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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 14760. Отображено 100.
20-09-2001 дата публикации

СИСТЕМА ДЛЯ ВЫДЕЛЕНИЯ ЦИТРАТА КАЛЬЦИЯ ИЗ ЦИТРАТСОДЕРЖАЩЕГО РАСТВОРА

Номер: RU0000019653U1

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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16-02-2012 дата публикации

Compound of salvianolic acid l, preparation method and use thereof

Номер: US20120041062A1
Принадлежит: Tianjin Tasly Pharmaceutical Co Ltd

The present invention relates to a new compound of salvianolic acid L, its preparation method, a pharmaceutical composition containing the salvianolic acid L, and its use for preparing a medicament for treating cardio-cerebrovascular diseases.

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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17-05-2012 дата публикации

Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas

Номер: US20120122940A1
Принадлежит: Individual

The present disclosure relates to lipid compounds of the general formula (I): R1-O—C(R2)(R3)-X  (I) wherein R 1 is a C 10 -C 22 alkyl group, a C 10 -C 22 alkenyl group having 1-6 double bonds, or a C 10 -C 22 alkynyl group having 1-6 triple bonds; R 2 and R 3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic, and inflammatory disease area.

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31-05-2012 дата публикации

Hydroxy fatty acid compounds and uses thereof for disease treatment and diagnosis

Номер: US20120136057A1
Принадлежит: Phenomenome Discoveries Inc

A compound of formula (I): wherein R represents a hydroxy substituted C 24 -C 40 straight chain aliphatic group containing at least one double bond in the carbon chain; and at least one carbon in the chain is substituted with a hydroxy group. Such compounds are useful for detecting inflammation, inflammatory disorders and cancer in a subject, and can also be used in therapeutic applications including treatment and/or prevention of these conditions. Pharmaceutical compositions, combinations and supplements, as well as methods of treatment using the described compounds are therefore also described.

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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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05-07-2012 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20120172398A1
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.

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06-09-2012 дата публикации

Microbial production of 3,4-dihydroxybutyrate (3,4-dhba), 2,3- dihydroxybutyrate (2,3-dhba) and 3-hydroxybutyrolactone (3-hbl)

Номер: US20120226055A1
Принадлежит: Massachusetts Institute of Technology

The invention relates to recombinant cells and their use in the production of 3,4-dihydroxybutyrate, 2,3-dihydroxybutyrate and 3-hydroxybutyrolactone.

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01-11-2012 дата публикации

Drug Loaded Polymeric Nanoparticles and Methods of Making and Using Same

Номер: US20120276162A1
Принадлежит: Individual

The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

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01-11-2012 дата публикации

Lipoxin compounds and their use in treating cell proliferative disorders

Номер: US20120277311A1
Автор: Charles N. Serhan
Принадлежит: Brigham and Womens Hospital Inc

Compounds having the active site of natural lipoxins, but a longer tissue half-life are disclosed. In particular, 15-epi-lipoxins and their use in ameliorating undesired cell proliferation, which characterizes diseases such as cancer, are also disclosed.

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15-11-2012 дата публикации

Additive and method for removal of impurities formed due to sulfur compounds in crude oils containing calcium naphthenate

Номер: US20120285865A1
Автор: Mahesh Subramaniyam
Принадлежит: Dorf Ketal Chemicals India Pvt Ltd

An additive capable of avoiding formation of impurities and capable of removing or dissolving impurities formed and accumulated at the interphase of organic and aqueous layers on reaction between calcium naphthenate and sulfur compound including H 2 S in presence of water in mixture of crude oils containing calcium naphthenate and sulfur compound or H 2 S, wherein the additive is glyoxylic acid is provided. A method for avoiding formation of impurities and for removing or dissolving impurities formed and accumulated at the interphase of organic and aqueous layers on reaction between calcium naphthenate and sulfur compound including H 2 S in presence of water in mixture of crude oils containing calcium naphthenate and sulfur compound including H 2 S, comprising treating mixture of crude oils containing calcium naphthenate and sulfur compound or H 2 S with glyoxylic acid is also provided.

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20-12-2012 дата публикации

4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

Номер: US20120322875A1
Принадлежит: Individual

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

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27-12-2012 дата публикации

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

Номер: US20120329832A1
Принадлежит: Merial Ltd

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

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10-01-2013 дата публикации

4-hydroxybutyric acid analogs

Номер: US20130012565A1
Принадлежит: Concert Pharmaceuticals Inc

This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.

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24-01-2013 дата публикации

Novel compounds

Номер: US20130022560A1
Принадлежит: DSM IP ASSETS BV

The invention relates to novel polyglycerol based UV-filters as well as to topical compositions comprising such novel polyglycerol based UV-filters. Furthermore, the invention relates to the use of such novel polyglycerol based UV-filters to enhance the solubility of butyl methoxydibenzoylmethane or bis-ethylhexyloxyphenol methoxyphenyl triazine in cosmetic oils.

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14-02-2013 дата публикации

Electroluminescent materials comprising fluorene derivatives

Номер: US20130037752A1
Автор: Gene Carl Koch
Принадлежит: Lomox Ltd

OLED compounds of the general structure: B—S-A-S—B in which rod-like nuclei A includes a condensed aromatic ring structure in turn having fluorene ring structures condensed with at least one additional fluorene ring structures wherein the fluorene ring systems provided by the condensed aromatic structure are substituted at the 9-position, and in which the 9-positions of the fluorenes are not susceptible to oxidation.

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21-02-2013 дата публикации

Salicylate fatty acid derivatives

Номер: US20130046013A1
Принадлежит: Individual

Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating various diseases comprising the administration of an effective amount of at least one compound according to the present disclosure.

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21-03-2013 дата публикации

CRYSTALLINE FORMS OF A PURINE DERIVATIVE

Номер: US20130072504A1
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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28-03-2013 дата публикации

NEURO-PROTECTIVE EFFECTS OF ADELOSTEMMA GRACILLIMUM AND ITS ISOLATED COMPOUNDS

Номер: US20130079293A1

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

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28-03-2013 дата публикации

PROCESS FOR THE PREPARATION OF PLEUROMUTILINS

Номер: US20130079400A1
Принадлежит: NABRIVA THERAPEUTICS AG

Process for the preparation of a compound of formula I 2. A compound of formula I as defined in in the form of a single stereoisomer in crystalline form.3. A compound according to claim 2 , which is 14-O-{[(1R claim 2 ,2R claim 2 ,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin in crystalline Form 1.4. A compound according to claim 2 , which is 14-O-{[(1R claim 2 ,2R claim 2 ,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin in crystalline Form 2 in the form of a n-butanol solvate.5. A compound of formula I as defined in in the form of a single stereoisomer in the form of a crystalline salt.6. A crystalline salt according to claim 5 , which is an acetate claim 5 , lactate or hydrogenmaleate.7. A compound according to claim 5 , which is selected from the group consisting of14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin acetate in crystalline Form A;14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin acetate in crystalline Form B14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin L-lactate in crystalline Form 1, and14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin hydrogenmaleate in crystalline Form 1.11. A compound of formula IIa as defined in claim 5 , for use as an intermediate in a process for the production of a compound of formula I as defined in claim 5 , in the form of a single stereoisomer.12. Pharmaceutical composition comprising crystalline 14-O-{[((1R claim 5 ,2R claim 5 ,4R)-4-amino-2-hydroxy-cyclohexyl) sulfanyl]acetyl}mutilin claim 5 , or comprising an claim 5 , optionally crystalline claim 5 , acetate claim 5 , lactate claim 5 , or hydrogenmaleate of 14-O-{[((1R claim 5 ,2R claim 5 ,4R)-4-amino-2-hydroxy-cyclohexyl)sulfanyl]acetyl}mutilin as an active ingredient in combination with pharmaceutically acceptable carrier or diluent.13. A compound of formula IIIa as defined in claim 5 , for use as an intermediate in a process for the production of a ...

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28-03-2013 дата публикации

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

Номер: US20130079405A1
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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28-03-2013 дата публикации

SUBSTITUTED CYCLOHEXANE-1, 3-DIONE COMPOUNDS, PROCESS FOR PREPARATION THEREOF AND ITS APPLICATIONS

Номер: US20130079545A1

A regio-selective and consecutive Michael-Claisen process has been developed for substituted cyclohexane-1,3-dione synthesis started from unsubstituted or substituted acetone and α,β-unsaturated esters. Substituted cyclohexane-1,3-diones are the basic unit found in several natural products, bioactive alkaloids and acridine dione type heterocycles, polyphenols, and unnatural amino acid synthesis. Most of the potent herbicidal and pesticidal active molecules contain cyclohexane-1,3-dione derivatives. Such an important intermediate synthesis using a facile, atom economy and one-pot process is a demandable area in organic synthesis. 6. The process as claimed in step (i) of claim 3 , wherein solvent used are selected from the group consisting of toluene claim 3 , tetrahydrofuran (THF) or benzene.7. The process as claimed in step (i) of claim 3 , wherein molar concentration of sodium hydride (NaH) base is 1.5 to 2 times the number of moles of the ketone.8. The process as claimed in step (ii) of claim 3 , wherein molar concentration of α claim 3 ,β-unsaturated ester is 1 to 2 times the number of moles of the ketone or substituted ketone.9. The process as claimed in step (v) of claim 3 , wherein solvent used for solvent extraction is selected from the group consisting of hexane claim 3 , ethyl acetate claim 3 , dichloromethane or chloroform.10. The compound as claimed in claim 1 , wherein said compounds are useful as an intermediate for the synthesis of several biological active heterocycles claim 1 , natural product analogues claim 1 , anisoles and aromatic poly phenol derivatives. The present invention relates to substituted cyclohexane-1,3-dione compounds of general formula Iwherein, R is selected from COY, B(OY), CHO, CHOY, CH(COY), PO(OY)and CONHZ, wherein Y is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, substituted alkyl, substituted alkenyl, cycloalkyl, substituted alkyl, substituted heteroaryl or tetrazolyl and Z is ...

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11-04-2013 дата публикации

SOLID STATE FORMS OF TAPENTADOL SALTS

Номер: US20130090314A1
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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25-04-2013 дата публикации

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

Номер: US20130101630A1
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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25-04-2013 дата публикации

COMPOSITIONS AND METHODS FOR DETECTING AMYLOID-BETA-DEGRADING ENZYME ACTIVITY

Номер: US20130102498A1
Принадлежит: Academia Sinica

Novel substrates for detection of activity of amyloid beta degrading enzyme, such as Neprilysin (NEP) and insulin degrading enzyme (IDE), associated with Alzheimer's disease, are provided. A quenched fluorogenic peptide substrate containing the first seven residues of the Aβpeptide plus a C-terminal Cys residue to detect neprilysin activity with a fluorophore attached to the C-terminal Cys and a quencher linked to the N-terminus of the peptide is disclosed. An assay system sensitive to endopeptidase activity of NEP and IDE, but insensitive to other Aβ-degrading enzymes is disclosed. Active compounds are identified by a cell-based assay system for high-throughput screening. 1. A peptide substrate for detection of amyloid-β degrading enzyme activity , the substrate comprising:(a) a peptide of the sequence DAEFRHDC (SEQ ID NO: 1) comprising residues 1-7 of the amyloid-β peptide and a cysteine residue at the C-terminal end, or an analog or derivative thereof, wherein the peptide comprises a cleavage site for an amyloid-β degrading enzyme;(b) a quencher coupled to the N-terminal end of the peptide; and(c) a fluorophor coupled with the C-terminal end of the peptide.2. The substrate of claim 1 , wherein the amyloid-β degrading enzyme is selected from the group consisting of neprilysin (NEP) and insulin degrading enzyme (IDE).3. The substrate of claim 1 , wherein the fluorophore is selected from the group consisting of fluorescein claim 1 , fluorescein derivatives claim 1 , rhodamines claim 1 , tetramethylrhodamines claim 1 , coumarins claim 1 , resorufins claim 1 , pyrenes claim 1 , anthracenes claim 1 , phenylenes claim 1 , phthalocyanines claim 1 , cyanines claim 1 , xanthenes claim 1 , amidopyrylium dyes claim 1 , oxazines claim 1 , quadrain dyes claim 1 , carbopyronines claim 1 , NBD derivatives claim 1 , BODIPY fluorophores claim 1 , ALEXA fluorophores claim 1 , ALEXA-350 claim 1 , lanthanide chelates claim 1 , metalloporphyrins claim 1 , NIR fluorophores claim 1 , ...

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02-05-2013 дата публикации

SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: US20130109710A1
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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16-05-2013 дата публикации

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

Номер: US20130122598A1
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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16-05-2013 дата публикации

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

Номер: US20130123520A1
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

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

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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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23-05-2013 дата публикации

Novel compound, method for producing the same and method for producing fluoropolymer

Номер: US20130131267A1
Принадлежит: Daikin Industries Ltd

The invention provides a compound which is useful in production of a fluoropolymer and easy to be removed from the produced fluoropolymer, a method of producing the compound, and a method of producing a fluoropolymer using the compound. The invention provides a compound which is represented by Rf 1 —CH 2 O—CF 2 —CHF—Rf 2 —X, wherein Rf 1 represents a fluoroalkyl group containing 1 to 5 carbon atoms, Rf 2 represents a fluoroalkylene group containing 1 to 3 carbon atoms, X represents —COOM or —SO 3 M, and M represents one of H, K, Na, and NH 4 .

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23-05-2013 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS

Номер: US20130131359A1
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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30-05-2013 дата публикации

Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases

Номер: US20130137727A1
Принадлежит: Acadia Pharmaceuticals Inc

Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

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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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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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27-06-2013 дата публикации

Aildenafil citrate crystal form o, preparation method and use thereof

Номер: US20130165448A1
Автор: Guikun Liu
Принадлежит: Guikun Liu

The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.

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27-06-2013 дата публикации

TETRASUBSTITUTED BENZENES

Номер: US20130165486A1
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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04-07-2013 дата публикации

METHOD FOR PRODUCING PYRIDAZINONE COMPOUNDS AND INTERMEDIATE THEREOF

Номер: US20130172556A1
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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11-07-2013 дата публикации

METHOD OF PRODUCING INGENOL-3-ANGELATE

Номер: US20130177952A1
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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11-07-2013 дата публикации

Processes for preparing 3-benzazepines

Номер: US20130178620A1
Принадлежит: Arena Pharmaceuticals Inc

The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.

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18-07-2013 дата публикации

Method to produce a stable dry ionic-bonded creatine alpha ketoglutarate of high oral absorbability

Номер: US20130184487A1
Принадлежит: Individual

The invention provides a method to produce a stable, ionic-bonded, dry creatine-α-ketoglutarate product at a molar ratio of about 2:1. The product is stable at room temperature when kept dry for periods of up to one year. The product can be supplemented with additional biologically active, natural amino acid, preferably l-arginine, l-taurine and l-citrulline. The serving dosage is typically between about 1 and 2 g.

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25-07-2013 дата публикации

CRYSTALLINE FORMS OF 4-[2-(4-METHYLPHENYLSULFANYL)-PHENYL] PIPERIDINE WITH COMBINED SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITION FOR THE TREATMENT OF NEUROPATHIC PAIN

Номер: US20130190352A1
Принадлежит: H. Lundbeck A/S

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain. 2. The compound according to claim 1 , which compound is the HBr addition salt.34-. (canceled)5. The compound according to claim 1 , which compound is the DL-lactic acid addition salt.67-. (canceled)8. The compound according to claim 1 , which compound is the glutaric acid addition salt (1:1).910-. (canceled)11. The compound according to claim 1 , which compound is the malonic acid addition salt (1:1).12. The compound according to claim 11 , which compound is characterized by peaks in an XRPD at 10.77° claim 11 , 16.70° claim 11 , 19.93° and 24.01°2θ claim 11 , or at 6.08° claim 11 , 10.11° claim 11 , 18.25° and 20.26°2θ.1310. The compound according to claim 11 , which compound is characterised by an XRPD as depicted in or .14. The compound according to which compound is L-aspartic acid addition salt (1:1) or L-aspartic acid addition salt hydrate (1:1).15. The compound according to which compound is glutamic acid addition salt (1:1) or glutamic acid addition salt monohydrate.16. (canceled)17. A pharmaceutical composition comprising a compound according to together with a pharmaceutically acceptable excipient.18. A method of treating a disease selected from chronic pain claim 1 , depression in partial responders claim 1 , treatment resistant depression claim 1 , Alzheimer's disease claim 1 , cognitive impairment claim 1 , ADHD claim 1 , melancholia claim 1 , PTSD claim 1 , hot flushes claim 1 , sleep apnea claim 1 , alcohol claim 1 , nicotine or carbohydrate craving claim 1 , substance abuse claim 1 , alcohol or drug abuse claim 1 , emesis claim 1 , eating disorders claim 1 , IBS claim 1 , affective disorders claim 1 , depression claim 1 , major depressive disorder claim 1 , postnatal depression claim 1 , depression associated with bipolar disorder claim 1 , Alzheimer's disease claim 1 , psychosis or Parkinson's disease claim ...

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25-07-2013 дата публикации

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

Номер: US20130190404A1

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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08-08-2013 дата публикации

Oxidized Lipid Compounds and Uses Thereof

Номер: US20130203707A1
Принадлежит: Vascular Biogenics Ltd

Novel oxidized lipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions.

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08-08-2013 дата публикации

Polymeric biomaterials derived from phenolic monomers and their medical uses

Номер: US20130203713A1
Принадлежит: Rutgers State University of New Jersey

The present invention provides new classes of phenol compounds, including those derived from tyrosol and analogues, useful as monomers for preparation of biocompatible polymers, and biocompatible polymers prepared from these monomeric phenol compounds, including novel biodegradable and/or bioresorbable polymers. These biocompatible polymers or polymer compositions with enhanced bioresorbabilty and processibility are useful in a variety of medical applications, such as in medical devices and controlled-release therapeutic formulations. The invention also provides methods for preparing these monomeric phenol compounds and biocompatible polymers.

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08-08-2013 дата публикации

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

Номер: US20130203727A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). 2. The compound of wherein Ris (C-C)alkyl claim 1 , (C-C)alkenyl or —O(C-C)alkyl wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claim 1 , halo claim 1 , oxo and —CN; and wherein Ris H.4. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —OH, —O(C-C)alkyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo;'}{'sub': 3', '14', '3', '14', '3', '7, 'sup': 1', '1, 'b) (C-C)carbocycle, wherein (C-C)carbocycle is optionally substituted with one or more Zgroups, wherein two Zgroups together with the atom or atoms to which they are attached optionally form a (C-C)carbocycle or heterocycle; and'}{'sup': 7', '1, 'c) aryl, heteroaryl and fused-heterocycle, wherein any aryl, heteroaryl and fused-heterocycle is substituted with one or more Zgroups and optionally substituted with one or more Zgroups.'}5. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and ...

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08-08-2013 дата публикации

Ionic Viscoelastics and Viscoelastic Salts

Номер: US20130204010A1
Принадлежит: Boston University

One embodiment of the present invention relates to ionic liquids and ionic viscoelastics formed between [1] a small molecule or macromolecule containing two or more cations; and [2] a small molecule or macromolecule containing two or more anions. Another embodiment of the invention is the use of the inventive ionic liquids and ionic viscoelastics, formed between a small molecule or macromolecule containing two or more cations and a small molecule or macromolecule containing two or more anions, to form a crosslinked network. In certain embodiments, the ionic liquids formed can be viscous liquids, viscous liquid formed networks, or viscoelastic networks/gels. In certain embodiments, the ionic material of the invention may be used for a variety of applications including, but not limited to, lubricants, additives, gas separation, liquid separation, membranes, fuel cells, sensors, batteries, coatings, heat storage, liquid crystals, biocompatible fluids, solvents, and electronic materials.

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15-08-2013 дата публикации

Compositions and Methods for Imaging

Номер: US20130209360A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.

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22-08-2013 дата публикации

Compounds and Compositions for the Treatment of Cancer

Номер: US20130217645A1
Принадлежит: PROMETIC BIOSCIENCES INC.

New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil. 130-. (canceled)37. The method of claim 31 , wherein the pharmaceutically acceptable salt is a base addition salt.38. The method of claim 37 , wherein the base addition salt comprises a metal counterion selected from sodium claim 37 , potassium claim 37 , magnesium claim 37 , calcium and lithium.39. The method of claim 38 , wherein the metal counterion is sodium.41. The method of claim 40 , wherein the compound is Compound I claim 40 , II claim 40 , VIII claim 40 , XIII claim 40 , XV claim 40 , XVII claim 40 , XVIII claim 40 , XIX or XX.42. The method of claim 40 , wherein the compound is Compound I claim 40 , II claim 40 , XV claim 40 , XVII or XIX.43. The method of claim 31 , wherein said subject is a human patient.44. The method of claim 31 , wherein the cancer is bladder cancer claim 31 , breast cancer claim 31 , colorectal cancer claim 31 , kidney cancer claim 31 , melanoma claim 31 , non-Hodgkin's lymphoma claim 31 , leukemia claim 31 , ovarian cancer claim 31 , pancreatic cancer claim 31 , prostate cancer or uterine cancer.45. The method of claim 31 , wherein the cancer is breast cancer claim 31 , colorectal cancer claim 31 , leukemia cancer claim 31 , melanoma cancer or pancreatic cancer.46. The method of claim 31 , wherein the compound is used in combination with an anticancer agent.47. The method of claim 46 , wherein ...

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29-08-2013 дата публикации

Phenylketone Carboxylate Compounds and Pharmaceutical Uses Thereof

Номер: US20130225681A1
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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29-08-2013 дата публикации

Process for the preparation of lubiprostone

Номер: US20130225842A1
Принадлежит: Individual

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

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05-09-2013 дата публикации

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

Номер: US20130228332A1
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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05-09-2013 дата публикации

Novel Intermediate for Preparing Tapentadol or Analogues Thereof

Номер: US20130231478A1
Принадлежит:

The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production. 2. The compound according to claim 1 , wherein Ris selected from Cl claim 1 , methyl claim 1 , OH claim 1 , NHor methoxy.3. The compound according to claim 1 , characterized in that Y is selected from OR claim 1 , wherein Ris selected from methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl.4. The compound according to claim 1 , characterized in that Y is selected from NRR claim 1 , wherein R claim 1 , Rand N form substituted or unsubstituted saturated nitrogen-containing heteorcyclyl containing oxygen or not jointly.5. The compound according to claim 4 , wherein R claim 4 , Rand N form tetrahydropyrrole ring claim 4 , piperidine ring claim 4 , 4-methylpiperidine ring claim 4 , morpholine ring claim 4 , methylpiperazine ring or 4-hydroxypiperidine jointly.6. The compound according to claim 1 , selected from the following compounds:valeryl 2-methyl-3-(3-methoxyphenyl)chloride;methyl 2-methyl-3-(3-methoxyphenyl)sulfovalerate;methyl 2-methyl-3-(3-hydroxyphenyl) ulfovalerate;2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-methoxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-diethyl-2-methyl-3-(3-methoxyphenyl)valeramide;3-(3-methoxyphenyl)-2-methyl-1-(piperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-(4-methylpiperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-(morpholin-1-yl)pentan- ...

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26-09-2013 дата публикации

LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS AND THEIR USE IN THE TREATMENT FIBROSIS

Номер: US20130253004A1
Принадлежит: Amira Pharmaceuticals, Inc.

Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. 2. The compound of claim 1 , wherein:{'sup': 1', 'D', '10', '9', '10, 'sub': 2', '2', '2', '2', '2', '2', '2', '3, 'Ris —COH, —COR, —C(═O)NHSOR, —C(═O)N(R), —SONHC(═O)R, —CN, —C(═O)NHCHCHSOH, tetrazolyl or 5-oxo-2,5-dihydro-[1,2,4]oxadiazol-3-yl;'}{'sup': '1', 'sub': 1', '6', '3', '6', '1', '4', '3', '6', '3', '6', '1', '4, 'Lis absent, C-Calkylene, —C-Ccycloalkylene-, —C-Calkylene-C-Ccycloalkylene-, or —C-Ccycloalkylene-C-Calkylene-;'}ring A is phenyl furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl.{'sup': '3', 'sub': 1', '4, 'Ris H or C-Calkyl;'}{'sup': 2', '2', '2', 'C, 'sub': 3', '6, 'Ris substituted or unsubstituted C-Ccycloalkyl, a substituted or unsubstituted phenyl, or a substituted or unsubstituted monocyclic heteroaryl, wherein if Ris substituted then Ris substituted with 1, 2 or 3 R;'}n is 0 or 1;p is 0 or 1.3. The compound of wherein:{'sup': 1', 'D', '10, 'sub': 2', '2', '2, 'Ris —COH, —COR, or —C(═O)NHSOR;'}{'sup': '1', 'sub': 2', '3', '3', '2', '2', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Lis absent, —CH—, —CH(CH)—, —C(CH)—, —CH(CHCH)—, —C(CHCH)—, —CHCH—, —CHCHCH—, cyclopropyl-1,1-diyl, cyclopropyl-1,2-diyl, cycloprop-2-enyl-1,1-diyl, cyclobutyl-1,1-diyl, cyclopentyl-1,1-diyl, cyclohexyl-1,1-diyl, —C(CHCH)CH— or —CHC(CHCH);'}{'sup': 2', '2', '2', 'C, 'Ris a substituted or unsubstituted phenyl, wherein if Ris substituted then Ris substituted with 1, 2 or 3 R.'}5. The compound of wherein:{'sup': 2', '2', '2', '12', '12, 'sub': 3', '6', '3', '6', '3', ...

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03-10-2013 дата публикации

COMPOUNDS AND METHOD FOR REDUCING URIC ACID

Номер: US20130259850A1
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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03-10-2013 дата публикации

NITRIC OXIDE AND ITS BIOMEDICAL SIGNIFICANCE

Номер: US20130261146A1

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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03-10-2013 дата публикации

Compounds and methods for delivery of prostacyclin analogs

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

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

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10-10-2013 дата публикации

Process to prepare treprostinil, the active ingredient in remodulin®

Номер: US20130267734A1
Принадлежит: United Therapeutics Corp

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

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17-10-2013 дата публикации

DERIVATIVES FOR PERFLUOROALKOXY SULFOSUCCINATES AS SURFACTANTS

Номер: US20130269568A1
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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17-10-2013 дата публикации

FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20130274240A1
Принадлежит:

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: 217.-. (canceled)18. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.1923.-. (canceled)24. A method of inhibiting PDHK in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.25. A method of inhibiting PDHK2 in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.26. A method of decreasing the blood glucose level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.27. A method of decreasing lactate level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.28. A method for the treatment or prophylaxis of diabetes claim 1 , diabetic complications claim 1 , insulin resistance syndrome claim 1 , metabolic syndrome claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , atherosclerosis claim 1 , ...

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17-10-2013 дата публикации

Guerbet Alcohols and Methods for Preparing and Using Same

Номер: US20130274511A1
Принадлежит:

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

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24-10-2013 дата публикации

Compounds for the treatment of metabolic disorders

Номер: US20130281705A1
Автор: Shalini Sharma
Принадлежит: Wellstat Therapeutics Corp

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

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31-10-2013 дата публикации

SALTS OF KUKOAMINE B, PREPARATION METHOD AND USE THEREOF

Номер: US20130289112A1

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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31-10-2013 дата публикации

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

Номер: US20130289117A1
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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07-11-2013 дата публикации

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

Номер: US20130295185A1
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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07-11-2013 дата публикации

3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS

Номер: US20130296358A1
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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07-11-2013 дата публикации

Novel Dihydroxybenzene Derivatives and Antiprotozoal Agent Comprising Same as Active Ingredient

Номер: US20130296422A1
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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07-11-2013 дата публикации

PHENYLGLYOXYLIC ACID DERIVATIVES AND THEIR PREPARATION AND USE

Номер: US20130296599A1
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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14-11-2013 дата публикации

Drug Loaded Polymeric Nanoparticles and Methods of Making and Using Same

Номер: US20130302432A1
Принадлежит: Bind Therapeutics Inc

The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

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19-12-2013 дата публикации

Pharmaceutically Acceptable Salts of Quinolinone Compounds Having Improved Pharmaceutical Properties

Номер: US20130338171A1
Принадлежит: NOVARTIS AG

A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R-Rand R-Rare as defined herein 1. A lactate salt of 4-amino-5-tluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one.2. The lactate salt of claim 1 , wherein the salt comprises the mono-lactate or bis-lactate salt.3. The lactate salt of claim 1 , wherein the salt comprises the mono-lactate salt.4. The lactate salt of claim 1 , wherein the solubility of the salt in water at 22° C. is greater than 30 mg/mL.5. The lactate salt of claim 1 , wherein the solubility of the salt in water at 22° C. is from about 150 mg/mL to about 250 mg/mL.6. The lactate salt of claim 1 , wherein the salt comprises the DL lactate salt.7. The lactate salt of claim 1 , wherein the salt comprises the D lactate salt.8. The lactate salt of claim 1 , wherein the salt comprises the L lactate salt.9. The lactate salt of claim 1 , wherein the salt comprises the D lactate salt claim 1 , the L lactate salt claim 1 , or a mixture thereof.10. The lactate salt of claim 1 , wherein the salt comprises plate-shaped crystals.11. A composition comprising a tablet of the lactate salt of .12. A method of preparing the lactate salt of claim 1 , comprising:(a) Suspending 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one in a solvent or mixture of solvents;(b) Contacting lactic acid with 4-amino-5-fluoro-3-[6-(4-methylpiperzain-1-O-1H-benzimidazol-2-yl]quinolin-2(1H)-one to provide a mixture;(c) Heating the mixture;(d) Cooling the mixture; and(e) Isolating the salt.13. The method of claim 12 , wherein the solvent is a protic solvent.14. The method of claim 12 , wherein the solvent is selected from the group consisting of methanol claim 12 , ethanol claim 12 , water claim 12 , tetrahydrofuran claim 12 , and mixtures thereof.15. A pharmaceutical formulation claim 1 , comprising the lactate salt of and a pharmaceutically acceptable ...

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19-12-2013 дата публикации

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

Номер: US20130338366A1
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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19-12-2013 дата публикации

Prostaglandin synthesis and intermediates for use therein

Номер: US20130338379A1
Принадлежит: Alphora Research Inc

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

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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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19-12-2013 дата публикации

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

Номер: US20130338395A1
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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26-12-2013 дата публикации

Compositions and Methods for Modification of Biomolecules

Номер: US20130344527A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

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26-12-2013 дата публикации

Methods of treatment using lipid compounds

Номер: US20130345269A1
Принадлежит: Individual

Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): or a pharmaceutically acceptable salt, or ester thereof, wherein R 1 and R 2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C 1 -C 6 alkyl groups, with the proviso that R 1 and R 2 are not both hydrogen or a pharmaceutically acceptable salt or ester thereof. Such diseases or conditions may relate to coronary heart disease (CHD), for example atherosclerosis; metabolic syndrome/insulin resistance; and/or a dyslipidemic condition such as hypertriglyceridemia (HTG), elevated LDL-cholesterol, elevated total-cholesterol, elevated Apo B and low HDL-cholesterol. The present disclosure further provides for a method of reducing atherosclerosis development. Pharmaceutical compositions comprising a compound of Formula (I) are also disclosed.

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26-12-2013 дата публикации

Ferric organic compounds, uses thereof and methods of making same

Номер: US20130345460A1
Принадлежит: Panion and 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.

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16-01-2014 дата публикации

Use Of 2,5-Dihydroxybenzene Compounds And Derivatives For The Treatment Of Rosacea

Номер: US20140018330A1
Принадлежит: AmDerma Pharmaceuticals LLC

The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.

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16-01-2014 дата публикации

FERRIC ORGANIC COMPOUNDS, USES THEREOF AND METHODS OF MAKING SAME

Номер: US20140018420A1
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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16-01-2014 дата публикации

PROCESS FOR PRODUCING GLYCOLIC ACID

Номер: US20140018514A1
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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30-01-2014 дата публикации

INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES

Номер: US20140031338A1
Принадлежит: LABORATOIRE BIODIM

The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. 2. A compound according to claim 1 , wherein Rrepresents hydrogen.3. A compound according to claim 1 , wherein Rrepresents hydrogen.1118-. (canceled)19. A pharmaceutical composition comprising a compound according to as an active ingredient and at least a pharmaceutically acceptable carrier.20. A pharmaceutical composition according to further comprising a further antiviral agent.2123-. (canceled)24. A method of treatment or prevention of a viral infection comprising administering a compound according to to a patient in need thereof.25. The method according to wherein said viral infection is a retroviral infection.26. The method according to wherein said retroviral infection is HIV.27. A method for the treatment of an HIV infection in a mammal being infected or having a risk to be infected by the HIV comprising administering the pharmaceutical composition according to .28. A method of inhibiting the replication of HIV comprising exposing said HIV to an effective amount of a compound according to under conditions where replication of HIV is inhibited. The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. The present invention also relates to methods for the preparation of such compounds. The present invention also relates to pharmaceutical compositions comprising such compounds. The present invention also relates to the treatment of viral infections by the administration of a therapeutically efficient amount of such compounds.The Acquired Immuno Deficiency Syndrome (AIDS) is a disease due to infection by the Human Immunodeficiency Virus (HIV). HIV is a retrovirus, belonging to the subclass of primate lentiviruses. Two types of HIV have been identified, HIV-1 and HIV-2. HIV-1 is responsible for the larger part of the AIDS global epidemic in the world, with virtually every ...

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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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13-02-2014 дата публикации

Substituted n-pentanamide compounds, preparation method and the use thereof

Номер: US20140046074A1
Принадлежит:

The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process. 2. The (2R claim 1 ,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compound according to claim 1 , wherein R and the phenolic hydroxyl group form an ether group or an ester group; wherein R is selected from C1-C6 linear or branched alkyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted arylalkyl claim 1 , alkylsilyl claim 1 , C1-C6 alkoxymethyl claim 1 , C1-C6 alkyloyl claim 1 , substituted or unsubstituted aryloyl; wherein the substituent is hydroxy claim 1 , halogen claim 1 , C1-C6 alkyl or C1-C6 alkoxy; said aryl is phenyl or naphthyl;wherein X is O; and Y is O;{'sub': '1', 'wherein Ris C1-C6 alkyl group, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, wherein the substituent on phenyl or benzyl is 1 to 3 substituent(s) selected from hydroxy, halogen, C1-C6 alkyl and C1-C6 alkoxy;'}{'sub': 2', '3, 'wherein Rand Rare each independently selected from H, C1-C6 alkyl and phenyl.'}3. The (2R claim 2 ,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compound according to claim 2 ,wherein R is benzyl, methyl, t-butyl, triphenylmethyl, methoxymethyl, trimethylsilyl, t-butyldimethylsilyl, acetyl or benzoyl;wherein X is O; and Y is O;{'sub': '1', 'wherein Ris phenyl; phenyl substituted with 1 to 3 substituent(s) selected from hydroxy, halogen, C1-C6 alkyl and C1-C6 alkoxy; benzyl;'}{'sub': 2', '3, 'wherein Rand Rare each independently selected from H, C1-C6 alkyl and phenyl.'}6. The method according to claim 5 , wherein claim 5 ,said hydrocarbylation agent is any one of methyl ...

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27-02-2014 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20140057879A1
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.

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27-02-2014 дата публикации

Ionic Viscoelastics and Viscoelastic Salts

Номер: US20140058047A1
Принадлежит: TRUSTEES OF BOSTON UNIVERSITY

One embodiment of the present invention relates to ionic liquids and ionic viscoelastics formed between [1] a small molecule or macromolecule containing two or more cations; and [2] a small molecule or macromolecule containing two or more anions. Another embodiment of the invention is the use of the inventive ionic liquids and ionic viscoelastics, formed between a small molecule or macromolecule containing two or more cations and a small molecule or macromolecule containing two or more anions, to form a crosslinked network. In certain embodiments, the ionic liquids formed can be viscous liquids, viscous liquid formed networks, or viscoelastic networks/gels. In certain embodiments, the ionic material of the invention may be used for a variety of applications including, but not limited to, lubricants, additives, gas separation, liquid separation, membranes, fuel cells, sensors, batteries, coatings, heat storage, liquid crystals, biocompatible fluids, solvents, and electronic materials. 2. The salt of claim 1 , wherein Y is —[CO].3. The salt of claim 1 , wherein X and W are the same.5. The salt of claim 1 , wherein R is a bond to W or is selected claim 1 , independently for each occurrence claim 1 , from the group consisting of hydrogen or alkyl.6. The salt of claim 1 , wherein said cationic component is W—[Z].7. The salt of claim 6 , wherein said anionic component is X—[Y]; X is C(R′)(A-) claim 6 , C(R′)[(AO)A-] claim 6 , C(R′)[(ANH)A-] claim 6 , N(A) claim 6 , N[(AO)A-] claim 6 , or N[(ANH)A-]; A is claim 6 , independently for each occurrence claim 6 , —(CQ)-; Q is claim 6 , independently for each occurrence claim 6 , hydrogen or methyl; p is claim 6 , independently for each occurrence claim 6 , 0-40 inclusive; and R′ is hydrogen claim 6 , halogen claim 6 , azide claim 6 , alkyl claim 6 , aralkyl claim 6 , alkenyl claim 6 , alkynyl claim 6 , cycloalkyl claim 6 , hydroxyl claim 6 , alkoxy claim 6 , aryloxy claim 6 , aryl claim 6 , heteroaryl claim 6 , heteroaralkyl ...

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27-02-2014 дата публикации

ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES

Номер: US20140058125A1
Принадлежит: Syddansk Universitet

There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels. 2. The compound of claim 1 , wherein X is —C(RR)—.3. The compound of claim 1 , wherein R claim 1 , Rand Rare independently selected from hydrogen and (C-C)alkyl.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of wherein Rand Rare hydrogen.6. The compound of claim 1 , wherein Ris hydrogen.7. The compound of claim 1 , wherein n is 1 and Ar is selected from the group consisting of an optionally substituted phenyl claim 1 , 2-pyridyl claim 1 , 3-pyridyl claim 1 , 4-pyridyl claim 1 , 2-thienyl claim 1 , 3-thienyl claim 1 , 2-thiazolyl claim 1 , 4-thiazolyl claim 1 , 5-thiazolyl claim 1 , 4-thiazolyl claim 1 , 2-furyl claim 1 , 3-furyl claim 1 , 2-oxazolyl claim 1 , 4-oxazolyl claim 1 , 5-oxazolyl claim 1 , 3-pyrrolyl claim 1 , 1-pyrrazolyl claim 1 , 2-pyrrazolyl claim 1 , 3-pyrrazolyl claim 1 , 2-pyrimidyl claim 1 , 4-pyrimidyl claim 1 , 5-pyrimidyl claim 1 , 4-triazolyl claim 1 , 5-tetrazolyl claim 1 , 2-naphthyl claim 1 , 3-naphthyl claim 1 , 2-quinolyl claim 1 , 3-quinolyl claim 1 , 4-quinolyl claim 1 , 5-quinolyl claim 1 , 6-quinolyl claim 1 , 7-quinolyl claim 1 , 8-quinolyl claim 1 , 2-benzothiazolyl claim 1 , 4-benzothiazolyl claim 1 , 5-benzothiazolyl claim 1 , 6-benzothiazolyl claim 1 , 7-benzothiazolyl claim 1 , 1-indolyl claim 1 , 2-indolyl claim 1 , 3-indolyl claim 1 , 4-indolyl claim 1 , 5-indolyl claim 1 , 6-indolyl and 7-indolyl.8. The compound of claim 1 , wherein n is 1 and Ar is phenyl.9. The compound of claim 1 , wherein n is 1 and Ar is 4-pyridyl.10. The compound of ...

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06-03-2014 дата публикации

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

Номер: US20140066460A1
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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20-03-2014 дата публикации

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

Номер: US20140080875A1
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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03-04-2014 дата публикации

Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20140094465A1
Принадлежит:

The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 1. What is claimed is: {'br': None, 'sub': 1', '2, 'HO-Cy-linker-Cy-acidic moiety\u2003\u2003Formula 1'}, 'A method of inhibiting GSNOR in a patient in need thereof by administering an effective amount of a compound of Formula 1 or a pharmaceutically acceptable salt thereofwherein{'sub': '1', 'Cyis selected from the group consisting of substituted and unsubstituted monocyclic aryl, substituted and unsubstituted bicyclic aryl, substituted and unsubstituted monocyclic heterocycle, substituted and unsubstituted bicyclic heterocycle, substituted and unsubstituted monocyclic heteroaryl, substituted and unsubstituted bicyclic heteroaryl, substituted and unsubstituted monocyclic cycloalkyl, and substituted and unsubstituted bicyclic cycloalkyl;'}{'sub': 2', '5', '6', '7', '2', '3', '2', '3', '2', '3', '5', '6', '1', '6', '1', '6', '1', '6', '7', '1', '6', '1', '6', '1', '6', '2', '3', '2', '3', '2', '3', '1', '3', '1', '3', '1', '3', '1', '8', '1', '8', '1', '8, 'linker is selected from the group consisting of a direct bond, O, S, SO, SO, C═O, CRR, NR, substituted and unsubstituted (C-C) alkyl, substituted and unsubstituted (C-C) heteroalkyl, substituted and unsubstituted (C-C) alkene, substituted and unsubstituted 5 or 6 membered aryl, substituted and unsubstituted 5 or 6 membered heteroaryl, substituted and unsubstituted 3-6 membered cycloalkyl, and substituted and unsubstituted 3-6 membered saturated heterocyclyl; wherein Rand Rare independently selected from the group consisting of hydrogen, (C-C) alkyl, (C-C) heteroalkyl, halogen, (C-C) haloalkyl, cyano, and hydroxyl; Ris selected from the group consisting of hydrogen, (C-C)alkyl, (C-C) haloalkyl, and (C-C) heteroalkyl; substitutions for the (C-C) alkyl, (C-C) heteroalkyl, and (C-C) alkene are selected from the group ...

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10-04-2014 дата публикации

CONTROLLED RELEASE OF BIOLOGICALLY ACTIVE COMPOUNDS

Номер: US20140099370A1
Автор: Bezwada Rao S
Принадлежит: BEZWADA BIOMEDICAL, LLC

The present invention relates to biodegradable polymers (e.g., polyesters and polyester amides) derived from functionalized biologically active compounds that can provide site specific delivery of bioactive compounds upon biodegradation in a controlled manner. 1. A biodegradable polyamide ester of formula VIII or IX , or a pharmaceutically acceptable salt thereof: {'br': None, 'sup': 1', '1', '2', '2, 'sub': c', '9', 'd', 'a', '2', '10', '2', 'b', 'o, '—[(X)—O(O═)C—R—C(═O)O—(Y)—(Y)—CH(O═)C—NH—R—NH—C(═O)CH—(X)]—\u2003\u2003VIII'}, '(C)'} [{'br': None, 'sup': 1', '1, 'sub': c', '9', 'd, 'H—(X)—O(O═)C—R—C(═O)O—(Y)—H\u2003\u2003Va'}, {'br': None, 'sub': 11', 'a', '2', '10', '2', 'b', '12, 'sup': 2', '2, 'R—(Y)—CH(O═)C—NH—R—NH—C(═O)CH—(X)—R\u2003\u2003VII;'}], 'wherein the polyamide ester of formula VIII is formed by condensation polymerization of monomers of formula Va and VII {'br': None, 'sub': a', '1', 'b', 'a', '2', '10', '2', 'b', 'p, 'sup': 2', '2, '—[(X)—O—R—O—(Y)—(Y)—CH(O═)C—NH—R—NH—C(═O)CH—(X)]—\u2003\u2003IX'}, '(D)'} [{'br': None, 'sub': a', '1', 'b, 'H—(X)—O—R—O—(Y)—H\u2003\u2003I'}, {'br': None, 'sub': 11', 'a', '2', '10', '2', 'b', '12, 'sup': 2', '2, 'R—(Y)—CH(O═)C—NH—R—NH—C(═O)CH—(X)—R\u2003\u2003VII;'}], 'wherein the polyamide ester of formula IX is formed by condensation polymerization of monomers of formula I and VII o and p are each independently an integer from about 5 to about 1000;', {'sub': 1', '9, 'Rand Rare each independently the remaining portion of a biologically active compound;'}, {'sub': '10', 'Ris the remaining portion of a biologically active compound or non-biologically active compound;'}, {'sub': 11', '12, 'Rand Rare each independently selected from Cl, F, Br, and I;'}, {'sup': 1', '2, 'sub': 2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', 'y', '2', '2', '2', 'z, 'X, Xand Xare independently at each occurrence —OC(═O)CH— (inverse glycolic acid moiety), —OC(═O)CH(CH)— (inverse lactic acid moiety), —OC(═O)CHOCHCH— (inverse dioxanone ...

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10-04-2014 дата публикации

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

Номер: US20140100278A1
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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02-01-2020 дата публикации

TOPICAL FORMULATION OF HYPERBRANCHED POLYGLYCEROL-COATED PARTICLES THEREOF

Номер: US20200000687A1
Принадлежит:

Core-shell particles have a hydrophobic core and a shell formed of or containing hyperbranched polyglycerol (HPG). The HPG can be covalently bound to the one or more materials that form the core or coated thereon. The HPG coating can be modified to adjust the properties of the particles. For example, unmodified HPG coatings impart stealth properties to the particles which resist non-specific protein absorption. Alternatively, the hydroxyl groups on the HPG coating can be chemically modified to form functional groups that react with functional groups on tissue or otherwise interact with tissue to adhere the particles to the tissue, cells, or extracellular materials, such as proteins. Such functional groups include, but not limited to, aldehydes, amines, and O-substituted oximes. Topical formulation for application to the skin contain these HPG coated nanoparticles. In some embodiments, the particles include therapeutic, diagnostic, nutraceutical, and/or prophylactic agents such as those used as sunblock compositions. 114-. (canceled)15. A method of adhering particles to a tissue , the method comprising administering particles a comprising:a hydrophobic polymer core and a shell comprising hyperbranched polyglycerol covalently bound to the hydrophobic polymer of the hydrophobic polymer core;wherein the hyperbranched polyglycerol is functionalized with one or more reactive functional groups, or functional groups having tissue targeting moieties bound thereto, or a combination thereof, whereinthe one or more reactive functional groups and the functional groups having tissue targeting moieties bound thereto adhere to tissue, cells, or proteins; andone or more agents selected from agents protecting the skin from ultraviolet light, therapeutic agents, diagnostic agents, prophylactic agents, and combinations thereof;wherein the one or more agents are encapsulated within the particles, associated with the surface of the particles, or a combination thereof.16. The method of ...

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07-01-2021 дата публикации

NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES

Номер: US20210000964A1
Принадлежит:

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: 124-. (canceled)26. The compound according to claim 25 , or an amide claim 25 , ester or pharmaceutically acceptable salt thereof claim 25 , wherein the compound is of Formula A1 wherein at least one of Rand Ris COH.29. A peptide selected from MH(199-308)hGDF15 (SEQ ID NO: 4) claim 25 , MHA(200-308)hGDF15 (SEQ ID NO: 6) claim 25 , AHA(200-308)hGDF15 (SEQ ID NO: 7) claim 25 , AH(199-308)hGDF15 (SEQ ID NO: 5) claim 25 , MHHHHHHM-hGDF15 (SEQ ID NO: 2) and MHHHHHH-hGDF15 (SEQ ID NO: 1). This application is a divisional application of U.S. application Ser. No. 15/985,060, filed on May 21, 2018, now allowed, which is a divisional of Ser. No. 14/738,272, filed on Jun. 12, 2015, now U.S. Pat. No. 10,588,980, which claims priority to, and the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Application No. 62/107,016, filed Jan. 23, 2015, U.S. Provisional Application No. 62/082,327, filed on Nov. 20, 2014, and U.S. Provisional Application No. 62/015,862 filed on Jun. 23, 2014, the entire contents of each of which are incorporated herein by reference in their entireties.The contents of the text file named “PAT056274-US-DIV02_Sequence Listing_ST25.txt,” which was created on May 26, 2020 and is 33 KB in size, are hereby incorporated by reference in their entireties.The present invention relates to novel conjugates of GDF15 which have improved half-life and duration of action, method of making them and using them. The invention further relates to novel fatty acids and their use in extending the half-life of biomolecules via conjugation.Peptides and proteins are widely used in medical practice, and since they can be produced by recombinant DNA technology it can be expected that their importance will increase also in the years to come. The number of known endogenous peptides and proteins with interesting biological ...

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07-01-2016 дата публикации

Phenylglyoxylic acid derivatives and their preparation and use

Номер: US20160002142A1
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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07-01-2016 дата публикации

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

Номер: US20160002165A1
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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04-01-2018 дата публикации

Hypdh inhibitors and methods of use for the treatment of kidney stones

Номер: US20180002275A1

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).

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02-01-2020 дата публикации

METHOD FOR THE PRODUCTION OF 2,4-DIHYDROXYBUTYRIC ACID

Номер: US20200002260A1
Принадлежит: DFI USA, LLC

Methods for the production of 2,4-dihydroxybutyrate (2,4-DHB) from erythrose and other four-carbon sugars are disclosed. The improved methods facilitate the production of 2,4-DHB that is a precursor for biorenewable and animal nutrition chemicals among others. 1. A method of producing 2 ,4-dihydroxybutyrate , comprising: mixing a four carbon sugar and a hydroxide salt in solution , wherein the four carbon sugar is erythrulose.2. The method of claim 1 , wherein the temperature of the solution is maintained below 100° C.3. The method of claim 1 , wherein the four carbon sugar is diluted sufficiently to result in a molar yield of DHB that is greater than 40%.4. The method of claim 1 , wherein the four carbon sugar is diluted with a solution containing DHB.5. The method of claim 1 , wherein the method is performed in a continuous reactor system.6. The method of claim 1 , wherein the hydroxide concentration of the solution is between 0.1 M and 4 M.7. The method of claim 6 , wherein the temperature of the solution is maintained below 100° C.8. The method of claim 7 , wherein the four carbon sugar is diluted with a solution containing DHB.9. The method of claim 1 , further comprising removing oxygen from the solution.10. The method of claim 9 , wherein oxygen is removed by venting the solution with a gas selected from the group consisting of: nitrogen claim 9 , argon claim 9 , and mixtures thereof.11. The method of claim 9 , wherein oxygen is removed by venting the solution with hydrogen.12. The method of claim 11 , wherein the temperature of the solution is maintained below 100° C.13. The method of claim 12 , wherein the erythrulose is diluted with a solution containing one or more other organic acid salts.14. The method of claim 13 , wherein the method is performed in a continuous reactor system.15. A method of producing 2 claim 13 ,4-dihydroxybutyrate claim 13 , comprising:mixing a four carbon sugar and a hydroxide salt in solution; andremoving oxygen from the solution ...

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07-01-2021 дата публикации

Substituted Aromatic Compounds and Pharmaceutical Uses Thereof

Номер: US20210002202A1
Принадлежит:

The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders. 2. The method of claim 1 , wherein Ris straight chain Calkyl claim 1 , Calkyl claim 1 , or C-Calkenyl; and Ris H claim 1 , halogen claim 1 , haloalkyl claim 1 , or OR.3. The method of claim 1 , wherein Ris independently chosen from: H claim 1 , halogen claim 1 , haloalkyl claim 1 , straight chain C-Calkyl claim 1 , or OR; and Ris independently chosen from: H claim 1 , halogen claim 1 , haloalkyl claim 1 , C-Calkyl claim 1 , or OR.4. The method of claim 1 , wherein Ris OR.5. The method of claim 1 , wherein the pharmaceutically acceptable salt is a base addition salt.6. The method of claim 5 , wherein the base addition salt is a metal counterion.7. The method of claim 6 , wherein the metal counterion is sodium claim 6 , magnesium claim 6 , calcium claim 6 , potassium or lithium.8. The method of claim 7 , wherein the metal counterion is sodium.11. The method of claim 1 , wherein the inflammatory-related disease is an immune mediated inflammatory disease or an autoimmune disease.12. The method of claim 1 , wherein the inflammatory-related disease is an autoimmune disease.13. The method of claim 1 , wherein the inflammatory-related disease is selected from the group consisting of arthritis claim 1 , systemic lupus erythematosus (SLE) claim 1 , ITP claim 1 , glomerulonephritis claim 1 , vasculitis claim 1 , psoriatic arthritis claim 1 , psoriasis claim 1 , Crohn's disease claim 1 , inflammatory bowel disease claim 1 , ankylosing spondylitis claim 1 , Sjögren's syndrome claim 1 , Still's disease ...

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07-01-2021 дата публикации

NOVEL CRYSTALLINE FORMS OF TAMIBAROTENE FOR TREATMENT OF CANCER

Номер: US20210002209A1
Принадлежит:

Synthesis and characterization of novel tamibarotene forms suitable for pharmaceutical compositions in drug delivery systems to treat human or warm-blooded mammal diseases. 1. A crystalline form of tamibarotene selected from the group consisting of: tamibarotene:adipic acid , tamibarotene:DL-aspartic acid , tamibarotene:acetylsalicylic acid , tamibarotene:biphenyl-4-carboxylic acid , tamibarotene:caffeic acid , tamibarotene:decanoic acid , tamibarotene:diphenic acid , tamibarotene:gallic acid , tamibarotene:fumaric acid , tamibarotene:ibuprofen , tamibarotene:maleic acid , tamibarotene:nicotinamide , tamibarotene:isonicotinamide , tamibarotene:citric acid , tamibarotene:nicotinic acid , tamibarotene:3 ,4-dihydroxybenzoic acid , tam ibarotene:glutaric acid , and tamibarotene:L-malic acid.2. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:adipic acid.3. The crystalline form of claim 2 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 10.5 claim 2 , 12.0 claim 2 , 14.5 claim 2 , 22.0 claim 2 , and 26.0° 2θ±0.2° 2θ.4. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:DL-aspartic acid.5. The crystalline form of claim 4 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 6.5 claim 4 , 10.0 claim 4 , 11.5 claim 4 , and 19.5° 2θ±0.2° 2θ.6. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:acetylsalicylic acid.7. The crystalline form of claim 6 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 8.0 claim 6 , 8.5 claim 6 , 15.5 claim 6 , 23.0 claim 6 , and 27.0° 2θ±0.2° 2θ.8. The crystalline ...

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02-01-2020 дата публикации

Systems and processes for polyacrylic acid production

Номер: US20200002446A1
Автор: Sadesh H. SOOKRAJ
Принадлежит: Novomer Inc

Disclosed are systems and methods for the production of polyacrylic acid and superabsorbent polymers from ethylene oxidation to form ethylene oxide. Reacting the ethylene oxide with carbon monoxide to form to beta propiolactone (BPL) or polypropiolactone (PPL), or a combination thereof. An outlet configured to provide a carbonylation stream comprising the BPL or PPL, or a combination thereof and using one or more reactors to convert BPL to acrylic acid or to convert at least some of the BPL to PPL, and then to convert PPL to acrylic acid. An outlet configured to provide a PPL stream to a second reactor tm to convert at least some of the PPL to AA or a third reactor to convert at least some of the PPL to AA. The outlet configured to provide an AA stream to a fourth reactor to convert the AA to polyacrylic acid.

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04-01-2018 дата публикации

Methods, reagents and cells for biosynthesizing compounds

Номер: US20180002729A1
Принадлежит: Invista North America LLC

This document describes biochemical pathways for producing 7-hydroxyheptanoate methyl ester and heptanoic acid heptyl ester using one or more of a fatty acid O-methyltransferase, an alcohol O-acetyltransferase, and a monooxygenase, as well as recombinant hosts expressing one or more of such exogenous enzymes. 7-hydroxyheptanoate methyl esters and heptanoic acid heptyl esters can be enzymatically converted to pimelic acid, 7-aminoheptanoate, 7-hydroxyheptanoate, heptamethylenediamine, or 1,7-heptanediol.

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