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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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Применить Всего найдено 9312. Отображено 200.
27-04-2011 дата публикации

ПРОИЗВОДНЫЕ ФТОРАЛКОКСИКОМБРЕТАСТАТИНА, СПОСОБЫ ИХ ПРОИЗВОДСТВА И ИСПОЛЬЗОВАНИЯ

Номер: RU2417216C2

Изобретение относится к новым производным комбретастатина формулы (I), обладающим свойствами ингибитора ангиогенеза, которые могут быть использованы в качестве противораковых и/или антиангиогенных средств. В формуле I ! ! Rf - алкильная группа, содержащая от 1 до 2 атомов углерода, в которой от 1 до 5 атомов водорода замещены 1-5 атомами фтора, a R - аминогруппа, или группа, представляющая собой аминогруппу, замещенную остатком аминокислоты общей формулы NH(COCHR′NH)-H, где R′ - водород, боковая цепь природной аминокислоты, представляющая собой С1-С4алкил, возможно замещенный гидроксигруппой, или гидроксильная группа, или динатрий, или аммоний фосфатная группа. Изобретение также относится к вариантам способа получения соединений формулы I, предусматривающим следующие стадии: фторалкилирование 4-гидрокси-3-метоксибензальдегида или 4- гидроксибензальдегида в присутствии катализатора межфазного переноса, с получением соответственно 4-фторалкокси-3-метоксибензальдегида (V) или 4-фторалкоксибензальдегида ...

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25-12-2020 дата публикации

ПОЛУЧЕНИЕ МОНОМЕРОВ ИЗ ЛИГНИНА В ПРОЦЕССЕ ДЕПОЛИМЕРИЗАЦИИ СОДЕРЖАЩЕЙ ЛИГНОЦЕЛЛЮЛОЗУ КОМПОЗИЦИИ

Номер: RU2739567C2

Настоящее изобретение относится к способу получения мономеров, способу получения фрагментов ксилана, применению формальдегида и применению мономеров. Способ получения мономеров из лигнина путем деполимеризации включает стадии: a) обеспечения содержащей лигноцеллюлозу композиции, b) нагревания композиции со стадии а) в кислых условиях совместно с альдегидом, кетоном, бороновой кислотой или соединением, выбранным из 2-метоксипропена, диметилкарбоната и 2,2-диметоксипропана, c) отделения фрагментов лигнина от смеси, полученной на стадии b), d) превращения фрагментов лигнина, полученных на стадии с), в мономеры. Способ получения фрагментов ксилана путем деполимеризации включает стадии: a) обеспечения содержащей лигноцеллюлозу композиции, b) нагревания композиции со стадии а) в кислых условиях совместно с альдегидом, кетоном, бороновой кислотой или соединением, выбранным из 2-метоксипропена, диметилкарбоната и 2,2-диметоксипропана, и с') отделения фрагментов ксилана от смеси, полученной на стадии ...

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10-08-2006 дата публикации

НЕНУКЛЕОЗИДНЫЕ ИНГИБИТОРЫ ОБРАТНОЙ ТРАНСКРИПТАЗЫ,ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИХ, ИХ ПРИМЕНЕНИЕ ПРИ ИЗГОТОВЛЕНИИ ЛЕКАРСТВЕННЫХ СРЕДСТВ ДЛЯ ЛЕЧЕНИЯ ВИЧ-1, ПРОМЕЖУТОЧНЫЕ ДЛЯ ИХ ПОЛУЧЕНИЯ

Номер: RU2281284C2
Принадлежит: МЕДИВИР АБ (SE)

Изобретение относится к новым ненуклеозидным ингибиторам обратной транскриптазы формулы I: где R1 представляет О, S; R2 представляет необязательно замещенный, азотсодержащий гетероцикл, в котором азот расположен в положении 2 относительно связи с (тио)мочевиной; R3 представляет Н, C1-С3алкил, R4-R7 независимо выбраны из Н, C1-С6алкила, С2-С6 алкенила, С2-С6алкинила, галогенС1-С6алкила, C1-С6алканоила, галогенС1-С6алканоила, C1-С6 алкокси, галогенС1-С6алкокси, гидрокси-С1-С6алкила, циано, галогена, гидрокси; Х представляет -(CHR8)n-D(CHR8)m -; D представляет -О- или -S-; R8 представляет Н, n и m представляют независимо 0, 1 или 2; и его фармацевтически приемлемым солям. Изобретение относится также к фармацевтической композиции на основе этих соединений, обладающей ингибирующей активностью в отношении обратной транскриптазы ВИЧ-1, а также к применению этих соединений при изготовлении лекарственных средств для лечения ВИЧ-1 и промежуточным соединениям. 6 н. и 39 з.п. ф-лы, 1 табл.

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20-08-2007 дата публикации

СПОСОБ СТАБИЛИЗАЦИИ ВОССТАНОВЛЕННОГО КОФЕРМЕНТА Q10 И КОМПОЗИЦИЯ НА ЕГО ОСНОВЕ

Номер: RU2304573C2
Принадлежит: КАНЕКА КОРПОРЕЙШН (JP)

Изобретение относится к способу стабилизации восстановленного кофермента Q10, который может применяться в качестве ингредиента в товарах пищевого назначения, пищевых добавках, компонентах питания, лекарствах для животных, напитках, косметических средствах и т.д., а также к композициям (вариантам) для поддержания восстановленного кофермента Q10 в стабильном состоянии. Способ включает получение композиции путем смешивания восстановленного кофермента Q10 с жиром или маслом (исключая оливковое масло) и/или полиолом в качестве основного компонента, в котором стабилизация восстановленного кофермента Q10 существенно не ингибируется, с защитой, таким образом, восстановленного кофермента Q10 от окисления, причем восстановленный кофермент Q10 добавляют извне. 3 н. и 55 з.п. ф-лы, 9 табл.

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27-05-2020 дата публикации

Номер: RU2018134925A3
Автор:
Принадлежит:

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10-08-1999 дата публикации

БИЦИКЛИЧЕСКОЕ АРОМАТИЧЕСКОЕ СОЕДИНЕНИЕ, ФАРМАЦЕВТИЧЕСКАЯ И КОСМЕТИЧЕСКАЯ КОМПОЗИЦИИ

Номер: RU2134256C1

Изобретение относится к новым биоароматическим соединениям общей формулы I, где значения R1, R2, R3, X и Ar указаны в п.1 формулы. Они обладают активностью в областях дифференциации и пролиферации клеток. Описывается также фармацевтическая композиция, предназначенная для лечения дерматологических, ревматических, респираторных, сердечно-сосудистых и офтальмологических заболеваний, а также и косметическая композиция для гигиены тела и для ухода за волосами. 3 с. и 13 з.п.ф-лы, 4 ил.

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27-08-2018 дата публикации

Номер: RU2016135789A3
Автор:
Принадлежит:

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20-11-1998 дата публикации

ПОЛИЕНОВЫЕ СОЕДИНЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ И КОСМЕТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Номер: RU2121995C1
Принадлежит: С.И.Р.Д.Галдерма (FR)

Изобретение относится к новым полиеновым соединениям формулы I, где R1 - COR9; R2, R4, R6 - водород; R3, R5, R10, R11 - водород или низший алкил; R7 - циклоалифатический радикал или низший алкил; R8 - радикал -O-CH2-OCH2-CH2 -O-CH3 или OR11; R4 и R6 взятые вместе могут образовывать с соседним бензольным циклом нафталиновый цикл; R9 - O-R10, а также их солям и их оптическим и геометрическим изомерам. Соединения I обладают значительной активностью в области дифференциации и пролиферации клеток и могут найти применение при местном и системном лечении дерматологических расстройств, связанных с нарушением кератинизации, дерматологических или других заболеваний с воспалительной и/или иммуноаллергической компонентой. 3 c. и 8 з.п. ф-лы, 2 ил., 1 табл.

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27-03-2008 дата публикации

АЛЬФА-(ТРИФТОРМЕТИЛЗАМЕЩЕННЫЕ АРИЛОКСИ, АРИЛАМИНО, АРИЛТИО ИЛИ АРИЛМЕТИЛ)ТРИФТОРМЕТИЛЗАМЕЩЕННЫЕ ФЕНИЛУКСУСНЫЕ КИСЛОТЫ И ПРОИЗВОДНЫЕ КАК ПРОТИВОДИАБЕТИЧЕСКИЕ СРЕДСТВА

Номер: RU2006133284A
Принадлежит:

... 1. Соединение формулыгде Х представляет собой элемент, выбранный из группы, состоящей из О, S, SO, SO, CHR и NR, где R представляет собой Н, (C-C)-алкил, COR, COORи CONRR, где Rи Rвыбирают, каждый независимо, из группы, состоящей из Н и (С-С)-алкила;Y представляет собой элемент, выбранный из группы, состоящей из CHOR, COR, тетразола, СНО, CONRR, CH(=NR) и CH(=NOR), где Rпредставляет собой элемент, выбранный из группы, состоящей из Н, (С-С)-алкила, (С-С)-алкенила, (С-C)-алкинила, (С-С)-циклоалкила, (С-С)-циклоалкилалкила, арила, арил-(С-С)-алкила и (С-С)-алкилен-Z, где Z выбирают из группы, состоящей из COR, COOR, NRR, NRCONRR, NRCOR, NRCOORи CONRR, где R, Rи Rвыбирают, каждый независимо, из группы, состоящей из Н, (C-C)-алкила и фенила, или, необязательно, два элемента из числа R, Rи R, когда они присоединены к одному и тому же атому азота, объединяются с образованием пяти- или шестичленного цикла; и где Rвыбирают из группы, состоящей из Н, (С-С)-алкила, арила и ОН, и Rи R, необязательно ...

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27-06-2014 дата публикации

ПРОИЗВОДНЫЕ ТРИС(2-ГИДРОКСИФЕНИЛ)МЕТАНА, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ

Номер: RU2012155044A
Принадлежит:

... 1. Производные трис(2-гидроксифенил)метана, отличающиеся тем, что они обладают общей формулой (I):,в которой остатки R, Rи R означают:R независимо друг от друга означают от 0 до 4 углеводородных остатков с 1-30 атомами углерода в каждом фенильном кольце,Rозначает остаток, выбранный из группы, включающей водород, гидроксил, фтор, хлор, бром, йод и углеводородные группы с 1-30 атомами углерода,Rнезависимо друг от друга означают остатки общей формулы (III) -(R-O-)-R-X, в которой n означает число от 1 до 50,причем остатки Rнезависимо друг от друга выбраны из группы, включающей остатки R, Rи R:,причем R, X, Rи Rнезависимо друг от друга означают:Rозначает простую связь или алкиленовую группу с 1-10 атомами углерода, которая при необходимости может быть замещена функциональными группами,X означает водород или гидрофильную группу,Rозначает водород или углеводородный остаток с 1-6 атомами углерода,Rозначает группу формулы -(R-O-)-R-X, в которой m означает число от 0 до 50,и причем общее число z ...

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27-12-1996 дата публикации

ПОЛИЕНОВЫЕ СОЕДИНЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ И КОСМЕТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Номер: RU95106674A
Принадлежит:

Изобретение относится к новым полиеновым соединениям, фармацевтическим и косметическим композициям на их основе.

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13-03-2018 дата публикации

КАТАЛИЗАТОР ДЛЯ ПИРОЛИЗА СЫРЬЯ

Номер: RU2016135789A
Принадлежит:

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10-01-2015 дата публикации

АЛКИНОВЫЕ И АЛКЕНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА СФИНГОЗИН 1-ФОСФАТА-1

Номер: RU2013129484A
Принадлежит:

... 1. Соединение, имеющее Формулу I, его энантиомеры, диастереоизомеры, гидраты, сольваты, кристаллические формы и индивидуальные изомеры, таутомеры или их фармацевтически приемлемые соли,где:«» представляет двойную связь «-CR=CR-» или тройную связь «-C≡C-»;A является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;B является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, Cарилом, гетероциклом, Cциклоалкилом, Cциклоалкенилом, NRRили гидроксилом;Rодинаково или независимо ...

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10-06-2008 дата публикации

СОЕДИНЕНИЯ С АКТИВНОСТЬЮ ЭСТРОГЕННЫХ РЕЦЕПТОРОВ

Номер: RU2006142683A
Принадлежит:

... 1. Соединение формулы (I): (I) или ее фармацевтически приемлемая соль или пролекарство, где n представляет собой целое число, выбранное из группы, состоящей из 3,4, 5 и 6; R1 выбран из группы, состоящей из водорода, C1-C8 линейного или разветвленного алкила, C1-C8 линейного или разветвленного алкенила, циклоалкила, циклоалкенила, замещенного или незамещенного гетероарила, замещенного или незамещенного арила, замещенного или незамещенного гетероалициклила, сульфонила, C1-C8 линейного или разветвленного пергалогеналкила, -C(=Z)R6, -C(=Z)OR6, и -C(=Z)N(R6)2; R2, R2a, R2b, R2c, по отдельности выбраны из группы, состоящей из водорода, алкила, алкенила, циклоалкила, циклоалкенила, замещенного или незамещенного арила, замещенного или незамещенного гетероарила, замещенного или незамещенного гетероалициклила, гидрокси, галогена, сульфонила, пергалогеналкила, -CN, -OR6, -NR6R6a, -NR6NR6aR6b, -NR6N=CR6aR6b, -N(R6)С(R6а)=HR6b, -C(=Z)R6, -C(=Z)OR6, -С(=Z)NR6R6а, -N(R6)-C(=Z)R6a, -N(R6)-C(=Z)NR6bR6a, ...

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10-04-2005 дата публикации

АНАЛОГИ ВИТАМИНА D

Номер: RU2003136744A
Принадлежит:

... 1. Аналоги витамина D, представляющие собой соединения, выбранные отдельно или в смеси, из группы, состоящей из: (4Е,6Е)-7-{3-[2-(3,4-Бис-гидроксиметилфенил)этил]фенил}-3-этил-нона-4,6-диен-3-ол, (Е)-6-[3-(3, 4-Бис-гидроксиметилбензилокси)фенил]-1,1,1-трифтор-2-трифторметилокт-5-ен-3-ин-2-ол, (3Е,5Е)-6-[3-(3,4-Бис-гидроксиметилбензилокси)фенил]-1,1,1-трифтор-2-трифторметилокта-3,5-диен-2-ол, (Е)-6-{3-[2-(3,4-Бис-гидроксиметилфенил)этил]фенил}-1,1,1-трифтор-2-трифторметилокт-5-ен-3-ин-2-ол, (3Е,5Е)-6-{3-[2-(3,4-Бис-гидроксиметилфенил)этил]фенил}-1,1, 1-трифтор-2-трифторметилокта-3,5-диен-2-ол, а также их геометрических изомеров и указанных выше соединений, в которых одна или несколько гидроксильных групп имеют защитную группу типа -(С=О)-R, где R обозначает линейный или разветвленный алкильный радикал, содержащий от 1 до 6 атомов углерода, или арильный радикал, содержащий от 6 до 10 атомов углерода, или аралкильный радикал, содержащий от 7 до 11 атомов углерода; при этом арильный радикал ...

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15-06-1984 дата публикации

Способ получения @ -кофигурированных замещенных фенилпропанола

Номер: SU1098519A3
Принадлежит: БАСФ АГ (ФИРМА)

СПОСОБ ПОЛУЧЕНИЯ S-КОНФИГУРИРОВАННЫХ ЗАМЕЩЕННЫХ ФЕНИЛПРОПАНОЛА общей формулы Б -( Нг- clH- ciHzон. тГ ОНз где R- водород или метоксил, водород, трет-бутил, третбутоксил или метоксил отличающийся тем, что, с целью получения (-) -энантиомеров -целевых соединений, соответствующее замещенное коричного альдегида подвергают микробиологическому гидрированию с помощью дрожжей СО Saccharomyces cerevisiae : при 1040°С под воздействием аэрации возс духом в присутствии сахарозы с последуюр ей экстракцией полученного продукта хлористым метиленом и вьщелением целевого продукта упариванием. со 00 СП ...

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15-09-1989 дата публикации

Способ получения алкеновых производных или их солей

Номер: SU1508955A3

Изобретение касается ациклических ненасыщенных соединений , в частности, способов получения алмкеновых производных общей формулы R4-CH2-(CH2M)N-C(-C6H4-N-R1)-C(-C6H4-N-R2)*M99.(-C6H4-N-R3), где N=1 или 2 R1и MR2-H или OH R3-H, OH, OCH3или 2-(NM,N-диметиламино)-этоксил R4-CI или BR, или их м солей, обладающих эстрогенной, антиэстрогенной, прогестановмой и противоопухолевой активностью, что может быть использовано в медицине. Цель - создание новых активных соединений указанного класса. Синтез ведут реакцией соединения формулы R5-CH2-(CH2)N-CH(-C6H4-N-R6)-C(O)-C6H4-N-R7, где N имеет указанные значения R5-тетрагидропиран-2-илокси или бензилокси R6-H или тетрагидропиран-2-илокси R7-H, метокси или тетрагидропиран-2-илокси, с соединением общей формулы R8-C6H4-N-MG BR, где R8-H, метокси, 2-(N,N-диметиламино)этокси или тетрагидропиран-2-илокси. Образующееся соединение, в котором R8-тетрагидропиран-2-илокси или бензилокси, подвергают кислотному гидролизу с последующей дегидратацией и замещением гидроксильной ...

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06-04-1989 дата публикации

3-(4-FLUOROPHENOXY)-1-PROPANOL

Номер: DE0003662189D1
Принадлежит: PFIZER

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07-11-2013 дата публикации

New phenol compounds, useful as intermediate for the preparation of polysubstituted benzene compounds

Номер: DE102013005820A1
Принадлежит:

Phenol compounds (I) are new. Phenol compounds of formula (I) are new. R : linear or branched, unsubstituted or mono- or polysubstituted 1-20C-alkyl, unsubstituted or mono- or polysubstituted cycloalkyl-, heterocyclylalkyl or aralkyl having 20C or unsubstituted or mono-or polysubstituted heteroaryl ring system having 5-60, where two or more substituents R form mono-or polycyclic, aliphatic or aryl ring system; n : 0-3; L1-L4 : H or F; and X : CF 3 or OCF 3. Independent claims are included for: (1) preparation of (I); and (2) preparing polysubstituted benzene compound with partial structure of formula (II), comprising reacting (I) with a bis(alkylthio)carbenium salt. [Image] [Image].

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11-09-2014 дата публикации

Elektrochemische Kupplung eines Phenols mit einem Naphthol

Номер: DE102013203866A1
Принадлежит:

Elektrochemisches Verfahren zur selektiven Kupplung von einem Phenol mit einem Naphthol, welche sich in ihrem Oxidationspotential unterscheiden. Verbindungen, welche beispielsweise durch die elektrochemische Kupplung hergestellt werden können.

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25-03-1941 дата публикации

Verfahren zur Herstellung von Durohydrochinonaethern

Номер: DE0000704171C
Принадлежит: MERCK AG E, FIRMA E. MERCK

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09-03-1955 дата публикации

Improvements in and relating to substituted methylol anisoles

Номер: GB0000725782A
Автор:
Принадлежит:

Compounds of the general formula where R is a radical selected from the group consisting of phenyl, cyclohexyl and methoxy (see Group IV (b)) are employed as modifying and plasticizing agents for phenolic resins. In addition, the compositions can be heated, preferably in the presence of an acidic catalyst such as para-toluene sulphonic acid or sulphamic acid, to give hard products which can be employed as moulding compositions, with or without fillers. Solutions of the compounds can be used for coating purposes, to deposit films which can be cured to the tack-free state. Example (3) describes the preparation and properties of resins obtained from the compounds by adding 0.1 per cent by weight of sulphamic acid and heating at 200 DEG C. for varying lengths of time.ALSO:Compounds of the general formula where R is a radical selected from the group consisting of phenyl, cyclohexyl and methoxy, are prepared by reacting the corresponding hydroxy ...

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08-07-1970 дата публикации

Process for the preparation of Novel Nickel Alcoholates and the Parent Alcohols thereof

Номер: GB0001197500A
Автор: WILKE G, HEIMBACH P
Принадлежит:

... 1,197,500. Alcohols and nickel alcoholates. STUDIENGESELLSCHAFT KOHLE m.b.H. 17 Oct., 1967 [26 May, 1967], No. 47171/67. Heading C2C. [Also in Division C5] Nickel alcoholates and their parent alcohols are prepared by (a) allowing carbonyl compounds and 1,3-diolefins to react with complexes of nickel (o) or (b) reacting #-allyl nickel compounds with carbonyl compounds and if desired hydrolysing the nickel alcoholate to the parent alcohol. The invention further comprises #-allyl-nickel alcoholates and the following alcohols: octene-(4)-diol-(2,7); 1,6-diphenyl-trans-hexane - (3) - diol - (1,6); 1,10 - diphenyldecatri- 1,5,9 - ene - diol - (3,8); 1,14 - diphenyltetradecapentaene - (1,3,7,11,13) - diol- (5,10); the compound of the formula 2,7 - dimethyloctene - (4) - diol - (2,7); 1,4 - di- (cyclohexanolyl - 1) - butene - (2); 2,7 - diphenyloctene - (4) - diol - (2,7); 1,6 - diphenyl- (3) - methylhexene - (3) - diol - (1,6); 1,6 - diphenyl - (3,4) - dimethylhexene - (3) - diol- (1,6); 1,3,4,6 ...

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07-06-1972 дата публикации

PROCESS FOR THE MONOALKYLATION OF UNSUBSTITUTED DIHYDRICPHENOLS

Номер: GB0001277186A
Принадлежит:

... 1277186 Monoalkyl ethers of dihydric phenols SOC DES USINES CHIMIQUES RHONEPOULENC 17 Feb 1970 [19 Feb 1969] 7660/70 Heading C2C A process for the preparation of monoethers of the unsubstituted dihydric phenols pyrocatechol, resorcinol and hydroquinone comprises reacting the dihydric phenol with an alkyl chloride having 1 to 5 carbon atoms in the presence of a carbonate or bicarbonate of an alkali metal. Amines such as di- and triethanolamine and di- and triethylamine may be employed as catalysts. The examples describe the preparation of monomethyl and monoethyl ethers.

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30-12-1971 дата публикации

Номер: GB0001258554A
Автор:
Принадлежит:

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28-01-1987 дата публикации

Antitussive and mucus regulating 2-substituted thiazolidines

Номер: GB0002177690A
Принадлежит:

... 2-Substituted thiazolidines compounds have the formula wherein: X is a CH2, O, S; R is hydroxy, or an ester thereof of formula Rc-CO2-C1-C6-alkoxy, CH2=CH-CH2O-; HC IDENTICAL C-CH2-O-; methyl R, is hydrogen and R2 is hydrogen or a free or esterified carboxy group; R3 is hydrogen, a C1-C2alkylsulphonyl group, a phenyl, p-Cl phenyl, p-methylsulphonyl group or an acyl group of formula RdCO; p is zero or 1 with the proviso that when X is sulphur p is zero; both Ra and Rb are hydrogen or methyl; Rc and Rd, which are the same or different are: hydrogen or are chosen from various defined organic groups, or are salts with non toxic bases or acids thereof, enantiomers, diastereoisomers or mixtures thereof. The compounds are useful as antitussive or mucus regulating agents.

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15-11-1989 дата публикации

Leukotriene disease antagonists

Номер: GB0002218416A
Принадлежит:

New alkenoic acid derivatives can be prepared by reaction of corresponding aldehydic esters with phosphorous compounds in inert solvents and in the presence of bases followed by hydrolysis of the intermediate esters. The new alkenoic acid derivatives can be used as active compounds in medicaments.

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07-04-2010 дата публикации

p-Alkyl phenol alkoxylate co-oligomers and process for preparing o- or p- alkyl or alkenyl phenol alkoxylate oligomers or co-oligomers useful as demulsifiers

Номер: GB0002463927A
Принадлежит:

A process for preparing an o- or p-alkyl or alkenyl phenol alkoxylate oligomer or co-oligomer comprises adding a methylene donor to one or more o- or p-alkyl or alkenyl phenol alkoxylates. Suitable methylene donors include aldehydes or derivatives thereof, hexamethlene tetramine, an N-(substituted hydroxyalkyl) melamine compound or various derivatives thereof, an alkyloxyalkylpyridinium compound, oxazolidine or N-methyl-1,3,5-dioxazene. In particular, paraformaldehyde is added to p-nonylphenol 4 mole ethoxylate. The oligomers or co-oligomers may be useful as demulsifiers or emulsion breakers in the petroleum industry. A non-statistical non-random p-alkyl phenol alkoxylate co-oligomer wherein there are at least two different C3-12-alkyl residues as the p-alkyl residues is also claimed.

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27-03-1968 дата публикации

Alkylidene acetic acid derivatives

Номер: GB0001107866A
Принадлежит:

Compounds of Formula I are prepared by reacting the corresponding cyclic ketone with a (C1- 4-alkoxy) acetylene in presence of BF3 and an inert organic solvent, the alkoxyacetylene being added portionwise to the ketone and BF3 at a rate such that the temperature does not exceed 20 DEG C., the reaction being continued at a temperature from 0 DEG to the b.p. of the solution, and the product being optionally separated, where applicable, into cis- and transisomers. In the formula, R1 is H or C1- 4 alkyl, R6 is C1- 4 alkyl, each of R2, R3, R4, R5 is H, C1- 4 alkyl, R6 is C1- 4 alkyl, each of R2, R3, R4, R5 is H, C1- 4 alkyl, or (optionally substituted) cycloalkyl or aryl, or two of R2, R3, R4, R5 together are a hydrocarbon radical which with the cyclohexane ring atoms form a bicyclic monoterpenylide radical, a tetralylidene radical or a totally or partially hydrogenated phenanthrylidene radical. Compounds of Formula Ia, where R11, R12, R13 and R14 are ...

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03-06-1970 дата публикации

Improvements in Oxyalkylation Processes

Номер: GB0001193924A
Автор:
Принадлежит:

... 1,193,924. Alkoxylation of alcohols. HENKEL & CIE. G.m.b.H. 15 May, 1968 [16 May, 1967], No. 22968/68. Heading C2C. [Also in Division C3] Ether and polyether alcohols are produced by reacting a compound containing a hydroxyl group with an alkylene oxide in the presence of a tertiary oxonium salt as catalyst. In the examples tertiary butanol, n-octanol-2, ntetradecanol-1, a mixture of isomers of see.-ntetradecanol, mixtures of primary C 12-18 and C 12-15 alcohols, hexanediol-1,6, and oleyl alcohol are reacted with ethylene oxide, n-octanol-2 with propylene oxide, butylene oxide and epichlorohydrin and n-octanol-1 with glycide.

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28-05-1981 дата публикации

Substituted amiline derivatives for use as anti-atherosclerotic agents

Номер: GB0002062621A
Принадлежит:

Novel 2-or 3-(aralkyl- and heteroaralkylamino)phenyl compounds useful as hypolipidemic and atherosclerotic agents are represented by the structural formulae: wherein A is a saturated or unsaturated alkylene group of 1-18 carbon atoms which may be branched or unbranched; Y is selected from the group consisting of substituted or unsubstituted aryl and heteroaryl groups, such that the total number of carbon atoms in Y and A shall not exceed 24; R is selected from the group consisting of hydrogen or a group convertible in vivo thereinto such as methyl, carboxymethyl, acetyl, succinyl, 1-(sodium sulfo)loweralkyl, 1-(sodium sulfo)polyhydroxyloweralkyl, and 3-aryl-1,3-bis-(sodium sulfo)loweralkyl; and Z is a> wherein D is selected from the group consisting of hydroxy, hydrogen, loweralkoxy, loweralkyl, benzyloxy, (mono- or polyhydroxy)loweralkoxy, loweralkoxyethoxy, diloweralkylaminoethoxy, (mono- or polycarboxy)loweralkoxy, (mono- or polycarboxy)hydroxyloweralkoxy, allyloxy, 2,3 ...

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15-02-1984 дата публикации

QUINONE COMPOUNDS THEIR PRODUCTION AND USE

Номер: GB0002074158B
Автор:

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27-10-1982 дата публикации

2,3 - DICHLORO - 4 - (2 - THENOYL) PHENOXYACETIC ACID AND INTERMEDIATES

Номер: GB0002034688B
Автор:
Принадлежит: SMITHKLINE CORP

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07-09-2016 дата публикации

Production method for generating 3, 5-dihydroxy-4-methoxybenzyl alcohol from oyster meat

Номер: GB0002536097A
Принадлежит:

... [Problem] The purpose of the present invention is to provide a production method with which 3,5-dihydroxy-4-methoxybenzyl alcohol, which is completely undetected in raw oyster meat, can be produced at the stage of extracting oyster meat extract. [Solution] The present invention is characterized by producing 3,5-dihydroxy-4-methoxybenzyl alcohol from heat-treated oyster meat juice by heating, for six hours or longer at 98 to 100˚C, raw oyster meat in which 3,5-dihydroxy-4-methoxybenzyl alcohol is not detected when the oyster meat is in a raw state.

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18-06-1980 дата публикации

Meta, para-substituted isopropylidene bisphenols and methods for making

Номер: GB0002035323A
Автор: Keeley, Donald Edward
Принадлежит:

Meta,para-substituted isopropylidene bisphenols are provided and methods for making such materials. Phenol, or substituted phenol is condensed with a meta-substituted isopropenyl phenol or a meta-hydroxy- alpha , alpha -dimethylbenzyl alcohol in the presence of an acid catalyst. The resulting meta,para-substituted isopropylidene bisphenols can be used as stabilizers for polyvinyl chloride resins and as intermediates for making high performance thermoplastics having chemically combined meta,para-isopropylidene diphenoxy units.

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08-02-1984 дата публикации

Silver halide photographic materials with antistatic layer containing a surfactant

Номер: GB0002123969A
Принадлежит:

A silver halide photographic light-sensitive material is disclosed. The photographic material is comprised of a support base, a silver halide emulsion layer and an antistatic layer. The antistatic layer contains a nonionic surface active agent having two polyoxyethylene chains in a molecule represented by the formula (I): wherein R1 and R3 each represents a substituted or unsubstituted alkyl group, an aryl group, an alkoxy group, a halogen atom, an acyl group, an amido group, a sulfonamido group, a carbamoyl group or a sulfamoyl group, R2 and R4 each represents a hydrogen atom, a substituted or unsubstituted alkyl group, an aryl group, an alkoxy group, a halogen atom, an acyl group, an amido group, a sulfonamido group, a carbamoyl group or a sulfamoyl group, R5 represents a hydrogen atom, a methyl group or an alpha -furyl group, and m and n independently represents an average degree of polymerization of ethylene oxide, which is 2 to 40. By utilizing the compound of general formula (I) it ...

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02-12-1987 дата публикации

HALOGENATED ESTERS

Номер: GB0008725064D0
Автор:
Принадлежит:

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04-06-1986 дата публикации

STABILIZATION OF DYE IMAGES

Номер: GB0008610610D0
Автор:
Принадлежит:

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09-05-1990 дата публикации

PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE INTERMEDIATES FOR INSECTICIDAL COMPOUNDS

Номер: GB0009005467D0
Автор:
Принадлежит:

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17-08-1994 дата публикации

Novel chiral cyclohexyl compounds

Номер: GB0009412709D0
Автор:
Принадлежит:

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24-06-1987 дата публикации

TETRAHYDRONAPHTHALINE & INDANE DERIVATIVES

Номер: GB0008712114D0
Автор:
Принадлежит:

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09-06-1999 дата публикации

Process for the preparation of prostaglandin precursors

Номер: GB0009908327D0
Автор:
Принадлежит:

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04-11-1970 дата публикации

BICYCLO-[4,3,0]-NONANE DERIVATIVES

Номер: GB0001210999A
Принадлежит:

... 1,210,999. Bicycle - nonane derivatives. JENAPHARM VEB. 7 July, 1969, No. 34187/69. Heading C2C. Novel compounds (I) wherein R 1 is phenyl optionally substituted by -OH, -OCH 3 or -OC 2 H 5 ; R 2 is H, CH 3 , C 2 H 5 or phenethyl; R 3 is CH 3 , C 2 H 5 or C 3 H 7 ; R 4 is OH, OCOCH 3 , OCOC 2 H 5 or OCOC 6 H 5 ; R 5 is H or aliphatic hydrocarbyl or R 4 and R 5 together are oxo, methylidene, ethylidene or propylidene; and R 6 is H or OH and wherein a 3,4 or 4,5 or 5,6 double bond or both 4,5 and 6,7 double bonds may be present are prepared by reaction of (II) with vinyl magnesium halide to give (III) which is reacted with thiourea in glacial acetic acid to give (IV), which is then reacted with a 2-alkyl-cyclopentane-1,3-dione to give (V) which is then cyclized in the presence of an acid to give (VI) or cyclodehydrated to give (VII). Any oxo group may be reduced to the hydroxy group which may then be acylated if desired, or any double bonds may be hydrogenated or reduced. Intermediates isolated ...

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03-03-1982 дата публикации

HYDROXY-AND OXO-SUBSTITUTED ALPHA-BENZYLIDENYLCYCLOALKANES

Номер: GB0002002760B
Автор:
Принадлежит: UNICLER

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05-09-1979 дата публикации

Chemical compounds

Номер: GB0002014993A
Принадлежит:

... 4-(6-Substituted naphthyl)butan-2-ols,-butan-2-ones,-pentan-2-ols and -pentan-2-ones bearing a fluoro group in the naphthyl ring, and pro-drugs thereof, are anti-inflammatory agents. A typical embodiment is 4-(4-fluoro-6-methoxy-2-naphthyl)-butan-2-one.

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01-12-1976 дата публикации

PREPARATION OF PYROCATECHOL DERIVATIVES AND INTERMEDIATES USED

Номер: GB0001457108A
Автор:
Принадлежит:

... 1457108 Preparation of pyrocatechol derivatives BASF AG 24 Oct 1973 [25 Oct 1972] 49404/73 Heading C2C Pyrocatechols ethers of formula where R denotes alkyl which may be substituted by halogen, alkenyl which may be substituted by halogen, alkynyl which may be substituted by halogen, or aralkyl are obtained by cleaving in an acid medium a compound of formula where R has the above meaning and R1 denotes H or (C 1-4 ) alkyl; R2 denotes H, benzyl, (C 1-4 ) alkyl which may be substituted with halogen, -OCH 3 or -OC 2 H 5 ; R3 denotes (C 1-4 ) alkyl, cycloalkyl, #-chloroethyl, alkoxyalkyl, phenyl, (C 2-4 ) alkenyl, (C 2-4 ) alkynyl, or acyl or R1 and R2, together with the carbon atoms whose substituents they are, and R1 and R3, together with the carbon and oxygen atom whose substituents they are, form a 5- or 6-membered ring. The invention also comprises compounds of Formula II wherein R, R1, R2 and R3 have ...

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07-04-1982 дата публикации

GLYCOL COMPOUNDS FOR LOWERING THE LIPID CONTENT

Номер: GB0002021102B
Автор:
Принадлежит: SIEGFRIED AG

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07-09-1966 дата публикации

Manufacture of guaiacol

Номер: GB0001041764A
Автор:
Принадлежит:

Guaiacol is prepared by reacting at pressures below 300 p.s.i.g. a water-insoluble divalent metal salt of catechol with a methyl halide in the presence of water and a water-immiscible organic solvent for guaiacol, separating the organic phase and recovering guaiacol therefrom, the divalent metal being a metal which forms a water insoluble sulphate, e.g. Ba++, Sr++, Ca++, Pb++, the organic solvent being inert to the divalent metal salt of catechol. The reaction takes place at 75 DEG to 150 DEG C. The divalent metal salt may be formed in situ from catechol, a water-soluble mineral acid salt, e.g. a chloride or a hydroxide of the divalent metal and caustic alkali, e.g. caustic soda. Preferably the reaction mixture contains at least 0.25 mole of water soluble divalent metal salt per mole of catechol and 0.7 to 2.00 moles of methyl chloride per mole of divalent metal salt of catechol. Specified organic solvents used are aliphatic and aromatic hydrocarbons which may be halogenated, and nitro ...

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07-09-2022 дата публикации

Novel compounds, methods for their manufacture, and uses thereof

Номер: GB0002604428A
Принадлежит:

Synthetic cannabinoid analogue compounds of formula (I), wherein X is a group as defined herein. Also provided is a pharmaceutical composition of compounds of formula (I). Also provided is a compound of formula (I), or pharmaceutical composition, for use in a method of treatment, or for use as a medicament; which may be for use in the treatment of, or for use as a medicament for treating, epilepsy, generalised seizure, tonic-clonic seizure. Also provided is a method of preparing a compound of formula (I), comprising reacting a compound of formula (II) with a compound of formula (III), both defined herein. The method may use a palladium catalyst. Also provided is a method of preparing compounds of formula (I), comprising reacting a compound of formula (II) with bis(pinacolato)diboron (B2pin2), and reacting the product of that with a compound of formula (IV). The steps of the method may use a palladium catalyst. Also provided is an intermediate compound of formula (II), for use in the preparation ...

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30-04-1993 дата публикации

COMPOUNDS

Номер: AP0009300509A0
Автор:
Принадлежит:

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30-04-2009 дата публикации

Process and intermediates for preparing integrase inhibitors

Номер: AP0200904831D0
Принадлежит:

Подробнее
25-01-1989 дата публикации

Insectidical ethers.

Номер: AP0000000034A
Принадлежит:

The invention provides novel insecticidally useful fluorinated ethers of formula Ar-CX(Z)-CHX-O-CH2-Y where Ar and Y are both substituted aryl groups, Z is a lower fluoroalkyl group (eg. trifluoromethyl), X1 is hydrogen and X is hydrogen, halo, hydroxy, alkoxy or acyloxy, as well as the compounds where X and X1 form a second bond between the adjacent carbon atoms. A typical example is 1,1,1-trifluoro-2-(4-ethoxyphenyl)-3-(3-fluoro-3-phenoxybenzyloxy) propane. The invention also provides novel intermediates for the preparation of the compounds including those of formulae ArCH (CF3) CH2OH, ArC(OH) (CF3) CH2OH, ArC(OH) (CF3) CH2Hal ...

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01-05-1992 дата публикации

Novel aryloxy alcohol benzenes, processes for their preparation as well as the pharmaceutical compositions containing them.

Номер: AP0000000188A
Принадлежит:

This invention has a subject matter novel aryloxy alkylbenzenes, their processes for production and the pharmaceutical compositions containing them.

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01-08-1986 дата публикации

INSECTICIDAL ETHERS

Номер: AP0008600041A0
Автор:
Принадлежит:

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31-10-2014 дата публикации

Process and intermediates for preparing integrase inhibitors

Номер: AP0000003004A
Принадлежит:

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31-01-1991 дата публикации

NOVEL ARYLOXY ALCOYL BENZENES,PROCESS FOR THEIR PREPARATION AS THE PHARMACEUTICAL COMPOSITION CONTAINING THEM

Номер: AP0009000223A0
Автор:
Принадлежит:

Подробнее
30-04-2009 дата публикации

Process and intermediates for preparing integrase inhibitors

Номер: AP2009004831A0
Принадлежит:

Подробнее
30-06-2005 дата публикации

Substituted aralkyl derivatives

Номер: AP2005003311A0
Принадлежит:

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30-06-2015 дата публикации

Family of aryl, heteroaryl, O-aryl and O-heteroaryl carbasugars

Номер: AP0000003308A
Принадлежит:

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31-12-2013 дата публикации

Family of aryl, heteroaryl, O-aryl and O-heteroaryl carbasugars

Номер: AP2013007322A0
Принадлежит:

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30-11-1988 дата публикации

Derived propargyloxybenzyenes their fungicidal preparations the container.

Номер: OA0000008595A
Автор: PLACE PIERRE, PEPIN REGIS
Принадлежит:

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15-04-1994 дата публикации

Orally active antiral compounds.

Номер: OA0000009828A
Принадлежит:

Подробнее
29-02-1988 дата публикации

Insecticidal ethers.

Номер: OA0000008381A
Принадлежит:

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05-05-1970 дата публикации

Method of preparation of derived from dimethoxybenzene

Номер: OA0000002000A
Автор:
Принадлежит:

Подробнее
13-10-2006 дата публикации

Substituted aralkyl derivatives.

Номер: OA0000012960A
Принадлежит:

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31-08-1984 дата публикации

A method for fighting against the infestations due to the ants.

Номер: OA0000007307A
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30-06-1981 дата публикации

Phenyl-alcoyléthers.

Номер: OA0000006329A
Автор:
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31-01-1987 дата публикации

Improvements relating to pesticides.

Номер: OA0000007988A
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30-06-2005 дата публикации

Substituted aralkyl derivatives

Номер: AP0200503311A0
Принадлежит:

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31-12-2013 дата публикации

Family of aryl, heteroaryl, O-aryl and O-heteroaryl carbasugars

Номер: AP0201307322A0
Принадлежит:

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31-01-1991 дата публикации

NOVEL ARYLOXY ALCOYL BENZENES,PROCESS FOR THEIR PREPARATION AS THE PHARMACEUTICAL COMPOSITION CONTAINING THEM

Номер: AP0009000223D0
Автор:
Принадлежит:

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30-06-2005 дата публикации

Substituted aralkyl derivatives

Номер: AP0200503311D0
Принадлежит:

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31-12-2013 дата публикации

Family of aryl, heteroaryl, O-aryl and O-heteroaryl carbasugars

Номер: AP0201307322D0
Принадлежит:

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30-04-1993 дата публикации

COMPOUNDS

Номер: AP0009300509D0
Автор:
Принадлежит:

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01-08-1986 дата публикации

INSECTICIDAL ETHERS

Номер: AP0008600041D0
Автор:
Принадлежит:

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21-06-2012 дата публикации

Cyclic compound, process for production of the cyclic compound, radiation-sensitive composition, and method for formation of resist pattern

Номер: US20120156615A1
Принадлежит: Mitsubishi Gas Chemical Co Inc

A cyclic compound represented by formula (1): wherein L, R 1 , R′, and m are as defined in the specification. The cyclic compound of formula (1) is highly soluble to a safety solvent, highly sensitive, and capable of forming resist patterns with good profile. Therefore, the cyclic compound is useful as a component of a radiation-sensitive composition.

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17-01-2013 дата публикации

Orally bioavailable stilbenoids- compositions and therapeutic applications thereof

Номер: US20130017605A1
Принадлежит: Individual

A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by SIR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising, dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by are also disclosed. An additional embodiment, also discloses the enhanced anti- Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.

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21-03-2013 дата публикации

PROCESS FOR PRODUCING HIGH MOLECULAR WEIGHT POLYETHYLENE

Номер: US20130072649A1
Принадлежит: TICONA GMBH

In a process for producing high molecular weight polyethylene, ethylene is contacted with a slurry of a catalyst composition comprising a Group 4 metal complex of a phenolate ether ligand under polymerization conditions comprising a temperature of about 20° C. to less than 90° C. and a pressure of about 4 bar to about 40 bar. 1. A process for producing high molecular weight polyethylene , the process comprising: contacting ethylene under polymerization conditions with a slurry of a catalyst composition comprising a Group 4 metal complex of a phenolate ether ligand , wherein the polymerization conditions comprise a temperature of about 20° C. to less than 90° C. and a pressure of 4 bar to 40 bar.2. The process of wherein the polymerization conditions comprise a temperature of 50° C. to 85° C.3. The process of wherein the polymerization conditions comprise a pressure of 4 bar to 20 bar.4. The process of wherein the Group 4 metal complex is disposed on a particulate support.5. The process of wherein the particulate support has an average particle size claim 4 , d50 claim 4 , of less than 58 microns claim 4 , preferably less than 50 microns claim 4 , more preferably less than 30 microns claim 4 , most preferably from 4 to 20 microns.6. The process of wherein the particulate support has a span claim 4 , log(d/d) less than 0.6.7. The process of wherein the particulate support comprises an inorganic oxide claim 4 , preferably silica.8. The process of wherein the particles of the support are substantially spherical.9. The process of wherein the particles of the support are treated with an organoaluminum compound before said Group 4 metal complex is deposited on the support.10. The process of wherein the Group 4 metal complex is a complex of a bis(phenolate) ether ligand.14. The process of wherein the Group 4 metal is zirconium.15. High molecular weight polyethylene powder produced by the process of .17. A complex of a Group 4 metal compound claim 16 , such as a zirconium or ...

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28-03-2013 дата публикации

NEURO-PROTECTIVE EFFECTS OF ADELOSTEMMA GRACILLIMUM AND ITS ISOLATED COMPOUNDS

Номер: US20130079293A1

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

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23-05-2013 дата публикации

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Номер: US20130131167A1
Принадлежит:

This invention provides bisphenol derivatives having a structure of formula 1. Said compounds are modulators of the androgen receptor activity and are useful in the treatment of various diseases, including prostate cancer, breast cancer, ovarian cancer, endometrial cancer, acne, ovarian cysts, polycystic ovarian disease, age-related macular degeneration, precocious puberty, hirsutism and hair loss. 282-. (canceled)83. The method of claim 1 , wherein the modulating of androgen receptor (AR) activity is in a mammalian cell.84. The method of claim 83 , wherein the modulating AR activity is for treatment of at least one indication selected from the group consisting of: prostate cancer claim 83 , breast cancer claim 83 , ovarian cancer claim 83 , endometrial cancer claim 83 , hair loss claim 83 , acne claim 83 , hirsutism claim 83 , ovarian cysts claim 83 , polycystic ovary disease claim 83 , precocious puberty claim 83 , and age-related macular degeneration.85. The method of claim 84 , wherein the indication is prostate cancer.86. The method of claim 85 , wherein the prostate cancer is androgen-independent prostate cancer.87. The method of claim 85 , wherein the prostate cancer is androgen-dependent prostate cancer.107. The compound or salt according to claim 88 , wherein G claim 88 , when present claim 88 , is CHC≡H or CH(CH).108. The compound or salt according to claim 88 , wherein each remaining Z is independently selected from: CCH; CH; and CBr.109. The compound or salt according to claim 88 , wherein each remaining Z is CH.110. The compound or salt according to claim 88 , wherein X is CH.111. The compound or salt according to claim 88 , wherein X is CHRand Ris CH.112. The compound or salt according to claim 88 , wherein X is CRRand each of Rand Ris CH.113. The compound or salt according claim 88 , wherein one or more of the OH groups of the compound or salt is optionally substituted to replace the H with a moiety selected from TABLE 1.116117-. (canceled)118. A ...

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13-06-2013 дата публикации

ALKYNE AND ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE-1 RECEPTOR MODULATORS

Номер: US20130150331A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'img': {'@id': 'CUSTOM-CHARACTER-00015', '@he': '3.89mm', '@wi': '6.69mm', '@file': 'US20130150331A1-20130613-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'sup': 14', '15, '“” represents a double bond “—CR═CR—”.'}3. A compound according to claim 1 , wherein:{'sup': '1', 'sub': '2', 'Lis CH.'}4. A compound according to claim 1 , wherein:{'sup': '1', 'Lis O, S or NH.'}7. A compound according to claim 1 , selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid.8. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.9. A pharmaceutical composition according to claim 8 , wherein the compound is selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid. This application is a Divisional of U.S. patent application Ser. No. 13/305,398, filed Nov. 28, 2011, which claims the benefit of U.S. Provisional Application Ser. No. 61/419,278 filed Dec. 3, 2010, both of which are hereby incorporated by reference in their entirety.The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of sphingosine-1-phosphate receptors. The invention relates specifically to the use of ...

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13-06-2013 дата публикации

Pharmaceutical composition comprising a curcumin derivative

Номер: US20130150628A1
Автор: Thomas M. DiMauro
Принадлежит: Individual

The present invention is directed to a pharmaceutical composition comprising:

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25-07-2013 дата публикации

Hydrocarbon Decomposition For Soil And Water Remediation

Номер: US20130187081A1
Принадлежит: Individual

Presented herein are compositions including a linear tenso-active surfactant which, upon contact and mechanical stirring of a hydrocarbon body, induces emulsification, resulting in oxidation of fatty acid aliphatic bodies. The compositions solve the problem of hydrocarbon pollution. The hydrocarbon decomposer and its by-products dissolve hydrocarbons present in polluted bodies such as clays, soils, water and sand. Methods of the invention create a residue that is a fertilizer, at room temperature and with no need for high pressure.

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01-08-2013 дата публикации

TRISUBSTITUTED METHYL ALCOHOLS AND THEIR POLYMERIZABLE DERIVATIVES

Номер: US20130197262A1
Принадлежит: Indicator Systems International, Inc.

Provided herein are trisubstituted methyl alcohols, preferably pH indicators that are substituted with optionally substituted aryl and or optionally substituted heteroaryl groups, and optionally include one or more polymerizable substituents. 7. The compound of claim 1 , wherein{'sup': 1', '8, 'Ris hydrogen or —OR;'}{'sup': 2', '8', '9', '2', '8', '8, 'sub': 1', '4, 'each of R-Rindependently is C-Calkyl or is -L-Rprovided that at least one of R-Ris -L-R;'}{'sup': '9', 'Ris a polymerizable group; and'}L is a covalent bond or a linker which joins the one or more polymerizable groups to oxygen atoms.8. The compound of claim 1 , wherein 1-7 of R-Rare -L-R.9. The compound of claim 1 , wherein 2-6 of R-Rare -L-R.10. The compound of claim 1 , wherein 1-6 of R-Ris C-Calkyl.11. The compound of claim 1 , wherein 1-6 of R-Ris methyl.13. The compound of claim 1 , wherein L is C-Calkylene or heteroalkylene optionally substituted with 1-10 substituents selected from the group consisting of oxo (═O) claim 1 , thio (═S) claim 1 , and C-Calkyl.15. The compound of claim 14 , wherein each Rindependently is methyl claim 14 , vinyl claim 14 , allyl claim 14 , —(CH)—OCOCH═CH claim 14 , or —(CH)—OCOC(Me)═CH claim 14 , provided that at least one Ris not methyl.16. The compound of claim 14 , wherein 1 claim 14 , 2 claim 14 , or 3 Rgroups are —(CH)—OCOC(Me)═CH.17. The compound of claim 1 , wherein at least one of R-Ris hydrogen or Ris OH. This application claims priority to U.S. provisional application Ser. No. 61/570,626, filed Dec. 14, 2011, and Ser. No. 61/698,427, filed Sep. 7, 2012. These applications are hereby incorporated by reference in their entireties.This invention relates to trisubstituted methyl alcohols that are substituted with optionally substituted aryl and or optionally substituted heteroaryl groups, which preferably act as pH indicators. This invention also relates to such trisubstituted methyl alcohols that contain one or more polymerizable functional groups so as to ...

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08-08-2013 дата публикации

Sugar plant derived by-products and methods of production thereof

Номер: US20130203688A1

The present document describes a nutraceutical or cosmeceutical composition for the prophylaxis of an ailment comprising a therapeutically effective amount of a sugar plant syrup filtration residue in association with a pharmaceutically acceptable carrier. The present document also describes a nutraceutical or cosmeceutical composition for improving health condition of skin. The present document describes a method of producing a sugar plant syrup-derived product; wherein the improvement is characterized in the step of: collecting a sugar plant syrup residue during the production of sugar or syrup to produce a syrup-derived by-product.

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15-08-2013 дата публикации

FLUOROPOLYETHER COMPOUND, LUBRICANT AND MAGNETIC DISK EACH CONTAINING THE SAME

Номер: US20130209837A1
Принадлежит: MORESCO CORPORATION

A compound of the formula (1), lubricant containing the compound and magnetic disk 2. A compound as defined in wherein x and y are each a real number of 0 to 10 claim 1 , and z is a real number of 1 to 10.4. A lubricant as defined in wherein x and y are each a real number of 0 to 10 claim 3 , and z is a real number of 1 to 10.6. A magnetic disk as defined in wherein x and y are each a real number of 0 to 10 claim 5 , and z is a real number of 1 to 10. The present invention relates to fluoropolyether compounds having an aromatic group and hydroxyl, lubricants containing the compound and magnetic disks having the lubricant applied thereto.With an increase in the recording density of magnetic disks, the distance between the magnetic disk serving as a recording medium and the head for use in recording of information or playback has become almost nil close to contact therebetween. The magnetic disk is provided over the surface thereof with a carbon protective film or lubricant film for the purpose of diminishing abrasion due to the contact or sliding of the head thereon or preventing contamination of the disk surface.The carbon protective film is produced generally by the sputtering process or CVD process. The disk surface is protected with the two films, i.e., the carbon protective film and the lubricant film thereover.The lubricants generally in use are fluoropolyethers having functional groups. Examples of functional groups are hydroxyl, amino and cyclophosphazene groups. Particularly, lubricants having a phosphazene group are materials having high resistance to decomposition and known as materials for giving high durability to magnetic disks (for example, Patent Literature 1, 2).The cyclophosphazene group takes the molecular structure of 6-membered ring comprised of three phosphorus atoms and three nitrogen atoms as a main skeleton, and two substituents lengthening up and down of the 6-membered ring from each phosphorus atom (for example, Nonpatent Literature 1). ...

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15-08-2013 дата публикации

NOVEL BIPHENYL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PREPARING NOVEL BIPHENYL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING DIABETES COMPLICATIONS

Номер: US20130210928A1
Принадлежит: KOREA INSTITUTE OF ORIENTAL MEDICINE

The present invention provides a novel biphenyl compound or pharmaceutically acceptable salts thereof, methods for preparing the same, and pharmaceutical compositions for preventing or treating diabetic complications containing the same as an active ingredient. Novel biphenyl compounds, according to the present invention, effectively suppress generation activity of advanced glycation end products, which cause diabetic complications and are a criterion for evaluating the effectiveness of a treating agent for diabetic complications, and show an excellent therapeutic effect on retina blood vessels, increased occludin, and decreased angiogenic growth factor in actual diabetic retinopathy induced retina. Thus, novel biphenyl compounds according to the present invention can be used effectively as an active ingredient in compositions for preventing or treating diabetic complications such as diabetic retinopathy. 2. A method for preparing a novel biphenyl compound , the method comprising the steps of:{'i': Osteomeles schwerinae', 'Osteomeles schwerinae, '(1) extracting Schneid with water, an alcohol, or a mixture thereof to obtain Schneid extract;'}{'i': Osteomeles schwerinae', 'Osteomeles schwerinae, '(2) suspending the Schneid extract obtained from step (1) in water and then obtaining n-hexane, ethyl acetate, and n-butanol fractions of Schneid by stepwise using n-hexane, ethyl acetate and n-butanol as an extraction solvent;'}{'i': 'Osteomeles schwerinae', '(3) carrying out a silica gel column chromatography on the ethyl acetate fraction of Schneid obtained from step (2) to separate and purify an active fraction; and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(4) carrying out Sephadex LH-20 column chromatography on the active fraction obtained from step (3) to separate and purify the compound represented by Chemical Formula 1 of .'}3. A pharmaceutical composition for preventing or treating diabetic complications claim 1 , the composition containing the novel ...

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22-08-2013 дата публикации

SHIP1 MODULATORS AND RELATED METHODS

Номер: US20130217674A1
Принадлежит: The University of British Columbia

Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, Rand A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed. 19. A composition comprising a compound of in combination with a pharmaceutically acceptable carrier or diluent.20. A method for modulating SHIP1 comprising administering an effective amount of a composition of to an animal in need thereof.21. A method for treating a disease claim 19 , disorder or condition comprising administering an effective amount of a composition of to an animal in need thereof claim 19 , where the disease claim 19 , disorder or condition is an autoimmune disease claim 19 , disorder or condition claim 19 , an inflammatory disease claim 19 , disorder or condition claim 19 , or a neoplastic or cell proliferative disease claim 19 , disorder or condition.22. The method of wherein the disease claim 21 , disorder or condition is an autoimmune disease claim 21 , disorder or condition selected from idiopathic pulmonary fibrosis claim 21 , an inflammatory bowel disease claim 21 , rheumatoid arthritis claim 21 , Still's Disease claim 21 , Sjögren's Syndrome claim 21 , systemic lupus erythematosus claim 21 , and systemic sclerosis.23. The method of claim 22 , wherein the disease claim 22 , disorder or condition is an inflammatory bowel disease selected from Crohn's Disease and ulcerative colitis.24. The method of wherein the disease claim 21 , disorder or condition is an inflammatory disease ...

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29-08-2013 дата публикации

DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES

Номер: US20130224135A1
Автор: Jia Qi, Zhao Ji-Fu
Принадлежит: Unigen, Inc.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier. 117-. (canceled)19. The compound of claim 18 , wherein the compound is isolated from one or more plants.20. The compound of claim 19 , wherein the compound is isolated from stems claim 19 , stem barks claim 19 , trunks claim 19 , trunk barks claim 19 , twigs claim 19 , tubers claim 19 , roots claim 19 , root barks claim 19 , young shoots claim 19 , seeds claim 19 , rhizomes claim 19 , flowers or other reproductive organs claim 19 , or leaves or other aerial parts of the one or more plants.21. The compound of claim 19 , wherein the compound is isolated from a Compositae claim 19 , Fabaceae claim 19 , Lauraceae claim 19 , Leguminosae claim 19 , Liliaceae claim 19 , Loranthaceae claim 19 , ...

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29-08-2013 дата публикации

SKIN LIGHTENING COMPOSITIONS

Номер: US20130224137A1
Принадлежит: LASYA, INC.

Compositions and methods for lightening mammalian skin are described herein. 2. The composition of claim 1 , wherein Z is O.3. The composition of claim 1 , wherein A and B are taken together with the atoms to which they are attached to form an optionally substituted ring having from 4-9 member atoms.4. The composition of claim 1 , wherein A and B are taken to taken together with the atoms to which they are attached to form a ring having 6 member atoms.12. The composition of claim 1 , wherein the compound of formula I is 4-(tetrahydro-2H-pyran-2-yloxy)phenol.13. The composition of claim 1 , wherein the compound of formula I is present in the composition at a concentration of about 0.5 wt. % to about 10 wt. %.14. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid claim 1 , tocopherol claim 1 , butylated hydroxybenzoic acid claim 1 , butylated hydroxytoluene claim 1 , butylated hydroxyanisole claim 1 , uric acid claim 1 , gallic acid claim 1 , sorbic acid claim 1 , glutathione claim 1 , and esters and salts of any thereof.15. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid or a salt thereof claim 1 , ascorbyl phosphate or a salt thereof claim 1 , ascorbyl palmitate or a salt thereof claim 1 , tocopherol or a salt thereof claim 1 , tocopheryl acetate and sodium metabisulfite.16. The composition of claim 1 , comprising at least two antioxidants.17. The composition of claim 1 , comprising at least three antioxidants.18. The composition of claim 1 , comprising at least four antioxidants.19. The composition of claim 1 , comprising at least five antioxidants.20. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant is present in an amount of about 0.01 wt. % to about 3.0 wt. %.21. The composition of claim 1 , wherein the composition comprises an antioxidant ...

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05-09-2013 дата публикации

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

Номер: US20130228332A1
Принадлежит:

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

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03-10-2013 дата публикации

PHENOXYPROPANOL DERIVATIVES AND THEIR USE IN TREATING CARDIAC AND CARDIOVASCULAR DISEASES

Номер: US20130261178A1
Принадлежит:

A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: 2. The compound as claimed in wherein Ris selected from unsubstituted and substituted Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , Calkyl claim 1 , Caryl-Calkyl claim 1 , Calkoxy-Caryl-Calkyl.3. The compound as claimed in wherein Xis selected from CO claim 1 , CS claim 1 , SOand a single bond.4. The compound as claimed in wherein Rand Rare selected from ROZO as hereinbefore defined claim 1 , m- claim 1 ,p-(OCH)or o- claim 1 , m- or p-OH claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , NH claim 1 , R claim 1 , OR claim 1 , or CFor a combination thereof.12. A process for the preparation of a compound of formula I-0 or subformulae as defined in .14. A composition comprising a therapeutically effective amount of a compound of formula I-0 or subformulae or its pharmaceutically acceptable salt and physiologically hydrolysable derivative as defined in in association with one or more pharmaceutical carriers or diluents.15. The use of a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition as defined in in the prevention or treatment of a condition selected from ischaemic heart disease claim 1 , hypertension and heart failure claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD.16. A method of treating a condition selected from ischaemic heart disease (also known as myocardial infarction or angina) claim 1 , hypertension and heart failure claim 1 , restenosis and cardiomyopathy claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD claim 1 , said method comprising administering to a subject in need thereof claim 1 , a compound of formula I-0 or subformulae or pharmaceutically acceptable salt or composition thereof as defined in in an amount sufficient to treat the condition.17. A method of ...

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10-10-2013 дата публикации

Novel phytochemicals from extracts of maple syrups and maple trees and uses thereof

Номер: US20130267474A1

The present invention describes phytochemicals present in maple syrup and maple tree extracts by butanol, ethyl acetate and methanol. Novel compounds are isolated from maple syrups, including one compound Quebecol generated in the maple syrup manufacturing process. Also described are digesting extract of maple syrup. The phytochemicals may be used for the treatment or prevention of cancers, metabolic syndromes, diabetes, microorganism infections and/or antioxidants.

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07-11-2013 дата публикации

PROCESS FOR PRODUCTION OF HYDROXYSTILBENE DERIVATIVE HAVING PHYSIOLOGICAL ACTIVITY

Номер: US20130296613A1
Принадлежит: UHA MIKAKUTO CO., LTD.

A process for producing a hydroxystilbene derivative represented by formula (1) (wherein X-Xindependently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms; Zand Zindependently represent a hydrogen atom, or a group represented by the formula (2) (wherein Xand Xindependently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms); and Zand Zmay be the same as or different from each other; wherein X-Xmay be the same as or different from one another), which is characterized by heating a 4-hydroxycinnamic acid compound and a hydroxystilbene compound in the presence of a metal salt. 3. The process according to claim 2 , wherein the 4-hydroxycinnamic acid compounds are one or more kinds of compounds selected from a group consisting of p-coumaric acid claim 2 , ferulic acid claim 2 , caffeic acid claim 2 , sinapic acid claim 2 , di-t-butyl hydroxycinnamic acid compound claim 2 , and artepillin C.5. The process according to claim 4 , wherein the hydroxystilbenes are one or more kinds of compounds selected from a group consisting of resveratrol claim 4 , piceatannol claim 4 , and pterostilbene.6. The process according to claim 1 , wherein the 4-hydroxycinnamic acid compounds are one or more kinds of compounds selected from the group consisting of p-coumaric acid claim 1 , ferulic acid claim 1 , caffeic acid claim 1 , sinapic acid claim 1 , di-t-butyl hydroxycinnamic acid compound claim 1 , and artepillin C claim 1 , and the hydroxystilbenes are one or more kinds of compounds selected from the group consisting of resveratrol claim 1 , piceatannol claim 1 , and pterostilbene.13. The process according to claim 1 , comprising performing heat treatment at 90° C ...

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14-11-2013 дата публикации

ANTIOXIDANT, ANTIOXIDANT COMPOSTION AND PRODUCTION METHOD THEREFOR

Номер: US20130303629A1
Принадлежит:

Problem To provide an antioxidant, an antioxidant composition, and a method for producing the antioxidant and the antioxidant composition, which feature a high content rate and degree of extraction of substances. These substances are taurine, glycogen, protein, so-called blood platelet anticoagulant with zinc, fat-soluble vitamin with a high activation such as vitamin D, and other useful substances. The antioxidant and the antioxidant composition also feature a so-called antioxidative property, which has recently attracted attention. 1. An antioxidant , comprising 3 ,5-dihydroxy-4-methoxybenzyl alcohol.2. An antioxidant composition , comprising 3 ,5-dihydroxy-4-methoxybenzyl alcohol.3. An antioxidant constituted comprising 3 ,5-dihydroxy-4-methoxybenzyl alcohol contained in a product generated from an oyster meat.4. An oyster meat extract with an antioxidant , comprising 3 ,5-dihydroxy-4-methoxybenzyl alcohol contained in an extract extracted from an oyster meat.5. A method for producing an antioxidant composition , comprising:recovering a 3,5-dihydroxy-4-methoxybenzyl alcohol fraction from an oyster meat using ethyl acetate.6. A method for producing an antioxidant composition , comprisingrecovering a 3,5-dihydroxy-4-methoxybenzyl alcohol fraction from an oyster meat using ethyl acetate and ethanol.7. A method for producing an antioxidant composition , comprising:storing an oyster meat in an extraction container where an extraction solution is accumulated;collecting a solution with an oyster meat extract;adding ethyl acetate to the collected solution with an oyster meat extract; andrecovering a 3,5-dihydroxy-4-methoxybenzyl alcohol fraction.8. A method for producing an antioxidant composition , comprising:storing an oyster meat in an extraction container where an extraction solution is accumulated;collecting a solution with an oyster meat extract;adding ethyl acetate and ethanol to the collected solution with an oyster meat extract; andrecovering a 3,5-dihydroxy-4- ...

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21-11-2013 дата публикации

PROCESS FOR PRODUCTION OF PHENOLIC POLYMERIZABLE COMPOUND HAVING PHYSIOLOGICAL ACTIVITY

Номер: US20130310611A1
Принадлежит: UHA MIKAKUTO CO., LTD.

A process for producing a phenolic polymerizable compound represented by formula (1) or (2); wherein X-Xindependently represent a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, or a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms; Y represents a hydrogen atom, a hydroxy group, a saturated or unsaturated linear or branched alkoxy group having 1-10 carbon atoms, a saturated or unsaturated linear or branched alkyl group having 1-10 carbon atoms, or a group represented by formula (6); and Z represents a hydrogen atom or a group represented by formula (3), which is characterized by heating a 4-hydroxycinnamic acid compound in the presence of a metal salt. 3. The process according to claim 2 , wherein the 4-hydroxycinnamic acid compounds are one or more kinds of compounds selected from a group consisting of p-coumaric acid claim 2 , ferulic acid claim 2 , coffeic acid claim 2 , sinapic acid claim 2 , di-t-butyl hydroxycinnamic acid compound claim 2 , and artepillin C.10. The process according to claim 1 , comprising performing heat treatment at 90° C. to 150° C.11. An anticancer agent claim 1 , comprising a phenolic polymerizable compound produced by the process according to .12. An anticancer agent to oral cancer claim 1 , comprising a phenolic polymerizable compound produced by the process according to .13. A lipase inhibitor claim 1 , comprising a phenolic polymerizable compound produced by the process according to .14. An anti-obesity agent claim 1 , comprising a phenolic polymerizable compound produced by the process according to .15. A skin disease therapeutic agent claim 1 , comprising a phenolic polymerizable compound produced by the process according to .16. A food claim 1 , a pharmaceutical agent claim 1 , a quasi-drug claim 1 , or cosmetics claim 1 , comprising a phenolic polymerizable compound produced by the process according to . The present invention ...

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12-12-2013 дата публикации

Synthesis Of Treprostinil And Intermediates Useful Therein

Номер: US20130331593A1
Принадлежит: Alphora Research Inc.

Treprostinil is prepared by a process which involves Pauson-Khan cyclization of an an alkene-substituted, alkyne-substituted benzene corresponding to formula: (I) where PMB represents para-methoxy benzyl protecting group and Rand Rare alcohol protecting groups. Following cyclization, the resulting compound can be subjected to several chemical trans-formations followed by alkylation, hydrolysis and salt formation to yield treprostinil sodium. The use of para-methoxybenzyl group as the phenolic protecting group confers several process advantages that result in simplified purification of the final product and improved yields. 2. The process of wherein the carbon monoxide for intramolecular cyclization is used in the form of a Group VIII transition metal-carbon monoxide complex3. The process of wherein the carbon monoxide for intramolecular cyclization is used in the form of a cobalt-carbon monoxide complex.6. The process of any preceding claim including the additional claim 1 , subsequent step of removing the p-methoxy benzyl protecting group and the group R.8. The process of including the additional claim 7 , final step of converting the treprostinil so formed to its sodium salt.9. The process of or wherein the alkylation step (j) is conducted using an alkyl bromoalkanoate. This invention relates to a novel synthesis of the prostacyclin derivative treprostinil and intermediates useful in such syntheses.Prostacyclin derivatives are naturally occurring pharmaceutically active compounds, with a variety of pharmacological properties and utilities. A specific example of such prostacyclin derivative is treprostinil, which has the structural formula depicted below:Treprostinil sodium, under the trade name Remodulin is indicated for oral use in management of pulmonary arterial hypertension in human patients. Other salt forms are proposed for administration by inhalation.Treprostinil synthesis has previously been described in U.S. Pat. Nos. 6,700,025; 6,765,117; and 6,809,223; ...

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13-02-2014 дата публикации

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

Номер: US20140046074A1
Принадлежит:

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

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20-03-2014 дата публикации

Ortho-phenylphenol compounds

Номер: US20140081051A1
Принадлежит: Angus Chemical Co

A compound having formula (I), wherein G 1 represents a C 4 -C 22 alkyl or alkenyl group, a C 8 -C 20 aralkyl group or formula (II) wherein G 3 is a difunctional C 2 -C 18 alkyl or alkenyl group, a difunctional C 6 -C 20 aryl group or G 3 is absent; provided that G 1 is not 2-butyl, n-hexyl, n-octyl, n-dodecyl, n-hexadecyl or 2-phenylethyl.

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04-01-2018 дата публикации

BENZOCYCLOOCTENE-BASED AND INDENE-BASED ANTICANCER AGENTS

Номер: US20180002355A1
Принадлежит:

Benzocyclooctene (fused 6,8 ring system) analogues and corresponding indene (fused 6,5 ring system) analogues function as inhibitors of tubulin polymerization. The compounds are useful as anticancer agents in a new therapeutic approach for cancer treatment utilizing small-molecule inhibitors of tubulin polymerization that also act as vascular disrupting agents (VDAs). 4. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt or hydrate thereof claim 1 , and a pharmaceutically acceptable excipient claim 1 , adjuvant claim 1 , carrier claim 1 , buffer claim 1 , stabilizer claim 1 , or mixture thereof.5. A method of treating a vascular proliferative disorder in a subject comprising administering the pharmaceutical composition of to the subject.6. The method of claim 4 , further comprising administering one or more additional therapies to the subject in combination with the pharmaceutical composition of .7. The method of claim 5 , wherein the vascular proliferative disorder is cancer.8. A method of inhibiting tubulin polymerization in a subject comprising administering the pharmaceutical composition of to the subject.9. The method of claim 4 , further comprising administering one or more additional therapies to the subject in combination with the pharmaceutical composition of .12. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 10 , or a pharmaceutically acceptable salt or hydrate thereof claim 10 , and a pharmaceutically acceptable excipient claim 10 , adjuvant claim 10 , carrier claim 10 , buffer claim 10 , stabilizer claim 10 , or mixture thereof.13. A method of treating a vascular proliferative disorder in a subject comprising administering the pharmaceutical composition of to the subject.14. The method of claim 12 , further comprising administering one or more additional therapies to the subject in combination with the ...

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20-01-2022 дата публикации

BENZHYDRYLATED AROMATIC SURFACTANTS

Номер: US20220017444A1
Принадлежит:

The present disclosure provides an alkoxylate compound containing aromatic groups in the hydrophobe allowing the compound to exhibit unique functionality, high performance and low cost, but without the toxicity and/or skin and eye irritation problems associated with conventional alkylphenol and mono-, di- and tristyrylphenol compounds. 2. The benzyhydrylated alkoxylate of claim 1 , wherein Z is oxygen and n is 1.3. The benzyhydrylated alkoxylate of claim 1 , wherein Z is oxygen and n is 2.4. The benzhydrylated alkoxylate of claim 1 , wherein Z is nitrogen.5. The benzhydrylated alkoxylate of claim 1 , wherein each Ris hydrogen.6. The benzhydrylated alkoxylate of claim 1 , wherein each Ris hydrogen.9. A method for preparing the benzyhydrylated alkoxylate of comprising the steps of: reacting a benzhydrol with an aromatic compound selected from phenol optionally substituted with an alkyl group claim 1 , a phenyl group or combination thereof claim 1 , a bisphenol claim 1 , a benzenediol optionally substituted with an alkyl group claim 1 , naphthol claim 1 , thiophenol and aniline optionally substituted with an alkyl group in the presence of an acid catalyst to form a benzhydrylated hydrophobe; and claim 1 , alkoxylating the benzyhydrylated hydrophobe with an alkylene oxide to form the benzhydrylated alkoxylate.10. The method of claim 9 , wherein the method further comprises the step of reacting the benzhydrylated alkoxylate with an acidic moiety and optionally neutralizing with a source of alkali metal claim 9 , alkaline earth metal claim 9 , amine or ammonia.11. A composition comprising the benzyhydrylated alkoxylate of and a solvent.12. A packaged product comprising: a) a container having at least an outlet; and b) the composition of .13. A concentrate composition comprising from about 50% by weight to about 99.5% by weight of the benzhydrylated alkoxylate of and from about 0.5% by weight to about 50% by weight of water and optionally one or more additives claim 1 , ...

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12-01-2017 дата публикации

BRANCHED CHAIN-CONTAINING AROMATIC COMPOUND

Номер: US20170008922A1
Автор: TAKAHASHI Daisuke
Принадлежит: AJINOMOTO CO., INC.

The present invention provides a particular branched chain-containing aromatic compound. The branched chain-containing aromatic compound of the present invention is easily-soluble in isopropyl acetate superior in liquid-separation operability, and can be used for a production method of peptide and the like, which provides a final product simply by extraction separation, without crystallization and isolation of each intermediate in each step. 125-. (canceled)2831-. (canceled) The present invention relates to an aromatic compound containing a particular branched chain. The present invention further relates to a protecting reagent containing the compound or an adduct thereof. The present invention also relates to a production method of peptide by using the compound, and further relates to an organic synthesis method including the production method of the peptide.The production methods of peptide are generally divided into solid phase methods and liquid phase methods. The solid phase methods are advantageous since isolation and purification after reaction can be performed by only washing resin. However, they are associated with problems in that the reaction is essentially that of heterogeneous phases, reaction agents and reagents need to be used in excess to compensate for the low reactivity, and tracing of reaction and analysis of reaction product supported by carrier are difficult. On the other hand, the liquid phase method is advantage since it shows good reactivity, and intermediate peptide can be purified by extraction and washing, isolation and the like after condensation reaction. However, the method is associated with problems since the production step is complicated due to an extraction and washing step with a nonpolar organic solvent and an acidic or basic aqueous solution to remove residual reagents and/or byproducts in each step of coupling reaction and deprotection, and/or an isolation and purification step such as crystallization and the like, and the like ...

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11-01-2018 дата публикации

FLUORINE-CONTAINING ETHER COMPOUND, LUBRICANT FOR MAGNETIC RECORDING MEDIUM, AND MAGNETIC RECORDING MEDIUM

Номер: US20180009773A1
Принадлежит: SHOWA DENKO K.K.

This fluorine-containing ether compound is represented by Formula (1). 1. A fluorine-containing ether compound represented by Formula (1) ,{'br': None, 'sup': 1', '2', '3', '4', '5, 'sub': 2', '2, 'R—R—CH—R—CH—R—R\u2003\u2003(1)'}{'sup': 1', '2', '3', '4', '5, '(in Formula (1), Ris an aryl group or an aralkyl group, Ris a divalent linking group having 0 or 1 polar group, Ris a perfluoropolyether chain, Ris a divalent linking group having 2 or 3 polar groups, and Ris an aryl group or an aralkyl group.)'}2. The fluorine-containing ether compound according to claim 1 ,{'sup': 2', '4, 'wherein at least one of the polar groups in the polar groups included in Rand Rof Formula (1) is a hydroxyl group.'}3. The fluorine-containing ether compound according to claim 1 ,{'sup': 2', '4, 'wherein the polar groups included in Rand Rof Formula (1) are all hydroxyl groups.'}6. The fluorine-containing ether compound according to claim 1 ,{'sup': '1', 'wherein Rin Formula (1) is any one selected from a benzene ring group which may have a substituent, a naphthalene ring group which may have a substituent, a benzyl group which may have a substituent, or a naphthylmethyl group which may have a substituent.'}8. The fluorine-containing ether compound according to claim 1 ,{'sup': 4', '5, 'sub': 2', '2', 'z, 'wherein Rin Formula (1) has —(CH—CH—O)—O— (z in the formula represents an integer of 1 to 3) at an end on the Rside.'}9. The fluorine-containing ether compound according to claim 1 ,{'sup': '5', 'wherein Rin Formula (1) is any one selected from a benzene ring group which may have a substituent, a naphthalene ring group which may have a substituent, a benzyl group which may have a substituent, or a naphthylmethyl group which may have a substituent.'}13. The fluorine-containing ether compound according to claim 1 ,wherein a number-average molecular weight is in a range of 500 to 10,000.14. A lubricant for a magnetic recording medium claim 1 , comprising:{'claim-ref': {'@idref': 'CLM- ...

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14-01-2016 дата публикации

ELECTROCHEMICAL COUPLING OF TWO PHENOLS WHICH DIFFER IN THEIR OXIDATION POTENTIAL

Номер: US20160010225A1
Принадлежит: EVONIK DEGUSSA GmbH

Electrochemical process for coupling two phenols of different oxidation potential, and novel biphenols which can be prepared by this electrochemical coupling. 2. Compound according to claim 1 ,{'sup': 2', '3', '4', '5', '6', '7', '10', '11', '12', '13', '14', '16', '18', '19', '20', '21', '24, 'where R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rare selected from: —H, -alkyl.'}3. Compound according to claim 1 ,{'sup': 4', '5, 'where Rand Rare —H.'}4. Compound according to claim 1 ,{'sup': 3', '6, 'where Rand Rare -alkyl.'}5. Compound according to claim 1 ,{'sup': '11', 'where Ris —O-alkyl.'}6. Compound according to claim 1 ,{'sup': '13', 'where Ris -alkyl.'}7. Compound according to claim 1 ,{'sup': '19', 'where Ris -alkyl.'}8. Electrochemical process for preparing biphenols claim 1 , comprising the process steps of:a) introducing a solvent or solvent mixture and a conductive salt into a reaction vessel,{'sub': 'Ox', 'b) adding a first phenol having an oxidation potential IE1I to the reaction vessel,'}{'sub': Ox', 'Ox', 'Ox', 'Ox', 'Ox, 'c) adding a second phenol having an oxidation potential IE2I to the reaction vessel, where: IE2I>IE1I and IE2I−IE1I=IΔEI, the second phenol being added in excess relative to the first phenol,'}and the solvent or solvent mixture being selected such that IΔEI is in the range from 10 mV to 450 mV,d) introducing two electrodes into the reaction solution,e) applying a voltage to the electrodes,f) coupling the first phenol to the second phenol to give a biphenol.9. Process according to claim 8 ,wherein the second phenol is used at least in twice the amount relative to the first phenol.10. Process according to claim 8 ,wherein the ratio of first phenol to the second phenol is in the range from 1:2 to 1:4.11. Process according to claim 8 ,wherein either the first phenol the second phenol has an —O-alkyl group.12. Process according to claim 8 ,wherein the solvent or solvent mixture is selected such that IΔEI is in the range from 20 mV to ...

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08-01-2015 дата публикации

EMULSIFIER FOR EMULSION POLYMERIZATION

Номер: US20150011790A1
Принадлежит:

An emulsifier for emulsion polymerization contains a compound represented by the following general formula (I). 2. (canceled)3. The emulsifier for emulsion polymerization according to claim 1 , wherein in the general formula (I) claim 1 , X represents a hydrogen atom or SOM claim 1 , wherein M represents a hydrogen atom claim 1 , an alkali metal atom claim 1 , an alkaline earth metal atom claim 1 , an ammonium residue claim 1 , or an alkanolamine residue claim 1 , and A represents an alkylene group having 2 carbon atoms. The present invention relates to an emulsifier to be used in an emulsion polymerization step, more particularly relates to an emulsifier for emulsion polymerization, which can enhance the stability of a polymer dispersion, and also enhance the physical properties of a polymer film obtained from the polymer dispersion.Heretofore, as emulsifiers for emulsion polymerization, anionic surfactants such as soaps, sodium dodecylbenzene sulfonate, polyoxyethylene alkyl phenyl ether sulfate ester salts, and polyoxyethylene alkyl ether sulfate ester salts; and nonionic surfactants such as polyoxyethylene nonyl phenyl ethers and polyoxyethylene alkyl ethers have been used. However, a polymer film obtained from a polymer dispersion using any of the above emulsifiers has problems that the emulsifier used remains in a free form in the polymer film, and therefore, the water resistance and the adhesiveness of the film are poor, etc. Therefore, as measures for the problems, a lot of reactive emulsifiers having a copolymerizable unsaturated group have been proposed (for example, PTL 1 to PTL 3).A reactive emulsifier having an acrylic group or a methacrylic group as a copolymerizable unsaturated group, which has been proposed in the prior art, has high copolymerizability with a monomer, but has a problem that the polymerization stability during emulsion polymerization is deteriorated. For example, agglomerates during emulsion polymerization are increased, particles ...

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08-01-2015 дата публикации

HIGH-YIELD SYNTHESIS OF P-(BENZYLOXY)CALIX[6, 7,8]ARENES

Номер: US20150011798A1
Принадлежит: UNIVERSITE PARIS-SUD XI

The high-yield synthesis of p-(benzyloxy)calix[6,7,8]arenes by bringing caesium hydroxide into contact with p-(benzyloxy)phenol and paraformaldehyde, and composite materials including these p-(benzyloxy)calix[6,7,8]arenes. 1. Process for the preparation of a compound consisting of a mixture comprising p-(benzyloxy)calix[6]arene and p-(benzyloxy)calix[7]arene , or a compound consisting of p-(benzyloxy)calix[6]arene or p-(benzyloxy)calix[7]arene comprising a stage of bringing caesium hydroxide into contact with p-(benzyloxy)phenol and paraformaldehyde , said base being at a total concentration of 0.09 equivalent to 0.5 equivalent with respect to said p-(benzyloxy)phenol.2. Process according to claim 1 , in which said base is at a total concentration comprised from 0.09 to 0.2 equivalent claim 1 , in particular 0.15 equivalent in order to obtain a mixture comprising p-(benzyloxy)calix[6]arene and p-(benzyloxy)calix[7]arene in the salified form.3. Process according to claim 2 , comprising an additional stage of filtration of the mixture comprising p-(benzyloxy)calix[6]arene and p-(benzyloxy)calix[7]arene in the salified form claim 2 , in order to obtain p-(benzyloxy)calix[7]arene in the form of a caesium monosalt followed by an additional stage of neutralization of p-(benzyloxy)calix[7]arene in the form of a caesium monosalt in order to obtain p-(benzyloxy)calix[7]arene in the neutralized form.4. Process according to claim 3 , comprising the following stages:a. bringing caesium hydroxide at a concentration from 0.09 to 0.2 equivalent, in particular 0.15 equivalent, into contact with p-(benzyloxy)phenol and paraformaldehyde in a solvent, then heating in order to obtain a mixture comprising p-(benzyloxy)calix[6]arene and p-(benzyloxy)calix[7]arene in the salified form,b. neutralization of the mixture comprising p-(benzyloxy)calix[6]arene and p-(benzyloxy)calix[7]arene in the salified form with an acid, in order to obtain a mixture comprising p-(benzyloxy)calix[6]arene and ...

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18-01-2018 дата публикации

Pro-fragrance compounds

Номер: US20180016521A1
Принадлежит: FIRMENICH SA

Precursor or pro-fragrance compounds used as a precursor to deliver at least one fragrant compound that is capable of imparting an odor, in particular one which imparts an odor to a material, more particularly to a fabric or textile. The pro-fragrant compounds of the invention include fragrant alcohols (R 1 OH) released from a compound of Formula I or in which Formula I is derived from (R 1 OH) and encompass any fragrant alcohol having more than three carbon atoms. Also, methods of generating the fragrant compounds and to improve, enhance or modify odoriferous properties of a perfuming composition or a perfumed article are also disclosed, as are the resultant perfuming compositions and articles.

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21-01-2016 дата публикации

ELECTROCHEMICAL COUPLING OF A PHENOL TO A NAPHTHOL

Номер: US20160017505A1
Принадлежит: EVONIK DEGUSSA GMBH

The invention relates to an electrochemical method for the selective coupling of a phenol to a naphthol which differ in their oxidation potential. The invention also relates to compounds which can be produced by electrochemical coupling. 2. Compound according to claim 1 , where R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rare selected from: —H claim 1 , -alkyl.3. Compound according to claim 1 , where Rand Rare -alkyl.4. Compound according to claim 1 , where Ris -alkyl.5. Compound according to claim 1 , where R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rare —H.6. Compound according to claim 1 , where R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rare —H.7. Electrochemical process comprising the process steps of:a) introducing a solvent or solvent mixture and a conductive salt into a reaction vessel,{'sub': 'Ox', 'b) adding a phenol having an oxidation potential |E1| to the reaction vessel,'}{'sub': 'Ox', 'c) adding a naphthol having an oxidation potential |E2| to the reaction vessel, the substance having the higher oxidation potential being added in excess, and'}{'sub': Ox', 'Ox, 'where: |E1|−|E2|=|ΔE| and'}the solvent or solvent mixture is selected such that |ΔE| is in the range from 10 to 450 mV,d) introducing two electrodes into the reaction solution,e) applying a voltage to the electrodes,f) coupling the phenol to the naphthol to give a cross-coupled product.8. Process according to claim 7 , wherein the substance having the higher oxidation potential is used at least in twice the amount relative to the substance having the lower ...

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15-01-2015 дата публикации

TUBULIN BINDING AGENTS

Номер: US20150018566A1
Принадлежит:

The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene. The second substituent on the B ring may for example be a substituent which has been found to provide enhanced tubulin binding activity (for example a carbonyl group), or may be a substituent that facilitates functionalisation of the B ring (for example an hydroxyl or amine group), or it may be a binding agent for a target that is preferentially expressed on vasculature undergoing angiogenesis, and not expressed on quiescent vasculature. 143-. (canceled)45. A compound of in which at least one of X claim 44 , Y and Z is C═O.46. A compound of in which Rand Rare each independently selected from H and a halogen.47. A compound of in which Rand Rare each claim 44 , independently claim 44 , selected from H claim 44 , OH claim 44 , amino and L(W).48. A compound according to in which Rand Rare each claim 44 , independently claim 44 , selected from H claim 44 , NH claim 44 , lower alkoxy claim 44 , alkylthio and OH.49. A compound according to in which Ris a lower alkoxy group in the para position.50. A compound according to in which Rand Rare each independently selected from H and a halogen claim 44 , Rand Rare each claim 44 , independently claim 44 , selected from OH claim 44 , amino and L(W) claim 44 , and Rand Rare each claim 44 , independently claim 44 , ...

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21-01-2016 дата публикации

Compound for forming organic film, and organic film composition using the same, process for forming organic film, and patterning process

Номер: US20160018735A1
Принадлежит: Shin Etsu Chemical Co Ltd

The invention provides a compound for forming an organic film having a partial structure represented by the following formula (vii-2), wherein R 1 represents a linear, branched or cyclic monovalent hydrocarbon group having 1 to 20 carbon atoms, and a methylene group constituting R 1 may be substituted by an oxygen atom; a+b is 1, 2 or 3; c and d are each independently 0, 1 or 2; x represents 0 or 1, when x=0, then a=c=0; L 7 represents a linear, branched or cyclic divalent organic group having 1 to 20 carbon atoms, L 8′ represents the partial structure represented by the following formula (i), 0≦o<1, 0<p≦1 and o+p=1, wherein the ring structures Ar3 represent a substituted or unsubstituted benzene ring or naphthalene ring; R 0 represents a hydrogen atom or a linear, branched or cyclic monovalent organic group having 1 to 30 carbon atoms; and L 0 represents a divalent organic group. There can be provided an organic film composition for forming an organic film having high dry etching resistance as well as advanced filling/planarizing characteristics.

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16-01-2020 дата публикации

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

Номер: US20200017433A1
Принадлежит: EMORY UNIVERSITY

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

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28-01-2016 дата публикации

6-HYDROXY-2-NAPHTHALENYL FLUORENE DERIVATIVES AND LENS AND CAMERA MODULE USING THE SAME

Номер: US20160023978A1
Принадлежит: SAMSUNG ELECTRO-MECHANICS CO., LTD.

Disclosed herein are 6-hydroxy-2-naphthalenyl fluorene derivatives and a lens and a camera module using the same. 2. The 6-hydroxy-2-naphthalenyl fluorene derivative according to claim 1 , wherein Ar is selected from the group consisting of a phenyl group claim 1 , a naphthyl group claim 1 , a biphenyl group claim 1 , an anthryl group claim 1 , and a phenanthryl group. This application claims the benefit under 35 U.S.C. Section [120, 119, 119(e)] of Korean Patent Application Serial Nos. 10-2014-0095904 and 10-2014-0137440, entitled “6-Hydroxy-2-naphthalenyl Fluorene Derivatives and Lens and Camera Module Using the Same” filed on Jul. 28, 2014 and Oct. 13, 2014, which are hereby incorporated by reference in their entirety into this application.1. Technical FieldThe present disclosure relates to 6-hydroxy-2-naphthalenyl fluorene derivatives and a lens and a camera module using the same.2. Description of the Related ArtAn optical glass or optical transparent resin has been used as a material of an optical element used in optical systems of various cameras such as a camera for a smart phone, a video camera, and the like.There are various kinds of optical glasses having excellent heat resistance, transparency, dimensional stability, chemical resistance, or the like, and having various refractive indexes (nD) or Abbe's numbers (uD), but there are problems such as an expensive material, poor formability, and low productivity. Particularly, since a significantly high technology and a high cost are required in order to process the optical glass into an aspheric lens used in aberration correction, there are various limitations in actually using the optical glass.Meanwhile, an optical lens made of an optical transparent resin, particularly, a thermoplastic transparent resin may be mass-produced by molding injection and easily manufactured in an aspheric lens form, such that the optical lens has been used as a camera lens.A resin composition having a fluorene compound as a ...

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22-01-2015 дата публикации

Fluorene derivatives and lens using the same

Номер: US20150025215A1
Принадлежит:

Disclosed herein are fluorene derivatives and a lens using the same. 2. The fluorene derivative of claim 1 , wherein Ar is a phenyl group.3. The fluorene derivative of claim 1 , wherein Ar is a naphthyl group.4. The fluorene derivative of claim 1 , wherein Ar is a biphenyl group.5. The fluorene derivative of claim 1 , wherein Ar is an anthryl group.6. The fluorene derivative of claim 1 , wherein Ar is a phenanthryl group.14. A lens comprising the copolymer of .15. The copolymer of claim 13 , wherein the copolymer is a copolymer of two or more dicarboxylic acids.16. The copolymer of claim 13 , wherein the copolymer is a copolymer of phosgene. This application is a continuation of U.S. patent application Ser. No. 14/288,368, filed on May 27, 2014, entitled “Fluorene derivatives and lens using the same,” which claims priority to Korean Patent Application No. 10-2013-0060651, filed on May 28, 2013, entitled “Fluorene Derivatives and Lens Using the Same”, to and Korean Patent Application No. 10-2014-0057361, filed on May 13, 2014, entitled “Fluorene Derivatives and Lens Using the Same”, all of which are hereby incorporated by reference in their entireties into this application.1. Technical FieldEmbodiments of the present invention relate to fluorene derivatives and relate to lenses using the same.2. BackgroundOptical glass and transparent optical resin can be used as a material for an optical element in optical systems of various kinds including cameras, such as cameras for smart phones, video cameras, and the like.Various kinds of materials can be used for optical glass, such as those having favorable heat resistance, transparency, dimensional stability, and chemical resistance, and the like. Materials can have various refractive indexes (nD) or abbe numbers (uD), but some materials can be expensive and can have low formability and low productivity. In some cases, such as some cases where the glass is used for an aspheric lens used in aberration correction, a ...

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22-01-2015 дата публикации

AROMATIC POLYACETALS AND ARTICLES COMPRISING THEM

Номер: US20150025278A1
Принадлежит:

A polymer includes repeat units having the structure 2. The polymer of claim 1 , wherein claim 1 , in at least one repeat unit claim 1 , at least one of Ar claim 1 , Arand Aris substituted with at least one hydroxyl.3. The polymer of claim 1 , wherein each occurrence of Ar claim 1 , Ar claim 1 , and Aris independently 1 claim 1 ,3-phenylene or 1 claim 1 ,4-phenylene.4. The polymer of claim 1 , wherein Arand Arare not further covalently linked with one another to form a ring structure that includes —Ar—O—C—O—Ar—.5. The polymer claim 1 , wherein{'sup': '1', 'each occurrence of Ris hydrogen; and'}{'sup': '2', 'each occurrence of Ris unsubstituted or substituted phenyl.'}9. The polymer of claim 1 , wherein{'sup': 1', '2, 'each occurrence of Arand Aris 1,4-phenylene;'}{'sup': 3', '3, 'each occurrence of Aris unsubstituted or substituted 1,3-phenylene, wherein, in at least 40 mole percent of the plurality of repeat units, Aris substituted with at least one hydroxyl;'}{'sup': '1', 'each occurrence of Ris hydrogen; and'}{'sup': '2', 'each occurrence of Ris phenyl.'}10. An article comprising the polymer of . The present invention relates to polymers, in particular aromatic polyacetals and polyketals.Poly(methacrylate)-based and poly(hydroxystyrene)-based chemically amplified photoresists have reached a performance limit that is defined by a trade-off triangle of resolution, line edge roughness, and sensitivity. This is the so-called RLS trade-off. There is empirical evidence that attempts to increase one of the key properties by using a formulation approach hurt the remaining properties of the triangle. This effect limits the achievable feature size in high resolution photolithography, including extreme ultraviolet (EUV) and electron beam. One way to escape the RLS trade-off triangle of poly(methacrylate)-based and poly(hydroxystyrene)-based chemically amplified photoresists would be to create new photoresist compositions based on a different polymer that provides one or ...

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28-01-2016 дата публикации

COMPOUND FOR FORMING ORGANIC FILM, AND ORGANIC FILM COMPOSITION USING THE SAME, PROCESS FOR FORMING ORGANIC FILM, AND PATTERNING PROCESS

Номер: US20160027653A1
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

The invention provides a compound for forming an organic film having a partial structure represented by the following formula (ii), 10. The organic film composition according to claim 9 , wherein the composition contains (D) a resin containing an aromatic ring which is different from the polymers (C-1) to (C-4).11. The organic film composition according to claim 10 , wherein (D) the resin containing an aromatic ring contains a naphthalene ring.14. The organic film composition according to claim 9 , wherein the composition further comprises at least one of (E) a compound containing a phenolic hydroxyl group claim 9 , (F) an acid generator claim 9 , (G) a cross-linking agent claim 9 , (H) a surfactant and (I) an organic solvent.15. The organic film composition according to claim 9 , wherein it is used as a resist underlayer film composition or a planarizing composition for manufacturing a semiconductor apparatus.16. A process for forming an organic film which acts as a resist underlayer film or a planarizing film for manufacturing a semiconductor apparatus of a multilayer resist film used in lithography claim 9 , which comprises coating the organic film composition according to on a substrate to be processed claim 9 , and subjecting the composition to heat treatment at a temperature of 100° C. or higher and 600° C. or lower for 10 seconds to 600 seconds to form a cured film.17. A process for forming an organic film which acts as a resist underlayer film or a planarizing film for manufacturing a semiconductor apparatus of a multilayer resist film used in lithography claim 15 , which comprises coating the organic film composition according to on a substrate to be processed claim 15 , and subjecting the composition to heat treatment at a temperature of 100° C. or higher and 600° C. or lower for 10 seconds to 600 seconds to form a cured film.18. A process for forming an organic film which acts as a resist underlayer film or a planarizing film for manufacturing a ...

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01-02-2018 дата публикации

IONONE STABILISERS FOR NITROCELLULOSE-BASED PROPELLANTS

Номер: US20180029951A1
Принадлежит: PB CLERMONT SA

The present disclosure is directed to a nitrocellulose-based propellant composition comprising: (a) a nitrate ester-based propellant comprising nitrocellulose; and (b) a stabiliser comprising a non-aromatic compound (12) consisting of a general ionone formula (12-I), (12-II), (12-III) or (12-IV): 2. The propellant composition according to claim 1 , wherein the nitrate ester-based propellant consists of nitrocellulose alone as a single base or of a mixture comprising nitrocellulose in combination with at least a blasting oil and/or at least one energetic additive as a double or higher base.3. The propellant composition according to claim 1 , wherein the non-aromatic compound is a substance capable of reacting by H-abstraction with radical groups formed by degradation of the nitrate ester to form a first by-product capable of further reacting with NOx and/or alkoxy groups formed by degradation of the nitrate ester to form a second by-product comprising no NNO groups.4. The propellant composition according to claim 3 , wherein the second by-product is capable of reaction with radical groups formed by degradation of the nitrate ester for forming third and subsequent by-products capable of reacting with such radical alkoxy groups or with NOx.5. The propellant composition according to claim 2 , wherein the blasting oil comprises at least a nitrated polyol obtainable by nitration of polyol selected from a group consisting of glycerol claim 2 , glycol claim 2 , diethylene glycol claim 2 , triethylene glycol and metriol claim 2 , and wherein the at least one energetic additive is an energetic plasticizer selected from the group of nitramines claim 2 , including butyl-NENA claim 2 , dinitrodiazaalkane (DNDA) claim 2 , or is an explosive comprising RDX claim 2 , HMX claim 2 , FOX-7 claim 2 , FOX-12 claim 2 , CL20.7. The propellant composition according to claim 1 , wherein the non-aromatic compound is present in the composition in an amount comprised between 0.1 and 5.0 wt. % ...

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01-02-2018 дата публикации

COMPOUND, RESIN, MATERIAL FOR FORMING UNDERLAYER FILM FOR LITHOGRAPHY, COMPOSITION FOR FORMING UNDERLAYER FILM FOR LITHOGRAPHY, UNDERLAYER FILM FOR LITHOGRAPHY, RESIST PATTERN FORMING METHOD, CIRCUIT PATTERN FORMING METHOD, AND PURIFICATION METHOD OF COMPOUND OR RESIN

Номер: US20180029968A1
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

A compound represented by the following formula (1). 2. The compound according to claim 1 , wherein at least one Rand/or at least one Rrepresents an alkoxy group having 1 to 30 carbon atoms.6. A resin obtained with the compound according to as a monomer.7. The resin according to claim 6 , which is obtained by a reaction of the compound with a compound having crosslinking reactivity.8. The resin according to claim 7 , wherein the compound having crosslinking reactivity is at least one selected from the group consisting of aldehyde claim 7 , ketone claim 7 , carboxylic acid claim 7 , carboxylic halide claim 7 , a halogen-containing compound claim 7 , an amino compound claim 7 , an imino compound claim 7 , isocyanate and an unsaturated hydrocarbon group-containing compound.10. A material for forming an underlayer film for lithography claim 1 , comprising the compound according to .11. A composition for forming an underlayer film for lithography claim 10 , comprising the material for forming an underlayer film for lithography according to claim 10 , and a solvent.12. The composition for forming an underlayer film for lithography according to claim 11 , further comprising a crosslinking agent.13. The composition for forming an underlayer film for lithography according to claim 11 , further comprising an acid generator.14. An underlayer film for lithography claim 11 , formed from the composition for forming an underlayer film for lithography according to .15. A resist pattern forming method claim 11 , comprising forming an underlayer film on a substrate by using the composition for forming an underlayer film according to claim 11 , forming at least one photoresist layer on the underlayer film claim 11 , thereafter irradiating a required region of the photoresist layer with radiation claim 11 , and developing it.16. A circuit pattern forming method claim 11 , comprising forming an underlayer film on a substrate by using the composition for forming an underlayer film ...

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01-02-2018 дата публикации

Phenolate Transition Metal Complexes, Production and Use Thereof

Номер: US20180030167A1
Принадлежит:

Phenolate ligands and transition metal complexes are disclosed for use in alkene polymerization, with optional chain transfer agent, to produce polyolefins. 4. The transition metal complex of claim 2 , wherein Rand Rare carbazolyl claim 2 , substituted carbazolyl claim 2 , indolyl claim 2 , substituted indolyl claim 2 , indolinyl claim 2 , substituted indolinyl claim 2 , imidazolyl claim 2 , substituted imidazolyl claim 2 , indenyl claim 2 , substituted indenyl claim 2 , indanyl claim 2 , substituted indanyl claim 2 , fluorenyl claim 2 , or substituted fluorenyl claim 2 , preferably Rand Rare the same.5. The transition metal complex of claim 2 , wherein Q is a neutral donor group comprising at least one atom from Group 15 or Group 16 and the -(-Q-R-Q-)- fragment can form a substituted or unsubstituted heterocycle which may or may not be aromatic and may have multiple fused rings.6. The transition metal complex of claim 2 , wherein each R claim 2 , R claim 2 , R claim 2 , R claim 2 , R claim 2 , R claim 2 , R claim 2 , and Ris independently a hydrogen claim 2 , a C-Chydrocarbyl radical claim 2 , a substituted hydrocarbyl radical claim 2 , a heteroatom claim 2 , or a heteroatom-containing group claim 2 , or may independently form a Cto Ccyclic or polycyclic ring structure with R claim 2 , R claim 2 , or R claim 2 , or a combination thereof.7. The transition metal complex of claim 2 , wherein M is Hf or Zr.8. The transition metal complex of claim 2 , wherein Q is O claim 2 , N claim 2 , S claim 2 , or P.9. The transition metal complex of claim 2 , wherein Rand Rare carbazolyl or substituted carbazolyl.10. The transition metal complex of claim 2 , wherein Ris a divalent C-Chydrocarbyl radical or divalent substituted hydrocarbyl radical comprising a portion that comprises a linker backbone comprising from 1 to 18 carbon atoms linking or bridging between the two Q groups.11. A catalyst system comprising activator and the complex of .12. The catalyst system of claim 11 , ...

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31-01-2019 дата публикации

TETRAHYDRONAPHTHALENE DERIVATIVE

Номер: US20190031605A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

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

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31-01-2019 дата публикации

PROCESS FOR PREPARING BIPHENYL COMPOUNDS

Номер: US20190032098A1
Принадлежит:

A process is provided for preparing a compound having the formula (I): 2. The process of claim 1 , wherein the water-miscible solvent is acetone.3Trametes versicolor.. The process of claim 1 , wherein the laccase is from4. The process of claim 1 , wherein the amount of laccase for one gram of compound of formula (II) is from 1.5 mg to 75 mg.5. The process of claim 1 , wherein the solution of the compound of formula (II) in a water-miscible solvent is prepared by adding said compound of formula (II) in said water-miscible solvent claim 1 , and adding a buffer solution.6. The process according to claim 5 , wherein the amount of water-miscible solvent is comprised between 5% and 10% of volume in comparison with the total volume of the mixture formed by said solvent and the buffer solution.7. The process of claim 1 , wherein the addition of an oxygen source according to a) is carried out for a sufficient time to saturate the solution in dissolved oxygen.8. The process of claim 1 , wherein the solution of the compound of formula (II) in the water-miscible solvent used for b) is saturated in oxygen.9. The process of claim 1 , wherein the pH of the solution of the compound of formula (II) in the water-miscible solvent is comprised between 4 and 7.10. The process of claim 1 , wherein step c) is a step of recovering the compound of formula (I) by centrifugation or filtration.11. The process of claim 1 , wherein the amount of laccase for one gram of compound of formula (II) is from 3 mg to 15 mg.12. The process of claim 5 , wherein the buffer solution is a sodium acetate buffer.13. The process of claim 7 , wherein the addition of an oxygen source according to step a) is carried out for 5 minutes. This application is a continuation of U.S. patent application Ser. No. 15/516,318, filed Mar. 31, 2017, which is a 371 application of International Application PCT/EP2015/072957, filed Oct. 5, 2015, and which claims the benefit of European Patent Office application Serial No. ...

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04-02-2021 дата публикации

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

Номер: US20210032198A1
Принадлежит:

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

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09-02-2017 дата публикации

NITRIFICATION INHIBITORS

Номер: US20170036969A1
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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08-02-2018 дата публикации

Myricanol Derivatives and Uses Thereof for Treatment of Neurodegenerative Diseases

Номер: US20180037529A1
Принадлежит:

The subject invention pertains to myricanol derivatives, therapeutic compositions, and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau. 2. A compound according to claim 1 , having a chemical structure of formula A.3. A compound according to claim 1 , having a chemical structure of formula B.4. A compound according to claim 1 , having a chemical structure of formula C.7. A pharmaceutical composition comprising a compound of .8. A pharmaceutical composition comprising a compound of .9. A pharmaceutical composition comprising a compound of .11. The method according to claim 10 , wherein the compound has a chemical structure of formula G.12. The method according to claim 10 , wherein the compound has a chemical structure of formula B.13. The method according to claim 10 , wherein the compound has a chemical structure of formula H.16. The method according to claim 10 , wherein the cells are in a subject in need of treatment for a neurodegenerative disease.17. The method of claim 16 , wherein the neurodegenerative disease is a tauopathy.18. The method of claim 17 , wherein the subject is a human.19. The method of claim 18 , wherein the neurodegenerative disease is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , frontotemporal dementia claim 18 , frontotemporal dementia with Parkinsonism claim 18 , frontotemporal lobe dementia claim 18 , pallidopontonigral degeneration claim 18 , progressive supranuclear palsy claim 18 , multiple system tauopathy claim 18 , multiple system tauopathy with presenile dementia claim 18 , Wilhelmsen-Lynch disease claim 18 , Pick's disease claim 18 , or Pick's disease-like dementia.20. The method of claim 19 , wherein the neurodegenerative disease is Alzheimer's disease. This application is a continuation of U.S. application Ser. No. 14/390,960, filed Oct. 6, 2014; which is the U.S. national stage application of ...

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24-02-2022 дата публикации

NEBIVOLOL SYNTHESIS METHOD AND INTERMEDIATE COMPOUND THEREOF

Номер: US20220056003A1
Автор: Zheng Zhiguo
Принадлежит:

The present invention relates to a nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound. 2. The process according to for preparation of the compound of formula VIII (R*/R*).3. (canceled)4. (canceled)5. (canceled)714-. (canceled)1641-. (canceled)43. A The compound of formula IV1′ according to .44. The compound of formula IV2′ according to .45. The compound of formula V′ (2R* claim 42 ,3R*) according to .46. The compound of formula VI′ (2R* claim 42 ,3S*) according to .47. The compound of formula XI′ according to .48. The compound of formula XII′ according to .49. The compound of formula XVI′ according to .50. A compound according to claim 42 , wherein the compound is selected from the group consisting of:1-benzyloxy-2-bromomethyl-4-fluorobenzene,4-[(2-benzyloxy-5-fluorophenyl)-butyn-1-yl]trimethylsilane,1-(benzyloxy)-2-(butyn-3-yl)-4-fluorobenzene,5-[2-(benzyloxy)-5-fluorophenyl]pent-2-yne-1-ol,trans-5-[2-(benzyloxy)-5-fluorophenyl]pent-2-ene-1-ol,(2R*,3R*)-3-[2-(benzyloxy)-5-fluorophenethyl]-2-hydroxymethyl-oxacyclopropane,1-[6-fluoro-(2S*)-3,4-dihydro-2H-benzopyran-2-yl]-(1R*)-1,2-ethylene glycol,cis-5-[2-(benzyloxy)-5-fluorophenyl]pent-2-ene-1-ol,(2R*,3S*)-3-[2-(benzyloxy)-5-fluorophenethyl]-2-hydroxymethyl-oxacyclopropane,1-[6-fluoro-(2R*)-3,4-dihydro-2H-benzopyran-2-yl]-(1R*)-1,2-ethylene glycol,(S*,R*)-(+/−)-α-[(p-tolylsulfonyloxy)methyl]-(6-fluoro-2-chromanyl)-methanol,(R*,R*)-(+/−)-α-[(p-tolylsulfonyloxy)methyl]-(6-fluoro-2-chromanyl)-methanol,(S*,R*)-(+/−)-α-[(benzylamino)methyl]-(6-fluoro-2-chromanyl)-methanol,(R*,R*)-(+/−)-α-[(benzylamino)methyl]-(6-fluoro-2-chromanyl)-methanol,(2R,3R)-3-[2-(benzyloxy)-5-fluorophenethyl]-2-hydroxymethyl-oxacyclopropane,(2S,3S)-3-[2-(benzyloxy)-5-fluorophenethyl]-2-hydroxymethyl-oxacyclopropane,(2R,3S)-3-[2-(benzyloxy)-5-fluorophenethyl]-2- ...

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18-02-2021 дата публикации

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

Номер: US20210047258A1
Принадлежит:

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

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18-02-2016 дата публикации

VINYL-GROUP-CONTAINING FLUORENE COMPOUND

Номер: US20160046551A1
Принадлежит:

A novel vinyl-group-containing fluorene compound and a method for producing the same, a polymerizable monomer and cross-linking agent including this compound, a leaving-group-containing fluorene compound, a monovinyl-group-containing fluorene compound, and methods for producing the same. This vinyl-group-containing fluorene compound is represented by formula (1). In the formula, Wand Wrepresent a group represented by formula (2), a group represented by formula (4), a hydroxyl group, or a (meth)acryloyloxy group, Rand Rrepresent a cyano group, a halogen atom, or a monovalent hydrocarbon, and n1 and n2 are integers of 0-4. In formulas (2) and (4), a ring (Z) is an aromatic hydrocarbon ring, X is a single bond or a group represented by —S—, Ris a single bond or a C1-4 alkylene group, Ris a specific substituent group such as a monovalent hydrocarbon, and m is an integer of 0 or greater. 2. The vinyl-group-containing fluorene-based compound according to claim 1 , wherein the ring Z is a benzene ring or a naphthalene ring.3. (canceled)4. A polymerizable monomer comprising the vinyl-group-containing fluorene-based compound according to .5. A crosslinking agent comprising the vinyl-group-containing fluorene-based compound according to wherein Wand Weach are independently the group represented by the general formula (2) or a (meth)acryloyloxy group.7. The process for producing a vinyl-group-containing fluorene-based compound according to claim 6 , wherein the ring Z is a benzene ring or a naphthalene ring.8. (canceled)10. The leaving group-containing fluorene-based compound according to claim 9 , wherein the ring Z is a benzene ring or a naphthalene ring.11. (canceled)13. The process for producing a vinyl-group-containing fluorene-based compound according to claim 12 , wherein the ring Z is a benzene ring or a naphthalene ring.14. (canceled)16. The process for producing a monovinyl-group-containing fluorene-based compound according to claim 15 , wherein the ring Z is a ...

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15-02-2018 дата публикации

2-METHOXY-4-(3-(4-METHOXYPHENYL)PROP-1-EN-1-YL)PHENOL AND PREPARATION METHOD THEREFOR

Номер: US20180044275A1

Provided herein are 2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol having a novel structure capable of being used to prevent or treat all diseases associated with NF-κB, IKK and STAT3, and a method of preparing the same. 3. The method of claim 2 , wherein the X is F claim 2 , Cl claim 2 , I claim 2 , or Br.4. The method of claim 2 , wherein the reaction is carried out in the presence of a palladium catalyst and a base.5. The method of claim 2 , wherein the reaction is carried out by additionally adding a ligand comprising a phosphine or phosphite. The present invention relates to 2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol having a novel structure and a method of preparing the same.NF-κB belongs to a protein family associated with inflammation modulation, immune modulation, apoptosis, cell proliferation, epithelial differentiation, etc., which regulates the expression of various genes and forms the backbone of an intracellular signaling pathway.The understanding of the regulatory function in the inflammatory response and the immune system during the action of NF-κB offers new possibilities for the inflammatory response and immunotherapy after attempts to develop therapeutic agents using TNF-α inhibitors, and also the understanding of apoptosis and cell proliferation is important for research on the mechanisms of tumor development and metastasis. That is, it can be seen which genes are expressed by NF-κB in response to which external stimuli.NF-κB is activated by inflammatory cytokines such as TNF-α interleukin-1 (IL-1), interleukin-6 (IL-6), GM-CSF, etc. Such activated NF-κB regulates the transcription of chemokines such as IL-8, macrophage-inflammatory protein (MIP)-1α, methyl accepting chemotaxis protein1 (MCP1), RANTES, eotaxin, etc.; adhesion molecules such as E-selectin, vascular cell adhesion molecule-1 (VCAM-1), endothelial leukocyte adhesion molecule 1 (ELAM1), intercellular cell adhesion molecule 1 (ICAM-1), etc.; inducible enzymes such as ...

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19-02-2015 дата публикации

Myricanol Derivatives and Uses Thereof for Treatment of Neurodegenerative Diseases

Номер: US20150051294A1
Принадлежит: Universtiy of South Florida

The subject invention pertains to myricanol derivatives, therapeutic compositions, and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau. 2. A compound according to claim 1 , having a chemical structure of formula A.3. A compound according to claim 1 , having a chemical structure of formula B.4. A compound according to claim 1 , having a chemical structure of formula C.7. A pharmaceutical composition comprising a compound of .8. A pharmaceutical composition comprising a compound of .9. A pharmaceutical composition comprising a compound of .11. The method according to claim 10 , wherein the compound has a chemical structure of formula A.12. The method according to claim 10 , wherein the compound has a chemical structure of formula B.13. The method according to claim 10 , wherein the compound has a chemical structure of formula C.16. The method according to claim 10 , wherein the cells are in a subject in need of treatment for a neurodegenerative disease.17. The method of claim 16 , wherein the neurodegenerative disease is a tauopathy.18. The method of claim 17 , wherein the subject is a human.19. The method of claim 18 , wherein the neurodegenerative disease is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , frontotemporal dementia claim 18 , frontotemporal dementia with Parkinsonism claim 18 , frontotemporal lobe dementia claim 18 , pallidopontonigral degeneration claim 18 , progressive supranuclear palsy claim 18 , multiple system tauopathy claim 18 , multiple system tauopathy with presenile dementia claim 18 , Wilhelmsen-Lynch disease claim 18 , Pick's disease claim 18 , or Pick's disease-like dementia.20. The method of claim 19 , wherein the neurodegenerative disease is Alzheimer's disease. This application claims the benefit of U.S. provisional application Ser. No. 61/621,278, filed Apr. 6, 2012, and U.S. provisional application Ser. No. ...

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25-02-2016 дата публикации

Solubilization of Pterostilbene and Resveratrol in Aqueous Beverages

Номер: US20160052850A1
Принадлежит: Ironstone Separations, Inc.

In one embodiment, the present application discloses compositions and methods of solubilizing pterostilbene or resveratrol, or mixture thereof in aqueous media. 1. A stable and homogeneous aqueous formulation comprising:a) a composition selected from the group consisting of a pterostilbene-caffeine co-crystal complex, a resveratrol-caffeine co-crystal complex and a mixture thereof; andb) an emulsifying agent in an amount sufficient to solubilize the pterostilbene-caffeine co-crystal complex, a resveratrol-caffeine co-crystal complex and a mixture thereof, to form the stable and homogeneous formulation.2. The stable and homogeneous aqueous formulation of claim 1 , wherein the emulsifying agent is selected from the group consisting of TPGS claim 1 , TPGS-300 claim 1 , TPGS-500 claim 1 , TPGS-600 claim 1 , TPGS-750 claim 1 , TPGS-1000 claim 1 , TPGS-M claim 1 , TPGS-300-M claim 1 , TPGS-500-M claim 1 , TPGS-600-M claim 1 , TPGS-750-M and TPGS-1000-M claim 1 , or a mixture thereof.3. The stable and homogeneous aqueous formulation of claim 2 , wherein the emulsifying agent is TPGS.4. The stable and homogeneous aqueous formulation of claim 2 , wherein the formulation is an emulsion or a clear solution.5. The stable and homogeneous aqueous formulation of claim 1 , wherein the solution is in water.6. The stable and homogeneous aqueous formulation of claim 1 , wherein the formulation comprising the pterostilbene-caffeine co-crystal complex claim 1 , a resveratrol-caffeine co-crystal complex and a mixture thereof in water is at a co-crystal complex:water (wt:wt) ratio of 10:90 claim 1 , 20:80 claim 1 , 30:70 claim 1 , 40:60 claim 1 , 50:50 claim 1 , 60:40 claim 1 , 70:30 claim 1 , 80:20 or 90:10.7. A method of solubilizing pterostilbene or resveratrol claim 1 , or a mixture thereof claim 1 , in an aqueous media comprising:a) dissolving the pterostilbene or resveratrol, or a mixture thereof, and an emulsifying agent in a suitable solvent to form a homogeneous solution;b) ...

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23-02-2017 дата публикации

Process for preparing unsymmetric oco pincer ligands from the group of the m-terphenyl compounds

Номер: US20170050910A1
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a process for preparing unsymmetric compounds from the group of the m-terphenyls which can be used as unsymmetric OCO pincer ligands, comprising the process steps of a) reacting a first substituted or unsubstituted phenol with a 1,3-disubstituted arene which may likewise be substituted in the 2 and 5 positions to obtain a phenol-arene coupling product and b) optionally protecting the OH group of the phenol-arene coupling product with a protecting group to obtain a protected phenol-arene coupling product, and c) reacting the phenol-arene coupling product from a) or b) with a second substituted or unsubstituted phenol to obtain an unsymmetric m-terphenyl, with the proviso that the first phenol and the second phenol have different substitution, characterized in that at least one of process steps a) and c) is conducted as an electrochemical process step.

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23-02-2017 дата публикации

PROCESS FOR PREPARING SYMMETRIC PINCER LIGANDS FROM THE GROUP OF THE M-TERPHENYL COMPOUNDS

Номер: US20170050918A1
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a process for preparing compounds of the formula ABA 2. Process according to claim 1 ,characterized in thatthe electrochemical process step is conducted in such a way thataa) a mixture of at least one solvent and at least one conductive salt is produced,bb) the compounds to be converted are added to this mixture, with addition of the compound of the formula (A) in a molar excess based on the compound (B),cc) at least two electrodes are introduced into the reaction solution obtained in bb) and a voltage is applied to the electrodes,dd) the compounds (A) and (B) are converted to the compound (ABA),ee) the voltage is switched off, and optionallyff) the compound (ABA) is isolated and/or purified.3. Process according to claim 1 ,characterized in thatthe molar ratio of the compound (A) to the compound (B) is in the range from 1.5:1 to 4:1, preferably from 1.8:1 to 2.5:1 and more preferably 2:1.4. Process according to claim 1 ,characterized in thatcompounds of the formula (A) used are compounds in which X═NHR′.5. Process according to claim 1 ,characterized in that{'sub': '2', 'compounds of the formula (A) used are compounds in which X═—NH.'}6. Process according to claim 1 ,characterized in that{'sup': 6', '8, 'Rand Rare identical and are preferably hydrogen.'}7. Process according to claim 1 ,characterized in thatthe reaction is conducted in the presence of a solvent and the solvent used is a solvent from the group of acetonitrile, propylene carbonate, methyl carbonate, nitromethane, ethylene glycol dimethyl ether, methanesulphonic acid, benzene, toluene, water, methanol, ethanol, propanol, isopropanol, halogenated solvents or halogenated or non-halogenated acids or mixtures thereof.8. Process according to claim 7 ,characterized in thatsolvents used are methanol, formic acid, trifluoroacetic acid, hexafluoroisopropanol or mixtures thereof, preferably methanol, hexafluoroisopropanol or mixtures thereof, and preferably hexafluoroisopropanol.9. ...

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22-02-2018 дата публикации

Vinyl-group-containing fluorene compound

Номер: US20180050973A1
Принадлежит: Daicel Corp, Tokyo Ohka Kogyo Co Ltd

A novel vinyl-group-containing fluorene compound and a method for producing the same, a polymerizable monomer and cross-linking agent including the compound, a leaving-group-containing fluorene compound, a monovinyl-group-containing fluorene compound, and methods for producing the same. The vinyl-group-containing fluorene compound is represented by formula (1) in which W 1 and W 2 represent a group represented by formula (2), a group represented by formula (4), a hydroxyl group, or a (meth)acryloyloxy group, R 3a and R 3b represent a cyano group, a halogen atom, or a monovalent hydrocarbon, and n1 and n2 are integers of 0-4. In formulas (2) and (4), (Z) is an aromatic hydrocarbon ring, X is a single bond or a group represented by —S—, R 1 is a single bond or a C1-4 alkylene group, R 2 is a substituent such as a monovalent hydrocarbon, and m is an integer of 0 or more).

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03-03-2016 дата публикации

PHENOL DERIVATIVE AND PREPARATION METHOD AND USE IN MEDICINE THEREOF

Номер: US20160060197A1
Принадлежит: Sichuan Haisco Pharmaceutical Co., Ltd.

The present invention relates to a phenol derivative and the preparation method and use in medicine thereof, and particular to a phenol derivative represented by general formula (A) or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or a cocrystal thereof, a preparation method thereof, a pharmaceutical composition comprising the same, and use of the compound or composition of the present invention in the field of the central nervous system; wherein the definitions of substituents in general formula (A) are the same as those in the Description. 19. The compound according to claim 1 , or a stereoisomer claim 1 , a solvate claim 1 , a metabolite claim 1 , a prodrug claim 1 , a pharmaceutically acceptable salt claim 1 , or a cocrystal thereof claim 1 ,wherein the salt includes an ammonium salt, a potassium salt, a sodium salt, a calcium salt, a magnesium salt, a tetramethylammonium salt, a tetraethylammonium salt, a tetrapropylammonium salt, a tetrabutylammonium salt, a tetra(isopentyl)ammonium salt, an ethanolamine salt, a diethanolamine salt, a triethanolamine salt, trimethylamine salt, N-methylglucosamine salt, hydrochloride sulfate, phosphate, acetate, trifluoroacetate, fumarate, hemifumarate, maleate, malate, citrate, succinate, benzenesulfonate, or p-toluenesulfonate.22. A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound according to , or a stereoisomer, a solvate, a metabolite, a pharmaceutically acceptable salt, a cocrystal, or a prodrug thereof; and'}one or more pharmaceutically acceptable vehicles and/or excipients.23. Use of the compound according to claim 1 , or a stereoisomer claim 1 , a solvate claim 1 , a metabolite claim 1 , a pharmaceutically acceptable salt claim 1 , a cocrystal claim 1 , or a prodrug thereof claim 1 , for the manufacture of a medicament forinducing and maintaining anesthesia in an animal or a human,facilitating sedation and hypnosis of ...

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03-03-2016 дата публикации

DIPHENYLMETHANE COMPOUND

Номер: US20160060198A1
Автор: TAKAHASHI Daisuke
Принадлежит: AJINOMOTO CO., INC.

The present invention aims to provide a compound superior in broad utility and stability, which is useful as a protecting reagent (anchor) of amino acid and/or peptide in liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide (—CONHR)-type, an organic synthesis reaction method (particularly peptide liquid phase synthesis method) using the compound, and a kit for peptide liquid phase synthesis containing the compound, and has found that the object can be achieved by a particular compound having a diphenylmethane skeleton. 2. The diphenylmethane compound according to claim 1 , wherein claim 1 , in the organic group(s) in the number of (k+l) claim 1 , the total carbon number of the aliphatic hydrocarbon groups is 16-200.3. The diphenylmethane compound according to claim 1 , wherein the aliphatic hydrocarbon group independently has a carbon number of not less than 5.4. The diphenylmethane compound according to claim 1 , wherein the aliphatic hydrocarbon group independently has a carbon number of 5-60.5. The diphenylmethane compound according to claim 1 , wherein the organic group is independently bonded directly to ring A or ring B by a carbon-carbon bond or via —O— claim 1 , —S— claim 1 , —COO— claim 1 , —OCONH— or —CONH—.6. The diphenylmethane compound according to claim 5 , wherein the organic group is bonded to the 4-position of ring A or ring B via —O—.8. The diphenylmethane compound according to claim 7 , wherein claim 7 , in the formula (a) claim 7 ,{'sub': '1', 'mis 1 or 2;'}{'sub': '1', 'Xis —O—; and'}{'sub': '1', 'Ris a divalent aliphatic hydrocarbon group having a carbon number of 5-60.'}9. The diphenylmethane compound according to claim 7 , wherein claim 7 , in the formula (b):{'sub': '2', 'mis 1;'}{'sub': 1', '2', '3', '4, 'n, n, nand nare each independently an integer of 0-1;'}{'sub': '2', 'Xis —O— or —CONH—;'}{'sub': 2', '2', '2, 'X′, X″ and X′″ are each independently absent or —O—;'}{'sub': 2', '4, 'Rand ...

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15-05-2014 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20140135374A1
Автор: David S. Garvey
Принадлежит: Bikam Pharmaceuticals Inc

Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.

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15-05-2014 дата публикации

PERFLUOROPOLYVINYL MODIFIED ARYL INTERMEDIATES AND MONOMERS

Номер: US20140135518A1
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

A compound of formula (I) 2. A compound of claim 1 , wherein Ris —CF.3. A compound of claim 1 , wherein Ris —CF.4. A compound of claim 1 , wherein Ris —CFCFXCFand X is —F.5. A compound of claim 1 , wherein Ris —CFCFXCFand X is —OCF.6. A compound of claim 1 , wherein R is —OH claim 1 , —(CH)OH claim 1 , —OCHCH)OH claim 1 , or —(CH)(OCHCH)OH.7. A compound of claim 1 , wherein R is —C(O)—O—Ror —C(O)R; n is 1 to 10; m is 1 to 10; Ris Cto Calkyl; and Ris —H claim 1 , Cto Calkyl claim 1 , —Cl claim 1 , or —OCHCHOH.8. A compound of claim 1 , wherein R is —C≡N claim 1 , —C≡CH claim 1 , or —NO.9. A compound of claim 1 , wherein R is —C(O)NH(CHCHOH)and w is 0 claim 1 , 1 or 2.10. A compound of Formula (I) wherein Y is H.11. A compound of Formula (I) wherein Y is Cl.12. A compound of Formula (I) wherein Y is Br.14. A method of claim 11 , wherein the solvent is tetrahydrofuran claim 11 , carbon tetrachloride claim 11 , or carbon tetrabromide.15. A method of claim 12 , wherein the solvent is tetrahydrofuran.16. A method of claim 11 , wherein the base is potassium carbonate claim 11 , sodium carbonate claim 11 , or potassium bicarbonate.17. A method of claim 14 , wherein the base is potassium carbonate. The present invention comprises aryl compounds having partially fluorinated tails which can be useful as intermediates and starting materials for producing various water and oil repellents, soil resists, and surfactants.Water and oil repellents, soil resists, and surfactants compounds generally are prepared from linear perfluorinated alcohols. These alcohols are expensive and are prepared through several step synthesis. These alcohols are either then reacted to make final products or further synthesized into intermediates prior to making final products. New starting materials are needed that do not utilize linear perfluorinated alcohols.U.S. Pat. No. 7,531,700 teaches fluorinated solvents having benzene rings with a) perfluorinated pendent alkyl groups, b) alkyl, alkoxy, or ...

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02-03-2017 дата публикации

Method of Using dihydro-resveratrol or its stilbenoid derivatives and/or chemical variants in treatments of fibrotic and diabetic conditions

Номер: US20170057896A1
Принадлежит: Hong Kong Baptist University HKBU

A polyphenol derivative of the stilbenoid family, namely trans-3,5,4′-trihydroxybibenzyl, also known as dihydro-resveratrol, is disclosed as a remedial agent. In particular, the usage of dihydro-resveratrol as an anti-fibrotic agent in suppressing the activation of pancreatic stellate cells (PSCs) is presented. One embodiment also relates to the management of pancreatic fibrosis, which is often accompanied with chronic pancreatitis and desmoplastic reaction of pancreatic cancer. Another embodiment has applications in preventing or alleviating or treating pancreatic cancer or pancreatogenic diabetes.

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02-03-2017 дата публикации

Skin-protection composition containing dendrobium-based ingredients

Номер: US20170057906A1
Принадлежит: Hong Kong Baptist University HKBU

A skin-protection composition is shown that comprises stilbenoid(s) and/or stilbenoid-containing extract(s) obtained from Dendrobium plants, such as Dendrobium officinale and Dendrobium nobile for the management of melanogenesis, skin-darkening and skin-aging. More particularly, the usage of Dendrobium ingredients and stilbenoids is shown to reduce the formation of melanin in melanocytes. The usage of Dendrobium ingredients and stilbenoids is also shown to reduce the generation of reactive oxygen species and oxidative free radicals. The use of Dendrobium -derived extracts or ingredients or stilbenoids is shown in the formulation of skin-protection, skin-whitening and/or anti-skin aging products.

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21-02-2019 дата публикации

COMPOUND, RESIN, RESIST COMPOSITION OR RADIATION-SENSITIVE COMPOSITION, RESIST PATTERN FORMATION METHOD, METHOD FOR PRODUCING AMORPHOUS FILM, UNDERLAYER FILM FORMING MATERIAL FOR LITHOGRAPHY, COMPOSITION FOR UNDERLAYER FILM FORMATION FOR LITHOGRAPHY, METHOD FOR FORMING CIRCUIT PATTERN, AND PURIFICATION METHOD

Номер: US20190056657A1
Принадлежит:

The present invention employs a compound represented by the following formula (1) and/or a resin comprising the compound as a constituent: 2. The compound according to claim 1 , wherein at least one selected from the group consisting of Rand Ris a group in which a hydrogen atom of a hydroxy group is replaced with an acid dissociation group.3. The compound according to claim 1 , wherein at least one selected from the group consisting of Rand Ris a group in which a hydrogen atom of a hydroxy group is replaced with an acid dissociation group.4. The compound according to claim 1 , wherein at least one selected from the group consisting of Rto Ris a group containing an iodine atom.9. A resin comprising the compound according to as a constituent.10. A resist composition comprising the compound according to .11. The resist composition according to claim 10 , further comprising a solvent.12. The resist composition according to claim 11 , further comprising an acid generating agent.13. The resist composition according to claim 11 , further comprising an acid diffusion controlling agent.1426-. (canceled)27. A purification method comprising the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'obtaining a solution (S) by dissolving the compound according to in a solvent; and'}extracting impurities in the compound and/or the resin by bringing the obtained solution (S) into contact with an acidic aqueous solution (a first extraction step), whereinthe solvent used in the step of obtaining the solution (S) comprises a solvent that does not inadvertently mix with water.28. The purification method according to claim 27 , whereinthe acidic aqueous solution is an aqueous mineral acid solution or an aqueous organic acid solution;the aqueous mineral acid solution is one or more aqueous mineral acid solutions selected from the group consisting of hydrochloric acid, sulfuric acid, nitric acid, and phosphoric acid; andthe aqueous organic acid solution is one or more aqueous ...

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20-02-2020 дата публикации

BENZOSUBERENE ANALOGUES AND RELATED COMPOUNDS WITH ACTIVITY AS ANTICANCER AGENTS

Номер: US20200055805A1
Принадлежит: BAYLOR UNIVERSITY

A series of benzosuberene analogues demonstrate effective inhibition of tubulin polymerization, cytotoxicity against human cancer cell lines, and vascular disruption in tumors. 2. The compound of claim 1 , wherein R is CH claim 1 , (CH)CH claim 1 , O(CH)O(CH)OCH claim 1 , O(CH)OH claim 1 , COOEt claim 1 , CHOH claim 1 , CN claim 1 , or CHO claim 1 , n is 1.3. The compound of claim 1 , wherein Ris CH claim 1 , Ris Br claim 1 , and Ris H.4. The compound of claim 1 , wherein Ris OH claim 1 , Ris Br claim 1 , and Ris H.5. The compound of claim 1 , wherein Ris OCH claim 1 , Ris H claim 1 , and Ris OH.6. A pharmaceutical formulation comprising a therapeutically effective amount of the compound of .7. A method for inhibiting tubulin polymerization and disrupting vascularization in a tumor in a patient claim 6 , comprising administering the pharmaceutical formulation of .9. The compound of claim 8 , wherein Ris (═O).10. A pharmaceutical formulation comprising a therapeutically effective amount of the compound of .11. A method for inhibiting tubulin polymerization and disrupting vascularization in a tumor in a patient claim 10 , comprising administering the pharmaceutical formulation of .13. A pharmaceutical formulation comprising a therapeutically effective amount of the compound of .14. A method for inhibiting tubulin polymerization and disrupting vascularization in a tumor in a patient claim 13 , comprising administering the pharmaceutical formulation of . This application claims priority to U.S. Provisional Patent Application Ser. No. 62/719,362, entitled “Benzosuberene Analogues and Related Compounds with Activity as Anticancer Agents,” filed Aug. 17, 2018, the entire contents of which are hereby incorporated by reference.The present disclosure relates to potent small-molecule inhibitors of tubulin polymerization and uses thereof.Cancer, known medically as a malignant neoplasm, is comprised of a broad group of diseases involving unregulated cell growth. In cancer, cells ...

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04-03-2021 дата публикации

FLUORINE-CONTAINING ETHER COMPOUND, LUBRICANT FOR MAGNETIC RECORDING MEDIA, AND MAGNETIC RECORDING MEDIUM

Номер: US20210062102A1
Принадлежит: SHOWA DENKO K.K.

A fluorine-containing ether compound represented by R—R—CH—R—CH—R—Ris provided. (Ris a perfluoropolyether chain; Rand Rare each independently any one of an alkyl group that may have a substituent, an organic group having at least one double bond or at least one triple bond, and a hydrogen atom; and —R—CH—Ris represented by Formula (2), and R—CH—R— is represented by Formula (3)) 2. The fluorine-containing ether compound according to claim 1 ,wherein the alkyl group that may have a substituent is an alkyl group having 1 to 6 carbon atoms, wherein the alkyl group includes a hydroxyl group or a cyano group.3. The fluorine-containing ether compound according to claim 1 ,wherein the organic group having at least one double bond or at least one triple bond is any one of a group containing an aromatic ring, a group containing a heterocyclic ring, an alkenyl group, and an alkynyl group.4. The fluorine-containing ether compound according to claim 1 ,{'sup': '3', 'claim-text': {'br': None, 'sub': 2', '2', '2', 'm', '2', 'n', '2, '—CFO—(CFCFO)—(CFO)—CF—\u2003\u2003(8)'}, 'wherein Rin Formula (1) is represented by any one of Formulas (8) to (10).'} {'br': None, 'sub': 3', '3', '2', 'y', '3, '—CF(CF)—(OCF(CF)CF)—OCF(CF)—\u2003\u2003(9)'}, '(m and n in Formula (8) represent average polymerization degrees, and each represent 0 to 30, with a proviso that m or n is 0.1 or more)'} {'br': None, 'sub': 2', '2', '2', '2', '2', 'z', '2', '2, '—CFCFO—(CFCFCFO)—CFCF—\u2003\u2003(10)'}, '(y in Formula (9) represents an average degree of polymerization and represents 0.1 to 30)'}(in Formula (10), z represents an average degree of polymerization and represents 0.1 to 30).5. The fluorine-containing ether compound according to claim 1 ,wherein a number-average molecular weight thereof is in a range of 500 to 10000.6. A lubricant for magnetic recording media claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the fluorine-containing ether compound according to .'}7. A magnetic ...

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22-05-2014 дата публикации

TELOMERASE ACTIVATING COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20140142067A1

The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto. 14. The method of claim 1 , wherein said islet cell or pancreatic tissue is contacted with a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier.15. The method of claim 1 , wherein said subject has diabetes.16. The method of claim 1 , wherein said subject is predisposed to diabetes.17. The method of claim 1 , wherein Z is carbon claim 1 , silicon or germanium and Ris methyl. This application is a Continuation of U.S. patent application Ser. No. 12/602,956, filed Jun. 17, 2010, which in turn is a 371 of PCT International Application No. PCT/IL2008/000756, filed Jun. 4, 2008, which claims the benefit of U.S. Provisional Application Nos. 60/924,875, filed Jun. 4, 2007, 60/929,524, filed Jul. 2, 2007, 60/929,525, filed Jul. 2, 2007 and 61/006,924, filed Feb. 6, 2008. The disclosures of all applications are herein incorporated by reference.The present invention is directed to use of a series of compounds and compositions comprising the same for enhancing expression and/or activating telomerase and for treating diseases, disorders and/or conditions related thereto.Telomerase is a ribonucleoprotein that catalyzes the addition of telomeric repeats to the ends of telomeres. Telomeres are long stretches of repeated sequences that cap the ends of chromosomes. In humans, telomeres are typically 7-10 kb in length and comprise multiple repeats. Telomerase is not expressed in most adult cells, and telomere length decreases with successive rounds of replicationTelomerase acts as reverse transcriptase in the elongation of telomeres, which prevent the loss of telomeres due to the end replication problems. Without telomerase the telomeres are shortened at each cell division which leads to senescence, apoptosis and cell death caused by chromosome ...

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08-03-2018 дата публикации

BISPHENOL ETHER DERIVATIVES AND METHODS FOR USING THE SAME

Номер: US20180064657A1
Принадлежит:

Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, L, L, L, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided. 2. The compound of claim 1 , wherein Rand Rare each independently H or halogen.3. The compound of claim 1 , wherein X is —C(RR)—.4. The compound of claim 1 , wherein Rand Rare each C-Calkyl.5. The compound of claim 1 , wherein Rand Rare each methyl.6. The compound of claim 3 , wherein Rand Rare both Calkyl claim 3 , and wherein Rand Rare joined together to form a cyclopropyl ring.7. The compound of claim 1 , wherein Ris H or C-Calkyl.8. The compound of claim 1 , wherein Lis hydroxyl or —OC(═O)CH.9. The compound of claim 1 , wherein Land Lare each independently H claim 1 , hydroxyl claim 1 , —OC-Calkyl claim 1 , or —OC(═O)C-Calkyl.10. The compound of claim 1 , wherein at least one of Land Lis selected from a group consisting of pyrrole claim 1 , furan claim 1 , thiophene claim 1 , pyrazole claim 1 , pyridine claim 1 , pyridazine claim 1 , pyrimidine claim 1 , imidazole claim 1 , thiazole claim 1 , isoxazole claim 1 , oxadiazole claim 1 , thiadiazole claim 1 , oxazole claim 1 , triazole claim 1 , isothiazole claim 1 , oxazine claim 1 , triazine claim 1 , azepine claim 1 , pyrrolidine claim 1 , pyrroline claim 1 , imidazoline claim 1 , imidazolidine claim 1 , pyrazoline claim 1 , pyrazolidine claim 1 , piperidine claim 1 , dioxane claim 1 , morpholine claim 1 , dithiane claim 1 , thiomorpholine claim 1 , piperazine claim 1 , and tetrazine.11. The compound of claim 1 , wherein a is 1.12. The compound of claim 1 , wherein b is 1.13. The compound of claim 1 , wherein c is 1.17. The pharmaceutical composition of claim 16 , further comprising a pharmaceutically acceptable carrier.18. The ...

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27-02-2020 дата публикации

POLYMER PHOTOPOLYMERIZATION SENSITIZER

Номер: US20200062692A1
Принадлежит: Kawasaki Kasei Chemicals Ltd.

To provide a photopolymerization sensitizer which will not cause problems of dusting or coloring of a cured product by bleeding of additives such as the photopolymerization sensitizer on the surface e.g. by blooming at the time of photo-curing or during storage of the cured product, and which imparts a practically sufficient photo-curing rate. 110-. (canceled)1314-. (canceled)15. A photopolymerization initiator composition claim 11 , comprising the photopolymerization sensitizer of claim 11 , and a photopolymerization initiator.16. A photopolymerizable composition claim 15 , comprising the photopolymerization initiator composition of claim 15 , and a photocationic polymerizable compound.17. A photopolymerizable composition claim 15 , comprising the photopolymerization initiator composition of claim 15 , and a photoradical polymerizable compound. The present invention relates to an oligomer of a 9,10-bis(substituted oxy)anthracene compound, its production method, and a photopolymerization sensitizer containing an oligomer of a 9,10-bis(substituted oxy)anthracene compound.A photo-curing resin polymerizable by active energy rays such as ultraviolet rays or visible rays, which is quickly cured and can thereby remarkably reduce the amount of an organic solvent used as compared with a thermosetting resin, is superior in that the working environment can be improved and the environmental burden can be reduced. A conventional photo-curing resin by itself lacks polymerization initiation function and usually requires a photopolymerization initiator so as to be cured. The photopolymerization initiator may, for example, be an alkylphenone polymerization initiator such as hydroxyacetophenone or benzophenone, an acylphosphine oxide photopolymerization initiator or an onium salt (Patent Documents 1, 2 and 3). If an onium salt initiator is used among such photopolymerization initiators, an onium salt has light absorption in the vicinity of from 225 nm to 350 nm and has no absorption ...

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27-02-2020 дата публикации

Small Molecule Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors and Methods of Treatment

Номер: US20200062745A1
Принадлежит:

Provided are compounds of formulas (I), (II), (III), and (IV), which effectively inhibit protein arginine methyltransferase 5 (PRMT5). Also provided are methods of using the compounds, including a method of treating cancer, a method of inhibiting the activity of PRMT5 in a cell, and a method of treating a disease associated with increased activity of PRMT5. 3. The compound of claim 2 , wherein Rishalo,heterocycloalkyl selected from the group consisting of isoxazolyl, thiazolinyl, imidazolidinyl, piperazinyl, homopiperazinyl, pyrrolyl, pyrrolinyl, pyrazolyl, pyranyl, piperidyl, oxazolyl, and morpholinyl, orheteroaryl selected from the group consisting of pyridinyl, pyridazinyl, pyrimidyl, pyrazinyl, benzimidazolyl, triazinyl, imidazolyl, (1,2,3)-triazolyl, (1,2,4)-triazolyl, pyrazinyl, tetrazolyl, furyl, pyrrolyl, thienyl, isothiazolyl, thiazolyl, isoxazolyl, and oxadiazolyl.4. The compound of or claim 2 , wherein Ris halo claim 2 , C-Chaloalkoxy claim 2 , C-Chaloalkyl claim 2 , haloaryl claim 2 , or haloaryloxy.5. The compound of any one of - claim 2 , wherein Ris C-Calkyl claim 2 , halo claim 2 , or C-Chaloalkyl.6. The compound of any one of - claim 2 , wherein Ris H.7. The compound of any one of - claim 2 , wherein X is a bond claim 2 , —(CH)NR— claim 2 , or —NR(CH)—.8. The compound of any one of - claim 2 , wherein m is 1.9. The compound of any one of - claim 2 , wherein o is 1 or 2.12. The compound of claim 11 , wherein Rishydrogen,halo,heterocycloalkyl selected from the group consisting of isoxazolyl, thiazolinyl, imidazolidinyl, piperazinyl, homopiperazinyl, pyrrolyl, pyrrolinyl, pyrazolyl, pyranyl, piperidyl, oxazolyl, and morpholinyl, orheteroaryl selected from the group consisting of pyridinyl, pyridazinyl, pyrimidyl, pyrazinyl, benzimidazolyl, triazinyl, imidazolyl, (1,2,3)-triazolyl, (1,2,4)-triazolyl, pyrazinyl, tetrazolyl, furyl, pyrrolyl, thienyl, isothiazolyl, thiazolyl, isoxazolyl, and oxadiazolyl.13. The compound of or claim 11 , wherein Ris —NR(CH) ...

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09-03-2017 дата публикации

NOVEL CROSSLINKING REAGENTS, MACROMOLECULES, THERAPEUTIC BIOCONJUGATES, AND SYNTHETIC METHODS THEREOF

Номер: US20170065726A1
Автор: Huang Yumei
Принадлежит:

The invention provides novel chemical entities based on sugar alcohols. These new chemical entities are biocompatible and biodegradable. The molecules can be made in a single and pure form. The molecular weights of these molecules range from small (<1000 Da) to large (1000-120,000 Da). The sugar alcohol-based molecules can have functional groups throughout the molecule for crosslinking compounds, such as the preparation of antibody-drug conjugates, or to facilitate the delivery of therapeutic proteins, peptides, siRNA, and chemotherapeutic drugs. Also provided are new conjugate entities prepared through sugar alcohol molecules. Methods of synthesizing sugar alcohol-based molecules and conjugates are also within the scope of the invention. 1103-. (canceled)111121-. (canceled)122. The compound of claim 104 , wherein each of Xand Yis a chemical-crosslinking group.123. The compound of claim 104 , wherein each of Xand Yis a photo-crosslinking group. The invention relates to novel sugar alcohol-based crosslinking reagents, macromolecules, therapeutic conjugates, and synthetic methods. More specifically, the invention relates to novel chemical entities that may be used for labeling, conjugation, modification, molecule immobilization, therapeutic or diagnostic agents, and in drug delivery. Furthermore, the invention relates to novel conjugates prepared through new sugar alcohol-based crosslinking reagents and macromolecules.Bioconjugation technologies have been adapted in the biotechnology and pharmaceutical industries for the preparation of drug entities, detection reagents, and formulation strategies (Greg T. Hermanson “Bioconjugate Techniques”, 2008, Elsevier Inc.; Christof M. Niemeyer “Bioconjugation Protocols: Strategies and Methods”, 2004, Humana Press, Inc.). Bioconjugation is a chemical process that links together two or more biomolecules, including conjugation, labeling, modification, or immobilization of the biomolecules.The present invention provides a novel ...

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12-03-2015 дата публикации

MATERIALS AND METHODS FOR REDUCTION OF PROTEIN TAU AND TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20150072029A1
Принадлежит:

The subject invention provides a myricanol compound that is in predominant form of (+)-αR,11S-myricanol as compared to (−)-αS,11R-myricanol. In one embodiment, the (+)-αR,11S-myricanol is isolated from and is in about 86% enantiomeric excess of (−)-αS,11R-myricanol. The subject invention also pertains to therapeutic compositions and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau. Specifically exemplified herein is the therapeutic use of myricanol and myricanone isolated from root barks of species. Also provided are methods for preparing extracts of the subject invention from species. 2. The myricanol compound of ; or an alcohol claim 1 , ether claim 1 , or ester derivative of the myricanol; or any salt thereof; wherein the (+)-αR claim 1 ,11S form is in about 86% enantiomeric excess of the (−)-αS claim 1 ,11R form.3Myrica. The myricanol compound of ; or an alcohol claim 1 , ether claim 1 , or ester derivative of the myricanol; or any salt thereof; wherein the myricanol is isolated from a species.4Myrica cerifera.. The myricanol compound of ; or an alcohol claim 3 , ether claim 3 , or ester derivative of the myricanol; or any salt thereof; wherein the myricanol is isolated from5. A pharmaceutical composition claim 1 , comprising the myricanol compound of ; or an alcohol claim 1 , ether claim 1 , or ester derivative of the myricanol; or any salt thereof.6. A plant extract claim 1 , comprising the myricanol compound of .7Myrica. The plant extract of claim 6 , wherein the plant is a species.8Myrica cerifera.. The plant extract of claim 7 , wherein the plant is10. The method of claim 9 , wherein the alcohol claim 9 , ether claim 9 , or ester derivative of myricanol of formula II claim 9 , or any salt thereof claim 9 , is in predominant form of (+)-αR claim 9 ,11S as compared to (−)-αS claim 9 ,11R claim 9 , and wherein the (+)-αR claim 9 ,11S form is in at least 10% ...

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11-03-2021 дата публикации

COMPOUND, RESIN, COMPOSITION, RESIST PATTERN FORMATION METHOD AND CIRCUIT PATTERN FORMATION METHOD

Номер: US20210070685A1
Автор: ECHIGO Masatoshi
Принадлежит:

The present invention provides a compound having a specific structure represented by the following formula (0), a resin having a constituent unit derived from the compound, various compositions containing the compound and/or the resin, and various methods using the compositions. 7. A resin having a unit structure derived from the compound according to .10. A composition comprising one or more selected from the group consisting of the compound according to and a resin having a unit structure derived from the compound.11. The composition according to claim 10 , further comprising a solvent.12. The composition according to claim 10 , further comprising an acid generating agent.13. The composition according to claim 10 , further comprising an acid crosslinking agent.14. The composition according to claim 10 , wherein the composition is used in film formation for lithography.15. The composition according to claim 10 , wherein the composition is used in optical component formation.16. A method for forming a resist pattern claim 14 , comprising the steps of: forming a photoresist layer on a substrate using the composition according to ; and then irradiating a predetermined region of the photoresist layer with radiation for development.17. A method for forming a resist pattern claim 14 , comprising the steps of: forming an underlayer film on a substrate using the composition according to ; forming at least one photoresist layer on the underlayer film; and then irradiating a predetermined region of the photoresist layer with radiation for development.18. A method for forming a circuit pattern claim 14 , comprising the steps of: forming an underlayer film on a substrate using the composition according to ; forming an intermediate layer film on the underlayer film using a resist intermediate layer film material; forming at least one photoresist layer on the intermediate layer film; then irradiating a predetermined region of the photoresist layer with radiation for development ...

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11-03-2021 дата публикации

Compound, resin, composition and pattern formation method

Номер: US20210070727A1
Автор: Masatoshi Echigo
Принадлежит: Mitsubishi Gas Chemical Co Inc

The present invention provides a compound represented by following formula (0):

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18-03-2021 дата публикации

NOVEL ALKYLDIPHENYLMETHANE PROTECTIVE AGENT

Номер: US20210079028A1
Принадлежит: SEKISUI MEDICAL CO., LTD.

Provided is an alkyldiphenylmethane protective agent, which can prevent solidification or insolubilization of a compound by protecting a functional group of the compound to achieve easy separation and purification after a reaction. 2: The protected amino acid or a protected peptide according to claim 1 , wherein Y is —OR(wherein Rrepresents a hydrogen atom) claim 1 , —NHR(wherein Rrepresents a hydrogen atom claim 1 , a Clinear or branched alkyl group claim 1 , or an aralkyl group) claim 1 , or an isocyanate group.3: The protected amino acid or a protected peptide according to claim 1 , wherein Z is a Clinear or branched alkyl group.4: The protected amino acid or a protected peptide according to wherein at least one of Rto Rand at least one of Rto Rare each independently a group represented by formula (2) claim 1 , and the others are each independently a hydrogen atom claim 1 , a Calkyl group claim 1 , or a Calkoxy group.5: The protected amino acid or a protected peptide according to wherein Ris a Clinear or branched alkylene group.6: The protected amino acid or a protected peptide according to wherein Ris a Clinear or branched alkylene group.7: The protected amino acid or a protected peptide according to claim 1 , wherein Ris a single bond or a methylene group claim 1 , and R claim 1 , R claim 1 , and Rare each independently a methylene group.8: A method for producing peptide in a liquid phase claim 1 , comprising a step of reacting in a solvent a first protected amino acid or a first protected peptide comprising a protected functional group selected from carboxy group claim 1 , hydroxy group claim 1 , amino group claim 1 , amido group and mercapto group with a second protected amino acid or a second protected peptide comprising functional group that is different from the first protected amino acid functional group or the first protected peptide functional group wherein the first and second protected functional groups are protected by reaction with an ...

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14-03-2019 дата публикации

METHOD OF PRODUCING SOLUTION COMPOSITION CONTAINING MONOETHERIFIED PRODUCT, SOLUTION COMPOSITION, AND METHOD OF PRODUCING POLYMERIZABLE COMPOUND

Номер: US20190077738A1
Принадлежит: ZEON CORPORATION

Provided is a method of efficiently producing a solution composition containing a monoetherified product (III) using a hydroquinone compound (I) and a hydroxyl group-containing etherifying agent (II). The method of producing a solution composition includes: a step (1) of reacting a hydroquinone compound (I) and a hydroxyl group-containing etherifying agent (II) in a two-phase system including an alkaline aqueous solution and a hydrophobic ether solvent, and in the absence of a phase transfer catalyst and a hydrophilic organic solvent; and a step (2) of separating and removing an aqueous phase of a two-phase reaction liquid by liquid separation, and washing an organic phase using an aqueous solution containing a neutral inorganic salt and a hydroxide of an alkali metal, or the like. 2. The method of producing a solution composition according to claim 1 , whereinthe hydroxide of an alkali metal or alkaline earth metal is sodium hydroxide or potassium hydroxide.4. The method of producing a solution composition according to claim 1 , whereinthe hydrophobic ether solvent is anisole or cyclopentyl methyl ether.5. The method of producing a solution composition according to claim 1 , whereinthe neutral inorganic salt is sodium chloride or a sulfate.6. The method of producing a solution composition according to claim 1 , whereinthe neutral inorganic salt is sodium sulfate.8. The solution composition according to claim 7 , whereinthe hydrophobic ether solvent is anisole or cyclopentyl methyl ether.11. The method of producing a polymerizable compound according to claim 9 , whereinthe carboxylic acid compound is acrylic acid.12. The method of producing a solution composition according to claim 3 , whereinthe hydrophobic ether solvent is anisole or cyclopentyl methyl ether.13. The method of producing a solution composition according to claim 3 , whereinthe neutral inorganic salt is sodium chloride or a sulfate.14. The method of producing a solution composition according to claim ...

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22-03-2018 дата публикации

METHODS FOR PREPARING BRIDGED BI-AROMATIC LIGANDS

Номер: US20180079704A1
Принадлежит: UNIVATION TECHNOLOGIES, LLC

New methods of preparing bridged bi-aromatic ligands are disclosed. The methods employ direct di-ortho-lithiation of aromatic rings of bridged protected bi-aromatic diphenols. The ligands may be used to prepare transition metal compounds useful as catalysts in olefin polymerization. 2. A method according to comprising at least one step of aryl coupling.3. A method according to wherein the aryl coupling comprises at least one step of Negishi coupling.6. A method according to claim 1 , wherein the bridging group B is selected from the group consisting of optionally substituted divalent hydrocarbyl and divalent heteroatom containing hydrocarbyl.7. A method according to claim 1 , wherein B is selected from the group consisting of optionally substituted divalent alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , heteroalkyl claim 1 , heteroalkenyl claim 1 , heteroalkynyl claim 1 , aryl claim 1 , heteroaryl and silyl.8. A method according to claim 1 , wherein B is represented by the general formula -(QR-)— wherein each Q is either carbon or silicon and each Rmay be the same or different from the others such that each Ris selected from the group consisting of hydride and optionally substituted hydrocarbyl and heteroatom containing hydrocarbyl claim 1 , and optionally two or more Rgroups may be joined into a ring structure having from 3 to 50 atoms in the ring structure not counting hydrogen atoms; z′ is an integer from 1 to 10; and z″ is 0 claim 1 , 1 or 2.9. A method according to wherein B comprises optionally substituted divalent alkyl.10. A method according to wherein each 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 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris independently selected from the group consisting of hydride claim 1 , and optionally substituted alkyl and aryl.11. A method according to wherein Ar is independently selected from the group consisting of optionally substituted phenyl claim 1 , ...

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23-03-2017 дата публикации

AROMATIC COMPOUNDS BEARING HYDROXYL-SUBSTITUTED (PER)FLUOROPOLYETHER CHAINS

Номер: US20170081266A1
Принадлежит:

Compounds [compounds (L)] comprising at least one monocyclic, polycyclic or polycondensed aromatic moiety [moiety (A*)], wherein: at least one carbon atom of moiety (A*) is substituted with a fluoropolyoxyalkene chain [chain (R)], said chain (R) comprising: a) a fluorocarbon segment having ether linkages in the main chain and b) at least one hydroxyl group and wherein: at least one other carbon atom of moiety (A*) is substituted with an electron-withdrawing group and mixtures thereof are herein disclosed. Disclosed are also a process for manufacturing compounds (L), a method for lubricating MRM comprising using compounds (L), a lubricant composition comprising one or more compounds (L) and a method for manufacturing a composition (C). 2. A compound (L) according to wherein at least two carbon atoms of moiety (A*) are substituted with a chain (R) claim 1 , each chain (R) comprising:a) a fluorocarbon segment having ether linkages in the main chain andb) at least one hydroxyl group.3. A compound (L) according to wherein claim 2 , in moiety (A*) claim 2 , all carbon atoms which do not bear chain (R) bear halogen atoms.4. A compound (L) according to wherein the halogen atom is fluorine.5. A compound (L) according to wherein moiety (A*) is selected from benzene claim 1 , biphenyl and naphthalene.6. A compound (L) according to wherein chain (R) comprises repeating units R° claim 1 , said repeating units being selected from:{'sub': '3', '(i) —CFXO—, wherein X is F or CF,'}{'sub': '3', '(ii) —CFXCFXO—, wherein X, equal or different at each occurrence, is F or CF, with the provision that at least one of X is —F,'}{'sub': 2', '2', '2, '(iii) —CFCFCWO—, wherein each of W, equal or different from each other, are F, Cl, H,'}{'sub': 2', '2', '2', '2, '(iv) —CFCFCFCFO—,'}{'sub': 2', 'j', 'f', '3', 'f', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '1', '3, '(v) —(CF)—CFZ—O— wherein j is an integer from 0 to 3 and Z is a group of general formula —OR′T, wherein R′ is a ...

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31-03-2022 дата публикации

Antihypertensive polyol compound and derivative thereof

Номер: US20220098134A1
Принадлежит: Tao Pharmaceutical Suzhou Co Ltd

The present invention provides a compound as represented by formula I, or a pharmaceutically acceptable salt or ester, a prodrug, an optical isomer, a stereoisomer, or a solvate thereof. The compound provided by the present invention can be used for preparing drugs for preventing or treating hypertension, or hypertension-related diseases, or pulmonary hypertension, or pulmonary hypertension-related diseases. The compound provided by the present invention has a different mechanism from existing drugs for treating hypertension and pulmonary hypertension, thereby laying a new material foundation for the development of drugs for treating hypertension and pulmonary hypertension.

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12-06-2014 дата публикации

METHOD OF TREATING CANCER USING A CURCUMIN DERIVATIVE

Номер: US20140163116A1
Автор: DiMauro Thomas M.
Принадлежит: DEPUY SYNTHES PRODUCTS, LLC

The present invention is directed to treating cancer with a compound represented by Structural Formula (I): 3. The method of claim 2 , wherein Rand Rare the same; and m and p are the same.4. The method of claim 3 , wherein Ris —OH or —O—(C-C)alkyl.7. The method of claim 6 , wherein Ris —OH or —OMe.8. The method of claim 7 , wherein m and p are an integer from 1 to 3.10. The method of claim 9 , wherein each Rand Rare independently —OH or —OMe.11. The method of wherein the cancer is colon carcinoma.12. The method of wherein the cancer is pancreatic cancer.13. The method of wherein the cancer is breast cancer.14. The method of wherein the cancer is ovarian cancer.15. The method of wherein the cancer is prostate cancer. This application is a continuation application claiming priority from copending U.S. Ser. No. 13/756,195, filed Jan. 31, 2013, which is a continuation of U.S. Ser. No. 12/571,303, filed Sep. 30, 2009, which is a continuation-in-part of International Application No. PCT/US2008/060569, which designated the United States and was filed on Apr. 17, 2008, published in English, and which claims the benefit of priority of U.S. application Ser. No. 11/736,278, filed Apr. 17, 2007 and U.S. application Ser. No. 12/029,904, filed Feb. 12, 2008.The entire teachings of the above applications are incorporated herein by reference.In Alzheimer's Disease (AD), the abnormal cleavage of beta amyloid protein precursor from the intracellular membrane often produces a protein Aβ 1-42 which is incompletely removed by normal clearance processes. It has been reported that soluble beta amyloid oligomers are highly neurotoxic. Moreover, over time, this soluble protein assemblage is deposited as a beta amyloid protein Aβ plaque within brain tissue, leading to the local destruction of neurons. The Aβ plaque deposition is also believed to provoke an inflammatory response by microglia and macrophages, which recognize the plaque as a foreign body. These cells are believed to respond to ...

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25-03-2021 дата публикации

DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES

Номер: US20210085580A1
Автор: Jia Qi, Zhao Ji-Fu
Принадлежит: Unigen, Inc.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier. 140-. (canceled)42. The method of claim 41 , wherein the compound is selected from the group consisting of 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(3′ claim 41 ,4′-dihydroxyphenyl)-1-propanol claim 41 , 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(3′ claim 41 ,4′-dimethoxyphenyl)-1-propanol claim 41 , 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(2′-hydroxyphenyl)-1-propanol claim 41 , 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(2′-methoxyphenyl)-1-propanol claim 41 , 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(4′-methoxyphenyl)-1-propanol claim 41 , 1-(2 claim 41 ,4 claim 41 ,6-trihydroxyphenyl)-3-(4′-aminophenyl)-1-propanol claim 41 , dihydroxyphenyl)-3-phenyl-1-propanol claim 41 , 1-(2 claim 41 ,4-dihydroxyphenyl)-3-(3′- ...

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31-03-2016 дата публикации

Cb2 receptor ligands for the treatment of psychiatric disorders

Номер: US20160089349A1

The present invention provides cannabinoid type 2 (CB2) receptor inverse agonists for treating or ameliorating psychiatric disorders. The present invention further provides pharmaceutical compositions comprising 4′-O-methylhonokiol for treating Attention Deficit Hyperactivity Disorder (ADHD) and Tourette's syndrome.

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21-03-2019 дата публикации

Fluorine-containing ether compound, lubricant for magnetic recording medium, and magnetic recording medium

Номер: US20190084911A1
Принадлежит: Showa Denko KK

(In Formula (1), R1 is an end group including an organic group having at least one double bond or triple bond, R2 is a divalent linking group bonded to R1 by etheric oxygen, R3 is a perfluoropolyether chain, R4 is an end group having two or three polar groups with each polar group being bonded to different carbon atoms, and the carbon atoms, to which the polar groups are bonded, being bonded to each other via a linking group including carbon atoms to which the polar groups are not bonded.)

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12-05-2022 дата публикации

Compound, resin, composition, resist pattern formation method, circuit pattern formation method, and method for purifying resin

Номер: US20220144738A1
Принадлежит: Mitsubishi Gas Chemical Co Inc

The present invention has an object to provide a new compound that is useful as a film forming material for lithography or an optical component forming material, a resin containing a constituent unit derived from said compound, a composition, a resist pattern formation method, a circuit pattern formation method, and a purification method. A compound represented by formula (1), a resin containing a constituent unit derived from said compound, a composition containing one or more selected from the group consisting of said compound and said resin, a resist pattern formation method using said composition, a circuit pattern formation method, and a purification method thereof.

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05-04-2018 дата публикации

COMPOUND, RESIN, AND PURIFICATION METHOD THEREOF, MATERIAL FOR FORMING UNDERLAYER FILM FOR LITHOGRAPHY, COMPOSITION FOR FORMING UNDERLAYER FILM, AND UNDERLAYER FILM, AS WELL AS RESIST PATTERN FORMING METHOD AND CIRCUIT PATTERN FORMING METHOD

Номер: US20180095368A1
Принадлежит:

The present invention provides a compound represented by following formula (1), 2. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , at least one Rand/or at least one Rrepresent/represents one or more selected from the group consisting of a hydroxyl group and a thiol group.7. A resin obtained with the compound according to as a monomer.8. The resin according to claim 7 , wherein the resin is obtained by reacting the compound with a compound having crosslinking reactivity.9. The resin according to claim 8 , wherein the compound having crosslinking reactivity is an aldehyde claim 8 , a ketone claim 8 , a carboxylic acid claim 8 , a carboxylic halide claim 8 , a halogen-containing compound claim 8 , an amino compound claim 8 , an imino compound claim 8 , an isocyanate or an unsaturated hydrocarbon group-containing compound.11. A material for forming an underlayer film for lithography claim 1 , comprising the compound according to .12. A composition for forming an underlayer film for lithography claim 11 , comprising the material for forming the underlayer film for lithography according to claim 11 , and a solvent.13. The composition for forming the underlayer film for lithography according to claim 12 , further comprising an acid generator.14. The composition for forming the underlayer film for lithography according to claim 12 , further comprising a crosslinking agent.15. An underlayer film for lithography claim 12 , wherein the underlayer film is formed from the composition for forming the underlayer film for lithography according to .16. A resist pattern forming method claim 12 , comprising{'claim-ref': {'@idref': 'CLM-00012', 'claim 12'}, 'a step of forming an underlayer film on a substrate by using the composition for forming the underlayer film according to ,'}a step of forming at least one photoresist layer on the underlayer film, anda step of irradiating a predetermined region of the photoresist layer with radiation, and ...

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08-04-2021 дата публикации

BISPHENOL ETHER DERIVATIVES AND METHODS FOR USING THE SAME

Номер: US20210100757A1
Принадлежит:

Compounds having a structure of Formula I: 120.-. (canceled)23. The method of claim 22 , wherein the condition or disease is prostate cancer.24. The method of claim 22 , wherein the condition or disease is castration resistant prostate cancer.25. The method of claim 22 , wherein the condition or disease is androgen-dependent prostate cancer.2628.-. (canceled)29. The method of claim 21 , wherein Rand Rare each independently H claim 21 , —CN claim 21 , or halogen.30. The method of claim 21 , wherein Rand Rare each methyl.31. The compound of claim 21 , wherein at least one of Land Lis substituted or unsubstituted group selected from a pyrrole claim 21 , furan claim 21 , thiophene claim 21 , pyrazole claim 21 , pyridine claim 21 , pyridazine claim 21 , pyrimidine claim 21 , imidazole claim 21 , thiazole claim 21 , isoxazole claim 21 , oxadiazole claim 21 , thiadiazole claim 21 , oxazole claim 21 , triazole claim 21 , isothiazole claim 21 , triazine claim 21 , tetrazine claim 21 , oxazine claim 21 , azepine claim 21 , pyrrolidine claim 21 , pyrroline claim 21 , imidazoline claim 21 , imidazolidine claim 21 , pyrazoline claim 21 , pyrazolidine claim 21 , piperidine claim 21 , dioxane claim 21 , morpholine claim 21 , dithiane claim 21 , thiomorpholine claim 21 , or piperazine.32. The method of claim 21 , wherein:a) a is 0 or 1;b) b is 0 or 1; orc) c is 0 or 1.35. The method of claim 22 , wherein Rand Rare each independently H claim 22 , —CN claim 22 , or halogen.36. The method of claim 22 , wherein Rand Rare each methyl.37. The compound of claim 22 , wherein at least one of Land Lis substituted or unsubstituted group selected from a pyrrole claim 22 , furan claim 22 , thiophene claim 22 , pyrazole claim 22 , pyridine claim 22 , pyridazine claim 22 , pyrimidine claim 22 , imidazole claim 22 , thiazole claim 22 , isoxazole claim 22 , oxadiazole claim 22 , thiadiazole claim 22 , oxazole claim 22 , triazole claim 22 , isothiazole claim 22 , triazine claim 22 , tetrazine claim ...

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03-07-2014 дата публикации

MONOMER FOR HARDMASK COMPOSITION AND HARDMASK COMPOSITION INCLUDING THE MONOMER AND METHOD OF FORMING PATTERNS USING THE HARDMASK COMPOSITION

Номер: US20140186777A1
Принадлежит:

A monomer for a hardmask composition represented by the following Chemical Formula 1, 3. The monomer as claimed in claim 1 , wherein the Aand Aare each independently a substituted or unsubstituted benzyl group claim 1 , a substituted or unsubstituted naphthyl group claim 1 , or a substituted or unsubstituted biphenyl group.6. The monomer as claimed in claim 1 , wherein the monomer has a molecular weight of about 500 to about 5 claim 1 ,000.7. A hardmask composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the monomer as claimed in , and'}a solvent.8. The hardmask composition as claimed in claim 7 , wherein the monomer is included in an amount of about 1 to about 50 wt % based on a total amount of the hardmask composition.9. A method of forming a pattern; the method comprising:providing a material layer on a substrate;{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'applying the hardmask composition as claimed in on the material layer;'}heat-treating the hardmask composition to provide a hardmask layer;forming a silicon-containing thin layer on the hardmask layer;forming a photoresist layer on the silicon-containing thin layer;exposing and developing the photoresist layer to form a photoresist pattern;selectively removing the silicon-containing thin layer and the hardmask layer using the photoresist pattern to expose a part of the material layer; andetching an exposed part of the material layer.10. The method as claimed in claim 9 , wherein the hardmask composition is applied using a spin-on coating method.11. The method as claimed in claim 9 , wherein the hardmask layer is formed by heat-treating the hardmask composition at about 100° C. to about 500° C. Korean Patent Application No. 10-2012-0155330, filed on Dec. 27, 2012, in the Korean Intellectual Property Office, and entitled: “Monomer For Hardmask Composition and Hardmask Composition Including the Monomer and Method of Forming Patterns Using the Hardmask Composition,” is ...

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20-04-2017 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS

Номер: US20170107173A1
Принадлежит:

Compounds of formula I: 3. The compound of claim 1 , wherein Ris hydrogen.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris hydrogen.7. The compound of claim 1 , wherein Ris —OR.8. The compound of claim 1 , wherein Ris —OR.10. The compound of claim 1 , wherein Ris a C-Csaturated or unsaturated hydrocarbon chain wherein the hydrocarbon chain is optionally substituted with one or more groups independently selected from halogen and —O(C-C)alkyl and Ris hydrogen claim 1 , halogen or —OH.11. The compound of claim 1 , wherein Ris a C-Csaturated or unsaturated hydrocarbon chain wherein the hydrocarbon chain is optionally substituted with one or more groups independently selected from halogen and —O(C-C)alkyl and Ris hydrogen claim 1 , halogen or —OH.13. The compound of claim 1 , wherein A is —C(═O)NH— or —NHC(═O)— claim 1 , and Ris a C-Csaturated or unsaturated hydrocarbon chain wherein the hydrocarbon chain is optionally substituted with one or more groups independently selected from halogen and —O(C-C)alkyl and Ris hydrogen claim 1 , halogen or —OH; or A is —C(═O)NH— or —NHC(═O)— claim 1 , and Ris a C-Csaturated or unsaturated hydrocarbon chain wherein the hydrocarbon chain is optionally substituted with one or more groups independently selected from halogen and —O(C-C)alkyl and Ris hydrogen claim 1 , halogen or —OH.15. The compound of claim 1 , wherein Ris a C-Csaturated or unsaturated hydrocarbon chain wherein the hydrocarbon chain is optionally substituted with one or more groups independently selected from halogen and —O(C-C)alkyl.17. The compound of claim 1 , wherein Rand Rare each independently (C-C)alkyl wherein any (C-C)alkyl of Ror Ris optionally substituted with one or more halogen.19. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.20. A method for treating pain claim 1 , a psychiatric condition claim 1 , or ...

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02-04-2020 дата публикации

NEBIVOLOL SYNTHESIS METHOD AND INTERMEDIATE COMPOUND THEREOF

Номер: US20200102282A1
Автор: Zheng Zhiguo
Принадлежит:

The present invention relates to nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound. 3. The process according to or , wherein in step 3) , epoxidation of the compound of formula IV1 in trans-configuration or the compound of formula IV2 in cis-configuration can be carried out by using the epoxidation methods commonly used in the art , for example , the epoxidating reagent which can be used in the reaction is selected from organic peroxy-acid , such as MCPBA , trifluoroperacetic acid , dimethyldioxirane (DMDO) , a mixture of hydrogen peroxide and acetic acid , and a mixture of VO(acac)and tert-butyl hydroperoxide , and the system of pyridine-HOin the presence of catalytic amount of methylrhenium trioxide (MTO) , and the solvent in the reaction is organic aprotic solvent , such as methylene dichloride , chloroform , tetrahydrofuran , toluene , or a mixture of any two or more of them.4. The process according to any one of the precedent claims , wherein in step 4) , the deprotection can be carried out by the conventional methods in the field of organic chemistry to remove the hydroxy-protecting group , for example , by hydrogenolysis in the presence of catalyst to remove benzyl protective group , and cyclization is carried out in the presence of base; the catalyst used in the hydrogenolysis is Pd catalyst , such as Pd/C , Pd(OH) , Pd(OAc) , PdCl , Pd; the base used in the cyclization is selected from alkali metal and alkaline earth metal hydroxide or carbonate , alkoxide , or organic heterocyclic base , such as NaOH , KOH , KCO , NaOMe , DBU; or the deprotection and the cyclization are carried out by hydrogenolysis using Pd/C as catalyst under basic condition to simultaneously remove benzyl protective group and perform cyclization , to directly give the cyclization product.5. The process ...

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30-04-2015 дата публикации

Process for the preparation of 2-substituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives

Номер: US20150119587A1
Принадлежит: Natco Pharma Ltd

Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I [Formula should be inserted here], wherein R 1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R 2 is C 1 -C 6 alkyl. 2,4-Dihydroxy-3-methylbenzal-dehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin

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18-04-2019 дата публикации

Bridged bi-aromatic ligands and olefin polymerization catalysts prepared therefrom

Номер: US20190111414A1
Принадлежит: Univation Technologies Llc

Disclosed are novel bridged bi-aromatic phenol ligands and transition metal catalyst compounds derived therefrom. Also disclosed are methods of making the ligands and transition metal compounds, and polymerization processes utilizing the transition metal compounds for the production of olefin polymers.

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07-05-2015 дата публикации

HALOGENATED COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

Номер: US20150125389A1
Принадлежит:

Compounds having a structure of Formula I: 3. (canceled)4. The compound of claim 1 , wherein three of X claim 1 , X claim 1 , Xand Xare H claim 1 , and the remaining X claim 1 , X claim 1 , Xor Xis F claim 1 , Cl claim 1 , Br claim 1 , I or I.5. The compound of claim 1 , wherein Xis F claim 1 , Cl claim 1 , Br or I or I.6. The compound of claim 1 , wherein Xis F claim 1 , Cl claim 1 , Br or I or I.713-. (canceled)14. The compound of claim 1 , wherein Rand Rare each C-Calkyl.15. The compound of claim 14 , wherein C-Calkyl is methyl.16. The compound of claim 1 , wherein at least one of R claim 1 , Ror Ris H.17. (canceled)18. The compound of claim 1 , wherein R claim 1 , Rand Rare each H.19. The compound of claim 1 , wherein at least one of R claim 1 , Ror Ris C-Calkyl.20. (canceled)21. The compound of claim 1 , wherein R claim 1 , Rand Rare each C-Calkyl.22. (canceled)23. The compound of claim 21 , wherein C-Calkyl is methyl claim 21 , isopropyl or n-butyl.2425-. (canceled)26. The compound of claim 1 , wherein at least one of R claim 1 , Ror Ris C-Calkylcarbonyl.27. (canceled)28. The compound of claim 1 , wherein R claim 1 , Rand Rare each C-Calkylcarbonyl.29. The compound of claim 28 , wherein C-Calkylcarbonyl is methyl carbonyl.31. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable carrier.32. A method of imaging cancer claim 1 , the method comprising administering a compound of to a subject and detecting the presence or absence of cancer by use of SPECT or PET.33. The method of claim 32 , wherein the method identifies the presence or absence of a tumor.34. The method of claim 32 , wherein the method identifies the location of a tumor.35. The method of claim 32 , wherein the cancer is prostate cancer.3644-. (canceled)45. A method for modulating androgen receptor (AR) activity claim 1 , the method comprising administering to a mammalian cell a compound of .46. The method of claim 45 , wherein modulating androgen receptor ...

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03-05-2018 дата публикации

Method of Using dihydro-resveratrol or its stilbenoid derivatives and/or chemical variants in treatment of tumorous pathologies

Номер: US20180118647A1
Принадлежит:

The present invention relates to a polyphenol derivative of the stilbenoid family, namely trans-3,5,4′-trihydroxybibenzyl, also known as dihydro-resveratrol, as a remedial agent. In particular, the present invention presents the usage of dihydro-resveratrol or its derivatives/chemical variants in the manufacture of a medicament for the treatment of tumors or cancers. The dihydrostilbenes can be used in the treatment or delay of progression of a cancer in a patient or used in a pharmaceutical formulation for the aforementioned purposes. 2. The method according to wherein said compound is dihydro-resveratrol.3. The method according to wherein said compound is trans-3 claim 1 ,5 claim 1 ,4′-trihydroxybibenzyl.4. The method according to wherein said effective dosage ranges from 1.62 mg/kg to 8.13 mg/kg in body weight per day.5. The method according to wherein said effective dosage is 8.13 mg/kg in body weight per day.6. The method according to wherein said subject is human.7. The method according to wherein said subject is human.8. The method according to wherein said compound is administered in situ to site of the colorectal claim 1 , melanoma and pancreatic carcinoma.9. The method according to wherein said compound is administered intraperitoneally to said subject in need thereof.10. The method according to wherein said subject is human.11. The method according to wherein the compound is administered every other day for an effective period of time.12. The method according to wherein said effective period of time is no less than 21 days. The present application is a continuation-in-part application of U.S. non-provisional application Ser. No. 15/633,780 filed on Jun. 27, 2017 which is a divisional application of the U.S. non-provisional patent application Ser. No. 15/351,636 filed on Nov. 15, 2016 which is a continuation-in-part application of the U.S. non-provisional patent application Ser. No. 14/740,410 filed on Jun. 16, 2015, which the disclosures are hereby ...

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03-05-2018 дата публикации

AMINE SALTS OF A PROSTACYCLIN ANALOG

Номер: US20180118656A1
Принадлежит: CAYMAN CHEMICAL COMPANY INCORPORATED

The present invention provides amine salts of the prostacyclin analogue of Formula I 3. The method of claim 1 , wherein the organic solvent of step viii) comprises a halogenated organic solvent.4. The method of claim 3 , wherein the halogenated organic solvent comprises dichloromethane claim 3 , chloroform claim 3 , or any combination thereof.6. The method of claim 5 , wherein the base of step ii) comprises an alkyllithium reagent.7. The method of claim 6 , wherein the alkyllithium reagent is sec-butyllithium.8. The method of claim 5 , wherein the organic solvent of step ii) comprises pentane claim 5 , hexane claim 5 , cyclohexane claim 5 , heptane claim 5 , tetrahydrofuran claim 5 , 1 claim 5 ,4-dioxane claim 5 , diethyl ether claim 5 , petro ether claim 5 , methyl-tert-butylether claim 5 , or any combination thereof.9. The method of claim 8 , wherein the organic solvent of step ii) comprises methyl-tert-butylether.11. The method of claim 10 , wherein the reducing agent of step x) comprises a chiral borane compound.12. The method of claim 11 , wherein the chiral borane compound is selected from (R)-1-methyl-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-1-butyl-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-tetrahydro-1 claim 11 ,3 claim 11 ,3-triphenyl-1H claim 11 ,3H-pyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxaborole claim 11 , (4S)-2-methyl-4 claim 11 ,5 claim 11 ,5-triphenyl-1 claim 11 ,3 claim 11 ,2-oxazaborolidine claim 11 , or any combination thereof.13. The method of claim 10 , wherein the organic solvent of step x) further comprises toluene.16. The method of claim 15 , wherein the oxidizing agent comprises MnOor Dess-Martin periodinane.17. The method of claim 16 , wherein the base of step ii) comprises an alkyllithium ...

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03-05-2018 дата публикации

Synthetic Route To Anhydroryanodol, Ryanodol And Structural Analogues

Номер: US20180118706A1
Принадлежит:

This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby. This application is a divisional of U.S. patent application Ser. No. 15/381,595, filed Dec. 16, 2016, which claims the priority of U.S. Provisional Patent Application No. 62/269,760, filed Dec. 18, 2015, both applications of which are incorporated by reference.This invention was made with government support under Grant No. DGE1144469 awarded by the National Science Foundation and Grant RGM097582-01 awarded by the national Institute of General Medical Sciences. The government has certain rights in invention.This disclosure is related to methods for producing anhydroryanodol, ryanodol, and analogues thereof.Terpenes are a large and structurally diverse family of natural products that range from simple hydrocarbons associated with flavors and fragrances, to complex, highly oxidized polycyclic molecules such as the anti-malarial drug artemisinin, and the anticancer compounds ingenol and taxol. Although terpenes are isolated from natural sources, it can be challenging to translate their biological activity into a practical application. In some cases, the hurdle is low natural abundance; other times, it is the difficulty encountered by chemists seeking to precisely edit a terpene's molecular structure in order to improve its drug-like properties or interrogate its role in modulating disease pathways. The development of concise chemical syntheses of terpenes can transform the ability to use these molecules and their synthetic derivatives as biological probes or as lead compounds for the development of new medicines. Furthermore, these scientific efforts often innovate chemical reactivity or synthetic design concepts.The natural product ryanodine (1) and its hydrolysis product ryanodol (2) are among the most highly oxidized and synthetically challenging diterpenoids reported to date.Isolated from the tropical shrub Ryania speciosa Vahl in ...

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04-05-2017 дата публикации

Diglycidic ether derivative therapeutics and methods for their use

Номер: US20170121261A1

This invention provides compound having a structure of Formula I or Formula II. Uses of such compounds for treatment of various indications, including prostrate cancer as well as methods of treatment involving such compounds are also provided.

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14-05-2015 дата публикации

TRITYLATED ETHERS

Номер: US20150128485A1
Принадлежит:

A compound having formula (PhC)Ar(GR), wherein Ph represents a phenyl group, Ar is an aromatic ring system having from six to twenty carbon atoms; G is O, S, SO or SO; R is: (a) C-Calkyl substituted by at least one of OH, SH, C-Calkoxy and cyano; or (b) C-Cheteroalkyl; m is one or two; and n is an integer from one to four. 1. A compound having formula (PhC)Ar(GR) , wherein Ph represents a phenyl group , Ar is an aromatic ring system having from six to twenty carbon atoms; G is O , S , SO or SO; R is: (a) C-Calkyl substituted by at least one of OH , SH , C-Calkoxy and cyano; or (b) C-Cheteroalkyl; m is one or two; and n is an integer from one to four.2. The compound of in which Ar is a C-Chydrocarbyl aromatic ring system and R is C-Cheteroalkyl.3. The compound of in which n is an integer from one to three.4. The compound of in which R is C-Cheteroalkyl not containing sulfur and G is O.5. The compound of in which Ar is a benzene ring system and n is two.6. A method for marking a petroleum hydrocarbon or a liquid biologically derived fuel; said method comprising adding to said petroleum hydrocarbon or liquid biologically derived fuel at least one compound having formula (PhC)Ar(GR) claim 4 , wherein Ph represents a phenyl group claim 4 , Ar is an aromatic ring system having from six to twenty carbon atoms; G is O claim 4 , S claim 4 , SO or SO; R is: (a) C-Calkyl substituted by at least one of OH claim 4 , SH claim 4 , C-Calkoxy and cyano; or (b) C-Cheteroalkyl; m is one or two; and n is an integer from one to four claim 4 , wherein each compound having formula (PhC)Ar(GR)is present at a level from 0.01 ppm to 20 ppm.7. The method of in which Ar is a C-Chydrocarbyl aromatic ring system and R is C-Cheteroalkyl.8. The method of in which n is an integer from one to three.9. The method of in which R is C-Cheteroalkyl not containing sulfur and G is O.10. The method of in which Ar is a benzene ring system and n is two. This invention relates to new compounds useful in a ...

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25-04-2019 дата публикации

ARYL ETHERS AND USES THEREOF

Номер: US20190119214A1
Принадлежит:

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo. 164.-. (canceled)66. The process of claim 65 , wherein P is selected from acyl and methoxymethyl ether.67. The process of claim 66 , wherein P is —C(═O)R claim 66 , wherein R is C-Calkyl.68. The process of claim 67 , wherein P is —C(═O)CH.69. The process of claim 65 , wherein the fluorinating comprises adding (diethylamino)sulfur trifluoride to the compound of Formula A.71. The process of claim 70 , wherein the hydrolyzing comprises a silver salt.72. The process of claim 71 , wherein the silver salt is selected from AgCO claim 71 , AgClOand AgBF.76. The process of claim 75 , wherein the fluorinating comprises adding N-fluoro-o-benzendisulfonamide claim 75 , acetyl hypofluorite claim 75 , Accufluor® claim 75 , Selectfluor® claim 75 , Selectfluor® II claim 75 , or N-fluorobenzenesulfonamide to the 3-fluoro-5-(7-methylsulfonyl-1-oxo-indan-4-yl)oxy-benzonitrile.77. The process of claim 75 , wherein the reducing is an asymmetric reduction.78. The process of claim 77 , wherein the reducing provides the 3-fluoro-5-(((1S claim 77 ,2R)-2-fluoro-1-hydroxy-7-(methylsulfonyl)-2 claim 77 ,3-dihydro-1H-inden-4-yl)oxy)benzonitrile with greater than 90% enantioselectivity.79. The process of claim 77 , wherein the asymmetric reduction is selected from Corey-Bakshi-Shibata reduction claim 77 , asymmetric hydrogenation claim 77 , and asymmetric transfer hydrogenation.80. The process of claim 77 , further comprising a ruthenium catalyst. This application is a Continuation of U.S. application Ser. No. 15/805,390, filed on Nov. 7, 2017, which is a Continuation of U.S. application Ser. No. 14/905,776, filed Jan. 15, 2016, which is a National Stage Entry of PCT/US2014/054375, filed Sep. ...

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16-04-2020 дата публикации

Polybrominated diphenyl-based flame retardant compounds

Номер: US20200115308A1
Принадлежит: International Business Machines Corp

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

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12-05-2016 дата публикации

NOVEL PHENYLNAPHTHOL DERIVATIVES

Номер: US20160130203A1
Принадлежит: TOKUYAMA CORPORATION

Phenylnaphthol derivatives represented by the following general formula (1), This invention relates to novel phenylnaphthol derivatives useful as intermediate products for the production of functional organic materials such as medicines and dyes. More specifically, the invention also relates to a process for producing indenonaphthol compounds and indenonaphthopyrans by using the phenylnaphthol derivatives.The phenylnaphthol compound which is a phenylnaphthalene compound is useful as an intermediate product for the production of functional organic materials such as medicines and dyes. For example, the indenonaphthopyran compound which is a photochromic coloring matter is synthesized from the indenonaphthol compound. So far, the indenonaphthol compound has been produced by using a benzophenone compound as a starting material.According to the conventional method of producing the indenonaphthol compounds from the benzophenone compounds, it was necessary to produce the phenylnaphthol compounds having, on the naphthalene ring thereof, a substituent that is to be converted into an indeno group. Thus, the phenylnaphthol compounds have heretofore been synthesized from the benzophenone compounds through the reactions of a multiplicity of stages. Therefore, the production steps were complex, yields were poor and, as a result, the production cost was high, and improvements have been urged. Specifically, if a benzophenone compound having an asymmetrical molecular structure is used as the starting material, there are formed structural isomers, the phenylnaphthol compound is obtained in a greatly decreased yield, and improvements have been urged (e.g., see patent documents 1 and 2).If it is attempted to synthesize a benzophenone compound represented by the following formula:by the Friedel-Craft' s acylation reaction, selectivity of the positions to be acylated is so low that it is difficult to obtain the desired product in a high yield. Therefore the benzophenone compound had to ...

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