записи: 6
19-09-2013 дата публикации

SUGAR METABOLISM IMPROVING COMPOSITION, AND PHARMACEUTICAL PREPARATION CONTAINING SAID COMPOSITION

Номер: US20130245325A1
Автор: Woo Je-Tae, YAGASAKI Kazumi, Yonezawa Takayuki
Принадлежит: ERINA CO., INC.

The purpose of the present invention is to provide a highly safe composition that improves glucose tolerance and sugar metabolism at skeletal muscles, and a prevention/treatment drug for diabetes/metabolic syndrome containing the composition. Provided is a composition that is for improving sugar metabolism and glucose tolerance and that contains a compound represented by formula (I) derived from a plant selected from the group consisting of , and as the active ingredient. 2. The AMPK activating agent according to the claim 1 , wherein in the chemical formula (I) claim 1 , Rand Rare a functional group selected from the group consisting of hydroxyl group claim 1 , methoxy group claim 1 , ethoxy group claim 1 , and acetyl group respectively claim 1 , Rand Rare a functional group a hydrogen atom claim 1 , methyl group claim 1 , and ethyl group respectively.414-. (canceled)15. A glucose uptake accelerating agent into a muscle comprising the AMPK activating agent claimed in any one of or as an active ingredient.16. A glucose tolerance improving agent comprising the AMPK activating agent claimed in any one of the or as an active ingredient.17. A blood lipid level reducing agent comprising the AMPK activating agent claimed in any one of the or as an active ingredient.18. A prevention and/or treatment agent for metabolic syndrome comprising the AMPK activating agent claimed in any one of the or as an active ingredient. A composition for ameliorating glucose metabolism and lipid metabolism, and a pharmaceutical preparation comprising thereof.The present invention relates to a composition for ameliorating glucose metabolism and lipid metabolism, and a pharmaceutical preparation comprising thereof for prophylaxis or treatment of metabolic syndrome.Recently, patient number of adult disease such as diabetes and so forth, which is caused by changing of diet or life style, is increasing, and some means are needed. Here, the adult disease is defined as a concept including many ...

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Номер записи: 7
21-11-2013 дата публикации

Phenolic compound having carbonyl as neighboring group and application thereof

Номер: US20130306909A1
Автор: Mayumi Goto, YASUYUKI Sasada
Принадлежит: JNC Corp, JNC Petrochemical Corp

To provide a liquid crystal compound having a large negative value of dielectric anisotropy (Δ∈). A compound is represented by formula (1): wherein, in formula (1), R 1 and R 2 are hydrogen, halogen or alkyl having 1 to 10 carbons, and in the alkyl, at least one of —CH 2 — may be replaced by —O—, at least one of —(CH 2 ) 2 — may be replaced by —CH═CH—, and at least one of hydrogen may be replaced by halogen; ring A 1 and ring A 2 are 1,4-cyclohexylene or 1,4-phenylene; Z 1 is a single bond, —(CH 2 ) 2 —, —CH 2 O—, —OCH 2 —, —CF 2 O—, —OCF 2 —, —COO—, or —OCO—; Y is halogen, —CF 3 , —CF 2 H or —CH 2 F; and m, n and p are 0, 1 or 2, and a sum (m+n) of m and n is 0, 1 or 2.

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Номер записи: 8
19-12-2013 дата публикации

Aspirin Derivatives and Uses Thereof

Номер: US20130338120A1
Автор: Sang Shengmin
Принадлежит:

The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer. 2. The compound of claim 1 , wherein Ris —OH.4. The compound of claim 3 , wherein each of Rand Ris —OH.5. The compound of claim 3 , wherein each of Rand Ris independently —O—Calkyl.6. The compound of claim 3 , wherein each of Rand Ris independently —O—Calkyl.7. The compound of claim 3 , wherein each of Rand Ris —O-Me.9. The compound of claim 8 , wherein each of Rand Ris —OH and Ris —O—C(O)Me.13. The method of claim 12 , wherein each of Rand Ris —OH.14. The method of claim 12 , wherein each of Rand Ris —O-Me.16. The method of claim 15 , wherein each of Rand Ris —OH and Ris —O—C(O)Me.20. The pharmaceutical composition of claim 19 , wherein each of Rand Ris —OH.21. The pharmaceutical composition of claim 19 , wherein each of Rand Ris —O-Me.23. The pharmaceutical composition of claim 21 , wherein each of Rand Ris —OH and Ris —O—C(O)Me. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application Ser. Nos. 61/791,826, filed Mar. 15, 2013, and 61/659,647, filed Jun. 14, 2012, the disclosure of each of which is incorporated herein by reference in its entirety.This invention was made with government support under 1-R03-CA159353-01A1, awarded by the National Institutes of Health. The government has certain rights in the invention.The present invention generally relates to novel aspirin derivatives and the prevention and/or treatment of disorders responsive to aspirin derivatives.Colorectal cancer (CRC) is a significant global health concern and is the third leading cause of death from cancer among both men and women worldwide.Observational studies and randomized trials have demonstrated an inverse association between the incidence of CRC and the use of aspirin ( ...

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Номер записи: 9
19-12-2013 дата публикации

Process for Preparing Benzofurans

Номер: US20130338398A1
Автор: Eklund Lars
Принадлежит:

There is provided a process for the preparation of a compound of formula (I), wherein R, R, R, R, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone. 132.-. (canceled)352. The compound of claim wherein Z represents phenyl substituted in the para-position by —OH , —OCHor —O-benzyl. This application is a Divisional of U.S. application Ser. No. 12/681,299, filed Jul. 28, 2010; which is a National Stage of International Application No. PCT/GB08/003,341, filed Oct. 2, 2008; which claims the benefit of priority from GB Application No. 0719180.2, filed Oct. 2, 2007, the entire contents of which are incorporated by reference in their entirety.The present invention relates to a process for the manufacture of various benzofurans by reaction of an arylhydroxylamine and a ketone, and the use of such benzofurans in the synthesis of compounds, e.g. drugs, containing such cores, for instance anti-arrhythmia drugs such as Dronedarone (N-{2-(n-butyl)-3-[4-(3-dibutylamino-propoxy)-benzoyl]-benzofuran-5-yl}methane-sulfonamide).Dronedarone is a Class III anti-arrhythmia drug for the prevention of cardiac arrhythmias such as atrial fibrillation (AF). AF is a condition characterised by an irregular heart beat and occurs when the atria (the upper chambers of the heart) contract very rapidly. This causes the lower chambers of the heart, the ventricles, to contract chaotically so that blood is inefficiently pumped to the body which can lead to tissue damage and even death.Dronedarone is prepared via a stepwise procedure which involves the synthesis of a number of intermediates, including 2-butyl-3-(4-methoxybenzoyl)-5-nitrobenzofuran and 2-butyl-3-(4-hydroxybenzoyl)-5-nitrobenzofuran.2-Butyl-3-aroyl-5-nitrobenzofurans are typically synthesised via Friedel-Craft acylation of 3-unsubstituted 2-butyl-5-nitrobenzofurans. Such reactions are described in U.S. Pat. No. 5,223,510 and U.S. Pat. No. 5,854 ...

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Номер записи: 10
09-01-2014 дата публикации

Method for Producing Fluorine-Containing Substituted Compound and Fluorine-Containing Substituted Compound

Номер: US20140012027A1
Автор: NAGAKI Aiichiro, YOSHIDA Junichi
Принадлежит:

A method for producing a fluorine-containing substituted compound, the method including: introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; and introducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound. 1. A method for producing a fluorine-containing substituted compound , the method comprising:introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; andintroducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound.2. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 6 carbon atoms, and {'br': None, 'i': T≦−', 't−, '3.848.'}, 'wherein a temperature T (° C.) inside the microreactor into which the organofluorine compound and the organolithium compound have been introduced and a residence time t (sec) thereof in the microreactor satisfy the following relation3. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 2 carbon atoms, andwherein a temperature T (° C.) inside the microreactor into which the organofluorine compound and the organolithium compound have been introduced and a residence time t (sec) thereof in the microreactor satisfy the relations −100≦T≦0 and 0.15≦t≦8.4, respectively.4. The method according to claim 1 ,wherein the organofluorine compound is a fluoroalkyl halide having 3 carbon atoms, and {'br': None, 'i': T≦−', 't−, '3.245.'}, 'wherein a temperature T (° C.) inside the microreactor into which the organofluorine ...

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Номер записи: 11
16-01-2014 дата публикации

PROCESS FOR THE MANUFACTURE OF DIBENZOYLMETHANE DERIVATIVES

Номер: US20140017183A1
Автор: Wehrli Christof
Принадлежит: DSM IP ASSETS B.V.

The invention relates to a process for the manufacture of substituted dibenzoylmethane derivatives. This economical process provides products in high purity and yields and results in shorter reaction times. 2. The process according to wherein Rand Rare independently selected from the group consisting of hydrogen claim 1 , Cto Calkyl and Cto Calkoxy.3. The process according to wherein Ris hydrogen and Ris methyl claim 1 , ethyl or 1 claim 1 ,1-dimethylethyl.4. The process according to wherein the condensation is carried out in an inert solvent.5. The process according to wherein the inert solvent is toluene and/or xylene claim 4 , preferably toluene.6. The process according to wherein the potassium alcoholate is potassium methylate and/or potassium tert.-butylate claim 1 , preferably potassium methylate.7. The process according to wherein the alcohols ROH and ROH are removed continuously as formed.8. The process according to wherein Ris methoxy claim 1 , Ris 1 claim 1 ,1-dimethylethyl and Ris methyl claim 1 , ethyl or 1 claim 1 ,1-dimethylethyl.9. The process according to wherein the molar ratio of the ketone of formula (II) to the ester of formula (III) is selected in the range of 0.5 to 1.25 claim 1 , preferably in the range of 0.9 to 1.10. The process according to wherein the molar ratio of the ketone of formula (II) to the potassium alcoholate is selected in the range of 0.5 to 1.1 claim 1 , preferably in the range of 0.8 to 111. The process according to wherein the solvent is toluene and the reaction temperature is selected in the range of 80° to 120° C.12. The process according to wherein the condensation step is followed by hydrolysis using an organic or mineral acid claim 1 , preferably a mineral acid.13. The process according to wherein the mineral acid is sulfuric acid.15. A composition according to claim 14 , wherein the composition is a topical composition further comprising a topical carrier. The invention relates to an improved process for the ...

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Номер записи: 12
20-02-2014 дата публикации

Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof

Номер: US20140051854A1
Автор: Damjan Sterk, Marko Jukic, Zdenko Casar
Принадлежит: Lek Pharmaceuticals dd

The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.

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Номер записи: 13
06-01-2022 дата публикации

Process for the direct alpha-methylenation of ketones

Номер: US20220002221A1
Автор: Olivier Back
Принадлежит: Rhodia Operations SAS

The invention relates to a process for preparing an α-methylene ketone comprising the step of reacting a ketone with formaldehyde in the presence of a catalyst which is an organic compound comprising at least one acid function or the corresponding salt, ester or amide thereof and at least one amine function or the corresponding ammonium salt, or a zwitterion thereof.

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Номер записи: 14
07-01-2021 дата публикации

METHOD FOR PURIFICATION OF 4-HYDROXYACETOPHENONE

Номер: US20210002200A1
Автор: BOLTE Karolin, LIUXIN Yan, PILLAI Ravikumar, Siegel Sven, SUESS Ev
Принадлежит:

Methods of purifying crude 4-hydroxyacetophenone using one or more solvents as well as products comprising or consisting of crystallized 4-hydroxyacetophenone and one, two or more solvent(s). The products may be obtained or obtainable from the methods for purifying crude 4-hydroxyacetophenone. 112-. (canceled)13. A method of purifying crude 4-hydroxyacetophenone comprising:(a) providing crude 4-hydroxyacetophenone,(b) mixing the crude 4-hydroxyacetophenone of step (a) with two or more solvents to obtain a mixture,(c) optionally, heating the mixture obtained in step (b) to dissolve the 4-hydroxyacetophenone,(d) optionally, adding an adsorbent to the mixture of step (b) or step (c), if present,(e) optionally, cooling the mixture of step (b), step (c) or step (d), if present, to a temperature above the crystallization temperature of 4-hydroxyacetophenone,(f) if step (d) is present, removing the adsorbent from the mixture of step (d) or step (e), if present,(g) cooling of the mixture of step (b) or step (c), if present, or further cooling of the mixture obtained in step (e), if step (d) is not present, or step (f), if present, to a temperature below the crystallization temperature of 4-hydroxyacetophenone to induce crystallization of 4-hydroxyacetophenone and to obtain crystallized 4-hydroxyacetophenone, 'optionally, carrying out steps (i) to (k) one or more times:', '(h) collecting the crystallized 4-hydroxyacetophenone, and'}(i) dissolving the crystallized 4-hydroxyacetophenone of step (h) or step (k) in two or more solvents, optionally under heating, to produce a solution,(j) cooling of the solution of step (i) to a temperature below the crystallization temperature of 4-hydroxyacetophenone to induce crystallization of 4-hydroxyacetophenone and to obtain crystallized 4-hydroxyacetophenone,(k) collecting the crystallized 4-hydroxyacetophenone obtained in step (j), 'wherein each of the two or more solvents used in steps (b) and (i), if present, is independently selected ...

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Номер записи: 15
20-01-2022 дата публикации

BENZOPHENONE DERIVATIVE

Номер: US20220017445A1
Автор: Belowich Matthew E., Maurice Alvin M., Stracke Jordan, Westmeyer Mark D.
Принадлежит:

The present invention relates to a compound which is a benzophenone substituted with a hydroxyl-terminated alkylene oxide group (R) of formula 1: 3. The compound of wherein x is from 2 to 8; and y is from 10 to 16; wherein y is greater x.4. The compound of wherein the calculated Log P of R is in the range of from −4.0 to −1.2.5. The compound of wherein the calculated Log P of R is in the range of from −3.5 to −1.3.6. A coating composition comprising an aqueous dispersion of a binder claim 1 , a rheology modifier claim 1 , an opacifying pigment claim 1 , and from 0.04 to 2 weight percent claim 1 , based on the weight of the coating composition of the compound of . The present invention relates to a benzophenone derivative, more particularly a benzophenone functionalized with pendant propylene oxide and ethylene oxide repeat units.Photoinitiators are used in exterior architectural coatings to improve dirt pickup resistance (DPUR) and gloss retention. Norrish type II photoinitiators are especially effective at improving these characteristics, presumably by crosslinking the surface of the polymer film. When excited by UV irradiation, the photoinitiator abstracts a hydrogen from the polymer, creating a reactive radical capable of crosslinking. It is also possible that the photoinitiator generates singlet oxygen via energy transfer to triplet oxygen. This singlet oxygen then reacts to form hydroperoxyl and hydroxyl radicals capable of inducing crosslinking via hydrogen abstraction from the polymer backbone.Ideally, photoinitiators will improve targeted exterior performance without adversely impacting film flexibility and will have minimal impact on coating color either from the inherent absorption of the photoinitiator or its reaction byproducts. Benzophenone is an example of a photoinitiator that is especially effective for improving coating performance because it is capable of diffusing through the film to the surface before initiating the photo-induced crosslinking ...

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Номер записи: 16
12-01-2017 дата публикации

ELECTROCHEMICALLY ACTIVE AGENTS FOR PH MODULATION IN BIOLOGICAL BUFFERS

Номер: US20170008825A1
Автор: Ahmad Habib, Fomina Nadezda, Johnson Christopher, Kavusi Sam, Lang Christoph, Maruniak Autumn, RAGHUNATHAN Ashwin
Принадлежит:

Device and methods for use in a biosensor comprising a multisite array of test sites, the device and methods being useful for modulating the binding interactions between a (biomolecular) probe or detection agent and an analyte of interest by modulating the pH or ionic gradient near the electrodes in such biosensor. An electrochemically active agent that is suitable for use in biological buffers for changing the pH of the biological buffers. Method for changing the pH of biological buffers using the electrochemically active agents. The methods of modulating the binding interactions provided in a biosensor, analytic methods for more accurately controlling and measuring the pH or ionic gradient near the electrodes in such biosensor, and analytic methods for more accurately measuring an analyte of interest in a biological sample. 1. An electrochemically active composition comprising a quinone derivative , wherein:a reactivity between a nucleophile and the quinone derivative is reduced compared to a reactivity between the nucleophile and an unsubstituted quinone from which the quinone derivative is derived, andthe composition is configured such that the pH of the composition is electrochemically modulated via the quinone derivative.3. The composition of claim 2 , wherein all of the R groups of the quinone derivative are different from each other.4. The composition of claim 2 , wherein two or more of the R groups of the quinone derivative are the same.5. The composition of claim 1 , wherein the composition is an aqueous solution.6. The composition of claim 1 , further comprising an additive selected from the group consisting of: an aqueous buffer claim 1 , an organic solvent claim 1 , an electrolyte claim 1 , a buffer salt claim 1 , a bioreagent claim 1 , a biomolecule claim 1 , a surfactant claim 1 , a preservative claim 1 , a cryoprotectant claim 1 , and combinations thereof.7. The composition of claim 1 , wherein the one or more nucleophiles are selected from the group ...

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Номер записи: 17
27-01-2022 дата публикации

UBIQUITIN-SPECIFIC PEPTIDASE 24 INHIBITOR, MEDICINAL COMPOSITION INCLUDING THE SAME AND METHOD OF DELAYING OR REVERSING MULTIDRUG RESISTANCE IN CANCERS USING THE SAME

Номер: US20220024887A1
Автор: Hung Chien-Chung, YOUNG Ming-Jer
Принадлежит:

The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition including the same and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer sternness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers. 6. The USP24 inhibitor of claim 1 , wherein the siRNA is a double-stranded USP24 RNA claim 1 , a short-hairpin USP24 (shUSP24) RNA claim 1 , an isolated ribonucleic acid sequence or a viral siRNA construct claim 1 , and the viral siRNA construct is a lentiviral siRNA construct.12. The medicinal composition of claim 7 , wherein the salt of the carbonyl substituted phenyl compound is selected from the group consisting of oxalate claim 7 , phosphate claim 7 , sulfate and chloride.13. The medicinal composition of claim 7 , wherein the siRNA is a double-stranded USP24 RNA claim 7 , and the siRNA is an isolated ribonucleic acid sequence or a viral siRNA construct.14. The medicinal composition of claim 7 , wherein the viral siRNA construct is a lentiviral siRNA construct claim 7 , and a value of m.o.i. of the lentiviral siRNA is 2.5 to 10.15. The medicinal composition of claim 7 , wherein a dosage of the carbonyl substituted phenyl compound is 12.5 mg/kg to 25 mg/kg of body weight.16. The medicinal composition of claim 7 , wherein the cancer cell is a solid tumor cell or a blood cancer cell claim 7 , and the cancer cell is selected from the group consisting of a lung cancer cell claim 7 , a nasopharyngeal carcinoma cell claim 7 , a brain cancer cell claim 7 , a colorectal carcinoma cell claim 7 , a lymphoma cell claim 7 , a leukemia cell and a multiple myeloma cell. This application is a Continuation-in-part of U.S. application ...

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Номер записи: 18
08-01-2015 дата публикации

ANTIBACTERIAL AGENTS: PHLOROGLUCINOL DERIVATIVES

Номер: US20150011647A1
Автор: Ebright Richard H., Shen Juan
Принадлежит:

The invention provides a compound of formula I: 3. A composition comprising a compound of formula I as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable vehicle.4. A method for inhibiting a bacterial RNA polymerase comprising contacting the bacterial RNA polymerase with a compound of formula I as described in claim 1 , or a salt thereof.5. A method for inhibiting the growth of a bacterium comprising contacting the bacterium with a compound of formula I as described in claim 1 , or a salt thereof.6. A method for treating a bacterial infection in a mammal comprising administering to the mammal an effective amount of a compound of formula I as described in claim 1 , or a pharmaceutically acceptable salt thereof.78-. (canceled)9Mycobacterium tuberculosis, Staphylococcus aureusEnterococcus faecalis, Enterococcus faecium, Bacillus anthracis, Escherichia coli, Haemophilus influenzae, Moraxella catarrhalis, Francisella tularensis,Burkholderia mallei.. The method of claim 6 , wherein the bacteria is selected from MSSA and MRSA claim 6 , and10. (canceled)11. The composition of claim 3 , in the form of a disinfectant claim 3 , sterilant claim 3 , antispoilant claim 3 , or antiseptic.12. A composition comprising a compound of formula I as described in claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , and a pharmaceutically acceptable vehicle.13. The composition of claim 12 , in the form of a disinfectant claim 12 , sterilant claim 12 , antispoilant claim 12 , or antiseptic.14. A method for treating a bacterial infection in a mammal comprising administering to the mammal an effective amount of a compound of formula I as described in claim 2 , or a pharmaceutically acceptable salt thereof.15Mycobacterium tuberculosis, Staphylococcus aureusEnterococcus faecalis, Enterococcus faecium, Bacillus anthracis, Escherichia coli, Haemophilus influenzae, Moraxella catarrhalis, Francisella tularensis,Burkholderia ...

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Номер записи: 19
18-01-2018 дата публикации

PHOTOSTABLE COMPOUNDS, ABSORBING COMPOUNDS AND USES THEREOF

Номер: US20180016233A1
Автор: Ryan John, YORK Mark
Принадлежит: Commonwealth Scientific and Industrial Research Or ganisation

The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing cyclic compounds capable of absorbing electromagnetic radiation energy and having improved photostability due to the presence and location of one or more fluorine groups in relation to the double bond of the ring. 2. The compound of wherein R′ is selected from Cto Calkenyl claim 1 , Cto Calkynyl claim 1 , Cto Caryl claim 1 , Cto Cheteroaryl claim 1 , Cto Caroyl claim 1 , Cto Calkenone claim 1 , Cto Ccycloalkenyl claim 1 , Cto Ccycloalkenone claim 1 , or Cto Cheterocyclic claim 1 , all of which groups may be substituted or unsubstituted.3. (canceled)5. (canceled)6. The compound of wherein A is a six-membered nitrogen heterocycle comprising at one double bond claim 4 , which nitrogen heterocycle may be further substituted or unsubstituted.7. The compound of wherein A is a six-membered nitrogen heterocycle comprising one double bond and having the carbon atom to which W is attached also attached to a double bonded ring carbon claim 4 , which nitrogen heterocycle may be further substituted or unsubstituted.9. The compound of wherein Rand Rare independently selected from Cto Calkyl claim 8 , Cto Calkenyl or Cto Calkoxy claim 8 , each of which groups may be substituted or unsubstituted.1012-. (canceled)13. The compound of wherein at least one of Rand Rare fluorine or wherein Rand Rcombine to form a 6-membered ring with one or more fluorine substituents on the ring.14. (canceled)15. The compound of wherein Ris selected from halo claim 1 , Cto Calkyl claim 1 , Cto Calkenyl claim 1 , C-Caryl claim 1 , C-Cheteroaryl claim 1 , Cto Calkanone claim 1 , C-Ccycloalkyl claim 1 , C-Ccycloalkanone claim 1 , C-Ccycloalkenyl claim 1 , Cto Calkanoyl claim 1 , Cto Calkanoyloxy claim 1 , Cto Calkoxycarbonyl claim 1 , Cto Ccarbamoyl claim 1 , Cto Ccarboxyl claim 1 , haloalkyl claim 1 , N-alkyl claim 1 , N-aryl claim 1 , ...

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Номер записи: 20
16-01-2020 дата публикации

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

Номер: US20200017433A1
Автор: Dugan Michael, Flynn Autumn, Jui Nathan, Mays Suzanne, Ortlund Eric
Принадлежит: EMORY UNIVERSITY

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein. 2. The compound of claim 1 , wherein Rand Rare hydrogen claim 1 , Ris 1-phenylvinyl or 1-phenylethyl claim 1 , and Ris phenyl.3. The compound of claim 1 , wherein Ris alkyl terminally substituted with a hydroxy claim 1 , carboxy claim 1 , or phosphate claim 1 , wherein the hydroxy claim 1 , carboxy claim 1 , or phosphate are optionally further substituted with R.5. The compound of claim 1 , wherein Ris hydroxyl claim 1 , alkyl claim 1 , amino claim 1 , aminoalkyl claim 1 , carbamoyl claim 1 , sulphate claim 1 , sulfonate claim 1 , aminosulfonyl claim 1 , phosphate claim 1 , phosphonate claim 1 , or heterocyclyl claim 1 , wherein Ris optionally substituted with R.7. The compound of claim 6 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, and Ris aminosulfonyl;'}{'sup': '1', 'e) X is —(C═O)—, Ris amino;'}{'sup': '1', 'f) X is O, Y is —(C═O)—, Ris amino;'}{'sup': '1', 'g) X is O, Y is —(C═O)—, Z is —NH—, and Ris sulfonate; and'}{'sup': '1', 'h) X is O, Y is —(C═O)—, Z is —NH—, and Ris aminosulfonyl.'}8. The compound of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl sulfamide or salt thereof.9. The compound of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl)acetamide or salt thereof.10. A pharmaceutical composition ...

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Номер записи: 21
24-01-2019 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20190023649A1
Автор: Berman Judd, Garvey David S., Quach Tan
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. 115-. (canceled)17. The method of claim 16 , wherein said visual cycle product is a toxic visual cycle product.18. The method of claim 17 , wherein said toxic visual cycle product is lipofuscin or N-retinylidene-N-retinylethanolamine (A2E).19. The method of claim 16 , wherein said compound reduces mislocalization of said opsin protein.20. The method of claim 16 , wherein said opsin protein is present in a cell.21. The method of claim 20 , wherein said cell is a cone cell or rod cell.22. The method of claim 20 , wherein said cell is present in a mammalian eye.23. A method of inhibiting the formation or accumulation of a visual cycle product claim 20 , comprising contacting an opsin protein with a compound selected from the group consisting of:3-(trifluoromethyl)-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline hydrochloride (Compound 1);3-methyl-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 2);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzamide (Compound 3);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzonitrile (Compound 4);3-chloro-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 5);1-methyl-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 6);1-fluoro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 7);1-chloro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 8);1-(trifluoromethyl)-3-((2,6,6-trimethylcyclohex- ...

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Номер записи: 22
24-01-2019 дата публикации

INHIBITORS OF BACTERIAL RNA POLYMERASE: ARYLPROPANOYL, ARYLPROPENOYL, AND ARYLCYCLOPROPANECARBOXYL PHLOROGLUCINOLS

Номер: US20190023682A1
Автор: Ebright Richard H., Freundlich Joel, Jaskowski Mark, Mittal Nisha, Shen Juan
Принадлежит: Rutgers, The State University of New Jersey

The invention provides compounds that are inhibitors of bacterial RNA polymerase. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy. 2. The compound tautomer or salt of which is a compound of formula I or a tautomer or salt thereof.3. The compound tautomer or salt of which is a compound of formula II or a tautomer or salt thereof.4. The compound tautomer or salt of which is a compound of formula III or a tautomer or salt thereof.5. The compound tautomer or salt of which is a compound of formula IV or a tautomer or salt thereof.6. The compound tautomer or salt of which is a compound of formula V or a tautomer or salt thereof.7. The compound tautomer or salt of which is a compound of formula VI or a tautomer or salt thereof.1115-. (canceled)16. A composition comprising a compound or tautomer as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable vehicle.17. A method for inhibiting a bacterial RNA polymerase comprising contacting the bacterial RNA polymerase with a compound or tautomer as described in claim 1 , or a salt thereof.18. A method for inhibiting the growth of bacteria comprising contacting the bacteria with a compound or tautomer as described in claim 1 , or a salt thereof.19. A method for treating a bacterial infection in a mammal comprising administering to the mammal an effective amount of a compound or tautomer as described in claim 1 , or a pharmaceutically acceptable salt thereof.2024-. (canceled) This invention was made with Government support under U19-A1109713 awarded by the National Institutes of Health. The government has certain rights in the invention.Bacterial infections remain among the most common and deadly causes of human disease. Infectious ...

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Номер записи: 23
04-02-2016 дата публикации

Preparation of Butanol from Ethanol Derived from Fermentation

Номер: US20160031776A1
Автор: Berggren Mark, Henri John T., Zubrin Robert, Zygmunt Jan
Принадлежит: Pioneer Energy, Inc.

In one embodiment, the present application discloses methods to selectively synthesize higher alcohols and hydrocarbons useful as fuels and industrial chemicals from syngas and biomass. Ketene and ketonization chemistry along with hydrogenation reactions are used to synthesize fuels and chemicals. In another embodiment, ketene used to form fuels and chemicals may be manufactured from acetic acid which in turn can be synthesized from synthesis gas which is produced from coal, biomass, natural gas, etc. 137-. (canceled)39. The method of claim 38 , wherein Rand Rare hydrogen and the formula I is ketene claim 38 , and the ketene is prepared from acetic acid.40. The method of where the acetic acid which is made from ethanol.41. The method of where the ethanol is prepared by fermentation.38. The method of where butanol is a product.43. The method of where the transition metal catalyst comprises more than one transition metal.44. The method of wherein the transition metal catalyst is a copper zinc oxide based catalyst.45. The method of wherein the transition metal catalyst is combined with a main group metal.46. The method of wherein the butanol is blended with an automotive fuel.48. The method of wherein the Calcohol is methanol.49. The method of where the Calcohol is butanol.50. The method of claim 41 , wherein Rand Rare hydrogen and the formula I is ketene claim 41 , and the ketene is prepared from acetic acid.51. The method of where the acetic acid which is prepared from ethanol.52. The method of where the ethanol is prepared by fermentation.53. The method of where the metal catalyst is a transition metal.54. The method of where the metal catalyst is a transition metal.55. The method of where the transition metal catalyst comprises a main group metal.56. The method of where the transition metal catalyst is a copper-zinc based catalyst. This application claims the benefit of U.S. Provisional Application No. 61/558,321 filed Nov. 10, 2011 entitled “Synthesis of Higher ...

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Номер записи: 24
04-02-2021 дата публикации

COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX

Номер: US20210032198A1
Автор: Albury Mary Susan, Elliott Catherine, Moore Anthony Lennox, Young Luke Edward
Принадлежит:

The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bccomplex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections. 133-. (canceled)35. The method according to claim 34 , wherein Ris a hydroxyl group.36. The method according to claim 34 , wherein Ris a straight chain or branched alkyl or alkylene with 6 to 15 C atoms claim 34 , 8 to 12 C atoms or 8 to 10 C atoms claim 34 , that is optionally mono- or polysubstituted by a Cto Calkyl group.37. The method according to claim 34 , wherein Ris a diene having 6 to 15 C atoms that is substituted with at least one methyl group.38. The method according to claim 34 , wherein Ris a chlorine claim 34 , bromine claim 34 , fluorine or iodine group.39. The method according claim 34 , wherein Ris a chlorine group; or wherein R6 is a methyl claim 34 , ethyl or propyl group.40. The method according claim 34 , wherein:—{'sub': 1', '2', '3', '3', '3, 'Ris selected from CHO; CN; C(O)NH; C(O)NHCH; C(O)CH; COOH; and COOCH;'}{'sub': '2', 'Ris a hydroxyl group;'}{'sub': 3', '1', '4, 'Ris a straight chain or branched alkyl or alkylene with 4 to 20 C atoms, that is optionally mono- or polysubstituted by a Cto Calkyl group;'}{'sub': '4', 'Ris a hydroxyl group;'}{'sub': '5', 'Ris a chlorine atom; and'}{'sub': 6', '1', '4, 'Ris H or a Cto Calkyl group.'}41. The method according to claim 34 , wherein:—{'sub': 1', '2', '3', '3', '3, 'Ris selected from CHO; CN; C(O)NH; C(O)NHCH; C(O)CH; COOH; and COOCH;'}{'sub': '2', 'Ris a hydroxyl group;'}{'sub': 3', '1', '2, 'Ris a straight chain or branched alkyl or alkylene with 6 to 15 C atoms, that is optionally mono- or polysubstituted by a Cto Calkyl group;'}{'sub': '4', 'Ris a hydroxyl group;'}{'sub': '5', 'Ris a chlorine atom; and'}{'sub': 6', '1', '4, 'Ris H or a Cto Calkyl group.'}42. The method according to claim 34 , wherein:—{'sub': 1', '2 ...

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Номер записи: 25
11-02-2016 дата публикации

TRPV-1 RECEPTOR ANTAGONIST COMPOUND DERIVED FROM 1,3,4-THIADIAZOLE ALKYLAMIDES AND CHALCONES

Номер: US20160039778A1
Автор: BRAUCHI ULLOA Sebastián, LESPAY REBOLLEDO Carolyne, ZÁRRAGA OLAVARRIA Miguel
Принадлежит:

This technology encompasses compounds derived from 1,3,4-thiadiazole alkylamides and chalcone, which inhibit the activation of the TRPV-1 receptor using capsaicin and temperature. Also disclosed is the use of these compounds in the treatment of diseases with TRPV-1 overexpression, such as chronic pain. 1. Compounds derived from 1 ,3 ,4-thiadiazol alkylamides wherein they inhibit TRPV-1 receptor activation.2. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they inhibit the capsaicin and temperature activation of the TRPV-1 receptor.3. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein their R structure is a saturated alkyl chain defined by saturated linear chains of 6 to 8 carbons where X is defined as a H atom or an iodine atom.4. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they are obtained through O-acylation reaction claim 1 , amine condensation claim 1 , oxidative cyclization of thiosemicarbazone claim 1 , N-acylation reaction and alkaline hydrolysis.5. Compounds derived from 1 claim 1 ,3 claim 1 ,4-thiadiazol alkylamides claim 1 , according to claim 1 , wherein they correspond specifically to the following compounds:a) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]nonamide,b) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-nonamide,c) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-octanamide,d) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-octanamide,e) N-[5-(4-hydroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-heptanamide,f) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-heptanamide,g) N-[5-(4-hidroxy-5-methoxy-3-iodophenyl)-1,3,4-thiadiazole-2-yl]-hexanamide, andh) N-[5-(4-hydroxy-3-methoxyphenyl)-1,3,4-thiadiazole-2-yl]-hexanamide.6. Compounds derived from chalcones claim 1 , wherein they inhibit the ...

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Номер записи: 26
12-02-2015 дата публикации

Bi-Aromatic And Tri-Aromatic Compounds As NADPH Oxidase 2 (Nox2) Inhibitors

Номер: US20150045387A1
Автор: Howlin Brendan, Li Jian-Mei, Meijles Daniel Nathan
Принадлежит:

Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflammatory diseases, cancers, ageing and age related disorders, kidney diseases, neurodegenerative diseases, diabetes and conditions associated with diabetes. The compounds, their preparation and pharmaceutical compositions comprising them are disclosed. 6. A compound according to any one of the preceding to , wherein{'sup': 1', '2', '3', '4', '5, 'Rand Rare OH and R, Rand Rare H; or'}{'sup': 4', '5', '1', '2', '3, 'Rand Rare OH and R, Rand Rare H.'}7. A compound according to any one of the preceding to , wherein Ris methyl , hydroxymethyl or OH; Ris methyl , hydroxymethyl or OH; and Rand Rare H.8. A compound which is selected from:2,3-dihydroxyphenyl)methyl 4-hydroxy-3-(hydroxymethyl)benzoate;3-(2,3-dihydroxyphenyl)-1-(4-hydroxy-3-(hydroxymethyl)phenyl)propan-1-one;3-(2,3-dihydroxyphenyl)-1-(3,4-dihydroxyphenyl)propan-1-one;N-(2,3-dihydroxybenzyl)-4-hydroxy-3-(dihydroxymethyl)benzamide;N-(2,3-dihydroxybenzyl)-3,4-dihydroxybenzamide;N-(2,3-dihydroxybenzyl)-3-hydroxy-4-(hydroxmethyl)benzamine;2,3-dihydroxybenzyl 4-hydroxy-3-(hydroxymethyl)benzimine;2,3-dihydroxybenzyl 4-hydroxy-3-(3-hydroxybenzyl)benzoate;2,3-dihydroxybenzyl 3-benzyl-4-hydroxybenzoate;2,3-dihydroxybenzyl 3-(hydroxymethyl)-4-(hydroxymethyl)benzoate;2,3-dihydroxybenzyl 3,4-dihydroxybenzoate;2,3-dihydroxybenzyl 3-hydroxy-4-methylbenzoate;2,4-dihydroxybenzyl 3-hydroxy-4-(hydroxymethyl)benzoate;2,3-dihydroxybenzyl 2-napthoate;2,3-dihydroxybenzyl 6-hydroxy-7-(4-hydroxyphenyl)-2-napthoate;2,3-dihydroxybenzyl 6-hydroxy-7-phenyl-2-napthoate;2,3-dihydroxybenzyl 6-hydroxy-7-methyl-2-napthoate;2,3-dihydroxybenzyl 6-hydroxy-7-(hydroxymethyl)-2-napthoate;2,3-dihydroxybenzyl 6,7-dihydroxy-2-napthoate;2,3-dihydroxybenzyl 7-hydroxy-2-napthoate;2,3-dihydroxybenzyl 6,8- ...

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Номер записи: 27
06-02-2020 дата публикации

METHOD FOR PURIFICATION OF 4-HYDROXYACETOPHENONE

Номер: US20200039911A1
Автор: BOLTE Karolin, LIUXIN Yan, PILLAI Ravikumar, Siegel Sven, SUESS Ev
Принадлежит:

Methods of purifying crude 4-hydroxyacetophenone using one or more solvents as well as products comprising or consisting of crystallized 4-hydroxyacetophenone and one, two or more solvent(s). The products may be obtained or obtainable from the methods for purifying crude 4-hydroxyacetophenone. 2. The method according to claim 1 , wherein the one or more solvent(s) used in steps (b) and (i) claim 1 , if present claim 1 , independently comprise one of the following combinations:ethanol/water,ethyl acetate/cyclohexane,dimethyl carbonate/cyclohexane,butyl acetate/cyclohexane, ordiethyl carbonate/cyclohexane.3. The method according to claim 1 , wherein in step(s) (b) and/or (i) claim 1 , if present claim 1 , independently 0.5 to 70 wt. % of 4-hydroxyacetophenone claim 1 , based on the total weight of the mixture obtained in step (b) or step (i) claim 1 , respectively claim 1 , is combined with the one or more solvent(s).4. The method according to claim 1 , wherein in step (c) claim 1 , the mixture obtained in step (b) is heated to reflux.5. The method according to claim 1 , wherein in step (d) claim 1 , 0.1 to 25 wt. % claim 1 , of the adsorbent claim 1 , based on the total weight of the mixture of step (d) claim 1 , is added to the mixture of step (b) or step (c) claim 1 , if present.6. The method according to claim 1 , wherein when step (c) and step (e) are present claim 1 , in step (e) the mixture of step (c) or step (d) claim 1 , if present claim 1 , is cooled to a temperature of 30 to 125° C.7. The method according to claim 1 , wherein in step (g) the mixture of step (b) or step (c) claim 1 , if present claim 1 , or the mixture of step (e) claim 1 , if step (d) is not present claim 1 , or step (f) claim 1 , if present claim 1 , or the solution obtained in step (i) claim 1 , if present claim 1 , is cooled to a temperature of −10° C. to below room temperature.8. The method according to claim 1 , wherein the drying of the crystallized 4-hydroxyacetophenone in step (1) ...

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Номер записи: 28
18-02-2021 дата публикации

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

Номер: US20210047258A1
Автор: Dugan Michael, Flynn Autumn, Jui Nathan, Mays Suzanne, Ortlund Eric
Принадлежит:

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein. 4. The method of claim 3 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, and Ris aminosulfonyl;'}{'sup': '1', 'e) X is —(C═O)—, Ris amino;'}{'sup': '1', 'f) X is O, Y is —(C═O)—, Ris amino;'}{'sup': '1', 'g) X is O, Y is —(C═O)—, Z is —NH—, and Ris sulfonate; and'}{'sup': '1', 'h) X is O, Y is —(C═O)—, Z is —NH—, and Ris aminosulfonyl.'}5. The method of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl sulfamide or salt thereof.6. The method of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl)acetamide or salt thereof.7. The method of claim 1 , wherein the cardiovascular disease is cardiovascular disease is selected from coronary artery disease (CAD) claim 1 , angina claim 1 , myocardial infarction claim 1 , stroke claim 1 , hypertensive heart disease claim 1 , rheumatic heart disease claim 1 , cardiomyopathy claim 1 , heart arrhythmia claim 1 , congenital heart disease claim 1 , valvular heart disease claim 1 , carditis claim 1 , aortic aneurysms claim 1 , peripheral artery disease claim 1 , and venous thrombosis.11. The method of claim 10 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, ...

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Номер записи: 29
14-02-2019 дата публикации

NUCLEAR RECEPTOR MODULATORS AND THEIR USE FOR THE TREATMENT AND PREVENTION OF CANCER

Номер: US20190047932A1
Автор: Kim Yeong Sang, Kumar Vineet, Lee Sunmin, Malhotra Sanjay V., Neckers Jane B.
Принадлежит: The United States of America, as represented by the Secretary, Department of Health and Human Serv

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: 162.-. (canceled)64102.-. (canceled) This application is a Divisional of U.S. patent application Ser. No. 14/126,178 filed Feb. 7, 2014, which is a U.S. National Phase of International Patent Application No. PCT/US2012/042753, filed Jun. 15, 2012, which claims the benefit of U.S. Provisional Patent Application No. 61/497,129, filed Jun. 15, 2011, each of which the disclosures are incorporated by reference.This invention was made with Government support under project number ZIC SC 006743 by the National Institutes of Health, National Cancer Institute. The Government has certain rights in the invention.Incorporated by reference in its entirety herein is a computer-readable nucleotide/amino acid sequence listing submitted concurrently herewith and identified as follows: One 1,910 Byte ASCII (Text) file named “740367 ST25.txt,” created on Aug. 21, 2018.In the United States there will be at least an estimated 217,000 new cases of prostate cancer, and over 32,000 deaths as a result of prostate cancer this year. Treatment of advanced prostate cancer is limited by the development of resistance to antiandrogen therapy. Androgen receptors (AR), as well as other sex steroid binding receptors, such as the estrogen receptor (ER) and progesterone receptor (PR) have been previously classified as type I nuclear receptors. Castrate-resistant prostate cancer (CRPC) is commonly associated with increased AR gene expression, which can occur through AR gene amplification or other mechanisms. Elevated AR expression is necessary and sufficient to confer resistance to antiandrogen therapy in mouse xenograft models. In addition, first generation AR antagonists such as bicalutamide (also called Casodex®) or flutamide demonstrate agonist properties in cells engineered to express higher AR amounts. The partial agonism of these compounds is a ...

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Номер записи: 30
25-02-2016 дата публикации

Eight Diasteromers of Vittatalactone and Methods of Making, and Methods of Attracting Acalymma vittatum

Номер: US20160052901A1
Автор: Chauhan Kamlesh R., Paraselli Bheema R.
Принадлежит:

Disclosed are methods for preparing a mixture of eight diasteromers of vittatalactone 4Acalymma vittatumAcalymma vittatumAcalymma vittatum. A method of attracting to an object or area claim 3 , comprising treating said object or area with a attracting composition comprising a attracting effective amount of the composition according to . This application claims the benefit of U.S. Provisional Application No. 62/040,102, filed 21 Aug. 2014, which is incorporated herein by reference in its entirety.Disclosed are methods for preparing a mixture of eight diasteromers of vittatalactoneAlso disclosed are mixtures of eight diasteromers of vittatalactone produced by the methods described herein. In addition there are described compositions comprising a mixture of eight diasteromers of vittatalactone and optionally 2E,6Z-nona-2,6-dienaland optionally cucurbitacin B or cucurbitacin B wherein the bond between carbons 1 and 2 is replaced with C═C, or cucurbitacin B wherein OH is attached to C25, or cucurbitacin B wherein the bond between carbons 1 and 2 is replaced with C═C and OH is attached to C25, or cucurbitacin B wherein the bond between carbons 1 and 2 is replaced with C═C and OH is attached to C25 and the bond between carbons 23 and 24 is C—C, or cucurbitacin B wherein OH is attached to C25 and the bond between carbons 23 and 24 is C—C, and optionally a carrier. Furthermore, there are describe methods of attracting to an object or area, involving treating said object or area with a attracting composition containing a attracting effective amount of the compositions described herein. The methods, mixtures, and compositions described herein exclude the following 24 diastereomers:Vegetable crops are an important commodity in the United States. These crops include cucurbit crops (e.g., squash, melons, cucumbers, pumpkins) (Cavanagh, A., et al., J. J. Econ. Entomol., 102: 1101-1107 (2009)). The main insect pest of these cucurbit crops is the striped cucumber beetle, (Coleoptera ...

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Номер записи: 31
22-05-2014 дата публикации

METHODS AND COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES

Номер: US20140142194A1
Автор: CHEN Chih-Ming, Liu Sheng-Yung, Wen Wu-Che
Принадлежит: GOLDEN BIOTECHNOLOGY CORPORATION

The present invention provides methods and compositions for treating neurodegenerative diseases by cyclohexenone compounds. 2. The method of claim 1 , wherein said method inhibits β-Amyloid induced neuronal damage in a subject.3. The method of claim 1 , wherein said neurodegenerative disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , multiple sclerosis claim 1 , stroke syndromes claim 1 , and amyotrophic lateral sclerosis.4. The method of claim 3 , wherein said neurodegenerative disease is Alzheimer's disease.5. The method of claim 1 , wherein said cyclohexenone compound inhibits β-Amyloid induced neuronal damage in a subject.7. The method of claim 6 , wherein the β-Amyloid induced disease is Alzheimer's disease or Down's syndrome.8. The method of claim 1 , wherein said cyclohexenone compound claim 1 , or a pharmaceutically acceptable salt claim 1 , metabolite claim 1 , solvate or prodrug thereof claim 1 , is administered orally claim 1 , parenterally or intravenously.9Antrodia camphorata.. The method of claim 1 , wherein said compound is isolated from10. The method of claim 1 , wherein R is a hydrogen claim 1 , C(═O)CH claim 1 , C(═O)CH claim 1 , or C(═O)CH.11. The method of claim 1 , wherein each of R claim 1 , Rand Rindependently is a hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , hexyl claim 1 , heptyl claim 1 , or octyl.12. The method of claim 11 , wherein Ris a hydrogen or methyl.13. The method of claim 11 , wherein Ris a hydrogen or methyl.14. The method of claim 1 , wherein Ris halogen claim 1 , NH claim 1 , NHCH claim 1 , N(CH) claim 1 , OCH claim 1 , OCH claim 1 , C(═O)CH claim 1 , C(═O)CH claim 1 , C(═O)OCH claim 1 , C(═O)OCH claim 1 , C(═O)NHCH claim 1 , C(═O)NHCH claim 1 , C(═O)NH claim 1 , OC(═O)CH claim 1 , OC(═O)CH claim 1 , OC(═O)OCH claim 1 , OC(═O)OCH claim 1 , OC(═O)NHCH claim 1 , OC(═O)NHCH claim 1 , or OC(═O)NH.15. The method of ...

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Номер записи: 32
12-03-2015 дата публикации

Optical Film

Номер: US20150068427A1
Автор: Cho Yong Gyun, Im Min Joung, Jo Yeong Min, Kim Hyuk Jun, Kim Myoung Lae, Kim Won Yeob, KWAK Hyo Shin, Lee Seung Eon
Принадлежит:

Provided is an optical film used for the optical compensation, in which additives are added to thereby have a good stability at high temperature and high humidity, a higher chromaticity, a higher Haze and a higher moisture resistance, as well as a small thickness direction retardation (Rth). 3. The optical film of claim 2 , wherein Rut claim 2 , Rand Rin Chemical formula 2 or 3 claim 2 , are each independently selected from hydrogen claim 2 , (C1-C5)alkyl claim 2 , (C3-C20)cycloalkyl claim 2 , (C3-C10)heterocycloalkyl claim 2 , (C6-C10)aryl claim 2 , and (C4-C10) heteroaryl claim 2 ,{'sub': 11', '21', '31, 'alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl of R, R, and Rare further substituted with at least one selected from (C1-C7)alkyl, halogen, nitro, cyano, hydroxy, and amino,'}{'sub': 11', '21', '31, 'provided that at least two of R, Rand Rinclude a ring-type substituent selected from (C3-C20)cycloalkyl, (C6-C20)aryl, (C3-C20)heterocycloalkyl, and (C4-C20)heteroaryl.'}6. The optical film of claim 1 , wherein Re (λ) and Rth (λ) are satisfied with the following Formulae (I) and (II).{'br': None, '0≦Re(587)≦10'}{'br': None, '−10≦Rth(587)≦10'}(In the Formulae, Re (λ) represents an in-plane retardation (unit: nm) at a wavelength of λ nm, and Rth (λ) represents a film thickness direction retardation (unit: nm) at a wavelength of λ nm.7. The optical film of claim 1 , wherein the optical film is a cellulose acetate film having a substitution degree measured according to ASTM D-817-91 of 2.7 to 3.0.9. The optical film composition of claim 8 , further comprising claim 8 , as an additive claim 8 , at least one or two selected from an anti-ultraviolet agent claim 8 , a fine particle claim 8 , a plasticizer claim 8 , a deterioration inhibitor claim 8 , a peeling agent claim 8 , an infrared absorbing agent claim 8 , and an optical anisotropy controlling agent.10. An optical structure using the optical film of .11. The optical structure of claim 10 , wherein the ...

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Номер записи: 33
27-02-2020 дата публикации

METHOD FOR MANUFACTURING 1,4-BIS(4-PHENOXYBENZOYL)BENZENE AT AN ELEVATED TEMPERATURE

Номер: US20200062683A1
Автор: AMSTUTZ Jérome, JOUANNEAU Julien, Le Guillaume
Принадлежит: Arkema France

The invention relates to a method for manufacturing 1,4-bis(4-phenoxybenzoylbenzene), comprising: 1. A method for manufacturing 1 ,4-bis(4-phenoxybenzoyl)benzene , comprising:providing a reactant mixture comprising terephthaloyl chloride and diphenyl ether in a solvent;adding a Lewis acid to the reactant mixture, so as to obtain a product mixture;wherein the temperature of the reactant mixture is greater than 5° C. during at least part of the step of adding the Lewis acid to the reactant mixture.2. The method of claim 1 , wherein the Lewis acid is aluminum trichloride.3. The method of or claim 1 , wherein the temperature of the reactant mixture is at least 15° C. during at least part of the step of adding the Lewis acid to the reactant mixture.4. The method of claim 1 , wherein the temperature of the reactant mixture is at least 30° C. claim 1 , after 20% by weight of Lewis acid has been added to the reactant mixture claim 1 , relative to the total weight of Lewis acid added to the reactant mixture.5. The method of claim 1 , wherein the temperature of the reactant mixture increases during the step of adding the Lewis acid to the reactant mixture claim 1 , from an initial temperature to a final temperature.6. The method of claim 5 , wherein the initial temperature is from 0 to 80° C.7. The method of claim 5 , wherein the final temperature is at least 30° C.8. The method of claim 1 , wherein the temperature of the reactant mixture does not exceed 100° C. during the step of adding the Lewis acid.9. The method of claim 1 , wherein the solvent is ortho-dichlorobenzene.10. The method of claim 1 , wherein a temperature difference between a final temperature and an initial temperature is from 1 to 120° C.11. The method of claim 1 , wherein the solvent is a separate solvent from the diphenyl ether.12. The method of claim 1 , wherein the concentration of terephthaloyl chloride (relative to a sum of the solvent claim 1 , the terephthaloyl chloride claim 1 , the diphenyl ether ...

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Номер записи: 34
15-03-2018 дата публикации

NOVEL ASPIRIN DERIVATIVES AND USES THEREOF

Номер: US20180072652A1
Автор: Sang Shengmin
Принадлежит:

The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer. 2. The method of claim 1 , wherein Ris —OH.4. The method of claim 3 , wherein each of Rand Ris —OH.5. The method of claim 3 , wherein each of Rand Ris independently —O—Calkyl.6. The method of claim 3 , wherein each of Rand Ris independently —O—Calkyl.7. The method of claim 3 , wherein each of Rand Ris —O-Me.9. The method of claim 8 , wherein Ris —OH and Ris —O—C(O)Me.12. The method of claim 11 , wherein Ris —OH.14. The method of claim 13 , wherein each of Rand Ris —OH.15. The method of claim 13 , wherein each of Rand Ris independently —O—Calkyl.16. The method of claim 13 , wherein each of Rand Ris independently —O—Calkyl.17. The method of claim 13 , wherein each of Rand Ris —O-Me.19. The method of claim 18 , wherein Ris —OH and Ris —O—C(O)Me. This application is a divisional of U.S. application Ser. No. 15/660,032, filed Jul. 26, 2017, which is a divisional of U.S. application Ser. No. 14/883,852, filed Oct. 15, 2015, now U.S. Pat. No. 9,745,248, issued Aug. 29, 2017, which is a continuation of and claims priority to U.S. application Ser. No. 13/918,394, filed Jun. 14, 2013, now U.S. Pat. No. 9,187,402, issued Nov. 17, 2015, which claims benefit of U.S. Provisional Patent Application Ser. Nos. 61/791,826, filed Mar. 15, 2013, and 61/659,647, filed Jun. 14, 2012, the disclosure of each of which is incorporated herein by reference in its entirety.This invention was made with government support under 1-R03-CA159353-01A1, awarded by the National Institutes of Health. The government has certain rights in the invention.The present invention generally relates to novel aspirin derivatives and the prevention and/or treatment of disorders responsive to aspirin derivatives.Colorectal cancer (CRC) is a ...

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Номер записи: 35
05-06-2014 дата публикации

Flame-Retardant Derivatives

Номер: US20140155569A1
Автор: Coughlin E. Bryan, Emrick Todd, Kiratitanavit Weeradech, Ku Bon-Cheol, KUMAR Jayant, Nagarajan Ramaswamy, Nagarajan Subhalakshmi, RAVICHANDRAN Sethumadhavan
Принадлежит: University of Massachusetts

A chemical compound of structural formula (I) useful in preparation of flame retardant materials is disclosed. Homopolymer, and copolymers of a compound of formula (I), as well as methods of preparing said homo- and copolymers are also disclosed. Polymers described herein advantageous possess low heat release capacities and high char yields. 3. The compound of claim 1 , wherein Ris —OH and Ris —OH or —OCH.4. The compound of claim 3 , wherein R claim 3 , R claim 3 , Rand Reach is independently —H or a C1-C8 alkyl.5. The compound of claim 1 , wherein:{'sub': 1', '2', '3', '4', '5', '6, 'Ris —OH, Ris —OH, and R, R, R, and Reach is each independently a C5-C8 alkyl, or'}{'sub': 1', '2', '3', '3', '4', '5', '6, 'Ris —OH, Ris —OCH, and R, R, R, and Reach is each independently a C5-C8 alkyl.'}6. The compound of claim 1 , wherein:{'sub': 1', '3', '4', '5', '6', '3, 'Ris —OH, R, R, R, and Reach is —CH; and'}{'sub': 2', '3, 'Ris —OH or —OCH.'}9. The homopolymer of claim 7 , wherein Ris —OH and Ris —OH or —OCH.10. The homopolymer of claim 9 , wherein{'sup': 3', '4', '5', '6, 'R, R, Rand Reach is independently —H or a C1-C8 alkyl.'}11. The homopolymer of claim 7 , wherein:{'sub': 1', '3', '4', '5', '6', '2', '3, 'Ris —OH, R, R, R, and Reach is independently a C5-C8 alkyl, and Ris —OH, or —OCH.'}12. The homopolymer of claim 7 , wherein:{'sub': 1', '3', '4', '5', '6', '3', '2', '3, 'Ris —OH, and R, R, R, and Reach is —CH, and Ris —OH or —OCH.'}13. The homopolymer of claim 7 , wherein:{'sub': 1', '3', '4', '5', '6', '2', '3, 'Ris —OH, and R, R, R, and Reach is —H, and Ris —OH or —OCH.'}16. The copolymer of claim 14 , wherein Ris —OH and Ris —OH or —OCH.17. The copolymer of claim 16 , wherein R claim 16 , R claim 16 , Rand Reach is independently —H or a C1-C8 alkyl.18. The copolymer of claim 14 , wherein:{'sub': 1', '3', '4', '5', '6', '2', '3, 'Ris —OH, R, R, R, and Reach is independently a C5-C8 alkyl, and Ris —OH or —OCH.'}19. The copolymer of claim 14 , wherein:{'sub': 1', '3', ...

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Номер записи: 36
12-03-2020 дата публикации

METHOD FOR MANUFACTURING 1,4-BIS (4-PHENOXYBENZOYL)BENZENE USING SUBSTANTIALLY NON-HYDROLYZED TEREPHTHALOYL CHLORIDE

Номер: US20200079717A1
Автор: JOUANNEAU Julien, Le Guillaume
Принадлежит: Arkema France

A method for manufacturing 1,4-bis(4-phenoxybenzoyl)benzene, including: providing terephthaloyl chloride, diphenyl ether, a solvent and a Lewis acid, wherein the terephthaloyl chloride is of a purity grade such that, 10 minutes after introducing it at a reference concentration of 6.5 wt. % into said solvent, at a temperature of 20° C., a solution is obtained having a turbidity of less than 500 NTU; mixing the terephthaloyl chloride, the diphenyl ether and the solvent so as to make a reactant mixture; adding the Lewis acid to the reactant mixture so as to effect the reaction of the terephthaloyl chloride with the diphenyl ether; recovering a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex. 1. A method for manufacturing 1 ,4-bis(4-phenoxybenzoyl)benzene , comprising:providing terephthaloyl chloride, diphenyl ether, a solvent and a Lewis acid, wherein the terephthaloyl chloride is of a purity grade such that, 10 minutes after introducing it at a reference concentration of 6.5 wt. % into said solvent, at a temperature of 20° C., a solution is obtained having a turbidity of less than 500 NTU;mixing the terephthaloyl chloride, the diphenyl ether and the solvent so as to make a reactant mixture;adding the Lewis acid to the reactant mixture so as to effect the reaction of the terephthaloyl chloride with the diphenyl ether;recovering a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex.2. The method of claim 1 , wherein the terephthaloyl chloride is of a purity grade such that:10 minutes after introducing it at a reference concentration of 6.5 wt. % into said solvent, at a temperature of 20° C., a solution is obtained having a turbidity of less than 200 NTU.3. The method of claim 1 , wherein the terephthaloyl chloride is kept in a sealed container without contact with ambient air prior to making the reactant mixture.4. The method of claim 1 , whereinthe diphenyl ether and solvent, in combination, contain less ...

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Номер записи: 37
30-03-2017 дата публикации

Fluorine-Containing Polymerizable Monomer and Polymer Compound Using Same

Номер: US20170088666A1
Автор: Junya Nakatsuji, Kazuhiro Yamanaka, Makoto Matsuura
Принадлежит: Central Glass Co Ltd

Disclosed in the present invention are a fluorine-containing polymerizable compound of the general formula (1) and a polymer compound obtained therefrom: where A represents a single bond, an oxygen atom, a sulfur atom, SO 2 , CH 2 , CO, C(CH 3 ) 2 , C(CH 3 )(CH 2 CH 3 ), C(CF 3 ) 2 , C(CH 3 )(C 6 H 5 ), CH 2 —C 6 H 4 —CH 2 or a divalent organic group obtained by elimination of two hydrogen atoms from benzene, biphenyl, naphtharene, cyclohexene or fluorene; and a and b each independently represent an integer of 0 to 2 and satisfy a relationship of 1≦a+b≦4. The thus-obtained polymer compound combines adequate hydrophilicity and high transparency with low water adsorption of fluorine-containing compound.

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Номер записи: 38
19-06-2014 дата публикации

NUCLEAR RECEPTOR MODULATORS AND THEIR USE FOR THE TREATMENT AND PREVENTION OF CANCER

Номер: US20140171503A1
Автор: Kim Yeong Sang, Kumar Vineet, Lee Sunmin, Malhotra Sanjay V., Neckers Jane B.
Принадлежит:

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein Rto Rand Xto Xare as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed. 2. The compound claim 1 , salt claim 1 , solvate claim 1 , or stereoisomer of claim 1 , wherein the electron withdrawing group is selected from the group consisting of N claim 1 , CN claim 1 , NO claim 1 , CHO claim 1 , NCS claim 1 , SCN claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , OCF claim 1 , SOH claim 1 , B(OH) claim 1 , PO(OH) claim 1 , PO(OH)(OR″) claim 1 , PO(OR″) claim 1 , SONHOH claim 1 , SONH claim 1 , CONH claim 1 , CONHOH claim 1 , SR″ claim 1 , SOR″ claim 1 , SOR″ claim 1 , SONHR″ claim 1 , SON(R″)R″ claim 1 , SONHCON(R″)R″ claim 1 , COOR″ claim 1 , COR″ claim 1 , CONHR″ claim 1 , CON(R″) R″ claim 1 , CONHSON(R″)R″ claim 1 , NHCOR″ claim 1 , N(R″)COR″ claim 1 , NHSOR″ claim 1 , N(R″)SOR″ claim 1 , NHR″ claim 1 , NHR″ claim 1 , NR″ claim 1 , wherein R″ is H or C-Calkyl claim 1 , and CY claim 1 , wherein Y is F claim 1 , Cl claim 1 , or Br.3. The compound claim 1 , salt claim 1 , solvate claim 1 , or stereoisomer of claim 1 , wherein Xor Xis CF claim 1 , Xor Xis H claim 1 , and Xis selected from the group consisting of H claim 1 , NO claim 1 , CN and CF.47.-. (canceled)8. The compound claim 1 , salt claim 1 , solvate claim 1 , or stereoisomer of claim 1 , wherein Xor Xis NO claim 1 , Xor Xis H claim 1 , and Xis selected from the group consisting of H claim 1 , NO claim 1 , CN and CF.912.-. (canceled)13. The compound claim 1 , salt claim 1 , solvate claim 1 , or stereoisomer of claim 1 , wherein X claim 1 , X claim 1 , X claim 1 , and Xare H claim ...

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Номер записи: 39
19-03-2020 дата публикации

COMPOSITIONS OF POLYHYDROXYLATED BENZOPHENONES AND METHODS OF TREATMENT OF NEURODEGENERATIVE DISORDERS

Номер: US20200087236A9
Автор: Haggarty Stephen J., PAO Ping-Chieh, Patnaik Debasis, Tsai Li-Huei
Принадлежит: The General Hospital Corporation D/B/A Massachusetts General Hospital

The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity. 87. The compound of claim , wherein each of R , R , R , R , Rand Ris CO(C-Calkyl).97. The compound of claim , wherein each of R , R , R , R , Rand Ris CO(Calkyl).12. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.13. A method of treating a disease associated with a deficiency in HDAC1 deacetylase activity comprising administering to a patient in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt or prodrug thereof.14. The method of claim 13 , wherein the compound activates HDAC1 deacetylase activity.15. The method of claim 13 , wherein the compound increases the expression of genes involved in cytokine responses claim 13 , neurogenesis claim 13 , and/or central nervous system development.16. The method of claim 15 , wherein the genes involved in cytokine responses are genes involved in interferon (IFN)-γ and/or IFN-β responses.17. The method of claim 13 , wherein the disease is a neurodegenerative disease claim 13 , neurological disorder claim 13 , psychiatric disorder claim 13 , or cognitive deficit.18. The method of claim 13 , wherein the disease is a dementia or amytrophic lateral sclerosis (ALS).19. The method of claim 18 , wherein the dementia is Alzheimer's disease claim 18 , frontotemporal dementia claim 18 , or Parkinson's disease.20. The method of claim 13 , wherein the disease is major depression claim 13 , bipolar disorder claim 13 , and schizophrenia.21. The method of claim 13 , wherein administering is performed orally claim 13 , parenterally claim 13 , intranasally claim 13 , subcutaneously claim 13 , by injection claim 13 , or by infusion.23. A method of activating HDAC1 activity comprising contacting a cell with a ...

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Номер записи: 40
19-03-2020 дата публикации

METHOD FOR MANUFACTURING 1,4-BIS(4-PHENOXYBENZOYL)BENZENE IN SUPERSATURATION CONDITIONS

Номер: US20200087456A1
Автор: JOUANNEAU Julien, Le Guillaume, VINCENT Guillaume
Принадлежит: Arkema France

The invention relates to a method for manufacturing 1,4-bis(4-phenoxybenzoylbenzene), comprising: 1. A method for manufacturing 1 ,4-bis(4-phenoxybenzoyl)benzene , comprising:providing a reactant mixture comprising terephthaloyl chloride, diphenyl ether and a Lewis acid in a solvent;reacting terephthaloyl chloride with diphenyl ether, so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex;wherein the 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex is dissolved in the solvent at a 1,4-bis(4-phenoxybenzoyl)benzene weight concentration in the solvent which is higher than the saturation limit of the 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex during at least part of the step of reacting terephthaloyl chloride with diphenyl ether.2. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex is dissolved in the solvent at a 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene weight concentration which is higher by at least 5% than the saturation limit of the 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex claim 1 , during part of the step of reacting terephthaloyl chloride with diphenyl ether.3. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex is dissolved in the solvent at a 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene weight concentration of more than 5 wt. % claim 1 , during part of the step of reacting terephthaloyl chloride with diphenyl ether.4. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex is dissolved in the solvent during at least 75% of the duration of the step of reacting terephthaloyl chloride with diphenyl ether.5. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent when an amount of 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene of 75 mol. % claim 1 , relative to the initial amount of terephthaloyl ...

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Номер записи: 41
13-04-2017 дата публикации

UNSATURATED DEOXYBENZOIN COMPOUNDS AND POLYMERS PREPARED THEREFROM

Номер: US20170101361A1
Автор: Choudhary Umesh, Emrick Todd, Mir Aabid A.
Принадлежит:

Deoxybenzoin compounds including unsaturation are disclosed. The unsaturated deoxybenxoin compounds have the structure (I), (II), or (III) 2. The deoxybenzoin compound of claim 1 , wherein each occurrence of Rand Ris hydrogen.3. The deoxybenzoin compound of claim 1 , wherein each occurrence of n is 1.4. The deoxybenzoin compound of claim 1 , wherein each occurrence of R claim 1 , R claim 1 , R claim 1 , and Ris hydrogen.9. The polyester of claim 8 , wherein Aris a phenylene group.10. The polyester of claim 8 , wherein m is 0.12. The polyester of claim 8 , wherein the polyester is a copolyester further comprising repeating units derived from bisphenol A.13. The polyester of claim 8 , wherein the polyester has a number average molecular weight of 1 claim 8 ,000 to 100 claim 8 ,000 Daltons.18. The polyester of claim 8 , wherein the polyester exhibits one or more of the following properties:a five percent weight loss temperature of greater than or equal to 350° C., as determined using thermogravimetric analysis;a char yield of at least 35 percent after 60 minutes at 750° C., as determined by thermogravimetric analysis;a heat release capacity of less than or equal to 150 joules per gram-Kelvin determined using a pyrolysis combustion flow calorimeter; anda total heat release of less than 15 kilojoules per gram determined using a pyrolysis combustion flow calorimeter. This invention was made with government support under grant number 14-G-012 001 awarded by the Federal Aviation Administration. The government has certain rights in the invention.Polymers are a mainstay of modern society, for example, widely used in fabricating textiles, upholstery, construction materials, various air, land or sea vehicles, and microelectronic devices and appliances. The inherent flammability of many polymers poses a significant threat, especially in enclosed or isolated spaces. Therefore, as synthetic polymers are used extensively in society as plastics, rubbers, and textiles, polymer ...

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Номер записи: 42
02-06-2022 дата публикации

Process and System to Make Olefin Epoxides

Номер: US20220169625A1
Автор: Shaffer Timothy D., Wang Kun
Принадлежит:

A method may include: oxidizing iso-butane with oxygen to produce t-butyl hydroperoxide and t-butyl alcohol; dehydrating at least a portion of the t-butyl alcohol to produce di-tert-butyl ether and isobutylene; epoxidizing at least a portion of the isobutylene with the t-butyl hydroperoxide to produce isobutylene oxide and t-butyl alcohol; and carbonylating at least a portion of the isobutylene oxide with carbon monoxide to produce pivalolactone. 1. A method comprising:introducing a branched alkane stream into an oxidation unit, the branched alkane stream comprising a branched alkane;oxidizing at least a portion of the branched alkane and generating at least an oxidized stream from the oxidation unit, the oxidized stream comprising an organic hydroperoxide and a branched alcohol;introducing at least a portion of the oxidized stream and a branched alkene stream into an epoxidation unit, the branched alkene stream comprising a branched alkene;epoxidizing at least a portion of the branched alkene with the organic hydroperoxide and generating a mixed intermediate product stream comprising a substituted olefin epoxide and additional branched alcohol;dehydrating at least a portion of the branched alcohol and generating at least a branched ether stream comprising a branched ether;introducing at least a portion of the mixed intermediate product stream, a carbon monoxide stream, and the branched ether stream into a carbonylation unit, the carbon monoxide stream comprising carbon monoxide and the branched ether stream comprising a branched ether; andcarbonylating at least a portion of the substituted olefin epoxide with the carbon monoxide and generating a product stream comprising a substituted lactone.4. The method of further comprising introducing an oxygen stream comprising oxygen into the oxidation unit claim 1 , wherein the step of oxidation comprises autocatalytic oxidation.5. The method of wherein the oxidized stream further comprises unreacted branched alkane claim 1 ...

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Номер записи: 43
03-07-2014 дата публикации

NEUROPROTECTIVE POLYPHENOL ANALOGS

Номер: US20140186328A1
Автор: Chiruta Chandramouli, Maher Pamela A., Schubert David R.
Принадлежит: SALK INSTITUTE FOR BIOLOGICAL STUDIES

The present invention provides neuroprotective polyphenol compounds, which can be synthetic analogs of fisetin, baicalein or chlorogenic acid, that maintain neuroprotective, anti-inflammatory, glutathione promoting, and/or antioxidant properties. The neuroprotective polyphenol compounds are useful for promoting, enhancing and/or increasing neuron protection, growth and/or regeneration. The polyphenol compounds further find use for increasing and or maintaining intracellular glutathione (GSH) levels. The polyphenol compounds are also useful for treating, preventing, mitigating and/or delaying neurodegenerative conditions, including diabetes, Parkinson's disease, Huntington's disease, Alzheimer's disease, non-Alzheimer's dementias, multiple sclerosis, traumatic brain injury, spinal cord injury or ALS. 3. The compound of claim 2 , wherein:{'sup': 1', '2', 'a', '3', '4, 'sub': 1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(a) the compound is of Formula II, and wherein each of Rand R, independent of the other, is —OR; Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', 'a', '3', 'a, 'sub': '1-6', '(b) the compound is of Formula IIIA, and wherein each of Rand R, independent of the other, is —OR; Ris H, Calkyl or —OR;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', '4, 'sub': 1-6', '2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(c) the compound is Formula IIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', 'a, 'sub': 1-6', '2', '1-6, '(d) the compound is of Formula IIIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); and Ris H, Calkyl or —OR;'}{'sup': 1', '2', 'a', '1', '2', 'c', '1', '2', '3', '4, 'sub': 2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, ...

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Номер записи: 44
03-07-2014 дата публикации

POLYPHENOL ANALOGS TO TREAT ISCHEMIA

Номер: US20140186329A1
Автор: Chiruta Chandramouli, Lapchak Paul A., Maher Pamela A., Schubert David R.
Принадлежит:

The present invention provides methods of use of polyphenol compounds for treating, preventing, mitigating and delaying ischemia or a condition where ischemia occurs. In one embodiment, the method comprises providing a polyphenol analog; and administering the polyphenol analog to a subject to treat ischemia or a condition where ischemia occurs. Various embodiments of the present invention are useful for the treatment of patients having, or at risk for, any of (1) ischemic stroke, (2) hemorrhagic stroke, (3) cardiovascular disease, (4) ischemia related spinal cord injury, (5) ischemia in diabetic patients, or (6) embolic stroke. For example, use of the polyphenol compounds can maintain glutathione levels in the patient. 3. The method of claim 2 , wherein:{'sup': 1', '2', 'a', '3', '4, 'sub': 1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(a) the compound is of Formula IIA, and wherein each of Rand R, independent of the other, is —OR; Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', 'a', '3', 'a, 'sub': '1-6', '(b) the compound is of Formula IIIA, and wherein each of Rand R, independent of the other, is —OR; Ris H, Calkyl or —OR;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', '4, 'sub': 1-6', '2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(c) the compound is of Formula IIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', 'a, 'sub': 1-6', '2', '1-6, '(d) the compound is of Formula IIIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); and Ris H, Calkyl or —OR;'}{'sup': 1', '2', 'a', '1', '2', 'c', '1', '2', '3', '4, 'sub': 2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(e) the compound is of Formula IIA, and wherein one of Rand Ris H or —ORand ...

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Номер записи: 45
10-07-2014 дата публикации

COMPOSITION FOR TREATING ATHEROSCLEROSIS AND A PREPARATION METHOD THEREOF

Номер: US20140194474A1
Автор: CHANG FANG-RONG, DU YING-CHI, HSIEH TUSTY-JIUAN, JUO SUH-HANG, LIN AN-SHEN, WU YANG-CHANG
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4′-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPARγ inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPARγ ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1β (IL-1β) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL). 2. The method according to being effective in regulating a pathway by one of inhibiting a p44/42 mitogen-activated protein kinase (MAPK) phosphorylation and activating a peroxisome proliferator activated receptor gamma (PPARγ).3. The method according to claim 2 , wherein the p44/42 MAPK phosphorylation is effective in promoting an expression of at least one of an interleukin-6 (IL-6) and an interleukin-1beta (IL-1β).4. The method according to claim 2 , wherein the PPARγ is effective in inhibiting an expression of at least one of an interleukin-6 (IL-6) and an interleukin-1beta (IL-1β).5. The method according to claim 2 , wherein the PPARγ is effective in inhibiting an expression of at least one of a cyclin D1 and a cyclin D3.7. The method according to claim 6 , wherein the PPARγ is translated from a messenger RNA claim 6 , and the method is effective in increasing an expression of the messenger RNA.10. The method according to claim 9 , wherein the inflammation is a symptom of an atherosclerosis. This application is a divisional application of U.S. patent application Ser. No. 13/570,963 filed Aug. 9, 2012, which claims the benefit of Taiwan Patent Application No. 100128614, filed on Aug. 10, 2011, in the Taiwan Intellectual Property Office, the disclosures of which are incorporated herein in ...

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Номер записи: 46
10-07-2014 дата публикации

USAGE OF NATURAL COMPOUND FOR TREATING INFLAMMATION AND CANCER

Номер: US20140194529A1
Автор: BIAN Zhaoxiang, CHAN Albert Sun Chi, CHEN Kaixian, Chen Shilin, LIN Chengyuan, LU Aiping, XU Hongxi, YANG Dajian, Zhang Dandan, ZHANG Hong
Принадлежит: HONG KONG BAPTIST UNIVERSITY

This invention relates to the use of a compound from natural sources for therapeutic uses. More particularly, it relates to a compound, Garcimultiflorone E, naturally occurring in the plant of Y. H. Li which has potent anti-inflammation and anti-cancer effect. 2. The composition according to wherein said compound comprising Garcimultiflorone E.3. The composition according to wherein said compound is extracted from a natural plant.4Garcinia.. The composition according to wherein the natural plant is from a genus5GarciniaGarcinia esculenta. The composition according to wherein the genus comprising a subspecies of Y. H. Li.6. The composition according to wherein the cancer comprising breast cancer and liver cancer.8. The composition according to wherein said compound comprising Garcimultiflorone E.9. The composition according to wherein said compound is extracted from a natural plant.10Garcinia.. The composition according to wherein the natural plant is from a genus11GarciniaGarcinia esculenta. The composition according to wherein the genus comprising a subspecies of Y. H. Li.12. A use of the composition according to for manufacture of a medicament for treatment of cancer.13. A use of the composition according to for manufacture of a medicament for treatment of inflammation.14. A method of treating cancer comprising administering a composition of claim 1 , wherein the cancer comprising breast or liver cancer.15. A method of treating inflammation comprising administering a composition of .16. The method according to wherein the effective amount is about 10 μM.17. The method according to wherein the effective amount is about 10 μM. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/750,887 filed on 10 Jan. 2013, disclosure of which is incorporated herein by reference in its entirety.This invention is in the field of pharmaceuticals and chemical industries. In particular, this invention relates to the use of a compound from natural ...

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Номер записи: 47
09-04-2020 дата публикации

DISSOCIATION OF A 1,4-BIS (4-PHENOXYBENZOYL)BENZENE- LEWIS ACID COMPLEX IN AN AQUEOUS SOLUTION

Номер: US20200109100A1
Автор: JOUANNEAU Julien, Le Guillaume
Принадлежит: Arkema France

A method for manufacturing 1,4-bis(4-phenoxybenzoyl)benzene, including: reacting terephthaloyl chloride with diphenyl ether in a reaction solvent and in the presence of a Lewis acid, so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex; putting the product mixture in contact with an aqueous solution, so as to obtain an aqueous phase containing the Lewis acid and an organic phase containing 1,4-bis(4-phenoxybenzoyl)benzene. 1. A method for manufacturing 1 ,4-bis(4-phenoxybenzoyl)benzene , comprising:reacting terephthaloyl chloride with diphenyl ether in a reaction solvent and in the presence of a Lewis acid, so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex; andputting the product mixture in contact with an aqueous solution, so as to obtain an aqueous phase containing the Lewis acid and an organic phase containing 1,4-bis(4-phenoxybenzoyl)benzene.2. The method of claim 1 , wherein the aqueous solution has a pH of not more than 5.3. The method of claim 1 , wherein the product mixture is poured into a vessel containing the aqueous solution.4. The method of claim 1 , further comprising:separating the aqueous phase from the organic phase; and/orheating the organic phase up to a maximum temperature, followed by cooling the organic phase down to a separation temperature.5. The method of claim 4 , wherein from 30 to 99.9 wt. of the 1 claim 4 ,4-bis(4-phenoxybenzoyl)benzene contained in the organic phase is dissolved in the organic phase at the maximum temperature.6. The method of claim 4 , wherein the maximum temperature is from 90 to 150° C.7. The method of claim 4 , wherein the separation temperature is at least 20° C.8. The method of claim 4 , wherein the organic phase is cooled down at a rate of from 10 to 50° C./h.9. The method of claim 1 , wherein at least the organic phase is subjected to a solid/liquid separation step claim 1 , so as to recover solid 1 claim 1 ,4-bis(4- ...

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Номер записи: 48
17-07-2014 дата публикации

FLUOROALKYL AND CHLOROFLUOROALKYL BENZENES

Номер: US20140200372A1
Автор: Petrov Viacheslav A.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

This invention relates to fluoroalkyl and chlorofluoroalkyl benzenes with relatively high boiling points, having zero ozone depletion potential and low global warming potential. This invention also relates to the preparation of such fluoroalkyl and chlorofluoroalkyl benzenes. These materials can be used as reaction and heat transfer media, cleaning agents and as intermediates for biologically active materials. 6. The process of wherein the Lewis acid is aluminum chlorofluoride. This invention relates to fluoroalkyl and chlorofluoroalkyl benzenes with relatively high boiling points, having zero ozone depletion potential and low global warming potential. This invention also relates to the preparation of such fluoroalkyl and chlorofluoroalkyl benzenes. The materials can be used as reaction and heat transfer media, cleaning agents and as intermediates for biologically active materials.The reaction of octafluorotoluene with hexafluoropropene is known to make the perfluorinated iso-butylbenzene as shown below:from “Syntesy Ftororganicheskich Soedinenii. Monomery I promezhutochnye porukty. Eds. I.Knunyants and G. Yakobson, Khimiay, Moskve, USSR, 1977, p. 141.One aspect of this invention is a process comprising reacting benzotrifluorides of Formula 1wherein X and Y are independently F, CI, Br, I, R, or OR; with a fluoro-olefin selected from the group consisting of tetrafluoroethylene (TFE), CFH═CF, CFCl═CFCl, CFCl═CF, CH═CF, and CF═CFCF, in the presence of strong Lewis acid selected from the group consisting of antimony pentafluoride (SbF) and aluminum chlorofluoride (AlClF), where x+y=3. As an illustration, when the fluoro-olefin is tetrafluoroethylene, the product comprises a fluoroalkylbenzene of Formula 2, where Ris —CFCFCFor —CF(CF)Another aspect of this invention is a composition comprising a fluoroalkylbenzene of Formula 2.Another aspect of this invention is a process comprising reacting a benzotrifluoride of Formula 3 with a fluoro-olefin selected from the group ...

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Номер записи: 49
13-05-2021 дата публикации

DISPLAY DEVICE

Номер: US20210143360A1
Автор: JEONG Eun Jae, KIM Su Jeong, KIM Yi Su, LEE Jin Hyeong, LEE Mi Hwa, SHIM Yi Seop
Принадлежит:

A display device includes: a base substrate; a light emitting element on the base substrate; a thin film encapsulation layer on the light emitting element to encapsulate the light emitting element; a touch member on the thin film encapsulation layer; a color filter layer on the touch member; and a planarization layer on the color filter layer to cover the color filter layer, wherein the planarization layer includes a light absorber represented by Formula 1: 6. The display device of claim 1 ,wherein the display device has an absorbance of 0.7 or more in a wavelength band of 380 nm to 410 nm.8. The display device of claim 1 ,wherein the light absorber is further in the color filter layer.9. The display device of claim 8 ,wherein the color filter layer is provided for each pixel,the color filter layer comprises a plurality of color filters and the plurality of color filters are spaced apart from each other at a boundary between adjacent pixels, anda light blocking layer is on the touch member at the boundary between adjacent pixels.10. The display device of claim 1 ,wherein the touch member comprises a first touch conductive layer, a first touch insulating layer on the first touch conductive layer, a second touch conductive layer on the first touch insulating layer, and a second touch insulating layer on the second touch conductive layer; andthe light absorber is further in the first touch insulating layer and/or the second touch insulating layer.11. The display device of claim 10 ,wherein the first touch conductive layer is directly on the thin film encapsulation layer.12. A display device claim 10 , comprising:a base substrate;a light emitting element on the base substrate;a thin film encapsulation layer on the light emitting element to encapsulate the light emitting element;a touch member on the thin film encapsulation layer;a color filter layer on the touch member; anda planarization layer on the color filter layer to cover the color filter layer,wherein the ...

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Номер записи: 50
04-05-2017 дата публикации

BULKY LIGANDS AND METAL COMPOUNDS COMPRISING BULKY LIGANDS

Номер: US20170121263A1
Автор: Marshak Michael Pesek
Принадлежит:

This disclosure provides, molecular metal catalysts supported by sterically bulky β-diketonate (acac) ligands. Disclosed herein are bulky β-diketonate ligands, methods of making bulky β-diketonate ligands, and methods of making metal catalysts supported by sterically bulky β-diketonate (acac) ligands. 4. The compound of claim 1 , having each of the groups X and Y bonded to a single metal atom;wherein said single metal atom is chosen from Li, Na, K, Rb, Cs, Be, Mg, Ca, Sr, Ba, Sc, Y, La, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Zr, Nb, Mo, Ru, Rh, Pd, Ag, Cd, Hf, Ta, W, Re, Os, Ir, Pt, Au, Al, Ga, In, TI, Ge, Sn, Pb, P, As, Sb, and Bi.5. The compound of claim 2 , having each of the groups X and Y bonded to a single metal atom;wherein said single metal atom is chosen from Li, Na, K, Rb, Cs, Be, Mg, Ca, Sr, Ba, Sc, Y, La, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Zr, Nb, Mo, Ru, Rh, Pd, Ag, Cd, Hf, Ta, W, Re, Os, Ir, Pt, Au, Al, Ga, In, TI, Ge, Sn, Pb, P, As, Sb, and Bi.6. The compound of claim 3 , having each of the groups X and Y bonded to a single metal atom; wherein said single metal atom is chosen from Li claim 3 , Na claim 3 , K claim 3 , Rb claim 3 , Cs claim 3 , Be claim 3 , Mg claim 3 , Ca claim 3 , Sr claim 3 , Ba claim 3 , Sc claim 3 , Y claim 3 , La claim 3 , Ti claim 3 , V claim 3 , Cr claim 3 , Mn claim 3 , Fe claim 3 , Co claim 3 , Ni claim 3 , Cu claim 3 , Zn claim 3 , Zr claim 3 , Nb claim 3 , Mo claim 3 , Ru claim 3 , Rh claim 3 , Pd claim 3 , Ag claim 3 , Cd claim 3 , Hf claim 3 , Ta claim 3 , W claim 3 , Re claim 3 , Os claim 3 , Ir claim 3 , Pt claim 3 , Au claim 3 , Al claim 3 , Ga claim 3 , In claim 3 , TI claim 3 , Ge claim 3 , Sn claim 3 , Pb claim 3 , P claim 3 , As claim 3 , Sb claim 3 , and Bi. This disclosure relates to sterically bulky ligands for use in making metal catalysts and metal catalysts including sterically bulky ligands.Reactive molecular metal catalysts are an important class of molecules because they permit chemical transformations not ...

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Номер записи: 51
16-04-2020 дата публикации

Polybrominated diphenyl-based flame retardant compounds

Номер: US20200115308A1
Автор: Brandon M. Kobilka, Jason T. Wertz, Joseph Kuczynski, Scott B. King
Принадлежит: International Business Machines Corp

A process of forming a flame retardant material is disclosed. The process includes forming a functionalized polybrominated diphenyl-based flame retardant compound having the following structural formula: In the structural formula, X corresponds to a functional group. The process also includes forming a flame retardant material by covalently bonding the functionalized polybrominated diphenyl-based flame retardant compound into a material using the functional group.

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Номер записи: 52
27-05-2021 дата публикации

PURIFICATION OF 1,4-BIS (4-PHENOXYBENZOYL)BENZENE BY CENTRIFUGAL FILTRATION

Номер: US20210155571A1
Автор: AMSTUTZ Jérome, JOUANNEAU Julien, Le Guillaume
Принадлежит: Arkema France

A method for manufacturing 1,4-bis(4-phenoxybenzoyl)benzene, including: reacting terephthaloyl chloride with diphenyl ether in a reaction solvent and in the presence of a Lewis acid, so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex; putting the product mixture in contact with a protic solvent, so as to obtain a first phase containing the Lewis acid and a second phase containing 1,4-bis(4-phenoxybenzoyl)benzene; subjecting at least the second phase to a solid/liquid separation step by centrifugal filtration, so as to recover solid 1,4-bis(4-phenoxybenzoyl)benzene. 1. A method for manufacturing 1 ,4-bis(4-phenoxybenzoyl)benzene , comprising:reacting terephthaloyl chloride with diphenyl ether in a reaction solvent and in the presence of a Lewis acid, so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex;putting the product mixture in contact with a protic solvent, so as to obtain a phase containing 1,4-bis(4-phenoxybenzoyl)benzene;subjecting the phase containing 1,4-bis(4-phenoxybenzoyl)benzene to a solid/liquid separation step by centrifugal filtration, so as to recover solid 1,4-bis(4-phenoxybenzoyl)benzene.2. The method of claim 1 , comprising one or more steps of washing the recovered solid 1 claim 1 ,4-bis(4-phenoxybenzoyl)benzene in a protic solvent claim 1 , and subjecting it to a further solid/liquid separation.3. The method of claim 2 , wherein at least one of the steps of washing the solid 1 claim 2 ,4-bis(4-phenoxybenzoyl)benzene is performed at a temperature of at least 20° C.4. The method of claim 2 , wherein each step of washing the recovered the solid 1 claim 2 ,4-bis(4-phenoxybenzoyl)benzene is performed in a centrifugal filtration device.5. The method of claim 1 , further comprising:heating the phase containing 1,4-bis(4-phenoxybenzoyl)benzene up to a maximum temperature, followed by cooling the phase down to a separation temperature, before subjecting the ...

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Номер записи: 53
07-08-2014 дата публикации

4-Acylaralkylphenols and Derivatives Thereof

Номер: US20140221680A1
Автор: Ojiri Akihiko, Tanba Kouichi, Tsujigami Takafumi
Принадлежит: HONSHU CHEMICAL INDUSTRY CO., LTD.

4-Aralkylphenols and derivatives thereof expressed by general formulas (6) and (7) are useful for producing trisphenols. This application is a divisional of U.S. patent application Ser. No. 13/321,535, filed Jan. 13, 2012, and claims the benefits thereof under U.S.C. §121 or §365(c), which is the U.S. National Phase under 35 U.S.C. §371 of International Application PCT/JP2010/058476, filed May 19, 2010, which claims priority to Japanese Patent Application Nos. 2009-121169, filed May 19, 2009 and 2009-121170, filed May 19, 2009, each disclosure of which is herein incorporated by reference in its entirety. The International Application was published under PCT Article 21(2) in the language other than English.1. Field of the InventionThe present invention relates to a method for producing with ease at high yield and high purity in industrial settings trisphenols, which are useful as materials for polymer compounds such as epoxy resins, polycarbonate resins or the like or as materials or additives for photoresists. It also relates to a new 4-acylaralkylphenol derivative having a bisphenyl molecular skeleton with the acyl group in one phenyl ring and the hydroxyl group or acyloxy group in the other phenyl ring. Such compound is useful as various reactive materials having the effect of improving heat resistance, etc., especially as intermediate materials for generating trisphenols used as materials for polymer compounds such as polycarbonate resins or the like or as materials for photoresists, etc., through reaction with phenols.2. Description of the Related ArtAmong trisphenols, especially trisphenols other than of the trisphenol methane type, 1-[1,1-bis(4-hydroxyphenyl)ethyl]-4-[1-methyl-1-(4-hydroxyphenyl)ethyl]benzene is known. These trisphenols are favorably used as materials for polymer compounds such as epoxy resins, polycarbonate resins or the like or as materials or additives for photoresists, etc. These trisphenols are known to be obtained by reacting ...

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Номер записи: 54
09-05-2019 дата публикации

METHOD FOR MANUFACTURING 1,4-BIS (4-PHENOXYBENZOYL)BENZENE IN SUPERSATURATION CONDITIONS

Номер: US20190135721A1
Автор: JOUANNEAU Julien, Le Guillaume, VINCENT Guillaume
Принадлежит: Arkema France

A method for manufacturing 1,4-bis(4-phenoxybenzoylbenzene), including: providing a reactant mixture including terephthaloyl chloride, diphenyl ether and a Lewis acid in a solvent; reacting terephthaloyl chloride with diphenyl ether, so as to obtain a product mixture including a 1,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex; wherein the 1,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent at a 1,4-bis(4-phenoxybenzoylbenzene) weight concentration in the solvent which is higher than the saturation limit of the 1,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex during at least part of the step of reacting terephthaloyl chloride with diphenyl ether. 2. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent at a 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene) weight concentration which is higher by at least 5% than the saturation limit of the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex claim 1 , during part of the step of reacting terephthaloyl chloride with diphenyl ether.3. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent at a 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene) weight concentration of more than 5 wt. % during part of the step of reacting terephthaloyl chloride with diphenyl ether.4. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent during at least 75% of the duration of the step of reacting terephthaloyl chloride with diphenyl ether.5. The method of claim 1 , wherein the 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene)-Lewis acid complex is dissolved in the solvent when an amount of 1 claim 1 ,4-bis(4-phenoxybenzoylbenzene) of 75 mol. % claim 1 , relative to the initial amount of terephthaloyl chloride claim 1 , is present in the reactant mixture.6. The method of claim 1 , wherein the step of reacting ...

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Номер записи: 55
28-05-2015 дата публикации

NOVEL PHENYL GLYOXAL PROBES

Номер: US20150148259A1
Автор: Bicker Kevin L., Subramanian Venkataraman, Thompson Paul R.
Принадлежит:

Novel phenyl-glyoxal based anti-citrulline probes and methods of synthesis are provided. Methods of use, such as, the development of methods for monitoring substrate citrullination over time; for identifying citrullinated proteins from cells are described. 1. A phenylglyoxal derivative comprising: an isotopically labeled , fluorophore labeled , or biotin labeled phenylglyoxal (biotin-PG).3. The phenylglyoxal derivative of claim 1 , wherein the fluorophore labeled phenylglyoxal comprises: rhodamine labeled phenylglyoxal (Rh-PG) or fluorescein labeled phenylglyoxal.4. The phenylglyoxal derivative of claim 1 , wherein the labeled phenylglyoxal is biotin labeled phenylglyoxal (biotin-PG).8. The method of or claim 1 , wherein the compounds having the general structures of compounds 5 and 10 are reacted with an alkyne comprising a reporter moiety.9. The method of claim 5 , wherein the reporter moiety comprises: fluorophores claim 5 , isotopes claim 5 , biotin claim 5 , or rhodamine.10. The method of claim 5 , wherein the phenylglyoxal is linked to the reporter moiety via the meta position.11. A method of labeling citrullinated proteins protein or fragments thereof in a biological sample claim 5 , comprising:contacting a biological sample with an effective amount of a phenylglyoxal probe, wherein the probe is detectably labeled and the detectably labeled phenylglyoxal probe is covalently bonded to a citrullinated protein or fragments thereof in the biological sample; thereby,labeling the citrullinated protein or fragments thereof in the biological sample.13. The method of claim 12 , wherein the detectable label comprises: fluorophores claim 12 , chromophores claim 12 , isotopes claim 12 , chemiluminescent molecules claim 12 , fluorescent molecules claim 12 , enzymes or coenzymes.14. The method of claim 12 , wherein the fluorophore comprises: rhodamine or fluorescein.15. The method of claim 12 , wherein the co-enzyme is biotin.16. The method of claim 11 , wherein the step ...

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Номер записи: 56
28-05-2015 дата публикации

NOVEL POLYMERIC PHOTOINITIATORS AND PHOTOINITIATOR MONOMERS

Номер: US20150148441A1
Автор: Anderson David George, Madsen Niels Joergen, Nielsen Bo Rud, Sehnal Petr
Принадлежит:

The present invention provides polymeric photoinitiators being co-polymers of photoinitiator monomers and at least one further monomer, as well as photoinitiator monomers being intermediates in the preparation of such polymeric photoinitiators. Additionally, there is provided polyacrylate obtained by radical polymerization of at least one acrylate monomer (Ac) in the presence of such polymeric photoinitiators. In the photoinitiator monomers and polymeric photoinitiators, a photoinitiator moiety, a hydrolytic stable linker and two polymerisable functional groups are incorporated into the photoinitiator structure. 167.-. (canceled)69. The polymeric photoinitiator according to claim 68 , wherein Z is selected from a C-Calkylene claim 68 , a C-Calkenylene claim 68 , a C-Ccycloalkyl claim 68 , an aryl claim 68 , a heterocyclyl claim 68 , a —[O—(C-Calkylene)]- claim 68 , a —[S—(C-Calkylene)]- claim 68 , a —[(C-Calkylene)-O]— claim 68 , a —[(C-Calkylene)-S-]- claim 68 , a —[O—(C-Calkylene)]-O— claim 68 , a —[S—(C-Calkylene)]-S— claim 68 , a —C(═O)— claim 68 , a —[C(═O)—(C-Calkylene)]- claim 68 , a —[C(═O)-aryl]- claim 68 , and a —[C(═O)-heterocyclyl]- claim 68 , where any of these moieties independently is optionally substituted with one or more substituents.70. The polymeric photoinitiator according to claim 68 , wherein n is 1.71. The polymeric photoinitiator according to claim 68 , wherein n is 2.72. The polymeric photoinitiator according to claim 68 , wherein Ris selected from H claim 68 , a C-Calkyl claim 68 , a C-Calkenyl claim 68 , a —[O—(C-Calkylene)]-H claim 68 , a —[S—(C-Calkylene)]-H claim 68 , a —C(═O)—H claim 68 , and a —[C(═O)—(C-Calkylene)]-H claim 68 , where any alkyl claim 68 , alkylene claim 68 , or alkenyl moiety independently is optionally substituted with one or more substituents.73. The polymeric photoinitiator according to claim 68 , wherein Xand Xeach independently are selected from a C-Calkylene claim 68 , a C-Calkenylene claim 68 , a —[O—(C- ...

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Номер записи: 57
10-06-2021 дата публикации

METHOD FOR PRODUCING KETENE DERIVATIVE

Номер: US20210171428A1
Автор: Okuyama Naoto, SASAKI Yukihiro, TSUGITA Nobuhiro
Принадлежит: Daicel Corporation

An object is to provide a method for producing a ketene derivative that decreases the consumption quantity of phosphorus compounds, and the discharge quantity of the phosphorus compounds into the environment. 1. A method for producing a ketene derivative , comprising:a step (i) of conducting thermal decomposition reaction of acetic acid in a presence of a phosphorus-containing catalyst in a reactor to produce a thermal decomposition gas containing ketene,a step (ii) of cooling the thermal decomposition gas to be separated into a gaseous component containing ketene, and a condensed liquid containing a phosphorus compound (a), anda step (iii) of causing the ketene to react with a different organic compound to produce a ketene derivative,wherein the step (i) includes: conducting the thermal decomposition reaction while supplying, into the reactor, the condensed liquid containing the phosphorus compound (a) or a concentrated liquid of the condensed liquid.2. The method for producing a ketene derivative according to claim 1 , wherein in the step (i) claim 1 , by concentrating the phosphorus compound (a) contained in the condensed liquid claim 1 , the condensed liquid is turned to the concentrated liquid claim 1 , and subsequently the concentrated liquid is supplied into the reactor.3. The method for producing a ketene derivative according to claim 2 , wherein a concentration of the phosphorus compound (a) contained in the concentrated liquid is from 5 to 20 times a concentration of the phosphorus compound (a) contained in the condensed liquid.4. The method for producing a ketene derivative according to claim 2 , wherein a method for concentrating the phosphorus compound (a) contained in the condensed liquid is a method selected from the group consisting of heating evaporation claim 2 , membrane separation claim 2 , and electrochemical treatment.5. The method for producing a ketene derivative according to claim 2 , wherein in the step (i) claim 2 , a liquid obtained by ...

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Номер записи: 58
10-06-2021 дата публикации

COMPOSITIONS OF POLYHYDROXYLATED BENZOPHENONES AND METHODS OF TREATMENT OF NEURODEGENERATIVE DISORDERS

Номер: US20210171429A1
Автор: Haggarty Stephen J., PAO Ping-Chieh, Patnaik Debasis, Tsai Li-Huei
Принадлежит:

The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity. 8. The prodrug of claim 7 , or a pharmaceutically acceptable salt claim 7 , hydrate claim 7 , solvate claim 7 , or tautomer thereof claim 7 , wherein each of R claim 7 , R claim 7 , R claim 7 , R claim 7 , Rand Ris CO(C-Calkyl).910-. (canceled)12. A pharmaceutical composition comprising the prodrug of claim 1 , or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or tautomer thereof claim 1 , and a pharmaceutically acceptable carrier.13. A method of treating a disease associated with a deficiency in HDAC1 deacetylase activity comprising administering to a patient in need thereof an effective amount of a prodrug of claim 1 , or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or tautomer thereof.14. The method of claim 13 , wherein the compound activates HDAC deacetylase activity.15. The method of claim 13 , wherein the compound increases the expression of genes involved in cytokine responses claim 13 , neurogenesis claim 13 , and/or central nervous system development.16. The method of claim 15 , wherein the genes involved in cytokine responses are genes involved in interferon (IFN)-y and/or IFN-β responses.17. The method of claim 13 , wherein the disease is a neurodegenerative disease claim 13 , neurological disorder claim 13 , psychiatric disorder claim 13 , or cognitive deficit.18. The method of claim 13 , wherein the disease is a dementia or amyotrophic lateral sclerosis (ALS).19. The method of claim 18 , wherein the dementia is Alzheimer's disease claim 18 , frontotemporal dementia claim 18 , or Parkinson's disease.20. The method of claim 13 , wherein the disease is major depression claim 13 , bipolar disorder claim 13 , and schizophrenia.21. The method ...

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Номер записи: 59
21-08-2014 дата публикации

COMPOUNDS AND METHODS FOR PREPARATION OF DIARYLPROPANES

Номер: US20140235899A1
Автор: Nandy Sandip K., Padmapriya Abeysinghe Arrachchigae
Принадлежит: Unigen, Inc.

Compounds of structure (I): 3. The compound of claim 2 , wherein each of Rand Rare alkyl.5. The compound of claim 2 , wherein each of Rand Rare aralkyl.7. The compound of claim 2 , wherein each of Rand Rare alkyl.11. The compound of claim 10 , wherein each of Rand Rare alkyl.13. The compound of claim 10 , wherein each of Rand Rare aralkyl.15. The compound of claim 10 , wherein each of Rand Rare alkyl.18. The compound of claim 1 , wherein at least one of Ror Ris allyl.19. The compound of claim 18 , wherein each of Rand Rare allyl.20. The compound of claim 18 , wherein at least one of Ror Ris methyl.2159.-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/425,959, filed Mar. 21, 2012, now allowed, which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 61/467,286 filed Mar. 24, 2011, which applications are incorporated herein by reference in their entirety.1. Technical FieldThe present invention is generally directed to compounds useful for the preparation of diarylpropanes and methods related to the same.2. Description of the Related ArtThere is great demand for products able to inhibit or prevent excessive pigmentation of the skin. Melanin, the skin's natural pigment, is a nitrogenous polymer synthesized in melanosomes, which are membrane-bound organelle present within melanocytes. Melanin is produced in varying concentrations, depending on skin type (genetic disposition) and environmental conditions. Melanocytes are cells that occur in the basal membrane of the epidermis, and account for between 5% and 10% of the cellular content (approximately 1200-1500 melanocytes/cm). When stimulated, by factors such as ultraviolet (UV) light, melanocytes divide more rapidly and produce greater quantities of melanin. The melanin is then transported in mature melanosomes to keratinocytes within the epidermis where it becomes visible as a brown skin color.The over production of melanin can cause different ...

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Номер записи: 60
09-06-2016 дата публикации

TARGETED, METAL-CATALYZED FLUORINATION OF COMPLEX COMPOUNDS WITH FLUORIDE ION VIA DECARBOXYLATION

Номер: US20160158388A1
Автор: Groves John T., Huang Xiongyi
Принадлежит: THE TRUSTEES OF PRINCETON UNIVERSITY

Methods of preparing fluorinated compounds by carboxylative fluorination using fluoride are contained herein. Fluorinated compounds are provided. Methods of using fluorinated compounds are contained herein. 1. A method of targeted fluorination comprising combining a mono-fluoro-aryl iodine-(III) carboxylate and a manganese catalyst.2. The method of claim 1 , wherein the manganese catalyst is a manganese porphyrin or a manganese salen.3. The method of further comprising mixing a compound containing a carboxyl group claim 1 , a nucleophilic fluoride source claim 1 , a solvent and an iodine (III) oxidant to form the mono-fluoro-aryl iodine-(III) carboxylate prior to the step of combining.4. The method of further comprising maintaining the mono-fluoro-aryl iodine-(III) carboxylate at a temperature from 25° C. to 80° C.5. The method of claim 3 , wherein the nucleophilic fluoride source is trialkyl amine trihydrofluoride.6. The method of claim 5 , wherein the trialkyl amine trihydrofluoride is triethylamine trihydrofluoride.7. The method of claim 1 , wherein the step of combining is performed under an inert atmosphere.8. The method of claim 3 , wherein the nucleophilic fluoride source is [F]-fluoride.9. The method of claim 3 , wherein prior to the step of mixing claim 3 , the method comprises obtaining an aqueous [F] fluoride solution from a cyclotron claim 3 , loading the aqueous [F] fluoride solution onto an ion exchange cartridge and releasing the [F] fluoride from the ion exchange cartridge with an alkaline solution.10. A method of targeted fluorination of a compound containing a carboxyl group claim 3 , the method comprising combining the compound claim 3 , a nucleophilic fluoride source claim 3 , a manganese catalyst claim 3 , a solvent and an iodine(III) oxidant.11. The method of claim 10 , wherein the manganese catalyst is a manganese porphyrin or a manganese salen.12. The method of claim 10 , wherein the nucleophilic fluoride source is trialkyl amine ...

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Номер записи: 61
18-06-2015 дата публикации

FLUORINE-CONTAINING COMPOUND, SUBSTRATE FOR PATTERN FORMATION, PHOTODEGRADABLE COUPLING AGENT, PATTERN FORMATION METHOD, AND COMPOUND

Номер: US20150168836A1
Автор: Yamaguchi Kazuo
Принадлежит:

A fluorine-containing compound represented by a following general formula (1) is provided. [In the general formula (1), X represents a halogen atom or an alkoxy group, Rrepresents a branched chain or cyclic alkyl group having 3 to 10 carbon atoms, and Rand Rrepresent fluorinated alkoxy groups. n represents an integer of 0 or greater. ] 2. The fluorine-containing compound according to claim 1 , wherein Rrepresents an isopropyl group claim 1 , an isobutyl group claim 1 , or a tert-butyl group.3. The fluorine-containing compound according to claim 1 , wherein Ror Rrepresent fluorinated alkoxy groups having 5 or more carbon atoms.4. A substrate for pattern formation having a surface chemically modified with the fluorine-containing compound according to .5. A photodegradable coupling agent formed of the fluorine-containing compound according to .6. A pattern formation method for forming a pattern on a work surface of an object claim 1 , the pattern formation method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying the work surface using the fluorine-containing compound according to ;'}generating a latent image formed of a hydrophilic region and a water repellent region by irradiating the chemically modified work surface with light having a predetermined pattern; anddisposing a pattern formation material in the hydrophilic region or the water repellent region.7. A pattern formation method for forming a circuit pattern for an electronic device on a substrate having flexibility claim 1 , the pattern formation method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying an entire surface or a specific region of the substrate using the fluorine-containing compound according to ;'}generating a latent image of the circuit pattern due to a difference in hydrophilicity and water repellency on the chemically modified surface of the substrate by irradiating with light energy having a distribution corresponding to the ...

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Номер записи: 62
25-06-2015 дата публикации

COPOLYMERIZABLE PHOTOINITIATORS

Номер: US20150175830A1
Автор: CASIRAGHI Angelo, Floridi Giovanni, Li Bassi Giuseppe, MENEGUZZO Enzo, NORCINI Gabriele
Принадлежит:

Benzophenone derivatives of formula (I) in which X is O, S or NR, and Ris H or linear or branched C-Calkyl; Ris H or methyl, Ris H, halogen, linear or branched C-Calkoxy, linear or branched C-Calkyl, linear or branched C-Calkylthio or a group NRR, wherein Rand Rare independently linear or branched C-Calkyl, can be used as copolymerizable photoinitiators and photocrosslinkers. 110-. (canceled)12. The copolymerizable benzophenone of wherein in formula I X is O or S and Ris H claim 11 , a linear or branched C-Calkyl or a linear or branched C-Calkoxy.13. The copolymerizable benzophenone of wherein in formula I X is O or S claim 12 , Ris methyl claim 12 , and Ris H.15. The process for preparing a copolymerizable benzophenone of wherein the Lewis acid is aluminum trichloride.16. The process for preparing a copolymerizable benzophenone of wherein in the alpha-halo acyl halide of formula (iii) claim 14 , Z and W are Cl.18. The polymerizable composition of comprising from about 85 to about 99 parts by weight of at least one ethylenically unsaturated compound and from about 1 to about 15 parts by weight of the copolymerizable benzophenone of formula I.19. The polymerizable composition of further comprising from about 0.2 to about 15% by weight of at least one coinitiator.20. The polymerizable composition of wherein the coinitiator is selected from the group consisting of: aliphatic claim 19 , cycloaliphatic claim 19 , aromatic claim 19 , arylaliphatic claim 19 , heterocyclic claim 19 , oligomeric and polymeric amines claim 19 , and combinations thereof.21. A method for coating a substrate comprising:{'b': '7', 'a) applying on the substrate a polymerizable composition of claim in an amount sufficient to result in a coating, after photopolymerization, having a thickness of from about 0.2 to about 100 micron; and'}b) photopolymerizing the coating with a light source with emission bands in the UV-visible region.227. The method of wherein the polymerizable composition of claim ...

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Номер записи: 63
01-07-2021 дата публикации

COMPOUND, COMPOSITION, CURED PRODUCT, OPTICALLY ANISOTROPIC BODY, AND REFLECTIVE FILM

Номер: US20210198230A1
Автор: KATOH Shunya, KODAMA Keisuke, Suzuki Yuko
Принадлежит: FUJIFILM Corporation

The present invention provides a compound having an excellent rate of change in HTP due to exposure. The present invention further provides a composition formed of the compound, a cured product, an optically anisotropic body, and a reflective film. 2. The compound according to claim 1 ,{'sup': '1', 'wherein Arepresents an aromatic hydrocarbon ring group or an aromatic heterocyclic group.'}3. The compound according to claim 1 ,{'sup': 1', '2, 'wherein Xand Xare bonded to each other to form a ring.'}4. The compound according to claim 1 ,{'sup': 1', '3', '5, 'wherein at least one of X, X, or Xrepresents the group represented by General Formula (2), and'}{'sup': 2', '4', '6, 'at least one of X, X, or Xrepresents the group represented by General Formula (2).'}5. The compound according to claim 1 ,{'sup': 3', '4', '5', '6, 'wherein at least one of X, X, X, or Xrepresents the group represented by General Formula (2), and'}{'sup': 1', '2, 'claim-text': {'br': None, 'sup': 3', '4', '2, 'sub': 'k', 'R-(A-Z)—*\u2003\u2003(A)'}, 'at least one of Xor Xrepresents a group represented General Formula (A),'}{'sup': 3', '2', '4, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'in General Formula (A), k represents an integer of 2 or more, Rrepresents a hydrogen atom or a substituent, Zrepresents a single bond, —O—, —S—, —CHO—, —CO—, —COO—, —CO—S—, —O—CO—O—, —CO—NH—, —CHS—, —CFO—, —CFS—, —CH═CH—COO—, —CH═CH—OCO—, —OCO—C(CN)═CH—, —COO—CHCH—, —OCO—CHCH—, —COO—CH—, —OCO—CH—, —CH═CH—, —N═N—, —CH═N—N═CH—, —CF═CF—, or —C═C—, Arepresents a hydrocarbon ring group or a heterocyclic group, and * represents a bonding position to the fused ring in General Formula (1).'}6. The compound according to claim 1 , {'br': None, 'sup': 2', '3', '1', '2', 'x, 'sub': 'm', 'R-(A-Z)-ACO—CH═CH—*\u2003\u2003(3)'}, 'wherein the group represented by General Formula (2) is a group represented by General Formula (3),'}{'sup': 2', '1', '2', '3', 'x', '2, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, ' ...

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Номер записи: 64
21-06-2018 дата публикации

Multifunctional cytoprotectant for treatment of pathogenic processes mediated by oxidative stress and toxic electrophiles

Номер: US20180169037A1
Автор: Richard M. LoPachin, Terrence Gavin
Принадлежит: Montefiore Medical Center

Methods, filters and compositions are disclosed for treating toxicity due to oxidative stress and toxic electrophiles.

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Номер записи: 65
08-07-2021 дата публикации

COMPOSITIONS AND METHODS FOR THE PREVENTION AND/OR TREATMENT OF MITOCHONDRIAL DISEASE, INCLUDING FRIEDREICH'S ATAXIA

Номер: US20210206736A1
Автор: Arsenjans Pavels, Keefe Dennis, Zheng Guozhu
Принадлежит:

The disclosure provides therapeutic compositions (i.e., therapeutic agents) and methods of preventing or treating Friedreich's ataxia in a mammalian subject, reducing risk factors, signs and/or symptoms associated with Friedreich's ataxia (e.g., Complex I deficiency), and/or reducing the likelihood or severity of Friedreich's ataxia. The disclosure further provides novel intermediates for the production of said therapeutic compositions and related reduced versions of said therapeutic compositions, which reduce forms may also be used as therapeutic agents (or prodrugs of the therapeutic agent(s)). 2. The compound of claim 1 , wherein E is 21 and F is 13 claim 1 , 14 claim 1 , 19 or 20.3. The compound of claim 1 , wherein E is 21 and F is 15 claim 1 , 16 claim 1 , 17 or 18.4. The compound of claim 1 , wherein J is O.5. The compound of claim 1 , wherein J is O and K is absent.6. The compound of claim 1 , wherein each of K and L is independently —(CH)— claim 1 , —(CD)- claim 1 , —(CHF)— claim 1 , —(CF)— claim 1 , —(CH(CH))— claim 1 , —(CF(CF))— claim 1 , —(C(CH))— or —(C(CF))—.7. The compound of claim 1 , wherein each of R claim 1 , Rand Ris independently H claim 1 , F claim 1 , —CH claim 1 , —OCH claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —OCF claim 1 , —C(CH) claim 1 , —C(CF) claim 1 , —CHCH claim 1 , —OCHCHor —CH(CH).8. The compound of claim 1 , wherein J is O; each of K and L is independently —(CH)— claim 1 , —(CD)- claim 1 , —(CHF)— claim 1 , —(CF)— claim 1 , —(CH(CH))— claim 1 , —(CF(CF))— claim 1 , —(C(CH))— or —(C(CF))—; and each of R claim 1 , Rand Ris independently H claim 1 , F claim 1 , —CH claim 1 , —OCH claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —OCF claim 1 , —C(CH) claim 1 , —C(CF) claim 1 , —CHCH claim 1 , —OCHCHor —CH(CH).9. The compound of claim 1 , wherein J is O; each of K and L is independently —(CH)— claim 1 , —(CD)- claim 1 , —(CHF)— claim 1 , —(CF)— claim 1 , —(CH(CH))— claim 1 , —(CF(CF))— claim 1 , —(C(CH))— or —(C(CF))—; ...

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Номер записи: 66
08-07-2021 дата публикации

PRODUCTION METHOD FOR FLUOROMETHYL DERIVATIVE

Номер: US20210206740A1
Автор: Higashi Masahiro, KISHIKAWA Yosuke, KITAMURA Tsugio
Принадлежит:

A method for producing a fluoromethyl derivative represented by formula (1), the method including step A of reacting an alkene compound represented by formula (2) with a fluorine source represented by formula MF, in the presence of a hypervalent-iodine aromatic compound (1a), or in the presence of an aromatic iodine compound (1b) and an oxidant (A) to fluorinate the alkene compound. 2. The production method according to claim 1 , wherein Rrepresents an aliphatic hydrocarbon group optionally having one or more substituents claim 1 , an aromatic hydrocarbon group optionally having one or more substituents claim 1 , an aliphatic heterocyclic group optionally having one or more substituents claim 1 , or an aromatic heterocyclic group optionally having one or more substituents.3. The production method according to claim 2 , wherein Rrepresents an aromatic hydrocarbon group optionally having one or more substituents or an aromatic heterocyclic group optionally having one or more substituents.4. The production method according to claim 1 , wherein Rrepresents hydrogen.5. The production method according to claim 1 , wherein Rrepresents hydrogen.6. The production method according to claim 1 ,{'sup': 4a', '4b, 'sub': 'm', 'wherein L represents —[C(—R)(—R)]—,'}{'sup': '4a', 'Rrepresents hydrogen or an organic group,'}{'sup': '4b', 'Rrepresents hydrogen or an organic group, and'}m represents an integer of 1 to 10.7. The production method according to claim 1 , wherein L represents —[C(—R)(—R)]— claim 1 ,{'sup': '4a', 'Rrepresents hydrogen or an organic group,'}{'sup': '4b', 'Rrepresents hydrogen or an organic group, and'}m represents an integer of 1 to 10, and{'sup': '4', 'Rrepresents hydroxyl.'}8. The production method according to claim 1 , wherein L represents —CO— claim 1 , and Rrepresents hydrogen claim 1 , halogen claim 1 , or an organic group.9. The production method according to claim 1 , wherein L represents —CO— claim 1 , and Rrepresents an aliphatic hydrocarbon group ...

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Номер записи: 67
04-06-2020 дата публикации

DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES

Номер: US20200170907A1
Автор: Jia Qi, Zhao Ji-Fu
Принадлежит: Unigen, Inc.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier. 133-. (canceled)35. The method of claim 34 , wherein the compound is selected from the group consisting of 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(3′ claim 34 ,4′-dihydroxyphenyl)-1-propanol claim 34 , 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(3′ claim 34 ,4′-dimethoxyphenyl)-1-propanol claim 34 , 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(2′-hydroxyphenyl)-1-propanol claim 34 , 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(2′-methoxyphenyl)-1-propanol claim 34 , 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(4′-methoxyphenyl)-1-propanol claim 34 , 1-(2 claim 34 ,4 claim 34 ,6-trihydroxyphenyl)-3-(4′-aminophenyl)-1-propanol claim 34 , dihydroxyphenyl)-3-phenyl-1-propanol claim 34 , 1-(2 claim 34 ,4-dihydroxyphenyl)-3-(3′- ...

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Номер записи: 68
23-07-2015 дата публикации

COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX

Номер: US20150203445A1
Автор: Albury Mary Susan, Elliott Catherine, Moore Anthony Lennox, Young Luke Edward
Принадлежит:

The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bccomplex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections. 2. Use according to claim 1 , wherein Ris a group selected from: CHO; CHOH; CN; CH; C(O)NH; C(O)NHCH; C(O)CH; CFCH; CHCH; CHOAc; COOH; and COOCH.3. Use according to claim 1 , wherein Ris a short-chain alkyl claim 1 , a methyl group claim 1 , an ethyl group claim 1 , a propyl group claim 1 , or hydroxyl group4. (canceled)5. Use according to claim 1 , wherein Ris a straight chain or branched alkyl or alkylene with 6 to 15 C atoms claim 1 , 8 to 12 C atoms or 8 to 10 C atoms claim 1 , that is optionally mono- or polysubstituted by a Cto Calkyl group.6. Use according to claim 1 , wherein Ris a branched diene having 6 to 15 C atoms that is substituted with at least one claim 1 , and preferably two claim 1 , methyl groups.7. Use according to claim 1 , wherein Ris a methyl claim 1 , ethyl claim 1 , propyl group; or hydroxyl group.8. (canceled)9. Use according to claim 1 , wherein Ris a chlorine claim 1 , bromine claim 1 , fluorine or iodine group.10. Use according to claim 1 , wherein Ris a chlorine group; or wherein Ris a methyl claim 1 , ethyl or propyl group or wherein Ris a methyl group.1112-. (canceled)13. Use according to claim 1 , wherein:—{'sup': '1', 'sub': 2', '3', '2', '3', '3', '2', '3', '2', '3', '2', '3, 'Ris selected from CHO; CHOH; CN; CH; C(O)NH; C(O)NHCH; C(O)CH; CFCH; CHCH; CHOAc; COOH; and COOCH; and wherein'}{'sup': '2', 'Ris a hydroxyl group;'}{'sup': '3', 'sub': 1', '4, 'Ris a straight chain or branched alkyl or alkylene with 4 to 20 C atoms, that is optionally mono- or polysubstituted by a Cto Calkyl group;'}{'sup': '4', 'Ris a hydroxyl group;'}{'sup': '5', 'Ris a chlorine atom; and'}{'sup': '6', 'sub': 1', '4, 'Ris H or a Cto Calkyl group.'}14. Use according to claim 1 , ...

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Номер записи: 69
14-07-2016 дата публикации

METHOD FOR PRODUCING ALPHA-HALOGENOACETOPHENON COMPOUND, AND ALPHA-BROMOACETOPHENON COMPOUND

Номер: US20160200654A1
Автор: AMAO Akihito, SHIMONO Katsuhiro, YOFU Katsuyuki
Принадлежит: FUJIFILM Corporation

A method for producing an α-halogenoacetophenon compound includes reacting a specific α-halogenocarboxylic halide compound and a specific phenyl compound in the presence of a Lewis acid in a solvent, in which the α-halogenoacetophenon compound and the phenyl compound are reacted with each other in a molar ratio of the Lewis acid to the phenyl compound represented below. 2. The method for producing an α-halogenoacetophenon compound according to claim 1 ,{'sup': '1', 'wherein, in Formula (1), Xrepresents a bromine atom.'}3. The method for producing an α-halogenoacetophenon compound according to claim 2 ,{'sup': 1', '2, 'wherein, in Formula (1), Rand Rare methyl.'}4. The method for producing an α-halogenoacetophenon compound according to claim 1 ,wherein aluminium (III) chloride is used as the Lewis acid.5. The method for producing an α-halogenoacetophenon compound according to claim 1 ,{'sup': '7', 'wherein Rin Formulae (2) and (3) is an alkylcarbonyl group or an arylcarbonyl group.'}6. The method for producing an α-halogenoacetophenon compound according to claim 1 ,wherein n in Formulae (2) and (3) is 2.7. The method for producing an α-halogenoacetophenon compound according to claim 2 ,wherein n in General Formulae (2) and (3) is 2.8. The method for producing an α-halogenoacetophenon compound according to claim 1 ,wherein at least one selected from dichloromethane, chlorobenzene, sulfolane, ethyl acetate, acetonitrile, 1,3,5-trimethylbenzene, methyl ethyl ketone, and o-dichlorobenzene is used as the solvent.9. The method for producing an α-halogenoacetophenon compound according to claim 1 ,wherein, at least one selected from dichloromethane, chlorobenzene, and o-dichlorobenzene is used as the solvent.10. The method for producing an α-halogenoacetophenon compound according to claim 2 ,wherein, at least one selected from dichloromethane, chlorobenzene, and o-dichlorobenzene is used as the solvent.11. The method for producing an α-halogenoacetophenon compound according ...

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Номер записи: 70
13-07-2017 дата публикации

METHOD FOR PREPARING 3-TRIFLUOROMETHYL CHALCONES

Номер: US20170197925A1
Автор: Annis Gary David
Принадлежит:

Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein Mis Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. 5. The method of wherein Ris Cl; Ris F; and Ris Cl.6. The method of wherein R claim 4 , Rand Rare Cl.7. The method of wherein Ris Cl; Ris H; and Ris Cl.8. The method of wherein Ris CF; Ris H; and Ris Cl.10. The method of wherein Ris Cl; Ris F; and Ris Cl.11. The method of wherein R claim 9 , Rand Rare Cl.12. The method of wherein Ris Cl; Ris H; and Ris Cl.13. The method of wherein Ris CF; Ris H; and Ris Cl.15. A compound which is 1-[3 claim 9 ,5-dichloro-4-fluorophenyl]2 claim 9 ,2 claim 9 ,2-trifluoroethanone. This invention pertains to a method for preparing 3-trifluoromethyl chalcones and trifluoroacetyl intermediates. The present invention also relates to novel trifluoroacetyl and halo compounds useful as starting materials and intermediates for the aforedescribed method.The present invention provides a method for preparing a compound of Formula 1whereinZ is optionally substituted phenyl; andQ is phenyl or 1-naphthalenyl, each optionally substituted;comprising distilling water from a mixture comprising a compound of Formula 2a compound of Formula 3a base comprising at least one compound selected from the group consisting ofM(OH)   4(M)CO   4aThis invention also provides a method for preparing a compound of Formula 2 wherein Z is optionally substituted phenyl, comprising(1) forming a reaction mixture comprising a Grignard reagent derived from a compound of Formula 5Z—X   5wherein X is Cl, Br or I, ...

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Номер записи: 71
25-09-2014 дата публикации

METHOD FOR PREPARING 2,6-DIFLUOROACETOPHENONES

Номер: US20140288316A1
Автор: Daub John P., Wagerle Ty
Принадлежит:

Disclosed are methods for preparing compounds of Formula 1 utilizing an intermediate of Formula 4 or an intermediate of Formula 6. 2. The method of wherein Ris H; and Rand Rare CHCH.3. The method of wherein the alkaline earth salt of a strong acid is magnesium chloride.4. The method of wherein the tertiary amine base is selected from the group consisting of tributylamine claim 1 , triethylamine claim 1 , diisopropylethylamine claim 1 , pyridine claim 1 , picolines claim 1 , lutidines claim 1 , N claim 1 ,N-dimethylaniline and N claim 1 ,N-diethylaniline.5. (canceled)6. The method of wherein the aprotic solvent is chlorobenzene claim 1 , toluene claim 1 , xylenes claim 1 , dichloromethane claim 1 , tetrahydrofuran claim 1 , acetonitrile or ethyl acetate.7. (canceled)8. The method of wherein in step (C) the compound of Formula 4 is contacted with water in a pressure reactor and the temperature is in the range of 130 to 160° C.9. The method of wherein in step (C) the compound of Formula 4 is contacted with water in the presence of an acid and heated to a temperature in the range of 85 to 130° C. to give the compound of Formula 1.10. The method of wherein in step (C) the acid is sulfuric acid claim 9 , acetic acid or mixtures thereof.12. (canceled)14. The method of wherein Ris H claim 13 , Ris CHCHand M is K.15. The method of wherein the alkaline earth salt of a strong acid is magnesium chloride.16. The method of wherein the tertiary amine base is selected from the group consisting of tributylamine claim 13 , triethylamine claim 13 , diisopropylethylamine claim 13 , pyridine claim 13 , picolines claim 13 , lutidines claim 13 , N claim 13 ,N-dimethylaniline and N claim 13 ,N-diethylaniline.17. (canceled)18. The method of wherein the aprotic solvent is chlorobenzene claim 13 , toluene claim 13 , xylenes claim 13 , dichloromethane claim 13 , tetrahydrofuran claim 13 , acetonitrile or ethyl acetate.19. (canceled)20. The method of wherein in step (C) the compound of Formula ...

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Номер записи: 72
30-07-2015 дата публикации

DIHYDROCHALCONE DERIVATIVES AND THEIR USE AS ANTIBIOTIC AGENTS

Номер: US20150210663A1
Автор: Legault Jean, Pichette André, Simard Francois
Принадлежит: UNIVERSITE DU QUEBEC A CHICOUTIMI

A compound of formula (I) as well as pharmaceutical compositions comprising same is provided. An extract of a plant belonging to a species of the extract comprising this compound is also provided. These can be used as antibacterial for treating bacterial infection. 3. The compound of wherein Ris H.4. The compound of claim 1 , wherein Ris H or CH.5. The compound of claim 1 , wherein Ris H.6. The compound of claim 1 , wherein Ris H or —CH.7. The compound of claim 1 , wherein Ris H claim 1 , —OH or —O—CH.8. The compound of claim 1 , wherein Ris H or —OH.1011-. (canceled)12. The compound of claim 1 , wherein said compound is in free base form.13. The compound of claim 1 , wherein said compound is a pharmaceutically acceptable salt.14. The compound of claim 1 , wherein said compound is a pharmaceutically acceptable ester.15. The compound of claim 1 , wherein said compound is a pharmaceutically acceptable solvate.16. The compound of claim 15 , wherein said solvate is an hydrate.17Populus. An extract of a plant belonging to a species of claim 1 , the extract comprising at least one compound of formula (I) as defined in .18Populus balsamifera.. The extract of claim 17 , wherein the plant is19Populus balsamifera. The extract of claim 18 , being an extract of buds.20. The extract of claim 19 , being an ethanolic extract claim 19 , or a combination of several such extracts claim 19 , in liquid form or dried form.21. A methanolic extract of the dried ethanolic extract of claim 20 , said methanolic extract fraction having optionally been extracted with hexane one or more times claim 20 , said methanolic extract being in liquid or dried form.22. A diethyl ether extract of the methanolic extract of claim 21 , said diethyl ether extract having optionally been extracted with water one or more times claim 21 , said diethyl ether extract being in liquid or dried form.23. A fraction of the dried diethyl ether extract of .2426-. (canceled)27. A pharmaceutical composition comprising (i) ...

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Номер записи: 73
18-06-2020 дата публикации

Compounds, compositions, and methods for use in treating autophagy-associated disorders

Номер: US20200190007A1
Автор: Ian Henderson
Принадлежит: Biophagy Inc

The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.

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Номер записи: 74
20-07-2017 дата публикации

PROCESSES FOR PREPARING (R)-1-(5-CHLORO-[1,1`-BIPHENYL]-2-YL)-2,2,2-TRIFLUOROETHANOL AND 1-(5-CHLORO-[1,1`-BIPHENYL]-2-YL)-2,2,2-TRIFLUOROETHANONE

Номер: US20170204041A1
Автор: DE LOMBAERT Stephane, Goldberg Daniel R.
Принадлежит:

The present invention relates to processes for the preparation of (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol, 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone, and intermediates thereof, which are useful in the preparation of inhibitors of TPH1 for the treatment of, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, low bone mass diseases, serotonin syndrome, and cancer. 181-. (canceled) The present invention relates to processes for the preparation of (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol, 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone, and intermediates thereof, which are useful in the synthesis of inhibitors of TPH1 for the treatment of, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, low bone mass diseases, serotonin syndrome, and cancer.Two vertebrate isoforms of TPH, namely TPH1 and TPH2, have been identified. TPH1 is primarily expressed in the pineal gland and non-neuronal tissues, such as enterochromaffin (EC) cells located in the gastrointestinal (GI) tract. TPH2 (the dominant form in the brain) is expressed exclusively in neuronal cells, such as dorsal raphe or myenteric plexus cells. TPH catalyzes the hydroxylation of tryptophan in the biosynthesis of 5-HT. Thus, the pharmacological effects of 5-HT can be modulated by agents affecting TPH.TPH1 inhibitors are known in the art. Spirocyclic compounds disclosed in U.S. Ser. No. 14/477,948, filed Sep. 5, 2014, can inhibit TPH1 and were found to reduce peripheral serotonin levels in animal models. The preparation of these compounds can include the coupling of an alcohol with a chloro-substituted heteroaromatic compound in the presence of base to yield an ether intermediate that can be used to make the final TPH1 inhibitor product. A particular chiral alcohol useful in the synthesis of TPH1 inhibitors is (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol (see Formula A below). ...

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Номер записи: 75
28-07-2016 дата публикации

COMPOSITION FOR TREATING METABOLIC SYNDROME AND A PREPARATION METHOD THEREOF

Номер: US20160214918A1
Автор: CHANG FANG-RONG, Fulop Ferenc, Hsieh Chi-Ting, HSIEH TUSTY-JIUAN, Ötvös Sándor Balázs, WU YANG-CHANG
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

A compound for treating a metabolic syndrome, comprising a structure of a 6Cs unit-3Cs unit-6Cs unit (C6-C3-C6) as shown in formula I, wherein: when Rand Rare both hydrogens, C3 has only single bonds; when Ris an oxygen and Ris one selected from a group consisting of an alkoxy, a benzyloxy and a halogen, C3 has only single bonds; when Ris a deuterium and Ris one selected from a group consisting of a hydrogen, an alkoxy, a benzyloxy and a halogen, C3 has one of a single bond and a double bond. 2. The compound as claimed in claim 1 , wherein the compound is used to regulate and stabilize a blood glucose level in a cell.3. The compound as claimed in claim 1 , wherein the compound is used to inhibit a glucose intolerance in a cell.4. The compound as claimed in claim 1 , wherein treating the metabolic syndrome includes one of inhibiting and delaying an onset of the metabolic syndrome in a cell.5. The compound as claimed in claim 1 , wherein the metabolic syndrome is related to a diabetes mellitus.7. The pharmaceutical composition as claimed in claim 6 , wherein the pharmaceutical composition is used to regulate and stabilize a blood glucose level in a cell.8. The pharmaceutical composition as claimed in claim 6 , wherein the pharmaceutical composition is used to inhibit a glucose intolerance in a cell.9. The pharmaceutical composition as claimed in claim 6 , wherein treating the metabolic syndrome includes one of inhibiting and delaying an onset of the metabolic syndrome in a cell.10. The pharmaceutical composition as claimed in claim 6 , wherein the metabolic syndrome is related to a diabetes mellitus.11. The pharmaceutical composition as claimed in claim 6 , wherein the C6-C3-C6 is a chalcone.12. The pharmaceutical composition as claimed in claim 6 , wherein the deuterium is prepared by a hydrogenation reduction.13. The pharmaceutical composition as claimed in claim 6 , wherein the triple bond is prepared by an Aldol condensation synthesis.14. The pharmaceutical ...

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Номер записи: 76
06-08-2015 дата публикации

CARBONYL DERIVATIVE, LIQUID CRYSTAL COMPOSITION CONTAINING COMPOUND THEREOF AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20150218452A1
Автор: Goto Mayumi
Принадлежит:

To provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds; a liquid crystal composition containing the compound; and a liquid crystal display device including the composition. The compound is represented by formula (1): 6. The compound according to , wherein , in formulas (1-21) to (1-27) according to , Ra and Rb are independently alkyl having 1 to 10 carbons , alkenyl having 2 to 10 carbons or alkoxy having 1 to 9 carbons;{'sup': 1', '2, 'Aand Aare independently 1,4-cyclohexylene, 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,3-difluoro-1,4-phenylene or tetrahydropyran-2,5-diyl;'}{'sup': '1', 'Zis a single bond; and'}{'sup': '1', 'sub': 2', '3, 'Yis —CFH or —CF.'}7. The compound according to , wherein , in formulas (1-21) to (1-27) according to , Ra and Rb are independently alkyl having 1 to 10 carbons or alkoxy having 1 to 9 carbons;{'sup': 1', '2, 'Aand Aare independently 1,4-cyclohexylene or 1,4-phenylene;'}{'sup': '1', 'Zis a single bond; and'}{'sup': '1', 'sub': '2', 'Yis CFH.'}8. The compound according to , wherein , in formulas (1-21) to (1-27) according to , Ra and Rb are independently alkyl having 1 to 10 carbons or alkoxy having 1 to 9 carbons;{'sup': 1', '2', '3, 'A, Aand Aare independently 1,4-cyclohexylene or 1,4-phenylene;'}{'sup': 1', '2, 'Zand Zare single bonds;'}{'sup': '1', 'sub': '3', 'Yis —CF.'}9. A liquid crystal composition claim 1 , containing at least one compound according to14. The liquid crystal composition according to claim 9 , further containing at least one optically active compound and/or at least one polymerizable compound.15. The liquid crystal composition according to claim 9 , further containing at least one ...

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Номер записи: 77
25-06-2020 дата публикации

SQUARYLIUM COMPOUNDS FOR USE IN DISPLAY DEVICES

Номер: US20200199058A1
Автор: Cai Jie, Hsieh Wan-Yun, Siddiqui Ozair, WANG Peng, Welch Michael, Zheng Shijun
Принадлежит:

Optionally substituted squarylium compounds, such as those depicted in Formula 1, may be useful in filters for display devices. 2. The squarylium compound of claim 1 , where each substituent of each Ar claim 1 , if present claim 1 , are represented by an empirical formula OH claim 1 , or CHO.3. The squarylium compound of claim 2 , wherein Ris H.4. The squarylium compound of claim 2 , wherein Ris —COCH.5. The squarylium compound of claim 2 , wherein Ris linear Calkyl.6. The squarylium compound of claim 2 , wherein Ris linear Calkenyl.7. The squarylium compound of claim 2 , wherein Ris optionally substituted —CH-phenyl.8. The squarylium compound of claim 2 , wherein Ris optionally substituted phenyl.9. The squarylium compound of claim 2 , wherein Ris optionally substituted —CHCH═CH-phenyl.13. The optical filter of claim 11 , wherein the polymer matrix comprises poly(methyl methacrylate) (PMMA).14. The optical filter of claim 11 , wherein the polymer matrix comprises oxygen scavenging agent.15. The optical filter of claim 11 , wherein the filter has a peak absorption of greater than 550 nm.16. The optical filter of claim 15 , wherein the filter has a peak absorbance wavelength of greater than 568 nm.17. The optical filter of claim 15 , or claim 15 , wherein the filter has a full width at half maximum (FWHM) of less than 50 nm.18. The optical filter of claim 17 , wherein the filter has a full width at half maximum (FWHM) of 40-50 nm.19. A display device comprising the optical filter of claim 11 , and an RBG source positioned to allow viewing of the RGB source through the optical filter. The embodiments include compounds for use in color filters through which light passes.In color reproduction, the color gamut can be a given complete subset of colors. The most common usage refers to the subset of colors which can be accurately represented in a given circumstance, such as by a certain output device. For example, the wide-gamut Red Green Blue (RGB) color space (or Adobe ...

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Номер записи: 78
26-07-2018 дата публикации

OPHTHALMIC LENS MATERIAL AND OPHTHALMIC LENS OF SUCH MATERIAL

Номер: US20180210114A1
Автор: CHIEN HSIU-WEN
Принадлежит:

A wetness-retaining ophthalmic lens material comprises an organic monomer, a cross-linking agent, an initiator, a salt, and a solvent. The salt dissolves in the water dissociates a plurality of anions and cations, which bind to water molecules and retard the evaporation of the water molecules, the ophthalmic lens material thus can keep wet for a long time. An ophthalmic lens made of the ophthalmic lens material is also provided. 1. An ophthalmic lens material comprising:an organic monomer;a cross-linking agent;an initiator;a salt; anda solvent comprising water.2. The ophthalmic lens material of claim 1 , wherein the organic monomer has a mass percentage of about 32% to about 81% of the total mass of the ophthalmic lens material claim 1 , the cross-linking agent has a mass percentage of about 0.08% to about 14.6% of the total mass of the ophthalmic lens material claim 1 , the initiator has a mass percentage of about 0.05% to about 12.1% of the total mass of the ophthalmic lens material claim 1 , the salt has a mass percentage of about 3% to about 21.5% of the total mass of the ophthalmic lens material claim 1 , and the solvent has a mass percentage of about 5.5% to about 51% of the total mass of the ophthalmic lens material.3. The ophthalmic lens material of claim 1 , wherein the organic monomer comprises hydrophilic monomer claim 1 , the hydrophilic monomer is selected from a group consisting of 2-hydroxyethylmethacrylate claim 1 , methyl methacrylate claim 1 , N claim 1 ,N-dimethyacrylamide claim 1 , glycidyl methacrylate claim 1 , N-vinyl-2-pyrrolidone claim 1 , and any combination thereof.4. The ophthalmic lens material of claim 3 , wherein the organic monomer further comprises an organic silicon monomer claim 3 , the organic silicon monomer is selected from a group consisting of 3-(methacryloyloxy)propyltris(trimethylsiloxy)silane claim 3 , poly(dimethylsiloxane) claim 3 , and any combination thereof.5. The ophthalmic lens material of claim 1 , wherein the cross ...

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Номер записи: 79
03-08-2017 дата публикации

PROCESS FOR THE PREPARATION OF 1-(3,5-DICHLOROPHENYL)-2,2,2-TRIFLUOROETHANONE AND DERIVATIVES THEREOF

Номер: US20170217865A1
Автор: Gribkov Denis
Принадлежит: SYNGENTA PARTICIPATIONS AG

A process for the preparation of a compound of formula (I) wherein Ris hydrogen, fluoro or chloro; which process comprises: a) reacting a compound of formula (II) wherein Ris hydrogen, fluoro or chloro; with a nitration agent to the compound of formula (III) wherein Ris hydrogen, fluoro or chloro; b) reacting the compound of formula (III) with trichloroisocyanuric acid in the presence of sulfuric acid or fuming sulfuric acid to the compound of formula (IV) wherein R1 is hydrogen, fluoro or chloro; and c) reacting the compound of formula (III) with chlorine gas at a temperature from 180° C. to 250° C. to the compound of formula (I). 2. The process according to claim 1 , characterized in that the nitration agent is selected from sulfuric acid claim 1 , nitric acid and their salts.3. The process according to claim 1 , characterized in that the process is performed without isolating the intermediate of formula III.5. (canceled) The present invention relates to the preparation of halo-substituted 1-aryl-2,2,2-trifluoro-ethanones (compounds Ia, Ib and Ic):and to intermediates useful for said process. Said compounds are important intermediates for the preparation of pesticidally active isoxazoline-substituted benzamides as for example 1-(3,5-dichloro-4-fluoro-phenyl)-2,2,2-trifluoro-ethanone (Ic) disclosed in EP 1932836A1.Typically said compounds of formula Ia, Ib and Ic are prepared by reaction of the corresponding organometallic reagents derived from halo-substituted 5-bromo-benzenes of formula VIa, VIb and VIcwith the derivatives of trifluoroacetic acid (for example ethyl trifluoroacetate). For example the preparation of 2,2,2-trifluoro-1-(3,4,5-trichlorophenyl)ethanone (I b) is described in WO 2012/120135.The corresponding bromo derivatives of the formula VIa, VIb and VIc are not easily available and prepared via multistep procedures. For example, 5-bromo-1,2,3-trichloro-benzene (VI b) can be prepared as described in Sott, R.; Hawner, C.; Johansen, J. E. Tetrahedron ...

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Номер записи: 80
12-08-2021 дата публикации

TRANSITION METAL-BASED HETEROGENEOUS CARBONYLATION REACTION CATALYST AND METHOD FOR PREPARING LACTONE OR SUCCINIC ANHYDRIDE USING CATALYST

Номер: US20210245144A1
Автор: Jiang Jianwei, Park Kwang Ho, Rajendiran Senkuttuvan, YOON Sungho
Принадлежит: KOOKMIN UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION

A transition metal-based heterogeneous carbonylation reaction catalyst has an excellent catalytic activity and selectivity in the carbonylation reaction and is easily separated from a product, by crosslinking polymerizing a transition metal-based homogeneous catalyst unit through a Friedel-Craft reaction. The catalyst may be used in a method for preparing lactone. The transition metal-based heterogeneous carbonylation reaction catalyst allows to produce lactone or succinic anhydride with an epoxide compound while showing a high selectivity, and can be applied in industrial very usefully due to easy separation from the product and thus reusing thereof. 1. A method for preparing a transition metal-based heterogeneous carbonylation reaction catalyst , the method comprising the steps of:(a) synthesizing a ligand compound having three or more metal coordination numbers to which a phenyl ring capable of carrying out a Friedel-Crafts reaction is bound;(b) synthesizing a transition metal-based homogeneous catalyst unit by reacting the ligand compound with a transition metal compound; and(c) preparing the transition metal-based heterogeneous carbonylation reaction catalyst by performing the Friedel-Crafts reaction of the transition metal-based homogeneous catalyst unit and reacting it with a counter anion-containing compound.2. The method for preparing the transition metal-based heterogeneous carbonylation reaction catalyst according to claim 1 , wherein the transition metal-based homogeneous catalyst unit represented by chemical formula 1 below is bonded through the Friedel-Crafts reaction:{'br': None, 'sub': 'n', 'M(L-R)X\u2003\u2003Chemical formula (1)'}{'sub': '4', 'sup': '−', 'in the chemical formula (1), M is a transition metal of Al, Ir, Pt, Pd, Ru, Rh, Ni, Fe, Cu, V, Co, Cr, Au, Re, W, Zr, Mo, Ti, Th or Si, L Is a ligand having three or more metal coordination numbers, R is a phenyl ring capable of carrying out the Friedel-Crafts reaction, n is an integer of 2 or ...

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Номер записи: 81
13-11-2014 дата публикации

ANTI-VIRULENCE COMPOSITIONS AND METHODS

Номер: US20140336258A1
Автор: Shoham Menachem
Принадлежит:

A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium. 126-. (canceled)29: The pharmaceutical composition of claim 27 , further comprising a pharmaceutically acceptable carrier.30: The pharmaceutical composition of claim 27 , further comprising an antibiotic. This application claims priority from U.S. Provisional Application No. 61/311,575, filed Mar. 8, 2010, the subject matter of which, are incorporated herein by reference in their entirety.This application relates to anti-virulence compositions and methods for treating bacterial infections and more particularly to compositions and methods for reducing the virulence of bacterium that expresses accessory gene regulator A (AgrA).is one of the most common causes of hospital-acquired and community-acquired infections worldwide, and reports of its growing levels of resistance to last-resort antibiotics, such as vancomycin, threaten a serious international public health problem. causes diseases ranging from minor skin infections to life-threatening deep infections such as pneumonia, endocarditis, meningitis, post-operative wound infections, septicemia, and toxic shock syndrome. causes such fatal diseases due to the expression of toxins and other virulence factors that have been shown to affect the outcome of the infective process. The expression of virulence factors is highly regulated and involves cell-cell communication, otherwise known as quorum sensing. Therefore, alternative methods for the prevention and treatment of bacterial infections in general and antibiotic resistant infections in particular are needed.This application relates to anti-virulence compositions and methods for treating bacterial infections and more particularly to compositions and methods for reducing the virulence of bacterium that expresses ...

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Номер записи: 82
23-09-2021 дата публикации

Process for Manufacture of Fluorinated Benzenes and Fluorinated Benzophenones, and Derivatives Thereof

Номер: US20210292264A1
Автор: DU Hongjun, Wu Wenting, Zhou Changyue
Принадлежит: Fujian Yongjing Technology Co., Ltd

The invention relates to a new process for the manufacture or synthesis, respectively, of fluorinated benzenes and fluorinated benzophenones, and derivatives thereof, in particular of fluorobenzenes and derivatives thereof. The present invention particularly pertains to a novel environmentally friendly process for the synthesis of fluorinated benzenes and benzophenones as raw materials for the manufacture of polyaryletherketones (PAEKs). 2. The process of preparing the compound according to claim 1 , wherein the compound prepared is fluorinated in a fluorination reaction.3. The process of preparing the compound according to claim 1 , wherein the starting material compound is selected from compounds having the formula (I) claim 1 ,whereinRn independently denotes a single substituent selected from the group consisting of hydrogen (H), fluorine (F), and chlorine (Cl); andHal denotes a halogen selected from the group consisting of fluorine (F) and chlorine (Cl).4. The process of preparing the compound according to claim 1 , wherein the starting material compound is selected from the group of compounds consisting of compounds wherein one of Rn claim 1 , is fluorine (F) or chlorine (Cl) claim 1 , and the others of Rn are hydrogen claim 1 , and Hal is fluorine (F) or chlorine (Cl).6. The process of preparing the compound according to claim 5 , wherein the Friedel-Crafts reagent is selected from compounds having the formula (II) claim 5 ,whereinR′n independently denotes a single substituents selected from the group consisting of hydrogen (H), fluorine (F), and chlorine (Cl); and{'sub': 3', '2', '3', '2, 'R1 and R2 independently from each other denote a hydrogen, a trichloromethyl group (—CCl), a carbonyl chloride group (—(C═O)Cl) or a chloromethyl group (—CHCl), and at least one of R1 and R2 is a trichloromethyl group (—CCl), a carbonyl chloride group (—(C═O)Cl) or a chloromethyl group (—CHCl); or a boronic acid group.'}7. The process of preparing the compound according to ...

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Номер записи: 83
08-09-2016 дата публикации

NOVEL PHENYL GLYOXAL PROBES

Номер: US20160258961A1
Автор: Bicker Kevin L., Subramanian Venkataraman, Thompson Paul R.
Принадлежит:

Novel phenyl-glyoxal based anti-citrulline probes and methods of synthesis are provided. Methods of use, such as, the development of methods for monitoring substrate citrullination over time; for identifying citrullinated proteins from cells are described. 1. A phenylglyoxal derivative comprising: an isotopically labeled , fluorophore labeled , or biotin labeled phenylglyoxal (biotin-PG).3. The phenylglyoxal derivative of claim 1 , wherein the fluorophore labeled phenylglyoxal comprises: rhodamine labeled phenylglyoxal (Rh-PG) or fluorescein labeled phenylglyoxal.4. The phenylglyoxal derivative of claim 1 , wherein the labeled phenylglyoxal is biotin labeled phenylglyoxal (biotin-PG).5. A method of labeling citrullinated proteins protein or fragments thereof in a biological sample claim 1 , comprising:contacting a biological sample with an effective amount of a phenylglyoxal probe, wherein the probe is detectably labeled and the detectably labeled phenylglyoxal probe is covalently bonded to a citrullinated protein or fragments thereof in the biological sample; thereby,labeling the citrullinated protein or fragments thereof in the biological sample.7. The method of claim 6 , wherein the detectable label comprises: fluorophores claim 6 , chromophores claim 6 , isotopes claim 6 , chemiluminescent molecules claim 6 , fluorescent molecules claim 6 , enzymes or co-enzymes.8. The method of claim 6 , wherein the fluorophore comprises: rhodamine or fluorescein.9. The method of claim 6 , wherein the co-enzyme is biotin.10. The method of claim 5 , wherein the step of contacting the biological sample with the phenylglyoxal probe is conducted in a medium having a pH value of about 0.001 to about 13.9.11. The method of claim 5 , wherein the step of contacting the biological sample with the phenylglyoxal probe is conducted in a medium having a pH value of about 0.001 to about 6.9.12. The method of claim 5 , wherein the step of contacting the biological sample with the ...

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Номер записи: 84
07-09-2017 дата публикации

METHOD FOR MAKING POLYARYLALIPHATICETHERKETONE POLYMERS AND COPOLYMERS THEREOF

Номер: US20170253696A1
Автор: SMITH Kaylie Jane, TOWLE Ian David Henderson
Принадлежит:

The present disclosure provides a process for producing a polymer, said process comprising polymerising a monomer system comprising a compound of formula: Ar—O—Ar—C(═O)—X—C(═O)—Ar—O—Ar in a reaction medium comprising a Lewis acid where: 1. A process for producing a polymer , said process comprising polymerizing a monomer system comprising a compound of formula: Ar—O—Ar—C(═O)—X—C(═O)—Ar—O—Ar in a reaction medium comprising a Lewis acid , wherein:X is an aliphatic moiety,andAr is an aromatic moiety.2. The process as claimed in claim 1 , wherein the reaction medium further comprises a dielectrophile.3. The process as claimed in claim 2 , wherein said dielectrophile is a compound of formula: L-(O═)C—Ar—C(═O)-L claim 2 , wherein L is a leaving group.4. The process as claimed in claim 1 , wherein X is selected from cyclohexyl (Cy) and —{CH}— claim 1 , wherein n is an integer from 1 to 100 claim 1 , preferably 2 to 50 claim 1 , most preferably 2 to 22 claim 1 , preferably 2 to 18 or 2 to 12 claim 1 , especially claim 1 , 3 to 10 claim 1 , e.g. 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 8 or 10.5. The process as claimed in claim 1 , wherein the compound of formula: Ar—O—Ar—C(═O)—X—C(═O)—Ar—O—Ar is polymerized in presence of a controlling agent.6. The process as claimed in claim 5 , wherein the controlling agent is a Lewis base (e.g. an aprotic Lewis base).7. The process as claimed in claim 5 , wherein the controlling agent is an aromatic carboxylic acid claim 5 , aromatic sulphonic acid or a derivative thereof.9. The process as claimed in claim 7 , wherein the controlling agent is benzoic acid.10. The process as claimed in claim 5 , wherein an amount of the controlling agent is from 0.25 to 4 equivalents claim 5 , especially 1 to 2 equivalents claim 5 , especially 2 equivalents claim 5 , per equivalent of acid halide groups.11. The process as claimed in claim 1 , wherein the aromatic moiety (Ar) is independently selected from the group consisting of substituted and ...

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Номер записи: 85
15-09-2016 дата публикации

C-HALOGEN BOND FORMATION

Номер: US20160264512A1
Автор: Groves John T., Huang Xiongyi, Liu Wei
Принадлежит: THE TRUSTEES OF PRINCETON UNIVERSITY

Fluorinated compounds are provided. Fluorinated compounds may be prepared by a method of halogenating a carbon containing compound having an sp3 C—H bond. 1. A composition comprising a product of a method direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond including combining the carbon containing compound , a fluorinating agent , a fluorinating catalyst , and an oxidant.2. (canceled)3. The composition of claim 1 , wherein the carbon containing compound is selected from the group consisting of ibuprofen claim 1 , ibuprofen methyl ester claim 1 , rasagiline claim 1 , nabumetone claim 1 , celestolide claim 1 , celecoxib analog claim 1 , papaverine claim 1 , protected enalaprilat claim 1 , protected fingolimod claim 1 , protected dopamine claim 1 , N-Boc-cinacalcet claim 1 , JNJ41510417 claim 1 , 5-OH-FPPAT claim 1 , FEP claim 1 , Acl703 claim 1 , BMIPP claim 1 , HAR claim 1 , flutemetamol claim 1 , and MK-9470.4. (canceled)5. A composition comprising at least one compound selected from the group consisting of fluoro-ibuprofen or the methyl ester thereof claim 1 , fluoro-rasagiline claim 1 , fluoro-nabumetone claim 1 , fluoro-celestolide claim 1 , fluoro-celecoxib analog claim 1 , fluoro-papaverine claim 1 , fluoro-protected enalaprilat claim 1 , fluoro-protected fingolimod claim 1 , fluoro-protected dopamine claim 1 , fluoro-N-Boc-cinacalcet claim 1 , fluoro-JNJ41510417 claim 1 , fluoro-5-OH-FPPAT claim 1 , fluoro-FEP claim 1 , fluoro-Acl703 claim 1 , fluoro-BMIPP claim 1 , fluoro-HAR claim 1 , fluoro-flutemetamol claim 1 , fluoro-MK-9470 claim 1 , fluoro-FACPC claim 1 , fluoro-CURB claim 1 , fluoro-MFES claim 1 , FES claim 1 , fluoro-2-ME claim 1 , fluoro-PHNO claim 1 , fluoro-PHNO claim 1 , fluoro-fallypride claim 1 , DMFP claim 1 , fluoro-5-OH-FPPAT claim 1 , fluoro-5-OH-DPAT claim 1 , fluoro-NPA claim 1 , fluoro-NNC112 claim 1 , fluoro-SCH claim 1 , fluoro-FDA claim 1 , fluoro-MNPA claim 1 , fluoro-MC113 claim 1 , fluoro-SA4503 ...

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Номер записи: 86
27-11-2014 дата публикации

NEW PROCESS FOR THE PREPARATION OF 2,4,5-TRIFLUOROPHENYLACETIC ACID

Номер: US20140350287A1
Автор: Caporale Andrea, De Lucchi Ottorino, Tartaggia Stefano
Принадлежит:

The present invention relates to a new process for the preparation of 2,4,5-trifluorophenylacetic acid and salts thereof by means of new synthetic intermediates. 2. Compound according to the in which in the compounds of formula (III) claim 1 , (IV) claim 1 , (V) claim 1 , (VI) and (VII) X is a chlorine atom.3. Compound according to in which in the compounds of formula (V) and (VI) X′ is a chlorine atom.4. Compound according to in which in the compounds of formula (V) and (VI) both X and X′ are a chlorine atom. This application claims priority to and is a divisional of U.S. Non-Provisional application entitled, “NEW PROCESS FOR THE PREPARATION OF 2,4,5-TRIFLUOROPHENYLACETIC ACID”, having Ser. No. 13/753,701, filed on Jan. 30, 2013, which claims benefit of Italian patent application MI2012A000114, filed Jan. 31, 2012, which both are entirely incorporated herein by reference.The present invention relates to a process for the preparation of 2,4,5-trifluorophenylacetic acid and salts thereof.Fluorophenylacetic acids are useful intermediates for the preparation of various pharmacologically active compounds. In particular trifluorophenylacetic acids are used in the preparation of inhibitors of the dipeptidyl peptidase-4 enzyme. These medicines are useful in treating diabetes, in particular type 2 diabetes (see for example WO 97/40832; WO 98/19998; U.S. Pat. No. 5,939,5606, 1163-1166 (1996); 6, 2745-2748 (1996))One of these active ingredients is Sitagliptin, available commercially under the brand name Januvia, which uses 2,4,5-trifluorophenylacetic acid as a key intermediate for its synthesis.US 20040068141 claims a process for the preparation of fluorophenylacetic acids starting from aromatic halides according to the method described in diagram 1 (X represents chlorine, bromine or iodine):The first step however requires the use of large quantities of copper salts, with obvious problems of extraction and disposal of the heavy metal, and the aromatic halide used often has ...

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Номер записи: 87
27-11-2014 дата публикации

COMPOSITION FOR TREATING DIABETES AND METABOLIC DISEASES AND A PREPARATION METHOD THEREOF

Номер: US20140350304A1
Автор: CHANG FANG-RONG, DU YING-CHI, Hsieh Chi-Ting, HSIEH TUSTY-JIUAN, Tsai Yi-Hong, WU YANG-CHANG
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

Disclosed is a chalcone composition for treating diabetes and metabolic syndromes. In particular, the chalcone compound bound with 2-halogen in ring A significantly decreases the blood glucose level in the in vitro anti-diabetic effect experiment. In the in vivo animal model, the leading chalcone compound can prevent the progression of diabetes and control the blood glucose level, and there is no significant difference in the gains in body weight. Throughout the seven-week administration, there are no hepatic or renal toxicity observed. 2. The composition according to claim 1 , wherein the halogen is selected from a group consisting of a fluoride claim 1 , a chloride claim 1 , a bromide and an iodine.3. The composition according to claim 1 , wherein one of the diabetes and the metabolic syndrome occurs in a subject.4. The composition according to claim 3 , wherein the subject is one of a human being and a rodent.5. The composition according to claim 3 , wherein the subject has a blood glucose value claim 3 , and the composition is effective in at least one treatment of regulating the blood glucose value and stabilizing the blood glucose value.6. The composition according to claim 3 , wherein the subject is subjected to at least one of an impaired glucose tolerance and a body weight gain claim 3 , and the composition is effective in inhibiting at least one of the impaired glucose tolerance claim 3 , the body weight gain and the accumulation of lipid droplets in adipocytes.7. The composition according to further being effective in at least one treatment of inhibiting the metabolic syndrome and delaying the metabolic syndrome.9. The composition according to claim 8 , wherein the body weight gain occurs in a subject.10. The composition according to claim 9 , wherein the subject is a mouse being continuously fed with a high fat diet and subjected to an impaired glucose intolerance claim 9 , and the high fat diet has at least 40 weight percentage of fat.11. The ...

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Номер записи: 88
06-08-2020 дата публикации

BENZIL MONOKETALS AND THE USE THEREOF

Номер: US20200247916A1
Автор: ENDERS Claudia, GNAUCK Steffen, Hahn Alexander, KIRSCH Peer, LEONHARD Peter, SCHUEPFER Sven, TONG Qiong, WEEGELS Leo
Принадлежит: Merck Patent GmBH

The present invention relates to the use of hydrophilic compounds of the formula I as photopolymerisation initiators of polymerisable substance mixtures which comprise unsaturated compounds, or for the photochemical crosslinking of linear polymers, 6. The process according to claim 1 , wherein the compounds of the formula I have an octan-1-ol/water partition coefficient of log P≤3.2.7. (canceled)9. The sealant according to claim 8 , that is photochemically curable.10. The sealant according to claim 9 , that is additionally thermally curable.12. A liquid-crystal display claim 8 , containing a sealant according to .13. A liquid-crystal display according to claim 12 , been produced by an ODF process.14. A liquid-crystal display according to claim 12 , that is a PS-VA claim 12 , PS-IPS claim 12 , PS-FFS claim 12 , PS-OCB or PS-TN display.15. The process according to claim 1 , comprising sealing a liquid crystalline display by said photopolymerization or crosslinking. The present invention relates to the use of hydrophilic benzil monoketals as photoinitiators in heat- and light-curing sealants, to the use of these sealants in a one drop filling (ODF) process for the production of liquid-crystal displays, to sealants which comprise the hydrophilic photoinitiators, to novel hydrophilic photoinitiators, and to the liquid-crystal displays produced using these sealants.Liquid crystals have found a broad range of applications since the first commercially usable liquid-crystalline compounds were found about 30 years ago. Known areas of application were initially, in particular, displays for watches and calculators, before the first displays for, for example, portable and desktop computers came out.The increasing popularity of liquid-crystal display devices (LCDs) resulted in rapid technical development and is attributable, in particular, to the fact that LCDs, compared with the previously prevailing technology of cathode ray tubes, have low power consumption, a lightweight ...

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Номер записи: 89
04-12-2014 дата публикации

MULTIFUNCTIONAL DEOXYBENZOIN-BASED MONOMERS AND RESINS HAVING REDUCED FLAMMABILITY

Номер: US20140357829A1
Автор: Emrick Todd, Szyndler Megan Warner, Timmons Justin
Принадлежит:

The invention provides a novel platform for minimal- or non-flammable polymers, which is based purely on hydrocarbon systems and does not need additives of any kind A key feature is that the hydrocarbons disclosed herein are characterized by degradation mechanisms that produce few flammable volatiles. For example, 2,4,4′,6-tetrahydroxydeoxybenzoin is employed as a multifunctional cross-linker in conjunction with bis-epoxydeoxybenzoin, affording new resins that combine excellent physical and mechanical properties with low flammability. 2. The compound of claim 1 , wherein i is 2 or 3 claim 1 , j is 1.3. The compound of claim 2 , wherein each of Rand Ris H.5. The compound of claim 4 , wherein each R is H.9. The polymer of claim 8 , wherein i is 2 or 3 claim 8 , j is 1.10. The polymer of claim 9 , wherein each of Rand Ris H.12. The polymer of claim 11 , wherein each R is H.16. The minimal- or non-flammable composition of claim 15 , wherein i is 2 or 3 claim 15 , j is 1.17. The minimal- or non-flammable composition of claim 16 , wherein each of Rand Ris H.19. The minimal- or non-flammable composition of claim 15 , wherein each R is H. This application claims the benefit of U.S. Provisional Application No. 61/824,476, filed May 17, 2013, the entire content of which is incorporated herein by reference in its entirety.The United States Government has certain rights to the invention pursuant to Grant No. 09-G-013 from Federal Aviation Administration, to the University of Massachusetts.The invention relates to flame retardant polymers. More particularly, the invention relates to cross-linked, deoxybenzoin-based resins, and related methods and uses thereof.Polymers are a mainstay of modern society, for example, widely used in fabricating textiles, upholstery, construction materials, various air, land or sea vehicles, and microelectronic devices and appliances. The inherent flammability of many polymers poses a significant threat, especially in enclosed or isolated spaces. ...

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Номер записи: 90
28-09-2017 дата публикации

Series of Skin Whitening (Lightening) Compounds

Номер: US20170275224A1
Автор: Hertel Carmen, Liu Jiyun, Nandy Sandip K., Nesterov Alexandre Mikhailovitch, Papmapiya Abeysinghe Arrachchigae
Принадлежит: Unigen, Inc.

The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin. 132-: (canceled)34. The compound of claim 33 , wherein R═R═H and Ris selected from 1′-(3′ claim 33 ,5′-dimethoxy)phenyl; 1′-(3′ claim 33 ,5′-dihydroxy)phenyl; 1-(2′ claim 33 ,4′ claim 33 ,6-trimethoxyphenyl); R=Me claim 33 , R═OH claim 33 , and Ris 1′-(2′ claim 33 ,4′-dihydroxy)phenyl; R=Me claim 33 , R═O claim 33 , and Ris 1′-(2′ claim 33 ,4′-dihydroxy)phenyl; and R═R═H claim 33 , R—CHCHOH.35. The compound of selected from the group consisting of 4-(3-(3 claim 33 ,5-dimethoxyphenyl)propyl)benzene-1 claim 33 ,3-diol (28) claim 33 , 4-(3-(3 claim 33 ,5-dimethoxyphenyl)-1-hydroxypropyl)benzene-1 claim 33 ,3-diol (29) claim 33 , 4-(3-(3 claim 33 ,5-dihydroxyphenyl)propyl)benzene-1 claim 33 ,3-diol (30) claim 33 , 4-(3-(2 claim 33 ,4 claim 33 ,6-trimethoxyphenyl)propyl)benzene-1 claim 33 ,3-diol (31) claim 33 , 4-(3-(2 claim 33 ,4-dihydroxyphenyl)propyl)-2-methylbenzene-1 claim 33 ,3-diol (32) claim 33 , 4-(3-(2 claim 33 ,4-dihydroxy-3-methylphenyl)-3-(2 claim 33 ,4-dihydroxyphenyl)propane-1-one (33) claim 33 , 4-(5-hydroxypentyl)benzene-1 claim 33 ,3-diol (34).36. A composition of matter comprising the compound of .37. The composition of matter of claim 36 , wherein the compound is selected from the group consisting of compounds 4-(3-(3 claim 36 ,5-dimethoxyphenyl)propyl)benzene-1 claim 36 ,3-diol (28) claim 36 , 4-(3-(3 claim 36 ,5-dimethoxyphenyl)-1-hydroxypropyl)benzene-1 claim 36 ,3-diol (29) claim 36 , 4-(3-(3 claim 36 ,5-dihydroxyphenyl)propyl)benzene-1 claim 36 ,3-diol (30) claim 36 , 4-(3-(2 claim 36 ,4 claim 36 ,6-trimethoxyphenyl)propyl)benzene-1 claim 36 ,3-diol (31) claim ...

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Номер записи: 91
20-08-2020 дата публикации

New Process for the Manufacture of Fluorinated Benzenes and Fluorinated Benzophenones, and Derivatives Thereof

Номер: US20200262776A1
Автор: DU Hongjun, Wu Wenting, Zhou Changyue
Принадлежит: Fujian Yongjing Technology Co., Ltd

The invention relates to a new process for the manufacture or synthesis, respectively, of fluorinated benzenes and fluorinated benzophenones, and derivatives thereof, in particular of fluorobenzenes and derivatives thereof. The present invention particularly pertains to a novel environmentally friendly process for the synthesis of fluorinated benzenes and benzophenones as raw materials for the manufacture of polyaryletherketones (PAEKs). 1. A process of preparing a compound , in particular a compound comprising one or more aromatic rings , by Friedel-Crafts reaction , characterized in that an aromatic ring of a starting material compound that serves as a precursor of a PAEK , is reacted with a Friedel-Crafts reagent in the presence of an antimony pentahalide catalyst (SbHal) , preferably in the presence of an activated antimony pentahalide catalyst (SbHal) , optionally activated by hydrogen fluoride (HF).2. The process of preparing a compound according to claim 1 , wherein the compound prepared is a fluorinated compound.4. The process of preparing a compound according to claim 1 , wherein the starting material compound is selected from compounds having the formula (I) as defined in claim 1 ,whereinRn independently denotes a single substituent selected from the group consisting of hydrogen (H), fluorine (F), or chlorine (Cl); andHal denotes a halogen selected from fluorine (F) or chlorine (Cl), preferably chlorine (Cl).5. The process of preparing a compound according to claim 3 , wherein the starting material compound is selected from the group of compounds consisting of compounds wherein one of Rn claim 3 , preferably a Rn in para-position (4-Rn) claim 3 , is fluorine (F) or chlorine (Cl) claim 3 , and the others of Rn are hydrogen claim 3 , and Hal is fluorine (F) or chlorine (Cl); preferably wherein the starting material compound is selected from the group of compounds consisting of the compounds chlorobenzene claim 3 , dichlorobenzene claim 3 , preferably 1 claim ...

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Номер записи: 92
25-11-2021 дата публикации

Method for manufacturing 1,4-bis (4-phenoxybenzoyl)benzene at an elevated temperature

Номер: US20210363088A1
Автор: Guillaume Le, Julien Jouanneau, Martin Herblot
Принадлежит: Arkema France SA

A method for manufacturing 1,4-bis(4-phenoxybenzoyl)benzene, including: providing a solvent, a Lewis acid, a first reactant and a second reactant, wherein the first reactant and the second reactant are respectively terephthaloyl chloride and diphenyl ether, or reversely; mixing the first reactant in the solvent to make a starting mixture; and, adding the second reactant to the starting mixture; wherein the Lewis acid is mixed, at least partly, to the starting mixture before adding the second reactant to the starting mixture, and/or wherein the Lewis acid is mixed, at least partly, with the second reactant and added together to the starting mixture, and wherein the temperature of the starting mixture is greater than 5° C. during at least part of the step of adding the second reactant to the starting mixture; so as to obtain a product mixture comprising a 1,4-bis(4-phenoxybenzoyl)benzene-Lewis acid complex.

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Номер записи: 93
12-09-2019 дата публикации

CALIXARENE COMPOUND AND CURABLE COMPOSITION

Номер: US20190276421A1
Автор: Imada Tomoyuki, Miyamoto Masanori, Yamamoto Shinya
Принадлежит:

A compound useful as a release agent, and a release agent, a curable composition, and a nanoimprint lithography resin material each containing the compound are provided. More specifically, a calixarene compound with a molecular structure represented by the following structural formula (1) and a composition containing the calixarene compound are provided. 2. (canceled)3. The release agent that is the calixarene compound according to claim 1 , wherein Rin the structural formula (1) denotes a structural moiety represented by the following structural formula (2).{'br': None, '[Chem. 2]'}{'br': None, 'sup': 4', '4', 'F, '—R—Y—R—R\u2003\u2003(2)'}{'sup': 4', 'F, '(wherein Rindependently denotes a direct bond or an alkylene group having 1 to 6 carbon atoms, Rdenotes a perfluoroalkyl group, and Y denotes a direct bond, a carbonyl group, an oxygen atom, or a sulfur atom)'}4. The release agent that is the calixarene compound according to claim 1 , wherein Rdenotes a hydroxy group claim 1 , a thiol group claim 1 , or a structural moiety with a hydroxy group claim 1 , an amino group claim 1 , a carboxy group claim 1 , a thiol group claim 1 , a phosphate group claim 1 , a phosphonate group claim 1 , a phosphinate group claim 1 , or an alkoxysilyl group.5. The release agent that is the calixarene compound according to claim 1 , wherein Rdenotes a vinyloxy group claim 1 , an ethynyloxy group claim 1 , a (meth)acryloyloxy group claim 1 , a glycidyloxy group claim 1 , a (2-methyl)glycidyloxy group claim 1 , a 3-alkyloxetanylmethyloxy group claim 1 , or a structural moiety with a vinyl group claim 1 , a vinyloxy group claim 1 , an ethynyl group claim 1 , an ethynyloxy group claim 1 , a (meth)acryloyl group claim 1 , a (meth)acryloyloxy group claim 1 , a glycidyl group claim 1 , a glycidyloxy group claim 1 , a (2-methyl)glycidyl group claim 1 , a (2-methyl)glycidyloxy group claim 1 , a 3-alkyloxetanylmethyl group claim 1 , or a 3-alkyloxetanylmethyloxy group.6. (canceled)7. A curable ...

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Номер записи: 94
04-10-2018 дата публикации

RESIST UNDERLAYER FILM COMPOSITION, PATTERNING PROCESS, AND METHOD FOR FORMING RESIST UNDERLAYER FILM

Номер: US20180284615A1
Автор: KORI Daisuke, NAGAI Hiroko, OGIHARA Tsutomu, WATANABE Takeru
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

Provided is a resist underlayer film composition which is excellent in resistance to a basic hydrogen peroxide aqueous solution, in gap-filling and planarization characteristics, and in dry etching characteristic, wherein the resist underlayer film composition is used for a multilayer resist method, comprising: (A1) a polymer (1A) comprising one, or two or more, of a repeating unit represented by following general formula (1); (A2) one, or two or more, of a polyphenol compound having a formula weight of 2,000 or less and not having a 3,4-dihydroxy phenyl group; and (B) an organic solvent. 5. The resist underlayer film composition according to claim 1 , wherein a weight average molecular weight of the polymer (1A) is in a range of 1 claim 1 ,000 to 20 claim 1 ,000.6. The resist underlayer film composition according to claim 1 , wherein the resist underlayer film composition further contains one or more additives out of (C) an acid generator claim 1 , (D) a surfactant claim 1 , (E) a crosslinking agent claim 1 , (F) a plasticizer claim 1 , and (G) a pigment.7. The resist underlayer film composition according to claim 1 , wherein the resist underlayer film composition is the resist underlayer film composition which gives a resist underlayer film having a resistance to an ammonia-containing hydrogen peroxide aqueous solution.8. The resist underlayer film composition according to claim 7 , wherein the resist underlayer film is the resist underlayer film which does not show any peel-off when a silicon substrate formed with the resist underlayer film is soaked into a 1.0% by mass hydrogen peroxide aqueous solution containing 0.5% by mass of ammonia at 70° C. for 5 minutes.9. A patterning process claim 7 , wherein the patterning process is to form a pattern on a substrate to be processed and comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(I-1) forming a resist underlayer film on the substrate to be processed by using the resist underlayer film composition ...

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Номер записи: 95
22-10-2015 дата публикации

MONOMER, HARD MASK COMPOSITION COMPRISING SAID MONOMER, AND METHOD FOR FORMING PATTERN USING SAID HARD MASK COMPOSITION

Номер: US20150301448A1
Автор: Cho Youn-Jin, KIM Hea-Jung, Lee Chul-Ho, LEE Sung-jae, PARK Yo-Choul, PARK You-Jung, YOON Yong-Woon
Принадлежит: CHEIL INDUSTRIES INC.

Disclosed are a monomer for a hardmask composition represented by the Chemical Formula 1, a hardmask composition including the monomer, and a method of forming a pattern using the same. 3. The monomer of claim 1 , wherein at least one of Ato Ais a polycyclic aromatic group.5. The monomer of claim 1 , wherein the monomer has a molecular weight of about 200 to about 5 claim 1 ,000.8. The hardmask composition of claim 6 , wherein at least one of Ato Ais a polycyclic aromatic group.10. The hardmask composition of claim 6 , wherein the monomer has a molecular weight of 200 to 5 claim 6 ,000.11. The hardmask composition of claim 6 , wherein the monomer is included in an amount of 0.1 to about 50 wt % based on the total amount of the hardmask composition.12. A method of forming a pattern claim 6 , comprising:providing a material layer on a substrate,{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'applying the hardmask composition according to on the material layer,'}heat-treating the hardmask composition to provide a hardmask layer,forming a silicon-containing thin layer on the hardmask layer,forming a photoresist layer on the silicon-containing thin layer,forming a photoresist pattern by exposing and developing the photoresist layer,selectively removing the silicon-containing thin layer and the hardmask layer using the photoresist pattern to expose a part of the material layer, andetching an exposed part of the material layer.13. The method of claim 12 , wherein the hardmask composition is applied using a spin-on coating method. A monomer, a hardmask composition including the monomer, and a method of forming patterns using the hardmask composition are disclosed.Recently, the semiconductor industry has developed to an ultra-fine technique having a pattern of several to several tens nanometer size. Such ultrafine technique essentially needs effective lithographic techniques.The typical lithographic technique includes providing a material layer on a semiconductor ...

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Номер записи: 96
11-10-2018 дата публикации

COMPOSITIONS OF POLYHYDROXYLATED BENZOPHENONES AND METHODS OF TREATMENT OF NEURODEGENERATIVE DISORDERS

Номер: US20180290960A1
Автор: Haggarty Stephen, PAO Ping-Chieh, Patnaik Debasis, Tsai Li-Huei
Принадлежит:

The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity. 87. The compound of claim , wherein each of R , R , R , R , Rand Ris CO(C-Calkyl).97. The compound of claim , wherein each of R , R , R , R , Rand Ris CO(Calkyl).12. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.13. A method of treating a disease associated with a deficiency in HDAC1 deacetylase activity comprising administering to a patient in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt or prodrug thereof.14. The method of claim 13 , wherein the compound activates HDAC1 deacetylase activity.15. The method of claim 13 , wherein the compound increases the expression of genes involved in cytokine responses claim 13 , neurogenesis claim 13 , and/or central nervous system development.16. The method of claim 15 , wherein the genes involved in cytokine responses are genes involved in interferon (IFN)-γ and/or IFN-β responses.17. The method of claim 13 , wherein the disease is a neurodegenerative disease claim 13 , neurological disorder claim 13 , psychiatric disorder claim 13 , or cognitive deficit.18. The method of claim 13 , wherein the disease is a dementia or amytrophic lateral sclerosis (ALS).19. The method of claim 18 , wherein the dementia is Alzheimer's disease claim 18 , frontotemporal dementia claim 18 , or Parkinson's disease.20. The method of claim 13 , wherein the disease is major depression claim 13 , bipolar disorder claim 13 , and schizophrenia.21. The method of claim 13 , wherein administering is performed orally claim 13 , parenterally claim 13 , intranasally claim 13 , subcutaneously claim 13 , by injection claim 13 , or by infusion.23. A method of activating HDAC1 activity comprising contacting a cell with a ...

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Номер записи: 97
27-10-2016 дата публикации

ACTIVATORS OF MYOSIN II FOR MODULATING CELL MECHANICS

Номер: US20160311764A1
Автор: ROBINSON DOUGLAS, Surcel Alexandra
Принадлежит:

The present invention discloses small molecule compounds as activators of myosin II by promoting its assembly and recruitment to contractile structures in the cell and methods of using such compounds. These compounds are useful to modulate cell and tissue mechanics. This class of molecules, which affect cell mechanics either by activating the contractile system of the cell or modulating cytokinesis, will be used for therapeutic and tissue engineering applications. 2. The method of claim 1 , wherein the method of administering is systemic delivery selected from the group consisting of oral claim 1 , parenteral claim 1 , intranasal claim 1 , sublingual claim 1 , rectal claim 1 , and transdermal administration.4. The method of claim 3 , wherein the method of administering is systemic delivery selected from the group consisting of oral claim 3 , parenteral claim 3 , intranasal claim 3 , sublingual claim 3 , rectal claim 3 , and transdermal administration.6. The method of claim 5 , wherein the method of administering is systemic delivery selected from the group consisting of oral claim 5 , parenteral claim 5 , intranasal claim 5 , sublingual claim 5 , rectal claim 5 , and transdermal administration.8. The method of claim 7 , wherein the method of administering is systemic delivery selected from the group consisting of oral claim 7 , parenteral claim 7 , intranasal claim 7 , sublingual claim 7 , rectal claim 7 , and transdermal administration.10. The compound of claim 9 , wherein the compound is administered by systemic delivery selected from the group consisting of oral claim 9 , parenteral claim 9 , intranasal claim 9 , sublingual claim 9 , rectal claim 9 , and transdermal administration.12. The compound of claim 11 , wherein the compound is administered by systemic delivery selected from the group consisting of oral claim 11 , parenteral claim 11 , intranasal claim 11 , sublingual claim 11 , rectal claim 11 , and transdermal administration.14. The compound of claim 13 ...

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Номер записи: 98
26-10-2017 дата публикации

PROCESS FOR THE PREPARATION OF 1-(3,5-DICHLORO-4-FLUORO-PHENYL)-2,2,2-TRIFLUORO-ETHANONE

Номер: US20170305828A1
Автор: SMITS HELMARS
Принадлежит: SYNGENTA PARTICIPATIONS AG

The invention relates to a process for the preparation of a compound of formula I comprising a) reacting a compound of formula II in the presence of magnesium or an organometallic reagent of formula III RMX (III), wherein Ris C-Calkyl; Mis Li or Mg and X is halogen or absent; with a compound of formula IV CF-C(O)-R(IV), wherein Ris halogen, hydroxyl, C-Calkoxy, (di-C-Calkyl)amino, OC(O)CF, phenoxy or OM; wherein Mis Lithium, Magnesium, Sodium or Potassium; to a compound of formula V, and b) reacting the compound of formula V with alkali metal fluoride in the presence of catalytic amounts of a phase transfer catalyst in the presence of a polar solvent to the compound of formula I. 3. A process according to claim 2 , wherein the organometallic reagent is isopropylmagnesiumchloride complexed with LiCl.4. A process according to claim 1 , wherein the alkali metal fluoride is selected from KF claim 1 , LiF and NaF.5. A process according to claim 1 , wherein the phase transfer catalyst is selected from the group consisting of phosphonium salts of general formula (R)PX and ammonium salts of general formula (R)NX wherein Ris C-Calkyl or phenyl and X is halogen.6. A process according to claim 1 , wherein the polar solvent is selected from the group consisting of sulfolane claim 1 , dimethylformamide and dimethylsulfoxide.8. A process according to claim 7 , wherein the organometallic reagent is isopropylmagnesiumchloride complexed with LiCl. The present invention relates to the preparation of 1-(3,5-dichloro-4-fluoro-phenyl)-2,2,2-trifluoro-ethanone using 5-bromo-1,2,3-trichloro-benzene as a starting material.1-(3,5-dichloro-4-fluoro-phenyl)-2,2,2-trifluoro-ethanone is an important intermediate for the preparation of pesticidally active isoxazoline-substituted benzamides as for example disclosed in EP 1932836A1.1-(3,5-dichloro-4-fluoro-phenyl)-2,2,2-trifluoro-ethanone can be advantageously prepared by using 5-bromo-1,2,3-trichloro-benzene as a starting material. 5-bromo-1,2,3- ...

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Номер записи: 99
26-10-2017 дата публикации

PHOSPHONIUM-BASED COMPOUND, EPOXY RESIN COMPOSITION CONTAINING SAME, SEMICONDUCTOR DEVICE MANUFACTURED USING SAME

Номер: US20170306079A1
Автор: CHEON Jin Min, CHOI Jin Woo, CHUNG Joo Young, KIM Min Gyum, KWON Ki Hyeok, Lee Dong Hwan
Принадлежит:

The present invention relates to a phosphonium-based compound represented by chemical formula 1, an epoxy resin composition containing the same, and a semiconductor device manufactured by using the same. 2. The phosphonium compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare a Cto Caryl group.3. The phosphonium compound according to claim 2 , wherein at least one of R claim 2 , R claim 2 , R claim 2 , and Ris substituted with a hydroxyl group.4. The phosphonium compound according to claim 1 , wherein X is a Cto Caryl group.6. An epoxy resin composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an epoxy resin, a curing agent, an inorganic filler, and a curing catalyst, the curing catalyst including the phosphonium compound according to .'}7. The epoxy resin composition according to claim 6 , wherein the epoxy resin includes one or more of a bisphenol A type epoxy resin claim 6 , a bisphenol F type epoxy resin claim 6 , a phenol novolac type epoxy resin claim 6 , a tert-butyl catechol type epoxy resin claim 6 , a naphthalene type epoxy resin claim 6 , a glycidyl amine type epoxy resin claim 6 , a cresol novolac type epoxy resin claim 6 , a biphenyl type epoxy resin claim 6 , a linear aliphatic epoxy resin claim 6 , a cycloaliphatic epoxy resin claim 6 , a heterocyclic epoxy resin claim 6 , a spiro ring-containing epoxy resin claim 6 , a cyclohexane dimethanol type epoxy resin claim 6 , a trimethylol type epoxy resin claim 6 , or a halogenated epoxy resin.8. The epoxy resin composition according to claim 6 , wherein the curing agent includes a phenol resin.9. The epoxy resin composition according to claim 6 , wherein the curing agent includes one or more of a phenolaralkyl type phenol resin claim 6 , a phenol novolac type phenol resin claim 6 , a xyloc type phenol resin claim 6 , a cresol novolac type phenol resin claim 6 , a naphthol type phenol resin claim 6 , a terpene type phenol resin claim 6 , a ...

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Номер записи: 100