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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 10162. Отображено 100.
20-09-2001 дата публикации

СИСТЕМА ДЛЯ ВЫДЕЛЕНИЯ ЦИТРАТА КАЛЬЦИЯ ИЗ ЦИТРАТСОДЕРЖАЩЕГО РАСТВОРА

Номер: RU0000019653U1
Автор: Аниськов В.Н., Когос А.Я., Козлов В.П., Мирошников В.П., Наумов Е.Г., Немцев Д.В.
Принадлежит: Закрытое акционерное общество "Белгородский завод лимонной кислоты" ("Цитробел")

Система для выделения цитрата кальция из жидких цитратсодержащих отходов, включающая нейтрализатор, коммуникационную линию для подвода, содержащую, по крайней мере, один трубопровод и трубопровод для подачи гидрооксида кальция, отличающаяся тем, что она дополнительно включает трубопровод для подачи соляной кислоты, причем этот трубопровод и трубопровод для подачи гидрооксида кальция оборудован клапанами с исполнительными механизмами, а нейтрализатор дополнительно снабжен датчиком уровня заполнения нейтрализатора с релейной схемой и реактором в виде изогнутого полукольцом трубопровода, внешний диаметр кольца которого близок к внутреннему диаметру нейтрализатора, размещенным внутри последнего в горизонтальной плоскости над уровнем заполнения нейтрализатора, а также датчиком потока с релейной схемой для блокирования с помощью клапана с исполнительным механизмом подачи соляной кислоты, при этом датчик потока установлен в нейтрализаторе против открытого конца полукольца реактора, второй конец которого соединен с клапаном трубопровода для подачи гидрооксида кальция, а к последнему перед входом в нейтрализатор подсоединен трубопровод с клапаном для подачи соляной кислоты. (19) RU (11) 19 653 (13) U1 (51) МПК C07C 59/265 (2000.01) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К СВИДЕТЕЛЬСТВУ (21), (22) Заявка: 2001106031/20 , 11.03.2001 (24) Дата начала отсчета срока действия патента: 11.03.2001 (46) Опубликовано: 20.09.2001 (73) Патентообладатель(и): Закрытое акционерное общество "Белгородский завод лимонной кислоты" ("Цитробел") U 1 1 9 6 5 3 R U (57) Формула полезной модели Система для выделения цитрата кальция из жидких цитратсодержащих отходов, включающая нейтрализатор, коммуникационную линию для подвода, содержащую, по крайней мере, один трубопровод и трубопровод для подачи гидрооксида кальция, отличающаяся тем, что она дополнительно включает трубопровод для подачи соляной кислоты, причем этот трубопровод и трубопровод для подачи ...

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Номер записи: 1
08-03-2012 дата публикации

Neutralization Process

Номер: US20120059138A1
Автор: Filip Mees, Karl J. Possemiers, Matthias Weismantel, Michael De Marco, Ronny De Kaey
Принадлежит: BASF SE

The invention relates to a neutralization process in which at least one ethylenically unsaturated carboxylic acid is preneutralized at least partly with a base, wherein the preneutralized solution is divided into at least two part-solutions and at least one part-solution is aftertreated so as to form part-solutions with different degree of neutralization and/or solids content, and also to an apparatus for carrying out the process.

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Номер записи: 2
03-05-2012 дата публикации

Process for the preparation of phytosteryl ferulate

Номер: US20120108833A1
Автор: Bethala Lakshmi Anu Prabhavathi Devi, Bhongiri Yadagiri, Kuncha Madhusudhana, Prakash Vamanrao Diwan, Rachapudi Badari Narayana Prasad, Sanjit Kanjilal, SISTLA Ramakrishna
Принадлежит: Individual

A method is provided for controlling the operating temperature of a catalytic reactor using a closed-loop system that provides for varying the reactor input and other operating parameters in order to maintain the operating temperature of the reactor at or near the initial setpoint temperature for operation of the reactor. In one example, maximum and minimum operating temperatures with a catalytic partial oxidation reactor are controlled, as well as maintaining control over the corresponding minimum required ratio of oxygen atoms to carbon atoms, such that the operating temperature within the reactor is maintained below the material limits but above threshold temperatures for coking.

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Номер записи: 3
21-06-2012 дата публикации

Process for the manufacture of sevoflurane

Номер: US20120157708A1
Автор: Max Josef Braun
Принадлежит: SOLVAY FLUOR GMBH

A process for the manufacture of Sevoflurane CF 3 —CH(OCH 2 F)—CF 3 which comprises (a) manufacturing a substituted malonic acid derivative of formula (I): R 1 OOC—CH(OCH 2 X)—COOR 2 or of formula (II): R 3 HNOC—CH(OCH 2 X)—CONHR 4 , wherein X is OH or a leaving group which can be substituted by nucleophilic substitution and wherein R 1 , R 2 R 3 , R 4 , equal to or different from each other, are independently selected from the group consisting of H, an alkyl group having from 1 to 10 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group, and an aryl group; and (b) further reacting said malonic acid derivative as intermediate for the manufacture of Sevoflurane CF 3 —CH(OCH 2 F)—CF 3 .

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Номер записи: 4
14-03-2013 дата публикации

Methods of treating or preventing cholesterol related disorders

Номер: US20130064825A1
Автор: Christi L. Clogston, Clapton S. DIAS, John P. GIBBS, Joyce Chi Yee Chan, Robert Andrew Donald Scott, Scott Wasserman, Timothy David Osslund
Принадлежит: AMGEN INC

The present invention relates to methods of treating or preventing cholesterol related disorders, such as hypercholesterolemia, hyperlipidemia or dyslipidemia, using antibodies against proprotein convertase subtilisin/kexin type 9 (PCSK9). Formulations and methods of producing said formulations are also described.

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Номер записи: 5
21-03-2013 дата публикации

CRYSTALLINE FORMS OF A PURINE DERIVATIVE

Номер: US20130072504A1
Автор: Atherton Jonathan Charles Christian, Fernades Philippe, Northen Julian Scott, Skead Benjamin Mark, Worrall Christopher Peter
Принадлежит: CYCLACEL LIMITED

The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. 2. The crystalline form of which is a tartrate salt.3. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 6.67±0.2 claim 2 , 8.237±0.2 claim 2 , 9.777±0.2 claim 2 , 11.96±0.2 claim 2 , 12.38±0.2 claim 2 , 13.06±0.2 claim 2 , 13.38±0.2 claim 2 , 13.94±0.2 claim 2 , 14.90±0.2 claim 2 , 15.40±0.2 claim 2 , 15.95±0.2 claim 2 , 16.27±0.2 claim 2 , 16.54±0.2 claim 2 , 17.36±0.2 claim 2 , 17.57±0.2 claim 2 , 17.86±0.2 claim 2 , 19.64±0.2 claim 2 , 19.86±0.2 claim 2 , 20.12±0.2 claim 2 , 20.73±0.2 claim 2 , 21.14±0.2 claim 2 , 21.58±0.2 claim 2 , 22.57±0.2 claim 2 , 22.95±0.2 claim 2 , 23.29±0.2 claim 2 , 23.57±0.2 claim 2 , 24.07±0.2 claim 2 , 24.63±0.2 claim 2 , 25.30±0.2 claim 2 , 26.38±0.2 claim 2 , 27.09±0.2 claim 2 , 27.67±0.2 claim 2 , 27.97±0.2 claim 2 , 28.91±0.2 claim 2 , 29.28±0.2 claim 2 , 30.08±0.2 claim 2 , 30.41±0.2 claim 2 , 31.90±0.2 and 34.49±0.2 (Form E).45-. (canceled)6. The crystalline form of which is characterized by a differential scanning calorimetry trace recorded at a heating rate of 20° C. per minute which shows a maximum endothermic peak at a temperature between about 176° C. and about 185° C. claim 2 , or a differential scanning calorimetry trace substantially in accordance with that shown in .7. (canceled)8. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 3.82±0.2 claim 2 , 7.57±0.2 claim 2 , 8.12±0.2 claim 2 , 10.53±0.2 claim 2 , 11.39±0.2 claim 2 , 12.00±0.2 ...

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Номер записи: 6
28-03-2013 дата публикации

Hydroxy Acid Ester Compound of Substituted Phenol, Preparation Method and Medical Use Thereof

Номер: US20130079405A1
Автор: LIU Jin, YANG Jun, Zhang Wensheng
Принадлежит: West China Hospital Sichuan University

Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y═Cstraight carbon chain. The compound can release 2,6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia. 2. The compound of claim 1 , wherein said straight carbon chain Y is a saturated carbon chain.3. The compound of claim 2 , wherein said straight carbon chain Y is —CH—CH— or —CH—CH—CH—.4. The compound of claim 1 , wherein at least one hydrogen atom of the straight carbon chain Y is substituted with a member of the group consisting of methyl claim 1 , ethyl claim 1 , cyclopropyl claim 1 , hydroxy claim 1 , sulfydryl claim 1 , amino or substituted amino group.6. The preparation method of claim 5 , wherein said deacidifying agent is pyridine or a tertiary amine compound including triethylamine.7. The preparation method of claim 5 , wherein said preparation method is performed in at least one organic solvent selected from the group consisting of methylene dichloride claim 5 , chloroform claim 5 , carbon tetrachloride claim 5 , chlorobenzene claim 5 , benzene claim 5 , methylbenzene claim 5 , petroleum ether claim 5 , cyclohexane claim 5 , n-hexane claim 5 , acetonitrile claim 5 , acetone claim 5 , DMF claim 5 , DMSO claim 5 , tetrahydrofuran claim 5 , diethyl ether claim 5 , triethylamine or pyridine.8. The preparation method of claim 7 , comprising the steps of:1′: dissolving 2,6-diisopropylphenol (II) in triethylamine, adding with dianhydride compound (III) and a catalytic amount of 4-dimethylaminopyridine; after completion of the reaction under stirring, removing triethylamine under reduced pressure, adding ...

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Номер записи: 7
11-04-2013 дата публикации

FILLER COMPRISING BEADS

Номер: US20130089585A1
Автор: Boderke Peter, Hauptmeier Bernhard, Kiehm Kevin
Принадлежит: MERZ PHARMA GmbH & CO., KGaA

The present invention pertains to a filler comprising beads wherein said beads comprise a polyanionic biopolymer and divalent cations and wherein said polyanionic biopolymer is not alginate. Further, the present invention pertains to a process for manufacturing the claimed filler, and to an injection device comprising the filler. 115-. (canceled)16. A filler comprising beads , wherein the beads comprise a polyanionic biopolymer and at least one divalent cation , and wherein the polyanionic biopolymer is not alginate.17. The filler of claim 16 , wherein the at least one divalent cation is selected from the group consisting of barium claim 16 , zinc claim 16 , copper claim 16 , calcium and magnesium claim 16 , and mixtures thereof.18. The filler of claim 16 , wherein the polyanionic biopolymer is pectin claim 16 , wherein:a. the pectin has a degree of amidation of from about 0% to about 30%;b. the pectin has a degree of esterification of from about 0% to bout 60%;c. the pectin has a molecular weight distribution from about 50 to about 5000 kDa; and/ord. the at least one divalent cation is selected from the group consisting of calcium, barium, zinc and copper, and mixtures thereof.19. The filler of claim 16 , wherein the polyanionic biopolymer is gellan claim 16 , wherein:a. the gellan exhibits a molecular weight distribution from about 50 to about 5000 kDa: and/orb. the at least one divalent cation is selected from the group consisting of copper, calcium, zinc, and mixtures thereof.20. The filler of claim 16 , wherein the beads exhibit a mass median diameter of less than or equal to 1500 μm as determined by laser diffraction analysis.21. The filler of claim 16 , wherein the filler further comprises one or more active pharmaceutical ingredients selected from the group consisting of anesthetics claim 16 , analgesics claim 16 , anti-microbials claim 16 , anti-inflammatory drugs claim 16 , growth factors claim 16 , hormones claim 16 , cosmeceuticals claim 16 , vitamins ...

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Номер записи: 8
11-04-2013 дата публикации

SOLID STATE FORMS OF TAPENTADOL SALTS

Номер: US20130090314A1
Автор: Ahirao Vikas Daulatrao, BONDGE Sandipan Prabhurao, Khunt Mayur Devjibhai, Pradhan Nitin Sharadchandra
Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt. 1. Solid state form of a salt of 3-[(1R ,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol (tapentadol salt) , wherein the salt of tapentadol is an L-(−)-camphorsulfonate salt , a dibenzoyl-(D)-tartrate salt , a malate salt , a maleate salt , or a salicylate salt.2. The solid state form of tapentadol salt of claim 1 , which is in a crystalline form or in an amorphous form claim 1 , and wherein the solid state form is anhydrous and/or solvent-free form claim 1 , or a hydrate and/or a solvate form.3. The solid state form of tapentadol salt of claim 1 , having the following characteristics claim 1 , wherein: [{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 3.93, 5.66, 14.94, 16.16 and 21.52±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional peaks at about 8.01, 11.36, 14.10, 15.27, 15.91, 16.72, 19.06, 19.88, 21.85, 22.56, 23.92 and 27.12±0.2 degrees 2-theta; and', {'figref': {'@idref': 'DRAWINGS', 'FIG. 2'}, 'iv) a differential scanning calorimetric (DSC) thermogram substantially in accordance with ;'}], 'a) the solid state form of tapentadol L-(−)-camphorsulfonate salt is characterized by one or more of the following properties [{'figref': {'@idref': 'DRAWINGS', 'FIG. 5'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 8.52, 9.39, 11.81, 12.28, 13.46, 14.06, 17.77, 17.97, 18.33, 18.79, 19.58 and 20.05±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional ...

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Номер записи: 9
18-04-2013 дата публикации

Vesicle-Containing Composition And Production Method Thereof

Номер: US20130093110A1
Автор: Araki Hidefumi, Ishino Hirokazu, Nagare Yuko, Nakama Yasunari, WATANABE Kei
Принадлежит: SHISEIDO COMPANY LTD.

To provide a vesicle-containing composition wherein a perfume component is stably incorporated in the vesicle bilayer membrane composed of a silicone surfactant and to provide a simple production method of the vesicle-containing composition wherein a perfume component is stably incorporated. A vesicle-containing composition comprising; (A) a perfume, (B) a silicone oil, (C) a silicone surfactant, (D) one or more selected from the group consisting of ethanol, propylene glycol, dipropylene glycol, and 1,3-butylene glycol, and (E) water; wherein the (C) silicone surfactant forms vesicles, and the (A) perfume and the (B) silicone oil are present in the vesicle bilayer membrane. 1. A method of producing a vesicle-containing composition comprising:(i) an oil component mixing step, wherein the oil component contains (A) a perfume, and (B) a silicone oil that are mixed, in which the mass ratio of the (A) perfume:the (B) silicone oil is in the range of 5:95 to 70:30, and(ii) a vesicle formation step, wherein the oil component mixture obtained in the step (i) is mixed with (C) a silicone surfactant and (D) one or more selected from the group consisting of ethanol, propylene glycol, dipropylene glycol, and 1,3-butylene glycol, and further mixed with the aqueous formulation containing (E) water to form vesicles of the (C) silicone surfactant.2. The method of claim 1 , further comprising step (iii) adding and mixing (F) a water-soluble low-molecular-weight surfactant following the step (ii).3. The method of claim 1 , further comprising mixing with (G) a polar oil having an IOB of 0.1 to 0.4 in the step (i).4. The method of claim 1 , wherein the (B) silicone oil is octamethylcyclotetrasiloxane and/or decamethylcyclopentasiloxane.6. The method of claim 2 , wherein the (F) water-soluble low-molecular-weight surfactant is a surfactant having a molecular weight of less than 2000.7. The method of claim 1 , wherein the (D) component is one or more selected from the group consisting of ...

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Номер записи: 10
18-04-2013 дата публикации

POLYMORPHIC FORMS OF LUBIPROSTONE

Номер: US20130096325A1
Автор: Ceccarelli Alfredo Paul, Kothakonda Kiran Kumar
Принадлежит: APOTEX PHARMACHEM INC.

There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone. 1. APO-II polymorphic form of Lubiprostone.2. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 8.98.3. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 13.53.4. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 18.06.5. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 20.57.6. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 20.80.7. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 22.74.8. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 13.53.9. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 18.06.10. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 20.57.11. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 20.80.12. The crystalline form of Lubiprostone of 5 wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 22.74.13. The crystalline form of Lubiprostone of wherein ...

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Номер записи: 11
25-04-2013 дата публикации

HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY

Номер: US20130101630A1
Автор: Kumar Arvapally Seshu, Pradhan Nitin Sharadchandra, Sharma Krishnadatt, Trivedi Nikhil
Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein is an impurity of varenicline, methylvarenicline, 6-methyl-5,8,14-triazatetracyclo[10.3.1.0,0]hexadeca-2(11),3,5,7,9-pentaene, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity. 1. Varenicline or a pharmaceutically acceptable salt thereof comprising a 6-methyl-5 ,8 ,14-triazatetracyclo[10.3.1.0 ,0]hexadeca-2(11) ,3 ,5 ,7 ,9-pentaene impurity (methylvarenicline impurity) in an amount of less than 0.15 area-% as measured by HPLC.2. Varenicline of claim 1 , comprising the methylvarenicline impurity in an amount of about 0.01 area-% to about 0.1 area-%; wherein the varenicline or a pharmaceutically acceptable salt thereof has a purity of about 99.5% to about 99.99% as measured by HPLC; and wherein the pharmaceutically acceptable salt of varenicline is a hydrochloride salt claim 1 , a hydrobromide salt claim 1 , a sulphate salt claim 1 , a phosphate salt claim 1 , a tartrate salt claim 1 , a fumarate salt claim 1 , a maleate salt claim 1 , an oxalate salt claim 1 , an acetate salt claim 1 , a propionate salt claim 1 , a succinate salt claim 1 , a mandelate salt claim 1 , a mesylate salt claim 1 , a besylate salt claim 1 , or a tosylate salt.3. Varenicline of claim 2 , comprising the methylvarenicline impurity in an amount of about 0.01 area-% to about 0.05 area-%; and wherein the pharmaceutically acceptable salt of varenicline is a tartrate salt.4. Varenicline of claim 1 , having a non-detectable amount of the methylvarenicline impurity as measured by HPLC.6. The process of claim 5 , wherein the reaction in step-(a) is carried out in the presence of a solvent selected from the group consisting of water ...

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Номер записи: 12
25-04-2013 дата публикации

DRIED FORMULATIONS OF NANOPARTICLE-COATED CAPSULES

Номер: US20130101651A1
Автор: PRESTIDGE Clive Allan, Simovic Spomenka
Принадлежит: University of South Australia

A method of producing a dried formulation for an active substance such as a drug compound is described. The method involves dispersing a discontinuous phase (e.g. an oil-based or lipidic medium) comprising the active substance into a continuous phase (e.g. water) so as to form a two-phase liquid system comprising droplets of said discontinuous phase, allowing nanoparticles to congregate at the phase interface at the surface of the droplets such that at least one layer of nanoparticles coat the droplets and thereby provide sufficient structural integrity to the droplets to enable the subsequent removal of the continuous phase, and thereafter removing the continuous phase from the nanoparticle-coated droplets to produce a dried formulation. 1. A method of producing a dried formulation for an active substance , said method comprising the steps of:(i) dispersing a discontinuous phase comprising an active substance into a continuous phase so as to form a two-phase liquid system comprising droplets of said discontinuous phase, each of said droplets having, at its surface, a phase interface;(ii) allowing nanoparticles provided to said two-phase liquid system to congregate at the phase interface to coat said surface of the droplets in at least one layer of said nanoparticles, wherein said at least one layer of nanoparticles provides sufficient structural integrity to the droplets to enable the subsequent removal of the continuous phase; and(iii) removing the continuous phase from the nanoparticle-coated droplets to produce a dried formulation.2. A method of producing a dried formulation for an active substance , said method comprising the steps of:(i) dispersing a discontinuous phase comprising an active substance into a continuous phase so as to form a two-phase liquid system comprising droplets of said discontinuous phase, each of said droplets having, at its surface, a phase interface; and(ii) removing the continuous phase to produce a dried formulation, during which ...

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Номер записи: 13
02-05-2013 дата публикации

SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: US20130109710A1
Автор: Aoyagi Kouichi, Katoh Susumu, Manabe Tomoyuki, Sasaki Shin-Ya, Shimada Takashi, Tsutsumi Kazuhiro, Ueno Hiroshi
Принадлежит: JAPAN TOBACCO INC.

The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof 3. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein the number of the double bond in ring A of the spiro-ring AB is 0 or 1.4. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein the number of the double bond in ring B of the spiro-ring AB is 0 or 1.5. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 , wherein n3 is 1 or 2.6. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed claim 1 , wherein the spiro-ring AB may be substituted by 1 to 3 same or different substituent(s).7. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 ,{'sup': '1', 'wherein Ris'}(1) a hydrogen atom,{'sub': 1', '6, '(2) a C-Calkyl group,'}{'sub': 2', '6, '(3) a C-Calkenyl group,'}{'sub': 2', '6, '(4) a C-Calkynyl group,'}{'sub': 1', '6, '(5) a C-Calkoxy group,'}{'sub': 1', '6', '1', '6, '(6) a C-Calkoxy(C-C)alkyl group,'}{'sup': 11', '12', '11', '12, 'sub': 1', '6, '(7) —CONRRin which Rand Rare the same or different and each represents a hydrogen atom or a C-Calkyl group, or'}{'sub': 1', '6, '(8) a five-membered heteroaryl group which has at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, and which may be substituted by a C-Calkyl group.'}8. The spiro compound claim 1 , the pharmaceutically acceptable salt thereof or the solvate thereof as claimed in claim 1 ,{'sup': '1', 'wherein Ris'}(1) a hydrogen atom,{'sub': 2', '6, '(2) a C-Calkenyl group,'}{'sub': 2', '6, '(3) a C-Calkynyl group,'}{'sub': 1', '6, '(4) a C-Calkoxy group or'}{'sub': 1', '6, '(5) a five- ...

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Номер записи: 14
16-05-2013 дата публикации

PROCESS FOR THE SPECIFIC ISOTOPIC LABELING OF METHYL GROUPS OF VAL, LEU AND ILE

Номер: US20130122598A1
Автор: AYALA Isabel, Boisbouvier Jérôme, Gans Pierre, HAMELIN Olivier
Принадлежит:

The invention relates to a process for the specific isotopic labeling of Valine, Leucine and Isoleucine amino acids. The process of the invention uses a 2-alkyl-2-hydroxy-3-oxobutanoic acid in which the alkyl substituent in position 2 is ethyl or methyl. The invention can be used for the analysis of proteins, in particular by NMR. 2. The process of further comprising:b) overexpression of the protein by the bacteria in the medium, andc) purification of the protein.3. The process of wherein:{'sup': '1', 'Ris selected from the group consisting of{'sup': 12', '12', '13', '13', '13', '13, 'sub': 3', '3', '3', '3', '2', '2, 'CH, CD, CH, CD, CHD, and CHD,'}{'sup': '2', 'Ris selected from the group consisting of{'sup': 12', '12', '13', '13', '13', '13', '12', '12', '12', '12', '13', '12', '13', '13', '13', '13', '13', '13', '13', '13', '13', '12', '13', '12, 'sub': 3', '3', '3', '3', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'CH, CD, CH, CD, CHD, CHD, CHCD, CDCD, CHCD, CHCD, CDCD, CHDCD, CHDCD, CHDCD, and CHDCD.'}4. The process of claim 1 , wherein the acetolactate compound is selected from the group consisting of:{'sup': 13', '2, 'sub': '3', '2-hydroxy-2-(C)methyl-3-oxo-4(H)butanoic acid (formula 4),'}{'sup': 2', '13, 'sub': '3', '2-hydroxy-2-(H)methyl-3-oxo-4(C)butanoic acid (formula 5),'}{'sup': 2', '13, 'sub': '5', '2-(H)ethyl-2-hydroxy-3-oxo-4-(C)methylbutanoic acid (formula 6),'}{'sup': 13', '2, 'sub': '5', '1,2,3,4-(C)-2-(H)ethyl-2-hydroxy-3-oxobutanoic acid (formula 9),'}{'sup': 13', '13', '2, 'sub': '3', '1,2,3-(C)-2-(C)methyl-2-hydroxy-3-oxo-4-(H)butanoic acid (formula 21),'}{'sup': 13', '2, 'sub': '3', '1,2,3,4-(C)-2-(H)methyl-2-hydroxy-3-oxobutanoic acid (formula 22),'}{'sup': 13', '2', '13', '2, 'sub': 2', '2', '3, '1,2,3-(C)-2-(1′-(H),C)ethyl)-2-hydroxy-3-oxo-4-(H)butanoic acid (formula 24),'}3,4-(13C)-2-(13C)methyl-2-hydroxy-3-oxo-4-(2H3)butanoic acid (formula 36),3,4-(13C)-2-(2H3,13C)methyl-2-hydroxy-3 ...

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Номер записи: 15
16-05-2013 дата публикации

Beta-Ketocarbonylquat Compounds and Process for the Preparation thereof

Номер: US20130123535A1
Автор: Herzig Christian
Принадлежит: Wacker Chemie AG

β-ketocarbonylquats contain at least one quaternary ammonium salt group, and may be prepared by the reaction of an alkyl ketene dimer with a tertiary amine group-containing compound also containing a protic group, followed by quaternization. 18.-. (canceled)9. A β-ketocarbonylquat comprising one or more β-ketocarbonyl groups of general formula{'br': None, 'sub': '2', 'R—CH—(C═O)—CHR—(C═O)—\u2003\u2003(I)'}and one or more quaternary ammonium groups, whereinR each, independently, is an aliphatic hydrocarbon radical of 6 to 28 carbon atoms, with the proviso that the β-ketocarbonyl group of formula (I) is bonded to a radical Y, wherein{'sup': '1', 'Y is a divalent radical of the formula —O—, —NH—, —NR—, and'}{'sup': '1', 'Ris a monovalent hydrocarbon radical of 1 to 30 carbon atoms.'}10. The β-ketocarbonylquat of claim 9 , wherein the aliphatic hydrocarbon radical R contains 10-26 carbon atoms.11. The β-ketocarbonylquat of claim 9 , wherein the aliphatic hydrocarbon radical R contains 12-20 carbon atoms.12. The β-ketocarbonylquat of claim 9 , wherein Y is —NH— claim 9 , —NR— claim 9 , or a trivalent radical of the formula =N—.13. The β-ketocarbonylquat of claim 9 , wherein Rcontains 1-18 carbon atoms.14. The β-ketocarbonylquat of claim 9 , having the formula{'br': None, 'sup': 3', '4', '5', '(+)', '2', '(−), 'sub': 'a', '[RRRN—R—]Y—Z X\u2003\u2003(II)'}whereina is 1 or 2, with the proviso that when a is 1, Y is a divalent radical and when a is 2, Y is a trivalent radical,{'sup': '1', 'Y is a divalent radical of formula —O—, —NH—, —NR—, or a trivalent radical of formula =N—,'}{'sup': '(−)', 'Xis a counter-ion to the positive charge on the quaternary nitrogen atom,'} {'br': None, 'sub': '2', 'R—CH—(C═O)—CHR—(C═O)—\u2003\u2003(I)'}, 'Z is a β-ketocarbonyl group of the formula'}R each, independently is an aliphatic hydrocarbon radical of 6 to 28 carbon atoms,{'sup': '1', 'Ris a monovalent hydrocarbon radical of 1 to 30 carbon atoms,'}{'sup': '2', 'sub': 1', '18, 'Ris a ...

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Номер записи: 16
23-05-2013 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS

Номер: US20130131359A1
Автор: Chen Minzhang, Forslund Raymond E., Jung Young Chun, Tanoury Gerald J.
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 2. The process of claim 1 , wherein R claim 1 , is C-Calkyl claim 1 , R′is H and R′is —NHRwherein Ris C-Calkyl or C-Ccycloalkyl.3. The process of claim 2 , wherein Ris propyl and Ris cyclopropyl.5. The process of claim 4 , wherein the aminating reagent is an azide salt and the intermediate azido compound is reduced by hydrogenation.7. The process of claim 6 , wherein the oxidizing reagent is t-butyl hydroperoxide.8. The process of claim 6 , wherein the oxidizing reagent includes a chiral reagent.9. The process of claim 8 , wherein the oxidizing reagent is a mixture of samarium (III) isopropoxide claim 8 , triphenyl arsine oxide claim 8 , S-(−)1 claim 8 ,1′-bi-2-naphthol and 4 Å molecular sieves.10. The process of claim 6 , wherein the oxidizing reagent is urea-hydrogen peroxide in the presence of trifluoroacetic anhydride.11. The process of claim 6 , wherein R′is —OE.12. The process of claim 6 , wherein Ris —NHR.13. The process of claim 11 , further comprising hydrolyzing the compound of Formula ii to give an acid and then converting the acid to an amide compound of Formula ii wherein R′is —NHR.15. The process of claim 14 , wherein the compound of Formula 1 is (2S claim 14 ,3S)-3-amino-N-cyclopropyl-2-hydroxyhexanamide.16. The process of claim 14 , wherein the organic acid is L-tartaric acid.17. The process of claim 14 , wherein the organic acid is deoxycholic acid.18. A compound which is N-cyclopropyl-3-propyloxirane-2-carboxamide.19. A compound which is N-cyclopropyl-3-propyloxirane-2-carboxamide.20. A compound which is 3-azido-N-cyclopropyl-2-hydroxyhexanamide.21. A compound which is 3-amino-N-cyclopropyl-2-hydroxyhexanamide claim 14 , L-tartaric acid salt.22. A compound which is 3-amino-N-cyclopropyl-2-hydroxyhexanamide claim 14 , deoxycholic acid salt. This application claims the benefits of U.S. Provisional Application Ser. No. 60/782,976, ...

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Номер записи: 17
13-06-2013 дата публикации

DIMERIC DOUBLE METAL SALTS OF (-) HYDROXYCITRIC ACID, METHODS OF MAKING AND USES OF SAME

Номер: US20130150448A1
Автор: Moffett Alex, Shah Parag
Принадлежит: GLYKON TECHNOLOGIES GROUP, LLC

The present invention relates to soluble dimeric double metal salt compositions of (−)-hydroxycitric acid (“HCA”), as well as methods for making and using the same. The invention provides dimeric double metal salts of group IA and IIA of HCA (hereinafter, “DDM-HCAs”). The present invention provides methods to make DDM-HCAs of the invention which can be employed to alter the polar/ionic qualities of HCA salts and derivatives to improve solubility of HCA compositions. DDM-HCAs of the invention are soluble HCA-containing compositions useful as dietary supplements and suitable for manipulations under those conditions necessary for tabletting, encapsulation, and the production of dry powders, particularly for use as a beverage premix. Methods of use of the composition include treatment for suppression of appetite, for weight loss, for an increase in the rate of fat metabolism, for reduction in blood lipids and postprandial lipemia, and to increase the plasma level of (−)-hydroxycitric acid. 2. The composition of claim 1 , wherein (i) X is magnesium metal; (ii) Y is potassium metal; and (iii) the relative molar ratio of magnesium metal to potassium metal is from at least about 1.0:3.5 to at least about 1.0:4.5.3. The composition of claim 1 , wherein the composition is formulated in a dry delivery system.4. The composition of claim 3 , wherein the dry delivery system is selected from the group consisting of: a tablet; a dry powder; and a dry meal replacement mixture.5. The composition of claim 1 , wherein the composition is formulated in a liquid delivery system.6. The composition of claim 5 , wherein the liquid delivery system is selected from the group consisting of: a capsule; a caplet; and a beverage.7. The composition of claim 1 , wherein the composition is formulated for oral delivery in a form selected from the group consisting of: a tablet; a caplet; and a capsule.8. The composition of claim 1 , further comprising a pharmaceutically-acceptable carrier.9. The ...

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Номер записи: 18
20-06-2013 дата публикации

Method of treating non-alcoholic fatty liver disease and steatohepatitis

Номер: US20130158123A1
Автор: Kazuko Matsuda
Принадлежит: Medicinova Inc

A compound of Formula (I): or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X 1 and X 2 are as defined herein, is useful for treating non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

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Номер записи: 19
27-06-2013 дата публикации

TETRASUBSTITUTED BENZENES

Номер: US20130165486A1
Автор: Chesworth Richard, Shapiro Gideon
Принадлежит: EnVivo Pharmaceuticals, Inc.

Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described. 162.-. (canceled)64. The compound of claim 63 , wherein Rand Rare independently selected from the group consisting of (a) H claim 63 , (b) (C-C)alkyl and (c) (C-C)alkyl-(C-C)cycloalkyl provided that both Rand Rare not H claim 63 , wherein each alkyl or cycloalkyl of Rand Ris optionally independently substituted with one or more groups selected from the group consisting of halo claim 63 , hydroxy claim 63 , cyano claim 63 , CFand (C-C)alkyl claim 63 ,or{'sub': 1', '2', '1', '4', '3', '1', '4, 'Rand Rtaken together with the carbon to which they are attached form a 3-7 membered cycloalkyl or heterocycloalkyl ring which optionally bears a C-Calkyl substituent that can be optionally independently substituted with one or more groups selected from the group consisting of halo, hydroxy, oxo, cyano, CFand (C-C)alkyl,'}or{'sub': 1', '2', '20', '21', '20', '21', '3', '1', '4, 'Rand Rare taken together with the carbon to which they are attached form a 3-7 membered cycloalkyl ring substituted with Rand Rwherein Rand Rtaken together with the carbon or carbons to which they are attached form a 3-7 membered cycloalkyl ring wherein each cycloalkyl is optionally independently substituted with one or more groups selected from the group consisting of halo, hydroxy, cyano, CFand (C-C)alkyl;'}Y is —O—,{'sub': '4', 'claim-text': [{'sub': 0', '3', '3', '7, '(a) (C-C)alkyl(C-C)cycloalkyl,'}, '(b) trifluoroethyl and', '(c) trifluoropropyl;', {'sub': 6', '3', '2', '1', '4', '2', '2', '3', '6', '6', '2', '6, 'Z is a phenyl ring optionally bearing up to 3 substituents independently selected from the group consisting of halogen, R, CF, CN, NO, OH, (C-C)alkoxy, OCHCHOCH, SR, S(O)Rand S(O)R;'}], 'Ris selected from the group consisting of'}{'sub': 5', '3, 'claim-text': [{'sub': '6', 'Ris selected ...

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Номер записи: 20
04-07-2013 дата публикации

Exendins To Lower Cholesterol And Triglycerides

Номер: US20130172250A1
Автор: Kristin Taylor, Leigh Macconell, Mark Fineman
Принадлежит: Amylin Pharmaceuticals LLC, AstraZeneca Pharmaceuticals LP

Provided herein are pharmaceutical formulations containing exendins, exendin agonists, or exendin analog agonists that are administered at therapeutic plasma concentration levels over a sustained period of time to lower total cholesterol levels; to lower LDL-cholesterol levels; to lower triglyceride levels; to treat dyslipidemia; to treat and slow the progression of atherosclerosis; and to treat, prevent, and reduce the risk of heart attacks and strokes in patients. In the pharmaceutical formulations and methods of the invention, the exendin may be exendin-4, an exendin-4 agonist, or an exendin-4 analog agonist. The pharmaceutical formulations may be polymer-based pharmaceutical formulations that may be administered once weekly. An exemplary pharmaceutical formulation comprises 5% (w/w) of exenatide, about 2% (w/w) of sucrose, and about 93% (w/w) of a poly(lactide-co-glycolide) polymer, wherein the poly(lactide-co-glycolide) polymer is in the form of microshperes encapsulating the exenatide.

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Номер записи: 21
04-07-2013 дата публикации

METHOD FOR PRODUCING PYRIDAZINONE COMPOUNDS AND INTERMEDIATE THEREOF

Номер: US20130172556A1
Автор: ANRYU Mitsuharu, JACHMANN Markus, WAKAMATSU Takayuki
Принадлежит:

The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification. 2. The method according to claim 1 , wherein n is an integer of 2.3. The method according to claim 1 , wherein G is a phenyl group wherein the phenyl group may optionally have one or more substituents selected from the Group R claim 1 , provided that when it has two or more substituents claim 1 , then the substituents may be same or different.4. The method according to claim 1 , wherein the Group Ris Group R;{'sup': '4-1', 'wherein the Group Rconsists of halogen, a cyano group, a nitro group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C3-C6 cycloalkyl group, a C2-C6 alkynyl group, and a phenyl group;'}{'sup': '4-1', 'in the Group R, the C1-C6 alkyl group, the C1-C6 alkoxy group, the C3-C6 cycloalkyl group, and the C2-C6 alkynyl group may be optionally substituted with one or more halogens, provided that when they are substituted with two or more halogens, then the halogens may be same or different; and'}the phenyl group may optionally have one or more substituents selected from Group 4-1, provided that when it has two or more substituents, then the substituents may be same or different;the Group 4-1 consists of halogen and a C1-C6 alkyl group;in the Group 4-1, the C1-C6 alkyl group may be optionally substituted with one or more halogens, provided that when it is substituted with two or more halogens, then the halogens may be same or different.5. The method according to claim 4 , wherein Ris hydrogen claim 4 , a C1-C6 alkyl group or a phenyl group claim 4 ,{'sup': '2', 'Ris hydrogen, a C1-C6 alkyl group or a phenyl group wherein the C1-C6 alkyl group may be optionally substituted with one or more halogens, provided that when it is substituted with two or more halogens, then the halogens may be same or different, and the phenyl group may optionally have one or more ...

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Номер записи: 22
11-07-2013 дата публикации

METHOD OF PRODUCING INGENOL-3-ANGELATE

Номер: US20130177952A1
Автор: Grue-Sørensen Gunnar, Högberg Thomas, Horneman Anne Marie, Liang Xifu, Petersen Anders Klarskov
Принадлежит:

The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). 4. The method according to claim 1 , wherein the method comprises the step of:(f) selective esterification of the 3-hydroxy group of compound (II) to obtain ingenol-3-angelate (I).5. The method according to claim 2 , wherein Rrepresents hydrogen or an ether claim 2 , acetal claim 2 , ketal claim 2 , silylether claim 2 , ester claim 2 , carbonate claim 2 , or a sulfenate derived hydroxyl protective group claim 2 , and Rrepresents hydrogen or an ether claim 2 , acetal claim 2 , ketal claim 2 , silylether claim 2 , ester claim 2 , carbonate claim 2 , or a sulfenate derived hydroxyl protective group.6. The method according to claim 2 , wherein D represents an acetal claim 2 , ketal- claim 2 , diacetal- claim 2 , diketal- claim 2 , ortho ester claim 2 , silyl claim 2 , boronate or a carbonate derived dihydroxyl protective group.7. The method according to claim 2 , wherein Ris selected from the group consisting of hydrogen or [(3 claim 2 ,4-dimethoxybenzyl)oxy]methyl claim 2 , guaiacolmethyl claim 2 , 2-methoxyethoxymethyl claim 2 , tetrahydropyranyl claim 2 , tetrahydrofuranyl claim 2 , 1-ethoxyethyl claim 2 , 1-methyl-1-methoxyethyl claim 2 , allyl claim 2 , prenyl claim 2 , p-methoxybenzyl claim 2 , triphenylmethyl claim 2 , 2-(trimethylsilyl)ethoxymethyl claim 2 , triethylsilyl claim 2 , triisopropylsilyl claim 2 , tert-butyldimethylsilyl claim 2 , dimethylisopropylsilyl claim 2 , diethylisopropylsilyl claim 2 , tert-butyldiphenylsilyl claim 2 , triphenylsilyl claim 2 , acetyl claim 2 , chloroacetyl claim 2 , phenoxyacetyl or angeloyl.8. The method according to claim 2 , wherein Ris selected from the group consisting of hydrogen or [(3 claim 2 ,4-dimethoxybenzyl)oxy]methyl claim 2 , guaiacolmethyl claim 2 , 2-methoxyethoxymethyl claim 2 , tetrahydropyranyl claim 2 , tetrahydrofuranyl claim 2 , 1-ethoxyethyl claim 2 , 1-methyl-1-methoxyethyl claim 2 , allyl claim 2 , prenyl ...

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Номер записи: 23
18-07-2013 дата публикации

PREPARATION OF LUBIPROSTONE

Номер: US20130184476A1
Автор: Dahanukar Vilas Hareshwar, Eda Vishnu Vardhana Verma Reddy, Jackson Mark, Joseph Suju Chuttippari, Ramdas Sandip Khobare
Принадлежит:

Aspects of the present application relate to process for the preparation of lubiprostone. 2. The process of claim 1 , wherein the reagent in step (a) comprises one or more of sodium carbonate claim 1 , potassium carbonate claim 1 , lithium carbonate and cesium carbonate.3. The process of claim 1 , wherein the solvent comprises any one or more of methanol claim 1 , ethanol claim 1 , 1-propanol and 2-propanol.4. The process of claim 1 , wherein the reagent in step (b) comprises one or more of pyridinium-p-toluenesulfonate claim 1 , pyridinium dichromate claim 1 , carbonyldiimidazole and dicyclohexylcarbodiimide.5. The process of claim 1 , wherein the oxidizing agent in step (g) comprises pyridine-sulfur trioxide.6. The process of claim 1 , wherein the acid in step (h) comprises one or more of hydrochloric acid claim 1 , hydrobromic acid claim 1 , and sulfuric acid. This application claims priority to Indian Provisional Application 2389/CHE/2011, filed on Jul. 13, 2011 and U.S. Provisional Application No. 61/527,737, filed on filed on Aug. 26, 2011; all of which are hereby incorporated by reference in their entirety.Aspects of the present application relates to process for the preparation of lubiprostone and intermediates thereof.Lubiprostone is chemically described as (−)-7-[(2R,4aR,5R,7aR)-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[b]pyran-5-yl]heptanoic acid. It has the structure of formula (I).Lubiprostone is a locally acting chloride channel activator and is indicated for: (a) treatment of chronic idiopathic constipation in adults; and (b) treatment of irritable bowel syndrome with constipation (IBS-C) in women 18 years old; and is contained in products sold as Amitiza®.U.S. Pat. No. 5,284,858 discloses 13,14-dihydro-15-keto-16,16-difluoro-prostaglandins. U.S. Pat. No. 7,355,064 discloses a process for the preparation of 15-keto-prostaglandin E derivatives by hydrolyzing or deprotecting the intermediate of a 15-keto-prostaglandin E derivative having ...

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Номер записи: 24
18-07-2013 дата публикации

PROCESS TO PREPARE S-2-HYDROXY-3-METHOXY-3,3-DIPHENYL PROPIONIC ACID

Номер: US20130184490A1
Автор: ADIBHATLA KALI SATYA Bhujanga Rao, Balina Veera Swamy, KASA Srinivasu, Kompella Amala, Nannapaneni Venkaiah Chowdary
Принадлежит: NATCO PHARMA LIMITED

Disclosed is a process for the preparation of S-2-Hydroxy-3-methoxy-3,3-diphenylpropionic acid (I) the key intermediate for the preparation of Ambrisentan [(+)-2(S)-(4,6-Dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid]. Ambrisentan of the formula (IA) is approved under the trademark “Letairis ®” by the US Food and Drug Administration for the treatment of Pulmonary artery hypertension (PAH). 2. The process as claimed in wherein the step (a) comprises:(i) Charging Toluene into the flask(ii) Charging benzophenone and stirring for 15 minutes(iii) Charging sodium methoxide and stirring for 15 minutes(iv) Cooling reaction mass to −10° to −5° C.(v) Slowly adding methyl chloroacetate at the same temperature(vi) Maintaining reaction mass at −10° C. to −5° C. for one hour(vii) Charging water and stirring for 30 minutes(viii) Separating organic layer and washing with DM water(ix) Distilling toluene completely under vacuum(x) Taking compound of Formula (II) to next stage3. The process as claimed in wherein the step (b) comprises:(i) Charging methanol to the compound of formula (II) and stirring for 30 minutes(ii) Dissolving p-Toluene sulphonic acid monohydrate in methanol and adding slowly at 25-55° C.(iii) Bringing reaction mass to room temperature and maintaining for one hour.(iv) Cooling reaction mass to 0-5° C. and maintaining at the same temperature for 2 hours(v) Filtering and washing with methanol(vi) Dissolving wet compound in ethyl acetate and washing with 5% sodium bicarbonate solution.(vii) distilling off completely under vacuum.(viii) Bringing residue to room temperature and charging n-hexane.(ix) Maintaining under stirring at room temperature for 2 hours.(x) Filtering and washing with n-hexane to yield compound of formula (III)4. The process as claimed in wherein the step (c) comprises:(i) Charging purified water into flask(ii) Charging compound of formula (III) and stirring for 10 minutes.(iii) Charging IN sodium hydroxide solution and stirring for ...

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Номер записи: 25
25-07-2013 дата публикации

CRYSTALS OF CARBOPROST TROMETHAMINE AND THE PREPARATION METHOD AS WELL AS THE USES THEREOF

Номер: US20130190404A1
Автор: Gao Xiaoliang, Ji Xiaoming, Li Ming, Tang Zhijun
Принадлежит: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.

Disclosed is a crystal of carboprost tromethamine as represented by Formula (I). The crystal has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 6.6±0.2°, 9.9±0.2°, 18.5±0.2° and 20.1±0.2°. Furthermore, also disclosed are preparation method and the use of the crystal. 2. The crystal of carboprost tromethamine according to claim 1 , wherein said crystal further has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 19.3±0.2° claim 1 , 19.5±0.2° claim 1 , 19.9±0.2° and 21.6±0.2°.3. The crystal of carboprost tromethamine according to claim 1 , wherein said crystal further has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 13.3±0.2° claim 1 , 15.8±0.2° claim 1 , 16.7±0.2° claim 1 , 17.7±0.2° claim 1 , 18.1±0.2° claim 1 , 20.8±0.2° claim 1 , 21.1±0.2° claim 1 , 26.9±0.2° claim 1 , 27.6±0.2° claim 1 , 33.8±0.2° and 40.8±0.2°.4. The crystal of carboprost tromethamine according to claim 1 , wherein the maximum peak is at 103.97±5° C. in the differential scanning calorimetry (DSC).5. The crystal of carboprost tromethamine according to claim 1 , wherein the infrared Spectrum of said crystal is shown in .7. The method according to claim 6 , wherein said solvent is selected from the group consisting of acetonitrile claim 6 , acetone claim 6 , ethyl ether claim 6 , and a C1-4 straight or branched chain alcohol.8. The method according to claim 6 , wherein the temperature for dissolving the carboprost in step a is 0° C.-100° C.9. The method according to claim 6 , wherein the amount of said solvent in step (a) ranges from 1000:1 to 1:1 (ml solvent/g carboprost).10. The method according to claim 6 , wherein when adding the aqueous trometamol into said solution dropwise in step (b) claim 6 , the temperature is 20° C.-100° C.11. The method according to claim 6 , wherein claim 6 , the molar ratio of trometamol added in step (b) to carboprost ranges from 0.8:1 to 1.2:1.12. The method ...

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Номер записи: 26
22-08-2013 дата публикации

ZINC OXIDE PARTICLES AND COSMETIC

Номер: US20130216834A1
Автор: Hakozaki Hiroshi, Hashimoto Mitsuo
Принадлежит: Sakai Chemical Industry Co., Ltd,

An object of the present invention is to provide large-sized zinc oxide particles that show, when incorporated to a cosmetic product, excellent properties including transparency, infrared reflection, and the like without deteriorating the feel; and also a cosmetic containing the same. 1. Zinc oxide particles having an average particle diameter of 3 to 20 μm , an average friction coefficient of 3 or less , a total visible light transmittance of 85% or more , and a near-infrared reflectance of 80% or more.2. A cosmetic comprising the zinc oxide particles according to . The present invention relates to zinc oxide particles and a cosmetic.In the field of cosmetic applications, zinc oxide particles have been used mainly as a UV absorber for sun screen products. In most cases, zinc oxide particles for such applications are ultrafine particles of 100 nm or less. However, zinc oxide particles are rarely used for skin-care cosmetics such as skin lotions and milky lotions or makeup cosmetics such as foundations, lip sticks, and eye shadows.In such skin-care cosmetics and makeup cosmetics, the feel is regarded as important. It is also important that they do not give a whitish finish when applied to the skin. Therefore, particles that are excellent in terms of these functions, such as talc, sericite, platy barium sulfate, and boron nitride, have been used in skin-care cosmetics or makeup cosmetics.It is known to incorporate zinc oxide in order to impart UV absorption ability to a skin-care cosmetic or a makeup cosmetic (Patent Documents 1, 2, and 3). However, in the case where zinc oxide particles are ultrafine particles of 100 nm or less, there has been a problem in that they cause squeakiness, resulting in the deterioration of the feel. Furthermore, in the case where zinc oxide particles are 100 nm to 3 μm, in addition to the same problem as in the case of using ultrafine zinc oxide particles, there has also been a problem in that transparency is significantly impaired, ...

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Номер записи: 27
29-08-2013 дата публикации

Phenylketone Carboxylate Compounds and Pharmaceutical Uses Thereof

Номер: US20130225681A1
Автор: ABBOTT Shaun, GAGNON Lyne, Grouix Brigette, LAURIN Pierre, Penney Christopher, ZACHARIE Boulos
Принадлежит: PROMETIC BIOSCIENCES INC.

Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R═C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction. 124-. (canceled)26. The compound of claim 25 , wherein R is —C(O)—.27. The compound of claim 25 , wherein p is 3-7.28. The compound of claim 25 , wherein the salt is a base addition salt.29. The compound of claim 28 , wherein the base addition salt comprises a metal counterion selected from sodium claim 28 , potassium claim 28 , magnesium claim 28 , calcium and lithium.30. The compound of claim 29 , wherein the metal counterion is calcium.32. The compound of claim 31 , wherein the compound is Compound I claim 31 , III or X.33. A pharmaceutical composition comprising a compound according to claim 25 , and a pharmaceutically acceptable carrier.34. A method for the prevention or treatment of: (i) a blood disorder claim 25 , (ii) an inflammation-related disease claim 25 , (iii) a renal disorder or a renal disorder complication claim 25 , or (iv) a fibrosis-related organ dysfunction wherein said method comprises administering claim 25 , to a patient in need of such treatment claim 25 , a compound of .35. The method of claim 34 , wherein the blood disorder is anemia or neutropenia.36. The method of claim 34 , wherein said method stimulates erythropoiesis and/or hematopoiesis in the subject.37. The method of claim 34 , wherein the renal disorder is a nephropathy.38. The method of claim 34 , used for nephroprotection of a subject ...

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Номер записи: 28
05-09-2013 дата публикации

DERIVATIVES OF TRIS(2-HYDROXYPHENYL)METHANES, PREPARATION THEREOF AND USE THEREOF FOR MINERAL OIL PRODUCTION

Номер: US20130228332A1
Автор: HANSCH Markus, Maitro-Vogel Sophie, Raether Roman Benedikt
Принадлежит:

Novel derivatives of tris(2-hydroxyphenyl)methanes which have, as functional groups, polyalkoxy groups unmodified or modified with terminal hydrophilic groups, preparation of such compounds and use thereof, especially for mineral oil production. 124-. (canceled)26. The compound according to claim 25 , wherein Ris a —COORgroup and Ris a methyl and/or ethyl group.27. The compound according to claim 25 , wherein Ris a —COORgroup and Ris H claim 25 , an alkali metal ion or an ammonium ion.28. The compound according to claim 25 , wherein Ris a —CH—O—(—CH—CH(R)—O—)—Rgroup where at least 50 mol % of the Rradicals present are H claim 25 , and Ris a methyl or ethyl group and z is a number from 2 to 10.29. The compound according to claim 25 , wherein compounds (I) claim 25 , as well as (IVa) radicals claim 25 , further comprise —CH—CH(R)— (IVb) radicals where Ris H claim 25 , methyl and ethyl.30. The compound according to claim 29 , wherein Ris H.31. The compound according to claim 25 , wherein the Rradicals are each independently radicals of the general formula{'br': None, 'sub': 2', 'a', '2', 'b, 'sup': 7b', '8, '—(—CH—CH(R)—O—)—(—CHCH(—COOR)—O—)—H \u2003\u2003(V)'}{'sup': 7b', '8, 'claim-ref': {'@idref': 'CLM-00025', 'claim 25'}, 'where the alkylene oxide blocks are arranged in the sequence specified, Rand Rare each as defined in and a and b are each numbers from 1 to 49, where the sum of a+b is 2 to 50.'}32. The compound according to claim 31 , wherein a is 2 to 30 and b is 1 to 20 in the formula (V) claim 31 , with the proviso that a>b.33. The compound according to claim 31 , wherein Ris H claim 31 , an alkali metal ion or an ammonium ion.34. The compound according to claim 25 , wherein X is an acidic group selected from the group consisting of carboxyl groups —COOM claim 25 , sulfo groups —SOM claim 25 , sulfate groups —OSOM claim 25 , phosphonic acid groups —POMand phosphoric acid groups —OPOM claim 25 , where M is H or a k-valent counterion 1/kY.35. The compound ...

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Номер записи: 29
03-10-2013 дата публикации

COMPOUNDS AND METHOD FOR REDUCING URIC ACID

Номер: US20130259850A1
Автор: "ONeil James Dennen", Arudchandran Ramachandran, BAMAT Michael K., SHARMA Shalini, Von Borstel Reid W.
Принадлежит: WELLSTAT THERAPEUTICS CORPORATION

Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. 2. The method of claim 1 , wherein A is substituted or unsubstituted phenyl.3. The method of claim 2 , wherein A is 2 claim 2 ,6-dimethylphenyl.4. The method of claim 1 , wherein r is 1 claim 1 , t is 0 claim 1 , and q is 0.5. The method of claim 1 , wherein Ris methoxy.8. The method of claim 7 , wherein Ris methyl and Ris methyl.9. The method of claim 8 , wherein the Compound is selected from the group consisting of:4-(3-(2,6-Dimethylbenzyloxy)phenyl)-4-oxobutyric acid;3-(2,6-Dimethylbenzyloxy)-phenylacetic acid; and4-3-(2,6-Dimethylbenzyloxy)-phenyl)-4-hydroxybutanoic acid.10. The method of claim 8 , wherein the Compound is selected from the group consisting of:2-(3-(2,6-Dimethylbenzyloxy)-4-methoxyphenyl)acetic acid;4-(3-(2-Methylbenzyloxy)phenyl)-4-oxobutanoic acid;4-(3-(2,6-Difluorobenzyloxy)phenyl)-4-oxobutanoic acid;4-(3-(2-Fluoro-6-methylbenzyloxy)phenyl)-4-oxobutanoic acid;4-(3-(2,6-Dimethylbenzyloxy)phenyl)-2,2-dimethyl-4-oxobutanoic acid;4-(3-(2,6-Dimethylbenzyloxy)phenyl)butanoic acid;Methyl 3-(3-(2,6-dimethylbenzyloxy)phenyl)-3-oxopropanoate;5-(3-(2,6-Dimethylbenzyloxy)phenyl)-5-oxopentanoic acid;2-(3-(2,6-Dimethylbenzyloxy)phenyl)-2-oxoacetic acid;5-(3-(2,6-Dimethylbenzyloxy)phenyl)pentanoic acid;3-(3-(2,6-Dimethylbenzyloxy)phenyl)propanoic acid;2-(3-(2,6-Difluorobenzyloxy)phenyl)acetic acid;4-(3-(2,6-Dichlorobenzyloxy)phenyl)-4-oxobutanoic acid;2-(3-(2,6-Dimethylbenzyloxy)phenyl)propanoic acid;2-(3-(4-Trifluoromethyl)benzyloxy)phenyl)acetic acid;2-(3-(2,4-bis(trifluoromethyl)benzyloxy)phenyl)acetic acid;2-(3-(2,6-Dimethylbenzyloxy)phenyl)butanoic acid;2-(3-(3,5-Dimethylbenzyloxy)phenyl)acetic acid;2-(3-(2,4-Dimethylbenzyloxy)phenyl)acetic acid;2-(3-(2,6-Dimethoxylbenzyloxy)phenyl)acetic acid;2-(3-(Benzyloxy)phenyl)acetic acid;2-(3-(2,6-Dimethylbenzyloxy)phenyl)propanoic acid;2-(3-(2, ...

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Номер записи: 30
03-10-2013 дата публикации

NITRIC OXIDE AND ITS BIOMEDICAL SIGNIFICANCE

Номер: US20130261146A1
Автор: Kream Richard M., Mantione Kirk, Stefano George B., Zhu Wei
Принадлежит: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK

A pharmaceutical composition for stimulating nitric oxide production in mammalian cells, the pharmaceutical composition including at least one compound selected from a group consisting of: 2,3-dihydroxypropyl oleate; bis(m-phenoxyphenyl) ether; 6-acetyl-5,6,6a,7-tetrahydro-4H-dibezo(de,g)quinoline; and (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline. 1. A pharmaceutical composition for stimulating nitric oxide production in mammalian cells , the pharmaceutical composition comprising:at least one compound selected from a group consisting of: 2,3-dihydroxypropyl oleate; bis(m-phenoxyphenyl)ether; 6-acetyl-5,6,6a,7-tetrahydro-4H-dibezo(de,g)quinoline; and (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline.2. The pharmaceutical composition of claim 1 , wherein the at least one compound includes 2 claim 1 ,3-dihydroxypropyl oleate.3. The pharmaceutical composition of claim 1 , wherein the at least one compound includes bis(m-phenoxyphenyl)ether.4. The pharmaceutical composition of claim 1 , wherein the at least one compound includes 6-acetyl-5 claim 1 ,6 claim 1 ,6a claim 1 ,7-tetrahydro-4H-dibezo(de claim 1 ,g)quinoline.5. The pharmaceutical composition of claim 1 , wherein the at least one compound includes (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline.6Allium vineale, Salix alba, AgropyrumPetroselinium crispum, Taraxacum officinale, Sesamum indicum, MedicagoPiper methysticum, AnthemisTurnera diffusa, Verbascum densiflorum, OcimumMaranta arundinaceae, Coriandrum sativum, Artemesia dracunculus, Lavendula augustifolia, Mentha pulegium, Centella asiatica, Ginko bilobaVitis vinifera.. The pharmaceutical composition of claim 1 , wherein the at least one compound is derived/extracted from at least one plant species selected from the group consisting of spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , and7. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has the ability to stimulate ...

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Номер записи: 31
17-10-2013 дата публикации

DERIVATIVES FOR PERFLUOROALKOXY SULFOSUCCINATES AS SURFACTANTS

Номер: US20130269568A1
Автор: Claus Eckhard, Hierse Wolfgang, Kleineidam Melanie
Принадлежит: Merck Patent GmBH

The present invention relates to novel compounds containing Rf end groups, to the use thereof as surface-active substances, and to processes for the preparation of these compounds. The claimed compounds fall under the following formula: (I), Two examples of claimed compound are: (II), (III). 2. Compounds according to claim 1 , characterised in that at least four claim 1 , preferably four claim 1 , six or nine claim 1 , Rfgroup are present.3. Compounds according to claim 1 , characterised in that Y claim 1 , Yand Yare equal to O.4. Compounds according to claim 1 , characterised in that L=L=Land are equal to linear or branched alkyl having 1 to 10 C atoms.5. Compounds according to claim 1 , characterised in that the fluorinated groups Rfused are branched or unbranched claim 1 , perfluorinated alkyl radicals having 1 to 10 C atoms claim 1 , preferably 1 to 6 C atoms claim 1 , in particular 1-4 C atoms.6. Compounds according to claim 1 , characterised in that X is an anionic group claim 1 , preferably —SO claim 1 , —OSO claim 1 , —PO claim 1 , or OPO claim 1 , in particular —SO.7. Compounds according to claim 1 , characterised in that X is a cationic group claim 1 , preferably —NRRRZ— claim 1 , where R claim 1 , Rand Reach stand claim 1 , independently of one another claim 1 , for H claim 1 , C-alkyl claim 1 , Ar or —CHAr and Ar stands for an unsubstituted or mono- or polysubstituted aromatic ring or condensed ring systems having 6 to 18 C atoms in which claim 1 , in addition claim 1 , one or two CH groups may be replaced by N.8. Compounds according to claim 1 , characterised in that X is a nonionic group claim 1 , preferably linear or branched alkyl claim 1 , where one or more non-adjacent C atoms may be replaced by O claim 1 , S and/or N claim 1 , —OH claim 1 , —OCOCR═CHand —O-(glycoside) claim 1 , wherein o stands for an integer from 1 to 10.9. Compounds according to claim 8 , characterised in that X equal to R—(O—CHCHR)— where m=an integer from the range from 1 to ...

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Номер записи: 32
17-10-2013 дата публикации

Vaccination against pcskk 9 for lowering cholesterol

Номер: US20130273081A1
Автор: Andrea Carfi, Paolo Monaci
Принадлежит: MSD Italia SRL

The present invention relates to pharmaceutical compositions comprising PCSK9 DNA or PCSK9 proteins or PC-SK9 peptides and CpG adjuvant; this composition is used to lower cholesterol levels specifically LDL cholesterol levels.

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Номер записи: 33
17-10-2013 дата публикации

PLEUROMUTILIN DERIVATIVES FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY MICROBES

Номер: US20130274329A1
Автор: Heilmayer Werner, Riedl Rosemarie, Thirring Klaus
Принадлежит: NABRIVA THERAPEUTICS AG

Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents. 1. A compound selected from the group consisting of N-unsubstituted , N-alkylated , and N-acylated{'sub': '0-4', '14-O-[(amino(C)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins,'}{'sub': '0-4', '14-O-[(amino(C)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins,'}{'sub': '0-4', '14-O-[(amino(C)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins,'}{'sub': '0-4', '14-O-[(amino(C)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, and'}{'sub': '0-4', '14-O-[(amino(C)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins.'}2. A compound according to which is an N-unsubstituted claim 1 , N-alkylated claim 1 , or N-acylated 14-O-[amino(C)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilin or an N-unsubstituted claim 1 , N-alkylated claim 1 , or N-acylated 14-O-[amino(C)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilin claim 1 ,wherein one ring of the bicyclic alkyl is a cyclopentyl ring.6. A compound according to claim 1 , selected from the group consisting of14-O-{[(1R,2R,4R)-4-Amino-2-hydroxy-cyclopentylsulfanyl]-acetyl}-mutilin and the (1S,2S,4S) diastereomer thereof,14-O-{[(1R,2R,4S)-4-Amino-2-hydroxy-cyclopentylsulfanyl]-acetyl}-mutilin and the (1S,2S,4R) diastereomer thereof ...

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Номер записи: 34
17-10-2013 дата публикации

Guerbet Alcohols and Methods for Preparing and Using Same

Номер: US20130274511A1
Автор: Foley Patrick, YANG Yonghua
Принадлежит:

The invention relates to Guerbet alcohol precursors and Guerbet alcohols, as well as to processes for synthesizing them.

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Номер записи: 35
31-10-2013 дата публикации

SALTS OF KUKOAMINE B, PREPARATION METHOD AND USE THEREOF

Номер: US20130289112A1
Автор: Cao Hongwei, Huang Min, Li Yan, Liu Xin, Lu Yongling, Wang Ning, Wei Guo, Yang Jingcheng, Yang Yang, Zhao Kecen, Zheng Jiang, Zheng Xinchuan, Zhou Hong, Zhu Yuanfeng
Принадлежит: TIANJIN CHASESUN PHARMACEUTICAL CO., LTD

Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis. 2. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a hydrogenacid claim 1 , and wherein the hydrogenacid is any one of hydrochloric acid and hydrobromic acid.3. The salts of kukoamine B as claimed in claim 1 , wherein A comprises an oxacid claim 1 , and wherein the oxacid is any one of sulfuric acid claim 1 , phosphoric acid claim 1 , and nitric acid.4. The salts of kukoamine B as claimed in claim 1 , wherein A comprises an inorganic acid claim 1 , and wherein the inorganic acid is any one of hydrochloric acid claim 1 , hydrobromic acid claim 1 , sulfuric acid claim 1 , and phosphoric acid.5. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a carboxylic acid claim 1 , and wherein the carboxylic acid is any one of acetic acid claim 1 , propionic acid claim 1 , butyric acid claim 1 , oxalic acid claim 1 , malonic acid claim 1 , succinic acid claim 1 , adipic acid claim 1 , benzoic acid claim 1 , phenylpropionic acid claim 1 , cinnamic acid claim 1 , stearic acid claim 1 , trifluoroacetic acid claim 1 , maleic acid claim 1 , fumaric acid claim 1 , nicotinic acid claim 1 , and palmitic acid.6. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a hydroxy acid claim 1 , and wherein the hydroxy acid is any one of malic acid claim 1 , citric acid claim 1 , lactic acid claim 1 , hydroxybutyric ...

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Номер записи: 36
31-10-2013 дата публикации

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

Номер: US20130289117A1
Автор: Dasseux Jean-Louis H., Oniciu Carmen Daniela
Принадлежит: ESPERION THERAPEUTICS, INC.

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The method of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The method of claim 1 , wherein m is 0.4. The method of claim 1 , wherein m is 1.5. The method of claim 1 , wherein n is 4.6. The method of claim 1 , wherein n is 5.7. The method of claim 1 , wherein z is 0.861-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures thereof; compositions comprising a hydroxyl compound or a pharmaceutically acceptable salt, hydrate, solvate, or mixtures thereof; and methods for treating or preventing a disease or disorder such as, but not limited to, aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic ...

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Номер записи: 37
07-11-2013 дата публикации

COMPOUNDS AND METHODS FOR INDUCING APOPTOSIS IN CANCER CELLS USING A BH3 ALPHA-HELICAL MIMETIC

Номер: US20130295185A1
Автор: Carie Adam, Hamilton Andrew D., Sebti Said M., Sill Kevin
Принадлежит:

A novel BH3 α-helical mimetic, BH3-M6, which binds to Bcl-Xand prevents its binding to fluorescently-labeled Bak-BH3 peptide in vitro with an ICvalue of 734 nM is presented herein. BH3-M6 is a pan-Bcl-2 antagonist that inhibits the binding of Bcl-X, Bcl-2 and Mcl-1 to multi-domain Bax or Bak, or BH3-only Bim or Bad in a cell-free system and in intact human cancer cells, freeing up pro-apoptotic proteins to induce apoptosis. BH3-M6-induced apoptosis is caspase- and Bax-dependent. Furthermore, human cancer cells with high Bcl-2 or Bcl-Xlevels are more sensitive to BH3-M6-induced cell death, suggesting that this compound can overcome drug resistance due to Bcl-2 or Bcl-Xoverexpression. The pan-Bcl-2 inhibitor BH3-M6 may be encapsulated in a micelle to provide a more bioavailable therapeutic agent. Specifically, the BH3-M6 compound may be encapsulated within a micelle comprising a multiblock copolymer according to the methods described herein. 3. The micelle of claim 2 , wherein Ris —N.4. The micelle of claim 2 , wherein Ris —CH.6. The micelle of claim 5 , wherein Rand Rare both —CH.7. The micelle of claim 5 , wherein M is iron.8. A method of treating cancer comprising administering a therapeutically effective amount of at least one pan-Bcl-2 inhibitor to a subject in need thereof wherein the at least one pan-Bcl-2 inhibitor is BH3-M6 or pharmaceutically acceptable salts claim 5 , prodrugs claim 5 , salts of a prodrugs and metabolites thereof.9. The method of claim 8 , wherein the pan-Bcl-2 inhibitor is encapsulated in a multiblock copolymer of Formula I.10. The method of claim 8 , wherein the pan-Bcl-2 inhibitor is encapsulated in a crosslinked multiblock polymer of Formula III.11. The method of claim 8 , wherein the cancer is characterized by the overexpression of an anti-apoptotic Bcl-2 family protein.12. The method of claim 8 , wherein the cancer is selected from the group consisting of breast cancer claim 8 , non-small cell lung cancer claim 8 , prostate cancer and ...

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Номер записи: 38
07-11-2013 дата публикации

Crystalline pharmaceutically active ingredients

Номер: US20130296353A1
Автор: Balazs Havasi, Balázs VOLK, Csaba Hamori, Éva SIPOS, Ferenc Jurak, Györgyi KOVÁNYINÉ LAX, Gyula LUKÁCS, Imre Markovits, Katalin KÁTAINÉ FADGYAS, Krisztina Fodorne Kocsmar, Mónika MEZŐVÁRI, Zsolt Runge
Принадлежит: EGIS PHARMACEUTICALS PLC

The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis.

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Номер записи: 39
07-11-2013 дата публикации

3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS

Номер: US20130296358A1
Автор: Ambarkhane Ameet Vijay
Принадлежит:

The invention relates to derivatives of formula (I), 1. A compound which is 2-Amino-N—[(R)-1-benzyloxymethyl-2-((4S ,5R)-2-methyl-1-oxo-4-phenyl-2 ,7-diaza-spiro[4.5]dec-7-yl)-2-oxo-ethyl]-2-methyl-propionamide L-malate salt.2. A crystalline form of the compound of .3. The crystalline form according to claim 2 , characterised by an X-ray diffraction pattern comprising four 2θ values selected from the group consisting of 8.493±0.2° claim 2 , 15.574±0.2° claim 2 , 19.339±0.2° claim 2 , 20.842±0.2° at a temperature of about 22° C.4. The crystalline form according to claim 2 , characterised by an X-ray diffraction spectrum substantially the same as the X-ray diffraction spectrum shown in .5. The crystalline form according to claim 2 , having a thermo gravimetric analysis (TGA) diagram substantially the same as that shown in .6. The crystalline form according to claim 2 , characterised by an X-ray diffraction pattern comprising four 2θ values selected from the group consisting of 8.383±0.2° claim 2 , 11.724±0.2° claim 2 , 17.918±0.2° claim 2 , 19.237±0.2° at a temperature of about 22° C.7. The crystalline form according to claim 2 , having an X-ray diffraction spectrum substantially the same as the X-ray diffraction spectrum shown in .8. The crystalline form according to claim 2 , having a thermo gravimetric analysis (TGA) diagram substantially the same as that shown in .9. The crystalline form according to claim 2 , characterised by an X-ray diffraction pattern comprising four 2θ values selected from the group consisting of 10.084±0.2° claim 2 , 16.209±0.2° claim 2 , 20.166±0.2° claim 2 , 22.325±0.2° at a temperature of about 22° C.10. The crystalline form according to claim 2 , having an X-ray diffraction spectrum substantially the same as the X-ray diffraction spectrum shown in .11. The crystalline form according to claim 2 , having a thermo gravimetric analysis (TGA) diagram substantially the same as that shown in .12. The crystalline form according to claim 2 , ...

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Номер записи: 40
07-11-2013 дата публикации

Novel Dihydroxybenzene Derivatives and Antiprotozoal Agent Comprising Same as Active Ingredient

Номер: US20130296422A1
Автор: Kita Kiyoshi, Saimoto Hiroyuki, Yabu Yoshisada, Yamamoto Masaichi
Принадлежит: ARIGEN PHARMACEUTICALS, INC.

Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) 2. The compound claim 1 , optical isomer thereof claim 1 , and pharmaceutically acceptable salt thereof of claim 1 , wherein the one or more substituents of Rare each any one of —COOH claim 1 , —COORa (wherein Ra represents a Calkyl group) claim 1 , —CHO claim 1 , —COOCHCH(OH)CHOH claim 1 , —COO—CH—Rb (wherein Rb represents a group formed by removing one hydrogen atom on a carbon atom of aromatic hydrocarbons claim 1 , such as benzene claim 1 , naphthalene claim 1 , and anthracene) claim 1 , —O—CO-Rc (wherein Rc represents a Calkyl group) claim 1 , —OH claim 1 , —O-Rd (Rd represents a Calkyl group) claim 1 , —O—CH—O—CH claim 1 , —HET (HET represents a group formed by removing one hydrogen atom on a carbon or nitrogen atom of heterocyclic compounds) claim 1 , and —O-HET (HET is defined as above).4. The pharmaceutical composition of claim 3 , wherein the one or more substituents of Ris any one of —COOH claim 3 , —COORa (wherein Ra represents a Calkyl group) claim 3 , —CHO claim 3 , —COOCHCH(OH)CHOH claim 3 , —COO—CH—Rb (wherein Rb represents a group formed by removing one hydrogen atom on a carbon atom of aromatic hydrocarbons claim 3 , such as benzene claim 3 , naphthalene claim 3 , and anthracene) claim 3 , —O—CO-Rc (wherein Rc represents a Calkyl group) claim 3 , —OH claim 3 , —O-Rd (wherein Rd represents a Calkyl group) claim 3 , —O—CH—O—CH claim 3 , —HET (wherein HET represents a group formed by removing one hydrogen atom on a carbon or nitrogen atom of heterocyclic compounds) claim 3 , and —O-HET (wherein HET is defined as above).5. The pharmaceutical composition of or claim 3 , further comprising glycerol.7Trypanosoma.. The agent of claim 6 , wherein the protozoans is8Cryptosporidium.. The agent of claim 6 , wherein the protozoans is9. The agent of any one of to claim 6 , further comprising glycerol.11. The kit of ...

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Номер записи: 41
07-11-2013 дата публикации

PHENYLGLYOXYLIC ACID DERIVATIVES AND THEIR PREPARATION AND USE

Номер: US20130296599A1
Автор: Andrews Robert Carl, Bondlela Muralidhar, Campian Eugene, Kache Rajashaker, Polisetti Dharma Rao, Santhosh Kalpathy, Yokum Thomas Scott
Принадлежит:

The invention provides novel phenylglyoxylic acid derivatives, which may be useful as intermediates for preparing stereoisomerically enriched drug compounds. The invention also provides methods of making phenylglyoxylic acid derivatives, and uses of phenylglyoxylic acid derivatives. 2. The compound of claim 1 , where R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare all hydrogen.3. The compound of claim 2 , where Ris hydrogen and Ris chloro claim 2 , or Ris chloro and Ris hydrogen.4. The compound of claim 3 , where Ris chloro.5. The compound of claim 4 , where Ris methyl.6. The compound of claim 1 , where Z is methylene.8. The method of claim 7 , where{'sup': 1', '5', '6', '7', '8', '9, 'R, R, R, R, R, and Rare all hydrogen;'}{'sup': 2', '4', '2', '4, 'Ris hydrogen and Ris chloro, or Ris chloro and Ris hydrogen;'}{'sup': '3', 'Ris chloro;'}{'sup': '10', 'Ris methyl; and'}Z is methylene.9. The method of claim 7 , where the step of oxidizing comprises contacting the compound with an oxidation catalyst.10. The method of claim 9 , where the oxidation catalyst is a metal oxide.11. The method of claim 9 , where the oxidation catalyst is a transition metal oxide.12. The method of claim 9 , where the oxidation catalyst is manganese (IV) oxide.13. The method of claim 9 , where the oxidation catalyst is an organic oxidation catalyst.14. The method of claim 9 , where the oxidation catalyst is a nitroxyl compound.15. The method of claim 9 , where the oxidation catalyst is 2 claim 9 ,2 claim 9 ,6 claim 9 ,6-tetramethylpiperidinyloxy claim 9 , 4-hydroxy-2 claim 9 ,2 claim 9 ,6 claim 9 ,6-tetramethylpiperidinyloxy claim 9 , 4-acetamido-2 claim 9 ,2 claim 9 ,6 claim 9 ,6-tetramethylpiperidinyloxy claim 9 , 4-methylsulfonyloxy-TEMPO claim 9 , 4-(2-bromoacetamido)-TEMPO claim 9 , 4-(2-iodoacetamido)-TEMPO claim 9 , 4-amino-TEMPO claim 9 , 4-carboxy-TEMPO claim 9 , 4-cyano-TEMPO claim 9 , 4-benzoyloxy-TEMPO claim 9 , 4-isothio-cyanato-TEMPO claim 9 , 4-maleimido- ...

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Номер записи: 42
07-11-2013 дата публикации

KETOCARBOXYLIC ACIDS, KETOCARBOXYLIC ESTERS, METHODS OF MANUFACTURE AND USES THEREOF

Номер: US20130296601A1
Автор: Leibig Cora M., Manzer Leo E., MULLEN Brian D.
Принадлежит:

Ketocarboxylic acids such as levulinic acid can be efficiently purified in high yield by esterification with a hydrocarbon polyol to the corresponding polyketocarboxylic ester, which can be readily purified, for example recrystallized. After purification, the ketocarboxylic ester can be hydrolyzed to provide pure ketocarboxylic acid, or a salt thereof, after removal of the esterifying hydrocarbon polyol, or used for other synthetic transformations. Advantageously, the polyketocarboxylic esters, ketocarboxylic acids, and salts thereof produced by this method are obtained in high purity. 2. The composition of claim 1 , wherein the residue comprises furfural claim 1 , formic acid claim 1 , furfuryl alcohol claim 1 , hydroxymethyl furfural claim 1 , angelica lactone claim 1 , a humin claim 1 , a polysaccharide claim 1 , a saccharide claim 1 , or a combination comprising at least one of the foregoing residues.4. The composition of claim 3 , wherein the impurity is a residue of a biomass.5. The composition of claim 4 , wherein the residue comprises furfural claim 4 , formic acid claim 4 , furfuryl alcohol claim 4 , hydroxymethyl furfural claim 4 , angelica lactone claim 4 , a humin claim 4 , a polysaccharide claim 4 , a saccharide claim 4 , or a combination comprising at least one of the foregoing residues.7. The compound of claim 6 , wherein the polyketocarboxy ester IIIa is crystalline.8. A composition comprising the compound of claim 6 , the composition comprising:at least 99 wt % of the polyketocarboxy ester IIIa; andup to 1 wt % of an impurity.9. The composition of claim 6 , wherein the polyketocarboxy ester IIIa is crystalline.10. The composition of claim 8 , wherein the impurity is a residue of a biomass.11. The composition of claim 10 , wherein the residue comprises furfural claim 10 , formic acid claim 10 , furfuryl alcohol claim 10 , hydroxymethyl furfural claim 10 , angelica lactone claim 10 , a humin claim 10 , a polysaccharide claim 10 , a saccharide claim 10 ...

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Номер записи: 43
14-11-2013 дата публикации

PROCESS FOR SYNTHESIZING PHENYLACETIC ACID BY CARBONYLATION OF TOLUENE

Номер: US20130303798A1
Автор: Huang Hanmin, Xia Chungu, Xie Pan
Принадлежит: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences

A production process for substituted phenylacetic acids or ester analogues thereof is disclosed. In this process toluene or toluene substituted with various substituents, an alcohol, an oxidant and carbon monoxide are used as raw materials to obtain compounds comprising structure of phenylacetic acid ester or analogues thereof by catalysis of the complex catalyst formed from transition metal and ligand, and such compounds are hydrolyzed to obtain various substituted phenylacetic acid based compounds. This type of compounds and their derivatives serve as important fine chemicals used widely in the industries of pharmaceuticals, pesticides, perfume and the like. 2. The preparation process according to claim 1 , characterized in that Rand Rare each independently selected from linear or branched Calkyl claim 1 , preferably methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl or isobutyl.3. The preparation process according to claim 1 , characterized in that Rand Rare each independently selected from linear or branched Calkoxy claim 1 , preferably methoxy claim 1 , ethoxy claim 1 , propoxy claim 1 , or butoxy.4. The preparation process according to claim 1 , characterized in that Rand Rare each independently selected from phenyl claim 1 , substituted phenyl claim 1 , benzyl claim 1 , substituted benzyl claim 1 , 1-naphthyl claim 1 , 2-naphthyl or substituted naphthyl.5. The preparation process according to claim 1 , characterized in that a precursor of the transition metal catalyst is one or more selected from: ruthenium-based metal catalyst precursors; ruthenium trichloride claim 1 , dodecacarbonyltriruthenium; rhodium-based metal catalyst precursors claim 1 , preferably rhodium trichloride claim 1 , rhodium acetate claim 1 , dodecacarbonyltetrarhodium claim 1 , tris(triphenylphosphinecarbonyl) rhodium hydride claim 1 , triphenylphosphinecarbonyl rhodium acetylacetonate claim 1 , vinyl rhodium chloride; palladium-based metal catalyst precursors ...

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Номер записи: 44
28-11-2013 дата публикации

SILICONE MODIFIED FATTY ACIDS, METHOD OF PREPARATION AND USAGE THEREOF

Номер: US20130317105A1
Автор: Falk Benjamin, Naue Jeferson A.
Принадлежит: Natura Inovacao e Tecnologia de Produtos Ltda.

The present invention relates to silicone modified fatty carboxylic acid compounds. More specifically, the present invention is derived from low molecular weight, i.e., short chain, silicone modified fatty carboxylic acids, their use and method of making same. The present invention provides for a silicone compound partially derived from a natural product, sapucainha oil, for use in cosmetic formulations. 1. A cosmetic product comprising a modified silicone compound comprising the reaction product of: {'br': None, 'sub': a', 'b', 'c', 'd', 'e', 'f', 'g, 'sup': A', 'B', 'C, 'MMDDTTQ'}, 'a) at least one cyclic ether silicone having the formula [{'sup': 1', '2', '3, 'sub': '1/2', 'M=RRRSiO'}, {'sup': A', '4', '5', '6, 'sub': '1/2', 'M=RRRSiO'}, {'sup': 7', '8, 'sub': '2/2', 'D=RRSiO'}, {'sup': B', '9', '10, 'sub': '2/2', 'D=RRSiO'}, {'sup': '11', 'sub': '3/2', 'T=RSiO'}, {'sup': C', '12, 'sub': '3/2', 'T=RSiO;'}, {'sub': '4/2', 'Q=SiO;'}], 'wherein;'}{'sup': 1', '2', '3', '5', '6', '7', '8', '10', '11, 'R, R, R, R, R, R, R, R, and Rare each independently a monovalent hydrocarbon radical having from 1 to 6 carbon atoms;'}{'sup': 4', '9', '12, 'R, R, and Rare each independently a monovalent hydrocarbon radical containing from 3 to 25 carbon atoms and possessing at least one epoxy or oxetane group;'}wherein subscripts a, b, c, d, e, f, and g are zero or positive and their sum is not greater than 25,with the proviso that at least one of subscripts b, d, and f is positive; andb) a substantially pure fatty carboxylic acid said fatty carboxylic acid prepared from sapucainha oil.2. The cosmetic product of wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently a monovalent hydrocarbon radical having from 1 to 3 carbon atoms.3. The cosmetic product of wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently a monovalent ...

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Номер записи: 45
28-11-2013 дата публикации

COPOLYMERIZABLE SURFACTANTS

Номер: US20130317190A1
Автор: Busch Stefan, Held Uwe, Klagge Ronald, Mausberg Thomas, Scherer Markus, Schliwka Thomas
Принадлежит: Cognis IP Management GmbH

The invention relates to the use of compounds of the formula (I), R—CH(O—(AO)X)—CH—O—(AO)—CH—CH═CH, where: R denotes an alkyl radical which has 8 to 18 carbon atoms and can be saturated or unsaturated, straight-chain or branched; X denotes a sulfate or phosphate group or hydrogen; (AO) denotes an alkylene oxide unit, selected from the group consisting of ethylene oxide, propylene oxide or butylene oxide; n denotes a number in the range of 0 to 50; and m denotes zero or a number in the range of 1 to 30; as copolymerizable emulsifiers in the emulsion polymerization of olefinically unsaturated monomers. 3. The method of claim 2 , wherein X is a sulfate or phosphate group.4. The method of claim 3 , wherein the sulfate or phosphate group is in partly or wholly neutralized form.5. The method of claim 2 , wherein the degree of alkoxylation n is from 1 to 30.6. The method of claim 5 , wherein the degree of alkoxylation n is from 3 to 10 and (AO) is an ethylene oxide unit.7. A process for preparing a polymer by emulsion polymerization of an olefinically unsaturated monomer claim 1 , which process comprises utilizing said compound (I) according to as a copolymerizable emulsifier.8. The compound of claim 1 , wherein X is a sulfate or phosphate group.9. The compound of claim 8 , wherein the sulfate or phosphate group is in partly or wholly neutralized form.10. The compound of claim 1 , wherein the degree of alkoxylation n is from 1 to 30.11. The compound of claim 10 , wherein the degree of alkoxylation n is from 3 to 10 and (AO) is an ethylene oxide unit.12. The method of claim 2 , wherein the compound of formula (I) is copolymerized in the polymer.13. The method of claim 2 , further comprising initiating the reaction with potassium peroxodisulfate or a redox initiator.14. The method of claim 2 , wherein the compound of formula (I) is in salt form. The present invention lies within the polymer sector and relates to allyl ethers with a specific structure and also to their use as ...

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Номер записи: 46
19-12-2013 дата публикации

PROCESS FOR THE PREPARATION OF PYRIDO [2,1-A] ISOQUINOLINE DERIVATIVES COMPRISING OPTICAL RESOLUTION OF AN ENAMINE

Номер: US20130338366A1
Автор: Abrecht Stefan, Adam Jean-Michel, Fettes Alec, Hildbrand Stefan
Принадлежит:

This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula 2. The process according to claim 1 , comprising step a).3. The process according to claim 1 , comprising the steps a) and b).4. The process according to claim 1 , comprising the steps a) to d).5. The process according to claim 1 , wherein the steps b) and c) are carried out without isolation of intermediate IV.6. The process according to claim 1 , characterized in that the optical resolution in step a) is a crystallization-induced dynamic resolution.9. The process according to claim 1 , characterized in that the optical resolution in step a) is performed with a resolving agent selected from (+)—O claim 1 ,O′-dibenzoyl-D-tartaric acid and (+)-O claim 1 ,O′-dibenzoyl-D-tartaric acid mono dimethylamide.10. The process according to claim 1 , characterized in that the optical resolution in step a) is performed in a solvent selected from the group consisting of water claim 1 , methanol claim 1 , ethanol claim 1 , isopropanol claim 1 , acetone claim 1 , tetrahydrofuran claim 1 , ethyl acetate claim 1 , toluene and mixtures thereof.11. The process according to claim 10 , characterized in that the optical resolution in step a) is performed with the enamine of formula II wherein Ris methyl claim 10 , ethyl or isopropyl.12. The process according to claim 1 , characterized in that the transformation of the (S)-enamine salt of formula III in step b) is performed by a reduction under acidic conditions followed by the introduction of an amino protecting group.13. The process according to claim 1 , characterized in that the reduction is performed with reducing agents selected from sodium borohydride claim 1 , lithium borohydride and sodium cyanoborohydride.14. The process according to claim 1 , characterized in that the reduction is performed in an organic solvent at temperatures of −40° C. to 30° C.15. The process according to claim 1 , characterized in that an amino ...

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Номер записи: 47
19-12-2013 дата публикации

METHOD OF PRODUCING OPTICALLY ACTIVE 1-AMINO-2-VINYLCYCLOPROPANE CARBOXYLIC ACID ESTER

Номер: US20130338392A1
Автор: Aikawa Toshiaki
Принадлежит: Sumitomo Chemical Company, Limited

An optically active 1-amino-2-vinylcyclopropanecarboxylic acid ester with high optical purity can be obtained by a method of producing an optically active 1-amino-2-vinylcyclopropanecarboxylic acid ester by reacting a 1-amino-2-vinylcyclopropanecarboxylic acid ester with an optically active tartaric acid or an optically active camphorsulfonic acid in a solvent, isolating one diastereomeric salt from the obtained diastereomeric salt mixture and treating the isolated diastereomeric salt with an inorganic acid or a base. 1. A method of producing an optically active 1-amino-2-vinylcyclopropanecarboxylic acid ester , comprising:reacting a 1-amino-2-vinylcyclopropanecarboxylic acid ester with optically active tartaric acid or optically active camphorsulfonic acid in a solvent to thereby obtain a mixture of diastereomeric salts and isolating one of the diastereomeric salts from the thus obtained mixture; andtreating the isolated diastereomeric salt with an inorganic acid or a base.3. The method of claim 1 , wherein the reaction of the 1-amino-2-vinylcyclopropanecarboxylic acid ester with the optically active tartaric acid or the optically active camphorsulfonic acid is carried out in an aromatic solvent claim 1 , a ketone solvent claim 1 , an ester solvent claim 1 , an alcohol solvent claim 1 , an ether solvent claim 1 , or a mixture thereof.4. The method of claim 1 , wherein the reaction of the 1-amino-2-vinylcyclopropanecarboxylic acid ester with the optically active tartaric acid or the optically active camphorsulfonic acid is carried out in a mixed solvent of an aromatic solvent and an alcohol solvent.7. The method of claim 6 , wherein Arand Ar are both 3 claim 6 ,5-bis(trifluoromethyl)phenyl groups claim 6 , Rand R are both hydrogen atoms claim 6 , and Rand Rare each independently an alkyl group having 1 to 12 carbon atoms.8. The method of claim 6 , wherein Aris an aromatic hydrocarbon group having 6 to 20 carbon atoms claim 6 , which has an alkoxy group having 1 to ...

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Номер записи: 48
19-12-2013 дата публикации

BIOMASS-RESOURCE-DERIVED POLYURETHANE, METHOD FOR PRODUCING SAME, AND BIOMASS-RESOURCE-DERIVED POLYESTER POLYOL

Номер: US20130338395A1
Автор: AOSHIMA Takayuki, Itou Hiroto, Matsumoto Takanao, Nakajima Yasuko, OHARA Teruhiko, Sugai Naoki, Suzuki Naoki
Принадлежит:

The invention relates to a method for producing a biomass-resource-derived polyurethane, which comprises: reacting a dicarboxylic acid and an aliphatic diol to produce a polyester polyol; and reacting the polyester polyol and a polyisocyanate compound, wherein the dicarboxylic acid contains at least one component derived from biomass resources, a content of an organic acid in the dicarboxylic acid is more than 0 ppm and not more than 1,000 ppm relative to the dicarboxylic acid, and a pKa value of the organic acid at 25° C. is not more than 3.7. 1. A biomass-resource-derived polyester polyol for production of a polyurethane , which at least comprises , as constituent units , a dicarboxylic acid unit , an aliphatic diol unit , and an organic acid unit having a pKa value at 25° C. of not more than 3.7 , wherein the dicarboxylic acid contains at least one component derived from biomass resources , and a content of the organic acid unit is more than 0% by mole and not more than 0.09% by mole relative to the dicarboxylic acid unit.2. The biomass-resource-derived polyester polyol according to claim 1 , wherein the at least one component of the dicarboxylic acid is one derived from biomass resources.3. The biomass-resource-derived polyester polyol according to claim 1 , wherein the dicarboxylic acid contains succinic acid derived from biomass resources.4. The biomass-resource-derived polyester polyol according to claim 1 , having a number average molecular weight of 500 or more and not more than 5 claim 1 ,000.5. The biomass-resource-derived polyester polyol according to claim 1 , wherein the organic acid unit is at least one member selected from malic acid claim 1 , tartaric acid claim 1 , and citric acid.6. The biomass-resource-derived polyester polyol according to claim 1 , having a value expressed as a Hazen color number (APHA value: in conformity with JIS-K0101) of not more than 50. The present application is a divisional of U.S. patent application Ser. No. 13/632,992, ...

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Номер записи: 49
16-01-2014 дата публикации

FERRIC ORGANIC COMPOUNDS, USES THEREOF AND METHODS OF MAKING SAME

Номер: US20140018420A1
Автор: KWOK David W.K., STOYNOV Nikolay Mintchev
Принадлежит: Panion & BF Biotech, Inc.

The present invention discloses a novel form of ferric organic compounds, including a form of ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. The ferric organic compounds of the present invention can be delivered effectively by oral route with better delivery to treat patients suffering from hyperphosphatemia, metabolic acidosis and other disorders responsive to ferric organic compound therapy. 174-. (canceled)75. A method of treating hyperphosphatemia , comprising:{'sup': '2', 'administering a therapeutically effective amount of an orally administrable form of ferric citrate to a subject, wherein the orally administrable form is prepared from a form of ferric citrate having an intrinsic dissolution rate of at least 1.88 mg/cm/min.'}76. The method of claim 75 , wherein the intrinsic dissolution rate is 1.88 to 4.0 mg/cm/min.77. The method of claim 75 , wherein the intrinsic dissolution rate is 1.9 to 4.0 mg/cm/min.78. The method of claim 75 , wherein the ferric citrate has the formula CHOFe.79. The method of claim 75 , wherein the orally administrable form is a tablet.80. The method of claim 75 , wherein the therapeutically effective amount is about 3 to 6 grams per day.81. The method of claim 75 , wherein the subject is a human being. This application is a Continuation of U.S. Ser. No. 12/711,679, filed Feb. 24, 2010 (now allowed), which is a Continuation of U.S. Ser. No. 11/206,981 (now U.S. Pat. No. 7,767,851), filed Aug. 18, 2005, which is a Continuation-in-part of International App'l No. PCT/US2004/004646, filed Feb. 18, 2004, which claims benefit of U.S. Ser. No. 60/462,684, filed Apr. 15, 2003, and U.S. Ser. No. 60/447,690, filed Feb. 19, 2003. The entire contents and disclosures of the preceding applications are hereby incorporated by reference into this application.Throughout this application, various publications are referenced. Disclosures of these publications in their entireties are hereby ...

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Номер записи: 50
16-01-2014 дата публикации

PROCESS FOR PRODUCING GLYCOLIC ACID

Номер: US20140018514A1
Автор: Itou Kiyoshi, Matoishi Kaori, Okazaki Shinya
Принадлежит: Mitsui Chemicals, Inc.

Glycolic acid having a high purity is obtained by subjecting glycolic acid or a glycolic acid solution containing contaminants to double-chamber electrodialysis combined with one or more treatments selected from among treatment with an activated carbon, treatment with an ion exchange resin, concentration treatment and cooling crystallization. 1. A glycolic acid obtained by a production process comprising carrying out 3 to 5 kinds of steps selected from the group consisting of the following steps (a1) , (a2) , (b) , (c) and (d) (but , the step (a2) must be employed) for a solution containing a glycolate one or two or more times in any order ,(a1) step for electrodialyzing with an anion exchange membrane and a cation exchange membrane;(a2) step for water-splitting electrodialysis;(b) step for cooling crystallization;(c) step for treatment with an activated carbon; and(d) step for treatment with an ion exchange resin.2. The glycolic acid according to claim 1 , wherein the kinds and order of the following steps are any one of (a1) (a2) (b) claim 1 , (c) (a2) (b) claim 1 , (c) (a2) (d) (c) or (c) (a2) (c) (d) for the solution containing the glycolate claim 1 ,(a1) step for electrodialyzing with anion exchange membrane and cation exchange membrane;(a2) step for water-splitting electrodialysis;(b) step for cooling crystallization;(c) step for treatment with an activated carbon; and(d) step for treatment with an ion exchange resin.3. The glycolic acid according to claim 1 , wherein 3 to 5 kinds of steps selected from the group consisting of following steps (a1) claim 1 , (a2) claim 1 , (b) claim 1 , (c) and (d) (but claim 1 , the step (a2) must be employed) are carried out one or two or more times in any order claim 1 , and the step (b) is subsequently carried out one or two or more times for a solution containing a glycolate claim 1 ,(a1) step for electrodialyzing with an anion exchange membrane and a cation exchange membrane;(a2) step for water-splitting electrodialysis;( ...

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Номер записи: 51
16-01-2014 дата публикации

HYDROGENATION OF CATMINT OIL

Номер: US20140018551A1
Автор: Hutchenson Keith W., Jackson Scott Christopher, Manzer Leo Ernest, SCHLEINITZ HENRY MAX, Scialdone Mark A.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Disclosed are methods for treating catmint oil. The treated catmint oil can be used for the production of hydrogenated catmint oil, which is enriched in the insect repellent, dihydronepetalactone. 1. A process for preparing hydrogenated catmint oil comprising:(a) distilling a beginning amount of crude catmint oil to produce (i) a distillate fraction comprising volatile components driven off from the crude catmint oil, wherein the weight of the distillate fraction comprises about 2% to about 20% of the weight of the beginning amount of crude catmint oil, and (ii) a pot fraction;(b) contacting the pot fraction produced in step (a) with hydrogen and a hydrogenation catalyst to produce hydrogenated catmint oil; and(c) optionally, recovering the hydrogenated catmint oil of step (b).2. The process of wherein the weight of the distillate fraction comprises about 5% to about 10% of the weight of the beginning amount of crude catmint oil.3. The process of wherein the step of distilling (a) comprises a step of (i) vacuum distilling claim 1 , (ii) steam distilling claim 1 , (iii) solvent distilling claim 1 , or (iv) steam distilling followed by solvent distilling.4. The process of which comprises a step of solvent distilling claim 3 , or of steam distilling followed by solvent distilling claim 3 , and wherein claim 3 , at the beginning of solvent distilling claim 3 , the weight of the solvent comprises about 5% to about 60% of the combined weight of catmint oil plus solvent.5. The process of wherein claim 4 , at the beginning of solvent distilling claim 4 , the weight of the solvent comprises about 10% to about 25% of the combined weight of catmint oil plus solvent.6. The process of which comprises a step of solvent distilling claim 3 , or of steam distilling followed by solvent distilling claim 3 , and wherein a solvent comprises a Cto Cstraight-chain or branched alcohol.7. The process of wherein the alcohol is selected from the group consisting of methanol claim 6 , ethanol ...

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Номер записи: 52
23-01-2014 дата публикации

PROCESS FOR TREPROSTINIL SALT PREPARATION

Номер: US20140024856A1
Автор: Bejan Elena, Giust Walter, Gorin Boris, OUDENES Jan, Souza Fabio
Принадлежит: Alphora Research Inc.

Disclosed is a process for preparing a treprostinil salt. The process involves the step of dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution. The treprostinil solution is reacted with an aqueous basic solution containing an alkali metal cation to form treprostinil salt. Allowing crystallization of the treprostinil salt to take place, and then collecting the treprostinil salt formed. 1. A process for preparing a treprostinil salt , comprising:dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution;reacting the treprostinil solution with an aqueous basic solution containing an alkali metal cation to form a reaction mixture containing the treprostinil salt;allowing crystallization of the treprostinil salt; andcollecting the treprostinil salt formed.2. The process according to claim 1 , wherein the water-miscible organic solvent is a water-miscible ketone solvent.3. The process according to claim 1 , wherein the water-miscible organic solvent is a hydrocarbon based water-miscible ketone solvent.4. The process according to claim 2 , wherein the water-miscible ketone solvent is a linear or branched alkyl ketone.5. The process according to claim 1 , wherein the water-miscible ketone solvent is acetone.6. The process according to claim 1 , wherein the water-miscible organic solvent is a water-miscible alcohol or water-miscible ether.7. The process according to claim 1 , wherein the water-miscible organic solvent is methanol claim 1 , ethanol claim 1 , 1-propanol claim 1 , 2-propanol claim 1 , tetrahydrofuran or acetonitrile.8. The process according to claim 1 , wherein ratio of treprostinil to the water-miscible organic solvent is 1 g of treprostinil to from 5 to 100 mL of the water-miscible organic solvent.9. The process according to claim 1 , wherein ratio of treprostinil to the water-miscible organic solvent is 1 g of treprostinil to from 15 to 50 mL of the water-miscible organic solvent.10. ...

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Номер записи: 53
06-02-2014 дата публикации

System For Purifying, Producing And Storing Biomolecules

Номер: US20140037961A1
Автор: Evans David
Принадлежит: ADC BIOTECHNOLOGY LIMITED

The invention relates to a lock-release method to be applied to biomolecules, such as antibodies, to improve the purification, production, stability and storage of biomolecules. A biomolecule is covalently bound to a polymer support comprising a diketone group so that the biomolecule can be purified, produced and/or stored before being released from the support. The diketone group of the polymer support is a 1,3-ketoester, 1,3-ketothioester or 1,3-ketoamide is a group of Formula (1): Ris an optionally substituted hydrocarbyl, perhalogenated hydrocarbyl, or a heterocyclyl group; Y is hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group; X is —O, —NRor —S, wherein the free valence of —O, —NRor —S is bonded to the support optionally via a linker; and Ris hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group. The invention also relates to a polymer support comprising the diketone group. 2. The method of claim 1 , wherein the method further comprises the step of washing the support-biomolecule compound.3. The method of or claim 1 , wherein the method further comprises the step of releasing the biomolecule from the support-biomolecule compound and recovering the biomolecule; and optionally recovering the support.4. The method of or claim 1 , wherein the method further comprises the steps of carrying out one or more chemical reactions on the support-biomolecule compound to synthesise support-biomolecule-drug compound;optionally washing the support-biomolecule-drug compound; andreleasing a biomolecule-drug conjugate from the support-biomolecule-drug compound,optionally, the method further comprises the step of recovering the support.5. The method of or claim 1 , wherein the method further comprises the step of drying the support-biomolecule compound;optionally, the method further comprises the step of releasing the biomolecule from the support-biomolecule compound and recovering the biomolecule.6. The method of any preceding claim ...

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Номер записи: 54
20-02-2014 дата публикации

METHOD FOR MANUFACTURING PHOSPHONOCROTONIC ACID DERIVATIVE

Номер: US20140051876A1
Автор: Ezaki Koji, Ina Shinji, Sakamoto Katsuhiro, Sakata Junichi, YAMAZAKI Takahiro
Принадлежит:

Provided is a method of manufacturing a high quality phosphonocrotonic acid derivative. 2: The method according to claim 1 , wherein said performing is at least one process of(A) a process of reacting the compound of Formula (I) with the compound of Formula (II), in the presence of the acid or the base, and(B) a process of reacting the compound of Formula (I) with the compound of Formula (II), followed by a treatment with the acid or the base.3: The method according to claim 1 , whereinthe compound of Formula (I) is triethyl phosphite,the compound of Formula (II) is ethyl 4-bromo-3-methylcrotonate,the compound of Formula (III) is triethyl-3-methyl-4-phosphonocrotonate.4: A method for manufacturing a compound comprising a 3-methylpenta-2 claim 1 ,4-dienoic acid residue claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'reacting the compound of Formula (III) obtained by the method according to with a carbonyl compound.'}5: The method according to claim 4 , whereinthe compound of Formula (III) is triethyl-3-methyl-4-phosphonocrotonate,the carbonyl compound is farnesal, andthe compound comprising 3-methylpenta-2,4-dienoic acid residue is (2E,4E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,4,6,10,14-pentaenoic acid.6: The method according to claim 4 , whereinthe compound of Formula (III) is triethyl-3-methyl-4-phosphonocrotonate,the carbonyl compound is β-ionylidene acetaldehyde, andthe compound comprising a 3-methylpenta-2,4-dienoic acid residue is (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexene-1-yl)nona-2,4,6,8-tetraenoic acid.7: The method according to claim 4 , whereinthe compound of Formula (III) is triethyl-3-methyl-4-phosphonocrotonate,the carbonyl compound is (2E,4E)-5-(4-methoxy-2,3,6-trimethylphenyl)-3-methylpenta-2,4-dienal, andthe compound comprising a 3-methylpenta-2,4-dienoic acid residue is ethyl (2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoate.9: The method according to claim 1 ...

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Номер записи: 55
20-02-2014 дата публикации

PROCESS FOR PREPARING METHACRYLIC ACID

Номер: US20140051886A1
Автор: Broell Dirk, Hiltner Horst, Krauss Thomas, Siegert Hermann
Принадлежит: Evonik Röhm GmbH

The present invention relates to a process for preparing methacrylic acid based on the hydrolysis of methacrylic esters. 1. A process for preparing methacrylic acid , the process comprising:converting acetone cyanohydrin to methacrylamide;esterifying methacrylamide in the presence of alcohols, thereby obtaining to methacrylic esters; andhydrolyzing the methacrylic esters in the presence of at least one heterogeneous catalyst, thereby obtaining methacrylic acid.2. (canceled)3. The process according to claim 1 , wherein the at least one heterogeneous catalyst is selected from the group consisting of a zeolite claim 1 , an ion exchange resin claim 1 , and an amorphous acid catalyst.4. The process according to claim 1 , wherein a flow through a catalyst bed is from bottom or from top.5. The process according to claim 1 , wherein said hydrolyzing occurs at a temperature of 50-200° C.6. The process according to claim 1 , wherein said hydrolyzing occurs at an elevated pressure.7. The process according to claim 1 , wherein a ratio of the methacrylic esters to water in said hydrolyzing is between 0.5 ad 5.8. The process according to claim 1 , wherein a residence time during said hydrolyzing is 10-120 min.9. The process according to claim 1 , wherein a mass or a volume ratio of circulation stream to feed stream is 5-50.10. The process according to claim 1 , wherein a methanol/methyl methacrylate mixture is supplied to during said esterifying.11. The process according to claim 1 , wherein said hydrolyzing occurs at a temperature of 70-150° C.12. The process according to claim 1 , wherein said hydrolyzing occurs at a temperature of 90-120° C.13. The process according to claim 1 , wherein said hydrolyzing occurs at a temperature of 100-110° C.14. The process according to claim 1 , wherein said hydrolyzing occurs at an elevated pressure of from 0.1 to 9 bar gauge.15. The process according to claim 1 , wherein said hydrolyzing occurs at an elevated pressure of from 2 to 4 bar ...

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Номер записи: 56
27-02-2014 дата публикации

POWDEROUS VITAMIN E FORMULATIONS

Номер: US20140056955A1
Автор: GADIENT Martin, KIRCHEN Stefanie, LINDEMANN Thomas, Schwaninger Mischa, Urban Kai, VOELKER Karl Manfred
Принадлежит: DSM IP ASSETS B.V.

The present invention relates to improved vitamin E formulations, as well as to the production of such formulations. 1. A powderous formulation comprising(i) at least 50 wt-%, based on the total weight of the powderous formulation, of vitamin E and/or vitamin E derivates, and(ii) 0.5 wt-%-8 wt-%, based on the total weight of the powderous formulation, of at least one auxiliary compound selected from the group consisting of aluminium ammonium sulphate, aluminium potassium sulfate, ammonium acetate, ammonium bisulphite, ammonium carbonate, ammonium chloride, ammonium dihydrogen phosphate, ammonium hydrogen carbonate, bentonite, montmorillonite, calcium aluminates, calcium carbonate, calcium silicate, synthetic calcium sulphate di-hydrate, calcium sulfate, kaolinitic clays (such as Kaolin), diatoma-ceous earth, perlite, potassium bisulphite, potassium hydrogen carbonate, potassium sulphate, potassium carbonate, sepiolitic clays, silicic acid, synthetic sodium aluminosilicate, sodium aluminosulfate, sodium bisulphate, sodium carbonate, sodium chloride, sodium hydrogen carbonate, sodium sulphate, vermiculite, calcium carbonate, magnesium carbonate, calcareous marine algae, magnesium oxide, magnesium sulphate, dicalcium phosphate, tri-calcium phosphate, mono-dicalcium phosphate, defluorinated rock-phosphate, monocalcium phosphate, calcium-magnesium phosphate, mono-ammonium phosphate, magnesium phosphate, sodium-calcium-magnesium phosphate, mono-sodium phosphate, glycerol, propylene glycol (E 1520), glyceryl triacetate (E1518), sorbitol (E420), polydextrose, lactic acid and urea, and(iii) at least 40 wt-%, based on the total weight of the powderous formulation, of a carrier material.2. A powderous formulation according to further comprising(iv) 0 to 5 wt-%, based on the total weight of the powderous formulation, of water.3. A powderous formulation according to claim 1 , wherein the carrier material is chosen from the group consisting of synthetically produced precipitated ...

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Номер записи: 57
27-02-2014 дата публикации

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

Номер: US20140058126A1
Автор: Caporale Andrea, De Lucchi Ottorino, Tartaggia Stefano
Принадлежит: F.I.S. - FABRICA ITALIANA SINTETICI S.P.A.

The present invention relates to a new process for the preparation of 2,4,5-trifluorophenylacetic acid and salts thereof by means of new synthetic intermediates. 2. Process according to the in which the steps (b) and (c) are carried out consecutively without the isolation of the compound of formula (IV).3. Process according to in which the steps (c) and (d) are carried out consecutively without the isolation of the compound of formula (II) and/or of the compound of formula (III).4. Process according to in which the steps (b) claim 1 , (c) and (d) are carried out consecutively without the isolation of the compound of formula (IV) claim 1 , (II) and/or of the compound of formula (III).6. Process according to claim 1 , in which in the compounds of formula (III) claim 1 , (IV) claim 1 , (V) claim 1 , (VI) and (VII) X is a chlorine atom.7. Process according to in which in the compounds of formula (V) and (VI) X′ is a chlorine atom.8. Process according to in which in the compounds of formula (II) and (III) R is Methyl or Ethyl.9. Process according to in which the step (a) is performed with PCl claim 1 , POClor PBr.10. Process according to in which the step (b) and/or the step (c) are carried out with KOH or an alkaline or earth alkaline C1-C5 linear or branched alkoxide.11. Process according to the in which the step (b) and/or the step (c) are carried out in presence of a linear or branched C1-C5 alcohol solvent.13. Compound according to the in which in the compounds of formula (III) claim 12 , (IV) claim 12 , (V) claim 12 , (VI) and (VII) X is a chlorine atom.14. Compound according to in which in the compounds of formula (V) and (VI) X′ is a chlorine atom.15. Compound according to in which in the compounds of formula (V) and (VI) both X and X′ are a chlorine atom.16. Use of the compounds according to for the preparation of the compound of formula (I) or salts thereof.17. Use of the compound of formula (I) or salts thereof prepared with the process according to for the ...

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Номер записи: 58
06-03-2014 дата публикации

Synthesis and novel salt forms of (r)-5-((e)-2-pyrrolidin-3ylvinyl)pyrimidine

Номер: US20140066460A1
Автор: Balwinder Singh Bhatti, Craig Harrison Miller, Gary Maurice Dull, Joseph Pike Mitchener, Julio A. Munoz, Pieter Albert Otten, Srinivasa Rao Akireddy, Timothy J. Cuthbertson
Принадлежит: Targacept Inc

The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.

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Номер записи: 59
20-03-2014 дата публикации

3,4-DIAMINOPYRIDINE TARTRATE AND PHOSPHATE, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Номер: US20140080875A1
Автор: GUYON Francois, HOURI Jean-Jacques, LE HOANG My Dung, PRADEAU Dominique
Принадлежит: Assistance Publique-Hopitaux De Paris

The invention relates to 3,4-diaminopyridine salts, pharmaceutical compositions containing at least one of said salts and uses thereof for the treatment of botulism, myasthenia, myasthenic syndromes or fatigue. 1. A stable salt of 3 ,4-diaminopyridine , selected from the group consisting of from 3 ,4-diaminopyridine tartrate and 3 ,4-diaminopyridine phosphate , wherein the salt is stable at 6 months when stored at 40 C and 73% relative humidity.2. A pharmaceutical composition , comprising , 3 ,4-diaminopyridine tartrate or phosphate and at least one pharmaceutically acceptable vehicle.3. The pharmaceutical composition as claimed in claim 2 , in the form of hard gelatin capsules claim 2 , of capsules claim 2 , of compressed tablets claim 2 , of oral suspensions claim 2 , of lozenges or of injectable solutions.4. The composition as claimed in wherein the amount of 3 claim 2 ,4-DAP tartrate or phosphate present corresponds to unit doses of between 5 mg and 20 mg claim 2 , expressed as weight of 3 claim 2 ,4-DAP in the free base form.5. The composition as claimed in claim 2 , comprising a pharmaceutically acceptable vehicle selected from the group consisting of antiagglomerating agents claim 2 , antioxidants claim 2 , dyes claim 2 , vitamins claim 2 , inorganic salts claim 2 , taste-modifying agents claim 2 , smoothing agents claim 2 , coating agents claim 2 , isolating agents and their mixtures.6. The composition as claimed in claim 2 , further comprising one or more additional active principles.7. A method of treating a condition claim 2 , comprising administering to a patient in need thereof claim 2 , an effective amount of the pharmaceutical composition of claim 2 , wherein said condition is one or more selected from the group consisting of botulism claim 2 , myasthenia claim 2 , myasthenic syndromes and fatigue related to a neurological pathology.8. The method of claim 7 , wherein the condition is multiple sclerosis or amyotrophic lateral sclerosis.9. The ...

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Номер записи: 60
27-03-2014 дата публикации

ULTRAVIOLET-SHIELDING AGENT, METHOD FOR PRODUCING THE SAME, ULTRAVIOLET-SHIELDING AGENT-CONTAINING DISPERSION LIQUID, AND COSMETIC PREPARATION

Номер: US20140086966A1
Автор: Matsushita Hirokazu
Принадлежит: Sumitomo Osaka Cement Co., Ltd.

The invention provides an ultraviolet-shielding agent including resin particles formed by coating a core portion with a coating layer, wherein the core portion is made of any one resin of an organic ultraviolet absorbent-containing resin and an inorganic particle-containing resin, and the coating layer is made of the other resin or both resins, a method for producing the same, an ultraviolet-shielding agent-containing dispersion liquid, and a cosmetic preparation. 1. Resin particles formed by coating a core portion with a coating layer ,wherein the core portion is made of any one resin of an organic ultraviolet absorbent-containing resin and an inorganic particle-containing resin, andthe coating layer is made of the other resin or both resins.2. The resin particles according to claim 1 ,wherein the core portion is made of the inorganic particle-containing resin, andthe coating layer is made of the organic ultraviolet absorbent-containing resin.3. The resin particles according to claim 1 ,wherein a refractive index of the inorganic particles is 1.9 or more.4. The resin particles according to claim 1 ,wherein the inorganic particles are metallic oxide particles.5. The resin particles according to claim 1 ,wherein the organic ultraviolet absorbent is at least one selected from the group consisting of dibenzoylmethane-based compounds, benzophenone derivatives, para-aminobenzoic acid derivatives, methoxycinnamic acid derivatives and salicylic acid derivatives.6. The resin particles according to claim 1 ,wherein an average particle diameter of the resin particles is 0.1 μm to 5 μm.7. The resin particles according to claim 1 ,wherein the core portion is made of an inorganic particle-containing resin, andthe core portion has a spherical shape with an average particle diameter of 0.05 μm to 5.0 μm.8. The resin particles according to claim 7 ,wherein the core portion has a spherical shape with an average particle diameter of 0.05 μm to 4.8 μm.9. The resin particles according ...

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Номер записи: 61
10-04-2014 дата публикации

FUNCTIONAL FOOD ADDITIVES

Номер: US20140100267A1
Автор: DUTTA Paresh
Принадлежит:

Novel compounds, and in particular to diacylglycerol (1, 3-DAG) and alpha-lipoic acid (LA) and/or dihydro-alpha-lipoic acid (DHLA) derivatives. In particular these novel compounds are used as functional food additives. These may for example be used as nutraceuticals and/or pharmaceuticals in the prevention and treatment of obesity, diabetes, atherosclerosis, oxidative stress and other lifestyle-related diseases. 2. The compound according to claim 1 , wherein the hydrocarbon chain has a length of 5 or more carbon atoms but with 21 carbon atoms or less.3. The compound according to claim 1 , wherein L is always the same if there is more than one L in the structure.4. A food additive comprising the compound according to .5. A nutraceutical comprising the compound according to .6. An anti-oxidant comprising the compound according to .7. An emulsifier for food comprising the compound according to .8. A stabilizer for food and pharmaceuticals comprising the compound according to .9. An agent for blocking food intake comprising the compound according to .11. A method of treating or inhibiting obesity and/or a disease or disease condition depending on an obesity status selected from the group consisting of diabetes claim 1 , atherosclerosis claim 1 , oxidative stress and other obesity-related diseases claim 1 , in a subject in need thereof claim 1 , comprising providing a composition comprising a molecule according to claim 1 , and administering a therapeutically effective amount of the composition to the subject. The present invention relates to functional food additives, and in particular to diacylglycerol (DAG) and alpha-lipoic acid (LA) and/or dihydro-alpha-lipoic acid (DHLA) derivatives. These may for example be used as nutraceuticals in the prevention and treatment of obesity, diabetes, atherosclerosis, oxidative stress and other lifestyle-related diseases.The term nutraceutical was introduced in the 1990's by Dr. Stephen De Feliceas: “A nutraceutical is any substance ...

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Номер записи: 62
10-04-2014 дата публикации

Injectable Formulation for Treatment and Protection of Patients Having an Inflammatory Reaction or an Ischemia-Reperfusion Event

Номер: US20140100278A1
Автор: Beck-Schimmer Beatrice, Herrmann Inge K., Limbach Ludwig K., Stark Wendelin J., Urner Martin
Принадлежит:

The present invention relates to compounds according to formula (I) for medical use. The compounds are particularly suitable for the treatment and/or prevention of a medical condition involving hypoxic, anoxic and/or inflamed mammalian tissue. Furthermore, the invention relates to the use of said compounds for preparing a medicament and to pharmaceutical preparations comprising such compounds. The invention also relates to methods of treating or protecting patients having or being prone to develop a medical condition involving hypoxic, anoxic and/or inflamed mammalian tissue, the methods comprising administration of a therapeutically effective amount of such compounds. 2. The method of claim 1 , wherein n is 1 to 3 claim 1 , m is 1 to 3 claim 1 , and Ris independently selected from the group consisting of —OH claim 1 , —NH claim 1 , and —COOH claim 1 , and Ris a Cto Calkyl.3. The method of claim 1 , wherein Ris a linear claim 1 , substituted or non-substituted Calkyl or a Calkyl.4. The method of claim 1 , wherein R2 is substituted with 1 to 3 substituents.5. The method of claim 1 , wherein the compound of formula (I) is selected from the group consisting of:1,1,1,3,3,3-Hexafluoro-2-methyl-2-propanol,2,2,3,4,4,4-Hexafluoro-1-butanol,Perfluoro-tert-butyl alcohol,2,2,3,3,3-Pentafluoro-1-propanol,1,1,1,3,3,4,4,4-Octafluoro-2-butanol,2,2,3,3,4,4,4-Heptafluoro-1-butanol,1,1,1,3,3,3-Hexafluoropropan-2-ol,3,4,4,4-Tetrafluoro-3-(trifluoromethyl)butan-1-ol,3-Amino-4,4,4-trifluorobutyric acid,3,3,3-Trifluoro-2-(hydroxymethyl)propanoic acid, and5,5,5-Trifluorleucine.6. The method of claim 1 , wherein the compound of formula (I) has an octanol-water partition coefficient of less than 20.7. The method of claim 1 , wherein the composition is a pharmaceutical composition formulated for inhalative administration.8. The method of claim 7 , wherein the administration is by inhalation.9. The method of claim 1 , wherein the administration is prior to claim 1 , after or concomitant with ...

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Номер записи: 63
07-01-2016 дата публикации

Phenylglyoxylic acid derivatives and their preparation and use

Номер: US20160002142A1
Автор: Dharma Rao Polisetti, Eugene Campian, Muralidhar Bondlela, Rajashaker Kache, Robert Carl Andrews, Santhosh Kalpathy, Thomas Scott Yokum
Принадлежит: vTvx Holdings I LLC

The invention provides novel phenylglyoxylic acid derivatives, which may be useful as intermediates for preparing stereoisomerically enriched drug compounds. The invention also provides methods of making phenylglyoxylic acid derivatives, and uses of phenylglyoxylic acid derivatives.

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Номер записи: 64
07-01-2016 дата публикации

SALT OF PYRROLIDIN-3-YL ACETIC ACID DERIVATIVE AND CRYSTALS THEREOF

Номер: US20160002165A1
Автор: Kushida Ikuo, Yoshida Kenshi
Принадлежит:

An organic carboxylic acid salt of 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl) piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid and a crystal thereof. 1. An organic carboxylic acid salt of 2-[(3S ,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid.2. The salt according to claim 1 , which is characterized by that the organic carboxylic acid is L-mandelic acid.3. (canceled)4. A crystal of the organic carboxylic acid salt of 2-[(3S claim 1 ,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl)piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid.5. The crystal according to claim 4 , which is characterized by that the organic carboxylic acid is L-mandelic acid.6. (canceled)7. The crystal according to claim 5 , which is characterized by having a diffraction peak at a diffraction angle (2θ±0.2°) of 7.2° in powder X-ray diffractometry.8. The crystal according to claim 7 , which is characterized by having further diffraction peaks at diffraction angles (2θ±0.2°) of 14.4° and 15.7° in powder X-ray diffractometry.9. The crystal according to claim 8 , which is characterized by having further diffraction peaks at diffraction angles (2θ±0.2°) of 10.3° and 23.5° in powder X-ray diffractometry.10. The crystal according to claim 9 , which is characterized by having further diffraction peaks at diffraction angles (2θ±0.2°) of 12.9° claim 9 , 14.9° claim 9 , 17.2° claim 9 , 20.10 and 24.7° in powder X-ray diffractometry.11. The crystal according to claim 5 , which is characterized by having peaks at chemical shifts (ppm) of 14.1 claim 5 , 52.9 claim 5 , 75.2 claim 5 , 144.7 and 174.0 in C solid state NMR spectrum.1215.-. (canceled) The present invention relates to a salt of a pyrrolidin-3-yl acetic acid derivative having an inhibitory action in a fractalkine-CX3CR1 pathway, and a crystal thereof ...

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Номер записи: 65
05-01-2017 дата публикации

PARTIALLY SATURATED TRICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20170001973A1
Автор: Cramp Susan M., Dyke Hazel J., Pallin Thomas D., Zahler Robert
Принадлежит:

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. This application is a continuation of U.S. patent application Ser. No. 14/116,023, filed Nov. 6, 2013, which is a national stage filing under U.S.C. §371 of PCT/US2012/036789, filed May 7, 2012, which claims priority to U.S. Provisional Patent Application 61/559,856, filed Nov. 15, 2011, and U.S. Provisional Patent Application 61/483,257, filed May 6, 2011, all of which are incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., diseases and other adverse health conditions associated with, exacerbated by, or precipitated by being overweight or obese. The estimated mortality from obesity-related conditions in the United States is over 300,000 annually (O'Brien et al. Amer J Surgery (2002) 184:4S-8S; and Hill et al. (1998) Science, 280:1371).There is no curative treatment for being overweight or obese. Traditional pharmacotherapies for treating an overweight or obese subject, such as serotonin and noradrenergic re-uptake inhibitors, noradrenergic re-uptake inhibitors, selective serotonin re-uptake inhibitors, intestinal lipase inhibitors, or surgeries such as stomach stapling or gastric banding, have been shown to provide minimal short-term benefits or significant rates of relapse, and ...

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Номер записи: 66
03-01-2019 дата публикации

COMPOSITIONS FOR IMPROVED PRODUCTION OF ACRYLIC ACID

Номер: US20190002385A1
Автор: Sherry Kyle Evan, Sookraj Sadesh H.
Принадлежит:

The present invention is directed to compositions which may undergo thermolysis to produce a higher purity acrylic acid product. In preferred embodiments of the present invention, the compositions comprise polypropiolactone and one or more active salts. The one or more active salts may catalyze thermolysis of the polypropiolactone so that the polymer depolymerizes into acrylic acid monomers. Certain concentrations of the one or more active salts result in higher purity acrylic acid products of thermolysis. In certain preferred embodiments, the one or more active salts include an acrylate group which may decompose under thermolysis to provide acrylic acid and thus decrease the concentration of undesirable contaminants in the acrylic acid product. In certain preferred embodiment, the one or more active salts comprise sodium acrylate. 1. A composition for producing a high purity acrylic acid thermolysis product , comprising:a. polypropiolactone; andb. one or more active salts for catalyzing thermolysis of said polypropiolactone when said composition undergoes thermolysis at thermolysis conditions.2. The composition of claim 1 , wherein a portion of said active salt is residual from a polymerization reaction producing said polypropiolactone.3. The composition of claim 1 , wherein said composition has a polypropiolactone concentration of at least 95% by weight.4. The composition of claim 1 , wherein said composition has polypropiolactone concentration of at least 98% by weight.5. The composition of claim 1 , wherein said polypropiolactone has a number average molecular weight between 750 g/mol and 10 claim 1 ,000 g/mol.6. The composition of claim 1 , wherein said polypropiolactone has a number average molecular weight of greater than 10 claim 1 ,000 g/mol.7. The composition of claim 1 , wherein said composition has a concentration of said one or more active salts of at least 0.01 by weight %8. The composition of claim 1 , wherein said composition has a concentration of ...

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Номер записи: 67
01-01-2015 дата публикации

Emollient Compounds Useful for Treating Dry Skin Conditions

Номер: US20150004139A1
Автор: Lewis Paige Mashara, Lewis Rodney David
Принадлежит:

The present invention provides a composition and method useful for creating a class of compounds that provide an emollient effect to the skin. The base formulation includes mixtures of certain oils that have high concentrations of Linoleic Acid, an essential fatty acid. Other oils are chosen which have high concentrations of Gamma-Linolenic Acid, Ricinoleic Acid and Oleic Acid. We have found that the incorporation of dl-alpha-tocopheryl and dl-alpha-tocopherol (vitamin E) improves the formulation and provides an anti-oxidative effect which preserves the end product and provides for a longer shelf life. The method disclosed creates free fatty acids, utilizing base catalyzed trans-esterification, inter-esterification and intra-esterification. The final products are lipid compounds which aid in treating dry skin conditions caused by deficiencies in Linoleic Acid or other fatty acids. 1. A lipid compound derived from blends of dl-alpha-tocopheryl , dl-alpha-tocopherol , a free fatty acid , and oils of varying concentrations containing the polyunsaturated fatty acids , linoleic acid , gamma-linolenic acid , ricinoleic acid , and oleic acid that are made freely available for use in skin formulations.21. The formulation of claim () that has been saponified.312. The formulation of any one of the claims ( , ) that has been acidified.4123. The formulation of any one of the claims ( , , ) that has been compounded with other substances to produce: soaps , cosmetics , lip balms , pharmaceuticals , emollients , skin creams , lotions.51234. The formulation of any one of the claims ( , , , ) that contains free fatty acids or fatty acid salts.61234. The formulation of any one of the claims ( , , , ) that may be incorporated with other compounds , including oils , water , cosmetic formulations , or pharmaceutical formulations.71. The formulation of claim () further comprising an additional component selected from additional oils , individual fatty acids and combinations thereof.87. ...

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Номер записи: 68
01-01-2015 дата публикации

CRYSTAL FORM OF PROSTAGLANDIN ANALOGUE, AND PREPARATION METHOD AND USE THEREOF

Номер: US20150005384A1
Автор: He Bingming, Ji Xiaoming, Liu Yubin, Tang Zhijun, YANG Jun
Принадлежит:

Provided are a crystal form A of a compound having the structure as represented by formula I, and preparation method and use thereof. The X-ray powder diffraction (XRPD) chart of the crystal form A has characteristic peaks at the following diffraction angles: 2.9±0.2°, 13.6±0.2°, 17.3±0.2° and 18.6±0.2°. 2. The crystalline form A of the compound according to claim 1 , wherein said crystalline form A may has other characteristic peak at the following 2θ angle in the X-ray powder diffraction pattern: 21.8±0.2°.3. The crystalline form A of the compound according to or claim 1 , wherein the maximum peak in the differential scanning calorimetry (DSC) for said crystalline form A exists at 123° C.-128° C.; and preferably claim 1 , at 125° C.4. The crystalline form A of the compound according to claim 3 , wherein the differential scanning calorimetry (DSC) for said crystalline form A is shown as in .54. The crystalline form A of the compound according to any one of - claims 1 , wherein Infrared Spectrum of said crystalline form A is shown in .65. A preparation method for crystalline form A of compound I according to any one of - claims 1 , comprising the following steps:(1) the crude compound of formula I is mixed with one or more solvents selected from following solvent 1 to obtain solution 1: methanol, acetonitrile, ethyl acetate, methyl acetate, isopropyl acetate, and t-butyl acetate;{'claim-ref': {'@idref': 'CLM-00001', 'claims 1'}, 'b': '5', '(2) solution 1 is stirred and cooled, or solvent 2 is added to give the crystalline form A of compound I according to any one of -, wherein said solvent 2 is selected from one or more of the following: water, and C5-C8 alkane.'}7. The preparation method according to claim 6 , wherein claim 6 , in step (1) claim 6 , the temperature for mixing is at 0-80° C.; preferably claim 6 , at 20-50° C.; more preferably claim 6 , at 30-50° C.8. The preparation method according to claim 6 , wherein claim 6 , in step (1) claim 6 , the weight to ...

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Номер записи: 69
01-01-2015 дата публикации

Method of treating non-alcoholic fatty liver disease and steatohepatitis

Номер: US20150005385A1
Автор: Kazuko Matsuda
Принадлежит: Medicinova Inc

A compound of Formula (I): or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X 1 and X 2 are as defined herein, is useful for treating non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

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Номер записи: 70
01-01-2015 дата публикации

INTERMEDIATES FOR THE PREPARATION OF LUBIPROSTONE

Номер: US20150005528A1
Автор: Chen Yung-Fa, Henschke Julian Paul, Liu Yuanlian, Xia Lizhen
Принадлежит:

Intermediates of the following formulae for the preparation of lubiprostone: This application is a divisional of U.S. patent application Ser. No. 13/876,418 which was filed with the U.S. Patent and Trademark Office on Mar. 27, 2013 as a U.S. national stage of application No. PCT/CN2010/001614, filed on Nov. 16, 2010, the content of which is incorporated here by reference.1. Field of the InventionThe present invention provides novel intermediates for making lubiprostone.2. Description of the Related ArtLubiprostone, 7-[(1R,3R,6R,7R)-3-(1,1-difluoropentyl)-3-hydroxy-8-oxo-2-oxabicyclo[4.3.0]non-7-yl]heptanoic acid, is the active pharmaceutical ingredient (API; drug substance) in the drug product Amitiza®, a gastrointestinal agent used for the treatment of Chronic Idiopathic Constipation in adults. It is marketed by Sucampo Pharmaceuticals, Inc. and was approved by the United States Food and Drug Administration (FDA) on Jan. 31, 2006. It is also approved by FDA to treat Irritable Bowel Syndrome with constipation (ISB-C) in adult women aged 18 and over on Apr. 29, 2008. Amitiza® is also being clinically tested for other gastrointestinal disorders. Lubiprostone is a bicyclic 13,14-dihydro-15-keto-16,16-difluoro-prostaglandin E1 derivative (a.k.a., a so-called 13,14-dihydro-15-keto-prostaglandin derivative). Prostaglandins possess the prostanoic acid backbone which is a C20 fatty acid ().The existence of an electron deficient ketone at C15, along with a conveniently positioned hydroxyl group at C11 results in lubiprostone existing predominantly in a bicyclic form that includes a 6-membered hemiketal ring. This form exists in equilibrium with a monocyclic form (Scheme 1). Taken together, these two forms are referred to as tautomeric isomers. In sugar chemistry this kind of equilibrium of cyclic and acyclic forms is referred to as ring-chain tautomerisation (R-CT).Whereas in DO, the ratio of the bicyclic form to monocyclic form is 6:1, in CDClit is 96:4.Despite this ...

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Номер записи: 71
14-01-2016 дата публикации

3'-substituted-abscisic acid derivatives

Номер: US20160007598A1
Автор: Daniel Heiman, Eiki Nagano, Gary T. Wang, Gregory D. Venburg, Joseph H. LUSTIG, Marci SURPIN
Принадлежит: Valent BioSciences LLC

The invention relates to a novel class of (S)-3′-substituted-abscisic acid derivatives and (±)-3′-substituted-abscisic acid derivatives, and methods of synthesizing the derivatives.

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Номер записи: 72
12-01-2017 дата публикации

PERSONALIZING SUBSTANCE FOR APPLICATION TO THE SKIN OR ADDITION TO TATTOO INK AND METHODS OF PREPARATION THEREOF

Номер: US20170007524A1
Автор: Duffy, Freebery Sherry, Jorgensen Ellen, JR. Patrick
Принадлежит:

Compositions for delivering personalizing substances, such as a biological material, sand, soil, metal, water, sea water, holy water, synthetic or biological polymers, ceramics, animal or plant tissue, or another physiologically compatible component having personal significance to an individual are described herein. The compositions include the personalizing substance in combination with a pharmaceutically acceptable carrier for injection, such as tattoo ink. Also disclosed are methods for administering a personalizing substance to a recipient. In some embodiments, the personalizing substance is added to a tattoo ink and incorporated in a tattoo created on an individual's skin. 1. A composition comprising a personalizing substance wherein the personalizing substance is not encapsulated in a polymeric nano- or microparticle , and a carrier suitable for injection into the skin.2. The composition of claim 1 , wherein the carrier is tattoo ink.3. The composition of claim 1 , wherein the personalizing substance is in the form of nanoparticles.4. The composition of claim 1 , wherein the personalizing substance is selected from the group consisting of isolated DNA claim 1 , sand claim 1 , soil claim 1 , metal claim 1 , ceramics claim 1 , and plant tissue.5. The composition of claim 4 , wherein the personalizing substance is isolated DNA and wherein the DNA further comprises a personal identification characteristic selected from the group consisting of short tandem repeats (STRs) claim 4 , single nucleotide polymorphisms (SNPs) claim 4 , epigenetic markers claim 4 , and methylated DNA patterns.6. The composition of claim 4 , wherein the personalizing substance is isolated DNA.7. The composition of claim 1 , wherein the carrier comprises alcohol and water.8. The composition of claim 7 , wherein the carrier comprises alcohol in a range from 5% to about 30% (w/w) claim 7 , and the amount of water in the carrier ranges from about 40% to about 70% (w/w).9. The composition of ...

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Номер записи: 73
08-01-2015 дата публикации

Methods of Treating Amyotrophic Lateral Sclerosis

Номер: US20150010549A1
Автор: Gjorstrup Per
Принадлежит: ANIDA PHARMA INC.

The present invention relates to use of DHA analogs and their pharmaceutical compositions for treating ALS, by administering these compounds or pharmaceutical compositions to subjects in need thereof. 2. The method of wherein said compound of Formula I claim 1 , II claim 1 , III claim 1 , or IV claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , metabolite claim 1 , analog or derivative thereof is in combination with a pharmaceutically acceptable excipient.3. The method of wherein treating ALS comprises alleviating at least one symptom of ALS.4. The method of claim 3 , wherein the symptom of ALS is selected from: twitching claim 3 , cramping or stiffness of muscles; muscle weakness affecting an arm of a leg; muscle atrophy; slurred and nasal speech; shortness of breath; and difficulty chewing claim 3 , swallowing or breathing.5. The method of claim 1 , wherein treating ALS comprises prolonging or increasing the survival of the subject suffering from ALS.6. The method of claim 1 , wherein treating ALS comprises reducing cell death or increasing cell survival of a cell from the subject suffering from ALS.7. The method of claim 6 , wherein the cell is a motor neuron or an astrocyte.8. The method of claim 1 , wherein the compound is any one of the compounds listed in Table 1.9. The method of claim 1 , wherein the compound is sodium (4Z claim 1 ,7Z claim 1 ,10R claim 1 ,11E claim 1 ,13E claim 1 ,15Z claim 1 ,17S claim 1 ,19Z)-10 claim 1 ,17-dihydroxydocosa-4 claim 1 ,7 claim 1 ,11 claim 1 ,13 claim 1 ,15 claim 1 ,19-hexaenoate or (4Z claim 1 ,7Z claim 1 ,10R claim 1 ,11E claim 1 ,13E claim 1 ,15Z claim 1 ,17S claim 1 ,19Z)-10 claim 1 ,17-dihydroxydocosa-4 claim 1 ,7 claim 1 ,11 claim 1 ,13 claim 1 ,15 claim 1 ,19-hexaenoic acid.10. The method of claim 1 , further comprising administering at least one second active therapeutic agent.11. The method of claim 10 , wherein the second active ...

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Номер записи: 74
12-01-2017 дата публикации

IONIC LIQUIDS

Номер: US20170009172A1
Автор: Bender Holger, Denzer Horst, Houdkamp Rob, Myrdek Thomas, Van Der Veen Reinout
Принадлежит: Kao Chemicals GmbH

The present invention relates to novel ionic liquids comprising polyethercarboxylate groups as anions, alkyl ammonium groups as cations, a process of preparation of said ionic liquids and its use in high duty lubricant. 2. The ionic liquid according to claim 1 , characterized in that the anion Y is an ether carboxylate anion of formula (II) claim 1 , wherein the alkenyl has up to 3 double bonds.3. The ionic liquid according to wherein Rhas 8 to 18 carbon atoms.4. The ionic liquid according to wherein P consists of{'sub': 2', '2', '2', '2, 'n units of —CHCHO— and m units of —CHCHRO— or —CHRCHO—, wherein n represents a number from 2 to 6, m represents a number from 0 to 3, and the sum of n+m represents the average alkoxylation degree which corresponds to a number from 2 to 9.'}5. An ionic liquid according to claim 1 , characterized in that the cation X is an alkyl ammonium cation of formula (III) claim 1 , wherein{'sub': '2', 'Rrepresents a linear or branched alkyl, a linear alkenyl or a linear alkynyl group having 10 to 18 carbon atoms,'}{'sub': '3', 'Rrepresents a methyl group,'}{'sub': '4', 'Rrepresents a methyl group.'}6. The ionic liquid according to claim 1 , characterized in that the cation X is an alkyl ammonium cation of formula (III) claim 1 , wherein{'sub': '2', 'Rrepresents a linear or branched alkyl, a linear alkenyl or a linear alkynyl group having 10 to 18 carbon atoms,'}{'sub': '3', 'Rrepresents a linear or branched alkyl group having 1 to 5 carbon atoms, preferably a methyl group,'}{'sub': '4', 'Rrepresents a linear or branched alkyl, a linear alkenyl or a linear alkynyl group having 10 to 18 carbon atoms.'}7. The ionic liquid according to wherein the anion Y is at least one selected from Laureth-3 carboxylate claim 1 , Laureth-4 carboxylate claim 1 , Laureth-5 carboxylate claim 1 , Laureth-6 carboxylate and Capryleth-6 carboxylate.8. The ionic liquid according to wherein the cation X is at least one selected from dodecyldimethyl ammonium and ...

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Номер записи: 75
14-01-2016 дата публикации

FLUORINATED ETHER COMPOUND, FLUORINATED ETHER COMPOSITION, AND COATING LIQUID, AS WELL AS SUBSTRATE HAVING SURFACE LAYER, AND METHOD FOR ITS PRODUCTION

Номер: US20160009929A1
Автор: HOSHINO Taiki, OTOZAWA Nobuyuki
Принадлежит: Asahi Glass Company, Limited

To provide a fluorinated ether compound, a fluorinated ether composition and a coating liquid, capable of forming a surface layer which has high initial water/oil repellency and which is excellent in abrasion resistance, fingerprint stain removability, lubricity and uniformity, as well as a substrate having such a surface layer, and a method for its production. A substrate having a surface layer formed of a fluorinated ether compound represented by D-R—O—CH—(CFO)-A (Dis CF— or CF—O—; Ris a Cfluoroalkylene group containing at least one hydrogen atom, etc.; m is 1 to 6; n is 1 to 200; A is —CF—B—CH—SiLR; B is —CHO—, —CHO—C(═O)NH—, etc.; L is a hydrolysable group; R is a monovalent hydrocarbon group, etc.; a is 1 to 5; b is 1 to 10; c is 1 to 3; g is 1 to 5; and h is 1 to 5) or a fluorinated ether composition containing the compound; and a method for its production. 2. The fluorinated ether compound according to claim 1 , wherein —CH—(CFO)is —CHCF—O{(CFO)(CFCFO)}(wherein n1 is an integer of at least 1 claim 1 , n2 is an integer of at least 1 claim 1 , n1+n2 is an integer of from 2 to 200 claim 1 , and the bond order of n1 CFO and n2 CFCFO is not limited).4. The fluorinated ether compound according to claim 1 , which has a number average molecular weight of from 2 claim 1 ,000 to 10 claim 1 ,000.5. A fluorinated ether composition comprising the fluorinated ether compound as defined in claim 1 , and a fluorinated ether compound other than the fluorinated ether compound represented by the above formula (1).6. The fluorinated ether composition according to claim 5 , wherein the content of the fluorinated ether compound represented by the above formula (1) is at least 70 mass % in the fluorinated ether composition (100 mass %).9. The fluorinated ether composition according to claim 7 , wherein the total content of the fluorinated ether compound represented by the above formula (1) and the fluorinated ether compound represented by the above formula (2) is at least 80 mass % ...

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Номер записи: 76
09-01-2020 дата публикации

POROUS CHIRAL MATERIALS AND USES THEREOF

Номер: US20200009531A1
Автор: Cheng Peng, Shi Wei, YAN Xiu-Ping, YANG Cheng-Xiong, Zaworotko Michael J., ZHANG Shi-Yuan
Принадлежит:

A porous chiral material of formula [M(L)(A)]Xwherein M is a metal ion; L is a nitrogen-containing bidentate ligand; A is the anion of mandelic acid or a related acid; and Xis an anion 1. A porous chiral material of formula [M(L)(A)]X wherein M is a metal ion; L is a nitrogen-containing bidentate ligand; A is the anion of mandelic acid or a related acid; and X is an anion.2. A porous chiral material according to wherein M is selected from a group consisting of: cobalt claim 1 , chromium claim 1 , iron claim 1 , nickel claim 1 , manganese claim 1 , calcium claim 1 , magnesium claim 1 , cadmium claim 1 , copper and zinc.3. A porous chiral material according to wherein L is selected from a group consisting of: 4 claim 1 ,4′-bipyridine claim 1 , 1 claim 1 ,2-bis(4-pyridyl)ethane claim 1 , and 4 claim 1 ,4′-bipyridylacetylene.4. A porous chiral material according to wherein A is the anion of (S)-(−)-mandelic acid.5. A porous chiral material according to wherein X is a triflate ion.6. (canceled)7. A material of formula [M(L)(A)]XGwherein M is a metal ion; L is a nitrogen-containing bidentate ligand; A is an anion of mandelic acid or a related acid; X is an organic anion; G is a guest molecule; and n is from 0 to 5.8. (canceled)9. A crystalline sponge comprising a porous chiral material of formula [M(L)(A)]X.10. A method of separating enantiomers claim 1 , the method comprising contacting a composition comprising a mixture of enantiomers with a material of .11. (canceled)12. A method of separating enantiomers according to claim 10 , the method comprising passing a composition comprising the mixture of enantiomers through a chromatography column comprising as a stationary phase a chiral porous material of formula [M(L)(A)]X wherein M is a metal ion; L is a nitrogen-containing bidentate ligand; A is an anion of mandelic acid or a related acid; and X is an anion.13. A method of separating enantiomers according to claim 12 , the method comprising:{'sub': '1.5', 'sup': +', '−, ...

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Номер записи: 77
08-01-2015 дата публикации

4-ALKANOYLAMINO-3-PYRAZOLONE DERIVATIVE

Номер: US20150011552A1
Автор: Fukuda Takeshi, Sakamoto Atsunobu, TANAKA Naoki
Принадлежит:

The present invention provides a compound which enhances the production of erythropoietin. The present invention provides, for example, a compound represented by the formula (1) wherein R: -Q, -Q-X-Q, or -Q-X-Q-Y-Q: a monocyclic or bicyclic aromatic heterocyclic group; Q, Q: an aromatic hydrocarbon ring group or a monocyclic aromatic heterocyclic group; X: —CONH—, —CONHCH—, —CHOCH—, —NHCHCH—, or the like; Y: a single bond, —O—, —(CH)—, or —O—(CH)—; m, n: an integer from 1 to 3; R: H or an alkyl group; and R: H, an alkoxycarbonyl group, a carboxy group, an aromatic hydrocarbon ring group, or a monocyclic aromatic heterocyclic group. 2. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein Ris a hydrogen atom or a methyl group.3. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein Ris a hydrogen atom claim 1 , a methoxycarbonyl group claim 1 , an ethoxycarbonyl group claim 1 , a propoxycarbonyl group claim 1 , a tert-butoxycarbonyl group claim 1 , a carboxy group claim 1 , a phenyl group claim 1 , or a pyridyl group.4. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein Ris a hydrogen atom claim 1 , a tert-butoxycarbonyl group claim 1 , or a carboxy group.5. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein Ris a hydrogen atom.6. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein m is 1 or 2.7. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein{'sup': 1', '1, 'Ris a group represented by -Q, and'}{'sup': '1', 'Qis a pyridyl group, a pyrimidinyl group, a pyrazinyl group, a pyridazinyl group, a quinolyl group, an isoquinolyl group, or a quinazolinyl group which may have 1 or 2 substituents independently selected from substituent group α.'}8. A compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein{'sup': 1', '1, 'Ris a ...

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Номер записи: 78
14-01-2021 дата публикации

QUINONES HAVING HIGH CAPACITY RETENTION FOR USE AS ELECTROLYTES IN AQUEOUS REDOX FLOW BATTERIES

Номер: US20210009497A1
Автор: Aziz Michael J., Gordon Roy G., Ji Yunlong, KWABI David Gator, Lin Kaixiang
Принадлежит:

We disclose quinone compounds and related species (Formula I) that possess significant advantages when used as a redox active material in a battery, e.g., a redox flow battery. In particular, the compounds provide redox flow batteries (RFBs) with extremely high capacity retention. For example, RFBs of the invention can be cycled for 500 times with negligible loss of capacity, and such batteries could be employed for years of service. Thus, the invention provides a high efficiency, long cycle life redox flow battery with reasonable power cost, low energy cost, and all the energy scaling advantages of a flow battery. 2. The battery of claim 1 , wherein Xand Xare O.3. The battery of or claim 1 , wherein each of R-Ris independently H; halo; optionally substituted Calkyl; —X-L-C(O)O—Y; or —X-L-C(O)O—Y.4. The battery of any one of - claim 1 , wherein Ris —X-L-C(O)O—Yand Ris —X-L-C(O)O—Y.5. The battery of any one of - claim 1 , wherein Yand Yare H.6. The battery of claim 1 , wherein Xand Xare O.7. The battery of claim 6 , wherein each of R-Ris independently H; halo; optionally substituted Calkyl; —X-L-P(═O)(OY); or —X-L-P(═O)(OY).8. The battery of or claim 6 , wherein Ris —X-L-P(═O)(OY)and Ris —X-L-P(═O)(OY).9. The battery of any one of - claim 6 , wherein Yand Yare H.16. The battery of any one of - claim 6 , wherein the second redox active material is the hydroquinone of formula I claim 6 , which is oxidized to the corresponding quinone during discharge.17. The battery of any one of - claim 6 , wherein the pH of the second aqueous electrolyte is 7.18. The battery of claim 17 , wherein the pH is from 8 to 13.19. The battery of any one of - claim 17 , wherein the first redox active material comprises bromine claim 17 , chlorine claim 17 , iodine claim 17 , oxygen claim 17 , vanadium claim 17 , chromium claim 17 , cobalt claim 17 , iron claim 17 , aluminum claim 17 , manganese claim 17 , cobalt claim 17 , nickel claim 17 , copper claim 17 , or lead.21. The compound of claim ...

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Номер записи: 79
08-01-2015 дата публикации

CRYSTAL FORM OF PROSTAGLANDIN ANALOGUE, AND PREPARATION METHOD AND USE THEREOF

Номер: US20150011637A1
Автор: He Bingming, Ji Xiaoming, Liu Yubin, Tang Zhijun, YANG Jun
Принадлежит:

Provided are a crystal form B of a compound having the structure as represented by formula I, and preparation method and use thereof. The X-ray powder diffraction (XRPD) chart of the crystal form B has characteristic peaks at the following diffraction angles: 2.9±0.2°, 6.5±0.2°, 12.6±0.2°, 13.1±0.2° and 20.6±0.2°. 2. The crystalline form B of the compound according to claim 1 , wherein said crystalline form B may has other characteristic peaks at the following 2θ angles in the X-ray powder diffraction pattern: 5.3+0.2° claim 1 , 10.64+0.2° claim 1 , 12.1+0.2° claim 1 , 18.7+0.2° claim 1 , 21.3+0.2° and 25.2+0.2°.3. The crystalline form B of the compound according to or claim 1 , wherein the maximum peak in the differential scanning calorimetry (DSC) for said crystalline form B exists at 123° C. −128° C.4. The crystalline form B of the compound according to claim 3 , wherein the maximum peak in the differential scanning calorimetry (DSC) for said crystalline form B is at 125° C.5. The crystalline form B of the compound according to claim 4 , wherein the differential scanning calorimetry (DSC) for said crystalline form B is shown as in .6. The crystalline form B of the compound according to or claim 4 , wherein Infrared Spectrum of said crystalline form B is shown in .76. A preparation method for crystalline form B of compound I according to any one of - claims 1 , comprising the following steps:(1) the crude compound of formula I is mixed with solvent 1 to obtain solution 1; and solvent 1 is selected from one or more of the following: acetone, isopropanol, n-propanol, and tetrahydrofuran;(2) solution 1 is cooled and stirred to give crystalline form B of compound 1.86. A preparation method for crystalline form B of compound I according to any one of - claims 1 , comprising the following steps:(1) the crude compound of formula I is mixed with solvent 1 to obtain solution 1; and solvent 1 is selected from one or more of the following: acetone, isopropanol, n-propanol, ...

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Номер записи: 80
10-01-2019 дата публикации

Salt of Quinolone Compound, Polymorphs thereof, Preparation Method therefor, Composition, and Applications

Номер: US20190010160A1
Автор: Bai Rui, Chen Na, Fan Yi, Hao Yu, LI Gongsheng, LIU Zhenying, Wang Yuji, YU Jianxin, Zhang Jing, ZHANG Leduo, ZHAO Fei
Принадлежит:

Disclosed is a salt of a quinoline derivative, polymorphic forms thereof, preparation methods thereof, a composition, and applications. The SPH1772 ditartrate or crystal form A thereof expresses the following excellent properties: high stability, great bioavailability, excellent pharmacokinetic properties, and better in vivo efficacy than SPH1772 free base. 2. The quinoline compound SPH1772 ditartrate according to claim 1 , wherein the tartaric acid is L-tartaric acid.3. A crystal form A of the quinoline compound SPH1772 ditartrate according to claim 1 , having an X-ray powder diffraction pattern represented by diffraction angle 2θ comprising characteristic peaks at 7.5±0.2° claim 1 , 9.2±0.2° claim 1 , 14.5±0.2° claim 1 , 16.6±0.2° claim 1 , 20.3±0.2° and 28.8±0.2°; the target used in the X-ray powder diffraction is Cu target.4. The crystal form A of the quinoline compound SPH1772 ditartrate according to claim 3 , wherein the melting point of the crystal form A of SPH1772 ditartrate is 202° C. claim 3 , and/or claim 3 , the DSC of the crystal form A of SPH1772 ditartrate has a main endothermic peak at 199.4° C.5. A preparation method for the crystal form A of the quinoline compound SPH1772 ditartrate according to claim 3 , comprising that in an organic solvent claim 3 , the compound SPH1772 reacts with tartaric acid; wherein the organic solvent is an alcoholic solvent claim 3 , ester solvent claim 3 , DCM:MeOH=6:1 to 9:1 v/v claim 3 , ether solvent or ketone solvent.6. The preparation method according to claim 5 , wherein the alcoholic solvent is methanol;and/or, the ester solvent is ethyl acetate;and/or, the ether solvent is tetrahydrofuran;and/or, the ketone solvent is acetone;and/or, the volume/mass ratio of the organic solvent to the SPH1772 is 40 mL/g to 80 mL/g;and/or, the molar ratio of SPH1772 to the tartaric acid is 1:2.0 to 1:2.2;and/or, the reaction temperature is 40 to 60° C.;and/or, the reaction time is 24 h to 72 h;and/or, the preparation method for ...

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Номер записи: 81
09-01-2020 дата публикации

PROCESSES FOR PREPARING PARTIALLY FLUORINATED EPOXIDES AND PERFLUORINATED EPOXIDES AND COMPOSITIONS RELATED THERETO

Номер: US20200010439A1
Автор: Brandt Drew Richard, PETROV VIACHESLAV A
Принадлежит: THE CHEMOURS COMPANY FC, LLC

This application relates to the preparation of partially fluorinated epoxides and perfluorinated epoxides which may be useful in various applications including refrigerants, heat transfer media, high-temperature heat pumps, organic Rankine cycles, fire extinguishing/fire suppression, propellants, foam blowing, solvents, gaseous dielectrics, and/or cleaning fluids. Compositions comprising the fluorinated epoxide compounds are also provided. 2. (canceled)3. (canceled)4. The process of claim 1 , wherein Rand Rare each independently H or F; and Rand Rare each independently selected from partially fluorinated or perfluorinated Calkyl.5. The process of claim 1 , wherein the hypohalite salt is selected from NaOCl claim 1 , KOCl claim 1 , NaOBr claim 1 , and Ca(OCl).6. (canceled)7. The process of claim 1 , wherein the cationic phase transfer catalyst is a quaternary ammonium salt or a quaternary phosphonium salt.8. (canceled)9. The process of claim 1 , the cationic phase transfer catalyst has formula (R)(R)(R)(R)NX or (R)(R)(R)(R)PX claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from Calkyl claim 1 , Ccycloalkyl claim 1 , 4-14 membered heterocycloalkyl claim 1 , Caryl claim 1 , 5-14 membered heteroaryl claim 1 , Ccycloalkyl-Calkylene claim 1 , 4-14 membered heterocycloalkyl-Calkylene claim 1 , Cmembered aryl-Calkylene claim 1 , and 5-14 membered heteroaryl-Calkylene claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 groups independently selected from OH claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Cfluoroalkyl claim 1 , di-(Calkyl)amino claim 1 , Ccycloalkyl claim 1 , 4-14 membered heterocycloalkyl claim 1 , Cmembered aryl claim 1 , and 5-14 membered heteroaryl; and X is an anion.10. The process of claim 1 , wherein the cationic phase transfer catalyst has formula (R)(R)(R)(R)NX claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare eah independently selected ...

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Номер записи: 82
14-01-2021 дата публикации

LINKER OF BIOPROBES

Номер: US20210011012A1
Автор: CHEN YU-CHE, LI CHING-WEN
Принадлежит:

A linker of bioprobes, suitable for immobilizing a bioprobe on a chip substrate of a sensor, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is greater than 250 nm, coverage of the linker on the chip substrate is 40%-80%. A further linker of bioprobes, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of less than 6, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is less than 250 nm, coverage of the linker on the chip substrate is 65%-100%. The optimal carbon chain length of the linker and the coverage are realized for substrates of various roughnesses, and grasping ability of an electrochemical sensor chip for a detected object are enhanced. 1. A linker of bioprobes , suitable for immobilizing a bioprobe on a chip substrate of a sensor , comprising:SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1,wherein when an average surface roughness (Ra) of the chip substrate is greater than 250 nm, a coverage of the linker on the chip substrate is in a range of 40% to 80%.2. The linker of bioprobes according to claim 1 , wherein a material of the chip substrate of the sensor is silicon claim 1 , glass claim 1 , graphene claim 1 , gold claim 1 , platinum or polymers.3. The linker of bioprobes according to claim 1 , wherein the chip substrate is subjected to surface treatment according to a proportion of 1 part of 98 wt % sulfuric acid and 3 parts of 33 wt % hydrogen peroxide claim 1 , and a specific roughness is obtained by different treatment time.4. The linker of bioprobes according to claim 1 , further comprising: soaking the chip substrate into a solution of a linker dissolved in 99.8 ...

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Номер записи: 83
18-01-2018 дата публикации

MODULATORS OF ALPHA-DICARBONYL DETOXIFICATION AND THEIR USE FOR THE TREATMENT OF DIABETIC PATHOLOGIES

Номер: US20180015051A1
Автор: BOSE NEELANJAN, CHAUDHURI JYOTISKA, KAPAHI PANKAJ
Принадлежит:

In various embodiments compositions and methods are provided for ameliorating a pathology characterized by elevated α-dicarbonyl compounds or prophylactically slowing or stopping the onset of said pathology in a mammal. In certain embodiments the method comprises administering to the mammal an agent that activates TRPA1 in an amount sufficient to activate TRPA1, and/or to ameliorate one or more symptoms of the pathology (e.g., diabetes or a complication thereof), and/or to slow or stop the onset of the pathology, and/or to lower the level of α-dicarbonyl compounds in the mammal. 1. A method for the treatment or prophylaxis of diabetes in a mammal , said method comprising:administering to a mammal identified as having diabetes or pre-diabetes an agent that activates TRPA1 in an amount sufficient to ameliorate one or more symptoms of diabetes or pre-diabetes.2. The method of claim 1 , wherein said amount sufficient to ameliorate one or more symptoms of diabetes or pre-diabetes is an amount sufficient to ameliorate a complication of diabetes selected from the group consisting of diabetic neuropathy claim 1 , cardiomyopathy claim 1 , nephropathy claim 1 , retinopathy claim 1 , microvascular damage claim 1 , and early mortality.3. A method of ameliorating a pathology characterized by elevated α-dicarbonyl compounds and advanced glycation endproducts or prophylactically slowing or stopping the onset of said pathology in a mammal claim 1 , said method comprising:administering to said mammal an agent that activates TRPA1 in an amount sufficient to activate TRPA1 and/or to ameliorate one or more symptoms of said pathology, and/or to slow or stop the onset of said pathology, and/or to lower the level of dicarbonyl compounds in said mammal.4. The method of claim 3 , wherein said pathology is selected from the group consisting of Diabetes claim 3 , Alzheimer's disease claim 3 , Parkinson's disease claim 3 , ATTR amyloidosis claim 3 , cataract formation claim 3 , stroke claim 3 ...

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Номер записи: 84
21-01-2016 дата публикации

ACRYLIC ACID PRODUCTION METHODS

Номер: US20160016876A1
Автор: MAHONEY James E.
Принадлежит:

In one aspect, the present invention encompasses safe and efficient methods for providing highly pure acrylic acid. In certain embodiments, the inventive methods include the step of producing polypropiolactone from ethylene oxide at a first location, transporting the polymer to a second location and pyrolyzing the polypropiolactone to provide glacial acrylic acid. In certain embodiments, the step of pyrolyzing the polymer is performed continuously in conjunction with a polymerization process to make SAPs.

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Номер записи: 85
21-01-2016 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20160016883A1
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: 1. A compound selected from the group consisting of travoprost free acid substantially free of 5 ,6-trans isomer , latanoprost free acid substantially free of 5 ,6-trans isomer , bimatoprost free acid substantially free of 5 ,6-trans isomer , tafluprost free acid substantially free of 5 ,6-trans isomer , fluprostenol substantially free of 5 ,6-trans isomer , cloprostenol substantially free of 5 ,6-trans isomer , and unoprostone substantially free of 5 ,6-trans isomer.2. A compound according to containing less than 0.1% of 5 claim 1 ,6-trans isomer.4. Latanoprost according to containing less than 0.2% of 5 claim 3 ,6-trans isomer.5. Latanoprost according to containing less than 0.1% of 5 claim 3 ,6-trans isomer7. Travoprost according to containing less than 0.2% of 5 claim 6 ,6-trans isomer.8. Travoprost according to containing less than 0.1% of 5 claim 6 ,6-trans isomer10. Tafluprost according to having a purity of greater than 99.8%.11. Tafluprost according to having a purity of greater than 99.9%.12. Unoprostone Isopropyl ester having a purity of greater than 99.5%.13. Unoprostone Isopropyl ester having a purity of greater than 99.7%.14. Unoprostone Isopropyl ester having a purity of greater than 99.9%. This application is a Divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013, the content of which is 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, Isopropyl unoprostone, Isopropyl cloprostenol, ...

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Номер записи: 86
21-01-2016 дата публикации

NEW TETRAKIS(ETHER-SUBSTITUTED FORMYLPHENYL)

Номер: US20160016884A1
Автор: IWAI Tatsuya, YOSHITOMO Akira
Принадлежит:

A tetrakis(ether-substituted formylphenyl) expressed by General Formula (1):

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Номер записи: 87
18-01-2018 дата публикации

PROCESS FOR PRODUCTION OF ACRYLIC ACID

Номер: US20180016219A1
Автор: Farmer Jay J., GALEBACH Peter, SHERRY Kyle, Sookraj Sadesh H.
Принадлежит: NOVOMER, INC.

Provided are integrated processes for the conversion of beta propiolactone to acrylic acid. Systems for the production of acrylic acid are also provided. 1. A method for producing acrylic acid , comprising:(a) providing a feedstock stream comprising beta propiolactone;(b) directing the feedstock stream to a reaction zone;(c) contacting the feedstock stream with a polymerization catalyst in the reaction zone;(d) polymerizing at least a portion of the beta propiolactone to poly(propiolactone) in the reaction zone, wherein the temperature of the reaction zone is at or above the pyrolysis temperature of poly(propiolactone);(e) thermally decomposing the poly(propiolactone) in the reaction zone to produce acrylic acid; and(f) withdrawing an acrylic acid product stream comprising the acrylic acid from the reaction zone;wherein steps (b) and (e) occur in the same reaction zone.2. The method of claim 1 , further comprising directing a return loop comprising a portion of the acrylic acid product stream to the reaction zone.3. The method of claim 2 , wherein the return loop of acrylic acid is combined with the feedstock stream.4. A method for producing acrylic acid claim 2 , comprising:(a) providing a feedstock stream comprising beta propiolactone;(b) directing the feedstock stream to a first reaction zone;(c) contacting the feedstock stream with a polymerization catalyst;(d) polymerizing at least a portion of the beta propiolactone to a poly(propiolactone) product stream, wherein the first reaction zone is maintained at a temperature to promote formation of poly(propiolactone);(e) directing the poly(propiolactone) product stream to a second reaction zone, wherein the second reaction zone is maintained at a temperature at or above the pyrolysis temperature of poly(propiolactone) such that the thermal decomposition of poly(propiolactone) produces acrylic acid; and(f) withdrawing an acrylic acid product stream from the second reaction zone.5. The method of claim 4 , wherein the ...

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Номер записи: 88
18-01-2018 дата публикации

IRON (III) CITRATE, SUBSTANTIALLY FREE OF BETA-IRON HYDROXIDE OXIDE

Номер: US20180016220A1
Автор: Ando Koji, Manta Naoki
Принадлежит: JAPAN TOBACCO INC.

This invention provides a method for producing high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, and medical uses thereof. 1. High-purity iron(III) citrate substantially free of beta-iron hydroxide oxide , wherein the beta-iron hydroxide oxide content is less than 6% by weight based on the total weight thereof.2. The high-purity iron(III) citrate according to claim 1 , wherein the beta-iron hydroxide oxide content is less than 2.5% by weight.3. The high-purity iron(III) citrate according to claim 1 , wherein the beta-iron hydroxide oxide content is less than 1.0% by weight.4. The high-purity iron(III) citrate according to claim 1 , wherein the molar ratio of iron(III) to citric acid is from 1:0.75 to 1:1.10.5. The high-purity iron(III) citrate according to claim 4 , wherein the molar ratio of iron(III) to citric acid is from 1:0.80 to 1:0.92.6. The high-purity iron(III) citrate according to claim 1 , wherein the percentage of iron(III) citrate dissolved within 15 minutes is 80% or more in dissolution testing conducted with the use of the first fluid of dissolution testing of the Japanese Pharmacopoeia claim 1 , Fifteenth Edition as a test liquid via the paddle method at 100 rpm in accordance with the Japanese Pharmacopoeia claim 1 , Fifteenth Edition.7. A pharmaceutical composition comprising claim 1 , as an active ingredient claim 1 , the high-purity iron(III) citrate according to .8. A method of treating hyperphosphatemia claim 1 , comprising administering the high-purity iron(III) citrate according to to a subject in need thereof.9. Powder of the high-purity iron(III) citrate according to claim 1 , which has an amorphous structure.10. Powder of the high-purity iron(III) citrate according to claim 1 , which has a specific surface area of 20 to 45 m2/g.11. Powder of the high-purity iron(III) citrate according to claim 9 , which has a specific surface area of ...

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Номер записи: 89
18-01-2018 дата публикации

4-AZIDOBUTYLAMINES AND PROCESSES FOR PREPARING

Номер: US20180016226A1
Автор: PEREIRA David Eugene, SCHNEIDER Stephen E.
Принадлежит:

Neat 4-azidobutylamine and sails of 4-azidobutylamine and processes for producing the same are described herein. Amines represent a large class of organic compounds containing a basic nitrogen atom having a lone pair of electrons and one or more substituent groups. Many amines are used as precursors and feedstocks in a wide variety of industries such as textiles, agriculture, plastics, and pharmaceuticals. One such amine is 4-azidobutylamine, N3-(CH2)4NH2, an amine of butane that also includes an azide. 1. A process for preparing 4-azidobutylamine , the process comprising isolating the 4-azidobutylamine from a solvent that is substantially free or free of a chlorinated solvent.2. The process of wherein the solvent is N claim 1 , N-dimethyformamide or MTBE claim 1 , or a mixture thereof.3. The process of wherein the solvent is an aqueous solution.4. The process of further comprising raising the pH of the mixture.5. The process of further comprising separating an aqueous layer from the mixture.6. (canceled)7. Isolated 4-azidobutylamine substantially free of or free of a chlorinated solvent.8. An isolated salt of 4-azidobutylamine claim 4 , where the salt comprises a nitrate claim 4 , fluoride claim 4 , bromide claim 4 , iodide claim 4 , sulfate claim 4 , chlorosulfonate claim 4 , methanesulfonate claim 4 , toluenesulfonate claim 4 , phosphate claim 4 , phosphonate claim 4 , oxalate claim 4 , borate claim 4 , citrate claim 4 , malonate claim 4 , formate claim 4 , butyrate claim 4 , maleate claim 4 , propionate claim 4 , pyruvate claim 4 , benzoate claim 4 , or lactate claim 4 , or a combination thereof.910.-. (canceled)11. The salt of comprising an acid claim 8 , wherein the acid is selected from the group consisting of hydroiodide claim 8 , hydrobromide claim 8 , hydrofluoride claim 8 , nitric acid claim 8 , chlorosulfonic acid claim 8 , malonic acid claim 8 , formic acid claim 8 , butyric acid claim 8 , maleic acid claim 8 , propionic acid claim 8 , pyruvic acid ...

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Номер записи: 90
15-01-2015 дата публикации

TREATMENT OF INFLAMMATORY BOWEL DISEASE

Номер: US20150018400A1
Автор: Donde Yariv, Donello John E., Gil Daniel W., IM WHA-BIN, Kedzie Karen M., Nguyen Jeremiah H.
Принадлежит:

Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I 1. (canceled)2. (canceled)4. The method of wherein Y is COR claim 3 , wherein Ris any linear claim 3 , branched claim 3 , or cyclic alkyl group having from 3 to 6 carbons.6. The method of wherein Y is COH or COMe.7. The method of wherein Ris naphthyl claim 5 , benzofuranyl claim 5 , or benzothienyl claim 5 , which may contain one or more substituents selected from the group consisting of halogen claim 5 , trihalomethyl claim 5 , cyano claim 5 , nitro claim 5 , amino claim 5 , hydroxy claim 5 , Calkyl claim 5 , OR claim 5 , SR claim 5 , and SOR.8. The method of wherein Ris 3-chlorobenzothien-2-yl.13. A method of activating an EP4 receptor claim 5 , the method comprising administering a compound selected from:(Z)-7-{(1R,4S,5R)-5-[(E)-5-(3-chloro-benzo[b]thiophene-2-yl)-3-hydroxy-pent-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxo-cyclopentyl}-hept-5-ynoic acid methyl ester;(Z)-7-{(1R,4S,5R)-5-[(E)-5-(3-chloro-benzo[b]thiophene-2-yl)-3-hydroxy-pent-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxo-cyclopentyl}-hept-5-ynoic acid;(Z)-7-{(1R,4S,5R)-5-[(E)-5-(3-chloro-benzo[b]thiophene-2-yl)-3-hydroxy-pent-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxo-cyclopentyl}-hept-5-enoic acid methyl ester;(Z)-7-{(1R,4S,5R)-5-[(E)-5-(3-chloro-benzo[b]thiophene-2-yl)-3-hydroxy-pent-1-enyl]-4-hydroxy-3,3-dimethyl-2-oxo-cyclopentyl}-hept-5-enoic acid;(Z)-7-[(1R,4S,5R)-4-Hydroxy-5-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-3,3-dimethyl-2-oxo-cyclopentyl]-hept-5-enoic acid methyl ester;(Z)-7-[(1R,4S,5R)-4-Hydroxy-5-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-3,3-dimethyl-2-oxo-cyclopentyl]-hept-5-enoic acid;(Z)-7-[(1R,4S,5R)-5-((E)-4-Benzo[b]thiophen-2-yl-3-hydroxy-but-1-enyl)-4-hydroxy-3,3-dimethyl-2-oxo-cyclopentyl]-hept-5-enoic acid;7-[(1R,4S,5R)-5-((E)-4-Benzo[b]thiophen-2-yl-3-hydroxy-but-1-enyl)-4-hydroxy-3,3-dimethyl- ...

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Номер записи: 91
15-01-2015 дата публикации

AROMATIC RING COMPOUND

Номер: US20150018422A1
Автор: Hirata Yasuhiro, Hitomi Yuko, Miwatashi Seiji, Miyamoto Yasufumi, Okawa Tomohiro, Shibuya Akito, Suzuki Hideo, Yamasaki Takeshi
Принадлежит:

Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): 2. The compound according to claim 1 , wherein ring A is a benzene ring or a pyridine ring claim 1 , each of which is optionally further substituted by 1 to 3 halogen atoms or 1 to 3 Calkoxy groups claim 1 , or a salt thereof.3. The compound according to claim 1 , wherein ring B is a benzene ring or a pyridine ring claim 1 , or a salt thereof.4. The compound according to claim 1 , wherein ring C is a benzene ring claim 1 , a pyridine ring or a pyrimidine ring claim 1 , or a salt thereof.5. The compound according to claim 1 , wherein X is —NH— claim 1 , —N(methyl)- claim 1 , —N(trifluoroethyl)- claim 1 , —N(acetyl)- claim 1 , —CHF— claim 1 , —O— claim 1 , —S— claim 1 , —S(O)— or —S(O)— claim 1 , or a salt thereof.6. The compound according to claim 1 , wherein Y is —CRR— or —O— [Rand Rare each independently (1) a Ccycloalkyl group optionally substituted by 1 to 3 substituents selected from a halogen atom and cyano claim 1 , (2) a hydrogen atom claim 1 , (3) a Calkyl group optionally substituted by 1 to 3 substituents selected from a halogen atom claim 1 , a Ccycloalkyl group claim 1 , cyano claim 1 , carboxyl claim 1 , a Calkoxy-carbonyl group and a carbamoyl group claim 1 , (4) a Calkenyl group optionally substituted by a halogen atom claim 1 , or (5) a Calkynyl group optionally substituted by 1 to 3 substituents selected from a halogen atom and a Ccycloalkyl group] claim 1 , or a salt thereof.7. The compound according to claim 1 , wherein Ris (1) a Calkoxy group optionally substituted by a halogen atom claim 1 , (2) a Calkyl group claim 1 , (3) hydroxy claim 1 , (4) carboxyl claim 1 , (5) a Calkyl-sulfonyl-amino group claim 1 , (6) a 5- to 10-membered non-aromatic heterocyclyl-oxy group claim 1 , (7) a 5- to 10-membered non-aromatic heterocyclyl-sulfonyl group claim 1 , or (8) cyano claim 1 , or a salt thereof.8. The compound according to claim 1 , ...

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Номер записи: 92
17-01-2019 дата публикации

PROCESS TO PREPARE LEVULINIC ACID

Номер: US20190016658A1
Автор: Brunelle Daniel Joseph, Bunning Donald L., Kapicak Louis A., Leibig Cora M., Louwagie Andrew J., MULLEN Brian D., Rodwogin Marc David, Shirtum Robert Page, Strand Steven R., Tjosaas Matthew John, Yontz Dorie Janine
Принадлежит:

The invention describes processes to prepare levulinic acid, formic acid and/or hydroxymethyl furfural from various biomass materials. 1. A process to prepare levulinic acid comprising the steps:a) heating an aqueous solution of a mineral acid to about 60° C. to about 110° C. in a reactor, wherein the reactor is a batch reactor; andb) continuously adding an aqueous mixture of sugars to the heated aqueous acid of step a) in the batch reactor over a period of from about 0.1 to about 40 hours to form a reaction mixture including levulinic acid,wherein the mineral acid percentage by weight is from about 20 to about 80 percent of the reaction mixture.2mineral. The process of claim 1 , wherein the acid is sulfuric acid (HSO) claim 1 , hydrochloric acid (HCl) claim 1 , hydrobromic acid (HBr) or hydroiodic acid (HI).3. The process of claim 1 , wherein the sugars are selected from high fructose corn syrup claim 1 , sucrose claim 1 , an aqueous mixture of fructose claim 1 , an aqueous mixture of hydroxymethylfurfural claim 1 , an aqueous mixture of glucose claim 1 , an aqueous mixture of maltose claim 1 , an aqueous mixture of inulin claim 1 , or mixtures thereof.4. The process of claim 1 , wherein the sugars are a mixture of at least two different sugars;wherein the at least two different sugars are selected from an aqueous mixture of fructose and glucose, and an aqueous solution of fructose and hydroxymethylfurfural.5. The process of claim 1 , wherein the sugars are an aqueous mixture of polysaccharides;wherein the aqueous mixture of polysaccharides is the aqueous mixture of inulin.6. The process of claim 1 , wherein the mineral acid percentage by weight is from about 20 to about 50 percent of the reaction mixture.7mineral. The process of claim 1 , wherein the aqueous solution of acid is stirred.8. The process of claim 1 , wherein the mixture is heated for an additional period of time from about 0.1 hour to about 20 hours at a temperature range of from about 25° C. to about ...

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Номер записи: 93
17-01-2019 дата публикации

HYDROXY METHIONINE ANALOG FORMULATIONS SUITABLE FOR SPECIALTY CHEMICAL APPLICATIONS

Номер: US20190016675A1
Автор: Arhancet Graciela, Long Scott, Mahoney Matthew, Rode Tracy, Wang Xiaojun
Принадлежит:

Formulations comprising hydroxy methionine analog and having low levels of sulfate ions and bisulfate salts, processes for preparing the formulations, compositions comprising the formulations, and methods of using the formulations. 2. The composition of claim 1 , wherein the at least one metal ion is calcium claim 1 , chromium claim 1 , cobalt claim 1 , copper claim 1 , iron claim 1 , manganese claim 1 , silver claim 1 , sodium claim 1 , zinc claim 1 , or a combination thereof.3. The composition of claim 1 , wherein the at least one compound of Formula (I) and the at least one metal ion are present at a ratio of 1:1 claim 1 , 2:1 claim 1 , or 3:1.4. The composition of claim 1 , wherein Ris methyl claim 1 , k is 1 claim 1 , and n is 2.5. The composition of claim 4 , wherein the at least one compound of Formula (I) and the at least one metal ion are present at a ratio of 2:1.6. The composition of claim 5 , wherein the metal ion is calcium claim 5 , copper claim 5 , manganese claim 5 , or zinc.7. The composition of claim 6 , wherein the metal ion is calcium.8. The composition of claim 1 , which comprises 2% or less by weight of water.9. The composition of claim 1 , which comprises 1000 ppm or less by weight of sulfate ion.10. The composition of claim 1 , which comprises 500 ppm or less by weight of bisulfate ion.11. The composition of claim 1 , which comprises 200 ppm or less by weight of bisulfate ion.12. The composition of claim 1 , wherein a 50 wt % solution has an American Public Health Association (APHA) color value of 200 or less.13. The composition of claim 12 , wherein the APHA color value is 500 or less after heating at 140° C. for up to 12 hours.14. The composition of claim 1 , wherein a 15 wt % solution has a pH value of at least 1.3.15. The composition of claim 1 , wherein the composition is a dry granulate or a powder.16. The composition of claim 7 , which comprises 2% or less by weight of water claim 7 , 1000 ppm or less by weight of sulfate ion claim 7 , ...

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Номер записи: 94
17-01-2019 дата публикации

PCSK9 ANTIBODY, ANTIGEN-BINDING FRAGMENT THEREOF, AND MEDICAL APPLICATION THEREOF

Номер: US20190016825A1
Автор: CUI Dongbing, HU Qiyue, QU Xiangdong, Sun Piaoyang, Tao Weikang, XU Shaoyu, XU Zhibin, YE Xin, YUAN Bei, ZHANG LEI, Zhang Lianshan
Принадлежит:

The present invention provides a PCSK9 antibody, an antigen-binding fragment thereof, and a medicinal application thereof. Provided in the invention is a chimeric antibody and a humanized antibody, both comprising a CDR of the PCSK9 antibody, and a pharmaceutical composition comprising the PCSK9 antibody and an antigen-binding fragment thereof, and an application of the PCSK9 antibody as a lipid-lowering agent. The invention specifically relates to an application of a humanized PCSK9 antibody for preparing a pharmaceutical drug to treat a PCSK9-induced disease or symptom. 13.-. (canceled)4. A PCSK9 antibody or the antigen-binding fragment thereof , wherein the antibody comprises a HCDR1 , a HCDR2 , and a HCDR3 as shown in SEQ ID NO: 12 , SEQ ID NO: 13 and SEQ ID NO: 14 , respectively , or comprises a HCDR1 , a HCDR2 and a HCDR3 having at least 95% identity to SEQ ID NO: 12 , SEQ ID NO: 13 and SEQ ID NO: 14 , respectively; anda LCDR1, a LCDR2, and a LCDR3 as shown in SEQ ID NO: 15, SEQ ID NO: 16 and SEQ ID NO: 17, respectively, or comprises a LCDR1, a LCDR2, and a LCDR3 having at least 95% identity to these sequences SEQ ID NO: 15, SEQ ID NO: 16 and SEQ ID NO: 17, respectively.5. The PCSK9 antibody or the antigen-binding fragment thereof according to claim 4 , wherein the PCSK9 antibody or antigen-binding fragment thereof is a murine antibody or fragment thereof.6. The PCSK9 antibody or the antigen-binding fragment thereof according to claim 4 , wherein the PCSK9 antibody light chain variable region further comprises light chain FR regions derived from a murine κ chain or a variant thereof claim 4 , or light chain FR regions derived from a murine λ chain or a variant thereof; wherein the PCSK9 antibody heavy chain variable region further comprises heavy chain FR regions derived from a murine IgG1 or a variant thereof claim 4 , or heavy chain FR regions derived from a murine IgG2 or a variant thereof claim 4 , or heavy chain FR regions derived from a murine IgG3 or a ...

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Номер записи: 95
16-01-2020 дата публикации

Compounds, Compositions, and Methods for Coloring Edible Materials

Номер: US20200017538A1
Автор: Hatzakis Emmanuel, Lambert Joshua David, Mazzola Eugene P., Ziegler Gregory Ray
Принадлежит:

The present invention provides compounds isolated from avocado seeds for use as a natural colorant in edible materials. The compounds of the invention are useful for coloring edible materials red, orange, or yellow. The invention also provides compositions and methods for coloring edible materials to a desired color such as red, orange, or yellow. 2. The compound of claim 1 , wherein Ris (C(RR))OR.3. The compound of claim 2 , wherein Ris a monosaccharide.4. The compound of claim 1 , wherein the compound of general formula (1) is a compound of general formula (2):wherein in general formula (2),{'sup': 21', '23', '26', '28', '213', '216', '21', '23', '26', '28', '213', '216, 'R, R, R-R, and R-Rare each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, and substituted heteroaryl, wherein any of R, R, R-R, and R-Rare optionally joined to form a ring, wherein the ring is optionally substituted;'}{'sup': 29', '210', '211', '29', '210, 'Rand Rare each independently selected from the group consisting of hydrogen, an alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, substituted heteroaryl, and C(═O)R, wherein Rand Rare optionally joined to form a ring;'}{'sup': '211', 'each occurrence Ris independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, substituted heteroaryl, a monosaccharide, a disaccharide, and a polysaccharide;'}{'sup': 217', '18', '217', '217', '217, 'Y is selected from the group consisting of C(RR), NR, SR, and ...

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Номер записи: 96
25-01-2018 дата публикации

METHOD OF TREATING IDIOPATHIC PULMONARY FIBROSIS

Номер: US20180021275A1
Автор: Iwaki Yuichi, MATSUDA Kazuko
Принадлежит: MediciNova, Inc.

A compound of Formula (I): 4. The method of claim 1 , wherein the compound is administered orally.5. The method of claim 4 , wherein the compound is administered as a tablet or a capsule.6. The method of claim 2 , wherein the compound is present in an orthorhombic crystalline polymorphic form.7. The method of claim 1 , wherein the compound is administered as a liquid dosage form.8. The method of claim 1 , wherein the effective amount of the compound is administered in an amount from about 250 to about 2 claim 1 ,000 mg/day claim 1 , divided into one claim 1 , two claim 1 , or three portions.9. The method of claim 1 , wherein the patient's pulmonary scarring is inhibited.10. The method of claim 1 , wherein the patient's elevated lung hydroxyproline levels are reduced and/or inhibited.11. The method of claim 1 , wherein the patient's elevated lung density is reduced.12. The method of claim 1 , wherein the patient's elevated total cell count (TCC) in bronchioalveolar lavage fluid (BALF) is reduced.14. The method of claim 13 , wherein the compound is administered orally.15. The method of claim 13 , wherein the compound is administered as a tablet or a capsule.16. The method of claim 13 , wherein the compound is administered as a liquid dosage form.17. The method of claim 13 , wherein the compound is administered in an amount from about 250 to about 2 claim 13 ,000 mg/day claim 13 , divided into one claim 13 , two claim 13 , or three portions.18. The method of claim 13 , wherein the patient's pulmonary scarring is inhibited.19. The method of claim 13 , wherein the patient's elevated lung hydroxyproline levels are reduced and/or inhibited.20. The method of claim 13 , wherein the patient's elevated lung density is reduced.2130-. (canceled) This application is a continuation of U.S. patent application Ser. No. 15/361,326, filed Nov. 25, 2016, which is a continuation of U.S. patent application Ser. No. 15/134,509, filed Apr. 21, 2016, which is a continuation of U.S. patent ...

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Номер записи: 97
10-02-2022 дата публикации

GENE THERAPY FOR TREATING FAMILIAL HYPERCHOLESTEROLEMIA

Номер: US20220040332A1
Автор: Rader Daniel J.
Принадлежит:

Regimens useful treating a human patient having familial hypercholesterolemia are described. Such regimens comprise co-administration of corticosteroids with a suspension of replication deficient recombinant adeno-associated virus (rAAV) comprising LDLR. 1. A regimen for use in the treatment of familial hypercholesterolemia (FH) , comprising administering to a patient a suspension comprising a recombinant adeno-associated virus (rAAV) viral particle which comprises a vector genome packaged in an AAV8 capsid , wherein the vector genome comprises AAV inverted terminal repeats (ITRs) and a nucleic acid sequence encoding a human low-density lipoprotein (LDL) receptor (hLDLR) operably linked to a liver specific promoter , wherein the suspension is administered to the patient at a dose of about 2.5×10Genome Copy (GC) of the rAAV viral particle per kilogram (kg) body weight of the patient , and wherein the genome copy is determined by optimized quantitative polymerase chain reaction (oqPCR) or digital droplet polymerase chain reaction (ddPCR).226-. (canceled)27. A suspension for use in the treatment of familial hypercholesterolemia (FH) , comprising a recombinant adeno-associated virus (rAAV) viral particle which comprises a vector genome packaged in an AAV8 capsid , wherein the vector genome comprises AAV inverted terminal repeats (ITRs) and a nucleic acid sequence encoding a human low-density lipoprotein (LDL) receptor (hLDLR) operably linked to a liver specific promoter , wherein the suspension is suitable for administering to a patient at a dose of about 2.5×10Genome Copy (GC) of the rAAV viral particle per kilogram (kg) body weight of the patient , and wherein the genome copy is determined by optimized quantitative polymerase chain reaction (oqPCR) or digital droplet polymerase chain reaction (ddPCR).2830-. (canceled)31. A method for treating a patient having familial hypercholesterolemia (FH) , comprising administering to the patient a suspension comprising a ...

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Номер записи: 98
28-01-2016 дата публикации

Process and Intermediates for the Preparation of Pregabalin

Номер: US20160024540A1
Автор: "ONeill Padraig Mary", Debarge Sebastien, Erdman David Thomas, Karmilowicz Michael John, Kumar Rajesh
Принадлежит:

The invention provides processes for the manufacture of a compound of formula (I). The invention further provides improved methods for the conversion of the compound of formula (I) into pregabalin. 4. The compound according to wherein R* is selected from (R)- or (S)-α-methyl benzyl claim 3 , (R)- or (S)-1-(1-naphthyl)ethyl claim 3 , (R)- or (S)-1-(2-naphthyl)ethyl claim 3 , menthyl and bornyl.5. The compound according to wherein R is R—C(O)— or R—SO- and Rand Rare chiral (C-C) hydrocarbon groups.7. The compound according to wherein n is 1 and M is selected from NH and ((C-C)alkyl)NH.8. The compound according to wherein n is 1 and M is selected from Li claim 6 , Na and K.10. The compound according to selected from:4-(2-methylpropenyl)-5-pyrrolidin-1-yl-5H-furan-2-one;4-(2-methylpropenyl)-5-piperidin-1-yl-5H-furan-2-one;4-(2-methylpropenyl)-5-morpholin-4-yl-5H-furan-2-one; or1,4-bis-(4-(2-methylpropenyl)-5H-furan-2-on-5-yl)piperazine.12. A process for the manufacture of a compound of formula (VI) according to wherein R is other than hydrogen claim 1 , R—C(O)— claim 1 , and R—SO— claim 1 , comprising the step of treating a compound of formula (VI) with an alcohol R—OH in the presence of an acid catalyst.13. A process for the manufacture of a compound of formula (VI) according to wherein R is other than hydrogen claim 1 , R—C(O)— claim 1 , and R—SO— claim 1 , comprising the step of treating a compound of formula (VII) with an alcohol R—OH in the presence of stoichiometric acid.14. A process for the manufacture of a compound of formula (VI) according to wherein R is R—C(O)— claim 1 , comprising the steps of treating a compound of formula (VI) with an acid chloride R—C(O)—Cl or acid anhydride (R—C(O))O.15. A process for the manufacture of a compound of formula (VI) according to wherein R is R—SO—; comprising the step of treating a compound of formula (VI) with a sulfonyl chloride R—SO—Cl.18. The process according to wherein step (a) comprises a process according to .23. ...

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Номер записи: 99
22-01-2015 дата публикации

IRON (III) CITRATE, SUBSTANTIALLY FREE OF BETA-IRON HYDROXIDE OXIDE

Номер: US20150025138A1
Автор: Ando Koji, Manta Naoki
Принадлежит: JAPAN TOBACCO INC.

This invention provides a method for producing high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, high-purity iron(III) citrate substantially free of beta-iron hydroxide oxide, and medical uses thereof. 1. High-purity iron(III) citrate substantially free of beta-iron hydroxide oxide , wherein the beta-iron hydroxide oxide content is less than 6% by weight based on the total weight thereof.2. The high-purity iron(III) citrate according to claim 1 , wherein the beta-iron hydroxide oxide content is less than 2.5% by weight.3. The high-purity iron(III) citrate according to claim 1 , wherein the beta-iron hydroxide oxide content is less than 1.0% by weight.4. The high-purity iron(III) citrate according to claim 1 , wherein the molar ratio of iron(III) to citric acid is from 1:0.75 to 1:1.10.5. The high-purity iron(III) citrate according to claim 4 , wherein the molar ratio of iron(III) to citric acid is from 1:0.80 to 1:0.92.6. The high-purity iron(III) citrate according to claim 1 , wherein the percentage of iron(III) citrate dissolved within 15 minutes is 80% or more in dissolution testing conducted with the use of the first fluid of dissolution testing of the Japanese Pharmacopoeia claim 1 , Fifteenth Edition as a test liquid via the paddle method at 100 rpm in accordance with the Japanese Pharmacopoeia claim 1 , Fifteenth Edition.7. A pharmaceutical composition comprising claim 1 , as an active ingredient claim 1 , the high-purity iron(III) citrate according to .8. A method of treating hyperphosphatemia claim 1 , comprising administering the high-purity iron(III) citrate according to to a subject in need thereof.9. Powder of the high-purity iron(III) citrate according to claim 1 , which has an amorphous structure.10. Powder of the high-purity iron(III) citrate according to claim 1 , which has a specific surface area of 20 to 45 m2/g.11. Powder of the high-purity iron(III) citrate according to claim 9 , which has a specific surface area of ...

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Номер записи: 100