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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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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 14840. Отображено 100.
15-03-2012 дата публикации

Methods of making lubiprostone and intermediates thereof

Номер: US20120065409A1
Автор: Alfredo Paul Ceccarelli, Bhaskar Reddy Guntoori, Fan Wang, Kaarina K. Milnes, Kevin Wade Kells, Kiran Kumar Kothakonda, Laura Kaye Montemayor, Minh T. N. Nguyen, Sammy Chris Duncan, Uma Kotipalli, Yajun Zhao
Принадлежит: Apotex Pharmachem Inc

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

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Номер записи: 1
17-05-2012 дата публикации

Method for making a peroxycarboxylic acid

Номер: US20120122980A1
Автор: Dan N. Tallman, David D. McSherry, Junzhong Li, Keith E. Lokkesmeo, Richard K. Staub
Принадлежит: ECOLAB USA INC

The present invention relates to apparatus and methods for making a peroxycarboxylic acid. The apparatus includes a reaction catalyst and a guard column for pretreating one or more reagents, which can increase the life, activity, and/or safety of the reaction catalyst. The peroxycarboxylic acid compositions made by the method and apparatus can include one or more peroxycarboxylic acids.

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Номер записи: 2
05-07-2012 дата публикации

GENERATION OF PEROXYCARBOXYLIC ACIDS AT ALKALINE pH, AND THEIR USE AS TEXTILE BLEACHING AND ANTIMICROBIAL AGENTS

Номер: US20120172439A1
Автор: David D. McSherry, Johannes G. Winter, Jonathan P. Fast, Junzhong Li, Peter J. Forth, Richard Staub, Robert D.P. Hei, Thomas J. Dürrschmidt, Thomas Merz
Принадлежит: ECOLAB USA INC

The present disclosure provides methods for generating percarboxylic acid compositions and/or peroxycarboxylic acid compositions formed external to a point of use in non-equilibrium reactions for use in certain bleaching and antimicrobial applications, in particular laundry applications. The compositions are generated external to a point of use, at alkaline pH levels, viz. greater than about pH 12, and optionally suitable for use with detergents and/or surfactants for synergistic bleaching efficacy. Methods of bleaching and/or disinfecting are further provided.

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Номер записи: 3
12-07-2012 дата публикации

Process For Producing Cyclohexylbenzene

Номер: US20120178969A1
Автор: Jane C. Cheng, Prasenjeet Ghosh, Tan-Jen Chen
Принадлежит: ExxonMobil Chemical Patents Inc

In a process for producing cyclohexylbenzene, benzene and hydrogen are contacted under hydroalkylation conditions with a catalyst system comprising a MCM-22 family molecular sieve and at least one hydrogenation metal. The conditions comprise a temperature of about 140° C. to about 175° C., a pressure of about 135 psig to about 175 psig (931 kPag to 1207 kPag), a hydrogen to benzene molar ratio of about 0.30 to about 0.65 and a weight hourly space velocity of benzene of about 0.26 to about 1.05 hr −1 .

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Номер записи: 4
20-09-2012 дата публикации

Anti-constipation composition

Номер: US20120237598A1
Автор: Ryuji Ueno
Принадлежит: SUCAMPO AG

An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X 1 and X 2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.

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Номер записи: 5
08-11-2012 дата публикации

Process for preparing alkyl hydroperoxide compounds

Номер: US20120283482A1
Автор: Fabien Bellenger, Laurent Diguet, Stéphane Streiff
Принадлежит: Rhodia Operations SAS

A method for making alkyl hydroperoxide compounds, specifically the preparation of cyclohexyl hydroperoxide is described. The preparation of cyclohexyl hydroperoxide by means of the oxidation of cyclohexane by oxygen in a multi-stage reactor or in reactors connected in series is also described. In these methods, the reactor surfaces in contact with the oxidation medium can be protected by a layer of heat-resistant PFA polymer.

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Номер записи: 6
21-02-2013 дата публикации

Process for the production of an alkyl hydroperoxide

Номер: US20130046115A1
Автор: Françoise Igersheim, Serge Veracini, Stéphane Streiff
Принадлежит: Rhodia Operations SAS

A method for preparing an alkyl hydroperoxide obtained by the oxidation of a saturated hydrocarbon using oxygen, preferably of a saturated cyclic hydrocarbon, is described. Also described, is a method for preparing cyclohexyl hydroperoxide by oxidizing cyclohexane with molecular oxygen or a gas containing molecular oxygen preferably in the absence of a catalyst.

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Номер записи: 7
14-03-2013 дата публикации

PROCESS FOR PRODUCTION OF HIGH PURITY BETA-CAROTENE AND LYCOPENE CRYSTALS FROM FUNGAL BIOMASS

Номер: US20130066124A1
Автор: Anandane Arnaud, Joseph Suresh
Принадлежит:

The present invention relates to a simple and economic method of extracting a crystalline Carotenoid compound, such as Beta-carotene, Lycopene, with a purity of at least 99%. The present invention further describes a process to prepare such a highly pure crystalline Carotenoid compound from microbial biomass, using an Anti-purity compound removal process followed by a mono-solvent extraction method. Further the process describes value addition of the co-products recovered during the extraction process thus resulting in a highly economical industrial method for the production of such high purity crystalline Carotenoids compound. 1. A method of extraction of high purity carotenoids from fungal biomass , said method comprising the steps of:a) treatment of carotenoid containing biomass by acidified alcohol;b) separating mechanically the treated biomass from step a) to obtain solid biomassc) extracting the treated biomass (the beta-carotene or lycopene) with an organic solvent;d) filtering the extracted mixture of step c) to recover mother liquor containing carotenoids crystals and the spent biomass;e) repeating the extraction of the spent biomass again with the same solvent;f) filtering the second extracted mixture obtained from the above step to recover mother liquor and the spent biomass;g) recovering pure crystals from the pooled mother liquor obtained from step d) and step f) under chilling conditions by a chilling crystallization method;h) filtering the chilled suspension to get high purity beta-carotene or lycopene crystals; andj) concentrating further the spent mother liquor from step g) with traces of carotenoid to produce oleoresin comprising beta-carotene or lycopene.2. The method of extraction according to wherein the purity of the obtained beta-carotene crystals is 99% or more.3. The method of extraction according to wherein the purity of the obtained lycopene crystals is 99.9%4Blakeslea. The method of extraction according to wherein the fungal biomass used ...

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Номер записи: 8
21-03-2013 дата публикации

RETINAL DERIVATIVES AND METHODS FOR THE USE THEREOF FOR THE TREATMENT OF VISUAL DISORDERS

Номер: US20130072559A1
Автор: Batten Matthew, PALCZEWSKI Krzysztof
Принадлежит: UNIVERSITY OF WASHINGTON

Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided. 184-. (canceled)85. A retinyl ester selected from the group consisting of a 9-cis-retinyl ester and an 11-cis-retinyl ester , wherein the ester substituent comprises a carboxylate radical of a Cto Cpolycarboxylic acid , with the proviso that the ester substituent is not tartarate.86. The retinyl ester of claim 85 , which is a 9-cis-retinyl ester of a Cto Cpolycarboxylate.87. The retinyl ester of claim 85 , which is a 9-cis-retinyl ester of a Cto Cpolycarboxylate.88. The retinyl ester of claim 85 , wherein the 9-cis-retinyl ester is 9-cis-retinyl succinate claim 85 , 9-cis-retinyl citrate claim 85 , 9-cis-retinyl ketoglutarate claim 85 , 9-cis-retinyl fumarate claim 85 , 9-cis-retinyl malate or 9-cis-retinyl oxaloacetate.89. The retinyl ester of claim 88 , wherein the 9-cis-retinyl ester is 9-cis-retinyl succinate.90. The retinyl ester of claim 85 , which is an 11-cis-retinyl ester of a Cto Cpolycarboxylate.91. The retinyl ester of claim 85 , which is an 11-cis-retinyl ester of a Cto Ccarboxylate.92. The retinyl ester of claim 90 , wherein the 11-cis-retinyl ester is 11-cis-retinyl succinate claim 90 , 11-cis-retinyl citrate claim 90 , 11-cis-retinyl ketoglutarate claim 90 , 11-cis-retinyl fumarate claim 90 , 11-cis-retinyl malate or 11-cis-retinyl oxaloacetate.93. A pharmaceutical ophthalmological composition claim 90 , comprising:{'sub': 3', '22, 'a synthetic retinyl ester and a pharmaceutically acceptable vehicle, wherein the synthetic retinyl ester is a 9-cis-retinyl ester or an 11-cis-retinyl ester, wherein the ester substituent comprises a carboxylate radical of a Cto Cpolycarboxylic acid.'}94. The pharmaceutical ophthalmological composition of claim 93 , wherein the composition is formulated for local administration to an eye of a human subject.95. The pharmaceutical ophthalmological composition of claim 93 , wherein the composition is ...

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Номер записи: 9
21-03-2013 дата публикации

PROSTAGLANDIN SYNTHESIS AND INTERMEDIATES FOR USE THEREIN

Номер: US20130072695A1
Автор: ALBERICO Dino, CLAYTON Joshua, GORIN Boris Ivanovich, OUDENES Jan
Принадлежит: Alphora Research Inc.

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

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Номер записи: 10
28-03-2013 дата публикации

DIBENZOYL PEROXIDE DERIVATIVES, PREPARATION METHOD THEREOF AND COSMETIC OR DERMATOLOGICAL COMPOSITIONS CONTAINING SAME

Номер: US20130079544A1
Автор: BOUIX-PETER Claire, Pascal Jean-Claude, RODEVILLE Nicolas
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

The use of compounds in the treatment of skin disorders is described. In particular, compounds having the general formula (I): 4. The compound according to claim 1 , wherein the compound is selected from the group consisting of:(2-acetoxy-5-octanoylbenzoyl)benzoyl peroxide;(2-ethoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-propionyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-butyryloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-isobutyryloxy-5-octanoylbenzoyl)benzoyl peroxide;[2-(2,2-dimethylpropionyloxy)-5-octanoylbenzoyl]benzoyl peroxide;(2-pentanoyloxy-5-octanoylbenzoyl)benzoyl peroxide;[2-(2-methylbutyryloxy)-5-octanoylbenzoyl]benzoyl peroxide;[2-(3-methylbutyryloxy)-5-octanoylbenzoyl]benzoyl peroxide;(2-hexanoyloxy-5-octanoylbenzoyl)benzoyl peroxide;[2-(2-ethylbutyryloxy)-5-octanoylbenzoyl]benzoyl peroxide;[2-(3,3-di methylbutyryloxy)-5-octanoylbenzoyl]benzoyl peroxide;(2-heptanoyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-octanoyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-nonanoyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-cyclopropanecarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-cyclobutanecarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-cyclopentanecarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-cyclohexanecarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-benzoyloxy-5-octanoylbenzoyl)benzoyl peroxide;[2-(adamantane-1-carbonyloxy)-5-octanoylbenzoyl]benzoyl peroxide;[2-(2-adamantan-1-ylacetoxy)-5-octanoylbenzoyl]benzoyl peroxide;(2-methoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-propoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-isopropoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-tert-butoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-butoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-sec-butoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-isobutoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;(2-pentoxycarbonyloxy-5-octanoylbenzoyl)benzoyl peroxide;[2-(1-ethylpropoxycarbonyloxy)-5-octanoylbenzoyl]benzoyl peroxide;[2-( ...

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Номер записи: 11
25-04-2013 дата публикации

2-methylene-vitamin d analogs and their uses

Номер: US20130102573A1
Автор: Hector F. DeLuca, Izabela Sibilska, Lori A. Plum, Rafal R. Sicinski
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-vitamin D 3 and (20R)-25-hydroxy-2-methylene-vitamin D 3 , as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.

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Номер записи: 12
09-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF OXOVINYLIONOL AND ITS O-PROTECTED DERIVATIVES

Номер: US20130116473A1
Автор: BENSON Stefan, Ernst Hansgeorg, PUHL Michael, SIEGEL Wolfgang
Принадлежит: BASF SE

The present invention relates to the preparation of oxovinylionol and its O-protected derivatives of the formula I 123.-. (canceled)25. The process according to claim 24 , wherein the oxidant comprises an organic hydroperoxide which is selected from among alkyl hydroperoxides and arylalkyl hydroperoxides.26. The process according to claim 25 , wherein the organic hydroperoxide is selected from among tertiary C-C-alkyl hydroperoxides.27. The process according to claim 24 , wherein the oxidant is employed in an amount of from 1 to 10 mol per mole of the compound of the formula II.28. The process according to claim 24 , wherein the transition metal is employed in the form of a transition metal compound.29. The process according to claim 24 , wherein the transition metal is selected from among Cu claim 24 , Co claim 24 , Fe and Mn and their mixtures.30. The process according to claim 29 , wherein the transition metal is employed in the form of at least one compound which is selected from among CuCl claim 29 , CuCl claim 29 , CuI claim 29 , CoCl claim 29 , Cu(II)oxalate claim 29 , Co(II) salts of organic monocarboxylic acids claim 29 , such as Co(acetate) claim 29 , Co(2-ethylhexanoate)or Co(naphthenate) claim 29 , Co(II)oxalate claim 29 , Co(acac) claim 29 , Co(acac) claim 29 , Co(salen) claim 29 , Co(salen)Cl claim 29 , Mn(salen) and Mn(salen)Cl claim 29 , and Mn(acac) claim 29 , where acac is acetylacetonate and salen is the N claim 29 ,N′-bis(salicylidene)ethylenediamino ligand.31. The process according to claim 24 , wherein the at least one transition metal is employed in a total amount of from 5×10to 0.5 mol per mole of the compound of the formula II.32. The process according to claim 24 , wherein the reaction with the oxidant is carried out in the presence of a complex ligand which has at least one nitrogen atom suitable for coordination with the transition metal.33. The process according to claim 34 , wherein the ligand has at least one group suitable for ...

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Номер записи: 13
20-06-2013 дата публикации

1-DEOXY ANALOGS OF 1,25-DIHYDROXYVITAMIN D3 COMPOUNDS

Номер: US20130157987A1
Автор: Hess Lindsey C., Kalinda Alvin S., Petkovich P. Martin, Posner Gary H., Saha Uttam, Slack Rachel D.
Принадлежит:

This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases. 2. The compound of claim 1 , whereinn is 0 or 1;{'sup': '1', 'Ris OH or halo;'}{'sup': 2', '3, 'sub': '2', 'Rand Rare either both H or together form ═CH;'}{'sup': '4', 'sub': '1-4', 'Ris Calkyl;'}{'sup': 5', '6', '5, 'sub': '1-2', 'img': {'@id': 'CUSTOM-CHARACTER-00040', '@he': '2.12mm', '@wi': '3.89mm', '@file': 'US20130157987A1-20130620-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'Rand Rare each independently H, halo, or Calkyl, with the proviso that when between carbon-23 and carbon-24 is a double bond, then Ris absent;'}{'sup': '7', 'sub': '1-6', 'Ris selected from the group consisting of O, NH, and N(Calkyl); and'}{'sup': '8', 'sub': 1-6', '3-6', '1-6', '3-6', '1-4', '1-4', '3', '2, 'Ris selected from the group consisting of Calkyl, Ccycloalkyl, aryl and heteroaryl, wherein each of Calkyl, Ccycloalkyl, aryl and heteroaryl are either unsubstituted or substituted with 1 to 5 substituents independently selected from the group consisting of Calkyl, OCalkyl, CF, NO, and halo.'}3. The compound of claim 2 , wherein{'sup': '1', 'Ris OH or F;'}{'sup': 2', '3, 'sub': '2', 'Rand Rtogether form ═CH;'}{'sup': '4', 'sub': '3', 'Ris CH;'}{'sup': 5', '6', '5, 'sub': '3', 'img': {'@id': 'CUSTOM-CHARACTER-00041', '@he': '2.12mm', '@wi': '3.89mm', '@file': 'US20130157987A1-20130620-P00001.TIF', '@alt': 'custom-character', '@img-content': ' ...

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Номер записи: 14
04-07-2013 дата публикации

"process for producing cycloalkylaromatic compounds"

Номер: US20130172514A1
Автор: Teng Xu, Wenyih F. Lai
Принадлежит: ExxonMobil Chemical Patents Inc

In a process for producing a cycloalkylaromatic compound, an aromatic compound, hydrogen and at least one diluent are supplied to a hydroalkylation reaction zone, such that the weight ratio of the diluent to the aromatic compound supplied to the hydroalkylation reaction zone is at least 1:100. The aromatic compound, hydrogen and the at least one diluent are then contacted under hydroalkylation conditions with a hydroalkylation catalyst in the hydroalkylation reaction zone to produce an effluent comprising a cycloalkylaromatic compound.

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Номер записи: 15
04-07-2013 дата публикации

CONTINUOUS PHOTOLYTIC PROCESS FOR THE PREPARATION OF VITAMIN D RELATED SUBSTANCES

Номер: US20130172588A1
Автор: Anderson Bruce Girard, Bauta William Edward, Cantrell, JR. William R.
Принадлежит: Genzyme Corporation

The present application provides a novel method for generation of a vitamin D2 compound using a continuous flow photoisomerization reactor. A compound represented by formula I: [structure] as further defined herein, is mixed with a solvent and a sensitizer, and is then passed through the continuous flow photoisomerization reactor. If X3 and X4 of formula II is tert-butyldimethylsilyl, then formula II is mixed with a deprotection reagent to obtain the vitamin D2 analog. 2. The method of wherein the sensitizer comprises 9-acetylanthracene.3. The method of wherein the deprotection reagent comprises tetrabutylammonium fluoride.4. The method of wherein the deprotection reagent comprises hydrochloric acid.5. The method of wherein the solvent in step a) is selected from the group consisting of heptane claim 1 , methanol claim 1 , toluene claim 1 , 1 claim 1 ,2-dichloroethane claim 1 , t-butyl methyl ether claim 1 , ethyl acetate claim 1 , and mixtures thereof.6. The method of wherein the solvent is deoxygenated.7. The method of wherein the solvent is deoxygenated by He sparging.8. The method of wherein the concentration of the compound of formula I in the solvent is about 5 mg/mL to about 50 mg/mL.9. The method of wherein the concentration of the compound of formula I in the solvent is at least about 50 mg/mL.10. The method of wherein the second mixture of step c) flows through the continuous flow photoisomerization reactor at a rate of about 2 mL/min to about 22 mL/min.11. The method of wherein the second mixture of step c) flows through the continuous flow photoisomerization reactor at a rate of at least about 22 mL/min.12. The method of wherein the second mixture of step c) flows through the continuous flow photoisomerization reactor at a temperature of between about 10° C. and about 30° C.13. The method of wherein the ratio of the sensitizer to the first mixture in step b) is about 0.4 wt % to about 16 wt %.14. The method of wherein the solvent in step a) comprises ...

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Номер записи: 16
11-07-2013 дата публикации

2-Methylene-20(21)-Dehydro-19,24,25,26,27-Pentanor-Vitamin D Analogs

Номер: US20130178449A1
Автор: Clagett-Dame Margaret, DeLuca Hector F., Glebocka Agnieska, Plum Lori A., Sicinski Rafal R.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

This invention discloses 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-1α-hydroxyvitamin D, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and lower in vivo intestinal calcium transport activity as compared to the native hormone 1α,25-dihydroxyvitamin D, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as secondary hyperparathyroidism and renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity. 2. The compound of wherein Xis hydrogen.3. The compound of wherein Xis hydrogen.4. The compound of wherein Xand Xare both t-butyldimethylsilyl.5. A pharmaceutical composition containing an effective amount of at least one compound as claimed in together with a pharmaceutically acceptable excipient.6. The pharmaceutical composition of wherein said effective amount comprises from about 0.01 μg to about 1000 μg per gram of composition.7. The pharmaceutical composition of wherein said effective amount comprises from about 0.1 μg to about 500 μg per gram of composition.9. A pharmaceutical composition containing an effective amount of 2-methylene-20(21)-dehydro-19 claim 5 ,24 claim 5 ,25 claim 5 ,26 claim 5 ,27-pentanor-1α-hydroxyvitamin Dtogether with a pharmaceutically acceptable excipient.10. The pharmaceutical composition of wherein said effective amount comprises from about 0.01 μg to about 1000 μg per gram of composition.11. The ...

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Номер записи: 17
11-07-2013 дата публикации

DERIVATIVES OF NOVEL PEROXIDES, METHOD OF PREPARATION THEREOF AND USE THEREOF IN HUMAN MEDICINE AS WELL AS IN COSMETICS FOR THE TREATMENT OR PREVENTION OF ACNE

Номер: US20130178648A1
Автор: BOUIX-PETER Claire, Pascal Jean-Claude, RODEVILLE Nicolas
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

Compounds of the following general formula (I): 3. The compound as defined by claim 1 , wherein the compound is selected from the group consisting of:bis(2-acetoxymethoxy)-benzoyl peroxide;(2-acetoxymethoxy-benzoyl)benzoyl peroxide;bis(2-propionyloxymethoxy)-benzoyl peroxide;(2-propionyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-butyryloxymethoxy)-benzoyl peroxide;(2-butyryloxymethoxy-benzoyl)benzoyl peroxide;bis(2-pentanoyloxymethoxy)-benzoyl peroxide;(2-pentanoyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-isobutyryloxymethoxy)-benzoyl peroxide;(2-isobutyryloxymethoxy-benzoyl)benzoyl peroxide;bis[2-(2,2-dimethyl-propionyloxymethoxy)]-benzoyl peroxide;[2-(2,2-dimethyl-propionyloxymethoxy)-benzoyl]benzoyl peroxide;bis[2-(1-acetoxy-ethoxy)]-benzoyl peroxide;[2-(1-acetoxy-ethoxy)-benzoyl]benzoyl peroxide;bis(2-ethoxycarbonyloxymethoxy)-benzoyl peroxide;(2-ethoxycarbonyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-propoxycarbonyloxymethoxy)-benzoyl peroxide;(2-propoxycarbonyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-butoxycarbonyloxymethoxy)-benzoyl peroxide;(2-butoxycarbonyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-isopropoxycarbonyloxymethoxy)-benzoyl peroxide;(2-isopropoxycarbonyloxymethoxy-benzoyl)benzoyl peroxide;bis(2-tert-butoxycarbonyloxymethoxy)-benzoyl peroxide;(2-tert-butoxycarbonyloxymethoxy-benzoyl)benzoyl peroxide;bis[2-(ethoxycarbonylamino-methoxy)]-benzoyl peroxide;[2-(ethoxycarbonylamino-methoxy)-benzoyl]benzoyl peroxide;bis(2-[ethoxycarbonyl-ethyl-amino)-methoxy])-benzoyl peroxide;(2-[(ethoxycarbonyl-ethyl-amino)methoxy]-benzoyl)benzoyl peroxide;bis(2-[(ethoxycarbonyl-methyl-amino)-methoxy])-benzoyl peroxide;(2-[ethoxycarbonyl-methyl-amino)methoxy]-benzoyl)benzoyl peroxide;bis(2-[(methyl-propoxycarbonyl-amino)methoxy]-benzoyl peroxide;(2-[(methyl-propoxycarbonyl-amino)-methoxy]-benzoyl)benzoyl peroxide;bis(2-[(butoxycarbonyl-methyl-amino)-methoxy]-benzoyl peroxide;(2-[(butoxycarbonyl-methyl-amino)-methoxy]-benzoyl)benzoyl peroxide;bis(2-[(isopropoxycarbonyl- ...

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Номер записи: 18
18-07-2013 дата публикации

Oxidation Catalyst for Hydrocarbon Compound, and Method and Apparatus for Producing Oxide of Hydrocarbon Compound Using Same

Номер: US20130184494A1
Автор: Joji Funatsu, Junichi Kugimoto, Kazunori Kurosawa, Naoya Katagiri
Принадлежит: USE Ind Ltd

According to the first embodiment of the present invention, an oxide of a hydrocarbon compound can be produced with high yield and high productivity by oxidizing the hydrocarbon compound with molecular oxygen in the co-presence of an N-hydroxy compound, such as methyl ethyl ketone or N-hydroxysuccinimide, and a phosphate ester, such as dibutyl phosphate. According to another embodiment of the present invention, an oxide of a hydrocarbon compound can be produced with high yield by using an oxidation catalyst that comprises an oxime compound, such as methyl ethyl ketone. According to another embodiment of the present invention, an alcohol and/or a ketone can be produced with high yield by oxidizing the hydrocarbon compound at a temperature of 160° C. or less, and by decomposing the resulting hydroperoxide, for example, in a unit having an inner surface formed by a material from which no transition metal ion is generated.

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Номер записи: 19
08-08-2013 дата публикации

USE OF MEXIPROSTIL IN THE TREATMENT OF INFLAMMATORY BOWEL DISEASE AND/OR OF IRRITABLE BOWEL SYNDROME

Номер: US20130202704A1
Автор: Assandri Alessandro, Moro Luigi
Принадлежит: COSMO TECHNOLOGIES LTD.

The invention relates to the use of mexiprostil in the treatment and/or prevention of inflammatory bowel disease and of irritable bowel syndrome, to the combinations of mexiprostil with other drugs, and also to a novel method for the synthesis of mexiprostil. 1. A method of treatment and/or prevention of inflammatory bowel disease (IBD) and/or of irritable bowel syndrome (IBS) comprising administering an effective amount of mexiprostil to patient in need thereof.2. The method according to claim 1 , for the treatment and/or prevention of ulcerative colitis.3. The method according to claim 1 , for the treatment and/or prevention of Crohn's disease.4. A method of treatment and/or prevention of the constipation (IBS-C) claim 1 , diarrhoeal (IBS-D) or alternating (IBS-A) variants of irritable bowel syndrome (IBS) comprising administering an effective amount of mexiprostil to patient in need thereof.5. The method according to claim 1 , wherein mexiprostil is administered at a rate of from 0.25 to 2.5 mg per day.6. The method according to claim 1 , wherein mexiprostil is administered in dosage units comprising from 0.5 to 1.5 mg of mexiprostil claim 1 , one or more times per day.7. The method according to claim 1 , wherein mexiprostil is formulated in gastroresistant and controlled-release compositions.8. The method according to claim 1 , wherein mexiprostil is formulated in compositions which comprise:a) a matrix which is composed of lipophilic compounds having a melting point of less than 90° C. and optionally of amphiphilic compounds in which the active ingredient is at least partially incorporated;b) optionally an amphiphilic matrix;c) an outer hydrophilic matrix in which the lipophilic matrix and the optional amphiphilic matrix are dispersed;d) optionally other excipients.9. The method according to claim 8 , characterized in that the composition comprises a gastroresistant coating.10. The method according to claim 1 , wherein mexiprostil is administered in combination ...

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Номер записи: 20
08-08-2013 дата публикации

"OXIDATION OF HYDROCARBONS"

Номер: US20130203984A1
Автор: Becker Christopher L., Benitez Franisco M., Dakka Jihad M., Mozeleski Edmund J.
Принадлежит:

In a process for oxidizing a hydrocarbon to a product comprising at least one of the corresponding hydroperoxide, alcohol, ketone, carboxylic acid and dicarboxylic acid, the hydrocarbon is contacted with an oxygen-containing compound in at least one oxidation zone in the presence of a catalyst comprising a cyclic imide having an imide group of formula (I): 2. The process of claim 1 , wherein the oxygen-containing compound is air that has been at least partially dehydrated.3. The process of claim 1 , wherein said hydrocarbon comprises an alkane or cycloalkane.4. The process of claim 1 , wherein said hydrocarbon comprises isobutane or cyclohexane.5. The process of claim 1 , wherein said hydrocarbon comprises cyclohexane claim 1 , the product comprises cyclohexanol and the process further comprises converting the cyclohexanol to adipic acid.6. The process of claim 1 , wherein said hydrocarbon comprises cyclohexane claim 1 , the product comprises cyclohexanone and the process further comprises converting the cyclohexanone to caprolactam.7. The process of claim 1 , wherein said hydrocarbon comprises iso-butane claim 1 , the product comprises tert-butyl hydroperoxide and the process further comprises using the tert-butyl hydroperoxide as an oxidation catalyst.9. The process of claim 8 , wherein said alkylaromatic compound of general formula (II) is selected from ethyl benzene claim 8 , cumene claim 8 , sec-butylbenzene claim 8 , sec-pentylbenzene claim 8 , p-methyl-sec-butylbenzene claim 8 , 1 claim 8 ,4-diphenylcyclohexane claim 8 , sec-hexylbenzene claim 8 , and cyclohexylbenzene.10. The process of claim 8 , and further comprising cleaving the hydroperoxide to produce phenol or a substituted phenol.13. The process of claim 1 , wherein said cyclic imide comprises N-hydroxyphthalimide.14. The process of claim 1 , wherein said oxygen-containing compound supplied to said oxidation zone has a water content of less than or equal to 0.3% by weight of the oxygen-containing ...

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Номер записи: 21
15-08-2013 дата публикации

23-yne-vitamin d3 derivative

Номер: US20130210781A1
Автор: Eiji Ochiai, Hiroshi Saito, Keiichiro Imaizumi, Kenichiro Takagi, Mariko Fujita, Masato Komiyama, Takayuki Chida, Toshiyuki Kaneko
Принадлежит: Teijin Pharma Ltd

To provide a novel vitamin D 3 derivative useful as a therapeutic agent for osteoporosis. Provided is a vitamin D 3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R 1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R 2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R 2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R 3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R 3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.

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Номер записи: 22
15-08-2013 дата публикации

Oxidation of Alkylbenzenes

Номер: US20130211036A1
Автор: Becker Christopher L., Dakka Jihad M., Mozeleski Edmund J., Smith Charles Morris, Zushma Stephen
Принадлежит: ExxonMobil Chemical Company - Law Technology

A process for oxidizing a composition comprising contacting an alkylbenzene of the general formula (I): 2. The process of claim 1 , and further comprising:(c) cleaving at least a portion of the alkylbenzene hydroperoxide produced by the contacting step (b) to produce phenol and cyclohexanone.3. The process of claim 2 , wherein at least a portion of the phenol present in the feed in the composition is provided from a recycle stream from the contacting step (b) and/or the cleaving step (c).4. The process of claim 1 , wherein the composition comprises from about 0.1 wt % to about 1 wt % of phenol based upon total weight of the composition.5. The process of claim 1 , wherein the composition comprises from about 0.15 wt % to about 0.5 wt % of phenol based upon total weight of the composition.6. The process of claim 1 , wherein the alkylbenzene is selected from cumene claim 1 , sec-butylbenzene claim 1 , cyclohexylbenzene and mixtures thereof.8. The process of claim 1 , wherein the cyclic imide comprises N-hydroxyphthalimide.9. The process of claim 1 , wherein the catalyst containing a cyclic imide having the general formula (II) is effective to remove at least a portion of the phenol.10. The process of claim 1 , wherein the cyclic imide is present in an amount of between 0.05 wt % and 5 wt % of the composition.11. The process of claim 1 , wherein the contacting step (b) is conducted at a temperature of between 90° C. and 150° C.12. The process of claim 1 , wherein the contacting step (b) is conducted at a temperature of between 105° C. and 120° C.13. The process of claim 1 , wherein the contacting step (b) is conducted at a pressure between 15 kPa and 500 kPa.14. (canceled)15. The process of claim 2 , wherein at least a portion of the phenol produced in the cleaving step (c) is converted to one or more of a phenolic resin claim 2 , bisphenol A claim 2 , ε-caprolactam claim 2 , an adipic acid claim 2 , or a plasticizer.16. The process of claim 2 , wherein at least a ...

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Номер записи: 23
22-08-2013 дата публикации

MODIFIED POLYMER COMPOSITIONS, MODIFICATION PROCESS AND FREE RADICAL GENERATING AGENTS FOR I.A. WIRE AND CABLE APPLICATIONS

Номер: US20130213688A1
Автор: NILSSON Daniel
Принадлежит: Borealis AG

A compound of formula (I) as defined in claims. 3. A compound as claimed in claim 1 , wherein Rand R are methyl.5. A compound as claimed in claim 1 , wherein the groups CRand CR are the same.7. A compound as claimed in wherein the dotted bond is present thus forming a triple bond.8. A compound as claimed in wherein Rz is a covalent bond.9. A polymer composition comprisingA) a polymer and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'B) a compound of formula I as claimed .'}10. A polymer composition as claimed in wherein said polymer is a polyolefin.11. A modified polymer composition in which the polymer composition of is cross-linked by initiating a radical reaction in the polymer composition.12. A crosslinkable cable which comprises a conductor which is surrounded by one or more layers claim 9 , wherein the at least one layer comprises the polymer composition as claimed in .13. A crosslinkable cable as defined in claim 12 , which is selected from any of the following cables:a low voltage cable comprising a conductor surrounded by an insulation layer and optionally a jacketing layer, wherein at least one layer, comprises the polymer composition; ora power cable comprising an electrical conductor surrounded by one or more layers comprising at least an inner semiconductive layer, insulation layer and an outer semiconductive layer, in that order, and optionally surrounded by a jacketing layer, wherein at least one of said layers comprises, the polymer composition.14. A process for producing a crosslinkable cable comprising applying one or more layers comprising a polymer composition on a conductor wherein at least one layer comprises a polymer composition as claimed in .15. A process as claimed in for crosslinking a cable by radical reaction claim 14 , comprising:applying one or more layers comprising the polymer composition on a conductor, andcrosslinking by radical reaction said at least one layer; optionallysubjecting the crosslinked cable thus obtained to a ...

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Номер записи: 24
29-08-2013 дата публикации

Process for the preparation of lubiprostone

Номер: US20130225842A1
Автор: Julian Paul Henschke, Lizhen Xia, Yuanlian Liu, Yung-Fa Chen
Принадлежит: Individual

Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

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Номер записи: 25
03-10-2013 дата публикации

Compounds and methods for delivery of prostacyclin analogs

Номер: US20130261187A1
Автор: David Mottola, Ken Phares
Принадлежит: United Therapeutics Corp

This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:

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Номер записи: 26
03-10-2013 дата публикации

INTEGRATED METHODS OF PREPARING RENEWABLE CHEMICALS

Номер: US20130261323A1
Автор: Al Obaidi Yassin, Griffith Josefa M., Gruber Patrick R., Henton David E., Manzer Leo E., Peters Matthew W., Taylor Joshua D.
Принадлежит: GEVO, INC.

Isobutene, isoprene, and butadiene are obtained from mixtures of Cand/or Colefins by dehydrogenation. The Cand/or Colefins can be obtained by dehydration of Cand Calcohols, for example, renewable Cand Calcohols prepared from biomass by thermochemical or fermentation processes. Isoprene or butadiene can be polymerized to form polymers such as polyisoprene, polybutadiene, synthetic rubbers such as butyl rubber, etc. in addition, butadiene can be converted to monomers such as methyl methacrylate, adipic acid, adiponitrile, 1,4-butadiene, etc. which can then be polymerized to form nylons, polyesters, polymethylmethacrylate etc. 1. An integrated process for preparing renewable hydrocarbons , comprising:(a) providing renewable isobutanol and renewable ethanol;(b) dehydrating the renewable isobutanol, thereby forming a renewable butene mixture comprising one or more renewable linear butenes and renewable isobutene;(c) dehydrating the renewable ethanol, thereby forming renewable ethylene; and{'sub': 3', '16, '(d) reacting at least a portion of the renewable butene mixture and at least a portion of the renewable ethylene to form one or more renewable C-Colefins.'}257-. (canceled)58. The integrated process of claim 1 , wherein the one or more renewable linear butenes comprise one or more of 1-butene claim 1 , cis-2-butene or trans-2-butene.59. The integrated process of claim 1 , wherein said reacting of step (d) comprises one or more reactions selected from the group consisting of disproportionation claim 1 , metathesis claim 1 , oligomerization claim 1 , isomerization claim 1 , alkylation claim 1 , dehydrodimerization claim 1 , dehydrocyclization claim 1 , and combinations thereof.60. The integrated process of claim 1 , wherein said reacting of step (d) comprises disproportionating at least a portion of the renewable ethylene formed in step (c) claim 1 , and at least a portion of the renewable 2-butene formed in step (b) and renewable 2-butene formed by isomerizing the ...

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Номер записи: 27
10-10-2013 дата публикации

Process to prepare treprostinil, the active ingredient in remodulin®

Номер: US20130267734A1
Автор: David A. Walsh, Hitesh Batra, Raju Penmasta, Sudersan M. TULADHAR
Принадлежит: United Therapeutics Corp

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

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Номер записи: 28
17-10-2013 дата публикации

Oxidation of Alkylaromatic Compounds

Номер: US20130274524A1
Автор: Dakka Jihad M., Stanat Jon E.R., Zushma Stephen
Принадлежит:

In a process for oxidizing an alkylaromatic compound to the corresponding hydroperoxide, a feed comprising an alkylaromatic compound is contacted with an oxygen-containing gas in the presence of a catalyst comprising a cyclic imide. The contacting is conducted at a temperature of about 90° C. to about 150° C., with the cyclic imide being present in an amount between about 0.05 wt % and about 5 wt % of the alkylaromatic compound in the feed and the catalyst being substantially free of alkali metal compounds. The contacting oxidizes at least part of the alkylaromatic compound in said feed to the corresponding hydroperoxide. 3. The process of claim 1 , wherein said cyclic imide comprises N-hydroxyphthalimide.4. The process of claim 1 , wherein said contacting is conducted at a temperature of between about 125° C. and about 140° C. and a pressure of about 15 kPa to about 150 kPa.5. The process of claim 1 , wherein said cyclic imide is present in an amount between about 0.1 wt % and about 1 wt % of the alkylaromatic in said feed during said contacting.6. The process of claim 1 , wherein said cyclic imide is present in an amount between about 0.05 wt % and about 0.5 wt % of the alkylaromatic in said feed during said contacting.7. The process of claim 1 , wherein said contacting converts at least 4 wt % per hour conversion of said alkylaromatic compound with a selectivity to the corresponding alkylaromatic hydroperoxide of at least 90 wt %.8. The process of claim 1 , wherein said alkylaromatic compound is cyclohexylbenzene.9. The process of claim 1 , further comprising the step of:cleaving the alkylaromatic hydroperoxide to produce phenol and the corresponding ketone.10. The process of claim 9 , wherein the cleaving is conducted in the presence of a catalyst.11. The process of claim 9 , wherein the cleaving is conducted in the presence of a homogeneous catalyst.12. The process of claim 11 , wherein said homogeneous catalyst comprises at least one of sulfuric acid claim 11 ...

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Номер записи: 29
05-12-2013 дата публикации

Ester Derivatives of Bimatoprost Compositions and Methods

Номер: US20130324606A1
Автор: Burk Robert M., Gac Todd S., Garst Michael E., Poloso Neil J., Wang Jenny W., Woodward David F.
Принадлежит: ALLERGAN, INC.

Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same. 2. The compound of claim 1 , wherein R claim 1 , Rand Rare independently substituted or unsubstituted C-Calkyl.3. The compound of claim 2 , wherein R claim 2 , Rand Rare independently substituted or unsubstituted C-Calkyl.4. The compound of claim 3 , wherein R claim 3 , Rand Rare independently substituted or unsubstituted Calkyl.5. The compound of claim 4 , wherein R claim 4 , Rand Rare independently methyl.6. The compound of claim 1 , wherein R claim 1 , Rand Rare independently substituted or unsubstituted C-Ccycloalkyl.7. The compound of claim 6 , wherein R claim 6 , Rand Rare independently unsubstituted C-Ccycloalkyl.8. The compound of claim 1 , wherein R claim 1 , Rand Rare independently substituted or unsubstituted aryl.9. The compound of claim 8 , wherein R claim 8 , Rand Rare independently aryl.10. The compound of claim 1 , wherein R claim 1 , Rand Rare independently phenyl.11. The compound of claim 1 , wherein Ris substituted or unsubstituted C-Calkyl claim 1 , or substituted or unsubstituted C-Ccycloalkyl.12. The compound of claim 11 , wherein Ris substituted or unsubstituted C-Calkyl.13. The compound of claim 12 , wherein Ris substituted or unsubstituted C-Calkyl.14. The compound of claim 13 , wherein Ris substituted or unsubstituted Calkyl.15. The compound of claim 14 , wherein Ris ethyl.16. The compound of claim 11 , wherein Ris substituted or unsubstituted C-Ccycloalkyl.17. The compound of claim 1 , wherein Ris hydrogen.22. The method of claim 21 , wherein said subject suffers from alopecia.23. The method of claim 21 , wherein said subject is in need of hair growth of the cilia claim 21 , the supercilia claim 21 , scalp pili claim 21 , or body pili.24. The method of claim 21 , wherein said administering is topical administering.25. The method of claim 24 , wherein said administering is topical epidermal administering. This application ...

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Номер записи: 30
05-12-2013 дата публикации

Crystallization of (20R) and (20S) Analogs of 2-Methylene-19-Nor-24-Dimethyl-1alpha,25-Dihydroxyvitamin D3

Номер: US20130324749A1
Автор: DeLuca Hector F., Flores Agnieszka, Holden Hazel M., Thoden James B.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are methods of purifying (20R) and (20S) analogs of 2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin Dto obtain the (20R) and (20S) analogs in crystalline form. The method includes the steps of preparing a solvent of either diethyl ether or a mixture of 2-propanol and hexane, dissolving a product containing the (20R) and (20S) analog to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. 2. (20S)-2-methylene-19-nor-22-dimethyl-1α ,25-dihydroxyvitamin Din crystalline form.3. A crystalline form of (20S)-2-methylene-19-nor-22-dimethyl-1α ,25-dihydroxyvitamin Dhaving molecular packing arrangement defined by space group P2 and unit cell dimensions a=7.57 Å b=14.79 Å c=14.48 Å α=90° , β=102.2° and γ=90°.4. A three dimensional structure for (20S)-2-methylene-19-nor-22-dimethyl-1α claim 3 ,25-dihydroxyvitamin Das defined by the molecular packing arrangement set forth in .5. A method of purifying (20S)-2-methylene-19-nor-22-dimethyl-1α claim 3 ,25-dihydroxyvitamin D claim 3 , comprising the steps of:(a) preparing a solvent comprising diethyl ether;{'sub': '3', '(b) dissolving a product containing (20S)-2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin Dto be purified in said solvent;'}{'sub': '3', '(c) cooling said solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of (20S)-2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin Dcrystals; and'}{'sub': '3', '(d) separating the (20S)-2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin Dcrystals from the solvent.'}6. The method of including the further step of allowing said solvent and dissolved product to cool to ambient temperature prior to cooling below ambient temperature.7. The method of wherein said solvent comprises 100% diethyl ether claim 5 , by volume.8. The method of wherein the step of separating ...

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Номер записи: 31
05-12-2013 дата публикации

Crystallization of (20R)-2-Methylene-19-Nor-24-Difluoro-1alpha,25-Dihydroxyvitamin D3

Номер: US20130324750A1
Автор: DeLuca Hector F., Flores Agnieszka, Holden Hazel M., Thoden James B.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are methods of purifying the compound (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin Dto obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. 2. A crystalline form of (20R)-2-methylene-19-nor-24-difluoro-1α ,25-dihydroxyvitamin Dhaving molecular packing arrangement defined by space group C2 and unit cell dimensions a=23.84 Å b=6.27 Å c=20.71 Å α=90° , β=126.52° and γ=90°.3. A three dimensional structure for (20R-2-methylene-19-nor-24-difluoro-1α claim 2 ,25-dihydroxyvitamin Das defined by the molecular packing arrangement set forth in .4. A method of purifying (20R)-2-methylene-19-nor-24-difluoro-1α claim 2 ,25-dihydroxyvitamin D claim 2 , comprising the steps of:(a) preparing a solvent comprising hexane;{'sub': '3', '(b) adding a product containing (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin Dto be purified to said hexane to form a suspension of the product in the hexane;'}(c) adding 2-propanol dropwise to the suspension to form a mixture of the product in the hexane and 2-propanol;{'sub': '3', '(d) heating the mixture to dissolve the product containing (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin Dto be purified in said mixture;'}{'sub': '3', '(e) cooling said mixture and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin Dcrystals; and'}{'sub': '3', '(f) separating the (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin Dcrystals from the solvent.'}5. The method of including the further step of allowing said mixture and dissolved product to cool to ambient temperature prior to cooling below ambient temperature.6. ...

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Номер записи: 32
05-12-2013 дата публикации

Crystallization of (20R) 19-Nor-24-Difluoro-1alpha,25-Dihydroxyvitamin D3

Номер: US20130324751A1
Автор: Agnieszka Flores, Hazel M. Holden, Hector F. DeLuca, James B. Thoden
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are methods of purifying the compound (20R)-19-nor-24-difluoro-1α,25-dihydroxyvitamin D 3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.

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Номер записи: 33
05-12-2013 дата публикации

Crystallization of (20R,22R)-2-Methylene-19-Nor-22-Methyl-1alpha,25-Dihydroxyvitamin D3 and Related Precursors

Номер: US20130324752A1
Автор: DeLuca Hector F., Flores Agnieszka, Grzywacz Pawel, Holden Hazel M., Plum Lori A., Thoden James B.
Принадлежит:

Disclosed are methods of purifying the compound (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Certain diol precursors formed during the synthesis of the compound and its diasteromers also may be obtained in crystalline form using ethyl acetate as a solvent. 2. A crystalline form of (20R ,22R)-2-methylene-19-nor-22-methyl-1α ,25-dihydroxyvitamin Dhaving molecular packing arrangement defined by space group C2 and unit cell dimensions a=27.03 Å b=6.47 Å c=17.41 Å α=90° , β=103.35° and γ=90°.3. A three dimensional structure for (20R claim 2 ,22R)-2-methylene-19-nor-22-methyl-1α claim 2 ,25-dihydroxyvitamin Das defined by the molecular packing arrangement set forth in .4. A method of purifying (20R claim 2 ,22R)-2-methylene-19-nor-22-methyl-1α claim 2 ,25-dihydroxyvitamin D claim 2 , comprising the steps of:(a) preparing a solvent comprising hexane;{'sub': '3', '(b) adding a product containing (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto be purified to said hexane to form a suspension of the product in the hexane;'}(c) adding 2-propanol dropwise to the suspension to form a mixture of the product in the hexane and 2-propanol;{'sub': '3', '(d) heating the mixture to dissolve the product containing (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto be purified in said mixture;'}{'sub': '3', '(e) cooling said mixture and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dcrystals; and'}{'sub': '3', '(f) separating the (20R,22R)-2-methylene-19-nor-22-methyl-1α,25- ...

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Номер записи: 34
12-12-2013 дата публикации

A-Ring Modified 19-Nor-Vitamin D Analogs and Their Uses

Номер: US20130331459A1
Автор: Clagett-Dame Margaret, DeLuca Hector F., Glebocka Agnieszka, Plum Lori A.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are 19-nor-vitamin D compounds, and specifically seco-A-2,19-dinor-1,25-dihydroxyvitamin Das well as pharmaceutical uses therefor. These compounds exhibit relatively high activity in vivo, specifically in intestinal tissues, but relatively low VDR binding activity, cell differentiation activity and gene transcription activity. There is thus potential for these compounds to have strong cell selectivity for use as therapeutic agents against some cancers, such as colon cancer or polyps, as well as hyperplastic intestinal disorders, such as Crohn's disease, ulcerative colitis and celiac disease. These compounds also have relatively high intestinal calcium transport activity evidencing potential in the treatment of bone diseases. 2. The compound of wherein X is hydrogen.4. The compound of wherein X is hydrogen.5. A pharmaceutical composition containing an effective amount of at least one compound as claimed in together with a pharmaceutically acceptable excipient.6. The pharmaceutical composition of wherein said effective amount composes from about 0.01 μg to about 1000 μg per gram of composition.7. The pharmaceutical composition of wherein said effective amount comprises from about 0.1 μg to about 500 μg per gram of composition.9. A pharmaceutical composition containing an effective amount of seco-A-2 claim 5 ,19-dinor-1 claim 5 ,25-dihydroxyvitamin Dtogether with a pharmaceutically acceptable excipient.10. The pharmaceutical composition of wherein said effective amount comprises from about 0.01 μg to about 1000 μg per gram of composition.11. The pharmaceutical composition of wherein said effective amount comprises from about 0.1 μg to about 500 μg per gram of composition.13. The method of wherein the vitamin D analog is administered orally.14. The method of wherein the vitamin D analog is administered parenterally.15. The method of wherein the vitamin D analog is administered transdermally.16. The method of wherein the vitamin D analog is administered ...

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Номер записи: 35
19-12-2013 дата публикации

Prostaglandin synthesis and intermediates for use therein

Номер: US20130338379A1
Автор: Boris Ivanovich Gorin, Dino Alberico, Jan Oudenes, Joshua Clayton
Принадлежит: Alphora Research Inc

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

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Номер записи: 36
09-01-2014 дата публикации

2-METHYLENE-19,23,24-TRINOR-1ALPHA-HYDROXYVITAMIN D3

Номер: US20140011778A1
Автор: Clagett-Dame Margaret, DeLuca Hector F., Glebocka Agnieszka, Plum Lori A., Sicinski Rafal
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Compounds of Formula I are provided where Rand Rare independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions. 2. The compound of claim 1 , wherein Rand Rare both hydroxy protecting groups.3. The compound of claim 2 , wherein Rand Rare both t-butyldimethylsilyl groups.9. A pharmaceutical composition comprising an effective amount of the compound of and a pharmaceutically acceptable carrier.10. The pharmaceutical composition of claim 9 , wherein the effective amount comprises from about 0.01 μg to about 1 mg of the compound per gram of the composition.11. The pharmaceutical composition of claim 9 , wherein the effective amount comprises from about 0.1 μg to about 500 μg of the compound per gram of the composition.12. A method of preventing or treating a biological condition comprising administering an effective amount of the compound of or a pharmaceutical composition comprising an effective amount of the compound of to a subject claim 9 , wherein the biological condition is selected from psoriasis; leukemia; colon cancer; breast cancer; prostate cancer; multiple sclerosis; lupus; diabetes mellitus; host versus graft reaction; rejection of organ transplants; an inflammatory disease selected from rheumatoid arthritis claim 9 , asthma claim 9 , or inflammatory bowel diseases; a skin condition selected from wrinkles claim 9 , lack of adequate skin firmness claim 9 , lack of adequate dermal hydration claim 9 , or insufficient sebum secretion; or renal osteodystrophy.13. The method of claim 12 , wherein the biological condition is psoriasis.14. The method of claim 12 , wherein the biological condition is renal osteodystrophy.15. The method of claim 12 , wherein the compound or the pharmaceutical composition is administered orally.16. The method of claim 12 , wherein the compound or the pharmaceutical composition is administered parentally.17. ...

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Номер записи: 37
30-01-2014 дата публикации

METHOD FOR TREATING SCHIZOPHRENIA

Номер: US20140031428A1
Автор: UENO Ryuji
Принадлежит: SUCAMPO AG

The present invention provides a novel fatty acid derivative. The present invention also provides a method for treating schizophrenia in a mammalian subject, which comprises administering to the subject in need thereof an effective amount of a fatty acid derivative. 2. The method as described in claim 1 , wherein Z is C═O.3. The method as described in claim 1 , wherein B is —CH—CH—.4. The method as described in claim 1 , wherein B is —CH—CH— and Z is C═O.5. The method as described in claim 1 , wherein L is hydroxy or oxo claim 1 , M is hydrogen or hydroxy claim 1 , N is hydrogen claim 1 , B is —CH—CH— and Z is C═O.6. A compound of 7-[2-(4 claim 1 ,4-difluoro-3-oxooctyl)-5-oxocyclopentyl]hept-2-enoic acid or functional derivative thereof.7. A compound of 7-[2-(4 claim 1 ,4-difluoro-3-oxooctyl)-5-oxocyclopentyl]hept-2-enoic acid. This is a continuation of application Ser. No. 13/566,353 filed Aug. 3, 2012, which claims benefit of Provisional Application No. 61/515,418 filed Aug. 5, 2011; the above noted prior applications are all hereby incorporated by reference.The present invention relates to a method for treating schizophrenia.Schizophrenia is a chronic, severe, and disabling brain disorder that has affected people throughout history. About 1 percent of Americans have this illness.People with the disorder may hear voices other people don't hear. They may believe other people are reading their minds, controlling their thoughts, or plotting to harm them. This can terrify people with the illness and make them withdrawn or extremely agitated.People with schizophrenia may not make sense when they talk. They may sit for hours without moving or talking. Sometimes people with schizophrenia seem perfectly fine until they talk about what they are really thinking.Families and society are affected by schizophrenia too. Many people with schizophrenia have difficulty holding a job or caring for themselves, so they rely on others for help. Treatment helps relieve many symptoms of ...

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Номер записи: 38
06-02-2014 дата публикации

Novel Vitamin D Receptor Modulators with Partial Agonist Activity

Номер: US20140038925A1
Автор: Kudo Takeru, Maekawa Kazuki, MAKISHIMA Makoto, Mourino Antonio, Tokiwa Hiroaki, WATARAI Yusuke, Yamada Sachiko
Принадлежит:

The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. 2. The compound claim 1 , solvate thereof or prodrug thereof according to claim 1 , wherein the compound represented by the formula (I) is selected from the group consisting of (25S)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,26 claim 1 ,27-trinorvitamin D claim 1 , (25R)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,26 claim 1 ,27-trinorvitamin D claim 1 , (25R)-26-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,27-dinorvitamin D claim 1 , (25S)-26-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,27-dinorvitamin D claim 1 , (25R)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-20 claim 1 ,20 claim 1 ,22 claim 1 ,22 claim 1 ,23 claim 1 ,23 claim 1 ,24 claim 1 ,24-octadehydro-19 claim 1 ,21 claim 1 ,26 claim 1 ,27-tetranorvitamin D claim 1 , (25S)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-20 claim 1 ,20 claim 1 ,22 claim 1 ,22 claim 1 ,23 claim 1 ,23 claim 1 ,24 claim 1 ,24-octadehydro-19 claim 1 ,21 claim 1 ,26 claim 1 ,27-tetranorvitamin D claim 1 , (25R)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,27-dinorvitamin Dand (25S)-25-(1-Adamantyl)-1α claim 1 ,25-dihydroxy-2-methylene-23 claim 1 ,23 claim 1 ,24 claim 1 ,24-tetradehydro-19 claim 1 ,27-dinorvitamin D.3. A composition comprising the compound claim 1 , solvate thereof or prodrug thereof according to .4. The composition according to ...

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Номер записи: 39
20-02-2014 дата публикации

CRYSTALLINE FORM OF MAXACALCITOL

Номер: US20140051875A1
Автор: HUANG PEI-CHEN, Wei Ching-Peng
Принадлежит: FORMOSA LABORATORIES INC.

The present invention relates to maxacalcitol hydrate, a new crystalline form of maxacalcitol, with superior technical properties e.g. in the manufacture of crystal suspension formulations, and with superior stability properties. 1. A crystalline form of maxacalcitol , which is maxacalcitol hydrate.2. The crystalline form of claim 1 , characterized by a X-ray powder diffraction (XRD) pattern comprising distinctive peaks at 2 theta values of approximately 5.8 claim 1 , 6.3 claim 1 , 12.0 claim 1 , 13.1 claim 1 , 13.5 claim 1 , 13.9 claim 1 , 14.2 claim 1 , 14.5 claim 1 , 14.9 claim 1 , 15.3 claim 1 , 16.0 claim 1 , 16.2 claim 1 , 17.0 claim 1 , 17.9 claim 1 , 18.3 claim 1 , 19.3 claim 1 , 23.5 claim 1 , 24.0 claim 1 , 24.3 claim 1 , 25.4 and 26.2 degree±0.2 degrees 2 theta.3. The crystalline form of claim 1 , characterized by a weight loss of about 4.5% at 120° C. for 240 minutes as measured by thermogravimetric analysis (TGA).4. The crystalline form of claim 1 , characterized by a water content of about 4.2% by weight as measured by Karl-Fischer method.5. The crystalline form of claim 1 , characterized by a melting point of about 86° C. as measured by differential scanning calorimetry (DSC) spectrum.6. The crystalline form of claim 1 , which is more stable to storage than anhydrous form claim 1 , showing no degradation under an inert gas atmosphere at 25° C. for at least 32 days.7. A process for preparing a crystalline form of maxacalcitol hydrate comprising:(a) dissolving a crystalline or non-crystalline maxacalcitol in a polar organic solvent to form a first solution;(b) combining the first solution with water to form a second solution;(c) cooling the second solution to form a crystalline precipitate; and(d) isolating the crystalline precipitate from the second solution to obtain the crystalline form of maxacalcitol hydrate.8. The process of claim 7 , wherein the crystalline form of maxacalcitol hydrate is characterized by a powder X-ray diffraction (XRD) pattern ...

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Номер записи: 40
13-03-2014 дата публикации

SYSTEM AND METHOD FOR GENERATION OF POINT OF USE REACTIVE OXYGEN SPECIES

Номер: US20140072653A1
Автор: Buschmann Wayne
Принадлежит: CLEAN CHEMISTRY, LLC

Systems and methods for generating reactive oxygen species formulations useful in various oxidation applications. Exemplary formulations include singlet oxygen or superoxide and can also contain hydroxyl radicals or hydroperoxy radicals, among others. Formulations can contain other reactive species, including other radicals. Exemplary formulations containing peracids are activated to generate singlet oxygen. Exemplary formulations include those containing a mixture of superoxide and hydrogen peroxide. Exemplary formulations include those in which one or more components of the formulation are generated electrochemically. Formulations of the invention containing reactive oxygen species can be further activated to generate reactive oxygen species using activation chosen from a Fenton or Fenton-like catalyst, ultrasound, ultraviolet radiation or thermal activation. Exemplary applications of the formulations of the invention among others include: cleaning in place applications, water treatment, soil decontamination and flushing of well casings and water distribution pipes. 1. A method for generating a reactive oxygen species formulation , the method comprising:generating an alkaline hydrogen peroxide solution;mixing the alkaline hydrogen peroxide solution with an acyl donor such that a peracid concentrate is produced, wherein the peracid concentrate has minimal hydrogen peroxide residual;adjusting the pH of the peracid concentrate to the activated pH range for generating the reactive oxygen species.2. The method of wherein the alkaline hydrogen peroxide solution is generated from the combination of an alkali and a hydrogen peroxide concentrate or wherein the alkaline hydrogen peroxide solution is generated electrochemically.3. The method of wherein the reactive oxygen species formulation is a singlet oxygen precursor formulation.4. The method of wherein the acyl donor is an acetyl donor.5. The method of wherein the hydrogen peroxide solution is generated using a molar ...

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Номер записи: 41
02-01-2020 дата публикации

Biodegradable compound, lipid particles, composition and kit comprising lipid particles

Номер: US20200000723A1
Автор: Eiichi Akahoshi, Katsuyuki Naito, Mitsuko Ishihara
Принадлежит: Toshiba Corp

[Problem] To provide a biodegradable compound having a structure decomposed in a cell, lipid particles containing the compound, and a pharmaceutical composition comprising the lipid particles. [Solution] The compound of the embodiment is represented by the formula (1): P—[X—R—Y—R′-Q] 2 (1). In the formula, P is an alkyleneoxy having an ether bond, X is a divalent linking group having a tertiary amine structure, R is a divalent linking group, R′ is a single bond or a C 1 to C 6 alkylene, and Q is a liposoluble vitamin residue, a sterol residue, or a C 12 to C 22 aliphatic hydrocarbon group. The structure of the compound contains at least one biodegradable group. From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

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Номер записи: 42
04-01-2018 дата публикации

ANTISEPTIC POLYMETHYLMETHACRYLATE BONE CEMENT

Номер: US20180000984A1
Автор: CALDERÓN ORTIZ Lorena, VOGT Sebastian
Принадлежит: HERAEUS MEDICAL GMBH

An antiseptic composition for use as bone cement, in particular an antiseptic polymethylmethacrylate bone cement. The composition can be cured and comprises a pharmacologically tolerable salt of a monoperoxy dicarboxylic acid, whereby the salt of the monoperoxy dicarboxylic acid can be dissolved from the composition in the presence of water. Preferably, the salt of the monoperoxy dicarboxylic acid in the composition is used in the form of a powder, whereby the powder has a mean particle size of not more than 250 μm. Preferably, the salt of the monoperoxy dicarboxylic acid, in solution at room temperature, is not degraded within 5 min by the catalase enzyme. 1. Composition for use as a bone cement , whereby the composition can be cured , wherein the composition comprises a pharmacologically tolerable salt of a monoperoxy dicarboxylic acid and the salt of the monoperoxy dicarboxylic acid can be dissolved from the composition in the presence of water.2. Composition according to claim 1 , wherein the composition is an antiseptic bone cement.3. Composition according to claim 1 , wherein the composition is an antiseptic polymethylmethacrylate bone cement.4. Composition according to claim 1 , wherein the salt of the monoperoxy dicarboxylic acid is in alkaline earth salt or an alkali salt.5. Composition according to claim 4 , wherein the alkaline earth salt is a magnesium salt.6. Composition according to claim 1 , wherein the salt of the monoperoxy dicarboxylic acid is not soluble in methylmethacrylate at room temperature.7. Composition according to claim 1 , wherein the salt of the monoperoxy dicarboxylic acid in the composition is used in the form of a powder claim 1 , whereby the powder has a mean particle size of not more than 250 μm.8. Composition according to claim 1 , wherein the salt of the monoperoxy dicarboxylic acid is not degraded within 5 min by the catalase enzyme in aqueous solution at room temperature.9. Composition according to claim 1 , which contains 0.5% ...

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Номер записи: 43
07-01-2016 дата публикации

Process for Making Alkylated Aromatic Compound

Номер: US20160001276A1
Автор: Gabor Kiss, Tan-Jen Chen, Terry E. Helton, Thomas E. Green, William A. Lamberti, William C. Horn
Принадлежит: ExxonMobil Chemical Patents Inc

A process for producing an alkylated aromatic compound comprises contacting an aromatic starting material and hydrogen with a plurality of catalyst particles under hydroalkylation conditions to produce an effluent comprising the alkylated aromatic compound, the catalyst comprising a composite of a solid acid, an inorganic oxide different from the solid acid and a hydrogenation metal, wherein the distribution of the hydrogenation metal in at least 60 wt % of the catalyst particles is such that the average concentration of the hydrogenation metal in the rim portion of a given catalyst particle is Crim, the average concentration of the hydrogenation metal in the center portion of the given catalyst particle is Ccenter, where 0.2≦Crim/Ccenter<2.0. Also disclosed are hydroalkylation catalyst and process for making phenol and/or cyclohexanone using the catalyst.

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Номер записи: 44
04-01-2018 дата публикации

PRODUCT, OR ACTIVE AGENT, OR COMPOSITION FOR THE CARE OF THE BREASTS IN A PREMENSTRUAL OR MENSTRUAL PERIOD OR FOR THE CARE OF THE SYMPTOMATOLOGY OF MASTODYNIA

Номер: US20180002281A1
Автор: DESJONQUERES Stéphane
Принадлежит:

A method for caring for or treating the breasts during premenstrual or menstrual phases and for the care or treatment of the symptomatology of mastodynia, comprising a step of selecting or identifying women needing care or treatment of the breasts, or suffering from symptomatology of mastodynia, and a step of applying to the skin areas in need thereof an effective amount of a product, active agent or composition, comprising peroxidized lipids or a peroxidised oil, or consisting essentially of peroxidized lipids or of a peroxidised oil. 1. A method for caring for or treating the breasts during premenstrual or menstrual phases and also for the care or treatment of the symptomatology of mastodynia , comprising a step of selecting or identifying women needing care or treatment of the breasts , or suffering from symptomatology of mastodynia , and a step of applying to the skin areas in need thereof an effective amount of a product , active agent or composition , comprising peroxidized lipids or a peroxidised oil , or consisting essentially of peroxidized lipids or of a peroxidised oil.2. The method of claim 1 , wherein the peroxidised lipids or peroxidised oil comprise/s or are/is consisting of peroxidized glycerol triesters.3. The method of claim 1 , wherein the peroxidised lipids or peroxidised oil are/is obtained from a vegetable oil chosen from a corn vegetable oil claim 1 , a soya vegetable oil claim 1 , a sweet almond vegetable oil claim 1 , a hazelnut vegetable oil claim 1 , a peanut vegetable oil claim 1 , a grapeseed vegetable oil claim 1 , a sesame vegetable oil and a safflower vegetable oil claim 1 , or a mixture of these oils in any proportion(s).4. The method of claim 1 , wherein the peroxidized lipids/peroxidised oil have/has a degree of peroxidation of between 5 and 600 milliequivalents per kg.6. The method of claim 1 , wherein the product claim 1 , active agent or composition is consisting essentially of the peroxidized lipids or peroxidised oil.7. The ...

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Номер записи: 45
02-01-2020 дата публикации

Radical initiators and chain extenders for converting methane gas into methane-sulfonic acid

Номер: US20200002276A1
Автор: Alan K. Richards
Принадлежит: Individual

Improved initiators, solvents, and SO3 mixtures are disclosed which can increase the yields and efficiency of a process which converts methane gas into methane-sulfonic acid (MSA). MSA is valuable in its own right, or it can be processed to create desulfured fuels and other chemicals. Preferred initiators have been identified, comprising at least one “primary” initiator, and at least one “extender” (or secondary, supplemental, enhancing, tuning, tweaking, or similar terms) initiator. “Primary” initiator(s) include (unmethylated) Marshall's acid, mono-methyl-Marshall's acid, and di-methyl-Marshall's acid, while a secondary/extender initiator comprises methyl-Caro's acid, which can oxidize sulfur DI-oxide (an unwanted chain terminator) into sulfur TRI-oxide (an essential reagent). Other enhancements to the MSA manufacturing process also are described.

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Номер записи: 46
03-01-2019 дата публикации

PREPARATION OF LATANOPROSTENE BUNOD OF DESIRED, PRE-DEFINED QUALITY BY GRAVITY CHROMATOGRAPHY

Номер: US20190002405A1
Автор: BUZDER-LANTOS Péter, FEKETE Ibolya, HAVASI Gábor, HORTOBÁGYI Irén, KARDOS Zsuzsanna, LÁSZLÓFI István, Takacs Laszlo
Принадлежит: CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT .

The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silica gel column chromatography where the used silica gel is irregular silica gel or spherical silica gel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silica gel filtration chromatography. 2. Process a.) or b.) as defined in claim 1 , characterized in that claim 1 , the eluent mixture contains as apolar solvent straight- or branched-chain aliphatic claim 1 , cyclic or aromatic hydrocarbons claim 1 , halogenated aliphatic hydrocarbons or ether-type solvents.3. Process as defined in claim 2 , characterized in that claim 2 , as apolar solvent pentane claim 2 , hexane claim 2 , heptane claim 2 , cyclohexane claim 2 , dichloromethane or diisopropyl ether claim 2 , preferably hexane is applied.4. Process a.) or b.) as defined in claim 1 , characterized in that claim 1 , as polar solvent an alcohol- claim 1 , ester- or ketone-type solvent containing straight- or branched-chain alkyl group is applied.5. Process as defined in claim 4 , characterized in that claim 4 , as polar solvent a C1-5 alcohol claim 4 , preferably ethyl alcohol or isopropyl alcohol is applied.6. Process as defined in claim 3 , characterized in that claim 3 , the eluent mixture is a gradient mixture containing hexane and ethyl alcohol in 6:1-8:1 volume ratios.7. Process as defined in claim 4 , characterized in that claim 4 , as polar solvent a ketone-type solvent claim 4 , preferably acetone is applied.8. Process as defined in claim 3 , characterized in that claim 3 , the eluent mixture contains hexane and acetone in 2:1 volume ratio.9. Filtration chromatography process as defined in claim 1 , characterized in that claim 1 , the eluent mixture contains an apolar and a ...

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Номер записи: 47
03-01-2019 дата публикации

13-Cis-RAMBA RETINAMIDES THAT DEGRADE MNKs FOR TREATING CANCER

Номер: US20190002411A1
Автор: Mbatia Hannah, Njar Vincent, Ramalingam Senthilmurugan, Ramamurthy Vidya
Принадлежит: University of Maryland, Baltimore

The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities. 2. The process as claimed in claim 1 , wherein the process is for the treatment of breast cancer or prostate cancer.3. The process as claimed in claim 2 , wherein R is an imidazole claim 2 , and wherein the compound is selected from the following:Compound 16 in which R′ is the hydrogen, and n is 0;Compound 17 in which R′ is a hydroxyl group in a para-position, and n is 0;Compound 18 in which R′ is a hydroxyl group in an ortho-position, and n is 0;Compound 19 in which R′ is a fluorine in a para-position, and n is 0;Compound 20 in which R′ is a fluorine in a meta-position, and n is 0;Compound 21 in which R′ is the hydrogen, and n is 1;Compound 22 in which R′ is the hydroxyl group in the para-position, and n is 1;Compound 23 in which R′ is the fluorine in the para-position, and n is 1;Compound 24 in which R′ is the fluorine in the meta-position, and n is 1; andCompound 25 in which R′ is the hydroxyl group in the para-position, and n is 2.4. The process as claimed in claim 3 , wherein the compound is selected from the following:Compound 16 in which R′ is the hydrogen, and n is 0;Compound 20 in which R′ is a fluorine in a meta-position, and n is 0; andCompound 22 in which R′ is the hydroxyl group in ...

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Номер записи: 48
13-01-2022 дата публикации

MANUFACTURE OF CAROTENOID COMPOSITIONS

Номер: US20220009886A1
Автор: Mehta Sevanti
Принадлежит: Unibar Corporation

A extract composition (600) includes capsanthin in the range from 50% to 80%, zeaxanthin in the range from 5% to 15%, and cryptoxanthin the range from 1% to 5%. 1600Capsicum annum. A extract composition () comprising:capsanthin in the range from 50% to 80%;zeaxanthin in the range from 5% to 15%; andcryptoxanthin in the range from 1% to 5%.2. The composition of claim 1 , wherein the capsanthin comprises trans-capsanthin (3R claim 1 ,3″S claim 1 ,5′R)-3 claim 1 ,3′-Dihydroxy-β claim 1 ,κ-caroten-6′-one) claim 1 , the zeaxanthin comprises trans-zeaxanthin (3R claim 1 , 3′R-β claim 1 ,β-carotene-3 claim 1 ,3′-diol) claim 1 , and the cryptoxanthin comprises beta-cryptoxanthin (3R claim 1 ,6′R)-4′ claim 1 ,5′-Didehydro-5′ claim 1 ,6′-dihydro-β claim 1 ,β-caroten-3-ol.3. The composition of claim 1 , wherein the color value of carotenoids ranges from 800 claim 1 ,000 to 1 claim 1 ,250 claim 1 ,000.4. The composition of claim 1 , wherein the composition aids in the management of age related macular degeneration conditions selected from the group consisting of: blurred vision claim 1 , distorted vision claim 1 , reduced central vision claim 1 , and difficulty in adopting low light levels.5. The composition of claim 1 , wherein the composition protects against blue light induced retinopathy by decreasing oxidative and endoplasmic reticulum stress.6. The composition of claim 1 , wherein the composition provides functional and morphological preservation of photoreceptors against blue light damage.7. The composition of claim 1 , wherein the composition lowers intraocular pressure.8. The composition of claim 1 , wherein the composition provides color for a cosmetic selected from the group consisting of: lipstick claim 1 , chap-stick claim 1 , liquid gloss claim 1 , lipstick paste claim 1 , blush claim 1 , lip liner claim 1 , foundation claim 1 , concealer claim 1 , eye contourer claim 1 , eyeliner claim 1 , mascara claim 1 , nail polish claim 1 , eye shadow claim 1 , and body make ...

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Номер записи: 49
01-01-2015 дата публикации

Ester derivatives of bimatoprost compositions and methods

Номер: US20150005377A1
Автор: David F. Woodward, Jenny W. Wang, Michael E. Garst, Neil J. POLOSO, Robert M. Burk, Todd S. Gac
Принадлежит: Allergan Inc

Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

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Номер записи: 50
12-01-2017 дата публикации

CRYSTAL FORMS OF ASTAXANTHIN

Номер: US20170008841A1
Автор: GUO Jingfei, JONES Matthew J., SCHAEFER Christian, Ulrich Joachim, VERLHAC-TRICHET Viviane
Принадлежит:

The invention describes previously undisclosed crystal forms of astaxanthin designated crystal form I and II. It has been surprisingly found that the two crystal forms of astaxanthin show an improved bioavailability, a relatively high solubility in specific organic solvents and an increased long-term stability. For example the new forms are stable in solid form for at least 90 days at a temperature of 20° C.-40° C. It was further found that the two crystal forms can be prepared from each other. Therefore the invention also relates to methods for preparing said crystal forms. In addition, the invention relates to administration forms (hereinafter also called “formulations”) comprising one of the two crystal forms according to the invention or mixtures thereof dissolved or suspended in oil or organic-solvent. 1. A method of preparing an administration form of astaxanthin with improved stability and bioavailability properties , the method comprising incorporating into the administration form at least one crystal form of astaxanthin designated crystal form I and II , whereincrystal form I is characterized by i) An XRPD (X-Ray Powder Diffraction) pattern comprising a peak between 20° and 21°, and ii) A DSC (Differential Scanning Calorimeter) scan showing a phase transition at 225° C.-235° C.; and whereincrystal form II is characterized by i) an XRPD pattern comprising a peak at approximately 11° and 18°, and ii) a DSC scan showing a phase transition at 200° C.-220° C.2. The method according to claim 1 , wherein crystal form I shows a phase transition at 230.8° C.±1.3. The method according to claim 1 , wherein crystal form II shows a phase transition at 210° C.±1.4. The method according to claim 1 , wherein the administration form is stable in solid form for at least 90 days at 20° C.5. An administration form prepared by the method according to claim 1 , wherein the administration form is a fish food comprising at least one of crystal forms I and II.6. An administration ...

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Номер записи: 51
14-01-2016 дата публикации

Process for Making Alkylated Aromatic Compound

Номер: US20160009613A1
Автор: Chen Tan-Jen, Green Thomas E., Helton Terry E., Horn William C., Kiss Gabor, Lamberti William A.
Принадлежит:

A process for producing an alkylated aromatic compound comprises contacting an aromatic starting material and hydrogen with a plurality of catalyst particles under hydroalkylation conditions to produce an effluent comprising the alkylated aromatic compound, the catalyst comprising a composite of a solid acid, an inorganic oxide different from the solid acid and a hydrogenation metal, wherein the distribution of the hydrogenation metal in at least 60 wt % of the catalyst particles is such that the average concentration of the hydrogenation metal in the rim portion of a given catalyst particle is Crim, the average concentration of the hydrogenation metal in the outer portion of a given catalyst particle is Couter, the average concentration of the hydrogenation metal in the center portion of the given catalyst particle is Ccenter, where Crim/Ccenter≧2.0 and/or Couter/Ccenter2.0. Also disclosed are rimmed catalyst and process for making phenol and/or cyclohexanone using the catalyst. 1. A process for producing an alkylated aromatic compound , the process comprising contacting an aromatic starting material and hydrogen with a plurality of catalyst particles under hydroalkylation conditions to produce an effluent comprising the alkylated aromatic compound , the catalyst comprising a composite of a solid acid , an inorganic oxide different from the solid acid and a hydrogenation metal , wherein the distribution of the hydrogenation metal in at least 60 wt % of the catalyst particles is such that:the average concentration of the hydrogenation metal in the rim portion of a given catalyst particle is Crim;the average concentration of the hydrogenation metal in the outer portion of a given catalyst particle is Couter; andthe average concentration of the hydrogenation metal in the center portion of the given catalyst particle is Ccenter; andat least one of the following conditions is met:(i) Crim/Ccenter≧2.0; and(ii) Couter/Ccenter≧2.0.2. The process of claim 1 , wherein the ...

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Номер записи: 52
09-01-2020 дата публикации

Retinoid derivatives with antitumor activity

Номер: US20200009091A1
Автор: Claudio Pisano, Lucio Merlini, Raffaella CINCINELLI, Sabrina Dallavalle
Принадлежит: Biogem Sc A Rl

The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

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Номер записи: 53
27-01-2022 дата публикации

Process for the preparation of latanoprostene bunod and intermediate thereof and compositions comprising the same

Номер: US20220024849A1
Автор: Ming-Kun Hsu, Shih-Yi Wei, Tzyh-Mann Wei
Принадлежит: Chirogate International Inc

Processes for preparing latanoprostene bunod and an intermediate prepared from the process. Also latanoprostene bunod compositions having high-purity latanoprostene bunod.

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Номер записи: 54
14-01-2021 дата публикации

ONLINE PRODUCTION OF ORGANIC PEROXIDE USING A CATALYST BED

Номер: US20210009515A1
Автор: Coleman Todd, FRY Slaton, YEAMAN Tim
Принадлежит:

A method of producing an organic peroxide includes introducing an organic solution and a peroxide solution into a mixing tank to form a mixture. The method further includes circulating the mixture over a fixed catalyst bed to form the organic peroxide and measuring a concentration of the organic peroxide in the mixture. Further, the method includes removing at least a portion of the mixture when the concentration reaches a set value. 1. A method of producing an organic peroxide comprising:introducing an organic solution and a peroxide solution into a mixing tank to form a mixture;circulating the mixture over a fixed catalyst bed to form the organic peroxide;measuring a concentration of the organic peroxide in the mixture; andremoving at least a portion of the mixture when the concentration reaches a set value.2. The method according to claim 1 , wherein the peroxide solution comprises hydrogen peroxide and water.3. The method according to claim 2 , wherein the peroxide solution comprises 10 to 50 wt % of hydrogen peroxide based on a total weight of the peroxide solution.4. The method according to claim 1 , wherein the organic solution comprises water and an organic acid having 1 to 8 carbon atoms.5. The method according to claim 4 , wherein the organic solution comprises 10 to 50 wt % of the organic acid based on a total weight of the organic solution.6. The method according to claim 4 , wherein the organic acid is acetic acid.7. The method according to claim 5 , wherein the organic acid is acetic acid.8. The method according to claim 1 , wherein the fixed catalyst bed comprises an acid resin.9. The method according to claim 1 , wherein the set value is between 50 and 2000 ppm of the organic peroxide.10. A system for online production of an organic peroxide comprising:a mixing tank;a peroxide supply in fluid communication with the mixing tank and configured to supply a peroxide solution to the mixing tank;an organic supply in fluid communication with the mixing tank ...

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Номер записи: 55
08-01-2015 дата публикации

IN SITU GENERATION OF PEROXYCARBOXYLIC ACIDS AT ALKALINE pH, AND METHODS OF USE THEREOF

Номер: US20150011632A1
Автор: David D. McSherry, Junzhong Li, Richard Staub
Принадлежит: ECOLAB USA INC

The present disclosure is related to percarboxylic acid compositions formed in situ in non-equilibrium reactions. The peroxycarboxylic acid compositions are formed using ester based starting materials. Methods for using the percarboxylic acid compositions are also disclosed.

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Номер записи: 56
08-01-2015 дата публикации

Amine salts of prostaglandin analogs

Номер: US20150011755A1
Автор: Mark P Jackson
Принадлежит: Dr Reddys Laboratories Ltd

The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.

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Номер записи: 57
14-01-2021 дата публикации

Formulation of di(4-tert-butylcyclohexyl) peroxydicarbonate

Номер: US20210009786A1
Автор: Antonie Den Braber, Auke Gerardus Talma, Geesje Klasina Spijkerman, Markus Oliver Majoor, Martin Hermanus Maria Jansen
Принадлежит: Nouryon Chemicals International BV

Powder formulation comprising 20-75 wt % of di(4-tert-butylcyclohexyl) peroxydicarbonate and 25-80 wt % of a phlegmatizer selected from the group consisting of ethylene glycol dibenzoate, phenyl benzoate, trimethylol propane tribenzoate, dimethylsulfon, ethylene glycol ditoluate, 1,3-propanediol ditoluate, ethylene glycol 4-tert-butylbenzoate, ethylene glycol monobenzoate monotoluate, 2,3-butanediol dibenzoate, 4-methylphenyl benzoate acid ester, and combinations thereof.

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Номер записи: 58
21-01-2021 дата публикации

WATER TEMPERATURE AS A MEANS OF CONTROLLING KINETICS OF ONSITE GENERATED PERACIDS

Номер: US20210015096A1
Автор: Herdt Brandon, Kraus Paul R., Li Junzhong, McSherry David D., Rustad Thomas C., Staub Richard, Walsh Richard
Принадлежит:

Methods and systems for temperature-controlled, on-site generation of peracids, namely peroxycarboxylic acids and peroxycarboxylic acid forming compositions are disclosed. In particular, methods for using an adjustable biocide formulator or generator system overcome the limitations of temperature on the kinetics of the peracid generation and/or peracid decomposition inside an adjustable biocide formulator or generator system. The methods include the controlling of the temperature of at least one raw starting material, namely water, to improve upon methods of on-site generation of peracids. The methods allow for the generation of user-selected chemistry without regard to the ambient temperatures of the raw starting materials and/or the biocide formulator or generator system. 1. A method for peroxycarboxylic acid forming composition generation or peroxycarboxylic acid generation comprising:inputting a user-desired or system-controlled volume or mass of a peroxycarboxylic acid forming composition or peroxycarboxylic acid into a control software for on-site generation; andcombining one or more esters of a polyhydric alcohol and a C1 to C18 carboxylic acid, a source of alkalinity and an oxidizing agent at an alkaline pH of at least about 12 in an adjustable biocide formulator or generator system, wherein said system is an apparatus that is insensitive to environmental temperatures of the location of the apparatus and/or reagents comprising a reaction vessel, a series of feed pumps, an outlet for dosing the peroxycarboxylic acid forming composition or the peroxycarboxylic acid from said reaction vessel and a controller for a user- or system-inputted selection device; andgenerating the peroxycarboxylic acid forming composition or peroxycarboxylic acid;wherein said temperature insensitivity to the environmental temperatures of the location of the apparatus and/or reagents is controlled by a mechanism for maintaining a controlled temperature of said reaction vessel and/or ...

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Номер записи: 59
18-01-2018 дата публикации

Salts of Prostaglandin Analog Intermediates

Номер: US20180016230A1
Автор: Duncan Sammy Chris, Kotipalli Uma, Li Kangying, Li Yonggang, Lv Honghai, Zhao Yajun
Принадлежит:

The present invention relates to crystalline 1-adamantanamine salts, and polymorphic forms thereof, of prostaglandin analog intermediates of formula 3a, 4a and 6a, useful in the preparation of Tafluprost and Lubiprostone and processes for their preparation. The process includes combining 1-adamantanamine, water, an organic solvent, and a compound of Formula 3 or 6, thereby obtaining a suspension. The process also includes isolating the solid salt of Formula 3a or 6a from the suspension. 2. The crystalline salt of having the Formula 3a.3. The crystalline salt of claim 2 , wherein the salt is characterized by a Powder X-Ray Diffraction (PXRD) diffractogram comprising a peak claim 2 , expressed in degrees two-theta claim 2 , at 11.0+/−0.2 claim 2 , and at least four peaks claim 2 , expressed in degrees two-theta claim 2 , selected from the group consisting of: 3.7+/−0.2 claim 2 , 7.5+/−0.2 claim 2 , 8.1+/−0.2 claim 2 , 9.5+/−0.2 claim 2 , 12.9+/−0.2 claim 2 , 13.6+/−0.2 claim 2 , 15.1+/−0.2 claim 2 , 15.7+/−0.2 claim 2 , 17.0+/−0.2 claim 2 , and 20.5+/−0.2.4. The crystalline salt of claim 3 , wherein the PXRD diffractogram comprises peaks claim 3 , expressed in degrees two-theta claim 3 , at: 3.7+/−0.2 claim 3 , 7.5+/−0.2 claim 3 , 8.1+/−0.2 claim 3 , 9.5+/−0.2 claim 3 , 11.0+/−0.2 claim 3 , 12.9+/−0.2 claim 3 , 13.6+/−0.2 claim 3 , 15.1+/−0.2 claim 3 , 15.7+/−0.2 claim 3 , 17.0+/−0.2 and 20.5+/−0.2.5. The crystalline salt of claim 3 , wherein the salt is characterized by a Differential Scanning Calorimetry (DSC) thermogram comprising an endothermic peak having a peak onset at approximately 78° C.6. The crystalline salt of having the Formula 4a.702. The crystalline salt of claim 6 , wherein the salt is Form APO-I characterized by a Powder X-Ray Diffraction (PXRD) diffractogram comprising a peak claim 6 , expressed in degrees two-theta claim 6 , at approximately 5.6+/−. claim 6 , and at least four peaks claim 6 , expressed in degrees two-theta claim 6 , selected from ...

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Номер записи: 60
15-01-2015 дата публикации

Process for Producing Phenol

Номер: US20150018583A1
Автор: Becker Christopher L., Kuechler Keith H., Lattner James R., Nair Hari
Принадлежит:

In a process for producing phenol, benzene is reacted with a source of hydrogen containing methane in the presence of a hydroalkylation catalyst under conditions effective to produce a hydroalkylation reaction effluent comprising cyclohexylbenzene, benzene, hydrogen, and methane. A first stream comprising hydrogen, methane, and benzene is removed from the hydroalkylation reaction effluent and the first stream is washed with a second stream containing cyclohexylbenzene to produce a benzene-depleted hydrogen stream containing hydrogen and methane and a wash stream containing cyclohexylbenzene and benzene. 1. A process for producing phenol , the process comprising:(a) reacting benzene with a hydrogen-containing stream in the presence of a hydroalkylation catalyst under conditions effective to produce a hydroalkylation reaction effluent comprising cyclohexylbenzene, benzene, and hydrogen;(b) removing a first stream from the hydroalkylation reaction effluent, said first stream comprising hydrogen and benzene; and(c) washing at least a portion of the first stream with a second stream containing cyclohexylbenzene to produce a benzene-depleted hydrogen stream and a wash stream containing cyclohexylbenzene and benzene.2. The process of claim 1 , wherein the first stream is substantially in the vapor phase and the second stream is substantially in the liquid phase.3. The process of claim 1 , wherein at least 50 wt % of the benzene contained in said at least a portion of the first stream is transferred to the wash stream in said washing (c) claim 1 , the wt % based upon the weight of said at least a portion of the first stream.4. The process of claim 1 , wherein the second stream contains less than 1 wt % of benzene claim 1 , based upon the weight of the second stream.5. The process of claim 1 , wherein the benzene-depleted hydrogen stream contains less than 0.1 wt % benzene claim 1 , based upon the weight of the benzene-depleted hydrogen stream.6. The process of claim 1 , ...

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Номер записи: 61
17-01-2019 дата публикации

COMPOSITIONS RELATING TO VITAMIN D

Номер: US20190016677A1
Автор: Drinan Martin A., Liao Qimu, Sharma Manoj, Teng Zhu, Wei Tie Quan
Принадлежит: SIEMENS HEALTHCARE DIAGNOSTICS INC.

Compounds include compounds of the Formula I, namely, (R)-(L)-Z wherein R, L, p and q are as defined herein. 819.-. (canceled) The subject application claims benefit under 35 USC § 119(e) of U.S. provisional Application No. 62/018,008, filed Jun. 27, 2014. The entire contents of the above-referenced patent application are hereby expressly incorporated herein by reference.This invention relates to compositions, methods and kits for determining the presence and/or amount of vitamin D analytes, including vitamin D isomers, and metabolites thereof in a sample suspected of containing the same.The term “vitamin D” refers to a group of fat-soluble secosteroids. In humans, vitamin D is unique because it can be ingested as cholecalciferol (vitamin D) or ergocalciferol (vitamin D) and because the body can also synthesize it (from cholesterol) when sun exposure is adequate. Because of this latter property, vitamin D is considered by some to be a non-essential dietary vitamin although most consider it an essential nutrient. Vitamin D has an important physiological role in the positive regulation of calcium ion homeostasis. Vitamin Dis the form of the vitamin synthesized by animals. It is also a common supplement added to milk products and certain food products as is vitamin D.Both dietary and intrinsically synthesized vitamin Dmust undergo metabolic activation to generate bioactive metabolites. In humans, the initial step of vitamin Dactivation occurs primarily in the liver and involves hydroxylation to form the intermediate metabolite 25-hydroxycholecalciferol. Calcidiol is the major form of Vitamin Din the circulatory system. Vitamin Dalso undergoes similar metabolic activation to 25-hydroxyvitamin D. Collectively these compounds are called 25-hydroxyvitamin D (abbreviated 25(OH)D) and they are the major metabolites that are measured in serum to determine vitamin D status; 25(OH)D and its epimers are both pre-hormones that need to be converted into 1,25(OH)D to exert ...

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Номер записи: 62
17-01-2019 дата публикации

Non-Alpha Substituted Peroxy Acids and Uses Thereof

Номер: US20190016678A1
Автор: Ganguly-Mink Sangeeta, Littel Kenneth J., Zhu Shui Ping
Принадлежит:

The present disclosure is related to non-alpha-substituted, low molecular weight peracid compositions. The peracids have no or a negligible amount of odor, have good stability, and have antimicrobial properties. The peracid compositions can be formulated into a wide variety of end use products, including disinfectants, sanitizers, sporicides, fungicides, laundry products, hard surface cleaners, bleaching agents, personal cleansers, and water treatment products. 2. The composition of claim 1 , wherein the peracid has the structure of Formula 1 claim 1 , n is 1 and X is OH.3. The composition of claim 1 , wherein the peracid has the structure of Formula 1 claim 1 , n is from 1 to 4 claim 1 , and X is Cl claim 1 , OH claim 1 , or OCH.4. The composition of claim 1 , wherein the composition is a concentrate and the peracid concentration is from about 0.001% to about 15% by weight claim 1 , based on the total weight of the concentrate.5. The composition of claim 4 , wherein the peracid concentration is from about 0.01% to about 10% by weight.6. The composition of claim 4 , wherein the peracid concentration is from about 0.1% to about 5% by weight.7. The composition of claim 4 , wherein the peracid concentration after dilution is from 1 to 10 claim 4 ,000 ppm.8. The composition of claim 4 , wherein the peracid concentration after dilution is from 100 to 5000 ppm.9. The composition of claim 1 , wherein the composition further comprises at least one surfactant selected from the group consisting of anionic claim 1 , nonionic claim 1 , amphoteric claim 1 , zwitterionic claim 1 , and cationic surfactants claim 1 , and combinations thereof.10. The composition of claim 9 , wherein the at least one surfactant comprises an alcohol ethoxylate nonionic surfactant.11. The composition of claim 10 , wherein the alcohol ethoxylate surfactant comprises an ethoxylated C10-C14 alkyl alcohol.12. The composition of claim 9 , wherein the at least one surfactant comprises a cationic quaternary ...

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Номер записи: 63
25-01-2018 дата публикации

POWDER MIXTURE COMPRISING ORGANIC PEROXIDE

Номер: US20180022892A1
Автор: DEN BRABER Antonie, JANSEN Martin Hermanus Maria, MAJOOR Markus Oliver, Steensma Maria, Zuijderduin Albert Roland
Принадлежит:

Powder mixture comprising: −20-90 wt % of one or more powdered organic peroxides and −10-80 wt % of one or more powdered filler materials, at least 60 wt % thereof being barium sulphate. 1. Powder mixture comprising:20-90 wt % of one or more powdered organic peroxides and10-80 wt % of one or more powdered filler materials, at least 60 wt % thereof being barium sulphate.2. Powder mixture according to wherein the powder mixture comprises 1-30 wt % of water.3. Powder mixture according to wherein the organic peroxide is selected from the group consisting of dibenzoyl peroxide claim 1 , substituted dibenzoyl peroxides claim 1 , di (tert-butylperoxyisopropyl)benzene claim 1 , dicumyl peroxide claim 1 , di(dichlorobenzoyl)peroxides claim 1 , diisopropyl peroxydicarbonate claim 1 , di(t-butylcyclohexyl)peroxydicarbonate claim 1 , dicetyl peroxydicarbonate claim 1 , dimyristyl peroxydicarbonate claim 1 , and didecanoyl peroxide.4. Powder mixture according to wherein the organic peroxide is selected from the group consisting of dibenzoyl peroxide and substituted dibenzoyl peroxides.5. Powder mixture according to wherein the organic peroxide is di(4-methylbenzoyl) peroxide.6. Powder mixture according to wherein barium sulphate contains primary particles with an average particle size (d50) in the range 0.5-3 microns.7. Process for the preparation of a powder mixture according to wherein 20-90 wt % of one or more powdered organic peroxides and 10-80 wt % of one or more powdered filler materials claim 1 , at least 60 wt % thereof being barium sulphate claim 1 , are homogenized and de-agglomerated until an average particle diameter (d50) below 200 microns is reached.8. Process according to wherein the powdered organic peroxide contains 5-70 wt % of water.9. Process according to wherein the organic peroxide is selected from the group consisting of dibenzoyl peroxide claim 7 , substituted dibenzoyl peroxides claim 7 , di(tert-butylperoxyisopropyl)benzene claim 7 , dicumyl peroxide ...

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Номер записи: 64
10-02-2022 дата публикации

Perfluoroacyl peroxide production method, and fluoroalkyl iodide production method

Номер: US20220041549A1
Автор: Shintaro Fukunaga, Tomoyuki Fujita
Принадлежит: Asahi Glass Co Ltd

To provide a method for producing a perfluoroacyl peroxide which can suppress formation of solid matters in a reaction apparatus, and a method for producing a fluoroalkyl iodide. The method for producing a perfluoroacyl peroxide of the present invention is a method for producing a perfluoroacyl peroxide, which comprises: mixing an organic solvent solution containing a perfluoroacyl halide and an organic solvent which is at least one perfluoroalkyl iodide selected from the group consisting of C 2 F 5 I, C 4 F 9 I and C 6 F 13 I, a first aqueous solution containing hydrogen peroxide, and a second aqueous solution containing a basic alkali metal compound, to obtain a mixed liquid, and reacting the perfluoroacyl halide and the hydrogen peroxide in the mixed liquid to produce a perfluoroacyl peroxide, wherein the pH of the aqueous phase of the mixed liquid is adjusted to be from 7 to 14.

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Номер записи: 65
10-02-2022 дата публикации

USE OF AT LEAST ONE HEMI-PEROXYACETAL, ALONE OR IN COMBINATION WITH OTHER PEROXIDES, TO PROMOTE POLYMERISATION OR COPOLYMERISATION OF ETHYLENE UNDER HIGH PRESSURE

Номер: US20220041550A1
Автор: MENENTEAU Vincent, Van Hemelryck Bruno
Принадлежит:

The present invention relates to the use of at least one peroxide selected from the group consisting of hemiperoxyacetals, alone or in combination with one or more distinct additional peroxides, for the radical polymerization or copolymerization of ethylene under high pressure. 121-. (canceled)22. An organic peroxide , for use alone or in combination with one or more distinct additional organic peroxides , selected from the group consisting of hemiperoxyacetals for the radical polymerization or copolymerization of ethylene under high pressure.23. The organic peroxide of claim 22 , which is selected from the group consisting of hemiperoxyacetals having a half-life temperature at one minute and at atmospheric pressure of from 125° C. to 160° C.25. The organic peroxide of claim 22 , wherein the organic peroxide is selected from the group consisting of 1-methoxy-1-tert-amylperoxycyclohexane (TAPMC) claim 22 , 1-methoxy-1-t-butylperoxycyclohexane (TBPMC) claim 22 , 1-methoxy-1-t-amylperoxy-3 claim 22 ,3 claim 22 ,5-trimethylcyclohexane claim 22 , 1-methoxy-1-t-butylperoxy-3 claim 22 ,3 claim 22 ,5-trimethylcyclohexane claim 22 , 1-ethoxy-1-t-amylperoxycyclohexane claim 22 , 1-ethoxy-1-t-butylperoxycyclohexane claim 22 , 1-ethoxy-1-t-butyl-3 claim 22 ,3 claim 22 ,5-peroxycyclohexane and mixtures thereof.26. The organic peroxide of claim 22 , wherein the organic peroxide is 1-methoxy-1-tert-amylperoxycyclohexane.27. The organic peroxide of claim 22 , wherein the additional peroxide or peroxides is or are selected from the group consisting of peroxyacetals.28. The organic peroxide of claim 22 , wherein the additional peroxide or peroxides is or are selected from the group consisting of peroxyacetals capable of initiating the radical polymerization or copolymerization of ethylene under high pressure in a temperature range of from 190° C. to 250° C.30. The organic peroxide of claim 22 , wherein the additional peroxide or peroxides is or are selected from the group consisting ...

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Номер записи: 66
22-01-2015 дата публикации

ESTERS OF O-SUBSTITUTED HYDROXY CARBOXYLIC ACIDS AND PREPARATIONS THEREOF

Номер: US20150025247A1
Автор: Boaz Neil Warren, DELAIRE Sabine, Deng Liu
Принадлежит:

Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: 124-. (canceled)26. The ester according to claim 25 , wherein Ris independently selected from the group consisting of substituted and unsubstituted claim 25 , branched- and straight-chain saturated C-Calkyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Calkenyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Cdienyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Ctrienyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Ctetraenyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Cpentaenyl; substituted and unsubstituted C-Ccycloalkyl; substituted and unsubstituted C-Ccarbocyclic aryl; substituted and unsubstituted C-Cheterocyclic group; and mixtures thereof.27. The ester according to claim 26 , wherein said alkyl claim 26 , alkenyl claim 26 , dienyl claim 26 , trienyl claim 26 , tetraenyl claim 26 , pentaenyl claim 26 , and cycloalkyl groups are substituted with at least one selected from the group consisting of C-C-alkoxy claim 26 , carboxyl claim 26 , amino claim 26 , C-Caminocarbonyl claim 26 , C-Camido claim 26 , cyano claim 26 , C-C-alkoxycarbonyl claim 26 , C-C-alkanoyloxy claim 26 , hydroxy claim 26 , aryl claim 26 , heteroaryl claim 26 , thiol claim 26 , thioether claim 26 , C-Cdialkylamino claim 26 , C-Ctrialkylammonium and halogen.28. The ester according to claim 26 , wherein said aryl group is at least one selected from the group consisting of phenyl claim 26 , naphthyl claim 26 , anthracenyl claim 26 , and phenyl claim 26 , naphthyl claim 26 , or anthracenyl substituted with one to five substituents.29. The ester according to claim 28 , wherein said one to five substituents of phenyl claim 28 , naphthyl claim 28 , or anthracenyl are selected from the group consisting of C-C-alkyl claim 28 , substituted C-C-alkyl claim 28 ...

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Номер записи: 67
22-01-2015 дата публикации

Process for preparing synthetic prostacyclins

Номер: US20150025255A1
Автор: Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev, George Petros Yiannikouros, Panos Kalaritis
Принадлежит: Lung Biotechnology Inc

The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.

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Номер записи: 68
10-02-2022 дата публикации

Release reagent for vitamin d compounds

Номер: US20220043012A1
Автор: Christian Vogl, Sascha Antoni
Принадлежит: Roche Diagnostics Operations Inc

A reagent composition for releasing vitamin D compounds bound to vitamin D-binding protein and an in vitro method for the detection of a vitamin D compound in which the vitamin D compound is released from vitamin D-binding protein by the use of this reagent composition as well as the reagent mixture obtained in this manner. Also disclosed is the use of the reagent compositions to release vitamin D compounds as well as a kit for detecting a vitamin D compound.

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Номер записи: 69
24-04-2014 дата публикации

Stabilized 1, 25-Dihydroxyvitamin D2 and Method of Making Same

Номер: US20140113886A1
Автор: Uttam Saha
Принадлежит: Cytochroma Inc

A stabilized 1,25-dihydroxyvitamin D 2 composition which is particularly well suited for pharmaceutical formulations, pharmaceutical formulations of the 1,25-dihydroxyvitamin D 2 composition, and a method of making the purified composition by purifying a crude 1,25-dihydroxyvitamin D 2 from acetone/water, are disclosed.

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Номер записи: 70
29-01-2015 дата публикации

SUGAR ESTER PERACID ON SITE GENERATOR AND FORMULATOR

Номер: US20150031764A1
Автор: Kraus Paul R., Mehus Richard J., Rustad Thomas C., Sanville Katherine M.
Принадлежит:

Methods and systems for on-site generation of peracid chemistry, namely peroxycarboxylic acids and peroxycarboxylic acid forming compositions, are disclosed. In particular, an adjustable biocide formulator or generator system is designed for on-site generation of peroxycarboxylic acids and peroxycarboxylic acid forming compositions from sugar esters. Methods of using the in situ generated peroxycarboxylic acids and peroxycarboxylic acid forming compositions are also disclosed. 1. An adjustable biocide formulator or generator system for on-site peroxycarboxylic acid forming composition generation comprising:an apparatus comprising at least one reaction vessel, a series of feed pumps and an outlet for dosing a peroxycarboxylic acid forming composition from said reaction vessel;wherein said feed pumps are in fluid connection with said reaction vessel and supply reagents to produce said peroxycarboxylic acid forming composition in said reaction vessel;wherein said reagents comprise an ester of a polyhydric alcohol and a C1 to C18 carboxylic acid, a source of alkalinity and an oxidizing agent;wherein said reaction vessel is in fluid connection with said outlet to dispense said peroxycarboxylic acid forming composition; andwherein said peroxycarboxylic acid forming composition is an individual or mixed peroxycarboxylic acid forming composition according to a user- or system-inputted selection.2. The system according to claim 1 , wherein the source of alkalinity is sodium hydroxide (e.g. caustic soda) claim 1 , and wherein said sodium hydroxide is provided to said reaction vessel prior to the addition of said ester in a solution that is less than about 20 wt-% sodium hydroxide on an actives basis.3. The system according to claim 1 , further comprising at least one measurement device claim 1 , wherein said measurement device measures one or more reaction kinetics or system operations for said peroxycarboxylic acid forming composition generation selected from the group ...

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Номер записи: 71
04-02-2016 дата публикации

SUGAR ESTER PERACID ON SITE GENERATOR AND FORMULATOR

Номер: US20160031809A1
Автор: Kraus Paul R., Mehus Richard J., Rustad Thomas C., Sanville Katherine M.
Принадлежит:

Methods and systems for on-site generation of peracid chemistry, namely peroxycarboxylic acids and peroxycarboxylic acid forming compositions, are disclosed. In particular, an adjustable biocide formulator or generator system is designed for on-site generation of peroxycarboxylic acids and peroxycarboxylic acid forming compositions from sugar esters. Methods of using the in situ generated peroxycarboxylic acids and peroxycarboxylic acid forming compositions are also disclosed. 1. An adjustable biocide formulator or generator system for on-site peroxycarboxylic acid forming composition generation comprising:an apparatus comprising at least one reaction vessel, a series of feed pumps and an outlet for dosing a peroxycarboxylic acid forming composition from said reaction vessel;wherein said feed pumps are in fluid connection with said reaction vessel and supply reagents to produce said peroxycarboxylic acid forming composition in said reaction vessel;wherein said reagents comprise an ester of a polyhydric alcohol and a C1 carboxylic acid and an oxidizing agent;wherein said reaction vessel is in fluid connection with said outlet to dispense said peroxycarboxylic acid forming composition; andwherein said peroxycarboxylic acid forming composition is an individual or mixed peroxycarboxylic acid forming composition according to a user- or system-inputted selection.2. The system according to claim 1 , wherein the reagents further comprise a source of alkalinity claim 1 , and wherein said alkalinity is sodium hydroxide is provided to said reaction vessel prior to the addition of said ester in a solution that is less than about 20 wt-% sodium hydroxide on an actives basis.3. The system according to claim 1 , further comprising at least one measurement device claim 1 , wherein said measurement device measures one or more reaction kinetics or system operations for said peroxycarboxylic acid forming composition generation selected from the group consisting of fluorescence claim 1 ...

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Номер записи: 72
29-01-2015 дата публикации

PROCESS FOR PREPARATION OF PROSTAGLANDIN F2 ALPHA ANALOGUES

Номер: US20150031898A1
Автор: Chodynski Michal, Cmoch Piotr, Dams Iwona, Kosinska Monika, Krupa Malgorzata, Kutner Andrzej, Pietraszek Anita, Zezula Marta
Принадлежит: INSTYTUT FARMACEUTYCZNY

A convergent synthesis of the prostaglandin F analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate. 2. The process of claim 1 , wherein the α-sulfonyl carbanion of the formula (II) is generated by an alkali metal amide claim 1 , selected from the group comprising lithium N claim 1 ,N-bis(trimethylsilyl)amide claim 1 , sodium N claim 1 ,N-bis(trimethylsilyl)amide claim 1 , lithium diisopropylamide and sodium diisopropylamide.3. The process of claim 2 , wherein the α-sulfonyl carbanion of the formula (II) is generated by lithium diisopropylamide.4. The process of claim 1 , wherein the desulfonation of the β-hydroxysulfones of the formula (V) is performed by using sodium amalgam in the presence of NaHPObuffer.5. The process of claim 1 , wherein the R-Rgroups are removed by reacting the compound of the formula (VI) with hydrogen fluoride or tetra-n-butylammonium fluoride.6. The process of claim 1 , wherein the Rgroup of the compound of the formula (VII) is hydrolyzed in the presence of an aqueous solution of citric acid.7. The process of claim 1 , wherein the Rgroup of the compound of the formula (VIII) is hydrolyzed with an alkali metal hydroxide claim 1 , preferably with lithium hydroxide.8. The process of claim 1 , wherein the compound of formula (VIII) is alkylated with a C-alkyl halogen in the presence of a base claim 1 , preferably 1 claim 1 ,8-diazabicyclo[5.4.0]undec-7-en (DBU).9. The process of claim 1 , wherein the prostamid of the formula (IC) claim 1 , which is isopropyl ester of 16-[3-(trifluoromethoxy)phenoxy]-17 claim 1 ,18 claim 1 ,19 claim 1 ,20-tetranor-prostaglandin F (travoprost) claim 1 , is obtained in a diastereoisomeric excess greater than ...

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Номер записи: 73
01-02-2018 дата публикации

PREPARATION OF COMPOUNDS FROM LEVULINIC ACID

Номер: US20180029980A1
Автор: Dutta Saikat, Mascal Mark, Wu Linglin
Принадлежит:

The present invention provides a method of making carboxylic acids from levulinic acid, such as succinic acid and 3-hydroxypropanoic acid, by reacting levulinic acid with an oxidant such as hydrogen peroxide under acidic or basic conditions. 1. A method of preparing a carboxylic acid , comprising:forming a reaction mixture comprising levulinic acid, an oxidant, and an acid or a base, under conditions suitable to prepare the carboxylic acid.3. The method of claim 1 , wherein the oxidant is hydrogen peroxide.4. The method of claim 3 , wherein the reaction mixture is substantially free of an oxidizing metal catalyst.5. The method of claim 1 , wherein the carboxylic acid is succinic acid.6. The method of claim 5 , the method comprising:forming the reaction mixture comprising levulinic acid, the oxidant and an acid, thereby preparing the succinic acid.7. The method of claim 5 , the method comprising:forming the reaction mixture comprising levulinic acid, the oxidant and an acid; andheating the reaction mixture at a temperature of from about 30° C. to about 100° C., thereby preparing the succinic acid.8. The method of claim 7 , wherein the acid is selected from the group consisting of hydrofluoric acid claim 7 , hydrochloric acid claim 7 , hydrobromic acid claim 7 , hypochloric acid claim 7 , sulfuric acid claim 7 , nitric acid claim 7 , phosphoric acid claim 7 , hexafluorophosphoric acid claim 7 , methanesulfonic acid claim 7 , benzenesulfonic acid claim 7 , p-toluenesulfonic acid claim 7 , trifluoromethanesulfonic acid claim 7 , fluoroacetic acid claim 7 , and trifluoroacetic acid.9. The method of claim 7 , wherein the acid is trifluoroacetic acid.10. The method of claim 7 , wherein the method comprises:forming the reaction mixture comprising levulinic acid, trifluoroacetic acid, and hydrogen peroxide; andheating the reaction mixture at a temperature of from about 50° C. to about 100° C., thereby preparing succinic acid.11. The method of claim 1 , wherein the carboxylic ...

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Номер записи: 74
31-01-2019 дата публикации

RETINOID DOUBLE CONJUGATE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS FOR TREATING OF SKIN CONDITIONS

Номер: US20190029941A1
Автор: II Joseph A., Lewis
Принадлежит:

Provided are methods of treating certain skin conditions in a human in which the skin of the human in need of such treatment is contacted with an effective amount of a particular composition. 2. The method of claim 1 , wherein the composition further comprises:a carrier; and0.01 to 0.5 wt %, relative to the total weight of the composition, of the molecule of formula Id.3. The method of claim 1 , wherein the composition further comprises:an α-hydroxy acid.6. The method of claim 1 , wherein the molecule of formula (Id) is present in an amount of 0.01 to 0.25 wt %.7. The method of claim 1 , wherein the molecule of formula (Id) is present in an amount of 0.01 to less than 0.2 wt %.8. The method of claim 1 , wherein the molecule of formula (Id) is present in the amount of 0.02 to 0.175 wt %. This is a continuation application of co-pending U.S. application Ser. No. 15/036,467, filed May 13, 2016, which is the U.S. national stage application under 35 U.S.C. § 371 of International Application No. PCT/US2014/065604, filed on Nov. 14, 2014, and claims benefit to U.S. Provisional Application Ser. No. 61/904,532, filed Nov. 15, 2013, the entire disclosures of each of which applications are hereby incorporated by reference herein. The international application was published in English on May 21, 2015, as WO 2015/073769 A1 under PCT Article 21(2).The present invention relates to retinoids, organic acids/alcohols, and alcohols or linked alkyl groups, syntheses and the use of the same in treating skin conditions.Skin is exposed to damage resulting from various sources, including both environmental factors and biochemical processes. Oxidative processes damage proteins, lipids, and other cellular components necessary to maintain the health and appearance of skin, resulting in skin changes, such as skin aging, hyperpigmentation, UV damage, lines, wrinkles, uneven skin texture, etc.Skin aging is accompanied by a number of morphophysiological changes which are described in the ...

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Номер записи: 75
30-01-2020 дата публикации

SITU GENERATION OF PEROXYCARBOXYLIC ACIDS AT ALKALINE pH, AND METHODS OF USE THEREOF

Номер: US20200029560A1
Автор: Li Junzhong, McSherry David D., Staub Richard
Принадлежит:

The present disclosure is related to percarboxylic acid compositions formed in situ in non-equilibrium reactions. The peroxycarboxylic acid compositions are formed using ester based starting materials. Methods for using the percarboxylic acid compositions are also disclosed. 119-: (canceled)20. A peroxycarboxylic acid forming composition comprising:an ester of a polyhydric alcohol and a C1 to C18 carboxylic acid, wherein said ester has an HLB value of 3 or greater;an oxidizing agent comprising a hydrogen peroxide donor; anda source of alkalinity;wherein said composition is not at equilibrium, forms a peroxycarboxylic acid in situ, and has a pH greater than about 12.21. The composition of claim 20 , wherein the polyhydric alcohol is a sugar and/or a sugar alcohol.22. The composition of claim 20 , further comprising a dispersing agent claim 20 , and wherein the dispersing agent is a sulfonated oleic acid claim 20 , 1-octanesulfonic acid claim 20 , and/or sodium lauryl sulfonate.23. The composition of claim 20 , further comprising a solvent.24. The composition of claim 23 , wherein the solvent is a water soluble alcohol and wherein the water soluble alcohol is methanol claim 23 , ethanol claim 23 , propanol claim 23 , isopropanol claim 23 , butanol claim 23 , an ether and/or a ketone.25. The composition of claim 20 , wherein the alcohol is ethylene glycol claim 20 , propylene glycol claim 20 , glycerol claim 20 , sorbitol claim 20 , and/or sorbitan claim 20 , and wherein the ester is glycerol monooctanoate claim 20 , glycerol dioctanoate claim 20 , glycerol trioctanoate claim 20 , sorbitan monooctanoate claim 20 , sorbitan dioctanoate claim 20 , sorbitan trioctanoate claim 20 , and/or laurate sucroside claim 20 , and wherein the oxidizing agent comprises a hydrogen peroxide donor.26. The composition of claim 20 , wherein the hydrogen peroxide donor is hydrogen peroxide claim 20 , a percarbonate claim 20 , a perborate claim 20 , urea hydrogen peroxide claim 20 , and/or ...

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Номер записи: 76
30-01-2020 дата публикации

PROCESS TO PREPARE TREPROSTINIL, THE ACTIVE INGREDIENT IN REMODULIN®

Номер: US20200030271A1
Автор: Batra Hitesh, Penmasta Raju, Tuladhar Sudersan M., Walsh David A.
Принадлежит: United Therapeutics Corporation

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil. 1. A pharmaceutical batch of a salt of treprostinil that can be stored as a stable compound at ambient temperature and that is prepared by a method comprising (a) alkylating a benzindene triol , (b) hydrolyzing the product of step (a) to form a solution comprising treprostinil , and (c) contacting the solution comprising treprostinil from step (b) with a base to form a salt of treprostinil , wherein forming the salt of step (c) reduces the amount of one or more impurities resulting from steps (a) and/or (b) in the pharmaceutical batch , said pharmaceutical batch being at least 2.9 grams.2. The pharmaceutical batch of claim 1 , wherein the method further comprises converting the salt of treprostinil to treprostinil by acidification.3. The pharmaceutical batch of claim 1 , wherein the pharmaceutical batch has been dried under vacuum.4. The pharmaceutical batch of claim 1 , wherein the base is diethanolamine.5. A pharmaceutical product comprising a carrier and a therapeutically effective amount of a salt of treprostinil claim 1 , wherein the salt of treprostinil is from a pharmaceutical batch as claimed in .6. A pharmaceutical product comprising a carrier and a therapeutically effective amount of treprostinil claim 2 , wherein the treprostinil is from a pharmaceutical batch as claimed in .7. The pharmaceutical product of claim 5 , wherein the salt is the diethanolamine salt of treprostinil.8. A method of preparing a pharmaceutical product from a pharmaceutical batch as claimed in claim 5 , comprising storing a pharmaceutical batch of a salt of treprostinil as claimed in at ambient temperature and preparing a pharmaceutical product from the pharmaceutical batch after storage.9. A method as claimed in claim 8 , wherein the salt of ...

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Номер записи: 77
04-02-2021 дата публикации

GENERATION OF PEROXYFORMIC ACID THROUGH POLYHYDRIC ALCOHOL FORMATE

Номер: US20210029996A1
Автор: Brewster Allison, Cheritu Taz, Fast Jonathan P., Hanson Catherine, Lange Steven J., Li Junzhong, Staub Richard
Принадлежит:

The present invention relates generally to peroxyformic acid forming compositions, methods for forming peroxyformic acid, preferably in situ, using the peroxyformic acid forming compositions. The present invention also relates to the peroxyformic acid formed by the above compositions and methods. The present invention further relates to the uses of the peroxyformic acid, preferably in situ, for treating a surface or a target. The present invention further relates to methods for treating a biofilm using peroxyformic acid, including peroxyformic acid generated in situ. 1192-. (canceled)193. A peroxyformic acid forming composition comprising:a) a first reagent that comprises an ester of a polyhydric alcohol and formic acid; andb) a second reagent that comprises hydrogen peroxide or that comprises a substance that generates hydrogen peroxide when in contact with a liquid;wherein the first reagent and the second reagent are kept separately prior to use, and when it is time to generate peroxyformic aid, the first reagent and the second reagent are contacted with each other to generate a formed liquid comprising peroxyformic acid; andwherein the pH of the formed liquid becomes about 8 or lower within about 1 minute after the contacting between the first reagent and the second reagent.194. The composition of claim 193 , wherein the ester of a polyhydric alcohol and formic acid is derived from a sugar alcohol and formic acid.195. The composition of claim 194 , wherein the sugar alcohol is ethylene glycol claim 194 , methylene glycol claim 194 , propylene glycol claim 194 , or a combination thereof.196. The peroxyformic acid forming composition of claim 193 , wherein the ester of a polyhydric alcohol and formic acid comprises glycerol formates claim 193 , pentaerythritol formates claim 193 , mannitol formates claim 193 , propylene glycol formates claim 193 , sorbitol formates claim 193 , sugar formates claim 193 , or a combination thereof.197. The peroxyformic acid forming ...

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Номер записи: 78
31-01-2019 дата публикации

TETRAHYDRONAPHTHALENE DERIVATIVE

Номер: US20190031605A1
Автор: INAGAKI Yuichi, KUSUMI Kensuke, WATANABE Toshihide
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by general formula (I-1): 3. The compound according to claim 1 , wherein Y is —CH— or —O— claim 1 , or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein ring 1 is a C3-10 carbocyclic ring claim 1 , or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein ring 3 is a C3-7 saturated carbocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a 3- to 7-membered saturated heterocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein Z is a carboxyl group which may be substituted with a C1-8 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.7. A pharmaceutical composition comprising the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.8. The pharmaceutical composition according to claim 7 , which is an S1Pbinder and/or modulator.9. The pharmaceutical composition according to claim 7 , which is an agent for preventing and/or treating a S1P-mediated disease.10. The pharmaceutical composition according to claim 9 , wherein the S1P-mediated disease is neurodegenerative disease claim 9 , autoimmune disease claim 9 , infection or cancer.11. The pharmaceutical composition according to claim 10 , wherein the neurodegenerative disease is schizophrenia claim 10 , Binswanger's disease claim 10 , multiple sclerosis claim 10 , neuromyelitis optica claim 10 , Alzheimer's disease claim 10 , cognitive impairment claim 10 , amyotrophic lateral sclerosis or spinocerebellar ataxia.12. A method for preventing and/or treating a S1P-mediated disease claim 1 , comprising administering to a mammal an effective amount of the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.1314-. (canceled)15. The compound according to claim 2 ...

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Номер записи: 79
04-02-2021 дата публикации

Radical initiators and chain extenders for converting methane gas into methane-sulfonic acid

Номер: US20210032200A1
Автор: Alan K. Richards
Принадлежит: Veolia North America Regeneration Services LLC

Improved initiators, solvents, and SO3 mixtures are disclosed herein, which can increase the yields and efficiency of a chemical manufacturing process which uses a radical chain reaction to convert methane (CH4), which is a gas under any normal conditions, into methane-sulfonic acid (MSA), a liquid. MSA is useful and valuable in its own right, and it also can be processed to create desulfured fuels and other valuable chemicals. A preferred initiator combination has been identified, comprising at least two different sulfate peroxide compounds. One type or class of initiator can be called a “primary” (or major, main, principle, dominant, or similar terms) initiator, and the other type or class of initiator can be can be regarded as an “extender” (or secondary, supplemental, enhancing, tuning, tweaking, or similar terms) initiator. “Primary” initiator(s) include (unmethylated) Marshall's acid, mono-methyl-Marshall's acid, and di-methyl-Marshall's acid, while a secondary/extender initiator comprises methyl-Caro's acid, which can oxidize sulfur DI-oxide (an unwanted chain terminator) into sulfur TRI-oxide (an essential reagent). Various other enhancements to the MSA manufacturing process also are described.

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Номер записи: 80
04-02-2021 дата публикации

PERFLUORO DIACYL PEROXIDE, SOLUTION, POLYMERIZATION INITIATOR, POLYMER PREPARATION METHOD, AND PERFLUORO ACYL CHLORIDE

Номер: US20210032201A1
Автор: ISAKA Tadaharu
Принадлежит: DAIKIN INDUSTRIES, LTD.

A perfluorodiacyl peroxide represented by the following formula (1): 1. A perfluorodiacyl peroxide represented by the following formula (1):{'br': None, 'sub': 5', '11', '2, '(CFCOO)\u2003\u2003(1).'}2. A solution comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the perfluorodiacyl peroxide according to , and'}a solvent.3. The solution according to claim 2 ,wherein the solvent is a fluorine-containing solvent.4. A polymerization initiator comprising the perfluorodiacyl peroxide according to .5. A method for producing a polymer claim 1 , comprising polymerizing a radically polymerizable monomer with the perfluorodiacyl peroxide according to .6. A perfluoroacyl chloride represented by the following formula (2):{'br': None, 'sub': 5', '11, 'CFCOCl \u2003\u2003(2).'} The disclosure relates to perfluorodiacyl peroxides, solutions, polymerization initiators, methods of producing a polymer, and perfluoroacyl chlorides.Fluorine-based diacyl peroxides are known as polymerization initiators.For example, Non-Patent Literature 1 discloses synthesis of a perfluorodiacyl peroxide from a perfluoroacyl halide in the presence of HOand NaOH.Patent Literature 1 discloses production of bis(perfluoro-n-butyryl)peroxide using perfluoro-n-butyryl chloride.Non-Patent Literature 1: Chemical reviews., 1996, vol. 96, pp. 1779-1808The disclosure provides a novel perfluorodiacyl peroxide. The disclosure also provides a solution containing the perfluorodiacyl peroxide, a polymerization initiator containing the perfluorodiacyl peroxide, and a method for producing a polymer with the perfluorodiacyl peroxide. The disclosure also provides a novel perfluoroacyl chloride.The disclosure provides a perfluorodiacyl peroxide represented by the following formula (1):(CFCOO)  (1).The disclosure also provides a solution containing the perfluorodiacyl peroxide and a solvent.The solvent is preferably a fluorine-containing solvent.The disclosure also provides a polymerization initiator containing ...

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Номер записи: 81
09-02-2017 дата публикации

NEUTRALIZATION OF ACIDIC CATALYSTS IN THE PRODUCTION OF PHENOL

Номер: US20170036979A1
Автор: Jiang Xin, MU Jianhai
Принадлежит:

An improved method for the production of phenol. The method comprises (a) synthesizing phenol through a process that utilizes an acidic catalyst; (b) neutralizing the acidic catalyst after substantial completion of step (a) by addition thereto of a neutralization composition, wherein the neutralization composition contains an ethyleneamine derivative. 2. The method of wherein the ethyleneamine derivative is selected from the group consisting of: ethylenediamine (EDA) claim 1 , diethylenetriamine (DETA) claim 1 , triethylenetetramine (TETA) aminoethylpiperazine (AEP) claim 1 , tetraethylenepentamine (TEPA) claim 1 , heavy polyamine X (HPA-X) claim 1 , and mixtures of two or more thereof.3. The method of wherein the ethyleneamine derivative is selected from the group consisting of: ethylenediamine (EDA) claim 1 , diethylenetriamine (DETA) claim 1 , triethylenetetramine (TETA) claim 1 , and mixtures of two or more thereof.4. The method of wherein the neutralization composition is substantially free of amine compounds other than ethyleneamines5. The method of wherein the neutralization composition further comprises claim 1 , methylpentamethyenediamine claim 1 , hexamethylenediamine claim 1 , or mixtures thereof.6. The method of wherein step (a) comprises decomposing of cumene hydroperoxide in the presence of an acidic catalyst to form phenol claim 1 , acetone claim 1 , and α-methylstyrene.7. The method of wherein step (a) comprises:(i) oxidizing at least a portion of a feed containing cyclohexylbenzene to produce an oxidation composition containing cyclohexyl-1-phenyl-1-hydroperoxide; and(ii) cleaving the oxidation composition in the presence of an acidic catalyst to produce a cleavage reaction mixture comprising the acidic catalyst, phenol, and cyclohexanone. This invention relates generally to an improved method for the production of phenol.A commonly used phenol production method is decomposition of cumene hydroperoxide to phenol, acetone, and α-methylstyrene in the ...

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Номер записи: 82
09-02-2017 дата публикации

NEW PROCESS FOR THE PREPARATION OF HIGH PURITY PROSTAGLANDINS

Номер: US20170037002A1
Автор: BUZDER-LANTOS Péter, HAVASI Gábor, HORTOBÁGYI Irén, KARDOS Zsuzsanna, LÁSZLÓFI István, Takacs Laszlo, VAJDA Ervin
Принадлежит: CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.

The subject of the invention is a process for the preparation of high purity prostaglandin acid of the general formula II wherein the bonds marked with dotted lines represent single or double bonds wherein the double bonds may be cis- or trans oriented, Y represents 0 or CH, and Rstands for a phenyl group which is optionally substituted with CF, wherein the crude prostaglandin acid of the general formula II is purified by normal phase silicagel chromatography. 2. The process as defined in claim 1 , wherein chromatography is carried out by normal phase gravitational claim 1 , medium- or high pressure silica gel chromatography.3. The process as defined in claim 1 , wherein the applied silica gel is a spherical silica gel having average particle size in a range of 10-150 micrometer.4. The process as defined in claim 1 , wherein a multicomponent eluent mixture is applied as eluent.5. The process as defined in claim 4 , wherein the eluent mixture contains one or more apolar solvents claim 4 , one or more polar solvents and solvent of acidic character claim 4 , in a ratio of (91-73%):(24-8.7%):(0.1-4.3%).6. The process as defined in claim 5 , wherein the apolar component of the eluent mixture is straight or branched open-chain or cyclic or aromatic hydrocarbon claim 5 , optionally containing one or more substituents.7. The process as defined in claim 6 , wherein the substituent is halogen atom.8. The process as defined in claim 6 , wherein as apolar solvent aliphatic hydrocarbon is applied.9. The process as defined in claim 5 , wherein as polar solvent an alcohol- claim 5 , ether- claim 5 , ester- or ketone-type solvent is applied which contains straight or branched open-chain alkyl claim 5 , alkenyl or cyclic or cycloalkyl group.10. The process as defined in claim 9 , wherein as polar solvent Calcohol is applied.11. The process as defined in claim 10 , wherein as polar solvent isopropyl alcohol is applied.12. The process as defined in claim 5 , wherein the solvent of ...

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Номер записи: 83
12-02-2015 дата публикации

LOW VISCOSITY DIAROYL PASTE AND METHOD FOR MAKING THE SAME

Номер: US20150041711A1
Автор: Guigley Kevin S., Helton Brian S.
Принадлежит:

In various embodiments, the present invention pertains to diaroyl peroxide compositions and methods for making the same. 1. A method of making a diaroyl peroxide paste comprising:blending a diaroyl peroxide, at least one surfactant, and at least one diluent;waiting a predetermined period of time; andadding paraffin oil;wherein the paste is at least about 45% by weight diaroyl peroxide and has a viscosity of less than about 10,000 cP.2. The method of claim 1 , wherein the paste is not agitated during the waiting.3. The method of claim 1 , wherein the predetermined period of time is at least 5 minutes.4. The method of claim 3 , wherein the predetermined period of time is at least 30 minutes.5. The method of claim 1 , further comprising adding a dispersant.6. The method of claim 5 , wherein the dispersant is water.7. The method of claim 6 , wherein the water is added subsequent to the paraffin oil.8. The method of claim 6 , further comprising adding a water soluble salt.9. The method of claim 1 , further comprising adding salt.10. The method of claim 9 , wherein the salt is added subsequent to the addition of paraffin oil.11. The method of claim 9 , wherein the salt is one of sodium chloride claim 9 , an alkali carboxylic acid claim 9 , or mixture thereof.12. The method of claim 1 , wherein the diaroyl peroxide is dibenzoyl peroxide.13. The method of claim 1 , wherein the at least one diluent is one of a phthalate claim 1 , benzoate and dibenzoate claim 1 , phosphate claim 1 , citrate claim 1 , or adipate claim 1 , or mixtures thereof.14. The method of claim 13 , wherein the at least one diluent is a benzyl ester or mixture of benzyl esters.15. The method of claim 1 , wherein the paste is at least about 50% by weight diaroyl peroxide claim 1 , and wherein the predetermined period of time is at least 15 minutes.16. The method of claim 1 , wherein the paste is at least about 53% by weight diaroyl peroxide and has a viscosity of less than about 5 claim 1 ,000 cP.17. A ...

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Номер записи: 84
12-02-2015 дата публикации

Process for Producing Phenol

Номер: US20150045587A1
Автор: Garcia Roberto, Kiss Gabor, Wang Kun
Принадлежит: Exxonmobil Chemical Patents, Inc.

A process for producing phenol is described in which a feed comprising cyclohexylbenzene hydroperoxide is contacted with a cleavage catalyst comprising an aluminosilicate zeolite of the FAU type having a unit cell size less than 24.50 Å under cleavage conditions effective to convert at least part of the cyclohexylbenzene hydroperoxide into phenol and cyclohexanone. 1. A process for producing phenol , the process comprising:(a) contacting a feed comprising cyclohexylbenzene hydroperoxide with a cleavage catalyst comprising an aluminosilicate zeolite of the FAU type having a unit cell size less than 24.50 Å under cleavage conditions effective to convert at least part of the cyclohexylbenzene hydroperoxide into phenol and cyclohexanone.2. The process of claim 1 , wherein the feed comprises greater than 1 wt % of cyclohexylbenzene hydroperoxide claim 1 , based upon total weight of the feed.3. The process of claim 1 , wherein the feed comprises greater than 50 wt % of cyclohexylbenzene claim 1 , based upon total weight of the feed.4. The process of claim 1 , wherein the conversion of the cyclohexylbenzene hydroperoxide in the contacting step (a) is greater than 30%.5. The process of claim 1 , wherein the FAU type zeolite has a unit cell size less than or equal to 24.35 Å.6. The process of claim 1 , wherein the cleavage catalyst is substantially metal-free.7. The process of claim 1 , wherein at least a portion of the cleavage catalyst is contained in a fixed bed.8. The process of claim 1 , wherein the cleavage conditions include a temperature of about 20° C. to about 200° C. and a pressure of about 100 kPa claim 1 , gauge to about 2000 kPa claim 1 , gauge.9. The process of claim 1 , wherein the contacting step (a) is conducted in at least a first reactor and a second reactor connected in series.10. The process of claim 1 , wherein the cleavage catalyst has a pore volume of greater than 0.3 cc/g.11. The process of claim 1 , wherein the phenol is converted to at least one ...

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Номер записи: 85
18-02-2016 дата публикации

Process and Apparatus for Making Phenol and/or Cyclohexanone

Номер: US20160046550A1
Автор: Becker Christopher L., Coleman John S., Davis Jason D., Nair Hari, Patel Bryan A.
Принадлежит:

A process for producing phenol and/or cyclohexanone by cleaving cyclohexylbenzene hydroperoxide in a loop cleavage reactor comprising multiple reaction zones connected in series. In desirable embodiments, fresh cyclohexylbenzene hydroperoxide feed(s) are supplied to reaction zones the final reaction zone, and fresh acid catalyst is supplied only to the final reaction zone. In desirable embodiments, a portion of the effluent exiting the final reaction zone is recycled to the first reaction zone. Each reaction zone is equipped with a heat exchanger downstream of the feed port to extract heat generated from the cleavage reaction. 1. A process for making phenol and/or cyclohexanone , the process comprising:(A) providing a cleavage reactor having a plurality of reaction zones connected in series, the reaction zones comprising a first reaction zone, a final reaction zone and optionally one or more intermediate reaction zone(s) between the first reaction zone and the final reaction zone; wherein:each of the reaction zones comprises a processed feed port, a fresh feed port, a heat exchanger at least partly downstream of the processed feed port and the fresh feed port in the same reaction zone, and an effluent port, except that the heat exchanger for the final reaction zone is optional;the effluent port of any given reaction zone other than the final reaction zone is in fluid communication with the processed feed port of the immediately following reaction zone in the series; andthe effluent port of the final reaction zone is in fluid communication with the processed feed port of the first reaction zone;(B) supplying a fresh reaction feed comprising cyclohexylbenzene hydroperoxide to each reaction zone other than the final reaction zone via the fresh feed port of the reaction zone and producing an effluent at the effluent port of the reaction zone;(C) supplying at least a portion of the effluent exiting the effluent port of each of the reaction zones other than the final ...

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Номер записи: 86
15-02-2018 дата публикации

METHOD FOR PRODUCING POWDERED LAUROYL PEROXIDE

Номер: US20180044289A1
Автор: HERMANN Dominik, Nagl Iris, WOLF Hanno
Принадлежит:

The present application relates to a method for producing powdered lauroyl peroxide which is characterised in that a reaction mixture is used which comprises water, lauric acid chloride, hydrogen peroxide, an inorganic base and an alkane. 1. Method for producing powdered lauroyl peroxide having a particle size according to the d90 value of from 50 μm to 400 μm , wherein a reaction mixture is used which comprises water , lauric acid chloride , hydrogen peroxide , an inorganic base and an alkane , and the method is carried out at a predetermined temperature in the range of from approximately 10° C. to approximately 30° C. , the lauroyl peroxide not being heated above the melting point thereof during the method.2. Method according to claim 1 , wherein production of lauroyl peroxide is carried out in the aqueous phase.3. (canceled)4. Method according to claim 1 , wherein the method is carried out at a predetermined temperature in the range of from approximately 15° C. to approximately 20° C.5. Method according to claim 1 , wherein the alkane is selected from the group consisting of straight-chain alkanes claim 1 , branched-chain alkanes claim 1 , cyclic alkanes claim 1 ,. and mixtures thereof.6. Method according to claim 1 , wherein the alkane is a C-alkane.7. Method according to claim 1 , wherein an aqueous solution of sodium hydroxide claim 1 , potassium hydroxide claim 1 , or mixtures thereof claim 1 , is used as the inorganic base.8. Method according to claim 1 , wherein a molar excess of hydrogen peroxide above a theoretically required amount in the reaction mixture is from approximately 30% to approximately 80%.9. Method according to claim 1 , wherein a mass ratio of alkane to lauric acid chloride in the reaction mixture is in the range of from approximately 1:10 to approximately 1:1.10. Method according to claim 1 , wherein the reaction mixture comprises further components selected from the group consisting of stabilisers for the hydrogen peroxide claim 1 , ...

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Номер записи: 87
23-02-2017 дата публикации

Generation of peroxyformic acid through polyhydric alcohol formate

Номер: US20170050927A1
Автор: Allison BREWSTER, Jonathan P. Fast, Junzhong Li, Richard Staub, Steven J. Lange, Taz Cheritu
Принадлежит: ECOLAB USA INC

The present invention relates generally to peroxyformic acid forming compositions, methods for forming peroxyformic acid, preferably in situ, using the peroxyformic acid forming compositions. The present invention also relates to the peroxyformic acid formed by the above compositions and methods. The present invention further relates to the uses of the peroxyformic acid, preferably in situ, for treating a surface or a target. The present invention further relates to methods for treating a biofilm using peroxyformic acid, including peroxyformic acid generated in situ.

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Номер записи: 88
22-02-2018 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20180050999A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 2. A compound according to wherein Ris methyl claim 1 , phenyl claim 1 , or p-phenylphenyl. This application is a Divisional of U.S. patent application Ser. No. 14/802,026 filed Jul. 17, 2015, which is a divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013 (now U.S. Pat. No. 9,115,109 issued Aug. 25, 2015), the contents of which are incorporated herein by reference.The present invention relates to novel processes and intermediates for the preparations of isomer free Prostaglandins and the derivatives thereof.Prostaglandin ester analogues of the following Formula I-2whereinis a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl; and Ris C-alkyl, such as, Latanoprost, Isoproyl unoprostone, Isoproyl cloprostenol, Travoprost and Tafluprost have been used in the management of open-angle glaucoma. The Prostaglandin ester analogues of Formula I-2 have been shown to have significantly greater hypotensive potency than the parent compound, presumably as a result of their more effective penetration through the cornea. They reduce intra-ocular pressure by enhancing uveoscleral outflow, and may also have some effect on trabecular meshwork as well.As shown in the following Scheme A:most of the Prostaglandin ester analogues of Formula I-2 disclosed in the prior art, such as in WO02096898, EP1886992, EP2143712, JP2012246301, U.S. Pat. No. 6,720,438, US2008033176, WO2010097672, and U.S. Pat. No. 7,582,779 were obtained by first synthesizing a Lactone VIII, whereinor is a protective group of carbonyl group; Pand Pare protective groups for the hydroxyl groups; is a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or ...

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Номер записи: 89
10-03-2022 дата публикации

PURIFICATION OF ALKYL HYDROPEROXIDE BY EXTRACTIVE DISTILLATION

Номер: US20220073456A1
Автор: HUB Serge, MAJ Philippe, Van Hemelryck Bruno
Принадлежит:

The invention relates to a method for purifying an alkyl hydroperoxide from dialkyl peroxide thereof, comprising a step of distillation in the presence of alcohol and water followed by extraction of the condensates using a hydrocarbon or a hydrocarbon blend. 116-. (canceled)17. A process for separating an alkyl hydroperoxide from a dialkyl peroxide , comprising the steps of: a) distilling a composition comprising the alkyl hydroperoxide and said dialkyl peroxide in the presence of alcohol and water , and b) extracting the dialkyl peroxide with the aid of a hydrocarbon.18. The process as claimed in claim 17 , wherein the alkyl hydroperoxide is selected from the group consisting of tert-butyl hydroperoxide claim 17 , tert-amyl hydroperoxide claim 17 , hexylene glycol hydroperoxide claim 17 , tert-octyl hydroperoxide claim 17 , tert-hexyl hydroperoxide claim 17 , 1-methylcyclopentyl hydroperoxide and 1-methylcyclohexyl hydroperoxide.19. The process as claimed in claim 17 , wherein the dialkyl peroxide is selected from the group consisting of di-tert-butyl claim 17 , di-tert-amyl peroxide claim 17 , di(3-hydroxy-1 claim 17 ,1-dimethylbutyl) peroxide claim 17 , di-tert-octyl peroxide claim 17 , di-tert-hexyl peroxide claim 17 , di(1-methylcyclopentyl) peroxide and di(1-methylcyclohexyl) peroxide.20. The process as claimed in claim 17 , wherein the content by weight of alcohol present in step a) is greater than 5 times that of said dialkyl peroxide.21. The process as claimed in claim 17 , wherein the extraction step b) is performed by contacting said hydrocarbon with the condensate obtained in step a) so as to obtain an organic phase containing said hydrocarbon and also all or some of the dialkyl peroxide and an aqueous phase containing the hydroperoxide claim 17 , the water and the alcohol.22. The process as claimed in claim 17 , wherein the hydrocarbon is selected from the group consisting of Cto Chydrocarbons.23. The process as claimed in claim 17 , wherein the aqueous ...

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Номер записи: 90
10-03-2022 дата публикации

METHOD FOR PURIFYING ALKYL HYDROPEROXIDE BY EXTRACTION WITH WATER AND SEPARATION OF THE AQUEOUS PHASE

Номер: US20220073457A1
Автор: BLUM Albert, HUB Serge, MAJ Philippe, Van Hemelryck Bruno
Принадлежит:

The present invention relates to a method for purifying a mixture containing at least one alkyl hydroperoxide, preferably tert-butyl hydroperoxide or tert-amyl hydroperoxide, and at least one corresponding dialkyl hydroperoxide, said method comprising at least one step of extraction with water and at least one separation step which is carried out within the aqueous phase, obtained following the extraction step, in order to recover an aqueous solution which is rich in alkyl hydroperoxide. The invention also relates to an aqueous composition which is rich in alkyl hydroperoxide and contains at least 0.1% by weight of dialkyl peroxide in relation to the total weight of the composition. 120-. (canceled)21. A process for the purification of a mixture containing at least one alkyl hydroperoxide and at least one alkyl peroxide , wherein it successively comprises:a) at least one stage of extraction, carried out with water, of said mixture so as to obtain a first phase rich in alkyl hydroperoxide and a second phase rich in dialkyl peroxide,b) at least one stage of concentration of the first phase obtained in stage a) so as to obtain two new phases, known as third and fourth phase,c) optionally a stage of separation by settling of the third phase so as to obtain a fifth and sixth phase,d) optionally a stage of recovery of the fifth phase obtained in stage c).22. The process as claimed in , wherein the extraction stage a) is carried out with a water content which is 5 times greater than the content by weight of the mixture as defined according to .23. The process as claimed in claim 21 , wherein the concentration stage b) is carried out starting from a process employing at least one semipermeable membrane or from a distillation process.24. The process as claimed in claim 21 , wherein the concentration stage b) is carried out in order to separate the solution containing at least 60% by weight of alkyl hydroperoxide and less than 0.1% by weight of dialkyl peroxide claim 21 , the ...

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Номер записи: 91
10-03-2022 дата публикации

METHOD FOR CONCENTRATING A WATER-SOLUBLE ORGANIC PEROXIDE

Номер: US20220073458A1
Автор: HUB Serge, MAJ Philippe
Принадлежит:

The present invention relates to a process for the concentration of a water-soluble organic peroxide, preferably an alkyl hydroperoxide, by reverse osmosis as well as to a process for the separation of a water-soluble organic peroxide and of a water-insoluble compound. 118-. (canceled)19. A process for the concentration of a composition comprising at least one water-soluble organic peroxide , said process comprising a stage of bringing said composition into contact with a reverse osmosis membrane.20. The process as claimed in claim 19 , in which the stage of bringing said composition into contact with the reverse osmosis membrane is carried out at a temperature ranging from 0° C. to 60° C.21. The process as claimed in claim 19 , in which the stage of bringing into contact is carried out at a pressure of between approximately 2000 and approximately 7000 kPa.22. The process as claimed in claim 19 , for obtaining a retentate forming two immiscible phases consisting of a phase concentrated in water-soluble organic peroxide and a phase diluted in water-soluble organic peroxide.23. The process as claimed in claim 22 , in which all or part of the diluted phase is recycled with the composition comprising the water-soluble organic peroxide to be concentrated.24. A process for the separation of at least one water-soluble organic peroxide and of at least one water-insoluble compound claim 22 , comprising the following stages:a) extraction, with an aqueous composition, of said water-soluble organic peroxide from a composition comprising said at least one water-soluble organic peroxide and said at least one water-insoluble compound;b) separation of the aqueous phase enriched in water-soluble organic peroxide and of the organic phase which are obtained in stage a);{'claim-ref': {'@idref': 'CLM-00019', 'claim 19'}, 'c) concentration of said aqueous phase enriched in water-soluble organic peroxide according to the concentration process as defined in .'}25. The process as claimed in ...

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Номер записи: 92
15-05-2014 дата публикации

NOVEL PROCESSES FOR THE PREPARATION OF PROSTAGLANDIN AMIDES

Номер: US20140135503A1
Автор: Bischof Zoltán, Bódis Ádám, HAVASI Gábor, HORTOBÁGYI Irén, KARDOS Zsuzsanna, Kiss Tibor, LÁSZLÓFI István
Принадлежит: CHINOIN ZRT.

The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, Rand Rindependently represent hydrogen atom or a straight or branched Calkyl- or aralkyl- group, optionally substituted with —ONOgroup, or an aralkyl- or aryl- group, which contains heteroatom, Rrepresents a straight or branched, saturated or unsaturated Chydrocarbon group, or a Calkylcycloalkyl- or cycloalkyl- group, or an optionally with alkyl group or halogen atom substituted phenyl-, Calkylaryl- or hetaryl- group, Y represents (CH), group or 0 atom or S atom, and where n=0-3. 4. Process according to method i.) of claim 1 , characterized in that the compound suitable to introduce the group R claim 1 , is 1 claim 1 ,1′-carbonyldiimidazole or 1 claim 1 ,1′-thiocarbonyldiimidazole.5. Process according to method ii.) of claim 1 , characterized in that for the introduction of group R claim 1 , N-hydroxysuccinimide claim 1 , N-hydroxyphthalimide claim 1 , N-hydroxy-5-norben-endo-2 claim 1 ,3-dicarboxamide claim 1 , 1-hydroxybenzotriazole claim 1 , (benzotriazol-1-yloxy)tris(dimethylamino)-phosphonium hexafluorophosphate claim 1 , N claim 1 ,N′-disuccinimidyl carbonate or N claim 1 ,N′-disuccinimidyl oxalate are used claim 1 , in a given case in the presence of an activating agent.6. Process according to claim 5 , characterized in that the applied activating agent is N claim 5 ,N′-diisopropylcarbodiimide claim 5 , N claim 5 ,N′-dicyclohexylcarbodiimide or 2-chloro-1 claim 5 ,3-dimethylimidazolinium chloride.7. Process according to claim 1 , characterized in that the reaction is carried out in an ether-type claim 1 , or aromatic claim 1 , or polar-aprotic solvent claim 1 , or in the mixture of them.8. ...

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Номер записи: 93
02-03-2017 дата публикации

Phenol Composition

Номер: US20170057895A1
Автор: Becker Christopher L., Davis Jason D., Poucher Ashley J., Watts Jonathan J., Weber Jörg F.W.
Принадлежит:

Disclosed is (i) a process of making phenol and/or cyclohexanone from cyclohexylbenzene including a step of removing methylcyclopentylbenzene from (a) the cyclohexylbenzene feed supplied to the oxidation step and/or (b) the crude phenol product (ii) a phenol composition and (iii) a cyclohexylbenzene composition that can be made using the process. 1. A phenol composition comprising phenol at a concentration of C(Phenol) wt % and methylcyclopentylbenzene at a concentration of C(MCPB) ppm , where the percentage and ppm are based on the total weight of the phenol composition , C(Phenol)≧95.00 , and 0.001≦C(MCPB)≦50.2. The phenol composition of claim 1 , wherein the methylcyclopentylbenzene comprises (a) cis-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2cis) ppm and (b) trans-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2trans) ppm claim 1 , and at least one of the following conditions (i) claim 1 , (ii) claim 1 , and (iii) is met:(i) 0.001≦C(MCPB2cis)≦45;(ii) 0.001≦C(MCPB2trans)≦45; and(iii) 0.001≦C(MCPB2cis)+C(MCPB2trans)≦45.3. The phenol composition of claim 1 , wherein 0.010≦C(MCPB)≦20.4. The phenol composition of claim 1 , wherein the methylcyclopentylbenzene comprises (a) cis-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2cis) ppm and (b) trans-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2trans) ppm claim 1 , and C(MCPB2trans)>C(MCPB2cis).5. The phenol composition of claim 1 , wherein 1.5≦C(MCPB2trans)/C(MCPB2cis)≦1000.6. The phenol composition of claim 1 , wherein the methylcyclopentylbenzene comprises (a) cis-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2cis) ppm; (b) trans-1-methyl-2-phenylcyclopentane at a concentration of C(MCPB2trans) ppm; (c) cis-1-methyl-3-phenylcyclopentane at a concentration of C(MCPB3cis) ppm; and (d) trans-1-methyl-3-phenylcyclopentane at a concentration of C(MCPB3trans) ppm claim 1 , and at least one of the following conditions (i) claim 1 , (ii) claim 1 , and (iii) is ...

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Номер записи: 94
20-02-2020 дата публикации

PREPARATION OF COMPOUNDS FROM LEVULINIC ACID

Номер: US20200055816A1
Автор: Dutta Saikat, Mascal Mark, Wu Linglin
Принадлежит:

The present invention provides a method of making carboxylic acids from levulinic acid, such as succinic acid and 3-hydroxypropanoic acid, by reacting levulinic acid with an oxidant such as hydrogen peroxide under acidic or basic conditions. 1. A method of preparing a carboxylic acid , wherein the carboxylic acid is 3-hydroxypropanoic acid , comprising:forming a reaction mixture comprising levulinic acid, an oxidant, and a base, under conditions suitable to prepare the carboxylic acid.2. (canceled)3. The method of claim 1 , wherein the oxidant is hydrogen peroxide.4. The method of claim 3 , wherein the reaction mixture is substantially free of an oxidizing metal catalyst.512.-. (canceled)13. The method of claim 1 , wherein the base is selected from the group consisting of sodium hydroxide and potassium hydroxide.14. The method of claim 1 , wherein the reaction mixture is at a temperature between about 75° C. and about 200° C.15. The method of claim 1 , wherein the method comprises:forming the reaction mixture comprising levulinic acid, hydrogen peroxide, and potassium hydroxide, wherein the reaction mixture is at a temperature between about 100° C. and about 150° C., thereby forming the 3-hydroxypropanoic acid.16. The method of claim 1 , wherein the reaction mixture is at a temperature between about 0° C. and about 50° C. such that the product of the forming step is 3-(hydroperoxy)propanoic acid claim 1 , and the method further comprises:forming a second reaction mixture comprising the 3-(hydroperoxy)propanoic acid and a hydrogenation agent, under conditions suitable to form the 3-hydroxypropanoic acid.17. The method of claim 16 , wherein the hydrogenation agent is palladium on carbon.18. The method of claim 16 , wherein the method comprises:forming the reaction mixture comprising levulinic acid, hydrogen peroxide, and potassium hydroxide, wherein the reaction mixture is at about room temperature, thereby preparing 3-(hydroperoxy)propanoic acid; andforming the ...

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Номер записи: 95
05-03-2015 дата публикации

Process for Producing Phenol and Cyclohexanone

Номер: US20150065753A1
Автор: Becker Christopher L., Benitez Francisco M., Chavez Krystle J., Heidman, JR. John L., Kuechler Keith H.
Принадлежит:

In a process for separating a mixture comprising cyclohexanone and phenol, at least a portion of the mixture is distilled in the presence of a solvent including at least two alcoholic hydroxyl groups attached to non-adjacent saturated carbon atoms and at least one hemiketal defined by the formula (I) or the formula (II): 2. The process of claim 1 , wherein the total concentration of the hemiketal and the enol-ether is at least 0.10%.3. The process of claim 1 , wherein said solvent is diethylene glycol and Ris an ethylene group.6. The process of claim 1 , wherein said solvent is 1 claim 1 ,4-butanediol and Ris 1 claim 1 ,4-butylene.9. The process of claim 1 , wherein at least a portion of said hemiketal and/or enol-ether is formed from the reaction of cyclohexanone and said solvent during said distilling step (a).10. The process of claim 1 , wherein said distilling step (a) is conducted in the presence of water.11. The process of claim 10 , wherein water is present in an amount in the range from 0.1 wt % to 20 wt % claim 10 , based on the total weight of feed to the distilling step (a).12. The process of claim 10 , wherein water is added to the distilling step (a) in an amount sufficient to suppress the formation of said hemiketal and/or enol-ether by an amount of at least 50% of that produced by a distillation under the same condition except in the absence of added water.13. The process of claim 1 , wherein said distilling step (a) separates the mixture into a first stream rich in cyclohexanone and a second stream rich in phenol claim 1 , the solvent claim 1 , and said hemiketal and/or enol-ether.14. The process of claim 13 , further comprising (b) distilling said second stream to separate at least part of the phenol therefrom and produce a recovered solvent.15. The process of claim 14 , wherein the recovered solvent further comprises said hemiketal and/or enol-ether and provides at least a portion of said hemiketal and/or enol-ether present in said distilling step ...

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Номер записи: 96
28-02-2019 дата публикации

1-DEOXY ANALOGS OF VITAMIN D-RELATED COMPOUNDS

Номер: US20190060456A1
Автор: Hess Lindsey C., Kalinda Alvin S., Petkovich P. Martin, Posner Gary H., Saha Uttam, Slack Rachel D.
Принадлежит:

This present disclosure is directed to novel prodrugs of activated vitamin Dcompounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases. 2. The compound of claim 1 , wherein{'sup': '1', 'Ris OH or halo;'}{'sup': 2', '3, 'sub': '2', 'Rand Rare either both H or together form ═CH;'}{'sup': '4', 'sub': '1-4', 'Ris Calkyl;'}{'sup': 5', '6', '5, 'sub': '1-2', 'img': {'@id': 'CUSTOM-CHARACTER-00041', '@he': '2.46mm', '@wi': '3.56mm', '@file': 'US20190060456A1-20190228-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'Rand Rare each independently H, halo, or Calkyl, with the proviso that when between carbon-23 and carbon-24 is a double bond, then Ris absent;'}{'sup': '7', 'sub': 1-4', '2-5', '1-4', '2-4', '1-4', '2-4', '1-4', '2-4', '1-4', '2-4', '1-4', '2-4', '3', '3, 'Ris selected from the group consisting of H, Calkyl, Calkenyl, aryl and heteroaryl, with Calkyl and Calkenyl being unsubstituted or substituted with 1 to 4 groups independently selected from Calkyl, Calkenyl, OCalkyl, OCalkenyl, OH, and halo, and with aryl and heteroaryl being unsubstituted or substituted with 1 to 5 groups independently selected from Calkyl, Calkenyl, OCalkyl, OCalkenyl, OH, CF, OCF, and halo; and'}{'sup': '8', 'sub': 1-4', '2-4', '3', '6', '5', '6', '1-4', '2-4', '1-4', '2-4', '1-4', '2-4', '3', '6', '5', '6', '1-4', '2-4', '1-4', '2-4', '3', '3, 'Ris selected from the group consisting of Calkyl, Calkenyl, cyclo(C-C)alkyl, cyclo(C-C)alkenyl, aryl, heteroaryl, with Calkyl and Calkenyl being ...

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Номер записи: 97
27-02-2020 дата публикации

Hydrogen peroxide and peracid stabilization with molecules based on a pyridine carboxylic acid

Номер: US20200060265A1
Автор: Chris Nagel, Junzhong Li, Keith G. LaScotte
Принадлежит: ECOLAB USA INC

Stabilized peroxycarboxylic acid compositions are provided. The stable peroxycarboxylic acid compositions are particularly suitable for use in sanitizing equipment and surfaces to reduce yeasts, spores and bacteria, including those having contact with food, food products and/or components thereof, which require or benefit from infection control suitable for direct contact with such food sources are provided.

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Номер записи: 98
28-02-2019 дата публикации

Process for the preparation of optically active beraprost

Номер: US20190062295A1
Автор: Iren Hortobagyi, Istvan Laszlofi, Jozsef Molnar, Laszlo Takacs, Tamas Ban, Zsuzsanna Kardos
Принадлежит: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Zrt

The invention provides a new process for the preparation of optically active Beraprost of formula (I) starting from racemic Beraprost alkyl ester through hydrolysis, enantiomer esterification, preparation of diacyl-Beraprost ester diastereomers and their separation and hydrolysis.

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Номер записи: 99
27-02-2020 дата публикации

Substituted 4-phenyl pyridine compounds as non-systemic tgr5 agonists

Номер: US20200062795A1
Автор: Dean Dragoli, Jason G. Lewis, Jeffrey W. Jacobs, Jeremy Caldwell, Matthew SIEGEL, Michael Robert Leadbetter, Noah Bell, Patricia FINN, Rakesh Jain, Tao Chen
Принадлежит: Ardelyx Inc

where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.

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Номер записи: 100