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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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Применить Всего найдено 8885. Отображено 100.
10-09-2004 дата публикации

УСТРОЙСТВО ДЛЯ ОБНАРУЖЕНИЯ СЛЕДОВЫХ КОЛИЧЕСТВ ВЗРЫВЧАТЫХ ВЕЩЕСТВ

Номер: RU0000040488U1
Автор: Ахметов И.З., Дружинин В.Л., Зорькин А.М., Ильин В.П., Колганов Е.В., Краснова Р.В., Смирнов С.П., Фурнэ И.В., Шкалябин И.О.
Принадлежит: Закрытое акционерное общество "Петро-Сорб", Федеральное государственное унитарное предприятие "Государственный научно-исследовательский институт "Кристалл"

1. Устройство для обнаружения и идентификации следовых количеств взрывчатых веществ, состоящее из контейнера с размещенным внутри детектором и вспомогательным приспособлением, отличающееся тем, что контейнер выполнен из пластмассы размером для переноски его к кармане, в качестве детектора используются флаконы с индикаторами, а функцию вспомогательного приспособления выполняет тестовая бумага. 2. Устройство по п.1, отличающееся тем, что контейнер выполнен в виде плоской пластмассовой коробки размером 100×105×20 мм и массой до 200 г. 3. Устройство по п.1, отличающееся тем, что в качестве индикаторов используются растворы щелочи (флакон А), сульфокислоты (флакон В) и амина (флакон С). 4. Устройство по п.1, отличающееся тем, что в качестве тестовой бумаги используется пористая (фильтровальная) бумага. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 40 488 (13) U1 (51) МПК G01N 31/22 C07C 203/00 C07C 243/02 C07C 205/06 (2000.01) (2000.01) (2000.01) (2000.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2004102851/22 , 06.02.2004 (24) Дата начала отсчета срока действия патента: 06.02.2004 (46) Опубликовано: 10.09.2004 U 1 4 0 4 8 8 R U Формула полезной модели 1. Устройство для обнаружения и идентификации следовых количеств взрывчатых веществ, состоящее из контейнера с размещенным внутри детектором и вспомогательным приспособлением, отличающееся тем, что контейнер выполнен из пластмассы размером для переноски его к кармане, в качестве детектора используются флаконы с индикаторами, а функцию вспомогательного приспособления выполняет тестовая бумага. 2. Устройство по п.1, отличающееся тем, что контейнер выполнен в виде плоской пластмассовой коробки размером 100×105×20 мм и массой до 200 г. 3. Устройство по п.1, отличающееся тем, что в качестве индикаторов используются растворы щелочи (флакон А), сульфокислоты (флакон В) и амина (флакон С). 4. Устройство по п.1, отличающееся тем, что в качестве ...

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Номер записи: 1
27-06-2009 дата публикации

УСТРОЙСТВО ДЛЯ ОБНАРУЖЕНИЯ СЛЕДОВЫХ КОЛИЧЕСТВ ВЗРЫВЧАТЫХ ВЕЩЕСТВ

Номер: RU0000084124U1
Автор: Ахметов Имаметдин Зинетович, Валиуллин Камиль Шафикович, Зорькин Алексей Михайлович, Ильин Владимир Петрович, Колганов Евгений Васильевич, Краснова Римма Васильевна, Судаков Владимир Владимирович, Шкалябин Игорь Олегович
Принадлежит: Общество с ограниченной ответственностью "Петро-Сорб-Комплектация", Федеральное государственное унитарное предприятие "Государственный научно-исследовательский институт "Кристалл"

1. Устройство для обнаружения и идентификации следовых количеств взрывчатых веществ, состоящее из контейнера в виде плоской пластмассовой коробки с ячейками, размещенными в них флаконами с индикаторами, в качестве которых используются раствор щелочи (флакон А), растворы сульфокислоты (флакон В) и амина (флакон С), отличающееся тем, что контейнер дополнительно снабжен ячейками, в которых размещены флаконы с индикаторами обнаружения следовых количеств селитры и пероксида. 2. Устройство по п.1, отличающееся тем, что в качестве индикатора обнаружения селитры используют реактив цинка (флакон D). 3. Устройство по п.1, отличающееся тем, что в качестве индикатора обнаружения пероксида используют реактив калия йодистого с крахмалом (флакон Е). РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 84 124 U1 (51) МПК G01N C07C C07C C07C 31/00 (2006.01) 203/00 (2006.01) 243/02 (2006.01) 205/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2008148914/22, 11.12.2008 (24) Дата начала отсчета срока действия патента: 11.12.2008 (45) Опубликовано: 27.06.2009 U 1 8 4 1 2 4 R U Формула полезной модели 1. Устройство для обнаружения и идентификации следовых количеств взрывчатых веществ, состоящее из контейнера в виде плоской пластмассовой коробки с ячейками, размещенными в них флаконами с индикаторами, в качестве которых используются раствор щелочи (флакон А), растворы сульфокислоты (флакон В) и амина (флакон С), отличающееся тем, что контейнер дополнительно снабжен ячейками, в которых размещены флаконы с индикаторами обнаружения следовых количеств селитры и пероксида. 2. Устройство по п.1, отличающееся тем, что в качестве индикатора обнаружения селитры используют реактив цинка (флакон D). 3. Устройство по п.1, отличающееся тем, что в качестве индикатора обнаружения пероксида используют реактив калия йодистого с крахмалом (флакон Е). Ñòðàíèöà: 1 ru CL U 1 (54) УСТРОЙСТВО ДЛЯ ОБНАРУЖЕНИЯ СЛЕДОВЫХ ...

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Номер записи: 2
27-05-2013 дата публикации

АППАРАТ ДЛЯ ПРОВЕДЕНИЯ ЖИДКОФАЗНЫХ ГЕТЕРОГЕННЫХ ПРОЦЕССОВ

Номер: RU0000128611U1
Автор: Валиуллин Камиль Шафикович, Ильин Владимир Петрович
Принадлежит: Открытое акционерное общество "Государственный научно-исследовательский институт "Кристалл" (ОАО "ГосНИИ "Кристалл")

Аппарат для проведения жидкофазных гетерогенных процессов, содержащий кожухотрубный теплообменник с нижним перетоком, промежуточную емкость, циркуляционную трубу, устройство для смешения и рециркуляции, выполненное в виде колеса осевого насоса, отличающийся тем, что циркуляционная труба дополнительно снабжена кожухотрубным теплообменником, установленным между колесом осевого насоса и нижним перетоком основного теплообменника. 128611 И 1 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ 7 ВУ’? 128 611” 91 ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ИЗВЕЩЕНИЯ К ПАТЕНТУ НА ПОЛЕЗНУЮ МОДЕЛЬ ММ9К Досрочное прекращение действия патента из-за неуплаты в установленный срок пошлины за поддержание патента в силе Дата прекращения действия патента: 18.01.2021 Дата внесения записи в Государственный реестр: 15.10.2021 Дата публикации и номер бюллетеня: 15.10.2021 Бюл. №29 Стр.: 1 ЕЕЭЗсСЬ па ЕП

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Номер записи: 3
05-04-2012 дата публикации

Radiation-sensitive resin composition, polymer and compound

Номер: US20120082934A1
Автор: Kazuo Nakahara, Mitsuo Sato, Yusuke Asano
Принадлежит: JSR Corp

[Problem] To reduce the time required for a film to exhibit decreased hydrophobicity after liquid immersion lithography while allowing the surface of a film to exhibit high hydrophobicity during liquid immersion lithography. [Solution] A radiation-sensitive resin composition including (A) a polymer that includes a repeating unit (a1) and a fluorine atom, and (B) a photoacid generator, the repeating unit (a1) including a group shown by any of the following formulas (1-1) to (1-3).

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Номер записи: 4
10-05-2012 дата публикации

Esters with Antimicrobial, Bioresistant and Fungal Resistant Properties

Номер: US20120116115A1
Автор: Thomas Daly
Принадлежит: Individual

A bromine/nitro moiety linked into the backbone of an ester or other compound over a wide range of occurrence rates provides antimicrobial, bio-resistant and fungal resistant properties for metal working fluids (MWF)s and other coatings. The moiety can be have the bromo and nitro groups linked to the same or different carbon atoms. The present invention also relates to urethanes, urea, amides, imides, carbonates, ethers, siloxanes, and many other types of linkages essential to MWF bases.

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Номер записи: 5
17-05-2012 дата публикации

Phenoxy substituted phenylamidine derivatives and their use as fungicides

Номер: US20120122678A1
Автор: Arnd Voerste, Birgit Kuhn, Dale Robert Mitchell, Darren James Mansfield, Jean-Pierre Vors, Jörg Nico Greul, Kerstin Ilg, Klaus Kunz, Oliver Guth, Peter Dahmen, Ralf Dunkel, Thomas Seitz, Tom Hough, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi
Принадлежит: Bayer CropScience AG

The present invention relates to 3-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

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Номер записи: 6
25-10-2012 дата публикации

Small molecules that covalently modify transthyretin

Номер: US20120270938A1
Автор: Jeffery W. Kelly, Sungwook Choi
Принадлежит: Scripps Research Institute

A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ε-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

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Номер записи: 7
17-01-2013 дата публикации

Synthesis and applications of soluble pentacene precursors and related compounds

Номер: US20130017497A1
Автор: Chung-Chih Wu, Hsin-Hui HUANG, Hsing-Hung HSIEH, Ta-Hsien CHUANG, Tahsin J. Chow
Принадлежит: Academia Sinica

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

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Номер записи: 8
07-02-2013 дата публикации

Di-Aspirin Derivatives

Номер: US20130035317A1
Автор: Christopher John Perry, Iain Douglas Nicholl
Принадлежит: Individual

The invention relates to the use of di-aspirin (bis(2-carboxyphenyl)succinate) and its derivatives in the treatment of colon and colorectal cancer. It also relates to novel derivatives of di-aspirin and to a method of synthesis of the di-aspirin and its derivatives.

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Номер записи: 9
21-03-2013 дата публикации

Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator

Номер: US20130072522A1
Автор: Adam R. Looker, Bobbianna J. Neubert-Langille, Brian R. Krueger, Dahrika Milfred Yap GUERETTE, Fredrick F. Van Goor, Gregor Zlokarnik, John Demattei, Martin Trudeau, Martyn Curtis Botfield, Michael P. Ryan, Peter Diederik Jan Grootenhuis, Stefanie Roeper
Принадлежит: Vertex Pharmaceuticals Inc

The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

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Номер записи: 10
28-03-2013 дата публикации

Anticancer and Tubulin Polymerisation Inhibition Activity of Benzylidene Indanones and Process of Preparing the Same

Номер: US20130079396A1
Автор: Ajit Kumar Saxena, Arvind Singh Negi, Atul Gupta, Ayyampudur Palanisamy Prakasham, Debabrata Chanda, Suaib Luqman, Tandeep Kaur
Принадлежит: Council of Scientific and Industrial Research CSIR

The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C 29 H 28 O 9 , was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.

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Номер записи: 11
16-05-2013 дата публикации

Fragmentation Reagents For Mass Spectrometry

Номер: US20130122599A1
Автор: Brousmiche Darryl W., Brown Jeffery Mark, Campuzano Iain, Dorschel Craig, Pringle Steven Derek, Richardson Keith, Williams Jonathan Paul
Принадлежит: MICROMASS UK LIMITED

A mass spectrometry electron transfer dissociation reagent comprising an unsaturated compound having a Frank Condon factor between 0.1 and 1.0 and an electron affinity having a positive value between 0.1 to 150 kJ/mol. 1. A mass spectrometry electron transfer dissociation reagent comprising an unsaturated compound having a Frank Condon factor between 0.1 and 1.0 and an electron affinity having a positive value between 0.1 to 200 kJ/mol.2. The reagent of claim 1 , wherein the unsaturated compound is a substituted aromatic or conjugated aliphatic compound.3. The reagent of claim 1 , wherein the electron affinity has a positive value between 0.1 to 150 kJ/mol claim 1 , preferably 0.1 to 100 kJ/mol.4. The reagent of claim 1 , wherein the unsaturated compound is an aromatic compound claim 1 , wherein the nucleus of the aromatic compound is substituted with one or more substituents consisting of cyano claim 1 , nitro claim 1 , nitroso claim 1 , carboxyl claim 1 , iodo claim 1 , aldehyde and acetoxy.5. The reagent of claim 4 , wherein the one or more substituents are cyano.6. The reagent of claim 4 , wherein the nucleus is selected from the group consisting of phenyl claim 4 , pyridinyl claim 4 , pyrimidinyl claim 4 , triazolyl claim 4 , styrenyl and picolinyl.7. The reagent of claim 1 , wherein the unsaturated compound is an unsaturated aliphatic compound selected from the group consisting of ethylene claim 1 , acetylene or acrylate substituted with one or more substituents.8. The reagent of claim 7 , wherein two or more unsaturated bonds are conjugated.9. The reagent of claim 7 , wherein the unsaturated aliphatic compound is selected from the group consisting of ethylene claim 7 , acetylene or acrylate substituted with one or more unsaturated groups selected from the group consisting off cyano claim 7 , nitro claim 7 , aceto claim 7 , carboxyl claim 7 , aldehyde and nitroso.10. The reagent of selected from the group consisting of 1 claim 1 ,4-dicyanobenzene claim 1 , 1 ...

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Номер записи: 12
23-05-2013 дата публикации

Esters with Antimicrobial, Bioresistant and Fungal Resistant Properties

Номер: US20130131365A1
Автор: Daly Thomas
Принадлежит:

A bromine/nitro moiety linked into the backbone of an ester or other compound over a wide range of occurrence rates provides antimicrobial, bio-resistant and fungal resistant properties for metal working fluids (MWF)s and other coatings. The moiety can be have the bromo and nitro groups linked to the same or different carbon atoms. The present invention also relates to urethanes, urea, amides, imides, carbonates, ethers, siloxanes, and many other types of linkages essential to MWF bases. 2. The anionic surfactant of where n=n′=7 claim 1 , m=m′=7 claim 1 , and A=Br.3. A metal working fluid base comprising a molecule according to .4. A foaming or anti-foaming agent comprising a molecule according to .6. The molecule of where R═R′=—(CH)CHA=—(CH2)CH.7. A metal working fluid base comprising a molecule according to .8. A surfactant comprising a molecule according to .9. A foaming or anti-foaming agent comprising a molecule according to . This is a continuation of application Ser. No. 13/351,512 filed Jan. 17, 2012 which was a continuation of Ser. No. 12/965,252 filed Dec. 10, 2010 which was a divisional from application Ser. No. 12/287,726 filed Oct. 10, 2008, now abandoned, which was a continuation-in-part of application Ser. No. 11/800,569 filed May 7, 2007, now U.S. Pat. No. 7,439,376 issued Oct. 21, 2008, which was a continuation in part of application Ser. No. 10/603,356 filed Jun. 25, 2003, now abandoned, which claimed priority from U.S. Provisional patent application No. 60/392,007 filed Jun. 26, 2002. Applications Ser. Nos. 13/351,512, 12/965,252, 12/287,726, 11/800,569, 10/603,356 and 60/392,007 are hereby incorporated by reference. This application also incorporates by reference my other patent application Ser. No. 10/350,928 filed Jan. 23, 2003 entitled Polymers with Antimicrobial, Bioresistant and Fungal Resistant Properties.The text of this continuation application is substantially identical to that of grandparent application Ser. No. 10/603,356.1. Field of ...

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Номер записи: 13
06-06-2013 дата публикации

NOVEL SELF-REACTIVE ARMS AND PRODRUGS COMPRISING SAME

Номер: US20130144045A1
Автор: Papot Sebastien, Thomas Mickael
Принадлежит:

The present invention relates to a compound of general formula (I): 2. The compound as claimed in claim 1 , wherein X is OH.3. The compound as claimed in claim 1 , wherein Y is NO.4. The compound as claimed in claim 1 , wherein Rand Rare H.5. The compound as claimed in claim 1 , wherein F is —C≡CR′″ claim 1 , —N claim 1 , —SH claim 1 , —C═CH claim 1 , cyclooctynes claim 1 , maleimide claim 1 , —SON claim 1 , or —COSR′″ claim 1 , wherein R′″ is H or a linear or branched claim 1 , saturated or unsaturated claim 1 , Cto Calkyl radical.7. The compound as claimed in claim 6 , wherein Y is NOin the ortho position of X′ claim 6 , and Rand Rare H.8. The compound as claimed in claim 6 , wherein D is a compound having therapeutic activity.9. The compound as claimed in claim 6 , wherein D is composed of an active compound or a plurality of active compounds.10. The compound as claimed in claim 6 , wherein the labile group E is a substrate of an enzyme selected from glucuronidases.11. The compound as claimed in claim 6 , wherein L is a ligand of a cellular receptor.12. The compound as claimed in wherein n=1 and Z is a C-C.13. The compound as claimed in claim 6 , wherein n=1 and Z is a glycosyl group selected from a glucosyl group claim 6 , a galactosyl group claim 6 , a mannosyl group claim 6 , a lactosyl group.14. The compound as claimed in claim 6 , wherein n=1 and Z is a O—(CHR—CHR—O—)or N—(CHR—CHR—O—)group wherein in is a natural integer varying from 2 to 18.15. The compound as claimed in wherein n=1 and Z is a group issuing from an amino acid or from a peptide.16. The compound as claimed in claim 6 , wherein n=1 and Z is a combination of a glycosyl group and a O—(CHR—CHR—O—)or N—(CHR—CHR—O—)group.17. The compound as claimed in claim 6 , wherein n=0.19. The method as claimed in claim 18 , wherein v is selected from NH claim 18 , NHR″ claim 18 , OH claim 18 , or SH.20. The method as claimed in claim 18 , wherein w is selected from a halide radical21. The method as claimed in ...

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Номер записи: 14
13-06-2013 дата публикации

NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES

Номер: US20130150577A1
Автор: Khile Anil Shahaji, Patel Jayesh, Pradhan Nitin Sharadchandra, Trivedi Nikhil
Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity. 2. The process of claim 1 , wherein the halogen atom in the compounds of formulae II claim 1 , III claim 1 , IV claim 1 , V claim 1 , VI and VII is F; and wherein the leaving group ‘X’ in the compound of formula VIII is Cl.3. The process of claim 1 , wherein the R claim 1 , Rand Rin the compounds of formulae II claim 1 , III claim 1 , IV claim 1 , V claim 1 , VI and VII are H claim 1 , and wherein the Rand Rare F.4. The process of claim 1 , wherein the first solvent used in step-(a) is selected from the group consisting of an aliphatic or alicyclic hydrocarbon claim 1 , a chlorinated aliphatic or aromatic hydrocarbon claim 1 , an aromatic mono or dinitro hydrocarbon claim 1 , and mixtures thereof; wherein the second solvent used in step-(b) is selected from the group consisting of a ketone claim 1 , an aliphatic amide claim 1 , a nitrile claim 1 , a hydrocarbon claim 1 , a cyclic ether claim 1 , an aliphatic ether claim 1 , a polar aprotic solvent claim 1 , and mixtures thereof; wherein the third solvent used in step-(c) is selected from the group consisting of a hydrocarbon claim 1 , a cyclic ether claim 1 , an aliphatic ether claim 1 , a chlorinated hydrocarbon claim 1 , and mixtures thereof; wherein the fourth solvent used in step-(d) is selected from the group consisting of a hydrocarbon claim 1 , cyclic ethers claim 1 , an ether claim 1 , an ester claim 1 , a nitrile claim 1 , an aliphatic amide claim 1 , a chlorinated hydrocarbon claim 1 ...

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Номер записи: 15
27-06-2013 дата публикации

TETRASUBSTITUTED BENZENES

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

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

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Номер записи: 16
15-08-2013 дата публикации

Compositions and Methods for Imaging

Номер: US20130209360A1
Автор: Alexander R. Lippert, Christopher J. Chang
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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Номер записи: 17
15-08-2013 дата публикации

Nitrated Lipids and Methods of Making and Using Thereof

Номер: US20130210917A1
Автор: "ODonnell Valerie", Baker Paul, Branchaud Bruce, Chen Yuqing E., Freeman Bruce A., Schopfer Francisco
Принадлежит:

Described herein are nitrated lipids and methods of making and using the nitrated lipids. 179-. (canceled)80. A compound comprising a lipid comprising at least one nitro group , wherein the compound is substantially pure.81. A method for producing a nitrated lipid , comprising(a) reacting an unsaturated lipid with a mercuric salt, a selenium compound, and a nitrating compound to produce a first intermediate, and(b) reacting the first intermediate with an oxidant.82. The method of claim 81 , wherein step (a) is performed under anaerobic conditions.83. The method of claim 81 , wherein step (a) is conducted under anhydrous conditions.84. The method of claim 81 , wherein the mercuric salt comprises HgCl claim 81 , Hg(NO) claim 81 , or Hg(OAc).85. The method of claim 81 , wherein the selenium compound comprises PhSeBr claim 81 , PhSeCl claim 81 , PhSeOCCF claim 81 , PhSeOH claim 81 , or PhSeCN.86. The method of claim 81 , wherein the nitrating compound comprises a nitrite salt.87. The method of claim 81 , wherein the nitrating compound comprises NaNOor AgNO.88. The method of claim 81 , wherein the oxidant comprises HOor an organic hydroperoxide.89. The method of claim 81 , wherein the lipid comprises 14:1 claim 81 , 16:1 claim 81 , 18:1 claim 81 , 18:2 claim 81 , 18:3 claim 81 , 20:4 claim 81 , or 22:6 claim 81 , the mercuric salt comprises HgCl claim 81 , the selenium compound comprises PhSeBr claim 81 , the nitrating compound comprises NaNO claim 81 , and the oxidant comprises HO.90. The method of claim 89 , wherein step (a) is performed under anaerobic and anhydrous conditions.91. The method of claim 81 , wherein when after step (b) two or more isomers of the nitrated lipid are produced claim 81 , separating each isomer so that each isomer is substantially pure.92. The method of claim 91 , wherein the separation step comprises chromatographing the isomers.93. A nitrated lipid produced by the method of .94. A method for reducing or preventing inflammation in a subject ...

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Номер записи: 18
22-08-2013 дата публикации

INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF FINGOLIMOD

Номер: US20130217899A1
Автор: Marom Ehud, Mizhiritskii Michael, Rubnov Shai
Принадлежит: MAPI PHARMA LTD.

The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes. 142-. (canceled)44. The process according to claim 43 , wherein step (a) is conducted in the presence of a Friedel-Crafts catalyst claim 43 , a metal salt of an organic acid claim 43 , or a protic acid claim 43 , wherein{'sub': 3', '3', '4', '4', '2', '3, 'the Friedel Crafts catalyst is selected from AlCl, FeCl, SnCl, TiCl, ZnCland BF;'}the metal salt of an organic acid is a metal triflate selected from hafnium triflate and cerium triflate; and{'sub': 2', '4', '3', '3, 'the protic acid is selected from HF, HSO, CFSOH and an ion-exchange resin which is selected from Nafion or zeolite.'}45. The process according to claim 43 , wherein the reducing agent in step (b) is NaBH.46. The process according to claim 43 , wherein the hydroxy protecting group P in compound (13A) is acetyl (COCH) claim 43 , and wherein in step (c) the protection of 3-nitro-1-(4-octylphenyl)propan-1-ol is carried out by acylation with acetic anhydride or acetyl chloride in the presence of a base.47. The process according to claim 43 , whereinthe reduction of 3-nitro-1-(4-octylphenyl)propan-1-one (12) to 3-nitro-1-(4-octylphenyl)propan-1-ol and its conversion to compound (13A) is carried out in one step without isolation of intermediates; orwherein in step (d) the bis-hydroxymethylation of compound (13A) is carried out with formaldehyde or paraformaldehyde in the presence of a base; orwherein in step (d) the bis-hydroxymethylation of compound (13A) and deprotection to compound (14) is carried out in one step without isolation of intermediates.48. The process according to claim 43 , wherein the reduction step (e) comprises hydrogenating compound (14) to Fingolimod (1) in the presence of a Pd/C catalyst.50. The process according to claim 49 , wherein step (a) is ...

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Номер записи: 19
19-09-2013 дата публикации

Compound having hetero ring skeleton, and process for producing optically active compound using the aforementioned compound as asymmetric catalyst

Номер: US20130245257A1
Автор: Kazuo Murakami, Yoshiji Takemoto
Принадлежит: KYOTO UNIVERSITY, Sumitomo Chemical Co Ltd

The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the substituents are as defined in the specification, as well as a tautomer thereof or a salt thereof. The invention also provides asymmetric synthesis methods involving the use of such a compound, tautomer thereof, or salt thereof, as a catalyst.

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Номер записи: 20
19-09-2013 дата публикации

Processes for preparing benzimidazole compounds

Номер: US20130245279A1
Автор: Anthony D. Piscopio, Bruno P. Hache, James Gair Ford, John Demattei, John Leonard, Koen Peeters, Matthew Charles Evans, Sagar Shakya, Simon Mark Pointon, Timothy John Lilley
Принадлежит: Array Biopharma Inc, AstraZeneca AB

Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X 5 , R 2b , R 2c and R 10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

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Номер записи: 21
26-09-2013 дата публикации

PROCESS FOR THE PRODUCTION OF AMIDES

Номер: US20130253225A1
Автор: Bonnett Paul, Corsi Camilla, Ehrenfreund Josef, George Neil, Giordano Fanny, Jones Ian, Seifert Gottfried, Shah Shailesh, Tobler Hans, Walter Harald, Zeller Martin
Принадлежит:

The present invention relates to a process for the preparation of compounds of formula I 2. A compound of formula IV according to claim 1 , wherein Rand Rare methyl.4. A compound of formula IV prepared by the process of . This application is a divisional application of U.S. Ser. No. 13/198,739 filed Jan. 8, 2013, which is a divisional application of U.S. Ser. No. 12/066,683 filed Jul. 16, 2008, which is a 371 of International Application No. PCT/EP2006/008982 filed Sep. 14, 2006, which claims priority to CH 01520/05 filed Sep. 16, 2005 and CH 0296/06 filed Feb. 24, 2006, the contents of which are incorporated herein by reference.The present invention relates to a process for the preparation of pyrazolyl-4-carboxylic acid benzo-norbornen-5-yl-amides and also to novel intermediates for use in such a process. The present invention further relates to a novel crystal modification of syn-3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-isopropyl-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide, compositions comprising it and to the use thereof in the control of fungus infestation in cultivated plants.Pyrazolyl-4-carboxylic acid benzonorbornen-5-yl-amides, for example 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-isopropyl-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide, are valuable fungicides, such as are described, for example, in WO 04/035589.WO 04/035589 describes a process for the preparation of pyrazolyl-4-carboxylic acid benzonorbornen-5-yl-amides (see Scheme 1):According to WO 04/035589, a 3-nitro-dehydrobenzene generated, for example, from 6-nitro-anthralinic acids of formula (A) wherein Rand Rmay be, inter alia, hydrogen, is first reacted in a Diels-Alder reaction with a cyclic 1,4-diene of formula (B) wherein R, R, Rand Rmay be, inter alia, hydrogen and Y may be, inter alia, —CH((i)-CH)—, to form a 5-nitro-benzonorbornadiene compound of formula (C). Subsequent catalytic reduction under standard conditions (for example, Ra/Ni or ...

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Номер записи: 22
12-12-2013 дата публикации

BENZOIC ACID COMPOUNDS FOR REDUCING URIC ACID

Номер: US20130331452A1
Автор: SHARMA Shalini, von Borstel Reid W
Принадлежит: WELLSTAT THERAPEUTICS CORPORATION

Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I). The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and -induced inflammation. In Formula I, t, q, r, R6, R7, X and A are as defined herein. 3. The compound or salt of claim 2 , wherein A is phenyl claim 2 , unsubstituted or substituted by one claim 2 , two or three groups selected from the group consisting of halo claim 2 , alkyl having 1 or 2 carbon atoms claim 2 , perfluoromethyl claim 2 , alkoxy having 1 or 2 carbon atoms claim 2 , perfluoromethoxy claim 2 , nitro claim 2 , and amino.4. The compound or salt of claim 3 , wherein A is 2 claim 3 ,6-dimethylphenyl.7. The compound or salt of claim 6 , wherein Ris methyl and Ris methyl.8. The compound or salt of claim 7 , wherein the compound is selected from the group consisting of:3-(2,6-dimethylbenzyloxy)-4-methylbenzoic acid;3-(2,6-dimethylbenzyloxy)-4-nitrobenzoic acid;3-(2,6-dimethylbenzyloxy)-4-methoxybenzoic acid; and3-(2,6-dimethylbenzyloxy)-4-fluorobenzoic acid.9. A method of reducing the uric acid concentration in blood of claim 1 , or increasing uric acid excretion from claim 1 , a mammalian subject claim 1 , comprising administering to the subject a compound or salt of claim 1 , in an amount effective to reduce the uric acid concentration in blood of claim 1 , or increase uric acid excretion from claim 1 , the subject.10Plasmodium falciparum. A method according to claim 9 , for treating or preventing a condition selected from the group consisting of gout claim 9 , hyperuricemia claim 9 , elevated ...

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Номер записи: 23
19-12-2013 дата публикации

Compounds for the treatment of neurodegenerative diseases

Номер: US20130338202A1
Автор: Alan D. Snow, F. Michael Hudson, Franz F. Hefti, Geoffrey Golding, Joel Cummings, Judy Cam, Luke A. Esposito, Marisa C. YADON, Qubai Hu, Seok-Rye Choi, Thomas Lake, Ximin Li
Принадлежит: Proteo Tech Inc

Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.

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Номер записи: 24
09-01-2014 дата публикации

New palladium catalyst, method for its preparation and its use

Номер: US20140012004A1
Автор: Gábor Vlád, Géza Timári, Tibor SOÓS, Zoltán DALICZEK, Zoltán Finta
Принадлежит: H4SEP KFT

The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

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Номер записи: 25
30-01-2014 дата публикации

Ester-Based Reactive Plasticizer For Plastic Bonded Explosives

Номер: US20140031580A1
Автор: Bae In Joo, Kim Jin Seuk, Kwon Young Hwan, Lee Bum Jae
Принадлежит: AGENCY FOR DEFENSE DEVELOPMENT

Disclosed is an energetic reactive plasticizer for a plastic bonded explosive (PBX), and specifically an energetic reactive plasticizer for PBX which has high performance and insensitiveness without a plasticizer migration by being bonded with a polymer binder for a plastic bonded explosive. 2. Method for preparing an ester compound according to claim 1 , which comprises an acetal forming reaction between 4 claim 1 ,4-dinitrovaleric acid and an alcohol containing an acetylene group. This application claims the benefit and priority of Korean Patent Application No. 10-2012-0081305 filed Jul. 25, 2012. The entire disclosure of the above application is incorporated herein by reference.The present invention relates to an energetic reactive plasticizer for a plastic bonded explosive, and specifically to an energetic reactive plasticizer for a plastic bonded explosive which has high performance and insensitiveness without a migration problem of a plasticizer by being bonded with a polymer binder for a plastic bonded explosive.Currently, efforts to make energetic materials insensitive have been a significant issue in development of explosives and a propellant. As a part of such efforts, plastic bonded explosives (PBXs) having low sensitivity and improved mechanical properties while maintaining high energy properties have been developed. Such PBX now becomes an elementary component of high-energy explosives, polymeric binders and other additives used in a small amount such as a plasticizer or a stabilizer.Currently, a polyurethane polymeric binder on the basis of a hydroxyl-terminated polybutadiene (HTPB) has been used as a widely applicable polymeric binder system, together with various additives so as to improve processability, mechanical properties and chemical stability. Although such polymeric binder shows excellent properties in making high-energy materials insensitive, it has been proposed that it generally disadvantageously reduces the energy density of PBX on the ...

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Номер записи: 26
30-01-2014 дата публикации

Ether-based reactive plasticizer for plastic bonded explosives

Номер: US20140031593A1
Автор: Bum Jae Lee, In Joo Bae, Jin Seuk Kim, Young Hwan Kwon
Принадлежит: Agency for Defence Development

Disclosed is an energetic reactive plasticizer for a plastic bonded explosive (PBX), and specifically an energetic reactive plasticizer for PBX which has high performance and insensitiveness without a plasticizer leak by being bonded with a polymer binder for a plastic bonded explosive.

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Номер записи: 27
30-01-2014 дата публикации

Apparatus and Process for Nitration Selectivity Flexibility Enabled by Azeotropic Distillation

Номер: US20140031594A1
Автор: Pendergast John G., Sawant Mahesh, Trauth Daniel M.
Принадлежит:

Disclosed are processes and apparatuses for concentrating at least one organic acid using an alkyl acetate as an entrainer. The processes and apparatuses may use the same alkyl acetate as an entrainer to concentrate a mixture of organic acids. 1. A process comprising:reacting a hydrocarbon feedstock with an aqueous feedstock in a reactor to produce a product stream comprising a nitroalkane and byproducts;processing the product stream to produce a first top stream and a first bottom stream, wherein the first top stream comprises the nitroalkane and the first bottom stream comprises at least a first organic acid and water;supplying at least a portion of the first bottom stream to an azeotropic distillation column;using an alkyl acetate as an entrainer in the azeotropic distillation column, such that the first bottom stream is separated into at least a second top stream and a second bottom stream, wherein the second top stream comprises the alkyl acetate and water and wherein the second bottom stream comprises the first organic acid;separating the second top stream in a phase separator into an organic phase and an aqueous phase, the organic phase comprising the alkyl acetate; andreturning at least a portion of the organic phase to the azeotropic distillation column.2. A process according to claim 1 , wherein the aqueous feedstock comprises water claim 1 , between about 10 and 50 weight percent of nitric acid claim 1 , and at least about 15 weight percent of the first organic acid.3. A process according to claim 1 , wherein the aqueous feedstock comprises at least about 40 weight percent of the first organic acid.4. A process according to claim 1 , wherein the first organic acid is selected from the group consisting of acetic acid claim 1 , propionic acid claim 1 , butyric acid claim 1 , and any combination thereof.5. A process according to claim 1 , wherein the first bottom stream further comprises at least a second organic acid.6. A process according to claim 5 , ...

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Номер записи: 28
06-02-2014 дата публикации

4-Biphenyl-substituted pyrazolidin-3,5-dione derivatives

Номер: US20140039215A1
Автор: ARNOLD Christian, Auler Thomas, BRETSCHNEIDER Thomas, Feucht Dieter, FISCHER Reiner, Gesing Ernst Rudolf F., Hills Martin Jeffrey, KEHNE Heinz, Kuck Karl-Heinz, Lösel Peter, MALSAM Olga
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) 124-. (canceled)27. A compound of the formula (XIX) according to claim 25 , wherein the reagent is dicyclohexylcarbodiimide or toluenesulphonyl chloride. This application is a Continuation of application Ser. No. 13/347,931, filed Jan. 11, 2012, now pending, which is a Division of application Ser. No. 10/567,788, §371(c) date: Feb. 16, 2007, now U.S. Pat. No. 8,119,556, which is U.S. National Phase of International Application No. PCT/EP2004/008638, filed Aug. 2, 2004, which claims the benefit of German Appl. No. DE 10337497.3, filed Aug. 14, 2003. The entirety of each of these applications is incorporated by reference herein.The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to novel selective herbicidal active compound combinations comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives and at least one crop plant compatibility-improving compound, which combinations can be used with particularly good results for the selective control of weeds in various crops of useful plants.4-Arylpyrazolidine-3,5-dione derivatives having herbicidal, acaricidal and insecticidal properties are described in EP-A-508 126, WO 92/16 150, WO 96/721 652, WO 99/43 649, WO 99/47 525, WO 99/48 869, WO 99/55 673, WO 01/17 351, WO 01/17 352, WO 01/17 353, WO 01/17 972, WO 01/17 973, WO 03/062 244, WO 03/028 446. Also known are 4-arylpyrazolidines, which have been described to have fungicidal properties (WO 96/36 229, WO 96/36 615, WO 96/36 616, WO 96/36 633).However, in particular at low application rates and concentrations, the activity and the activity spectrum of these compounds are not always entirely satisfactory. Furthermore, the plant compatibility of ...

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Номер записи: 29
06-02-2014 дата публикации

PROCESS FOR SCRUBBING DINITROTOLUENE

Номер: US20140039227A1
Автор: Ahrens Sebastian, ALLARDT Holger, BECKER Barbara, Fritz Ruediger, HAENDEL Mirko, HEMPEL Renate, HERMANN Heinrich, Leschinski Julia, Neto Samuel, POEHLMANN Juergen
Принадлежит:

The invention relates to a process for scrubbing a crude mixture comprising dinitrotoluene, nitric acid, nitrogen oxides and sulfuric acid obtained in the nitration of toluene after the nitrating acid has been separated off, which comprises two scrubbing steps (SS-I) and (SS-II), wherein 1. A process for scrubbing a crude mixture comprising dinitrotoluene , nitric acid , nitrogen oxides and sulfuric acid obtained in the nitration of toluene after the nitrating acid has been separated off , the process comprising:i) extracting a crude mixture with a scrubbing acid I comprising nitric acid, nitrogen oxides and sulfuric acid in a scrub comprising at least one extraction stage, such that scrubbing acid discharged from a first extraction stage (SS-I-1) of the extracting i) has a total acid content of from 20 to 40% by weight, to obtain a prescrubbed crude mixture;ii) extracting, the prescrubbed crude mixture comprising dinitroluene with a scrubbing acid II in a scrub comprising at least one extraction stage, such that scrubbing acid discharged from a first extraction stage (SS-II-1) of the extracting ii) has a pH of less than or equal to 4, to obtain a mixture comprising dinitrotoluene which is essentially free of nitric acid, sulfuric acid and nitrogen oxides.2. The process according to claim 1 , wherein the extracting i) comprises from 2 to 4 extraction stages and is carried out in countercurrent.3. The process according to claim 1 , wherein the extracting ii) comprises from 2 to 4 extraction stages and is carried out in countercurrent.4. The process according to claim 1 , wherein the scrubbing acid discharged from the first extraction stage (SS-II-1) of the extracting ii) has a pH of from 0 to 3.5. The process according to claim 1 , wherein the scrubbing acid discharged from the first extraction stage (SS-II-1) of the extracting ii) has a pH of from 0.5 to 2.6. The process according to claim 1 , wherein water or a scrubbing acid having a total acid content of from 0.2 ...

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Номер записи: 30
20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 31
20-02-2014 дата публикации

METHOD FOR PRODUCING FIVE-MEMBERED RING-CONTAINING COMPOUND

Номер: US20140051874A1
Автор: Hayashi Yujiro
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The present invention provides a method that allows production of stereospecific and asymmetrical five-membered ring-containing compounds serving as synthetic intermediates for formation of five-membered rings of prostaglandins and the like, with high yield and excellent stereoselectivity in terms of diastereoselectivity and enantioselectivity in a short process without requiring troublesome procedures such as optical resolution. The method for producing a five-membered ring-containing compound includes a cyclization step of condensing and cyclizing an α,β-unsaturated nitro compound represented by the following chemical formula (I) with a 1,4-butanedione compound, in the presence of a catalyst formed by a compound having a pyrrolidine ring and an optically active α-carbon relative to the nitrogen on the ring, in a water-insoluble organic solvent and/or a non-oxygen atom-containing water-soluble organic solvent so as to produce the five-membered ring-containing compound represented by the following chemical formula (II). 2. The method for producing a five-membered ring-containing compound according to claim 1 , further comprising claim 1 , after the cyclization step claim 1 , a reduction step of reducing claim 1 , with a reducing agent claim 1 , the Athat is the aldehyde group to the hydroxymethyl group.6. The method for producing a five-membered ring-containing compound according to claim 1 , wherein the water-insoluble organic solvent is at least one selected from a halogen-containing organic solvent claim 1 , an aromatic organic solvent claim 1 , a hydrocarbon organic solvent and an acyclic ether organic solvent claim 1 , and the non-oxygen atom-containing water-soluble organic solvent is a nitrile-substituted hydrocarbon organic solvent.7. The method for producing a five-membered ring-containing compound according to claim 6 , wherein the water-insoluble organic solvent is the halogen-containing organic solvent selected from dichloromethane claim 6 , ...

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Номер записи: 32
27-02-2014 дата публикации

METHOD FOR PRODUCING AMINOTHIAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE

Номер: US20140058104A1
Автор: Aida Yoshiyuki, Asami Kazuyasu, NAGASAWA Masaaki, Nakao Ryu, Tanaka Nobuyuki
Принадлежит: ZERIA PHARMACEUTICAL CO., LTD.

Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions. 1. (canceled)3. The compound of claim 2 , wherein ring A represents a benzene ring.4. The compound of claim 2 , wherein ring A represents a 6-membered aromatic heterocycle.5. The compound of claim 2 , wherein Ris a hydrogen atom.6. The compound of claim 2 , wherein Ris an electron-withdrawing group. This application is a divisional of U.S. application Ser. No. 11/573,409 filed Jul. 10, 2013 and which is a National Stage of PCT/JP05/15259.The present invention relates to a method for selectively demethylating a methoxy group present at the ortho position (2-position) of an aromatic carboxylic acid, and a method for producing an aminothiazole derivative via the demethylation method.It is known that compounds in which 2-hydroxybenzoic acids are amide-bonded to 2-aminothiazoles have an excellent gastroprokinetic effect and are useful as prophylactic and therapeutic agents for epigastric indefinite complaints, nausea, vomiting, heartburn, anorexia, abdominal bloating, gastro-oesophageal reflux, and the like (patent documents 1 to 3). Among these compounds, the compound represented by formula (7a) below:particularly, has a high safety as well as an excellent gastroprokinetic effect and is useful as a prophylactic and therapeutic agent for the above-described various gastroprokinetic disorders.As a method for producing these 2-hydroxybenzoic acid amide derivatives, patent document 1 adopts a method which involves reacting a 2-methoxybenzoic acid amide derivative with a demethylating reagent such as pyridine hydrochloride to make a 2-hydroxybenzoic acid derivative. However, the demethylation reaction has been problematic to adopt industrially because the reaction produces many side reactions, making it difficult to selectively demethylate only a methoxy group selectively at the 2- ...

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Номер записи: 33
20-03-2014 дата публикации

IRE-1alpha INHIBITORS

Номер: US20140080832A1
Автор: Flynn Gary A., LONERGAN David Gregory, PALLAI Peter V., PATTERSON John Bruce, ZENG Qingping
Принадлежит: MANNKIND CORPORATION

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies. 2. The compound of claim 1 , wherein the compound is represented by structural formula (E).3. The compound of claim 1 , wherein the compound is represented by structural formula (X).8. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound of or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable carrier.9. A method of inhibiting IRE-1α activity claim 1 , comprising administering to a subject a compound of or a pharmaceutically acceptable salt of the compound.10. The method of claim 1 , wherein the compound is a compound of .11. The method of claim 1 , wherein the compound is a compound of .12. The method of claim 1 , wherein the compound is a compound of .13. The method of claim 1 , wherein the compound is a compound of .14. The method of claim 1 , wherein the compound is a compound of15. The method of claim 1 , wherein the compound is a compound of .16. The method of wherein cells of the subject have an activated unfolded protein response.17. The method of claim 9 , wherein the subject has cancer.18. The method of claim 17 , wherein the cancer is myeloma.19. The method of claim 9 , further comprising administering to the subject an agent that induces or up-regulates IRE-1α expression.20. The method of claim 9 , further comprising administering to the subject a biotherapeutic agent claim 9 , a chemotherapeutic agent claim 9 , radiation claim 9 , or a proteasome inhibitor. This application is a division of Ser. No. 12/941,530 filed on Nov. 8, 2010, which is a continuation of Ser. No. 12/135,571 filed on Jun. 9, 2008, now U.S. Pat. No. 7,858,666, which claims the benefit of Ser. No. 60/942,743 filed Jun. 8, 2007. ...

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Номер записи: 34
27-03-2014 дата публикации

Chalcone derivatives as nrf2 activators

Номер: US20140088052A1
Автор: Kim Jung-hyun, Rajesh Thimmulappa, Sanjay V. MALHOTRA, Sarvesh Kumar, Shyam Biswal, Vineet Kumar
Принадлежит: JOHNS HOPKINS UNIVERSITY

Compounds and methods for treating or preventing a disease, disorder or condition associated with an Nrf2-regulated pathway, including those associated with an autoimmune disease, comorbidity associated with diabetes, such as retinopathy and nephropathy, bone marrow transplant for leukemia and related cancers, bone marrow deficiencies, inborn errors of metabolism, and other immune disorders, oxidative stress, respiratory infection, ischemia, neurodegenerative disorders, radiation injury, neutropenia caused by chemotherapy, autoimmunity, and congenital neutropenic disorders, and for restoring a corticosteroid responsiveness, in a subject are provided.

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Номер записи: 35
03-04-2014 дата публикации

Process for producing ester compound

Номер: US20140094616A1
Автор: Leopold Mpaka LUTETE, Tetsuya Ikemoto, Toshiaki Aikawa
Принадлежит: Sumitomo Chemical Co Ltd

Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R 5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.

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Номер записи: 36
02-01-2020 дата публикации

ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PESTICIDE

Номер: US20200000777A1
Автор: KIKUCHI Takamasa, KOMODA Mitsuaki, MITA Takeshi, MIZUKOSHI Takashi, Takii Shinji, YAOSAKA Manabu
Принадлежит: NISSAN CHEMICAL CORPORATION

A substituted alkenylbenzene compound of formula (4): 2. The substituted alkenylbenzene compound of formula (4) according to claim 1 , wherein:{'sup': '1', 'sub': 5', '1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a halogen atom, —SF, C-Chaloalkyl, C-Chaloalkoxy and C-Chaloalkylthio;'}{'sup': '3', 'sub': 1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C-Calkyl, C-Chaloalkyl and C-Calkoxy;'}{'sup': '4', 'Xis a hydrogen atom or halogen atom;'}{'sup': 3a', '3b, 'Rand Rare each a fluorine atom;'}{'sup': 3c', '2', '3', '4', '1', '3', '4', '1', '3', '4', '3c, 'Ris selected from the group consisting of a hydrogen atom, fluorine atom, chlorine atom, bromine atom and trifluoromethyl, with a proviso that in case where Xis a fluorine atom, chlorine atom or trifluoromethyl and both Xand Xare a hydrogen atom, in case where both Xand Xare a fluorine atom and Xis a hydrogen atom, and in case where both Xand Xare trifluoromethyl and Xis a hydrogen atom, Ris a hydrogen atom, chlorine atom, bromine atom or trifluoromethyl.'} This application is a continuation of U.S. patent application Ser. No. 15/972,939, filed May 7, 2018, which is a continuation of U.S. patent application Ser. No. 15/097,002, filed Apr. 12, 2016, now U.S. Pat. No. 10,045,969, which is a continuation of U.S. patent application Ser. No. 14/568,964, filed Dec. 12, 2014, which is a continuation of U.S. patent application Ser. No. 13/850,067, filed Mar. 25, 2013, now U.S. Pat. No. 8,946,492, which is a divisional of U.S. patent application Ser. No. 13/350,297, filed Jan. 13, 2012, now U.S. Pat. No. 8,492,311, which is a divisional of U.S. patent application Ser. No. 13/166,294, filed Jun. 22, 2011, now U.S. Pat. No. 8,138,213, which is a divisional of U.S. patent application Ser. No. 12/509,859, filed Jul. 27, 2009, now U.S. Pat. No. 8,022,089, which is a divisional of U.S. patent application Ser. No. 11/514,921, filed Sep. 5, ...

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Номер записи: 37
04-01-2018 дата публикации

COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20180002298A1
Автор: CAM JUDY, CUMMINGS JOEL, ESPOSITO LUKE A., HU QUBAI, HUDSON F. MICHAEL, Lake Thomas, Snow Alan D., YADON MARISA C.
Принадлежит:

Compounds and their pharmaceutically acceptable salts for treatment of tauopathies, such as Alzheimer's disease, Pick's disease, progressive supranuclear palsy, corticobasal degeneration, familial frontotemporal dementia/Parkinsonism linked to chromosome 17, amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia. 2. A method of disrupting or inhibiting the formation claim 1 , deposition claim 1 , accumulation claim 1 , or persistence of tau fibrils and/or aggregates claim 1 , comprising administering a therapeutically effective amount of the compounds of .3. The method of claim 2 , where the compound administered is in an amount between 0.1 mg/Kg/day and 1000 mg/Kg/day.4. The method of claim 2 , where the compound is administered in an amount between 1 mg/Kg/day and 100 mg/Kg/day.5. The method of claim 2 , where amount of compound administered is in an amount between 10 mg/Kg/day and 100 mg/Kg/day.6. A method resulting in neuroprotection from a tauopathy in a mammal comprising the step of administrating a therapeutically effective amount of a compound of .7. The method of where the tauopathy is one selected from; Alzheimer's disease claim 6 , Pick's disease claim 6 , progressive supranuclear palsy claim 6 , corticobasal degeneration claim 6 , familial frontotemporal dementia/Parkinsonism linked to chromosome 17 claim 6 , amyotrophic lateral sclerosis/Parkinsonism-dementia complex claim 6 , argyrophilic grain dementia claim 6 , dementia pugilistic claim 6 , diffuse neurofibrillary tangles with calcification claim 6 , progressive subcortical gliosis and tangle only dementia.8. An article of manufacture claim 1 , comprising packaging material claim 1 , the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , contained within packaging material claim 1 , which is used for treating ...

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Номер записи: 38
02-01-2020 дата публикации

METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG

Номер: US20200002261A1
Автор: Chambournier Gilles, Endres Gregory William, Fedij Victor, Hering Kirk William, II Thomas James, Krell, MAHMOUD Hussien Mahmoud
Принадлежит: CAYMAN CHEMICAL COMPANY INCORPORATED

The present invention provides processes for preparing a prostacyclin analogue of Formula I 4. The method of claim 3 , wherein the transition metal catalyst comprises a compound or complex either of which comprises copper having a +1 oxidation state.5. The method of claim 4 , wherein the transition metal catalyst comprises CuI.15. The method of claim 14 , further comprising the step of:xxiv) reacting the compound of Formula I with diethanolamine in the presence of an organic solvent to generate the diethanolamine salt of the compound of Formula I.18. The method of claim 17 , wherein the derivatizing reagent comprises 3 claim 17 ,5-dinitrobenzoyl chloride and the alcohol comprises methanol.20. The method of claim 19 , further comprising the step:xlii) recrystallizing the precipitate of step xli). This application is a divisional application of U.S. patent application Ser. No. 15/874,093, filed Jan. 18, 2018, which is a divisional application of U.S. patent application Ser. No. 15/583,457, filed May 1, 2017, now U.S. Pat. No. 9,908,834, issued Mar. 6, 2018, which is a divisional application of U.S. patent application Ser. No. 14/650,234, filed Jun. 5, 2015, which is a 35 U.S.C. § 371 United States National Phase Application of PCT Application Serial No. PCT/US2013/073474, filed Dec. 6, 2013, which claims the benefit of and priority to U.S. provisional application Ser. No. 61/734,672, filed Dec. 7, 2012, and 61/777,882, filed Mar. 12, 2013. The entire contents of the aforementioned disclosures are incorporated herein by reference in their entireties.The present invention relates to processes and intermediates for the preparation of prostacyclin analog that are useful for treating hypertension and other diseases.Prostacyclin derivatives and analogs are useful pharmaceutical compounds possessing activities such as platelet aggregation inhibition, gastric secretion reduction, lesion inhibition, vasodilation, and bronchodilation.Treprostinil is a synthetic prostacyclin ...

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Номер записи: 39
02-01-2020 дата публикации

METHODS OF PREPARING CYTOTOXIC BENZODIAZEPINE DERIVATIVES

Номер: US20200002360A1
Автор: Gerard Baudouin, Miller Michael Louis, Shizuka Manami, Silva Richard A.
Принадлежит:

The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors. 140-. (canceled)44. (canceled)45. The method of claim 41 , wherein the reaction between the compound of formula (I) and hydrochloric acid is carried out at a temperature between 40° C. and 105° C.46. The method of claim 45 , wherein the reaction is carried out at a temperature between 90° C. and 100° C.4755-. (canceled)56. The method of claim 42 , wherein the alcohol activating agent is triphenylphosphine and the azodicarboxylate is diisopropyl azodicarboxylate (DIAD).5758-. (canceled)59. The method of claim 42 , wherein the reaction of step 2) comprises the steps of i) mixing the alcohol activating agent and the azodicarboxylate to form an alcohol activating agent-azodicarboxylate complex; ii) reacting the compound of formula (II) with the alcohol activating agent-azodicarboxylate complex to form a mixture of the compound of formula (II) and the alcohol activating agent-azodicarboxylate complex; and iii) reacting the mixture of step ii) with the monomer compound of formula (a).6061-. (canceled)62. The method of claim 42 , wherein in step 3) claim 42 , the base is potassium carbonate.63. The method of claim 62 , wherein in step 3) claim 62 , the reaction between the compound of formula (III) or a salt thereof and the monomer compound of formula (b) is carried out in the presence of potassium iodide.64. The method of claim 43 , wherein in step 4) claim 43 , the reducing agent is Fe/NHCl.66. (canceled)67. The method of claim 65 , wherein Pand Pare both —OBu.6875-. (canceled)76. The method of claim 65 , wherein the activating agent 2 claim 65 ,4 claim 65 ,6-tripropyl-1 claim 65 ,3 claim 65 ,5 claim 65 ,2 claim 65 ,4 claim 65 ,6-trioxatriphosphorinane 2 claim 65 ,4 claim 65 ,6-trioxide.77. The method of claim 42 , wherein the reaction between the compound of formula (I) and hydrochloric acid is carried out at a temperature between 40° C. and 105° C. ...

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Номер записи: 40
07-01-2021 дата публикации

CHEMICALLY CLEAVABLE GROUP

Номер: US20210002320A1
Автор: Robillard Marc Stefan, ROSSIN RAFFAELLA, Ten Hoeve Wolter, Versteegen Ronny Mathieu
Принадлежит: TAGWORKS PHARMACEUTICALS B.V.

Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactice components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine. 1. A dienophile as a chemically cleavable group attached to a Construct , thereby provoking the release , in vitro , of the Construct by allowing the dienophile to react with a diene , wherein the dienophile is an eight-membered non-aromatic cyclic alkenylene group , preferably a cyclooctene group , and more preferably a trans-cyclooctene group.11. The dienophile according to claim 10 , wherein the diene satisfies formula (7) as defined in the description. This application is a continuation of U.S. application Ser. No. 14/646,619, filed May 21, 2015, which in turn is a 371 of PCT/NL2013/050850, filed Nov. 22, 2013, which claims the benefit of priority from European Patent Application No. 12193911.0, filed Nov. 22, 2012, the contents of each of which are hereby incorporated by reference.The invention pertains to the field of provoked chemical cleavage. Particularly, the invention pertains to providing chemical substances with a functional group capable of acting as a Trigger for release of an entity attached to said chemical group. This plays a role, e.g., in solid phase synthesis, biomolecule interactions, modification of surfaces (including cell surfaces), and modification of molecules under physiological conditions (e.g., in a cellular environment).The current state of the art in organic chemistry enables the preparation of highly complex molecular structures, by application of a wide toolbox of synthetic transformations. Unfortunately, the vast majority of chemical techniques is executed under strictly defined conditions, requiring toxic solvents, stoichiometric reagents, extreme ...

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Номер записи: 41
01-01-2015 дата публикации

SMALL MOLECULE XANTHINE OXIDASE INHIBITORS AND METHODS OF USE

Номер: US20150004699A1
Автор: Chen Changyi, Lu Jian-Ming, Yao Qizhi
Принадлежит:

Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. 115-. (canceled) This application claims priority to U.S. Provisional Application No. 61/734,409, filed Dec. 7, 2012, which is incorporated herein by reference in its entirety.Gout is caused by hyperuricemia, namely, abnormally high levels of uric acid in the blood. Gout is usually present as acute inflammatory arthritis, as well as tophi, kidney stones, or urate nephropathy. Gout affects 1-2% of adults in developed countries and represents the most common case of inflammatory arthritis in men. In the United States, gouty arthritis accounts for millions of outpatient visits annually. Furthermore, gout and hyperuricemia are associated with chronic diseases such as hypertension, diabetes mellitus, metabolic syndrome, and renal and cardiovascular disease.Xanthine oxidase (XO) is a form of a molybdoflavin protein, xanthine oxidoreductase (XOR). It plays an important role in the catabolism of purines in humans, as it catalyzes the oxidation of hypoxanthine to xanthine and then catalyzes the oxidation of xanthine to uric acid. Meanwhile, reactive oxygen species (ROS), including superoxide and HO, are generated during this process. Uric acid can serve as an antioxidant to prevent macromolecular damage by ROS. However, overproduction of uric acid can cause hyperuricemia and lead to gout and other diseases. Therefore, maintaining uric acid at normal levels represents an important therapeutic goal for the prevention of gout and related disorders. For most patients with primary gout, overproduction of uric acid is the primary cause of hyperuricemia.Currently, two drugs have been developed to treat gout. Allopurinol is the most commonly used therapy for chronic gout and has been used clinically for more than 40 years. Allopurinol lowers uric acid production by inhibiting XO activity, and is used as a first-line urate-lowering phamacotherapy. Allopurinol, ...

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Номер записи: 42
01-01-2015 дата публикации

Small Molecule Xanthine Oxidase Inhibitors and Methods of Use

Номер: US20150005389A1
Автор: Chen Changyi, Lu Jian-Ming, Yao Qizhi
Принадлежит:

Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. 115-. (canceled)18. The method of claim 16 , wherein the compound is administered orally. This application claims priority to U.S. Provisional Application No. 61/734,409, filed Dec. 7, 2012, which is incorporated herein by reference in its entirety.Gout is caused by hyperuricemia, namely, abnormally high levels of uric acid in the blood. Gout is usually present as acute inflammatory arthritis, as well as tophi, kidney stones, or urate nephropathy. Gout affects 1-2% of adults in developed countries and represents the most common case of inflammatory arthritis in men. In the United States, gouty arthritis accounts for millions of outpatient visits annually. Furthermore, gout and hyperuricemia are associated with chronic diseases such as hypertension, diabetes mellitus, metabolic syndrome, and renal and cardiovascular disease.Xanthine oxidase (XO) is a form of a molybdoflavin protein, xanthine oxidoreductase (XOR). It plays an important role in the catabolism of purines in humans, as it catalyzes the oxidation of hypoxanthine to xanthine and then catalyzes the oxidation of xanthine to uric acid. Meanwhile, reactive oxygen species (ROS), including superoxide and HO, are generated during this process. Uric acid can serve as an antioxidant to prevent macromolecular damage by ROS. However, overproduction of uric acid can cause hyperuricemia and lead to gout and other diseases. Therefore, maintaining uric acid at normal levels represents an important therapeutic goal for the prevention of gout and related disorders. For most patients with primary gout, overproduction of uric acid is the primary cause of hyperuricemia.Currently, two drugs have been developed to treat gout. Allopurinol is the most commonly used therapy for chronic gout and has been used clinically for more than 40 years. Allopurinol lowers uric acid production by inhibiting XO activity, ...

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Номер записи: 43
07-01-2021 дата публикации

NONAQUEOUS ELECTROLYTE, ENERGY STORAGE DEVICE, AND METHOD FOR PRODUCING ENERGY STORAGE DEVICE

Номер: US20210005931A1
Автор: HACHIDA Takeshi, NISHIE Katsushi
Принадлежит:

Provided is a nonaqueous electrolyte capable of suppressing swelling of an energy storage device caused by repeated charge-discharge, an energy storage device including the nonaqueous electrolyte, and a method for producing the energy storage device. One aspect of the present invention is a nonaqueous electrolyte which is used for an energy storage device and contains halogenated toluene and halogenated nitrotoluene. Another aspect of the present invention is an energy storage device including the nonaqueous electrolyte. Another aspect of the present invention is a method for producing an energy storage device, which uses the nonaqueous electrolyte. 1. A nonaqueous electrolyte which is used for an energy storage device and comprises halogenated toluene and halogenated nitrotoluene.2. The nonaqueous electrolyte according to claim 1 , wherein the halogenated toluene is fluorotoluene.3. The nonaqueous electrolyte according to claim 1 , wherein a content of the halogenated toluene is 0.1% by mass or more and 8% by mass or less based on a total mass of the nonaqueous electrolyte.4. The nonaqueous electrolyte according to claim 1 , wherein the halogenated nitrotoluene is fluoronitrotoluene.5. The nonaqueous electrolyte according to claim 1 , wherein a content of the halogenated nitrotoluene is 0.001% by mass or more and 3% by mass or less based on the total mass of the nonaqueous electrolyte.6. An energy storage device comprising the nonaqueous electrolyte according to .7. A method for producing an energy storage device claim 1 , the method using the nonaqueous electrolyte according to . The present invention relates to a nonaqueous electrolyte, an energy storage device, and a method for producing an energy storage device.Nonaqueous electrolyte secondary batteries typified by lithium ion secondary batteries are widely used in electronic apparatuses such as personal computers and communication terminals, automobiles and the like because of their high energy density. In ...

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Номер записи: 44
08-01-2015 дата публикации

Substitute diphenylamine compounds use thereof as antitumor agents

Номер: US20150011628A1
Автор: Aiying Guan, Baoshan Chai, Changling Liu, Huichao Li
Принадлежит: Shenyang Research Institute of Chemical Industry Co Ltd, Sinochem Corp

The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.

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Номер записи: 45
10-01-2019 дата публикации

Methods for the synthesis of activated ethylfumarates and their use as intermediates

Номер: US20190010131A1
Автор: Freeman John J., Kaur Navneet, Kraft Kelly Sullivan, Pavia Vincent, Phanstiel Otto, Serwinski Paul
Принадлежит:

Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput. 2. The method of claim 1 , wherein the organic solvent is selected from acetone claim 1 , acetonitrile claim 1 , ethyl acetate claim 1 , tetrahydrofuran claim 1 , and dichloromethane.3. The method of claim 1 , wherein the inorganic metallic base is selected from sodium carbonate and sodium hydroxide.4. The method of claim 1 , wherein the base is provided in an amount of 1 to 2 equivalents based on the amount of 4-nitrophenol.5. The method of claim 1 , wherein the ethyl fumaryl chloride is provided in an amount of 0.5 to 2 equivalents based on the amount of 4-nitrophenol.6. The method of claim 1 , wherein the inorganic metallic base is added as an aqueous mixture to a solution of 4-nitrophenol in the organic solvent.7. The method of claim 1 , wherein the ethyl fumaryl chloride is added to a mixture of 4-nitrophenol and the inorganic metallic base claim 1 , with cooling.8. The method of claim 1 , wherein the aminoalkyl-diketopiperazine is mixed with an organic solvent to form an aminoalkyl-diketopiperazine-containing mixture prior to adding the aminoalkyl-diketopiperazine.9. The method of claim 8 , wherein the organic solvent in the aminoalkyl-diketopiperazine-containing mixture is the same organic solvent used to form the mono-ethyl fumarate ester.10. The method of claim 8 , wherein the ...

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Номер записи: 46
21-01-2016 дата публикации

BICYCLO [2.2.1] ACID GPR120 MODULATORS

Номер: US20160016880A1
Автор: Cheng Peter T.W., Shi Yan, Wang Ying, Wu Shung C., ZHANG Hao
Принадлежит:

The present invention provides compounds of Formula (I): (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

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Номер записи: 47
18-01-2018 дата публикации

PROCESS FOR THE PREPARATION OF BENZONORBORNENES

Номер: US20180016211A1
Автор: ANTELMANN Bjorn, BOIS Fanny, DE MESMAEKER Alain, Gribkov Denis, Walter Harald
Принадлежит: SYNGENTA CROP PROTECTION, LLC

The present invention relates to a novel a process for the preparation of 9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-ylamine which process comprises a) reacting cyclopentadiene in the presence of a radical initiator and CXCl3, wherein X is chloro or bromo, to a compound of formula II, or aa) reacting cyclopentadiene with CXCl3, wherein X is chloro, in the presence of a metal catalyst to a compound of formula II, wherein X is chloro, b) reacting the compound of formula II with a base in the presence of an appropriate solvent to the compound of formula III, c) and converting the compound of formula III in the presence of 1,2-dehydro-6-nitrobenzene to the compound of formula IV, and d) hydrogenating the compound of formula IV in the presence of a metal catalyst. 1. A compound of formula IV This application is a divisional of U.S. patent application Ser. No. 14/603857, filed Jan. 23, 2015 which is a divisional of U.S. patent application Ser. No. 13/126380 filed Apr. 27, 2011, now patented as U.S. Pat. No. 9,115,043 issued Aug. 25, 2015, which was a 371 application of International Application No. PCT/EP2009/062525, filed Sep. 28, 2009, which claims priority to EP Patent Application 08018721.4, filed Oct. 27, 2008, and EP Patent Application No. 09161388.5 filed May 28, 2009, the contents of which are incorporated herein by reference herein.The present invention relates to the preparation of 9-dichloromethylene-1,2,3,4-tetrahydro-1, 4-methano-naphthalen-5-ylamine.The compound 9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-ylamine is a valuable intermediate for the preparation of benzonorbornene fungicides, as described for example in WO 2007/048556.It is known from WO 2007/048556 to prepare 9-dichloromethylene-1,2,3,4-tetrahydro-1, 4-methano-naphthalen-5-ylamine bya) reacting the compound of formula Ain the presence of an alkyl nitrite with a compound of formula Bwherein R′ and R″ are e.g. C-Calkyl, to a compound of formula Cb) ...

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Номер записи: 48
17-04-2014 дата публикации

Biobased plasticizer and surface covering employing same

Номер: US20140102335A1
Автор: DONG Tian, Mary Kate DAVIES
Принадлежит: AWI Licensing LLC

Described herein are biobased plasticizer compositions comprising a compound having the structure of Formula I: wherein R is C 6 -C 1 alkyl; along with methods of making and using same.

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Номер записи: 49
16-01-2020 дата публикации

PROCESS AND PLANT FOR THE ADIABATIC NITRATION OF AROMATIC COMPOUNDS

Номер: US20200017421A1
Автор: FANKEL Stefan, HÄNDEL Dr. Mirko, HERMANN Dr. Heinrich, PÖHLMANN Dr. Jürgen, Wernitz Sophie
Принадлежит: Josef Meissner GmbH & Co. KG

The invention relates to a method for preferably adiabatic nitration of nitratable aromatic organic compounds (aromatics) and to a corresponding plant, in particular a production plant (nitration plant) for carrying out said method. 115-. (canceled)16. A process for the adiabatic nitration of nitratable aromatic organic compounds for producing the corresponding nitrated aromatic organic compounds ,wherein the nitratable aromatic organic compounds are converted, via a nitration reaction in the presence of a nitrating acid mixture comprising nitric acid and sulfuric acid, into the corresponding nitrated aromatic organic compounds,wherein the corresponding nitrated aromatic organic compounds are added to a reaction starting mixture, which reaction starting mixture comprises (i) the nitratable aromatic organic compounds to be nitrated and (ii) a nitrating acid mixture comprising nitric acid and sulfuric acid, and wherein the nitration reaction is started and carried out in the presence of the corresponding nitrated aromatic organic compounds; andwherein the nitrated aromatic organic compounds obtained are partly recirculated to the nitration reaction and the subsequent nitration reaction is started and carried out in the presence of these nitrated aromatic organic compounds;wherein the nitration reaction is carried out under adiabatic reaction conditions,wherein the nitration reaction is carried out in a tube reactor, andwherein the amount of corresponding nitrated aromatic organic compounds added to the nitration reaction is selected in such a way that the amount of added nitrated aromatic organic compounds effects lowering of the interfacial tension between organic phase and acid phase and effects an improved dispersibility of organic phase and acid phase.17. The process as claimed in claim 16 ,wherein the spent nitrating acid mixture resulting after the nitration reaction is recycled and circulated to the nitration reaction after the crude nitrated aromatic organic ...

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Номер записи: 50
10-02-2022 дата публикации

ELECTROPHILES AND ELECTROPHILE PRO-DRUGS AS RAD51 INHIBITORS

Номер: US20220040134A1
Автор: Freeman Bruce A., Neumann Carola, Schopfer Francisco J.
Принадлежит: University of Pittsburgh - of the Commonwealth System of Higher Education

A method comprising co-administering to a subject having cancer, suspected of having cancer, or at risk of developing cancer: 1. A method comprising co-administering to a subject having cancer , suspected of having cancer , at risk of developing cancer , or in cancer remission:a therapeutically effective amount of at least one compound (a) selected from (a)(i) a nitroalkene fatty acid, (a)(ii) an unsaturated fatty acid having an electron withdrawing group, a leaving group, and a carbon-carbon double bond disposed between the electron withdrawing group and the leaving group, (a)(iii) a thiolated nitro fatty acid, or (a)(iv) a dicarboxylic acid compound containing an electron withdrawing group; anda therapeutically effective amount of at least one anti-neoplastic agent (b),wherein the cancer is a cancer with hereditary etiology of defects in DNA repair genes, a cancer with a high rate of spontaneous genomic instability, a cancer that is treated with DNA damaging agent(s), or a cancer that is treated with a combination of DNA damaging agent(s) with immunotherapy.2. The method of claim 1 , wherein the cancer is breast cancer claim 1 , colon cancer claim 1 , prostate cancer claim 1 , pancreatic cancer claim 1 , ovarian cancer claim 1 , brain cancer claim 1 , or skin cancer.3. The method of claim 1 , wherein the cancer is triple negative breast cancer.4. The method of claim 1 , wherein the cancer is fibrosarcoma claim 1 , myxosarcoma claim 1 , liposarcoma claim 1 , chondrosarcoma claim 1 , osteogenic sarcoma claim 1 , chordoma claim 1 , angiosarcoma claim 1 , endotheliosarcoma claim 1 , lymphangiosarcoma claim 1 , lymphangioendotheliosarcoma claim 1 , synovioma claim 1 , mesothelioma claim 1 , Ewing's tumor claim 1 , leiomyosarcoma claim 1 , rhabdomyosarcoma claim 1 , colon carcinoma claim 1 , pancreatic cancer claim 1 , breast cancer claim 1 , ovarian cancer claim 1 , prostate cancer claim 1 , squamous cell carcinoma claim 1 , basal cell carcinoma claim 1 , ...

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Номер записи: 51
25-01-2018 дата публикации

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF NEP INHIBITORS

Номер: US20180022690A1
Автор: MANDRELLI Francesca, MARTIN Benjamin, VENTURONI Francesco
Принадлежит:

The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route. 7. The process according to claim 6 , comprising the step of simultaneously or separately esterifiying the obtained compound of formula (1) claim 6 , or a salt thereof claim 6 , wherein R1 is hydrogen claim 6 , with a C-C-aliphatic alcohol claim 6 , to yield the compound of formula (1) wherein R1 is C-C-alkyl.15. (canceled)19. (canceled)21. (canceled)24. (canceled) The present invention relates to a new chemical synthesis route and intermediates useful for the preparation of neprilysin (NEP) inhibitors and their prodrugs, in particular for the NEP inhibitor prodrug sacubitril.The NEP inhibitor prodrug sacubitril (N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester; IUPAC name 4-{[(1S,3R)-1-([1,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoic acid) is represented by the following formula (A)Sacubitril together with valsartan, a known angiotensin receptor blocker (ARB), forms a sodium salt hydrate complex, known as LCZ696, comprising the anionic forms of sacubitril and valsartan, sodium cations and water molecules in the molar ratio of 1:1:3:2.5, respectively (ratio of 6:6:18:15 in the asymmetric unit cell of the solid state crystal), and which is schematically present in formula (B).Said complex is also referred to by the following chemical names: Trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate or Octadecasodium hexakis(4-{[(1S,3R)-1-([1,1′-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate) hexakis(N-pentanoyl-N-{[2′-(1H-tetrazol-1-id-5-yl)[1,1′-biphenyl]-4-yl]methyl}-L- ...

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Номер записи: 52
22-01-2015 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20150025077A1
Автор: Argade Ankush B., Datwani Akash, Ermini Florian, Pan Yonghua, Serizawa Hiroaki, Spencer Natalie
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.43. A pharmaceutical composition comprising a compound of any one of - and a pharmaceutically acceptable excipient.53. A pharmaceutical composition comprising a sufficient amount of 5E claims 1 , 9E claims 1 , 13E geranylgeranyl acetone or a GGA derivative of any one of - claims 1 , and optionally at least one pharmaceutical excipient claims 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more ...

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Номер записи: 53
10-02-2022 дата публикации

Resist composition and patterning process

Номер: US20220043343A1
Автор: Jun Hatakeyama, Tomomi Watanabe
Принадлежит: Shin Etsu Chemical Co Ltd

A resist composition is provided comprising a base polymer and a quencher comprising a cyclic ammonium salt having a fluorinated saturated hydrocarbyl group or fluorinated aryl group. The resist composition has a high sensitivity and forms a pattern with improved LWR or CDU, independent of whether it is of positive or negative tone.

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Номер записи: 54
02-02-2017 дата публикации

LABILE ESTERS OF AGROCHEMICALS FOR CONTROLLED RELEASE AND REDUCTION OF OFF-SITE MOVEMENT

Номер: US20170029355A1
Автор: Morgenstern David A.
Принадлежит:

The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical. 2. The ester of a carboxylic acid agrochemical of claim 1 , wherein the carboxylic acid agrochemical is a herbicide claim 1 , a fungicide claim 1 , an insecticide claim 1 , a plant health agent claim 1 , or a plant growth regulator.3. The ester of a carboxylic acid agrochemical of claim 2 , wherein the carboxylic acid agrochemical is a herbicide selected from the group consisting of dicamba claim 2 , 2 claim 2 ,4-dichlorophenoxyacetic acid (2 claim 2 ,4-D) claim 2 , fenoxaprop claim 2 , fenoxaprop-P claim 2 , desmedipham claim 2 , cyhalofop claim 2 , carfentrazone claim 2 , flufenpyr claim 2 , fluthiacet claim 2 , fluroglycofen claim 2 , pyraflufen claim 2 , flumiclorac claim 2 , 4-(4-chloro-2-methylphenoxy)butanoic acid (MCPB) claim 2 , fluroxypyr claim 2 , picloram claim 2 , quinclorac claim 2 , benazolin claim 2 ,clodinafop, 4-(2,4-dichlorophenoxy)butanoic acid (2,4-DB), 2,4,5-trichlorophenoxyacetic acid (2,4,5-T), dichlorprop, dichlorprop-P, diethatyl, endothall, fluazifop, flufenpyr, flumiclorac, fluoroglycofen, haloxyfop, indole-3-acetic acid, indole-3-butyric acid, mecoprop, mecoprop-P, pyrafluren, fenoprop, triclopyr, aminopyralid, bispyribac, chlorthal, imazamethabenz, pyrothiobac, quinmerac, quizalofop, quizalofop-P, diclofop, and lactofen.4. The ester of a carboxylic ...

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Номер записи: 55
02-02-2017 дата публикации

HALOGENATED ANILINE AND METHOD FOR PRODUCING SAME

Номер: US20170029361A1
Автор: Inoue Hiroki, ITO Yoshikazu, KITAYAMA Takashi, Kobayashi Shinichi, Sakata Yuzuru
Принадлежит: NIPPON SODA CO., LTD.

The present invention provides a halogenated aniline represented by formula (I) (wherein each of Xand Xindependently represents a chlorine atom, a bromine atom or an iodine atom), a method for producing the halogenated aniline, and other aspects. 1. (canceled)34.-. (canceled)6. The method for producing a halogenated nitrobenzene according to claim 5 , wherein fuming sulfuric acid and concentrated nitric acid are added to the halogenated benzene represented by formula (III) to nitrate the halogenated benzene.7. The method for producing a halogenated nitrobenzene according to claim 5 , wherein fuming sulfuric acid and fuming nitric acid are added to the halogenated benzene represented by formula (III) to nitrate the halogenated benzene.810.-. (canceled)11. A method for producing 1 claim 5 ,2-dichloro-4 claim 5 ,5-difluorobenzene claim 5 , comprising a step of chlorinating 1 claim 5 ,2-difluorobenzene. The present invention relates to a novel halogenated aniline, which can be used as a production raw material for compounds that are useful as electronic materials, medicines, and agricultural chemicals and the like, as well as a method for producing the halogenated aniline.Priority is claimed on Japanese Patent Application No. 2012-280691, filed Dec. 25, 2012, the content of which is incorporated herein by reference.The compound 2,3-difluoroaniline is the starting raw material for producing 2-[2-fluoro-6-(7,8-difluoro-2-methylquinolin-3-yloxy)phenyl]propan-2-ol and 2-[2-fluoro-6-(7,8-difluoroquinolin-3-yloxy)phenyl]propan-2-ol, which are known as active ingredients for agricultural and horticultural germicides (Patent Document 1).Further, 2,3-difluoroaniline is also used in the production of medicines such as antibiotics (Patent Document 2), c-Met protein kinase inhibitors (Patent Document 3), drugs for Alzheimer's disease (Patent Document 4), Aurora B kinase inhibitors (Patent Document 5), and drugs for neuropathic pain (Patent Document 6).Moreover, 2,3-difluoroaniline ...

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Номер записи: 56
29-01-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150031722A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 57
02-02-2017 дата публикации

IODONIUM ANALOGS AS INHIBITORS OF NADPH OXIDASES AND OTHER FLAVIN DEHYDROGENASES; FORMULATIONS THEREOF; AND USES THEREOF

Номер: US20170029424A1
Автор: DOROSHOW James Halpern, HOSSAIN Md Tafazzal, JR. Charles T., KANE, LU Jaimo, RISBOOD Prabhakar, ROY Krishnendu
Принадлежит:

Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity. 2. The method of claim 1 , wherein X is a halide claim 1 , an alkyl sulfonate claim 1 , an aryl sulfonate claim 1 , a phosphate claim 1 , or a nitrate.3. The method of claim 1 , wherein X is chloride claim 1 , bromide claim 1 , iodide claim 1 , CHSO— claim 1 , CHSO— claim 1 , CFSO— claim 1 , 4-CHCHSO— claim 1 , or CHSO—.4. The method of claim 1 , wherein Arand Arare each independently phenyl claim 1 , naphthyl claim 1 , bi-phenyl claim 1 , benzofuranyl claim 1 , benzothiazolyl claim 1 , coumarinyl claim 1 , furanyl claim 1 , imidazolyl claim 1 , imidazo[1 claim 1 ,2-a]pyridine claim 1 , indolyl claim 1 , isoquinolinyl claim 1 , isoxazolyl claim 1 , 3-methylisoxazole claim 1 , oxazolyl claim 1 , pyrazinyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , pyrrolyl claim 1 , quinazolinyl claim 1 , quinolinyl claim 1 , thiazolyl claim 1 , triazinyl claim 1 , or thienyl.5. The method of claim 1 , wherein Cy is cyclohexanone or a 3-hydroxycyclohex-2-enone.6. The method of claim 1 , wherein{'sup': '1', 'Aris thienyl,'}{'sup': '2', 'Aris thienyl, and'}Z is absent;{'sup': 1', 'a', '2', 'b, 'wherein Aris substituted by a Rgroup, Aris substituted by a Rgroup, or a combination thereof.'}7. The method of claim 1 , wherein{'sup': '1', 'Aris phenyl,'}{'sup': '2', 'Aris thienyl, and'}Z is absent;{'sup': 1', 'a', '2', 'b, 'wherein Aris substituted by a Rgroup, Aris substituted by a Rgroup, or a combination thereof.'}8. The method of claim 1 , wherein{'sup': '1', 'Aris quinolinyl,'}{'sup': '2', 'Aris quinolinyl, and'}Z is absent or O.9. The method of claim 1 , wherein{'sup': '1', 'Aris phenyl,'}{'sup': '2', 'Aris phenyl, and'}{'sub': 2', '2', '6, 'sup': c', 'c, 'Z is absent, a bond, O, S, CH, or NRwhere Ris C-Calkanoyl;'}{'sup': 1', 'a', '2', 'b, 'wherein Aris substituted by a Rgroup, Aris substituted by a Rgroup, or a combination thereof.'}10. The method of claim 1 , wherein{'sup': '1', ' ...

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Номер записи: 58
31-01-2019 дата публикации

PHOSPHINE SUBSTITUTED FERROCENYL COMPLEX

Номер: US20190031697A1
Автор: AZIZ Md. Abdul, HELAL Aasif, SHAIKH M. Nasiruzzaman
Принадлежит: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS

A functionalized magnetic nanoparticle including an organometallic sandwich compound and a magnetic metal oxide. The functionalized magnetic nanoparticle may be reacted with a metal precursor to fol in a catalyst for various C—C bond forming reactions. The catalyst may be recovered with ease by attracting the catalyst with a magnet. 2. (canceled)3. The complex of claim 1 , wherein Ris an optionally substituted alkyl.4. The complex of claim 1 , wherein Ris an optionally substituted aryl.5. The complex of claim 1 , wherein X is NH.620-. (canceled) This application claims the priority of the filing date of the U.S. Provisional Patent Application No. 62/406,449 filed Oct. 11, 2016, the disclosure of which is hereby incorporated herein by reference in its entirety.This project was funded by the National Plan for Science, Technology and Innovation (MAARIFAH)-King Abdulaziz City for Science and Technology through the Science and Technology Unit at King Fahd University of Petroleum and Minerals (KFUPM), the Kingdom of Saudi Arabia, award number 15-NAN4650-04.Aspects of this technology are described in an article “Magnetic nanoparticle-supported ferrocenylphosphine: a reusable catalyst for hydroformylation of alkene and Mizoroki-Heck olefination” by M. Nasiruzzaman Shaikh, Md. Abdul Aziz, Aasif Helal, Mohamed Bououdina, Zain H. Yamania, and Tae-Jeong Kim, in RSC Advances, 2016, pages 41687-41695, which is incorporated herein by reference in its entirety.The present disclosure relates to a functionalized magnetic nanoparticle including an organometallic sandwich compound and a functional group which can bind to a nanoparticle. The disclosure also relates to a magnetic catalyst which catalyzes C—C bond forming reactions such as hydroformylation and the Mizoroki-Heck coupling reaction.Carbon-carbon bond formation reactions mediated by various transition metals have emerged as increasingly important methodologies for the preparation of numerous organic building blocks for drugs, ...

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Номер записи: 59
11-02-2016 дата публикации

Methods for synthesis of graphene derivatives and functional materials from asphaltenes

Номер: US20160039678A1
Автор: Olanrewaju W. Tanimola
Принадлежит: Individual

Embodiments described are directed to methods for the functionalization of asphaltene materials and to compositions made from functionalized asphaltenes. Disclosed is a method for synthesizing graphene derivatives, such as 2D single crystalline carbon allotropes of graphene and functional materials, such as sulfonic acid and its derivatives. Also disclosed is a method for the transformation of asphaltene into a source of graphene derivatives and functional materials, such as, 0D, 1D, 2D and combinations of 0D and 1D by utilizing chemical substitution reaction mechanism, such as, electrophilic aromatic substitution, nucleophilic aromatic substitution and Sandmeyer mechanism. Also disclosed are novel graphene materials comprising: acetylenic linkage and hydrogenated graphene. These novel materials, which may be produced by these methods, include, e.g.: 2D single crystalline carbon allotropes of graphene with asymmetric unit formulas C 7 H 6 N 2 O 4 , C 6 H 4 N 2 O 4 , C 7 H 7 O 3 S− H 3 O+, C 7 H 7 O 3 SH+, and a 2D single crystal with asymmetric unit formula (Na 6 O 16 S 4 )n.

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Номер записи: 60
11-02-2016 дата публикации

NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE

Номер: US20160039843A1
Автор: Green George D., James Richard L., Swedo Raymond J., Tomlinson Ian A., Trauth Daniel M.
Принадлежит:

Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications. 2. The compound of selected from formula I-1.3. The compound of claim 2 , wherein Rand Rare unsubstituted.4. The compound of claim 2 , wherein the compound is selected from the group consisting of 3-nitrodecane claim 2 , 4-nitrodecane claim 2 , 5-nitrodecane claim 2 , 4-nitrotridecane claim 2 , 5-nitrotridecane claim 2 , 7-nitrotridecane claim 2 , 2-nitrotetradecane claim 2 , 3-nitrotetradecane claim 2 , 4-nitrotetradecane claim 2 , 5-nitrotetradecane claim 2 , 6-nitrotetradecane claim 2 , 7-nitrotetradecane claim 2 , 2-nitropentadecane claim 2 , 3-nitropentadecane claim 2 , 4-nitropentadecane claim 2 , 5-nitropentadecane claim 2 , 6-nitropentadecane claim 2 , 7-nitropentadecane claim 2 , 8-nitropentadecane claim 2 , 3-nitrohexadecane claim 2 , 4-nitrohexadecane claim 2 , 5-nitrohexadecane claim 2 , 6-nitrohexadecane claim 2 , 7-nitrohexadecane claim 2 , 8-nitrohexadecane claim 2 , 2-nitroheptadecane claim 2 , 3-nitroheptadecane claim 2 , 4-nitroheptadecane claim 2 , 5-nitroheptadecane claim 2 , 6-nitroheptadecane claim 2 , 7-nitroheptadecane claim 2 , 8-nitroheptadecane claim 2 , 9-nitroheptadecane claim 2 , 3-nitrooctadecane claim 2 , 4-nitrooctadecane claim 2 , 5-nitrooctadecane claim 2 , 6-nitrooctadecane claim 2 , 7-nitrooctadecane claim 2 , 8-nitrooctadecane claim 2 , and 9-nitrooctadecane.5. The compound of selected from formula II-1.6. The compound of claim 5 , wherein Ris a linear C-Calkyl; and Ris H claim 5 , linear C-Calkyl claim 5 , or CHOH.7. The compound of claim 5 , wherein Ris H or linear C-Calkyl claim 5 , and Rand R claim 5 , together with the carbon to which they are attached form a linear C-Calkyl ...

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Номер записи: 61
09-02-2017 дата публикации

NITRIFICATION INHIBITORS

Номер: US20170036969A1
Автор: Dickhaut Joachim, EBENHOECH Johan, Nave Barbara, SISAY Mihiret Tekeste, WEIGELT Wolfgang, Wissemeier Alexander, ZERULLA Wolfram
Принадлежит:

The present invention relates to novel nitrification inhibitors of formula I. Moreover, the invention relates to the use of these novel nitrification inhibitors for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors. Further encompassed by the present invention are methods for reducing nitrification comprising the treatment of plants, soil and/or loci with said nitrification inhibitors, and methods for treating a fertilizer or a composition by applying said nitrification inhibitor. 116-. (canceled)18: The compound of claim 17 , wherein in said compound of formula I claim 17 , A is phenyl or a 6-membered hetaryl claim 17 , preferably phenyl claim 17 , wherein the aromatic ring may in each case be unsubstituted or may be partially or fully substituted by substituents claim 17 , which are independently of each other selected from R.19: The compound of claim 17 , wherein in said compound of formula I claim 17 , Rand Rboth represent hydrogen.20: The compound of claim 17 , wherein in said compound of formula I claim 17 , Ris hydrogen claim 17 , C-C-haloalkyl or ethinylhydroxymethyl claim 17 , and preferably Ris hydrogen.21: The compound of claim 17 , wherein in said compound of formula I claim 17 , R claim 17 , if present claim 17 , is{'sup': a', 'b', 'c', '1', 'c', '1', 'c', '1', 'c', '1', 'a', 'b', '2', '1', '2', '1', 'a', 'b', 'g', 'd', 'e', 'f, 'sub': 2', '2', '1', '6', '2', '6', '1', '4', '1', '4', '2', '4', '1', '2', '2', '4, '(i) halogen, CN, NRR, OR, C(═Y)R, C(═Y)OR, C(═Y)SR, C(═Y)NRR, YC(═Y)R, YC(═Y)NRR, NRN═C(R)(R), S(═O)R, NO, C-C-alkyl, C-C- C-C-haloalkyl, C-C-alkoxy, C-C-alkynyl-C-C-hydroxyalkyl, C-C-alkynyloxy;'}{'sub': 2', '4', '2', '4', '1', '4', '2', '4, 'sup': 1', 'c', '2', '1', 'c, '(ii) C-C-alkenylene-C(═Y)R, C-C-alkenylene-Y—C(═Y)R, wherein the C-C-alkylene or C-C-alkenylene chain may in each case be unsubstituted or may be partially or fully substituted by CN or halogen;'}{'sup': 'h', '( ...

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Номер записи: 62
09-02-2017 дата публикации

Method of Manufacturing Nitrone Compound

Номер: US20170036989A1
Автор: Hong Bor-Cherng, LIN Cheng-Wei
Принадлежит:

A method of manufacturing nitrone compounds is provided. The method includes: providing a nitro compound; and performing a photoreaction of the nitro compound, a catalyst and an additive under visible light to obtain the nitrone compound. 1. A method of manufacturing nitrone compound , comprising:providing a nitro compound; andperforming a photoreaction of the nitro compound, a catalyst and an additive under visible light to obtain the nitrone compound.2. The method of claim 1 , wherein the catalyst is Ru(bpy)Cl.6HO claim 1 , Ru(bpy)Cl claim 1 , Ru(bpy)(BF) claim 1 , Ru(bpy)(PF) claim 1 , Ir[dF(CF)ppy](dtbbpy)(PF) or Ir(ppy)(dtbbpy)(PF).3. The method of claim 1 , wherein a wavelength of the visible light is within the range of 350 to 700 nm.4. The method of claim 3 , wherein a wavelength of the visible light is within the range of 450 to 460 nm.5. The method of claim 1 , wherein the nitro compound is a second order or third order nitro compound.6. The method of claim 1 , wherein the additive is diisopropylethylamine (DIPEA) claim 1 , diisopropylisobutylamine (DIPIBA) or a derivative of 1 claim 1 ,4-Dihydropyridine (DHP).7. The method of claim 6 , wherein when the additive is diisopropylisobutylamine (DIPIBA) claim 6 , an aldehyde compound is further added in the photoreaction.8. The method of claim 6 , wherein the derivative of 1 claim 6 ,4-Dihydropyridine (DHP) is Hantzsch ester.9. The method of claim 1 , wherein the catalyst is performed a photoredox catalyst reaction in the photoreaction. This application claims priority from Taiwan Patent Application No. 104125714, filed on Aug. 6, 2015, in the Taiwan Intellectual Property Office, the content of which are hereby incorporated by reference in their entirety for all purposes.1. Field of the InventionThe present invention relates to a manufacturing method, in particular with respect to a manufacturing method of manufacturing nitrone compound.2. Description of the Related ArtNitrone compound is a key intermediate for ...

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Номер записи: 63
09-02-2017 дата публикации

PHENYL BENZYL ETHER DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF

Номер: US20170037008A1
Автор: Cui Mengchao, GUO Yuzhi, Lin Chunping, Liu Boli, Zhang Zhiyong
Принадлежит:

Parts of compounds, after being labeled by radionuclide, of the phenyl benzyl ether derivative, are used as Aβ plaque imaging agent. The structural formula of the phenyl benzyl ether derivative is shown by formula (I). The present invention develops a kind of brand new phenyl benzyl ether derivative which has high affinity with Aβ plaques in brains of AD patients. The chemical structure of the phenyl benzyl ether derivative is different from that of compounds disclosed in the prior art and the phenyl benzyl ether derivative belongs to a brand new compound for diagnosing and treating AD. The obtained Aβ plaque imaging agent has the advantages that the in-vivo stability is good, the fat solubility is low, the removal speed for the brain is fast, the problem of removing the radionuclide in vivo does not exist, and the application prospect and the market value are great. 115-. (canceled)17. The phenyl benzyl ether derivative according to claim 16 , wherein Rand Rare o-substituents claim 16 , m-substituents or p-substituents.18. The phenyl benzyl ether derivative according to claim 16 , wherein the halogen is fluorine claim 16 , chlorine claim 16 , bromine or iodine; the alkoxy is C-Calkoxy claim 16 , preferably C-Calkoxy; the alkyl is C-Calkyl claim 16 , preferably C-Calkyl; the carbocyclic alkyl is three-membered to six-membered carbocyclic alkyl claim 16 , preferably cyclopropyl claim 16 , cyclopentyl or cyclohexyl; heterocyclic alkyl is three-membered to six-membered heterocyclic alkyl claim 16 , preferably piperidyl claim 16 , piperazinyl or morpholine cyclic group; the alkylamino is C-Calkylamino claim 16 , preferably C-Calkylamino claim 16 , more preferably N-methylamino claim 16 , dimethylamino claim 16 , diethylamino claim 16 , dipropylamino or diisopropylamino; the aryl is phenyl or naphthyl; the heteraryl is pyridyl claim 16 , furyl claim 16 , thienyl claim 16 , benzothiazolyl claim 16 , benzofuryl or benzoxazolyl; the arylalkoxy is C-Caryl C-Calkoxy claim 16 ...

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Номер записи: 64
07-02-2019 дата публикации

CELL SEEDING PLATE, METHOD FOR MANUFACTURING THE SAME, AND CELL SHEET SEPARATING METHOD

Номер: US20190039999A1
Автор: CHIEN HSIU-WEN
Принадлежит:

A cell seeding plate comprises a substrate and a photolysis layer formed on a surface of the substrate. The photolysis layer comprises a plurality of photolysis groups, and each of the plurality of photolysis groups has a chemical structural formula of 2. The cell seeding plate of claim 1 , wherein the substrate is transparent claim 1 , and made of plastic or glass.3. The cell seeding plate of claim 1 , wherein Ris a natural polymer comprising sulfur group or a synthetic polymer comprising sulfur group claim 1 , the natural polymer is selected from collagen claim 1 , hyaluronic acid claim 1 , protein for functionalizing cell claim 1 , or peptides for functionalizing cell.6. The method of claim 5 , wherein the substrate is transparent claim 5 , and made of plastic or glass.9. The cell sheet separating method of claim 8 , wherein the substrate is transparent claim 8 , and made of plastic or glass. The subject matter herein generally relates to a cell seeding plate, a method for manufacturing the cell seeding plate, and a cell sheet separating method using the cell seeding plate.Cells are usually seeded on a thermoresponsive plate to form a cell sheet. The whole thermoresponsive plate can be deformed when cooled, thus allowing the cell sheet to be separated from the thermoresponsive plate. However, an activity of the cells may be decreased when cooled.It will be appreciated that for simplicity and clarity of illustration, where appropriate, reference numerals have been repeated among the different figures to indicate corresponding or analogous elements. In addition, numerous specific details are set forth in order to provide a thorough understanding of the embodiments described herein. However, it will be understood by those of ordinary skill in the art that the embodiments described herein can be practiced without these specific details. In other instances, methods, procedures, and components have not been described in detail so as not to obscure the related relevant ...

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Номер записи: 65
01-05-2014 дата публикации

1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT

Номер: US20140121187A1
Автор: Choi Ihl Young, Han Soo Bong, Jung Young Sik, Kim Hae Soo, Kim Pil Ho, Lee Chong Kgo, Neyts Johan, Thibaut Hendrik Jan
Принадлежит:

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. 3. The 1 claim 1 ,3-Dioxoindene derivatives claim 1 , pharmaceutically-acceptable salt thereof or optical isomer thereof as set forth in claim 1 , wherein claim 1 , A claim 1 , A claim 1 , Aand Aare claim 1 , either independently or optionally claim 1 , any one selected from a group consisting of —H claim 1 , halogen and —NRR;{'sup': 1', '2', '1', '2, 'G is —OH, —NR(C═O)Ror —NR(C═O)OR;'}{'sup': 1', '2', '3', '4', '1', '2, 'sub': 1', '10, 'D, D, Dand Dare, either independently or optionally, any one selected from a group consisting of halogen, C˜Cstraight- or side-chain alkyl and —NR(C═O)R;'}{'sup': 1', '1', '1', '1', '2, 'E is —H, —OH, —OR, —O(C═O)R, —O(C═O)ORor —O(C═O)NRR;'}{'sup': 1', '2', '3, 'sub': 1', '8', '1', '4', '6', '10, 'R, Rand Rare, each independently, hydrogen, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkyl, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkenyl or C˜Caryl;'}X and Y are oxygen;{'sup': 1', '2', '3, 'Z, Zand Zare carbon;'}n is integer between 1˜3; and{'img': {'@id': 'CUSTOM- ...

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Номер записи: 66
01-05-2014 дата публикации

GEM-DINITRO ESTER COMPOUND AS ENERGETIC MATERIAL AND PREPARATION METHOD THEREOF

Номер: US20140121401A1
Автор: KIM Jin-Seuk, Kim Seung-Hee
Принадлежит: AGENCY FOR DEFENSE DEVELOPMENT

Provided is a gem-dinitro ester compound, represented by Formula 1 below: 2. The gem-dinitro ester compound of claim 1 , wherein the substituted or unsubstituted straight-chain or side-chain alkyl group of C˜Cis a substituted or unsubstituted straight-chain or side-chain butyl group claim 1 , pentyl group claim 1 , hexyl group claim 1 , heptyl group or octyl group.4. The method of claim 3 , wherein the substituted or unsubstituted straight-chain or side-chain alkyl group of C˜Cis a substituted or unsubstituted straight-chain or side-chain butyl group claim 3 , pentyl group claim 3 , hexyl group claim 3 , heptyl group or octyl group.5. The method of claim 3 , wherein the reaction of the compound represented by Formula 2 with the compound represented by Formula 3 is performed in the presence of a strong base.6. The method of claim 3 , wherein the reaction of the compound represented by Formula 2 with the compound represented by Formula 3 is performed using at least one solvent selected from the group consisting of lower alcohols of C˜Cand water. This application claims the benefit of Korean Patent Application No. 10-2012-0121335, filed on Oct. 30, 2012, which is hereby incorporated by reference in its entirety into this application.1. Technical FieldThe present invention relates to gem-dinitro ester compounds as energetic materials and a method of preparing the same.2. Description of the Related ArtA composite explosive has been developed in order to improve both performance and insensitivity of an explosive. Generally, a composite explosive includes a granular molecular explosive, such as a research development explosive (RDX), to provide explosiveness, and a binder composition. The binder composition is used in an amount of 2˜20 wt % based on the total amount of the composite explosive, and functions to provide dimensional stability and obtuseness to the granular molecular explosive. However, the binder composition does not have a nitro group for exhibiting ...

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Номер записи: 67
14-02-2019 дата публикации

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

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

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

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Номер записи: 68
14-02-2019 дата публикации

INSECT REPELLENT COMPOUNDS AND COMPOSITIONS, AND METHODS THEREOF

Номер: US20190047937A1
Автор: Coats Joel R., Klimavicz James Scott, Norris Edmund J.
Принадлежит:

The present invention relates to monoterpenoid and phenylpropanoid containing derivative compounds, methods of making the compounds, compositions comprising the compounds, and methods of repelling pests using the compounds and/or compositions. 2. The compound of claim 1 , wherein Ris a monoterpenoid moiety.4. The compound of claim 1 , wherein Ris a phenylpropanoid moiety.6. The compound of claim 1 , wherein Ris H.12. The compound of claim 11 , wherein{'sub': 3', '4, 'Rand Rare both H,'}{'sub': 3', '4', '3, 'Rand Rare both CH,'}{'sub': 3', '3', '4, 'Ris CHand Ris H, or'}{'sub': 3', '4, 'Ris allyl and Ris H.'}14. The compound of claim 1 , wherein the compound is selected from the group consisting of: menthyl cyclopropanecarboxylate claim 1 , citronellyl isovalerate claim 1 , citronellyl cyclopropanecarboxylate claim 1 , thymyl cyclopropanecarboxylate claim 1 , thymyl isovalerate claim 1 , eugenyl isovalerate claim 1 , carvacryl cyclopropanecarboxylate claim 1 , carvacryl isovalerate claim 1 , citronellyl formate claim 1 , thymyl formate claim 1 , carvacryl formate claim 1 , thymyl cyclobutanecarboxylate claim 1 , thymyl isobutyrate claim 1 , eugenyl formate claim 1 , eugenyl cyclopropanecarboxylate claim 1 , eugenyl isobutyrate claim 1 , eugenyl cyclobutanecarboxylate claim 1 , eugenyl isovalerate claim 1 , vanillin formate claim 1 , vanillin cyclopropanecarboxylate claim 1 , vanillin isobutyrate claim 1 , vanillin cyclobutanecarboxylate claim 1 , vanillin isovalerate claim 1 , myrtenyl cyclopropanecarboxylate claim 1 , geranyl cyclopropanecarboxylate claim 1 , neryl cyclopropanecarboxylate claim 1 , geranyl cyclobutanecarboxylate claim 1 , neryl cyclobutanecarboxylate claim 1 , citronellyl cyclobutanecarboxylate claim 1 , linalyl isobutyrate claim 1 , perillyl cyclopropanecarboxylate claim 1 , perillyl cyclobutanecarboxylate claim 1 , perillyl isobutyrate claim 1 , perillyl isovalerate claim 1 , cinnamyl cyclopropanecarboxylate claim 1 , cinnamyl ...

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Номер записи: 69
14-02-2019 дата публикации

IODONIUM ANALOGS AS INHIBITORS OF NADPH OXIDASES AND OTHER FLAVIN DEHYDROGENASES; FORMULATIONS THEREOF; AND USES THEREOF

Номер: US20190048001A1
Автор: DOROSHOW James Halpern, HOSSAIN Md Tafazzal, JR. Charles T., KANE, LU Jiamo, RISBOOD Prabhakar, ROY Krishnendu
Принадлежит:

Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity. 2. The method of claim 1 , wherein X is a halide claim 1 , an alkyl sulfonate claim 1 , an aryl sulfonate claim 1 , a phosphate claim 1 , or a nitrate.3. The method of claim 1 , wherein X is chloride claim 1 , bromide claim 1 , iodide claim 1 , CHSO— claim 1 , CHSO— claim 1 , CFSO— claim 1 , 4-CHCHSO— claim 1 , or CHSO—.4. The method of claim 1 , wherein m is 1 or 2 and n is 1 or 2.5. The method of claim 1 , wherein Z is O claim 1 , CH claim 1 , or NRwhere Ris C-Calkyl claim 1 , C-Chaloalkyl claim 1 , or C-Calkanoyl.6. The method of claim 1 , wherein Z is O claim 1 , CH claim 1 , or NRwhere Ris C-Calkanoyl.7. The method of claim 1 , wherein Z is O.8. The method of claim 1 , wherein Z is CH.9. The method of claim 1 , wherein the cancer is colon cancer claim 1 , kidney cancer (renal cell) claim 1 , melanoma claim 1 , leukemia claim 1 , prostate cancer claim 1 , breast cancer claim 1 , squamous lung cancer claim 1 , ovarian cancer claim 1 , pancreatic cancer claim 1 , Non-Hodgkin lymphoma claim 1 , or Glioblastoma Multiforme.10. The method of claim 9 , wherein the cancer is colon cancer.12. The method of claim 11 , wherein X is a halide claim 11 , an alkyl sulfonate claim 11 , an aryl sulfonate claim 11 , a phosphate claim 11 , or a nitrate.13. The method of claim 11 , wherein X is chloride claim 11 , bromide claim 11 , iodide claim 11 , CHSO— claim 11 , CHSO— claim 11 , CFSO— claim 11 , 4-CHCHSO— claim 11 , or CHSO—.14. The method of claim 11 , wherein m is 1 or 2 and n is 1 or 2.15. The method of claim 11 , wherein m is 1 claim 11 , 2 claim 11 , or 3 and n is 1 claim 11 , 2 claim 11 , or 3.16. The method of claim 11 , wherein m is 1 claim 11 , 2 claim 11 , 3 claim 11 , or 4 and n is 1 claim 11 , 2 claim 11 , 3 claim 11 , or 4.17. The method of claim 11 , wherein the cancer is colon cancer claim 11 , kidney cancer (renal cell) claim 11 , melanoma claim 11 , leukemia claim 11 ...

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Номер записи: 70
25-02-2016 дата публикации

METAL-CATALYZED COUPLING OF ARYL AND VINYL HALIDES WITH ALPHA, ALPHA-DIFLUOROCARBONYL COMPOUNDS

Номер: US20160052854A1
Автор: CHAKADAJ Wojciech, GE Shaozhong, Hartwig John F.
Принадлежит:

The coupling of aryl, heteroaryl, and vinyl halides with α,α-difluoroketones or silyl ethers or siylenol ethers of α,α-difluoroketones and α,α-difluoroamides and esters are described. Further derivatization of the coupling products (such as ketone cleavage and Baeyer-Villiger oxidation) is also described. 2. The composition according to claim 1 , wherein said complex is present in said composition in an amount of less than 10 mol % relative to said α claim 1 ,α-difluoromethyl carbonyl compound.3. The composition according to claim 2 , wherein said complex is present in said composition in an amount of about 2 mol % to about 5 mol % relative to said α claim 2 ,α-difluoromethyl carbonyl compound.5. The composition according to claim 4 , wherein said complex is present in said composition in an amount of less than 10 mol % relative to said silyl enol ether.6. The composition according to claim 5 , wherein said complex is present in said composition in an amount of about 2 mol % to about 5 mol % relative to said silyl enol ether.76. The composition according to any one of - claims 4 , wherein said composition does not contain BuSnF.87. The composition according to any one of - claims 4 , wherein said composition does not contain an organotin reagent.98. The composition according to any one of - claims 4 , wherein R claims 4 , R claims 4 , and Rare independently selected from unsubstituted C claims 4 , C claims 4 , C claims 4 , C claims 4 , Cand Calkyl.10. The composition according to claim 9 , wherein one or more of R claim 9 , R claim 9 , and Rare methyl.11. The composition according to any preceding claim claim 9 , further comprising a solvent.12. The composition according to claim 11 , wherein said solvent is a non-polar claim 11 , organic solvent.13. The composition according to claim 12 , wherein said solvent is toluene.14. The composition according to any preceding claim claim 12 , wherein said base is a member selected from CsCOand KPO.17. The composition ...

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Номер записи: 71
25-02-2016 дата публикации

Biological buffers with wide buffering ranges

Номер: US20160052868A1
Автор: Thomas P. Daly
Принадлежит: TPAT IP LLC

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 72
25-02-2016 дата публикации

PROCESS FOR PRODUCTION OF GLYCOPYRRONIUM TOSYLATE

Номер: US20160052879A1
Автор: Molteni Renato, SHAW Anthony Adrian, Vigano Enrico
Принадлежит:

Provided herein are methods for the production of glycopyrronium tosylate and glycopyrronium tosylate compositions. Also provided herein are compositions useful in the production of glycopyrronium tosylate. Additionally provided herein are glycopyrronium tosylate compositions. Glycopyrronium tosylate is useful for the treatment of, among other conditions, hyperhidrosis. 2. The method of claim 1 , wherein the glycopyrrolate base contacted with methyl tosylate is contacted with an organic solvent.3. The method of claim 2 , wherein the organic solvent is acetone or ethyl acetate.4. The method of claim 1 , wherein the glycopyrronium tosylate is purified by one or more crystallizations in an aqueous solvent.5. The method of claim 4 , wherein the purified glycopyrronium tosylate is in the form of glycopyrronium tosylate monohydrate.6. The method of claim 4 , wherein the purified glycopyrronium tosylate is a mixture of threo-glycopyrronium tosylate and erythro-glycopyrronium tosylate claim 4 , and the threo-glycopyrronium tosylate is at least 99% of the total glycopyrronium tosylate in the mixture and the erythro-glycopyrronium tosylate is less than 1% of the total glycopyrronium tosylate in the mixture.7. The method of claim 6 , wherein the threo-glycopyrronium tosylate is at least 99.5% of the total glycopyrronium tosylate in the mixture and the erythro-glycopyrronium tosylate is less than 0.5% of the total glycopyrronium tosylate in the mixture.8. The method of claim 6 , wherein the threo-glycopyrronium tosylate is at least 99.6% of the total glycopyrronium tosylate in the mixture and the erythro-glycopyrronium tosylate is less than 0.4% of the total glycopyrronium tosylate in the mixture.10. The method of claim 9 , wherein the glycopyrrolate base claim 9 , 5-nitroisophthalate salt and inorganic base are contacted with an organic solvent.11. The method of claim 10 , wherein the organic solvent is toluene.12. The method of claim 9 , wherein the inorganic base is aqueous ...

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Номер записи: 73
01-03-2018 дата публикации

METHOD FOR PREPARING 3-TRIFLUOROMETHYL CHALCONES

Номер: US20180057468A1
Автор: Annis Gary David
Принадлежит:

Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein Mis Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is ORor NRR, and R, Rand Rare as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above. 1. A compound which is 1-chloro-3-iodo-5-(trifluoromethyl)benzene. This invention pertains to a method for preparing 3-trifluoromethyl chalcones and trifluoroacetyl intermediates. The present invention also relates to novel trifluoroacetyl and halo compounds useful as starting materials and intermediates for the aforedescribed method.The present invention provides a method for preparing a compound of Formula 1whereinZ is optionally substituted phenyl; andQ is phenyl or 1-naphthalenyl, each optionally substituted;comprising distilling water from a mixture comprising a compound of Formula 2a compound of Formula 3a base comprising at least one compound selected from the ...

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Номер записи: 74
05-03-2015 дата публикации

MATERIALS COATED WITH CALIXARENES

Номер: US20150064455A1
Автор: HAPIOT Philippe, JABIN Ivan, Lagrost Corlnne, MATTIUZZI Alice, REINAUD Olivia
Принадлежит:

This invention relates to the direct grafting of a calixarene mostly onto the surface of a material, as well as to a grafting process, and certain calixarene intermediates useful for carrying the grafting process. 3. The material according to claim 1 , wherein the ultra-thin layer grafted on the surface of the material is a monolayer.4. The material according to wherein the material is a conductor claim 1 , semiconductor claim 1 , insulator claim 1 , a composite material claim 1 , a nanoparticle claim 1 , a polymer or a nanotube.6. The (thia)calix[n]arene-diazonium salt according to claim 5 , wherein X is a chloride claim 5 , bromide claim 5 , or BF.8. A (thia)calix[n]-aniline of formula II as defined in claim 7 , wherein X claim 7 , R claim 7 , R claim 7 , R claim 7 , R claim 7 , R claim 7 , R claim 7 , and wherein Y claim 7 , Y claim 7 , Y claim 7 , Y claim 7 , Yare each independently selected from the group consisting of OH claim 7 , hydrogen claim 7 , NOor halogen; provided that the compound of formula (II) is not a calix[4]arene wherein X=CH claim 7 , R=R=R=R=Pr claim 7 , Y=Y=Y=NH claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=Pr and R=CHCOOEt claim 7 , Y=Y=Y=NH claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=OH claim 7 , Y=Y=Y=NH claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=decyl claim 7 , Y=NH claim 7 , Y=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=decyl claim 7 , Y=NHY=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=decyl claim 7 , Y=Y=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=Pr claim 7 , Y=NH claim 7 , Y=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=Pr claim 7 , Y=NHY=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=Pr claim 7 , Y=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=OH claim 7 , R=R=Me claim 7 , Y=NH claim 7 , Y=Y=H claim 7 , or a calix[4]arene wherein X=CH claim 7 , R=R=R=R=Me claim 7 , Y=Y=Y=NH claim 7 , ...

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Номер записи: 75
05-03-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150065487A1
Автор: Anna Hazlewood, Ashvani Singh, Fred Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 76
28-02-2019 дата публикации

ALPHA-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20190062261A1
Автор: Deutsch Dale, Elmes Matthew, Hu Kongzhen, Kaczocha Martin, Ojima Iwao, TONG Simon, Yan Su
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure: Formula (I) 3. The compound of claim 1 , wherein when one of Ror Ris —C(═O)OH and R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each H claim 1 , then the other of Ror Ris other than —C(═O)ORwhere Ris tolyl claim 1 , 1-naphthalene or 2-naphthalene claim 1 , or —C(═O)O-alkyl-Rwhere the alkyl is a branched Calkyl and the Ris phenyl.4. The compound of claim 1 , wherein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene claim 1 , then one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris other than —H; or{'sub': 1', '2', '1', '2', '13', '13', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12, 'wherein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene, then two of R, R, R, R, R, R, R, R, Rand Ris other than —H; or'}{'sub': 1', '2', '1', '2', '13', '13', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12, 'herein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene, then four of R, R, R, R, R, R, R, R, Rand Ris other than —H.'}56.-. (canceled)7. The compound of claim 1 ,wherein{'sub': 1', '2', '13, 'claim-text': {'sub': '13', 'wherein Ris cycloalkyl, aryl or heteroaryl; and'}, 'one of Ror Ris —C(═O)OR,'}{'sub': 1', '2, 'the other of Ror Ris —C(═O)OH.'}8. The compound of claim 1 ,wherein{'sub': 1', '2', '14, 'claim-text': {'sub': 14', '3, 'wherein Ris CF, cycloalkyl, aryl or heteroaryl; and'}, 'one of Ror Ris —C(═O)O-alkyl-R,'}{'sub': 1', '2, 'the other of Ror Ris —C(═O)OH.'}910.-. (canceled)117. The compound of claim 1 , wherein the aryl or heteroaryl is a substituted aryl or heteroaryl claim 1 , wherein ...

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Номер записи: 77
17-03-2022 дата публикации

Process for preparation of 2-amino-5-hydroxy propiophenone

Номер: US20220081388A1
Автор: Jagadeeswara Rao Dadi, Raj Koti Katkuri, Sridhar Tummu, Uma Maheswer Rao Vasirredi, Venkata Ramana Kintali
Принадлежит: Laurus Labs Pvt Ltd

The present invention relates to a process for preparation of 2-Amino-5-hydroxy propiophenone, a key intermediate for the synthesis of camptothecin analogs including 7-Ethyl-10-hydroxycamptothecin (SN-38).

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Номер записи: 78
17-03-2022 дата публикации

Prostaglandin E Synthase Inhibitors and Methods for Utilizing the Same

Номер: US20220081432A1
Автор: Ding Kai, Zhan Chang-Guo, Zheng Fang, Zhou Ziyuan
Принадлежит:

Compounds and compositions are provided that can inhibit microsomal prostaglandin E synthase-1 (mPGES-1). The compounds and compositions can reduce inflammation in a subject, such as inflammation caused by an inflammation disorder or symptoms thereof. Pharmaceutical compositions comprising the compound are also provided. Furthermore, methods are provided for reducing inflammation and/or inhibiting mPGES-1. The methods can comprise administering an effective amount of the composition to a subject. 7. A pharmaceutical composition claim 1 , comprising a compound of and a pharmaceutically-acceptable carrier.8. The pharmaceutical composition of claim 7 , and further comprising:a second compound or composition having mPGES-1 inhibition activity, having anti-inflammatory activity, being useful for treatment of an inflammation disorder, being useful for treatment of symptoms associated inflammation and/or an inflammation disorder, or combinations thereof.9. A method of reducing inflammation in a subject claim 1 , comprising administering to the subject an effective amount of a compound of .10. The method of claim 9 , wherein the subject includes an inflammation disorder or symptoms thereof.11. The method of claim 10 , wherein the inflammation disorder is selected from the group consisting of inflammation claim 10 , arthritis claim 10 , fever claim 10 , pain claim 10 , cancer claim 10 , stroke claim 10 , bone disorders claim 10 , and combinations thereof.12. The method of claim 9 , wherein the compound inhibits microsomal prostaglandin E synthase-1 (mPGES-1). This application is a division of U.S. patent application Ser. No. 16/305,386, filed Nov. 28, 2018, which is a national stage entry of PCT/US2017/039785, filed Jun. 28, 2017, which claims the benefit of U.S. Provisional Application Ser. No. 62/355,739, filed Jun. 28, 2016, the entire disclosure of each of which is incorporated herein by this reference.The presently-disclosed subject matter relates to prostaglandin E ...

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Номер записи: 79
09-03-2017 дата публикации

Isoxazoline-substituted benzamide compound and pesticide

Номер: US20170065565A1
Автор: Manabu Yaosaka, Mitsuaki Komoda, Takamasa Kikuchi, Takashi Mizukoshi, Takeshi Mita
Принадлежит: Nissan Chemical Corp

A substituted alkenylbenzene compound of formula (4): wherein X 1 is selected from the group consisting of halogen atom, —SF 5 , C 1 -C 6 halo alkyl, hydroxy C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy C 1 -C 6 haloalkyl, C 3 -C 8 halocycloalkyl, C 1 -C 6 haloalkoxy, C 1 -C 3 haloalkoxy C 1 -C 3 haloalkoxy, C 1 -C 6 haloalkylthio, C 1 -C 6 haloalkylsulfinyl and C 1 -C 6 haloalkylsulfonyl; X 3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy and C 1 -C 6 alkylthio; X 4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C 1 -C 4 alkyl, C 1 -C 4 alkoxy and C 1 -C 4 haloalkoxy; R 3 is —C(R 3a )(R 3b )R 3c , where R 3a and R 3b independently of each other are a halogen atom, or R 3a and R 3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C 2 -C 5 haloalkylene chain, and R 3c is selected from the group consisting of a hydrogen atom, halogen atom, C 1 -C 5 alkyl, C 1 -C 5 haloalkyl, C 1 -C 4 haloalkoxy and C 1 -C 4 haloalkylthio, with a proviso that in case where X 1 is a fluorine atom, chlorine atom or trifluoromethyl, and both X 2 and X 3 are a hydrogen atom, in case where both X 1 and X 2 are fluorine atom and X 3 is a hydrogen atom, and in case where both X 1 and X 2 are trifluoromethyl and X 3 is a hydrogen atom, R 3c is a hydrogen atom, chlorine atom, bromine atom, iodine atom, C 1 -C 5 alkyl, C 1 -C 5 haloalkyl, C 1 -C 4 haloalkoxy or C 1 -C 4 haloalkylthio.

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Номер записи: 80
08-03-2018 дата публикации

NOVEL POLYAMIDEIMIDE HAVING LOW THERMAL EXPANSION COEFFICIENT

Номер: US20180066110A1
Автор: Kim Sang Youl, Kim Sun Dal
Принадлежит:

A polyamideimide includes an asymmetric dicarboxylic acid derivative wherein, from among a cyclic group A and a cyclic group B, two substituents groups R and R′ are bonded only to the cyclic group A on one side. A polymer produced by means of the present invention can have adequate solubility with respect to organic solvents, high thermal stability, a high glass transition temperature, high transparency and a low thermal expansion coefficient, and is able not only to satisfy requirements for core substrate materials of flexible displays but also to be used as a material for various soft electronic data devices. 2. Polyamideimide according to claim 1 , wherein R and R′ are identical to or different from each other claim 1 , and are hydrocarbyl group comprising fluorine.3. Polyamideimide according to claim 1 , wherein Lis anyone selected from the group consisting of a direct bond claim 1 , —O— claim 1 , and —S—.9. A process for producing the polyamideimide according to claim 7 , wherein diamine compound represented as Formula B-2 is any one selected from the group consisting of 2 claim 7 ,2′-bis(trifluoromethyl)benzidine claim 7 , 2 claim 7 ,6-bis(trifluoromethyl)benzidine claim 7 , p-phenylenediamine claim 7 , m-phenylenediamine claim 7 , p-aminobenzylamine claim 7 , m-aminobenzylamine claim 7 , 4 claim 7 ,4′-diaminodiphenylmethane claim 7 , 3 claim 7 ,4′-diaminodiphenylmethane claim 7 , 3 claim 7 ,3′-diaminodiphenylmethane claim 7 , 4 claim 7 ,4′-diaminodiphenylethane claim 7 , 4 claim 7 ,4′-diaminobenzanilide claim 7 , 4 claim 7 ,4′-diaminodiphenyl ether claim 7 , 3 claim 7 ,4′-diaminodiphenyl ether claim 7 , 3 claim 7 ,3′-diaminodiphenyl ether claim 7 , 2 claim 7 ,4′-diaminodiphenyl ether claim 7 , 2 claim 7 ,2′-diaminodiphenyl ether claim 7 , 2 claim 7 ,3′-diaminodiphenyl ether claim 7 , 1 claim 7 ,4-bis(4-aminophenoxy)benzene claim 7 , 1 claim 7 ,4-bis(3-aminophenoxy)benzene claim 7 , 1 claim 7 ,3-bis(4-aminophenoxy)benzene claim 7 , 1 claim 7 ,3-bis(3- ...

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Номер записи: 81
12-03-2015 дата публикации

METHOD FOR CONTINUOUS PRODUCTION OF NITROBENZENE

Номер: US20150073180A1
Автор: Knauf Thomas, Merkel Michael
Принадлежит: Bayer Intellectual Property GmbH

The invention relates to a method for producing nitrobenzene, in which crude nitrobenzene is first produced by nitrating benzene and said crude nitrobenzene is then washed in succession in at least one acid wash, in at least one alkaline wash and in at least one neutral wash, at least one additional wash with an aqueous solution of a potassium salt being interposed between the last alkaline wash and the first neutral wash. 1. Method for producing nitrobenzene bya) nitration of benzene with nitric acid or mixtures of nitric acid and sulfuric acid and subsequent phase separation into an aqueous phase and an organic phase containing nitrobenzene,b) washing of the organic nitrobenzene-containing phase obtained in step a) in at least one wash and subsequent phase separation into an aqueous phase and an organic phase containing nitrobenzene, sodium hydroxide, sodium carbonate and sodium hydrogen carbonate,', 'and subsequent phase separation into an aqueous phase and an organic phase containing nitrobenzene,, 'c) washing of the organic nitrobenzene-containing phase obtained in step b) in at least one alkaline wash with an aqueous solution of a base selected from the group consisting of'}d) washing of the organic nitrobenzene-containing phase obtained in step c) in at least one wash with an aqueous solution of a potassium salt and subsequent phase separation into an aqueous phase and an organic phase containing nitrobenzene,e) washing of the organic nitrobenzene-containing phase obtained in step d) in at least one neutral wash with water and subsequent phase separation into an aqueous phase and an organic phase containing nitrobenzene,f) processing of the organic nitrobenzene-containing phase obtained in step e), wherein purified nitrobenzene is obtained.2. Method according to claim 1 , wherein in step c) an aqueous solution of sodium hydroxide is used.3. Method according to or claim 1 , wherein in step d) a molar ratio of potassium to sodium ions of 1:1 to 20:1 is ...

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Номер записи: 82
17-03-2016 дата публикации

PROCESS FOR THE PREPARATION OF DIHYDROPYRROLE DERIVATIVES

Номер: US20160073631A1
Автор: Cassayre Jerome Yves, El Qacemi Myriem, GODINEAU EDOUARD, Mulholland Nicholas Phillip, Pitterna Thomas, Renold Peter, SMITS HELMARS
Принадлежит:

The present invention provides stereoselective processes for the preparation of compounds of formula (I) 5. A method of controlling insects claim 2 , acarines claim 2 , nematodes or molluscs which comprises applying to a pest claim 2 , to a locus of a pest claim 2 , or to a plant susceptible to attack by a pest an enantiomerically enriched mixture of a compound of formula I as defined in . This is a divisional application of U.S. patent application Ser. No. 13/703,630 filed on Dec. 11, 2012, which is a 371 of International Application No. PCT/EP2011/059823 filed Jun. 14, 2011 which claims priority to PCT/EP2010/058207 filed Jun. 11, 2010 and EP10196633.1 filed Dec. 22, 2010, the contents of which are incorporated herein by reference.The present invention relates to the synthesis of substituted dihydro-pyrrole derivatives and in particular to the stereoselective synthesis of substituted dihydro-pyrrole derivatives. The present invention relates more particularly to the stereoselective synthesis of substituted dihydro-pyrrole derivatives that have pesticidal activity.Certain dihydro-pyrrole derivatives with insecticidal properties are disclosed in, for example, JP 2007/091708, JP 2008/133273, JP 2010/254629, WO09097992, WO09072621 and WO2010/020522. Such dihydro-pyrrole derivatives include at least one chiral centre at one of the ring members of the dihydro-pyrrole moiety. The present invention provides a process for selectively synthesizing enantiomers of such compounds as well as intermediates that can be used in the synthesis of such compounds.Accordingly, in a first aspect the invention provides a process for the preparation of the compound of formula Iwherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; Ris ...

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Номер записи: 83
16-03-2017 дата публикации

Novel gamma-aminobutyric acid (gaba) analogues for the treatment of pain and other disorders

Номер: US20170071909A1
Автор: Franz Kricek, Premji Meghani
Принадлежит: Novassay SA

A compound of Formula 1 wherein R 1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R 2 represents or a tautomer thereof; and R 3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.

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Номер записи: 84
17-03-2016 дата публикации

SYNTHETIC ANALOGUES OF XANTHOHUMOL

Номер: US20160075652A1
Автор: ALBINI Adriana, Bartolini Desiree, Cantelmo Anna Rita, Gallo Cristina, NENCETTI Susanna, Noonan Douglas M., NUTI Elisa, ORLANDINI Elisabetta, ROSSELLO Armando
Принадлежит:

The present invention relates to novel synthetic analogues of xanthohumol and the use thereof. 2. Compounds according to claim 1 , wherein said aromatic or non-aromatic heterocyclic ring is benzofused and/or further substituted with halogen claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , alkoxy claim 1 , amino claim 1 , amido claim 1 , acylamido claim 1 , sulphonamido claim 1 , acyl claim 1 , sulphonyl claim 1 , aryl or heteroaryl.6. Compounds according to claim 1 , wherein A is a 2- claim 1 , 3- or 4-pyridyl ring.7. Compounds according to claim 1 , wherein Rand Rare claim 1 , independently from each other claim 1 , hydrogen or methoxymethyl and the substituents on ring A or R claim 1 , R claim 1 , R claim 1 , Rand Rare independently H claim 1 , —OCHfluorine claim 1 , chlorine claim 1 , —NO claim 1 , —CONHCH claim 1 , —SONH claim 1 , —NHSOCH claim 1 , or the —SONHCOCH(Et)NHCOOCHPh group claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , Rand Ris H.8. Compound according to claim 1 , selected from:(E)-3-(3,4-dichloro-phenyl)-1-(6-methoxy-2,4-bis(methoxymethyloxy)-3-(3-methyl-but-2-enyl)phenyl)prop-2-en-1-one;(E)-3-(3,4-dichloro-phenyl)-1-[2-hydroxy-6-methoxy-4-(methoxymethyloxy)-3-(3-methyl-but-2-enyl)-phenyl]-prop-2-en-1-one;(E)-3-(3,4-dichloro-phenyl)-1-[2,4-dihydroxy-6-methoxy-3-(3-methyl-but-2-enyl)-phenyl]-prop-2-en-1-one;(E)-3-(3,4-diclorophenyl)-1-(5-hydroxy-7-methoxy-2,2-dimethylchroman-6-yl)prop-2-en-1-one;(E)-3-(4-fluorophenyl)-1-[6-methoxy-2,4-di-methoxymethyloxy-3-(3-methyl-but-2-enyl)-phenyl]-prop-2-en-1-one;(E)-1-[2,4-dihydroxy-6-methoxy-3-(3-methyl-but-2-enyl)prenyl]-3-(4-fluorophenyl)-prop-2-en-1-one;(E)-3-(4-fluorophenyl)-1-[2-hydroxy-6-methoxy-4-(methoxymethyloxy)-3-(3-methyl-but-2-enyl]-phenyl)prop-2-en-1-one;(E)-1-[6-methoxy-2,4-dimethoxymethyloxy)-3-(3-methylbut-2-enyl)phenyl]-3-(4-nitrophenyl)prop-2-en-1-one;(E)-1-[2-hydroxy-6-methoxy-4-(methoxymethyloxy)-3-(3-methylbut-2-enyl)phenyl]-3-(4-nitrophenyl)prop-2-en-1- ...

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Номер записи: 85
05-03-2020 дата публикации

HALOGEN-SUBSTITUTED PHENOXYPHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

Номер: US20200068886A1
Автор: BRUNET Stephane, ES-SAYED Mazen, Hillebrand Stefan, Wachendorff-Neumann Ulrike
Принадлежит:

The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat. 2. The process of claim 1 , wherein{'sup': '1', 'Ris selected from the group consisting of fluoro, chloro, bromo, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, and trifluoromethyl;'}{'sup': '2', 'Ris methyl; and'}{'sup': '3', 'Ris selected from the group consisting of bromo, chloro and fluoro.'}3. The process of claim 1 , wherein{'sup': '1', 'Ris selected from the group consisting of chloro, bromo, difluoromethyl, and trifluoromethyl;'}{'sup': '2', 'Ris methyl; and'}{'sup': '3', 'Ris fluoro or chloro.'}4. The process of claim 1 , wherein{'sup': '1', 'Ris chloro,'}{'sup': '2', 'Ris methyl; and'}{'sup': '3', 'Ris fluoro.'}5. The process of claim 1 , wherein the phenoxyphenylamidine is selected from the group consisting of N′-[2-chloro-4-(2-fluorophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , N′-[2-(difluoromethyl)-4-(2-fluorophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , N′-[2-bromo-4-(2-fluorophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , N′-[2-bromo-4-(2-chlorophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , N′-[2-chloro-4-(2-chlorophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , N′-[2-chloro-4-(2-iodophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide claim 1 , and N′-[2-bromo-4-(2-bromophenoxy)-5-methylphenyl]-N-ethyl-N-methylimidoformamide.7. The nitrophenyl ether of claim 6 , wherein{'sup': '1', 'Ris ...

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Номер записи: 86
07-03-2019 дата публикации

Indole derivatives and their use as protein kinase inhibitors

Номер: US20190071399A1
Автор: Christopher Scott STEVENSON, Iain Walters, Louise BIRCH, Stephen Paul Collingwood
Принадлежит: Respivert Ltd

The present invention relates inter alia to a compound of formula (I) wherein R 1 , R 2 and R 3 , are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

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Номер записи: 87
19-03-2015 дата публикации

Compounds, Compositions, and Methods For Modulating Ferroptosis and Treating Excitotoxic Disorders

Номер: US20150079035A1
Автор: Brent R. Stockwell, Rachid Skouta, Scott J. Dixon
Принадлежит: Columbia University of New York

The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

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Номер записи: 88
05-03-2020 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20200071582A1
Автор: Daly Thomas
Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A═D═—CH3 and m=1.3. The biological buffer and its salts of wherein A═D═—CH2OH and m=1.4. The biological buffer and its salts of wherein A═D—CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A═—CH2CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A═—CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.10. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.11. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′=—CH3 and G═—CH2CH3. This is a continuation of U.S. application Ser. No. 15/649,869 filed Jul. 14, 2017 and other previous parent applications claimed in the Application Data Sheet. U.S. application Ser. No. 15/649,869 is hereby incorporated by reference in its entirety.The present invention relates generally to the field of amines and more particularly to a classes of amines used as buffers in biological systems.Amines are very useful compounds in the buffering of biological systems. Each class of amine has various limitations which require choosing an amine ...

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Номер записи: 89
05-06-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140155431A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 90
05-06-2014 дата публикации

Method for preparing 3-trifluoromethyl chalcones

Номер: US20140155617A1
Автор: Gary David Annis
Принадлежит: EI Du Pont de Nemours and Co

Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M 1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR 11 or NR 12 R 13 , and R 11 , R 12 and R 13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

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Номер записи: 91
18-03-2021 дата публикации

METHOD FOR PREPARATION OF 5-FLUORO-2-METHYL-3-NITROBENZOIC ACID AND ITS METHYL ESTER

Номер: US20210078933A1
Автор: AELLIG Christof, Bersier Michael, FILLIGER Sarah, HANSELMANN Paul, KULESZA Anna
Принадлежит:

The invention discloses a method for preparation of 5-fluoro-2-methyl-3-nitrobenzoic acid and its methyl ester by conversion of 5-fluoro-2-methylbenzoic acid with fuming nitric acid and oleum and subsequent conversion with methanol. 2. Method according to claim 1 , wherein{'sub': 2', '4, 'the concentrated sulfuric acid has a content of from 94 to 100 wt % of HSO;'}the wt % based on the weight of the concentrated sulfuric acid.3. Method according to claim 1 , wherein{'sub': '3', 'the oleum contains 50 to 70 wt % of SO.'}4. Method according to claim 1 , wherein{'sub': '3', 'the fuming nitric acid has a content of from 95 to 100 wt % of HNO.'}5. Method according to claim 1 , wherein MIX contains{'sub': 2', '4, 'concentrated sulphuric acid in an amount of 4 to 12 times of molar equivalents of HSOrelative to compound of formula (1),'}{'sub': 2', '4, 'oleum in an amount of 1 to 4 times of molar equivalents of HSOrelative to compound of formula (1),'}{'sub': '3', 'fuming nitric acid in an amount of 1 to 2 times of molar equivalents of HNOrelative to compound of formula (1).'}6. Method according to claim 1 , wherein the amounts of concentrated sulfuric acid claim 1 , oleum and fuming nitric acid in MIX add up to 95 to 100 wt % claim 1 , more preferably to 98 to 100 wt % claim 1 , the wt % being based on the total weight of MIX; even more preferably MIX consists of concentrated sulfuric acid claim 1 , oleum and fuming nitric acid.7. Method according to claim 1 , wherein the reaction temperature TEMPI of REAC1 is from −10 to 30° C.8. Method according to claim 1 , wherein the reaction time TIME1 of REAC1 is from 1 sec to 2 h.9. Method according to claim 1 , wherein REAC1 is done in a continuous way.11. Method according to claim 10 , wherein{'sub': 2', '4, 'REAC2 is done in the presence of an acid ACID2, ACID2 is HSO.'}12. Method according to claim 10 , whereinboth REAC1 and REAC2 are done in a continuous way and are done consecutively without isolation of compound of formula ( ...

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Номер записи: 92
18-03-2021 дата публикации

Nitrile oxide compound

Номер: US20210078944A1
Автор: Hiromitsu SOGAWA, Tadashi KANBARA, Toshikazu Takata, Tsuyoshi Noguchi
Принадлежит: Daikin Industries Ltd, Tokyo Institute of Technology NUC

The present invention provides a compound represented by formula (I) wherein symbols in the formula are as defined in the specification.

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Номер записи: 93
31-03-2022 дата публикации

ARYL COMPOUNDS AND POLYMERS AND METHODS OF MAKING AND USING THE SAME

Номер: US20220098137A1
Автор: Chalifoux Wesley A., Sproul Kyle C., Yang Wenlong
Принадлежит: Nevada Research & Innovation Corporation

Disclosed herein are embodiments of aryl compounds and polymers thereof that are made using methods that do not require harsh conditions or expensive reagents. The methods disclosed herein utilize precursor compounds that can be polymerized to form polycyclic aromatic hydrocarbons and polymers, such as carbon-based polymers like nanostructures (e.g., graphene or graphene-like nanoribbons). 2. The compound of claim 1 , wherein the heteroaliphatic moiety comprises at least one carbon atom and one or two sulfur atoms.3. The compound of claim 1 , wherein each Rindependently is a thiol.4. The compound of claim 1 , wherein each Rindependently is a thioether.6. The compound of claim 5 , wherein the electron-donating group is an alkoxy group.9. The compound of claim 8 , wherein the electron-donating group is an alkoxy group. This application is a continuation of U.S. application Ser. No. 16/696,790, filed Nov. 26, 2019, which is a continuation of U.S. application Ser. No. 15/558,978, filed on Sep. 15, 2017, issued as U.S. Pat. No. 10,550,056 on Feb. 4, 2020, which is the U.S. National Stage of International Application No. PCT/US2016/023179, filed Mar. 18, 2016, which was published in English under PCT Article 21(2), which claims the benefit of, and priority to, the earlier filing date of U.S. Provisional Patent Application No. 62/135,692, filed on Mar. 19, 2015, and U.S. Provisional Patent Application No. 62/182,351, filed on Jun. 19, 2015; each of these prior applications is herein incorporated by reference in its entirety.The present disclosure concerns aryl compounds and polymeric aryl compounds and methods of making and using the same.Peropyrene compounds, as large polycyclic aromatic hydrocarbons (LPAH), comprise structural features that convey unique photophysical properties to such compounds. However, due to difficult preparation and derivatization of such compounds, their utility has yet to be utilized in various applications. Perylenediimide derivatives, which ...

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Номер записи: 94
12-06-2014 дата публикации

MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT

Номер: US20140162989A1
Автор: Moulton Brian, Rodriguez-Hornedo Nair, Zaworotko Michael J.
Принадлежит:

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions. 136-. (canceled)37. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a co-crystal comprising supramolecular synthons , each supramolecular synthon formed from stoichiometric amounts of at least one active pharmaceutical ingredient (API) and at least one co-former ,wherein the API has a first chemical functionality that permits formation of API homosynthons through non-covalent hydrogen bonding when the API is in its pure form,wherein the co-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,wherein said co-former is not an API, andwherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former.38. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a supramolecular heterosynthon dimer formed by non-covalent hydrogen bonding of the API to the co-former.39. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a plurality of the API and a plurality of the co-former claim 37 , wherein the supramolecular synthon is a chain of supramolecular heterosynthons claim 37 , each supramolecular heterosynthon formed by non-covalent hydrogen bonding of one API to one co-former claim 37 , and wherein the supramolecular heterosynthons are bonded to one another by non-covalent hydrogen bonding.40. The pharmaceutical composition of claim 37 , ...

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Номер записи: 95
12-06-2014 дата публикации

Small Molecule Xanthine Oxidase Inhibitors and Methods of Use

Номер: US20140163045A1
Автор: Chen Changyi, Lu Jian-Ming, Yao Qizhi
Принадлежит: Baylor College of Medicine

Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia. 3. The method of claim 1 , further comprising administering a second therapeutic agent to the subject.4. The method of claim 3 , wherein the second therapeutic agent is an anti-gout agent.5. The method of claim 4 , wherein the anti-gout agent is selected from the group consisting of allopurinol claim 4 , benzbromarone claim 4 , colchicine claim 4 , probenecid claim 4 , and sulfinpyrazone.6. The method of claim 3 , wherein the second therapeutic agent is an anti-inflammatory agent.7. The method of claim 3 , wherein the second therapeutic agent is an antioxidant.8. The method of claim 1 , wherein the compound is administered orally.11. The method of claim 9 , wherein the method further comprises selecting a subject having gout or hyperuricemia.14. The method of claim 12 , wherein the contacting is performed in vivo.15. The method of claim 12 , wherein the contacting is performed in vitro. This application claims priority to U.S. Provisional Application No. 61/734,409, filed Dec. 7, 2012, which is incorporated herein by reference in its entirety.Gout is caused by hyperuricemia, namely, abnormally high levels of uric acid in the blood. Gout is usually present as acute inflammatory arthritis, as well as tophi, kidney stones, or urate nephropathy. Gout affects 1-2% of adults in developed countries and represents the most common case of inflammatory arthritis in men. In the United States, gouty arthritis accounts for millions of outpatient visits annually. Furthermore, gout and hyperuricemia are associated with chronic diseases such as hypertension, diabetes mellitus, metabolic syndrome, and renal and cardiovascular disease.Xanthine oxidase (XO) is a form of a molybdoflavin protein, xanthine oxidoreductase (XOR). It plays an important role in the catabolism of purines in humans, as it catalyzes the oxidation of hypoxanthine to xanthine and then ...

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Номер записи: 96
02-04-2015 дата публикации

DINITRO COMPOUND, DIAMINE COMPOUND, AND AROMATIC POLYIMIDE

Номер: US20150094430A1
Автор: Chen Wen-Hsiang
Принадлежит: TAIWAN TEXTILE RESEARCH INSTITUTE

A dinitro compound I, a diamine compound II and polyimides are provided. The diamine compound II is a reduction product of the dinitro compound I. The polyimides using the diamine compound II as one of the monomers can increase the solubility of the polyimides in various organic solvents and make the color of the polyimides to be transparent and colorless. 9. The polyimide of claim 5 , wherein a molar ratio of the second aromatic diamine monomer to the first aromatic diamine monomer is 0-99.11. The polyimide of claim 5 , wherein the second aromatic diamine monomer is 4 claim 5 ,4′-oxydianiline. This application claims the priority benefit of Taiwanese application serial no. 102135362, filed Sep. 30, 2013, the full disclosure of which is incorporated herein by reference.1. Technical FieldThe disclosure relates to a polyimide and a preparation method thereof. More particularly, the disclosure relates to a polyimide with pale color and a preparation method thereof.2. Description of Related ArtPolyimide is a common engineering plastic. Since polyimide has properties of wide applicable temperature range, excellent chemical resistance, and high mechanical strength, the polyimide has a wide application range. Although aromatic polyimide has good thermal stability, the solubility of the aromatic polyimide, which is polymerized by aromatic diamine and aromatic tetracarboxylic dianhydride, in most common organic solvents is very poor, and some aromatic polyimide even only may be dissolved in concentrated sulfuric acid. Therefore, the aromatic polyimide cannot be easily processed. Moreover, since intermolecular or intramolecular charge transfer is easily occurred in aromatic polyimide to form charge transfer complex (CTC), most aromatic polyimides have a deep color. Therefore, the application on optoelectronic products, such as flexible liquid crystal displays, color e-papers, organic light emitting diodes, organic photovoltaics or aerospace, of the aromatic polyimide is ...

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Номер записи: 97
02-04-2015 дата публикации

Esters with antimicrobial, bioresistant and fungal resistant properties

Номер: US20150094480A1
Автор: Daly Thomas
Принадлежит:

A bromine/nitro moiety linked into the backbone of an ester or other compound over a wide range of occurrence rates provides antimicrobial, bio-resistant and fungal resistant properties for metal working fluids (MWF)s and other coatings. The moiety can be have the bromo and nitro groups linked to the same or different carbon atoms. The present invention also relates to urethanes, urea, amides, imides, carbonates, ethers, siloxanes, and many other types of linkages essential to MWF bases. 2. The molecule of where R═R′=—(CH)CHA=—(CH2)CH.3. A metal working fluid base comprising a molecule according to .4. A surfactant comprising a molecule according to .5. A foaming or anti-foaming agent comprising a molecule according to . This is a continuation of application Ser. No. 14/293,054 filed Jun. 2, 2014, now U.S. Pat. No. 8,901,332 issued Dec. 2, 2014 which was a divisional of application Ser. No. 13/741,518 filed Jan. 15, 2013, now U.S. Pat. No. 8,742,151 issued Jun. 3, 2014. Application Ser. No. 13/741,518 was a continuation of application Ser. No. 13/351,512 filed Jan. 17, 2012, now abandoned, which was a continuation of application Ser. No. 12/965,252 filed Dec. 10, 2010, now abandoned, which was a divisional of application Ser. No. 12/287,726 filed Oct 10, 2008, now abandoned, which was a continuation-in-part of application Ser. No. 11/800,569 filed May 7, 2007, now U.S. Pat. No. 7,439,376 issued Oct. 21, 2008, which was a continuation in part of application Ser. No. 10/603,356 filed Jun. 25, 2003, now abandoned, which claimed priority from U.S. Provisional patent application No. 60/392,007 filed Jun. 26, 2002. Application Ser. Nos. 14/293,054, 13/741,518, 13/351,512, 12/965,252, 12/287,726, 11/800,569, 10/603,356 and 60/392,007 are hereby incorporated by reference in their entireties. This application also incorporates by reference my patent application Ser. No. 10/350,928 filed Jan. 23, 2003 entitled Polymers with Antimicrobial, Bioresistant and Fungal Resistant ...

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Номер записи: 98
19-06-2014 дата публикации

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

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

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

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Номер записи: 99
19-03-2020 дата публикации

THERAPEUTIC DNP DERIVATIVES AND METHODS USING SAME

Номер: US20200087242A1
Автор: SHULMAN Gerald I., SPIEGEL DAVID A.
Принадлежит:

The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent. 119-. (canceled)20. A method of ameliorating a disease or disorder in a subject in need thereof , wherein the disease or disorder is at least one selected from the group consisting of hypertriglyceridemia , fatty liver , and insulin resistance , the method comprising:{'sub': '6', 'administering to the subject a therapeutically effective amount of a nitrophenyl derivative selected from the group consisting of 2,4-dinitrophenyl vinyl ether, 2,4-dinitrophenyl methyl ether-d, and solvates thereof.'}21. The method of claim 20 , wherein the method further comprises administering to the subject at least one additional therapeutic agent.22. The method of claim 21 , wherein the nitrophenyl derivative and the at least one additional therapeutic agent are co-administered to the subject.23. The method of claim 22 , wherein the nitrophenyl derivative and the at least one additional therapeutic agent are co-formulated.24. The method of claim 20 , wherein the subject is a mammal.25. The method of claim 24 , wherein the mammal is human.26. The method of claim 20 , wherein the administering is by an administration route selected from the group consisting of oral claim 20 , transdermal claim 20 , transmucosal claim 20 , intravesical claim 20 , intrapulmonary claim 20 , intraduodenal claim 20 , intragastrical claim 20 , intrathecal claim 20 , subcutaneous claim 20 , intramuscular claim 20 , intradermal claim 20 , intra-arterial claim 20 , intravenous claim 20 , intrabronchial claim 20 , inhalation claim 20 , and topical.27. The method of claim 26 , wherein the administering is oral and wherein the nitrophenyl derivative is formulated as a tablets claim 26 , dragee claim 26 , liquid claim 26 , drop claim 26 , capsule claim 26 , caplet ...

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Номер записи: 100