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Небесная энциклопедия

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

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

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Применить Всего найдено 4492. Отображено 196.
20-02-2016 дата публикации

СОЕДИНЕНИЯ, ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ СПИДА

Номер: RU2575845C2

Изобретение относится к применению соединения формулы (I) или любой из его фармацевтически приемлемых солей, где означает ароматическое кольцо, где V представляет собой С или N, и, когда V представляет собой N, V находится в мета- или пара-положении к Z, R независимо представляет собой атом водорода, атом галогена или группу, выбранную из группы -CN, гидроксильной группы, группы -COOR1, (С1-С3)фторалкильной группы, группы (С1-С3)фторалкокси, группы -NO2, группы -NR1R2, группы (С1-С4)алкокси, группы фенокси и (С1-С3)алкильной группы, где указанный алкил возможно является монозамещенным гидроксильной группой, R1 и R2 независимо представляют собой атом водорода или (С1-С3)алкильную группу, n равно 1, 2 или 3, n′ равно 1 или 2, R′ представляет собой атом водорода, атом галогена или группу, выбранную из (С1-С3)алкильной группы, группы -NO2, группы -NR1R2, группы морфолинил, N-метилпиперазинильной группы, (С1-С3)фторалкильной группы и группы (С1-С4)алкокси, R″ представляет собой атом водорода ...

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27-04-2006 дата публикации

ОРТОЗАМЕЩЕННЫЕ АЗОТСОДЕРЖАЩИЕ БИСАРИЛЬНЫЕ СОЕДИНЕНИЯ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ КАЛИЕВОГО КАНАЛА, А ТАКЖЕ СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Номер: RU2275360C2

Изобретение относится к новым биологически активным орто-замещенным азотсодержащим бисарильным соединениям. Описываются соединения формулы 1, в которой: А1, А2, A3, А4, А5, А6, А7 и А8 независимо друг от друга обозначают азот или СН, причем, по крайней мере, одна или самое большее две из этих групп обозначают азот; R(1) обозначает C(O)OR(9) или COR(11); R(9) и R(11) независимо друг от друга обозначают СхН2х-R(14); x имеет значение 0, 1, 2, 3 или 4, R(14) обозначает алкил с 1, 2, 3, 4, 5 или 6 С-атомами, фенил или изоксазолил, причем фенил и изоксазолил не замещены или замещены 1, 2 или 3 заместителями, выбранными из группы, состоящей из F, Cl, Br, I, CF3, OCF3, алкила с 1, 2, 3 или 4 С-атомами и алкоксигруппы с 1, 2, 3 или 4 С-атомами; R(2) обозначает водород; R(3) обозначает CyH2y-R(16); y имеет значение 0, 1, 2, 3 или 4, причем y не может быть 0, если R(16) обозначает OR(17); R(16) обозначает алкил с 1, 2, 3, 4, 5 или 6 С-атомами, циклоалкил с 3, С-атомами, OR(17), фенил или пиридил, ...

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10-12-2001 дата публикации

НОВЫЕ ГЕТЕРОАРИЛОКСИЭТИЛАМИНЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ СРОДСТВОМ К 5НТ1A РЕЦЕПТОРАМ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ

Номер: RU2176639C2

Изобретение относится к новым гетероарилоксиэтиламинам общей формулы I, в которой Аr представляет собой бициклический гетероарил, содержащий один или два атома азота, необязательно замещенный гидрокси, галогеном или низшим алкилом, Y представляет собой радикал -C(O)NH- или -NHC(O)-, R представляет собой низший алкильный радикал, С3-С6циклоалкил, необязательно замещенный низшим алкилом, или фенил, или к солям указанных соединений. Также раскрыты способ получения этих соединений, содержащая их фармацевтическая композиция, обладающая сродством к 5HT1A рецепторам, и промежуточные соединения общей формулы V, где значения радикалов Аr, Y, R такие же, как и в формуле I. Изобретение может быть использовано в медицине в качестве ингибиторов секреции желудочной кислоты или в качестве противорвотных средств. 4 с. и 10 з. п. ф-лы, 2 табл.

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20-01-2007 дата публикации

КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ТЕРАПЕВТИЧЕСКИ АКТИВНЫЕ КОМПОНЕНТЫ, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ

Номер: RU2291685C2
Принадлежит: АЛЛЕРГАН ИНК. (US)

Изобретение относится к медицине. Описана композиция для офтальмологических средств, содержащая терапевтически активный компонент, представляющий собой тартрат 5-бромо-6-(2-имидазолин-2-иламино)хиноксалина, компоненты, повышающие растворимость, отличные от циклодекстринов, и хлороксикомпоненты, в основном эффективные в качестве консервантов. Хлороксикомпоненты являются предпочтительными для сохранения терапевтически активных компонентов. Компоненты, повышающие растворимость, включают карбоксиметилцеллюлозу. 5 з.п. ф-лы, 7 табл., 1 ил.

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20-10-2007 дата публикации

СПОСОБЫ ПОЛУЧЕНИЯ РАЦЕМИЧЕСКОГО АМИНОЗАМЕЩЕННОГО 5,6,7,8-ТЕТРАГИДРОХИНОЛИНА ИЛИ РАЦЕМИЧЕСКОГО АМИНОЗАМЕЩЕННОГО 5,6,7,8-ТЕТРАГИДРОИЗОХИНОЛИНА, СПОСОБЫИХ РАЗДЕЛЕНИЯ И РАЦЕМИЗАЦИИ, СПОСОБ ПОЛУЧЕНИЯ КЕТОЗАМЕЩЕННОГО 5,6,7,8-ТЕТРАГИДРОХИНОЛИНА ИЛИ КЕТОЗАМЕЩЕННОГО 5,6,7,8-ТЕТРАГИДРОИЗОХИНОЛИНА, СПОСОБ ПОЛУЧЕНИЯ ЭНАНТИОМЕРА КОНДЕНСИРОВАННОГО БИЦИКЛИЧЕСКОГО КОЛЬЦА, ЗАМЕЩЕННОГО ПЕРВИЧНЫМ АМИНОМ, ПРОИЗВОДНЫЕ 5,6,7,8-ТЕТРАГИДРОХИНОЛИНА

Номер: RU2308451C2
Принадлежит: АНОРМЕД, ИНК. (CA)

Изобретение относится к способам получения и разделения рацемических аминозамещенных конденсированных бициклических кольцевых систем. В одном из способов применяют селективное гидрирование аминозамещенной конденсированной ароматической кольцевой системы. В альтернативном способе получают рацемическую аминозамещенную конденсированную бициклическую кольцевую систему через нитрозирование. Кроме того, изобретение относится к ферментативному разделению рацемической смеси с получением (R)- и (S)-форм аминозамещенных конденсированных бициклических колец, а также к способу рацемизации для повторного получения непредпочтительного энантиомера. Настоящее изобретение также предлагает способ получения энантиомера конденсированного бициклического кольца, замещенного первичным амином путем получения соответствующего энантиомерно чистого имина конденсированного бициклического кольца, диастереоселективного восстановления его и удаления вспомогательного хирального фрагмента. В указанных процессах используют ...

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20-12-2007 дата публикации

ИНГИБИТОРЫ КАТЕПСИН-ЦИСТЕИНПРОТЕАЗЫ

Номер: RU2312861C2

Изобретение относится к соединениям, представленным формулой где значения заместителей указаны в описании, и их фармацевтически приемлемым солям, которые могут использоваться для лечения и/или профилактики катепсин-зависимых состояний или болезней млекопитающих, нуждающихся в этом. Эти соединения являются полезными для лечения заболеваний, при которых показано ингибирование резорбции кости, таких как остеопороз, повышение минеральной плотности кости и снижение риска переломов. Задачей настоящего изобретения является применение заявленных соединений для изготовления лекарственного средства, обладающего ингибирующей активностью в отношении катепсина. 8 н. и 16 з.п. ф-лы, 4 табл.

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20-07-2002 дата публикации

ГЕТЕРОЦИКЛИЧЕСКИЕ ТЕТРАКАРБОНИТРИЛЫ

Номер: RU2185377C1

Изобретение относится к новым гетероциклическим тетракарбонитрилам общей формулы I где X = σ-связь, Соединения могут быть использованы для получения полигексазоцикланов - флуорофоров, бифлуорофоров, трифлуорофоров. Такие полигексазоцикланы перспективны для использования в качестве активных сред жидких и твердых лазеров, сцинтилляторов, особенно для индикации жесткого излучения, для трансформации коротковолнового излучения в длинноволновое при передаче информации по волоконно-оптическим линиям связи, для увеличения мощности солнечных батарей, для защиты ценных бумаг, для изготовления рекламных щитов. 2 табл.

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10-04-2006 дата публикации

ПРОИЗВОДНЫЕ 1-ПРОПАНОЛА И 1-ПРОПИЛАМИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ГЛЮКОКОРТИКОИДНЫХ ЛИГАНДОВ

Номер: RU2005124558A
Принадлежит:

... 1. Соединение формулы (IA) где R1 означает арил, гетероарил или С5-С15циклоалкил, каждый из которых необязательно и независимо содержит от одного до трех заместителей, причем каждый заместитель группы R1 независимо означает C1-С5алкил, С2 -С5алкенил, С2-С5алкинил, С3-С8циклоалкил, гетероциклил, арил, гетероарил, C1-C5алкокси, С2-С5 алкенилокси, С2-С5алкинилокси, арилокси, ацил, С1-С5алкоксикарбонил, С1-С5алканоилокси, С1-С5алканоил, ароил, аминокарбонил, алкиламинокарбонил, диалкиламинокарбонил, аминокарбонилокси, С1-С5алкиламинокарбонилокси, С1-С5диалкиламинокарбонилокси, С3-С5циклоалкиламинокарбонилокси, С1-С5алканоиламино, С1-С5алкоксикарбониламино, С1-С5алкилсульфониламино, аминосульфонил, С1-С5алкиламиносульфонил, С1-С5диалкиламиносульфонил, галоген, гидрокси, оксо, карбокси, циано, трифторметил, трифторметокси, нитро или амино, причем атом азота необязательно независимо моно- или дизамещен группой С1-С5алкил или арил; или уреидо, причем каждый атом азота необязательно независимо замещен ...

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10-10-2005 дата публикации

ПОЛУЧЕНИЕ ЭНАНТИОМЕРНО ЧИСТЫХ АМИНОЗАМЕЩЕННЫХ КОНДЕНСИРОВАННЫХ БИЦИКЛИЧЕСКИХ КОЛЕЦ

Номер: RU2004110928A
Принадлежит:

... 1. Способ получения рацемического аминозамещенного 5,6,7,8-тетрагидрохинолина или рацемического аминозамещенного 5,6,7,8-тетрагидроизохинолина, включающий: a) взаимодействие аминозамещенного хинолина формулы I или аминозамещенного изохинолина формулы II с соединением, имеющим аминозащитную группу, в органическом растворителе с получением аминозамещенного хинолина или изохинолина с защищенной аминогруппой: b) гидрирование аминозамещенного хинолина или изохинолина с защищенной аминогруппой в сильнокислом растворителе при повышенной температуре с образованием 5,6,7,8-тетрагидрохинолина или 5,6,7,8-тетрагидроизохинолина; и c) гидролиз аминозащитной группы с получением требуемого рацемического аминозамещенного 5,6,7,8-тетрагидрохинолина или рацемического аминозамещенного 5,6,7,8-тетрагидроизохинолина; причем NH2-группа находится в любом положении бензольной части молекулы хинолина или изохинолина, Rl находится в положении любого другого атома водорода хинолинового или изохинолинового цикла; ...

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15-11-1990 дата публикации

Способ получения 2-ароилметилен-3-метоксикарбонилметил-1,2-дигидрохиноксалинов

Номер: SU1606509A1
Принадлежит:

Изобретение касается гетероциклических веществ, в частности получения 3-метоксикарбонилметил-2-п-метил(или метокси)бензоилметилен-1,2-дигидрохиноксалинов, обладающих антимикробным действием, что может быть использовано в медицине. Цель - создание нового способа получения новых активных веществ указанного класса. Синтез ведут реакцией 2-метоксикарбонилметилен-5-п-толил(или метоксифенил)-2,3-дигидрофуран-3-она с о-фенилендиамином в среде этанола в присутствии HCL при 60-78°С. Выход, % т.пл., °С брутто-ф-ла минимальная ингибирующая концентрация, мкг/мл: а) 66 169-170 C20H18N2O3 500 и 250 б) 74 133-134 C20H18N2O4 не указана.

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15-11-1985 дата публикации

Способ получения производных 2-хиноксалинил-1,4-диоксида

Номер: SU1192622A3

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 2-ХИНОКСАЛИНШ1- 1 , 4-ДИОКСИДА формулы I «J он М I i О где R - группа HOj -CH-CHj или 4-оксо 2 тион-5-тиаэолидинил, отличающийся тем, что соединение формулы подвергают взаимодействию с соединением формулы И - R, где R имеет указанное значение, в присутствии основного катализатора , такого как пиперидин или гидроокись щелочного металла.

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08-07-2010 дата публикации

Verfahren zur Herstellung von ß- Heteroaryl-2-alanin-Verbindungen über 2-Amino-2-(heteroarylmethyl)-carbonsäure-Verbindungen

Номер: DE0010332560B4
Принадлежит: CHIRACON GMBH

... β-Heteroaryl-α-alanin-Verbindungen der allgemeinen Formel I, worin Y und Y'' zusammen eine Kette bilden, worin X1 für eine CR3-Gruppe steht, X2 für eine CR4-Gruppe steht, R1 und R2, gleich oder verschieden, jeweils für ein Wasserstoff, ein Halogen, einen Alkylrest, einen halogensubstituierten Alkylrest oder einen Alkoxyrest stehen, R3 und R4, gleich oder verschieden, jeweils für ein Wasserstoff, ein Halogen, einen Alkylrest, einen halogensubstituierten Alkylrest oder einen Alkoxyrest stehen, R für eine Alkyloxycarbonylgruppe steht, R5 für ein Wasserstoff oder eine CO2X''-Gruppe steht, wobei X'' für eine Alkyl-, oder Aryl-gruppe steht, X' für eine Alkyl- oder Aryl-gruppe steht, in Form ihrer Diastereomere, ihrer Enantiomere und Gemischen daraus, einschließlich ihrer Racemate sowie in Form der freien Basen, Salze und/oder Solvate und deren Lösungen.

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21-01-1982 дата публикации

"6-STYRYLCHINOXALINE UND DEREN VERWENDUNG ALS OPTISCHE AUFHELLER"

Номер: DE0003115871A1
Принадлежит:

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12-07-1973 дата публикации

VERFAHREN ZUM OPTISCHEN AUFHELLEN VON ORGANISCHEN MATERIALIEN

Номер: DE0001594833B2
Автор:
Принадлежит:

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30-06-1971 дата публикации

QUINOXALINE DERIVATIVES

Номер: GB0001237438A
Принадлежит:

... 1,237,438. Quinoxaline-1,4-dioxide derivatives. IMPERIAL CHEMICAL INDUSTRIES Ltd. 28 May, 1969 [17 June, 1968; 12 Sept., 1968], Nos. 28678/68 and 43452/68. Heading C2C. [Also in Division A5] Novel quinoxaline-1,4-dioxide derivatives of the formula wherein R1 is H, formyl, alkylcarbonyl, (haloalkyl)-carbonyl, alkoxycarbonylalkylcarbonyl, alkanesulphonyl, or alkoxycarbonyl and R2 is H or alkyl, but excluding 5-acetamidoquinoxaline-1,4-dioxide are prepared by oxidizing the corresponding 5-substituted quinoxaline derivative. 5-Amino-quinoxaline-1,4-dioxide is prepared by hydrolysing 5-trifluoroacetamidoquinoxaline-1,4-dioxide with sodium hydroxide. 7 - Methyl - 5 - acetamido., 5 - propionamido- and 5 - trifluoroacetamido - quinoxalines are prepared by reacting 5-aminoquinoxaline with the appropriate acid anhydride. 5 - Butyramido-, 5 - chloroacetamido- and 5- dichloroacetamido-quinoxalines are prepared by reacting 5-aminoquinoxaline with the corresponding acid chloride. 5 ...

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25-06-1969 дата публикации

Furan Flavouring Agents

Номер: GB0001156480A
Принадлежит:

... 1,156,480. Furan derivatives. R. FIRMENICH, G. FIRMENICH, R. E. FIRMENICH, and F. H. FIRMENICH, [trading as FIRMENICH & CIE.]. 2 May, 1966 [30 April, 1965; 18 April, 1966], No. 2381/69. Divided out of 1,156,472. Heading C2C. [Also in Division A2] 2-Isopropenyl-benzofuran.-According to the method described in J.A.C.S. 73, 754 (1951), 2-acetyl-benzofuran is reacted with methylmagnesium bromide to form 2-(2-hydroxyisopropyl)-benzofuran which is converted to its acetate. Pyrolysis of the acetate yields 2-isopropenyl-benzofuran of b.p. 81-83‹ C./0À001 mm. Hg. 7-Ethyl-benzofuran is prepared by the method described in J. Chem. Soc. 1920, 1534, but using o-ethylphenol instead of o-cresol. The MS. of the product thus obtained shows the following ion peaks with the relative intensities given within brackets: 131 (100%), 146 (38%) and 77 (10%). 2,7 - Dimethyl - benzofuran.-7 - Methylbenzofuran is subjected to a WILSMEYER reaction to form 7-methyl-benzofuran-2-aldehyde which is converted into 2,7-dimethylbenzofuran ...

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08-01-1975 дата публикации

PROCESS FOR THE PRODUCTION OF QUINOXALINE

Номер: GB0001379870A
Автор:
Принадлежит:

... 1379870 Quinoxaline CHEMICZNA SPOLDZIELNIA PRACY SYNTEZA 25 May 1973 [26 May 1972 8 June 1972] 25233/73 Heading C2C Quinoxaline is produced by reacting at least 11 % by weight of orthophenylenediamine with at least 6% by weight of glyoxal in an aqueous solution in the presence of a salt of an alkali metal and a weak acid. The preferred salt is sodium carbonate. The glyoxal may be used in the form of a solution obtained by the oxidation of acetaldehyde or paraldehyde with nitric acid and which contains up to 30% of other compounds, in particular organic acids.

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25-05-1977 дата публикации

POLYETHERQUINOXALINES AND METHOD FOR MAKING SAME

Номер: GB0001474754A
Автор:
Принадлежит:

... 1474754 Polyetherquinoxalines GENERAL ELECTRIC CO 2 Aug 1974 [23 Nov 1973] 34253/74 Heading C3R The invention comprises polyetherquinoxalines having recurring units of formula where R is hydrogen or a hydrocarbon radical, R1 is a divalent aromatic radical and R2 is a tetravalent aromatic radical. The polymers are obtained by reacting a tetracarbonyl compound of formula with a tetra-amine of formula at 25‹ to 200‹ C. In examples polymers are obtained in which R is phenyl, R1 radicals are derived from biphenyl and diphenylmethane, and R2 radicals are derived from biphenyl, benzophenone, diphenylether and diphenylsulphone; one polymer is mixed with fume silica.

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01-09-1966 дата публикации

Fungicidal compositions and halogenated quinoxalines

Номер: GB0001041011A
Принадлежит:

The invention comprises compounds of the formula where R1 and R2 are hydrogen, alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, hydroxy, halogen or alkoxy and R3, R4, R5 and R6 are hydrogen, halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, acylamino, nitro or substituted alkyl, at least three of R1-R6 being halogen, and salts thereof. Such compounds may be prepared by reacting an R3-R6-substituted o-phenylenediamine with R1CO.-COR2 or with an oxime derived therefrom; or by conversion of one substituent into another. Examples are given. Analogous compounds.-6-Fluoro-, 6-methyl-, 6,7-dinitro- and 2(3)-methyl-5,7-dichloro-quinoxalines are made similarly. 6-Acetylaminoquinoxaline is made by acetylation of the 6-amino-compound. Other compounds which can be made by the above methods include 6-amino-, 6-dimethylamino- and 6-chloroethylquinoxaline. These and other quinoxalines are fungicides (see Division A5).ALSO:Fungicidal compositions contain as active ...

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25-06-1969 дата публикации

Pyrrole Aldehydes

Номер: GB0001156477A
Принадлежит:

... 1,156,477. Pyrrole aldehydes. R. FIRMENICH, G. FIRMENICH, R. E. FIRMENICH, and F. H. FIRMENICH, [trading as FIRMENICH & CIE.]. 2 May, 1966 [30 April, 1965; 18 April, 1966], No. 2378/69. Divided out of 1,156,472. Heading C2C. [Also in Division A2] The invention relates to compounds having the formulµ where R represents an amyl, alpha-methylbuty or thenyl group; and where R1 represents a butyl, amyl, alphamethylbutyl or furfuryl group. Examples describe the preparation of all the above compounds.

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30-09-2001 дата публикации

Benzoheterocycles and their use mek inhibitors

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Автор:
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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

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31-01-1990 дата публикации

FUNGICIDES

Номер: AP0008900147D0
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30-04-2006 дата публикации

Novel phenyl-propargylether derivatives

Номер: AP0000001601A
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20-03-1991 дата публикации

Fungicides

Номер: AP0000000127A
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Compounds having ...

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19-01-2005 дата публикации

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases.

Номер: AP0000001362A
Принадлежит:

This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or t cell activation and proliferation ...

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Sulfonamide inhibitors of aspartyl protease

Номер: AP0000001717A
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31-01-1990 дата публикации

FUNGICIDES

Номер: AP0008900147A0
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31-12-1999 дата публикации

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

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31-12-2000 дата публикации

Sulfonamide inhibitors of aspartyl protease

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31-12-1999 дата публикации

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Номер: AP0009901711A0
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31-12-2002 дата публикации

Novel phenylpropargylether derivatives

Номер: AP2002002649A0
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30-06-2003 дата публикации

Guanidinobenzamides as MC4-R agonists

Номер: AP2003002755A0
Принадлежит:

Compounds of formula (IA) and (IB) arc new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type Tl diabetes, and may be provided as pharmaceutical formulations in conjunction with a pliarmaceutically acceptable carrier- ...

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31-12-1999 дата публикации

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Номер: AP0009901710A0
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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

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30-09-2001 дата публикации

Benzoheterocycles and their use as MEK inhibitors.

Номер: AP2001002224A0
Принадлежит:

The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.

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15-09-2006 дата публикации

Novel phenyl-propargylether derivatives.

Номер: OA0000012830A
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30-04-1984 дата публикации

New derivative of the isopropylamino pyrimidin, its preparation and compositions therapeutic containing its compounds.

Номер: OA0000007230A
Автор: ESANU ANDRE
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13-05-2005 дата публикации

Benzoheterocycles and their use as MEK inhibitors.

Номер: OA0000011746A
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31-12-2002 дата публикации

Novel phenylpropargylether derivatives

Номер: AP0200202649A0
Автор:
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30-06-2003 дата публикации

Guanidinobenzamides as mc4-r agonists

Номер: AP0200302755A0
Автор:
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31-12-1999 дата публикации

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31-12-1999 дата публикации

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31-12-2000 дата публикации

Sulfonamide inhibitors of aspartyl protease

Номер: AP0200002023D0
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31-12-1999 дата публикации

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31-12-2002 дата публикации

Novel phenylpropargylether derivatives

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30-06-2003 дата публикации

Guanidinobenzamides as mc4-r agonists

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30-09-2001 дата публикации

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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

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31-12-2000 дата публикации

Sulfonamide inhibitors of aspartyl protease

Номер: AP0200002023A0
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25-09-1979 дата публикации

PROCEDURE FOR THE PRODUCTION OF COLORPHOTOGRAPHIC PICTURES AFTER THE SILVER COLOR BLEACHING PROCESS

Номер: AT0000352527B
Автор:
Принадлежит:

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15-05-1988 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN CHINOXALIN-1,4-DIOXID-DERIVATEN UND VON DEREN SALZEN UND ISOMEREN

Номер: ATA246481A
Автор:
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15-09-2009 дата публикации

ALPHA SULFONYLAMINO ACETONITRILE ONE

Номер: AT0000440080T
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15-02-1979 дата публикации

VERFAHREN ZUR HERSTELLUNG FARBPHOTOGRAPHISCHER BILDER NACH DEM SILBERFARB- BLEICHVERFAHREN

Номер: ATA366477A
Автор:
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15-02-1979 дата публикации

PROCEDURE FOR THE PRODUCTION OF COLORPHOTOGRAPHIC PICTURES AFTER THE SILVER COLOR BLEACHING PROCESS

Номер: AT0000366477A
Автор:
Принадлежит:

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15-02-1979 дата публикации

PROCEDURE FOR THE PRODUCTION OF COLORPHOTOGRAPHIC PICTURES AFTER THE SILVER COLOR BLEACHING PROCESS

Номер: AT0000366577A
Автор:
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15-01-1997 дата публикации

RETROVIRALE PROTEASE INHIBITORS

Номер: AT0000147378T
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15-04-1993 дата публикации

FUNGICIDES.

Номер: AT0000087613T
Принадлежит:

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27-09-2012 дата публикации

Quinoxaline Derivative, and Light Emitting Element, Light Emitting Device, and Electronic Device Using the Quinoxaline Derivative

Номер: US20120242936A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

To provide a new bipolar organic compound. In particular, to provide a bipolar organic compound having excellent heat resistance and to provide a bipolar organic compound which is electrochemically stable. Further, to provide a light emitting element and a light emitting device of which a driving voltage and power consumption are reduced by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have excellent heat resistance by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have a long life by using a new bipolar organic compound.

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06-06-2013 дата публикации

CO-CRYSTAL INTERMEDIATES OF ROSUVASTATIN AND METHODS OF USING SAME

Номер: US20130143890A1

Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions. 2. The method of claim 1 , wherein Rosuvastatin is a calcium salt.3. The method of wherein step (a) further comprises the addition of a conformer to a solution of Rosuvastatin in Toluene claim 1 , MIK or water.4. The method of wherein step (a) is performed at a temperature below about 40° C.5. A co-crystal of Rosuvastatin selected from the group consisting of:Rosuvastatin 2-aminopyrimidine hemihydrate,Rosuvastatin pyrazine hydrate,Rosuvastatin quinoxaline (1:2).6. The co-crystal of Rosuvastatin of comprising Rosuvastatin 2-aminopyrimidine hemihydrate.7. The co-crystal of Rosuvastatin of having a Powder X-Ray Diffractogram (PXRD) with characteristic peaks expressed in 2 Theta value of: 9.40 (vs) claim 6 , 13.50 (s) claim 6 , 14.08 (m) claim 6 , 15.15 (m) claim 6 , 18.59 (m) claim 6 , 21.67 (m) claim 6 , 22.16 (m) claim 6 , 22.21 (m) claim 6 , 22.66 (m) claim 6 , (+/−) 0.10; wherein (vs)=very strong intensity claim 6 , (s)=strong intensity claim 6 , and (m)=medium intensity.8. The co-crystal of Rosuvastatin of having a melting point of about 109.4° C.9. A method for treating conditions associated with hypercholesterolemia comprising administering a co-crystal of Rosuvastatin according to .10. The method of wherein the co-crystal of Rosuvastatin is the co-crystal Rosuvastatin pyrazine hydrate.11. A pharmaceutical composition comprising the co-crystal of Rosuvastatin according to and one or more pharmaceutically acceptable excipients claim 5 , carriers and/or diluents. This application claims priority to and benefit of European Patent Application No. 11192188.8 filed Dec. 6, 2011, the contents of which are incorporated by reference in their entirety.The present invention ...

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03-10-2013 дата публикации

HETEROCYCLIC COMPOUNDS FOR TREATING OR PREVENTING DISORDERS CAUSED BY REDUCED NEUROTRANSMISSION OF SEROTONIN, NOREPHNEPHRINE OR DOPAMINE

Номер: US20130261081A1
Принадлежит:

A heterocyclic compound represented by the general formula (1) or a salt thereof: 6. The heterocyclic compound represented by the general formula (1) or a salt thereof according to claim 5 , which is selected from(4aS,8aR)-1-(4-chlorophenyl)-3,3-dimethyldecahydroquinoxaline,2-chloro-4-((4aS,8aS)-3,3-dimethyloctahydroquinoxalin-1(2H)-yl)benzonitrile,(4aS,8aR)-1-(3-chloro-4-fluorophenyl)-3,3-dimethyldecahydroquinoxaline,(4aS,8aR)-1-(7-fluorobenzofuran-4-yl)-3,3-dimethyldecahydroquinoxaline,5-((4aR,8aS)-3,3-dimethyloctahydroquinoxalin-1(2H)-yl)-1-methyl-1H-indole-2-carbonitrile,(4a′R,8a′S)-4′-(7-methoxybenzofuran-4-yl)octahydro-1′H-spiro[cyclobutane-1,2′-quinoxaline],(4aS,8aR)-1-(6,7-difluorobenzofuran-4-yl)-3,3-dimethyldecahydroquinoxaline,5-((4aS,8aS)-3,3-dimethyloctahydroquinoxalin-1(2H)-yl)-1H-indole-2-carbonitrile,(4aS,8aR)-1-(7-chloro-2,3-dihydro-1H-inden-4-yl)-3,3-dimethyldecahydroquinoxaline,6-((4aS,8aS)-3,3-dimethyloctahydroquinoxalin-1(2H)-yl)-2-naphthonitrile,(4aS,8aS)-3,3-dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-4-yOdecahydroquinoxaline, and(4aS,8aS)-1-(4-(difluoromethoxy)-3-fluorophenyl)-3,3-dimethyldecahydroquinoxaline.7. A pharmaceutical composition comprising a heterocyclic compound represented by the general formula (1) or a salt thereof according to as an active ingredient and a pharmaceutically acceptable carrier.8. A prophylactic and/or therapeutic agent for disorders caused by reduced neurotransmission of serotonin claim 1 , norepinephrine or dopamine claim 1 , comprising as an active ingredient a heterocyclic compound of general formula (1) or a salt thereof according to .9. A prophylactic and/or therapeutic agent according to claim 8 , wherein the disorder is selected from the group consisting of depression claim 8 , depression status caused by adjustment disorder claim 8 , anxiety caused by adjustment disorder claim 8 , anxiety caused by various diseases claim 8 , generalized anxiety disorder claim 8 , phobia claim 8 , obsessive-compulsive disorder ...

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03-10-2013 дата публикации

Novel Substituted Bicyclic Aromatic Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20130261123A1
Принадлежит:

The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 2. The compound of wherein when Zand Zare both N claim 1 , and Zis CR claim 1 , then Ris selected from the group consisting of hydrogen claim 1 , C-Calkyl claim 1 , fluorinated C-Calkyl claim 1 , and cyano.3. The compound of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}5. The compound of wherein A is COOH.7. The compound of wherein when Zis N claim 6 , and Zis CR claim 6 , then Ris selected from the group consisting of hydrogen claim 6 , C-Calkyl claim 6 , fluorinated C-Calkyl claim 6 , and cyano.8. The compound of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}11. The compound of wherein Ris selected from the group consisting of hydrogen claim 10 , C-Calkyl claim 10 , fluorinated C-Calkyl claim 10 , and cyano.12. The ...

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14-11-2013 дата публикации

HERBICIDAL COMPOUNDS

Номер: US20130303370A1
Принадлежит:

The present invention provides a compound of formula (I) wherein Ris of sub-formula (a) or (b) and wherein the other substituents are as defined in the specification. The compounds of formula (I) are potentially useful as herbicides. 2. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , Cfluoroalky claim 1 , C-Calkoxy claim 1 , or Cfluoroalkoxy.3. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , methyl or ethyl4. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently C-Calkyl claim 1 , C-C-fluoroalkyl claim 1 , C-Calkenyl claim 1 , C-C-fluoroalkenyl claim 1 , Cchloroalkenyl claim 1 , C-Calkynyl claim 1 , C-Ccycloalkyl claim 1 , C-Ccycloalkyl-CH— claim 1 , or phenyl.5. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , Cfluoroalkyl-CH— claim 1 , vinyl claim 1 , allyl claim 1 , Cfluoroalkenyl claim 1 , propargyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclopropyl-methyl- claim 1 , or phenyl.6. The compound of formula (I) according to claim 1 , wherein Ris of sub-formula (a) and claim 1 ,{'sup': 4a', '4e, 'sub': 1', '3', '1', '2', '3', '2', '2', '2, 'Rand Rare independently hydrogen, fluorine, chlorine, bromine, methyl, Cfluoroalkyl (e.g. CF), methoxy, Cfluoroalkoxy (e.g. CHFO, CFO or CHFO, in particular CHFO), or methyl-S(O)—;'}{'sup': 4b', '4c', '4d', '7, 'sub': 1', '4', '1', '2', '2', '2', '3', '5', '1', '3', '1', 'r', '3', '2', '2', '2', '1', '3', '2', '1', '3', '2', '2, 'R, Rand Rare independently hydrogen, halogen, C-Calkyl, Cfluoroalkyl, methoxymethyl-, MeOCHCHOCH—, C-Ccycloalkyl, C-Calkoxy, Cfluoroalkoxy, CCalkyl-S(O)—, HN—S(O)—, C-Calkyl-NH—S(O)—, or (C-Calkyl)N—S(O)—; phenyl or phenyl substituted by ...

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14-11-2013 дата публикации

QUINOXALINES AND AZA-QUINOXALINES AS CRTH2 RECEPTOR MODULATORS

Номер: US20130303517A1
Принадлежит:

The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J, J, R, R, R, R, R, R, R, R, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction. 3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted at the 4 or 5 position of the illustrated bicyclic ring of Formula (I).5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of:{'sup': 6a', '6b, '(i) —C(O)—N(R)(R), and'}{'sub': '2', 'sup': 6a', '6b, '(ii) —S(O)—N(R)(R).'}6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein{'sup': '6a', 'claim-text': {'sup': 6b', 'AH', 'HC, 'Ris -Q-Ror -Q-R; or'}, '(i) Ris H and'}{'sup': 6a', '6b', '6H, '(ii) Rand Rtogether with the N atom to which they are attached form R.'}7. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris —C(O)—N(R)(R).8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein{'sup': '6a', 'Ris H and'}{'sup': 6b', 'AH', 'HC, 'Ris -Q-Ror -Q-R.'}9. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Rand Rtogether with the N atom to which they are attached form R.14. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:(14) 5-(3-phenyl-7-{[4-(trifluoromethyl)benzyl]carbamoyl}pyrido[2,3-b]pyrazin-2-yl)pentanoic acid;(14D) 5-{7-[4-chlorobenzyl)carbamoyl]-3-phenylpyrido[2,3-b]pyrazin-2-yl}pentanoic acid;(14G) 5-{3-phenyl-7-[(4-phenylpiperazin-1-yl)carbonyl]pyrido[2,3-b]pyrazin-2-yl}pentanoic acid;(15A) 5-(3-phenyl-7-{[(1R)-1- ...

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14-01-2016 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20160009663A1
Принадлежит:

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris hydrogen claim 1 , cyano claim 1 , halo claim 1 , hydroxy claim 1 , carboxy claim 1 , optionally substituted alkoxy claim 1 , optionally substituted aryloxy claim 1 , optionally substituted alkoxycarbonyl claim 1 , optionally substituted alkyl claim 1 , optionally substituted aryl claim 1 , optionally substituted heteroaryl claim 1 , optionally substituted amino claim 1 , optionally substituted acyl claim 1 , optionally substituted alkoxycarbonyl claim 1 , optionally substituted aminocarbonyl claim 1 , optionally substituted aminosulfonyl claim 1 , optionally substituted carbamimidoyl claim 1 , or optionally substituted alkynyl.3. (canceled)4. The compound or pharmaceutically acceptable salt of claim 2 , wherein Ris optionally substituted aryl claim 2 , optionally substituted heterocycloalkyl claim 2 , or optionally substituted heteroaryl.5. (canceled)6. The compound or pharmaceutically acceptable salt of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently hydrogen claim 1 , halo claim 1 , cyano claim 1 , optionally substituted alkoxy claim 1 , or optionally substituted alkyl.7. (canceled)8. (canceled)9. The compound or pharmaceutically acceptable salt of wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently hydrogen claim 1 , cyano claim 1 , halo claim 1 , optionally substituted alkoxy claim 1 , optionally substituted alkyl claim 1 , optionally substituted acyl claim 1 , optionally substituted alkoxycarbonyl claim 1 , optionally substituted aminocarbonyl claim 1 , or optionally substituted aminosulfonyl.1012.-. (canceled)13. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris hydrogen claim 1 , optionally substituted lower alkyl claim 1 , optionally substituted cycloalkyl claim 1 , optionally substituted ...

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28-01-2016 дата публикации

INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE (IDO)

Номер: US20160022619A1
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 9. The compound according to wherein the ICin the HEK Human IDO-1 assay is <10 nM.10. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable carrier or diluent.11. (canceled)12. (canceled)13. (canceled)14. A method for the treatment of a disease selected from the group consisting of cancer claim 1 , viral infections claim 1 , depression claim 1 , organ transplant rejection and autoimmune disease in a patient comprising administering to said patient a therapeutically effective amount of a compound or pharmaceutically acceptable salt thereof according to .15. The method according to further comprising administering to the patient a therapeutically effective amount of at least one of an anti-viral agent claim 14 , a chemotherapeutic agent claim 14 , an immunosuppressant claim 14 , radiation claim 14 , an anti-tumor vaccine claim 14 , an antiviral vaccine claim 14 , cytokine therapy or a tyrosine kinase inhibitor prior to claim 14 , simultaneously with or after administration of the compound.16. A method of inhibiting the activity of indoleamine 2 claim 1 ,3-dioxygenase comprising contacting said indoleamine 2 claim 1 ,3-dioxygenase with a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.17. The method of claim 14 , wherein said disease is cancer.18. The method of wherein said cancer is selected from the group consisting of colon claim 17 , glioblastoma claim 17 , pancreatic claim 17 , breast claim 17 , prostate claim 17 , lung claim 17 , ovarian claim 17 , cervical claim 17 , renal claim 17 , head and neck claim 17 , lymphoma claim 17 , leukemia and melanoma.19. A ...

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25-01-2018 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20180022714A1
Принадлежит:

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. 145.-. (canceled)47. The method of claim 46 , wherein Ris hydrogen claim 46 , cyano claim 46 , halo claim 46 , hydroxy claim 46 , carboxy claim 46 , optionally substituted alkoxy claim 46 , optionally substituted aryloxy claim 46 , optionally substituted alkoxycarbonyl claim 46 , optionally substituted alkyl claim 46 , optionally substituted aryl claim 46 , optionally substituted heteroaryl claim 46 , optionally substituted heterocycloalkyl claim 46 , optionally substituted amino claim 46 , optionally substituted acyl claim 46 , optionally substituted alkoxycarbonyl claim 46 , optionally substituted aminocarbonyl claim 46 , optionally substituted aminosulfonyl claim 46 , optionally substituted carbamimidoyl claim 46 , or optionally substituted alkynyl.48. The method of claim 46 , wherein Ris optionally substituted aryl claim 46 , optionally substituted heterocycloalkyl claim 46 , or optionally substituted heteroaryl.49. The method of claim 46 , wherein Ris optionally substituted morpholinyl claim 46 , optionally substituted piperazinyl claim 46 , optionally substituted pyrrolidinyl claim 46 , optionally substituted piperidinyl claim 46 , optionally substituted imidazolyl claim 46 , optionally substituted pyrazolyl claim 46 , or optionally substituted pyridyl.50. The method of claim 46 , wherein R claim 46 , R claim 46 , R claim 46 , and Rare independently hydrogen claim 46 , halo claim 46 , cyano claim 46 , optionally substituted alkoxy claim 46 , or optionally substituted alkyl.51. The method of claim 46 , wherein R claim 46 , R claim 46 , R claim 46 , and Rare independently hydrogen or halo.52. The method of claim 46 , wherein R claim 46 , R claim 46 , R claim 46 , and Rare independently hydrogen claim 46 , cyano claim 46 , halo claim 46 , optionally substituted alkoxy claim 46 , optionally substituted alkyl claim 46 , optionally substituted ...

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24-04-2014 дата публикации

AMINOQUINOXALINE DERIVATIVES FOR TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20140113903A1
Принадлежит:

The present invention relates to compounds of formula (I) below: for which: —X represents a hydrogen atom, a halogen atom, a group NOor NH, —Rrepresents H or —CH—C≡CH, and —Rand Reach represent, independently of one another, a hydrogen atom; a saturated or unsaturated, linear or branched hydrocarbon-based chain comprising from 1 to 10 carbon atoms; or an optionally substituted aryl group, and also the pharmaceutically acceptable salts thereof, the stereoisomers thereof or mixtures of stereoisomers thereof in any proportion, in particular for use thereof as a medicament, in particular in the treatment or prevention of neurodegenerative diseases, and also the processes for the preparation thereof and the pharmaceutical compositions comprising same. 118.-. (canceled)20. The method according to claim 19 , wherein the mixture of stereoisomers is a mixture of enantiomers.21. The method according to claim 20 , wherein the mixture of enantiomers is a racemic mixture.22. The method according to claim 19 , wherein X represents a hydrogen atom claim 19 , a bromine atom claim 19 , an NHgroup or an NOgroup.23. The method according to claim 19 , wherein X represents a hydrogen atom.24. The method according to claim 19 , wherein Rrepresents H.25. The method according to claim 19 , wherein Rand Reach represent claim 19 , independently of one another claim 19 , a hydrogen atom; a saturated or unsaturated claim 19 , linear or branched hydrocarbon chain comprising 1 to 10 carbon atoms; or an aryl group optionally substituted by one or more groups selected from the group consisting of a halogen atom claim 19 , (C-C)alkyl claim 19 , (C-C)alkoxy claim 19 , aryl claim 19 , N claim 19 , NO claim 19 , NHand —NH—((C-C)alkyl).26. The method according to claim 19 , wherein Rand Reach represent claim 19 , independently of one another claim 19 , a hydrogen atom; a saturated or unsaturated claim 19 , linear or branched hydrocarbon chain comprising 1 to 10 carbon atoms; or an aryl group optionally ...

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04-02-2016 дата публикации

HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20160031876A1
Принадлежит:

Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. 5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —C(O)NH(OH).6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —N(OH)C(O)R.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris chosen from hydrogen and lower alkyl.8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Ris lower alkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 2.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 3.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein claim 1 , for each occurrence claim 1 , Ris independently chosen from halo and lower alkyl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently chosen from halo claim 1 , alkyl claim 1 , cycloalkyl claim 1 , haloalkyl claim 1 , hydroxyl claim 1 , alkoxy claim 1 , and nitrile.15. The compound of claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently chosen from halo claim 14 , lower alkyl claim 14 , and haloalkyl.16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris chosen from phenyl claim 15 , 2-fluorophenyl claim 15 , 2-methyl claim 15 , 3-fluoro-2-methylphenyl and 2-methylphenyl.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof ...

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31-01-2019 дата публикации

NOVEL MONOTHIOL MUCOLYTIC AGENTS

Номер: US20190031679A1
Принадлежит:

Provided are mucolytic agents represented by formula (Ia)-(Id): 126.-. (canceled)28. The compound of claim 27 , wherein{'sup': 5', '7', '10', '7', '10', '10', '10', '8', '8', '8, 'sub': 2', 'm', '2', 'm', '2', 'm', '2', 'm', '2', 'n', '2, 'each Ris, independently, hydrogen, —O—(CH)—NRR, —O—(CH)—NRR7, —O—(CH)—NRR, or —O—(CH)—NR—CH(CHOR)(CHOR)—CHOR;'}{'sup': 7', '8', '8, 'sub': 2', 'm', '2, 'each Ris, independently, hydrogen or —CH(CHOR)—CHOR; and'}{'sup': '10', 'sub': 2', 'n', '2, 'each Ris, independently, —H or —CH—(CHOH)—CHOH.'}29. The compound of claim 28 , wherein{'sup': 5', '10', '10, 'sub': 2', 'm, 'each Ris, independently hydrogen or —O—(CH)—NRR;'}{'sup': '10', 'sub': 2', 'n', '2, 'each Ris —CH—(CHOH)—CHOH;'}each m is 1; andeach n is 4.31. The compound of claim 30 , wherein Ris hydrogen.33. The compound of claim 32 , which is an acid addition salt of an inorganic acid or an organic acid selected from the group consisting of hydrochloric acid claim 32 , hydrobromic acid claim 32 , sulfuric acid claim 32 , phosphoric acid claim 32 , nitric acid claim 32 , acetic acid claim 32 , oxalic acid claim 32 , tartaric acid claim 32 , succinic acid claim 32 , maleic acid claim 32 , furmaric acid claim 32 , gluconic acid claim 32 , citric acid claim 32 , malic acid claim 32 , ascorbic acid claim 32 , benzoic acid claim 32 , tannic acid claim 32 , palmitic acid claim 32 , alginic acid claim 32 , polyglutamic acid claim 32 , naphthalensulfonic acid claim 32 , methanesulfonic acid claim 32 , p-toluenesulfonic acid claim 32 , naphthalenedisulfonic acid claim 32 , polygalacturonic acid claim 32 , malonic acid claim 32 , sulfosalicylic acid claim 32 , glycolic acid claim 32 , 2-hydroxy-3-naphthoate claim 32 , pamoate claim 32 , salicylic acid claim 32 , stearic acid claim 32 , phthalic acid claim 32 , mandelic acid claim 32 , and lactic acid.34. The compound of claim 32 , which is an acid addition salt of hydrochloric acid.36. The compound of claim 30 , wherein Ris —C(═O)—R.37. ...

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25-02-2021 дата публикации

Heterocyclic Lipoxin Analogs and Uses Thereof

Номер: US20210053927A1
Принадлежит:

The present invention relates to a compound of formula (I): wherein L is an optionally substituted heterocyclic group excluding unsubstituted monocyclic pyridine groups; wherein a is 0, 1 or 2; wherein Ris H or with Ris a bond; wherein Ris an optionally substituted alkoxy or aryloxy group, or with Rforms a bond; wherein Ris an optionally substituted alkyl group; and wherein Ris CH, CMeor O. Such compounds may be used in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis. 2. The compound according to claim 1 , wherein L is selected from an optionally substituted pyrimidine claim 1 , quinoline claim 1 , isoquinoline claim 1 , quinazoline claim 1 , five-membered heterocyclic ring or benzo-fused five membered heterocyclic ring.6. The compound according to claim 1 , wherein Ris a Calkoxy group.8. The compound according to claim 1 , wherein Ris an optionally substituted Calkyl group.11. A composition comprising a compound according to and a pharmaceutically acceptable diluent claim 1 , lubricant or carrier.12. A medicament comprising the composition according to .13. The medicament according to for use in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis is beneficial.14. The medicament according to for use in the treatment or prophylaxis of atherosclerosis.15. The medicament according to for use in the treatment or prophylaxis of macrovascular complications claim 12 , microvascular complications claim 12 , or both claim 12 , associated with a metabolic disease.16. A medicament comprising the compound of .17. The medicament of for use in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis is beneficial.18. The medicament of for use in the ...

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23-02-2017 дата публикации

SUBSTITUTED QUINOXALINES AS B-RAF KINASE INHIBITORS

Номер: US20170050938A1
Принадлежит:

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. 152-. (canceled)54. The compound or pharmaceutically acceptable salt of claim 53 , wherein Ris hydrogen claim 53 , cyano claim 53 , optionally substituted alkoxy claim 53 , optionally substituted aryloxy claim 53 , optionally substituted amino claim 53 , optionally substituted alkyl claim 53 , optionally substituted heterocycloalkyl claim 53 , optionally substituted aryl claim 53 , optionally substituted pyridyl claim 53 , optionally substituted pyrazinyl claim 53 , optionally substituted pyrimidinyl claim 53 , optionally substituted imidazolyl claim 53 , optionally substituted isoxazolyl claim 53 , optionally substituted oxazolyl claim 53 , optionally substituted tetrazolyl claim 53 , optionally substituted pyridazinyl claim 53 , or optionally substituted triazolyl.55. The compound or pharmaceutically acceptable salt of claim 54 , wherein Ris optionally substituted aryl claim 54 , optionally substituted heterocycloalkyl claim 54 , optionally substituted pyridyl claim 54 , optionally substituted pyrazinyl claim 54 , optionally substituted pyrimidinyl claim 54 , optionally substituted imidazolyl claim 54 , optionally substituted isoxazolyl claim 54 , optionally substituted oxazolyl claim 54 , optionally substituted tetrazolyl claim 54 , or optionally substituted triazolyl.56. The compound or pharmaceutically acceptable salt of claim 53 , wherein R claim 53 , R claim 53 , R claim 53 , and Rare independently hydrogen claim 53 , halo claim 53 , cyano claim 53 , optionally substituted alkoxy claim 53 , or optionally substituted alkyl.57. The compound or pharmaceutically acceptable salt of claim 56 , wherein R claim 56 , R claim 56 , R claim 56 , and Rare independently hydrogen or halo.58. The compound or pharmaceutically acceptable salt of claim 53 , wherein Ris hydrogen claim 53 , cyano claim 53 , or optionally substituted alkyl.59. The compound or ...

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26-02-2015 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20150057276A1
Принадлежит:

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris hydrogen claim 1 , cyano claim 1 , optionally substituted alkoxy claim 1 , optionally substituted aryloxy claim 1 , optionally substituted amino claim 1 , optionally substituted alkyl claim 1 , optionally substituted heterocycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl.3. The compound or pharmaceutically acceptable salt of claim 2 , wherein Ris optionally substituted aryl claim 2 , optionally substituted heterocycloalkyl claim 2 , or optionally substituted heteroaryl.4. The compound or pharmaceutically acceptable salt of claim 3 , wherein Ris optionally substituted morpholinyl claim 3 , optionally substituted piperazinyl claim 3 , optionally substituted pyrrolidinyl claim 3 , optionally substituted piperidinyl claim 3 , optionally substituted imidazolyl claim 3 , optionally substituted pyrazolyl claim 3 , or optionally substituted pyridyl.5. The compound or pharmaceutically acceptable salt of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently hydrogen claim 1 , halo claim 1 , cyano claim 1 , optionally substituted alkoxy claim 1 , or optionally substituted alkyl.6. The compound or pharmaceutically acceptable salt of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , and Rare independently hydrogen or halo.7. The compound or pharmaceutically acceptable salt of claim 6 , wherein R claim 6 , R claim 6 , R claim 6 , and Rare hydrogen.8. The compound or pharmaceutically acceptable salt of claim 5 , wherein Ris hydrogen or halo.9. The compound or pharmaceutically acceptable salt of claim 8 , wherein Ris halo.10. The compound or pharmaceutically acceptable salt of claim 9 , wherein Ris fluoro or chloro.11. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris hydrogen claim 1 , ...

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03-03-2016 дата публикации

IDO INHIBITORS

Номер: US20160060237A1
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention. Formula (I). 3. The compound according to wherein X is NRRand/or a stereoisomer claim 2 , a tautomer or a pharmaceutically acceptable salt thereof.4. The compound according to wherein X is ORand/or a stereoisomer claim 2 , a tautomer or a pharmaceutically acceptable salt thereof.7. A compound according to which is 3-(4-(diisobutylamino)-3-(3-(3-methylisoxazol-5-yl)ureido)phenyl)butanoic acid claim 1 , and/or a stereoisomer claim 1 , a tautomer or a pharmaceutically acceptable salt thereof.8. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable carrier or diluent.9. (canceled)10. (canceled)11. (canceled)12. A method for the treatment of a disease selected from the group consisting of cancer claim 1 , viral infections claim 1 , depression claim 1 , and inflammatory disorders in a patient comprising administering to said patient a therapeutically effective amount of a compound or pharmaceutically acceptable salt thereof according to .13. The method according to further comprising administering to the patient a therapeutically effective amount of at least one of an anti-viral agent claim 12 , a chemotherapeutic agent claim 12 , an immunosuppressant claim 12 , radiation claim 12 , an anti-tumor vaccine claim 12 , an antiviral vaccine claim 12 , cytokine therapy or a tyrosine kinase inhibitor prior to claim 12 , simultaneously with or after administration of the compound.14. A method of inhibiting the activity of indoleamine 2 claim 1 ,3-dioxygenase comprising contacting said indoleamine 2 claim 1 ,3-dioxygenase with a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.15. ...

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20-02-2020 дата публикации

ANTI-FIBROTIC COMPOUNDS

Номер: US20200055814A1
Принадлежит:

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound KIN or composition described herein. (Formula (I)) 235-. (canceled)36. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , whereinG is hydrogen;m is H or 2; and{'sup': '6', 'each occurrence of Ris, independently, F or Cl.'}37. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '7', 'G is C(O)R;'}m is 0;{'sup': 7', '9, 'Ris NHR; and'}{'sup': '9', 'Ris tetrazolyl, pyridinyl, pyrazolyl, imidazolyl, or triazolyl, each of which is optionally substituted with up to two alkyl groups.'}40. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , whereinX is O;{'sup': '10', 'Y is NR; and'}{'sup': '10', 'sub': '1-4', 'Ris Calkyl.'}41. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein{'sup': '10', 'X is NR; and'}Y is O.42. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein Rand Rtogether with the carbon atom to which they are attached form a carbonyl.44. A compound selected from the group consisting of:(E)-N-(2-fluorophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (1);(E)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)-N-(2-(5-methyl-1H-1,2,4-triazol-3-yl)phenyl)acrylamide (2);(E)-N-(2-chlorophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (3);(E)-N-(2-bromophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (4);(E)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)-N-(o-tolyl)acrylamide (5);(E)-N-(2-cyanophenyl)-3-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)acrylamide (6);(E)-N-(3,4-dichlorophenyl)-3-(3- ...

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05-03-2015 дата публикации

Cadherin-11 Inhibitors and Methods of Use Thereof

Номер: US20150064168A1
Принадлежит:

Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis. 2. (canceled)3. (canceled)4. (canceled)5. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. A composition comprising a compound of and a pharmaceutically acceptable carrier.13. (canceled)15. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)24. (canceled)26. (canceled)27. (canceled)28. (canceled)31. The method of claim 14 , wherein the cadherin-11 related disease is rheumatoid arthritis.32. The method of claim 14 , wherein the cadherin-11 related disease is a cancer.33. The method of claim 32 , wherein the cancer is breast cancer claim 32 , prostate cancer claim 32 , glioma claim 32 , glioblastoma claim 32 , myeloma claim 32 , leukemia claim 32 , a poor prognosis or invasive cancer claim 32 , a basal-like cancer claim 32 , a mesenchymal-like cancer claim 32 , or metastatic.34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. (canceled)42. (canceled)43. The method of claim 14 , wherein the method further comprises administering a second therapeutic agent to the subject.44. The method of claim 43 , wherein the second therapeutic agent is a chemotherapeutic agent or an anti-inflammatory agent.45. (canceled)46. A method of preventing or treating cancer in a subject claim 43 , comprising:a) selecting a subject with a poor prognosis cancer; andb) administering to the subject a cadherin-11 inhibitor.47. (canceled)48. The method of claim 46 , wherein the cadherin-11 inhibitor is an antibody. This application is a continuation of U.S. application Ser. No. 13/148,579, filed Feb. 8, 2012, which is currently pending and which is a U.S. national stage filing of PCT/US10/23556, filed Feb. 9, 2010, which claims priority to U.S. Provisional Application No. 61/151,038, filed Feb. 9, 2009. These ...

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02-03-2017 дата публикации

CARRIER GENERATION MATERIAL AND ORGANIC LIGHT-EMITTING DIODE

Номер: US20170062771A1
Принадлежит:

A carrier generation material is provided, which has a chemical structure of: 7. An organic light-emitting diode , comprising:an anode;a cathode;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a carrier generation material layer, including the carrier generation material as claimed in , disposed between the anode and the cathode;'}a first light-emitting layer disposed between the anode and the carrier generation material layer; anda second light-emitting layer, disposed between the cathode and the carrier generation material layer. This Application claims priority of Taiwan Patent Application No. 104127446, filed on Aug. 24, 2015, the entirety of which is incorporated by reference herein.The disclosure relates to an organic light-emitting diode, and in particular it relates to the composition of a carrier generation layer thereof.Compared to inorganic compounds, organic compounds are more varied in terms of their material system. Organic materials with any function can be synthesized through the appropriate molecular designs. The films of organic compounds have extremely high flexibility and excellent processability. In recent years, functional organic materials with the above advantages have attracted attention among those in the photonics and electronics industries.Because organic compounds are inherently free of carriers, they normally have excellent insulative properties. In the electronics field, these organic compounds generally served as insulators, being used in insulation materials, protection materials, encapsulation materials, etc. However, a mechanism wherein a large current flows through organic materials was initially developed in the electronics field. For example, organic films with a total thickness of about 100 nm can be disposed between electrodes. Organic hole transport layers and organic electron transport layers are stacked to constitute a stack of the organic films, and a light-emitting material (phosphorescent material) may serve as an ...

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28-02-2019 дата публикации

QUINOXALINE AND PYRIDOPYRAZINE DERIVATIVES AS PI3KB INHIBITORS

Номер: US20190062311A1
Принадлежит:

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) 2. The compound according to claim 1 , wherein{'sup': '1a', 'sub': '1-4', 'Rrepresents Calkyl;'}{'sup': 5a', '5b, 'Rand Reach independently are selected from the group consisting of hydrogen,'}{'sub': 1-4', '1-4', '2', '2', '2', '1-4', '2', '3-6, 'Calkyl, —O—Calkyl, —S(═O)—NH, —S(═O)—Calkyl, —S(═O)—Ccycloalkyl,'}{'sub': '1-4', 'Calkyl substituted with one or more halo atoms, and'}{'sub': 1-4', '1-4', '2', '1-4', '1-4', '2, 'Calkyl substituted with one substituent selected from the group consisting of hydroxyl, —O—Calkyl, —S(═O)—Calkyl, —O—Calkyl-NH,'}{'sub': 1-4', '1-4', '1-4', '1-4', '2', '2', '1-4, '—O—Calkyl-NH(Calkyl), —O—Calkyl-N(Calkyl), —NH, —NH(Calkyl) and'}{'sub': 1-4', '2, '—N(Calkyl).'}7. The compound according to claim 1 , wherein{'sup': '3', 'Y represents CR;'}{'sup': 1a', '1c, 'L represents —CHR—X— or —X—CHR—;'}{'sup': '1b', 'X represents NR;'}{'sup': '1a', 'sub': '1-4', 'Rrepresents Calkyl;'}{'sup': '1c', 'sub': '1-4', 'Rrepresents hydrogen or Calkyl;'}{'sup': '1b', 'Rrepresents hydrogen.'}8. The compound according to claim 1 , wherein{'sup': 1b', '1a', '1c, 'sub': 2', '3, 'Ris taken together with Ror Rto form —(CH)—.'}10. The compound according to claim 1 , wherein Y represents CR.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and claim 1 , as active ingredient claim 1 , a therapeutically effective amount of a compound according to .12. A compound as defined in for use as a medicament.13. A compound as defined in for use in the treatment or prevention of a disease or condition selected from cancer claim 1 , autoimmune disorders claim 1 , cardiovascular diseases claim 1 , inflammatory diseases claim 1 , neurodegenerative diseases claim 1 , allergy claim 1 , pancreatitis claim 1 , asthma claim 1 , multiorgan failure claim 1 , kidney diseases claim 1 , platelet aggregation claim 1 , sperm motility claim 1 , ...

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27-02-2020 дата публикации

AIE-ACTIVE CHEMO SENSORS FOR AMINE DETECTION AND RELATED FOOD-SAFETY MONITORING

Номер: US20200062718A1
Принадлежит:

AIE-active chemosensors, according to the present teachings, exhibit UV-vis absorption change and become non-luminescent upon protonation. Upon deprotonation, the chemosensors revert to their original absorption and emission. This deprotonation process can be triggered in the presence of amines, and specifically, biogenic amines. The chemosensors can detect amine species, e.g., biogenic amines produced during food fermentation, quickly and with high sensitivity. Further, due to the AIE nature of the compounds, the chemosensors can be loaded onto a physical support and sealed inside a food package to monitor food spoilage. 4. The AIE chemosensor of claim 1 , wherein the unsubstituted imine nitrogen can be protonated.5. The AIE chemosensor of claim 4 , wherein deprotonation of the imine nitrogen produces a detectable change in light absorption.6. The AIE chemosensor of claim 4 , wherein deprotonation of the imine nitrogen produces a detectable change in light emission.7. The AIE chemosensor of claim 1 , wherein the chemosensor exhibits aggregation induced emission upon exposure to an amine.8. The AIE chemosensor of claim 7 , wherein the amine is a gaseous amine.12. A method of detecting food spoilage in a sample claim 7 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering the AIE chemosensor of to the sample; and'}detecting the presence of food spoilage by measuring light emission.13. The method of claim 12 , furthering comprising waiting for a period of time after administering the AIE chemosensor and before detecting the presence of food spoilage.14. The method of claim 12 , wherein the AIE chemosensor is loaded onto a filter paper strip prior to administering the AIE chemosensor to the sample.15. The method of claim 12 , wherein the light emission is a luminescent color change from yellow to red.16. The method of claim 12 , wherein the light emission is fluorescence in response to UV excitation.17. The method of claim 12 , wherein the food ...

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02-04-2015 дата публикации

NOVEL DIAMINE COMPOUND AND METAL COMPLEXES, AND METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUNDS

Номер: US20150094468A1
Автор: TOUGE Taichiro
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention relates to a novel diamine compound represented by the general formula (1), a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex having the diamine compound as a ligand. Furthermore, the present invention relates to methods for selectively producing optically active compounds by using any of these complexes as a catalyst. 3. A method for producing an optically active amine or an optically active compound , comprising:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'reducing an imino group of an imine compound or an unsaturated bond of a heterocyclic compound in the presence of the complex according to and a hydrogen donor.'}4. The production method according to claim 3 , wherein the hydrogen donor is hydrogen.5. The production method according to claim 3 , wherein the hydrogen donor is selected from formic acid claim 3 , alkali metal formates claim 3 , and alcohols having a hydrogen atom on a carbon atom at an α-position of a carbon atom substituted with a hydroxyl group.6. A catalyst for asymmetric reduction claim 2 , comprising the complex according to .7. A method for asymmetric reduction of an imine compound or a heterocyclic compound comprising: reducing an imino group of the imine compound or an unsaturated bond of the heterocyclic compound in the presence of a catalyst comprising the complex according to and a hydrogen doner. The present invention relates to a novel diamine compound, a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex having the diamine compound as a ligand, and methods for selectively producing optically active compounds important as precursors for synthesis of pharmaceuticals and functional materials by using any of these complexes as a catalyst.In the field of production of optically active amines, many asymmetric reactions including asymmetric reduction have been developed, and many asymmetric reactions using asymmetric metal complexes having ...

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12-05-2022 дата публикации

Heteroaromatic and Heterobicyclic Aromatic Derivatives for the Treatment of Ferroptosis-Related Disorders

Номер: US20220144826A1

The present application discloses heteroaromatic and heterobicyclic aromatic derivative compounds and compositions, and methods for treating ferroptosis-related disorders and diseases inpatients using the compounds and compositions as disclosed herein. 2. The compound of wherein Y is —N—.3. The compound of wherein X is —N—.5. The compound of wherein X and Y are —CH— claim 4 , and Z is —CH—.6. The compound of wherein X and Y are —CH— and Z is O.7. A compound selected from the group consisting of the compounds listed in Table 1.8. A pharmaceutical composition comprising a therapeutically effective amount of a compound of and a pharmaceutically acceptable excipient.9. A pharmaceutical composition comprising a therapeutically effective amount of a compound of and a pharmaceutically acceptable excipient.11. The method of wherein the ferroptosis-related disease is selected from the group consisting of lipid peroxidation-related degenerative diseases claim 9 , excitotoxic diseases claim 9 , neurodegenerative diseases claim 9 , non-apoptotic regulated cell-death diseases claim 9 , wasting- or necrosis-related diseases claim 9 , intoxication-related diseases claim 9 , and infectious diseases.12. The method of wherein the ferroptosis-related disease is selected from the group consisting of lipid peroxidation-related degenerative diseases claim 10 , excitotoxic diseases claim 10 , neurodegenerative diseases claim 10 , non-apoptotic regulated cell-death diseases claim 10 , wasting- or necrosis-related diseases claim 10 , intoxication-related diseases claim 10 , and infectious diseases. Described herein are heteroaromatic and heterobicyclic aromatic compounds, compositions and methods of using them for treatment of ferroptosis-related disorders including lipid peroxidation-related degenerative diseases, excitotoxic diseases, neurodegenerative diseases, non-apoptotic regulated cell-death diseases, wasting- or necrosis-related diseases, intoxication-related diseases, and ...

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26-03-2020 дата публикации

COMPOSITIONS AND METHODS OF MODULATING SHORT-CHAIN DEHYDROGENASE

Номер: US20200095206A1
Принадлежит:

Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein. 196-. (canceled)102: The method of claim 97 , the compound being administered to a tissue of a subject at an amount effective to increase prostaglandin levels in the tissue.103: The method of claim 97 , the compound being administered to a subject to promote wound healing claim 97 , tissue repair claim 97 , and/or tissue regeneration.104: The method of claim 97 , the compound being administered to a subject to treat at least one of oral ulcers claim 97 , gum disease claim 97 , colitis claim 97 , ulcerative colitis claim 97 , gastrointestinal ulcers claim 97 , inflammatory bowel disease claim 97 , vascular insufficiency claim 97 , Raynaud's disease claim 97 , Buerger's disease claim 97 , diabetic neuropathy claim 97 , pulmonary artery hypertension claim 97 , cardiovascular disease claim 97 , and renal disease.105: The method of claim 97 , the compound being administered to tissue of the subject to increase tissue stem cells.106: The method of claim 97 , the compound being administered to a tissue graft donor claim 97 , bone marrow graft donor claim 97 , and/or a hematopoietic stem cell donor to increase the fitness of a donor tissue graft claim 97 , a donor bone marrow graft claim 97 , and/or a donor hematopoietic stem cell graft.107: The method of claim 97 , the compound being administered to bone marrow of a subject to increase stem cells in the subject or to increase the fitness of the marrow as a donor graft.108: The method of claim 97 , the compound being administered to a preparation of hematopoietic stem cells of a subject to increase the fitness of the stem cell preparation as a donor graft or to increase the fitness of the stem cell preparation as a donor graft.109: The method of claim 97 , ...

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26-03-2020 дата публикации

Method for producing fullerene derivative

Номер: US20200095209A1
Принадлежит: Showa Denko KK

(in formula (1), C* are each carbon atoms adjacent to each other for forming a fullerene skeleton, A is a linking group having 1-4 carbon atoms for forming a ring structure with two C*, in which a portion thereof may be a substituted or condensed group).

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13-05-2021 дата публикации

PROSTAGLANDIN ANALOGS AND USES THEREOF

Номер: US20210139435A1
Принадлежит:

The present invention relates to pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, including, as an active ingredient, a prostaglandin analog or a pharmaceutically acceptable salt thereof, wherein the compound has excellent effects in inducing Nurr1, and thus, can be useful as a pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, in particular, cancer, autoimmune disease such as rheumatoid arthritis, schizophrenia, manic depression and neurodegenerative disease such as Alzheimers disease or Parkinson's disease. 2. The prostaglandin analog claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , solvate claim 1 , polymorph claim 1 , ester claim 1 , tautomer claim 1 , or prodrug thereof according to claim 1 ,{'sub': a', 'a', 'b, 'wherein X is —(C1-C8) alkyl or —(C1-C8) alkenyl which is optionally substituted with one or more substituents selected from the group consisting of hydroxyl, —(C1-C6) alkoxy, —C(═O)OR, —C(═O)NRR,'}{'sub': a', '2', 'c', 'c', 'c', '3, 'where Ris H, (C1-C8) alkyl, (C6-C9) aryl, (C6-C9) aryloxy, —NH(C6-C9)aryl, 5- to 12-membered heteroaryl having one or more heteroatom selected from the group consisting of N, O and S, said (C1-C8) alkyl, (C6-C9) aryl, 5- to 12-membered heteroaryl may be optionally substituted with halo, hydroxyl, cyano, nitro, amino, substituted amino, (C1-C6)acyl, —ONO, (C1-C8) alkoxy, (C1-C8)alkyl, substituted (C1-C8)alkyl, (C1-C8)haloalkyl, (C3-C7)cycloalkyl, (C1-C8)alkylcarboxy, —NHC(═O)R, or —C(═O)R, where Ris (C1-C8) alkyl or (C6-C9) aryl which may be optionally substituted with one or more substituents of halo, CF, (C1-C6)acyl, amino, substituted amino, cyano, nitro, (C1-C8)alkyl, substituted (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)alkoxy, (C1-C3)acyloxy, and (C6-C9)aryloxy 5- to 12-membered heterocycloalkyl having one or more heteroatoms selected from the group ...

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28-05-2015 дата публикации

NON-SYSTEMIC TGR5 AGONISTS

Номер: US20150148311A1
Принадлежит:

Compounds having the following structure (I): 29-. (canceled)11. The compound of claim 10 , wherein Y is O and Z is CRR.12. The compound of claim 10 , wherein Y is NRand Z is CRR.13. The compound of claim 10 , wherein Y is CRRand Z is O.14101-. (canceled)102. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , Ror Ris halogen claim 1 , C-alkyl claim 1 , halogen-C-alkyl claim 1 , C-alkoxy claim 1 , halogen-C-alkoxy or cyano.103. The compound of claim 102 , wherein the halogen is chloro.104105-. (canceled)106. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , Ror Ris Q.107109-. (canceled)110. The compound of claim 106 , wherein Lis —O— claim 106 , —Calkylene-; —Calkylene-NR— claim 106 , —Calkylene-NRC(═O)— claim 106 , —Calkylene-C(═O)NR— or —Calkylene-NRC(═O)NR—.111. The compound of claim 106 , wherein Q is -LCRR(CRR)G claim 106 , wherein:{'sup': 81', '82', '83', '84, 'R, R, Rand Rare independently, at each occurrence, hydrogen or hydroxyl;'}{'sub': 3', '2', '2, 'sup': '3', 'G is —CH, —CHOH, —COH or -L-I; and'}m1 is an integer ranging from 1 to 21.112. (canceled)113. The compound of claim 111 , wherein for each occurrence of Rand R claim 111 , one of Ror Ris hydrogen and the other of Ror Ris hydroxyl.115116-. (canceled)117. The compound of claim 106 , wherein Q is -L[(CH)O](CH)R claim 106 , wherein m2 is 2 or 3 claim 106 , m3 is an integer ranging from 1 to 21 and Ris hydrogen claim 106 , hydroxyl or L-I.118. (canceled)121125-. (canceled)126. A compound of any one of Examples 1-291.127. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or adjuvant.128. (canceled)129. Use of a compound of as a therapeutic active substance for the treatment of diseases which are associated with the modulation of TGR5 activity.130. A method for the treatment of diseases which are associated with the modulation of TGR5 activity claim 1 , wherein the diseases are selected ...

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02-06-2016 дата публикации

Cadherin-11 Inhibitors and Methods of Use Thereof

Номер: US20160151363A1
Принадлежит: GEORGETOWN UNIVERSITY

Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis. 2. The compound of claim 1 , wherein Ris hydroxyl.3. The compound of claim 1 , wherein Ris chloro.4. The compound of claim 1 , wherein Ris hydroxyl.5. The compound of claim 1 , wherein Ris hydroxyl claim 1 , chloro claim 1 , or carboxyl.13. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.14. A method of preventing or treating a cadherin-11 related disease in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to the subject an effective amount of a compound of .'}17. The method of claim 14 , wherein the cadherin-11 related disease is rheumatoid arthritis.18. The method of claim 14 , wherein the cadherin-11 related disease is a cancer.19. The method of claim 18 , wherein the cancer is breast cancer claim 18 , prostate cancer claim 18 , glioma claim 18 , glioblastoma claim 18 , myeloma claim 18 , leukemia claim 18 , a poor prognosis or invasive cancer claim 18 , a basal-like cancer claim 18 , a mesenchymal-like cancer claim 18 , or metastatic cancer.20. The method of claim 14 , wherein the method further comprises administering a second therapeutic agent to the subject.21. The method of claim 20 , wherein the second therapeutic agent is a chemotherapeutic agent or an anti-inflammatory agent. This application is a continuation of U.S. application Ser. No. 14/323,374, filed Jul. 3, 2014, which is currently pending and which is a continuation of U.S. application Ser. No. 13/148,579, filed Feb. 8, 2012, now issued U.S. Pat. No. 8,802,687, which is a U.S. national stage filing of PCT/US10/23556, filed Feb. 9, 2010, which claims priority to U.S. Provisional Application No. 61/151,038, filed Feb. 9, 2009. These applications are incorporated by reference herein in their entireties.This invention ...

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15-09-2022 дата публикации

RNA-TARGETING LIGANDS, COMPOSITIONS THEREOF, AND METHODS OF MAKING AND USING THE SAME

Номер: US20220289688A1
Принадлежит:

The disclosure is directed to compounds that bind to a target RNA molecule, such as a TPP riboswitch, compositions comprising the compounds, and methods of making and using the same. The compounds contain two structurally different fragments that allow for binding with the target RNA at two different binding sites thereby producing a higher affinity binding ligand compared to compounds that only bind to a single RNA binding site. 2. The compound of claim 1 , wherein at least one of X claim 1 , X claim 1 , or Xis N.3. The compound of claim 2 , wherein n is 2.4. (canceled)7. (canceled)1012.-. (canceled)13. The compound of claim 9 , wherein m is 1 and W is selected from —NH claim 9 , —O claim 9 , and —N(C-Calkyl).1415.-. (canceled)16. The compound of claim 13 , wherein at least one of X claim 13 , X claim 13 , X claim 13 , and Xis N.17. (canceled)1920.-. (canceled)21. The compound of claim 18 , wherein Yis CRand Ris selected from —H claim 18 , —F claim 18 , —OH claim 18 , and —NH.23. The compound of claim 1 , wherein the compound binds to a region of an RNA molecule.24. The compound of claim 23 , wherein the RNA molecule is a non-coding RNA molecule selected from rRNA claim 23 , microRNAs claim 23 , siRNAs claim 23 , piRNAs claim 23 , snoRNAs claim 23 , snRNAs claim 23 , exRNAs claim 23 , and scaRNAs.25. (canceled)26. The compound of claim 23 , wherein the RNA molecule is a coding RNA molecule selected from mRNA.27. (canceled)28. The compound of claim 26 , wherein the region of the mRNA is a TPP riboswitch.2930.-. (canceled)31. A composition comprising a therapeutically effective amount of the compound of any one of in a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , or excipient.32. A method of treating a disease or disorder associated with a dysfunction in RNA expression claim 1 , the method comprising administering to a subject in need thereof a dose of a therapeutically effective amount of a compound of .33. The method of claim 32 , wherein ...

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31-05-2018 дата публикации

Magnetically separable iron-based heterogeneous catalysts for dehydrogenation of alcohols and amines

Номер: US20180147568A1

The present invention discloses an iron-based nitrogen doped graphene catalyst, process for preparation thereof and use of said catalyst in oxidant-free catalytic dehydrogenation of alcohols and amines to the corresponding carbonyl compounds, amines and N-heterocylic compounds with extraction of molecular hydrogen as the only by-product.

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31-05-2018 дата публикации

SUBSTITUTED QUINOXALINE DERIVATIVES

Номер: US20180148429A1
Принадлежит:

The present invention relates to substituted quinoxaline derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases. 2. Compound according to claim 1 , or derivatives claim 1 , prodrugs claim 1 , solvates claim 1 , tautomers or stereoisomers thereof as well as the physiologically acceptable salts of each of the foregoing claim 1 , including mixtures thereof in all ratios claim 1 ,wherein{'sup': '7', 'X denotes N—Ror O;'}{'sup': 1', 'X', 'X', 'Y', 'X', 'Y', 'X', 'X', 'X', 'Z', 'Y, 'Rdenotes Ar, Ar-Hetar, Ar-Hetcyc, Hetar, Hetcyc, Hetar-LA-Ar;'}{'sup': 2', '3, 'sub': 1-6', '1-6', '2, 'Rand Rdenote independently from each other H, —OH, unsubstituted straight-chain or branched —C-alkyl, unsubstituted straight-chain or branched —O—C-alkyl, Hal, —CN, —C(═O)—NH;'}{'sup': 4', 'X', 'X', 'Y', 'X', 'Y', 'X', 'Y', 'X', 'X', 'Y', 'X', 'Y', 'X', 'Y', 'X', 'X', 'Y', 'X', 'Z', 'Y', 'X', 'Z', 'Y', 'Z', 'Y, 'Rdenotes Ar, Ar—Ar, Ar-Hetar, Ar-Hetcyc, Hetar, Hetar-Ar, Hetar-Hetar, Hetar-Hetcyc, Hetcyc, Hetcyc-Hetar, Hetcyc-LA-Ar, LA, LA-Hetar, LA-Hetcyc;'}{'sup': 5', 'X', 'X', 'X', 'X', 'X7', 'X8, 'Rdenotes H, Hetar, Hetcyc, LA, CA, —C(═O)—NRR;'}or{'sup': 4', '5', 'A1', 'A2', 'A3, 'Rand Rform together with the carbon atom to which they are attached to a saturated or partially unsaturated ring system A which ring system A is mono- or bicyclic and has 3, 4, 5, 6, 7, 8, 9, 10 ring atoms and may contain no hetero ring atom or 1, 2, 3 hetero ring atom(s) independently from each other selected from N, O and/or S that ring system A may be unsubstituted or mono-, di- or trisubstituted with independently from each other R, R, R;'}{'sup': 6', 'X', 'X', 'X, 'Rdenotes denotes H, Hetar, Hetcyc, LA;'}or{'sup': 5', '6', 'D1', 'D2', 'D3, 'Rand Rform together with the carbon atom to which they are attached to a saturated or partially unsaturated ring system D which ring system D is mono- or bicyclic and ...

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11-06-2015 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20150158826A1
Принадлежит:

Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions containing the inhibitor compounds and methods of treatment of cancer comprising administering an effective amount of the Braf inhibitor compound are described. 126-. (canceled)28. The compound or pharmaceutically acceptable salt of claim 27 , wherein Rand Rare hydrogen.29. (canceled)30. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris optionally substituted aryl claim 27 , optionally substituted heterocycloalkyl claim 27 , or optionally substituted heteroaryl.31. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris optionally substituted morpholinyl claim 27 , optionally substituted piperazinyl claim 27 , optionally substituted pyrrolidinyl claim 27 , optionally substituted piperidinyl claim 27 , optionally substituted imidazolyl claim 27 , optionally substituted pyrazolyl claim 27 , or optionally substituted pyridyl.32. The compound or pharmaceutically acceptable salt of claim 27 , wherein R claim 27 , R claim 27 , R claim 27 , and Rare independently hydrogen claim 27 , halo claim 27 , cyano claim 27 , optionally substituted alkoxy claim 27 , or optionally substituted alkyl.33. (canceled)34. (canceled)35. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris fluoro.36. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris hydrogen or halo.3739-. (canceled)40. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris optionally substituted lower alkyl claim 27 , optionally substituted aryl claim 27 , or optionally substituted heteroaryl.41. (canceled)42. (canceled)43. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris —COR claim 27 , —COR claim 27 , —CONRR claim 27 , —C(NR)NRR claim 27 , ...

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01-07-2021 дата публикации

ORGANIC COMPOUNDS AND ORGANIC LIGHT EMITTING DISPLAY DEVICE USING THE SAME

Номер: US20210198212A1
Принадлежит:

The present disclosure relates to an organic compound and an organic light emitting display device using the same wherein the organic compound is represented by Chemical Formula 1 and a display device using the organic compound. The organic compound represented by Chemical Formula 1 has excellent electron transport properties and durability and is used for an electron transport layer of an organic light emitting element, thereby lowering a driving voltage and improving the luminous efficiency and lifetime. 4. The organic compound according to claim 1 , wherein in the above Chemical Formula 1 claim 1 , Arand Arare different from each other.9. The organic compound according to claim 1 , wherein the organic compound has a band gap of 3.6 eV to 4.1 eV.10. The organic compound according to claim 1 , wherein the organic compound has an HOMO level of −6.4 eV to −5.7 eV and an LUMO level of −2.4 eV to −1.8 eV.12. The organic light emitting display device according to claim 11 , wherein the organic layer includes an organic light emitting layer disposed on the anode and an electron transport layer disposed on the organic light emitting layer and containing the organic compound represented by Chemical Formula 1. This application claims the priority of Korean Patent Application No. 10-2019-0179779 filed on Dec. 31, 2019, in the Korean Intellectual Property Office, the disclosure of which is incorporated herein by reference.The present disclosure relates to organic compounds and an organic light emitting display device using the same, and more particularly, to novel organic compounds with excellent electron transport properties and durability and an organic light emitting display device which can have high efficiency and long lifetime by applying the organic compounds to an organic layer.An organic light emitting display device (OLED) uses an organic light emitting element that is a self-light emitting element. Thus, the organic light emitting display device has a simple ...

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22-06-2017 дата публикации

POLYMERIZABLE LIQUID CRYSTAL COMPOUND, COMPOSITION, LIQUID CRYSTAL POLYMERIZATION FILM-KIND THEREOF AND USE THEREOF

Номер: US20170174992A1
Автор: OOTSUKI Daisuke
Принадлежит:

An object is to provide a polymerizable liquid crystal compound, a polymerizable liquid crystal composition containing the compound and liquid crystal polymerization film-kind capable of controlling chromatic dispersion characteristics and having low positive chromatic dispersion characteristics. 2. The polymerizable liquid crystal compound according to claim 1 , wherein claim 1 ,G is(A) a divalent functional group that has a quinoline skeleton, and is connected in 5-position and 8-position of the quinoline skeleton, respectively,(B) a divalent functional group that has an isoquinoline skeleton, and is connected in 5-position and 8-position of the isoquinoline skeleton, respectively,(C) a divalent functional group that has a quinoxaline skeleton, and is connected in 5-position and 8-position of the quinoxaline skeleton, respectively, or(D) a divalent functional group that has a quinazoline skeleton, and is connected in 5-position and 8-position of the quinazoline skeleton, respectively.3. The polymerizable liquid crystal compound according to claim 1 , wherein claim 1 ,{'sup': '1', 'Ais independently 1,4-phenylene, 1,4-cyclohexylene, 1-cyclohexene-1,4-ylene or 2-cyclohexene-1,4-ylene, and in the 1,4-phenylene, at least one piece of hydrogen may be replaced by fluorine, chlorine, trifluoromethyl, alkyl having 1 to 5 carbons, alkoxy having 1 to 5 carbons, alkoxycarbonyl having 1 to 5 carbons or alkanoyl having 1 to 5 carbons, and'}{'sup': '1', 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Zis independently a single bond, —OCH—, —CHO—, —COO—, —OCO—, —CFO—, —OCF—, —CHCH—, —OCHCHO—, —CHCHCOO—, —OCOCHCH—, —CHCHOCO— or —COOCHCH—.'}4. The polymerizable liquid crystal compound according to claim 1 , wherein claim 1 , both pieces of Rare a group represented by formula (2).7. The polymerizable liquid crystal compound according to or claim 1 , wherein claim 1 , in formula (G-1) claim 1 , Tand Tare bonded to each other to form a ring claim ...

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09-07-2015 дата публикации

FUSED HETEROCYCLIC COMPOUND

Номер: US20150191474A1
Принадлежит:

The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. 2. The compound according to claim 1 , wherein{'sup': '1', 'Ris a C1 to C6 alkyl group optionally having one or more atoms or groups selected from halogen atoms and cyclopropyl groups (wherein the cyclopropyl group optionally has one or more halogen atoms or one or more C1 to C3 alkyl groups), a C2 to C6 alkenyl group optionally having one or more halogen atoms, a C2 to C6 alkynyl group optionally having one or more halogen atoms, or a cyclopropyl group optionally having one or more halogen atoms or one or more C1 to C3 alkyl groups,'}{'sup': 2', '4', '7, 'R, Rand Rare the same or different and are a halogen atom or a hydrogen atom,'}{'sup': 3', '19', '19', '19', '19, 'sub': m', '5, 'Ris a C1 to C6 alkyl group optionally having one or more halogen atoms, a C2 to C6 alkenyl group optionally having one or more halogen atoms, a C2 to C6 alkynyl group optionally having one or more halogen atoms, a 5- or 6-membered aromatic heterocyclic group (wherein the 5- or 6-membered aromatic heterocyclic group optionally has one or more atoms or groups selected from the group consisting of halogen atoms, C1 to C3 alkyl groups optionally having a halogen atom, and C1 to C3 alkoxy groups optionally having a halogen atom), —OR(wherein Ris a C1 to C6 alkyl group optionally having one or more halogen atoms), —S(O)R(wherein Ris a C1 to C6 alkyl group optionally having one or more halogen atoms, and m is 0, 1 or 2), —SF, a cyano group, a nitro group, a halogen atom or a hydrogen atom,'}{'sup': 5', '6', '21', '21', '21', '21, 'sub': m', '5, 'one of Rand Ris a C1 to C6 alkyl group optionally having one or more halogen atoms, —OR(wherein Ris a C1 to C6 alkyl group optionally having one or more halogen atoms), —S(O)R(wherein Ris a C1 to C6 alkyl group optionally having one or more halogen atoms, and m is 0, 1 or 2), —SFor a halogen atom, and the other is a halogen atom or a hydrogen atom ...

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18-09-2014 дата публикации

DNA-PK INHIBITORS

Номер: US20140275059A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. 2. The compound according to claim 1 , wherein X is NH.7. The compound according to claim 6 , wherein{'sup': 3', '3, 'sub': 1-4', '1-2', '1-2', '1-2', '2', '1-2, 'Ris hydrogen, Calkyl, fluoro, chloro, OCalkyl, C(O)OH, C(O)OCalkyl, CN, C(O)NHCalkyl, or C(O)NH, wherein each of said Ralkyl is optionally substituted with up to 3 fluorine atoms, up to two OH, or up to two OCalkyl groups;'}{'sup': '4', 'sub': 1-4', '2-4', '2-4', '3-5, 'Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, phenyl, a 5-10-membered monocyclic or bicyclic heteroaryl ring selected from pyrrole, imidazole, pyrazole, triazole, thiazole, isothiazole, oxazole, pyridine, pyrimidine, pyrimidinone, pyrazine, pyridazine, or quinoline, or a 4-10-membered monocyclic or bicyclic heterocyclyl ring selected from oxetane, tetrahydrofuran, tetrahydropyran, dihydroisoxazole, pyrimidine-2,4(1H,3H)-dione, dihydrofuropyrimidine, dihydropyranopyrimidine, dihydropyrrolopyrimidine, tetrahydropteridine, or tetrahydropyridopyrimidine;'}{'sup': 4', '5', '5', '5', '5', '5', '5', 'S', '4, 'sub': 1-4', '2-4', '2-4', '3-6', '2', '2', '2', '2', '1-4', '1-4', '1-4, 'each of said Rgroups is optionally substituted with Br, Cl, up to three fluorine atoms, up to three Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, an oxetane ring, a tetrahydrofuran ring, a dihydropyran ring, a tetrahydropyran ring, a pyrrolidine ring, a pyrazole ring, a triazole ring, a tetrazole ring, an oxadiazole ring, CN, CHOR, C(O)R, C(O)N(R), C(O)OR, NO, NHC(O)R, N(R), or up to two OR, wherein each of said optional Rsubstituents is optionally substituted with up to 3 fluorine atoms, up to two Calkyl groups, up to two OH groups, up to two OCalkyl groups, or up to two SCalkyl groups; and'}{'sup': ...

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06-07-2017 дата публикации

Redoxindicators

Номер: US20170191990A1
Принадлежит:

The present invention relates to a chemical compound or a salt or solvate thereof being a phenazine-, phenanthridine-, phenanthroline-, quinoline-, quinoxaline-, acridine- isoquinoline-, pyrazine- or pyridine-derivative comprising a conjugated π-system and a π-acceptor group, and to uses thereof. The present invention further relates to a chemistry matrix and to a test element comprising the chemical compound of the present invention. The present invention also relates to a method of determining the amount of an analyte in a test sample, comprising contacting said test sample with a chemical compound, with a chemistry matrix, or with a test element of the invention and estimating the amount of redox equivalents liberated or consumed by the chemical compound, by the chemical compound comprised in said chemistry matrix, or by the chemical compound comprised in said test element, in the presence of said test sample, thereby determining the amount of an analyte in said test sample. Moreover, the present invention relates to a system comprising a test element according to the present invention and a device comprising a sensor for measuring the amount of redox equivalents liberated or consumed. 2. The tricyclic chemical compound or a salt or solvate thereof of claim 1 , wherein(i) X is —N— and wherein the π-system is covalently bonded to C1, C2, C3, or C4 of the heteroaromatic system as indicated in formula (I), or(ii) X is —CH— and wherein the π-system is covalently bonded to C2 or C4 of the heteroaromatic system as indicated in formula (I).3. The tricyclic chemical compound or a salt or solvate thereof of or claim 1 ,(i) X is —N— and wherein the π-system is covalently bonded to C1 of the heteroaromatic system as indicated in formula (I), or(ii) X is —CH— and wherein the π-system is covalently bonded to C2 of the heteroaromatic system as indicated in formula (I).5. The tricyclic chemical compound or a salt or solvate thereof of any one of to claim 1 , wherein said ...

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30-07-2015 дата публикации

PROCESS FOR PRODUCING OPTICALLY ACTIVE AMINE

Номер: US20150210657A1
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

A process for producing an optically active amine compound, characterized by asymmetrically hydrogenating a prochiral carbon-nitrogen double bond in the presence of a ruthenium complex represented by general formula (1) or (2) (wherein P represents an optically active diphosphine, X represents an anionic group, and Ar represents an optionally substituted arylene group). 16-. (canceled)13. The production method according to claim 9 , wherein{'sup': 1', '2', '3', '4, 'R, R, R, and Rin general formula (5) are 3,5-xylyl groups.'}14. The production method according to claim 10 , wherein{'sup': 1', '2', '3', '4, 'R, R, R, and Rin general formula (5) are 3,5-xylyl groups.'}15. The production method according to claim 11 , wherein{'sup': 1′', '2′', '3′', '4′, 'R, R, R, and R in general formula (6) are 3,5-xylyl groups.'}16. The production method according to claim 12 , wherein{'sup': 1′', '2′', '3′', '4′, 'R, R, R, and R in general formula (6) are 3,5-xylyl groups.'}17. The production method according to claim 7 , whereinthe method is conducted in the presence of a base compound. The present invention relates to a method for producing an optically active amine compound. Moreover, the present invention relates to a method for producing an optically active amine compound by an asymmetric hydrogenation of a prochiral carbon-nitrogen double bond in the presence of a ruthenium complex having a ruthenabicyclic structure. More specifically, the present invention relates to a novel highly practical method for producing an optically active amine compound, which is useful as a synthetic intermediate of a pharmaceutical.As methods for obtaining an optically active amine compound, classical methods have been often used, such as a method in which a naturally-derived amine compound is used, and a method in which a racemic amine compound is synthesized, and then subjected to optical resolution using an optically active organic acid. However, the former method is still disadvantageous in ...

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06-08-2015 дата публикации

Selective inhibition of c4-pep carboxylases

Номер: US20150216167A1
Принадлежит: Heinrich Heine Universitaet Duesseldof

The present invention relates to the use of a compound, a salt or solvate thereof as C4 plant selective herbicide wherein said compound comprises a cyclic alkyl, aryl, heterocycloalkyl or heteroaryl group, and wherein said compound further comprises a) at least a functional group Z being —C(═Y z )R 1 , wherein Y z is selected from the group consisting of O, NH and S, preferably wherein Y z is O, and wherein R 1 is selected from the group consisting of H, OH and N(R 2 R 3 ), —O(R 2 ) and —S(R 2 ), wherein R 2 and R 3 , are independently of each other, selected from the group consisting of H, alkyl, cycolalkyl, aryl and heteroaryl and a functional group Q which is —C(═Y Q )R 4 , wherein Y Q is selected from the group consisting of O, NH and S, preferably wherein Y Q is O, and wherein R 4 is selected from the group consisting of H, OH and NR 4# R 5# , OR 4# , SR 4# wherein R 4# and R 5# , are independently of each other, selected from the group consisting of H, alkyl, cycloalkyl, aryl and heteroaryl, or b) at least one electron donating group selected from the group consisting of OH, —SH, —O—R p , S—R p —NR p R q and O—C(═Y p )R r , wherein R p and R q are, independently of each other, selected from the group consisting of H, alkyl, cycloalkyl and heteroaryl, and wherein R r is —OH, —NH 2 , —NH-Alkyl, —O-Alkyl or —NH-Alkyl, and wherein Y p is selected from the group consisting of —S—, —O—, —NH, said compound being capable of binding to the malate binding site comprised by a phosphoenolpyruvate carboxylase from a C4 plant, thereby inhibiting said phosphoenolpyruvate carboxylase, and wherein the cyclic alkyl, aryl, heterocycloalkyl or heteroaryl group inhibits binding to the malate binding site of a phosphoenolpyruvate carboxylase from a C3 plant.

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06-08-2015 дата публикации

MATERIALS HAVING ELECTRON DEFICIENT MOIETIES AND METHODS OF SYNTHESIZING THEREOF

Номер: US20150218115A1
Принадлежит:

Various materials and polymers having electron deficient moieties and methods of synthesizing thereof are described herein. Specifically, a C—H bond activation method is disclosed wherein an electron deficient group having one or more activated C—H bonds is coupled to one or more aryl groups to afford materials or polymers which may be used in organic electronic and photonic applications. 5. The method of claim 1 , wherein the first aryl group comprises an electron donor.7. The method of claim 1 , wherein the first aryl group comprises an electron acceptor group.9. The method of claim 1 , further comprising a second C—H activated coupling of the dicyanobenzodiimine with a second aryl group claim 1 , whereby a covalent bond is formed between the second aryl group and the dicyanobenzodiimine such that His substituted with the second aryl group.12. The method of claim 11 , wherein the first aryl group and the second aryl group are identical.13. The method of claim 11 , wherein the first aryl group and the second aryl group are different.14. The method of claim 9 , wherein the first aryl group and the second aryl group independently comprise electron donor groups.16. The method of claim 9 , wherein the first aryl group and the second aryl group independently comprise electron acceptor groups.18. The method of claim 9 , wherein the first aryl group is an electron acceptor and the second aryl group is an electron donor or the first aryl group is an electron donor group and the second aryl group is an electron acceptor group. This application claims the benefit of U.S. Ser. No. 61/934,283, filed on Jan. 31, 2014, which is incorporated herein in its entirety.This invention was made with government support under Grant Award No. CHE-1205646 awarded by the National Science Foundation. The government has certain rights in the invention.The present invention generally relates to materials having electron deficient moieties and methods of synthesizing such materials.Electron ...

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27-07-2017 дата публикации

BIMESOGENIC COMPOUNDS AND MESOGENIC MEDIA

Номер: US20170210990A1
Принадлежит: Merck Patent GmBH

The invention relates to bimesogenic compounds of formula I 2. Bimesogenic compounds according to claim 1 , characterized in thatat least one of{'sup': 11', '12, 'MGand MGcomprises one fused ring structure, two or more fused ring structures, at least part of which fused ring structure or fused ring structures is aromatic in character'}3. Bimesogenic compounds according to claim 1 , characterized in that both MGand MGcomprise one claim 1 , two or more ring structures claim 1 , linked by a 1 claim 1 , 2 or 3 atomic spacer claim 1 , preferably selected from —CO—O— claim 1 , —O—CO— claim 1 , —O—CH— claim 1 , —CH—O— claim 1 , —CF—O— claim 1 , —O—CF— claim 1 , —C≡C— claim 1 , —CH═CH— claim 1 , —CF═CF— and —CHF═CHF—.4. Bimesogenic compounds according to claim 1 , characterized in that Ris selected from OCF claim 1 , CF claim 1 , F claim 1 , Cl claim 1 , CN and NO.5. Bimesogenic compounds according to claim 1 , characterized in that Spis —(CH)— and o is 1 claim 1 , 3 or an integer from 5 to 15.6. A method which comprises including one or more bimesogenic compounds according to in a liquid crystalline medium.7. Liquid-crystalline medium claim 1 , characterised in that it comprises one or more bimesogenic compounds according to .8. Liquid-crystalline medium according to claim 7 , characterised in that it additionally comprises one or more compounds selected from the group of the compounds of the formulae III{'br': None, 'sup': 31', '31', '31', '3', '32', '32', '32, 'R-MG-X-Sp-X-MG-R\u2003\u2003III'}wherein{'sup': 31', '32, 'sub': 2', '3, 'Rand Rare each independently H, F, Cl, CN, NCS or a straight-chain or branched alkyl group with 1 to 25 C atoms which may be unsubstituted, mono- or polysubstituted by halogen or CN, it being also possible for one or more non-adjacent CHgroups to be replaced, in each case independently from one another, by —O—, —S—, —NH—, —N(CH)—, —CO—, —COO—, —OCO—, —O—CO—O—, —S—CO—, —CO—S—, —CH═CH—, —CH═CF—, —CF═CF— or —C≡C— in such a manner that oxygen ...

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04-08-2016 дата публикации

NOVEL MONOTHIOL MUCOLYTIC AGENTS

Номер: US20160222023A1
Принадлежит: PARION SCIENCES, INC.

Provided are mucolytic agents represented by formula (Ia)-(Id): 2. A method of liquefying mucus from mucosal surfaces , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering an effective amount of the compound of to a mucosal surface of a subject.'}3. A method of treating chronic bronchitis , treating bronchiectasis , treating cystic fibrosis , treating chronic obstructive pulmonary disease , treating asthma , treating pulmonary fibrosis , treating sinusitis , treating vaginal dryness , treating dry eye , promoting ocular hydration , promoting corneal hydration , promoting mucus clearance in mucosal surfaces , treating Sjogren's disease , treating distal intestinal obstruction syndrome , treating dry skin , treating esophagitis , treating dry mouth , treating nasal dehydration , treating ventilator-induced pneumonia , treating asthma , treating primary ciliary dyskinesia , treating otitis media , inducing sputum for diagnostic purposes , treating cystinosis , treating emphysema , treating pneumonia , treating constipation , treating chronic diverticulitis , and/or treating rhinosinusitis , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering an effective amount of the compound of to a subject in need thereof.'}4. A method of treating an eye disease characterized by the presence of ocular discharge comprising administering to a subject in need thereof an effective amount of the compound of .5. The method of claim 4 , wherein the eye disease is one or more conditions selected from the group consisting of blepharitis claim 4 , allergies claim 4 , conjunctivitis claim 4 , corneal ulcer claim 4 , trachoma claim 4 , congenital herpes simplex claim 4 , corneal abrasions claim 4 , ectropion claim 4 , eyelid disorders claim 4 , gonococcal conjunctivitis claim 4 , herpetic keratitis claim 4 , ophthalmitis claim 4 , Sjogren's Syndrome claim 4 , Stevens-Johnson Syndrome6. A method of treating a disease ameliorated by increased ...

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04-08-2016 дата публикации

SPIROQUINOXALINE DERIVATIVES AS INHIBITORS OF NON-APOPTOTIC REGULATED CELL-DEATH

Номер: US20160222025A1
Принадлежит:

The present invention relates to compounds which are inhibitors of non-apoptotic regulated cell death, and to pharmaceutical compositions containing such compounds. Furthermore, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, in particular in the treatment of a condition, disorder or disease that is characterised by non-apoptotic regulated cell-death or where non-apoptotic regulated cell-death is likely to play or plays a substantial role. The compounds and pharmaceutical compositions described herein are also useful in the treatment of a condition, disorder or disease that is characterised by oxidative stress or where oxidative stress is likely to play or plays a substantial role; and/or a condition, disorder or disease that is characterised by activation of (1) one or more components of the necrosome; (2) death domain receptors; and/or (3) Toll-like receptors; and/or (4) players in ferroptotic/ferroptosis signalling, or where activation of any one of (1) to (3) and/or (4) is likely to play or plays a substantial role. 4. (canceled)6. The method of claim 1 , wherein ring A is a monocyclic 4- to 10-membered N-heterocycloalkylene.8. The method of claim 1 , wherein ring A is saturated.9. The method of claim 1 , wherein ring A contains 1 ring nitrogen atom and is 4- to 8-membered or contains 2 or 3 ring nitrogen atoms and is 5- to 8-membered claim 1 , preferably ring A is 5- claim 1 , 6- or 7-membered claim 1 , more preferably 6- or 7-membered.10. The method of claim 1 , wherein ring A is selected from the group consisting of piperidinylene claim 1 , azepanylene (e.g. claim 1 , homopiperidinylene) claim 1 , azetidinylene claim 1 , pyrrolidinylene claim 1 , azocanylene claim 1 , pyrazolidinylene claim 1 , hexahydropyridazinylene claim 1 , hexahydropyrimidinylene claim 1 , diazepanylene (e.g. claim 1 , homopiperazinylene) claim 1 , diazocanylene claim 1 , triazepanylene claim 1 , and triazocanylene claim 1 , each of ...

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02-08-2018 дата публикации

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Номер: US20180215745A1
Принадлежит:

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. 121.-. (canceled)23. The method of claim 22 , wherein said condition or disorder is a neurodegenerative disease.24. The method of claim 22 , wherein said condition or disorder is Huntington's Disease.25. The method of claim 22 , wherein said condition or disorder is a polyglutamine disorder claim 22 , a spinocerebellar ataxias neurodegenerative disease claim 22 , a psychiatric of neurological disease or disorder claim 22 , Alzheimer's disease claim 22 , Parkinson's disease claim 22 , amyotropic lateral sclerosis claim 22 , Creutzfeld-Jacob disease claim 22 , trauma-induced neurodegeneration claim 22 , high-pressure neurological syndrome claim 22 , dystonia claim 22 , olivopontocerebellar atrophy claim 22 , amyotrophic lateral sclerosis claim 22 , multiple sclerosis claim 22 , epilepsy claim 22 ...

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12-08-2021 дата публикации

ANTI-FIBROTIC COMPOUNDS

Номер: US20210246100A1
Принадлежит: Certa Therapeutics Pty Ltd

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein. 5. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond;Z is O or a bond;{'sup': 1', '2', '1', '2', '8, 'Rand Rare independently hydrogen, alkyl, alkynyl, cycloalkylalkyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Rand Rare each optionally substituted with 1 or 2 independent substituents R;'}{'sup': 1', '2, 'or Rand Rtogether with the atoms to which they are attached form a heterocyclyl ring;'}{'sup': 3', '3', '8, 'Ris hydrogen, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein Ris optionally substituted with 1 or 2 independent substituents R;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2;{'sup': 8', 'a', 'b, 'each occurrence of Ris, independently, alkyl or NRR; and'}{'sup': a', 'b', 'c, 'each occurrence of R, R, and Ris, independently, hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and heterocyclyl.'}8. The compound of or , or a pharmaceutically acceptable salt thereof , whereinX is O or a bond;Y is O or a bond; provided that at least one of X and Y is O;{'sup': 1', '2, 'Rand Rare independently, alkyl, alkynyl, heteroarylalkyl, heterocyclyl, or heterocyclylalkyl, wherein said heteroarylalkyl, heterocyclyl, and heterocyclylalkyl are optionally substituted with 1 or 2 independent alkyl groups;'}{'sup': 6', 'c, 'sub': '2', 'each occurrence of Ris, independently, halogen, cyano, alkyl, heteroaryl, heterocyclyl, or —S(O)R;'}m is 1 or 2 ...

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02-07-2020 дата публикации

A PLURALITY OF HOST MATERIALS AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

Номер: US20200212310A1
Принадлежит:

The present disclosure relates to a plurality of host materials and organic electroluminescent devices comprising the same. The present disclosure may provide a plurality of host materials having a composition favorable to thermal denaturation due to a low deposition temperature, while improving hole properties and electronic properties of HOMO and LUMO, by comprising separate compounds represented by formulas 1 and 2 into a light-emitting layer. By comprising the plurality of host materials of the present disclosure, it is possible to provide an organic electroluminescent device having a lower driving voltage, higher luminous efficiency and/or longer lifetime. 4. The plurality of host materials according to claim 1 , wherein the substituents of the substituted aryl(ene) claim 1 , the substituted heteroaryl(ene) claim 1 , the substituted mono- or di-alkylamino claim 1 , the substituted mono- or di-arylamino claim 1 , the substituted alkylarylamino claim 1 , the substituted alkyl claim 1 , the substituted alkenyl claim 1 , the substituted cycloalkyl claim 1 , the substituted alkoxy claim 1 , the substituted trialkylsilyl claim 1 , the substituted dialkylarylsilyl claim 1 , the substituted alkyldiarylsilyl claim 1 , the substituted triarylsilyl claim 1 , or the substituted mono- or polycyclic ring in Lto L claim 1 , Arto Ar claim 1 , HAr claim 1 , and Rto R claim 1 , each independently claim 1 , are at least one selected from the group consisting of deuterium claim 1 , a halogen claim 1 , a cyano claim 1 , a carboxyl claim 1 , a nitro claim 1 , a hydroxyl claim 1 , a (C1-C30)alkyl claim 1 , a halo(C1-C30)alkyl claim 1 , a (C2-C30)alkenyl claim 1 , a (C2-C30)alkynyl claim 1 , a (C1-C30)alkoxy claim 1 , a (C1-C30)alkylthio claim 1 , a (C3-C30)cycloalkyl claim 1 , a (C3-C30)cycloalkenyl claim 1 , a (3- to 7-membered)heterocycloalkyl claim 1 , a (C6-C30)aryloxy claim 1 , a (C6-C30)arylthio claim 1 , a (5- to 30-membered)heteroaryl claim 1 , a (C6-C30)aryl claim 1 , a tri( ...

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06-11-2014 дата публикации

Novel Substituted Bicyclic Aromatic Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20140329821A1
Принадлежит:

The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 2. The method of wherein when Zand Zare both N claim 1 , and Zis CR claim 1 , then Ris selected from the group consisting of hydrogen claim 1 , C-Calkyl claim 1 , fluorinated C-Calkyl claim 1 , and cyano.3. The method of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}5. The method of wherein A is COOH.7. The method of wherein when Zis N claim 6 , and Zis CR claim 6 , then Ris selected from the group consisting of hydrogen claim 6 , C-Calkyl claim 6 , fluorinated C-Calkyl claim 6 , and cyano.8. The method of whereinm is selected from the group consisting of 0 and 1;{'sub': 2a', '2b', '2c', '3', '2, 'R, R, and R, are independently selected from the group consisting of hydrogen, chloro, fluoro, methyl, trifluoromethyl, cyano, methoxy, and N(CH);'}n is selected from the group consisting of 0 and 1; and{'sub': 3', '4', '4′', '4', '4′, 'Ris independently selected from the group consisting of fluoro, chloro, methyl, trifluoromethyl, cyano, methoxy, and NRR where Rand R are methyl, or alternatively together with the said N form the ring aziridin-1-yl or morpholino.'}11. The method of wherein Ris selected from the group consisting of hydrogen claim 10 , C-Calkyl claim 10 , fluorinated C-Calkyl claim 10 , and cyano.12. The method of ...

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01-08-2019 дата публикации

Trisubstitutedsilylphenoxyheterocycles and analogues

Номер: US20190233444A1
Принадлежит: Bayer CropScience AG

The present disclosure relates to fungicidal active compounds, more specifically to trisubstitutedsilylphenoxyhetero-cycles and analogues thereof, processes and, intermediates for their preparation and use thereof as fungicidal active compound, particularly in the form of fungicide compositions. The present disclosure also relates to methods for the control of phytopathogenic fungi of plants using these compounds or compositions comprising thereof.

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17-09-2015 дата публикации

INDICATION OF NAPHTHO[2,3-F]QUINOXALINE-7,12-DIONE COMPOUND IN ALLEVIATING PAIN

Номер: US20150259302A1
Принадлежит: National Central University

Disclosed are naphtho[2,3-f]quinoxaline compounds and pharmaceutical composition thereof. The compounds of the invention have been demonstrated as having analgesic effects and therefore may be applicable for use as a novel agent in relieving acute or chronic pain. 2. The method as claimed in claim 1 , wherein the pain is one of an acute pain and a chronic pain caused by one selected from a group consisting of an inflammation claim 1 , an injury claim 1 , and a neuropathy.3. The method as claimed in claim 1 , wherein the pain is one of an acute pain and a chronic pain caused by one of a cancer and a cancer treatment.5. The method as claimed in claim 4 , wherein the pain is one of an acute pain and a chronic pain caused by one selected from a group consisting of an inflammation claim 4 , an injury claim 4 , and a neuropathy.6. The method as claimed in claim 4 , wherein the pain is one of an acute pain and a chronic pain caused by one of a cancer and a cancer treatment.8. The method as claimed in claim 7 , wherein the pharmaceutical compound is administered to the subject with a pharmaceutical excipient. This application claims benefit under 35 U.S.C. §119 of Taiwan Application No. 103108518, filed Mar. 11, 2014, the contents of which are incorporated by reference as if fully set forth.The present invention relates to naphtho[2,3-f]quinoxaline compounds and pharmaceutical compositions thereof, which demonstrates analgesic effects. In particular, the present invention relates to an application in the pharmaceutical field.Naphtho[2,3-f]quinoxaline-7,12-dione compounds such as Formula I and Formula II are kinds of anthraquinone derivatives containing a heterocyclic group, where the synthesis and the effectiveness of the compounds to inhibit cancer cell activity through stabilizing G-quadruplex construction to suppress telomerase activity are both disclosed in Taiwan Patent Application No. 097112087.The R4 is selected from hydrogen or methyl.The known tricyclic ...

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08-08-2019 дата публикации

PD-CATALYZED GAMMA-C(SP3)-H ARYLATION / HETEROARYLATION OF FREE AMINES

Номер: US20190241508A1
Автор: YU JIN-QUAN
Принадлежит:

Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction. 3. The method of claim 1 , wherein TDG is 2-hydroxynicotinaldehyde (TDG4).4. The method of claim 1 , wherein the primary amino compound of formula (I) is contacted with an aryl iodide and group AH in the compound of formula (II) is aryl.5. The method of claim 4 , wherein the reaction milieu further comprises silver trifluoroacetate.6. The method of claim 2 , wherein group AH in the compound of formula (III) is aryl.7. The method of claim 1 , wherein the primary amino compound of formula (I) is contacted with a heteroaryl iodide and group AH in the compound of formula (II) is heteroaryl.8. The method of wherein the reaction milieu further comprises silver trifluoroacetate or pyridone claim 7 , or both.9. The method of claim 2 , wherein group AH in the compound of formula (III) is heteroaryl. This application claims the priority of U.S. provisional application Ser. No. 62/411,978, filed Oct. 24, 2016, the disclosure of which is incorporated by reference herein in its entirety.This invention was made with government support under 2R01GM084019 awarded by the National Institutes of Health. The government has certain rights in the invention.In the past decade, directed C—H activations have been extended to a wide range of synthetically useful substrates and transformations.Nevertheless, the covalent installation and removal of directing groups often poses a major obstacle for their synthetic applications. In addition to adding two steps to the synthetic ...

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20-11-2014 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20140343068A1
Автор: Qian Xiangping, Zhu Yong
Принадлежит:

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. Specifically quinoxaline derivatives of Formula I and their use in modulating the activity of Braf and/or mutant Braf kinase to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism are disclosed. Also disclosed are methods of treating cancer associated with Braf and/or mutant Braf kinase activity in a subject, comprising administering the compounds of Formula I. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris hydrogen claim 1 , cyano claim 1 , optionally substituted alkoxy claim 1 , optionally substituted aryloxy claim 1 , optionally substituted amino claim 1 , optionally substituted alkyl claim 1 , optionally substituted heterocycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl.3. The compound or pharmaceutically acceptable salt of claim 2 , wherein Ris optionally substituted aryl claim 2 , optionally substituted heterocycloalkyl claim 2 , or optionally substituted heteroaryl.4. The compound or pharmaceutically acceptable salt of claim 3 , wherein Ris optionally substituted morpholinyl claim 3 , optionally substituted piperazinyl claim 3 , optionally substituted pyrrolidinyl claim 3 , optionally substituted piperidinyl claim 3 , optionally substituted imidazolyl claim 3 , optionally substituted pyrazolyl claim 3 , or optionally substituted pyridyl.5. The compound or pharmaceutically acceptable salt of any one of to claim 3 , wherein R claim 3 , R claim 3 , R claim 3 , and Rare independently hydrogen claim 3 , halo claim 3 , cyano claim 3 , optionally substituted alkoxy claim 3 , or optionally substituted alkyl.6. The compound or pharmaceutically acceptable salt of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , and Rare independently hydrogen or halo.7. The compound or pharmaceutically acceptable salt of claim 6 , ...

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27-11-2014 дата публикации

ANTIMICROBIAL AGENTS

Номер: US20140350024A1
Принадлежит:

The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of Xto Xare N and the remaining of Xto Xare CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. 11. The method of wherein Ris phenyl claim 1 , 3-biphenyl claim 1 , 3-tert-butylphenyl claim 1 , 4-tert-butylphenyl claim 1 , 3-fluorophenyl claim 1 , 3-methoxycarbonyl-5-(4-tert-butylphenyl)phenyl claim 1 , 3-aminocarbonyl-5-(4-tert-butylphenyl)phenyl claim 1 , 3-(N-(2-hydroxyethyl)aminocarbonyl)-5-(4-tert-butylphenyl)phenyl claim 1 , or 3-methylphenyl.12. The method of wherein Ris guanadinomethyl claim 1 , 2-aminoethylamino claim 1 , aminomethyl claim 1 , —CH—NH—C(═NH)—CH claim 1 , or —CH—N═C(NH)—NH.13. The method of wherein Ris methyl and X is I.15. The method of wherein Ris 3-(N-(2-aminoethyl)-aminocarbonyl)-5-(4-tert-butylphenyl)phenyl.17. The method of wherein the bacterial infection is a Gram-negative bacterial strain infection.18Escherchia coli, Caulobacter crescentus, Pseudomonas aeruginosa, Agrobacterium tumefaciens, Branhamella catarrhalis, Citrobacter diversus, Enterobacter aerogenes, Enterobacter cloacae, Enterobacter sakazakii, Enterobacter asburiae, Pantoea agglomerans, Klebsiella pneumoniae, Klebsiella oxytoca, Klebsiella rhinoscleromatis, Proteus mirabilis, Salmonella typhimurium, Salmonella enteriditis, Serratia marcescens, Shigella sonnei, Neisseria gonorrhoeae, Acinetobacter baumannii, Acinetobacter calcoaceticus, Acinetobacter lwoffi, Salmonella enteriditis, Fusobacterium nucleatum, Veillonella parvula, Bacteroides forsythus, Actinobacillus actinomycetemcomitans, Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis, Helicobacter pylori, Francisella tularensis, Yersinia pestis, ...

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13-09-2018 дата публикации

Heterocyclic bridged biphenyls

Номер: US20180258053A1
Принадлежит:

The present invention relates electroluminescent devices, comprising a compound of the formula 110.-. (canceled)16. Electroluminescent device according to claim 11 , comprising a cathode claim 11 , an anode claim 11 , and therebetween a light emitting layer containing a host material and a phosphorescent light-emitting material claim 11 , wherein the host material is a compound of formula I.19. Solar cells claim 18 , dye lasers or electroluminescent devices comprising a compound of formula I according to . The present application is a continuation of U.S. patent application Ser. No. 12/310,737, filed Mar. 5, 2009, which is the U.S. National Stage Application filed under 35 U.S.C. § 371 of International Patent Application No. PCT/EP2007/059218, filed Sep. 4, 2007, which claims priority to European Patent Application No. 06120674.7, filed Sep. 14, 2006, all of which applications are hereby incorporated by reference in their entireties.The present invention relates electroluminescent devices, comprising a compound of the formulaespecially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.JP9013025 relates to an electroluminescent element a quinoxaline derivative represented by the formulawherein X is a C-Calkyl or the like; and Rto R, which are independent of each other, are each H, a halogen, a C-Calkyl or the like.JP11251063 discloses triphenylene compounds expressed by the formulawhich are used as a component material of an organic EL element.In the formula, Rto Reach independently represent an hydrogen atom, a halogen atom, a hydroxyl group, a substituted or unsubstituted amino group, a nitro group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted alkoxy group, a ...

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01-10-2015 дата публикации

QUINOXALINE COMPOUNDS AND USES THEREOF

Номер: US20150274709A1
Принадлежит:

Disclosed herein are compounds of formula (I) and methods of inhibiting IKKβ and the NF-κB signaling and mTOR pathways. 177.-. (canceled)86. A method comprising contacting a cell with the compound of in an amount effective to decrease activity of IKKβ.87. The method of claim 86 , wherein the IKKβ is a hyperphosphorylated form of IKKβ.88. A method of inhibiting NFκB signaling pathway comprising contacting a cell with the compound of in an amount effective to inhibit the NFκB signaling pathway.89. A method of inhibiting mTOR signaling pathway comprising contacting a cell with the compound of in an amount effective to inhibit the mTOR signaling pathway. This application claims the benefit of U.S. Provisional Application No. 61/416,001, filed Nov. 22, 2010, and U.S. Provisional Application No. 61/415,934. filed Nov. 22, 2010, each of which is incorporated by reference in its entirety.This invention was made with U.S. government support under Grant No. R01 CA127239, awarded by the National Institutes of Health. The U.S. government has certain rights in the invention.Since its discovery 25 years ago, NF-κB has been shown to regulate the expression of over 200 immune, growth and inflammation genes. NF-κB is constitutively active in proliferating T cells, B cells, thymocytes, monocytes and astrocytes. The clinically silent onset of PC has been attributed to the upregulation of pro-inflammatory pathways such as NF-κB. NF-κB is constitutively active in most tumor cell lines and many tumor tissues derived from patients, but not in normal tissues. A similar observation was made in PC cell lines and pancreatic adenocarcinoma which showed constitutively activated RelA (p65 subunit of NF-κB), but not in normal pancreatic tissues or immortalized/non-tumorigenic pancreatic epithelial cells. Studies also showed that PC cell lines had increased levels of NF-κB subunits compared to non-malignant proliferating intestinal cells. These preclinical observations extend to PC patients: (i) ...

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11-12-2014 дата публикации

NOVEL OXIDATION DYE PRECURSORS

Номер: US20140359951A1
Принадлежит:

An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I). 2. The agent according to claim 1 , wherein formula (I) is constituted such that X and Y in each case denote a group N—R7.3. The agent according to claim 1 , wherein formula (I) is constituted such that oxygen and Y denotes sulfur.4. The agent according to claim 1 , wherein formula (I) is constituted such that the residues R3 claim 1 , R4 claim 1 , R5 or R6 in each case mutually independently denote a hydrogen atom claim 1 , a C-Calkyl group claim 1 , a C-Calkoxy group claim 1 , an amino group claim 1 , a di(C-C-alkyl)amino group claim 1 , an N-(azacycloalkyl) group or a C-C-dialkylamino-C-C-alkyl group.5. The agent according to claim 1 , wherein formula (I) is constituted such that X and Y do not simultaneously denote oxygen and one of the two residues R1 or R2 denotes hydrogen and the other residue R2 or R1 denotes a group which is selected from a C-Calkyl group claim 1 , a C-Calkenyl group claim 1 , a C-Chydroxyalkyl group claim 1 , a C-Cpolyhydroxyalkyl group claim 1 , a hydroxyl group claim 1 , a C-Calkoxy group or a halogen atom.6. The agent according to claim 1 , wherein formula (I) is constituted such that X and Y do not simultaneously denote oxygen and one of the two residues R1 or R2 denotes hydrogen and the other residue R2 or R1 denotes a methoxy group.7. The agent according to claim 1 , wherein formula (I) is constituted such that X and Y do not simultaneously denote oxygen and the two residues R1 and R2 mutually independently denote a group which is selected from a C-Calkyl group claim 1 , a C-Calkenyl group claim 1 , a C-Chydroxyalkyl group claim 1 , a C-Cpolyhydroxyalkyl group claim 1 , a hydroxyl group claim 1 , a C-Calkoxy group or a halogen atom.8. The agent according to claim 1 , wherein formula (I) is constituted such that X and Y do not simultaneously denote ...

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20-10-2016 дата публикации

Fused Bicyclic Heteroaromatic Derivatives As Modulators of TNF Activity

Номер: US20160304470A1
Принадлежит:

A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. 3. The compound as claimed in wherein Rrepresents aryl or heteroaryl claim 2 , either of which groups may be optionally substituted by one or more substituents.5. The compound as claimed in wherein Rrepresents hydroxy(C)alkyl.8. The compound as claimed in wherein Rrepresents hydrogen claim 6 , fluoro or hydroxy.9. The compound as claimed in wherein E represents —O— claim 1 , —CH— or —CH(CH)—.10. The compound as claimed in wherein Rrepresents difluoromethoxy.11. A compound as herein specifically disclosed in any one of the Examples.12. (canceled)13. (canceled)14. (canceled)15. A pharmaceutical composition comprising a compound of formula (I) as defined in or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , or a glucuronide derivative thereof claim 1 , or a co-crystal thereof claim 1 , in association with a pharmaceutically acceptable carrier.16. The pharmaceutical composition as claimed in further comprising an additional pharmaceutically active ingredient.17. (canceled)18. (canceled)19. A method for the treatment and/or prevention of disorders for which the administration of a modulator of TNFα function is indicated which comprises administering to a patient in need of such treatment an effective amount of a compound of formula (I) as defined in or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , or a glucuronide derivative thereof claim 1 , or a co-crystal thereof.20. A method for the treatment and/or prevention of an inflammatory or autoimmune disorder claim 1 , a ...

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26-10-2017 дата публикации

HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20170305900A1
Принадлежит:

Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. 136.-. (canceled)40. The method of claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , wherein Ris —C(O)NH(OH).41. The method of claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , wherein Ris —N(OH)C(O)R.42. The method of claim 37 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , alkyl claim 37 , cycloalkyl claim 37 , haloalkyl claim 37 , hydroxyl claim 37 , alkoxy claim 37 , and nitrile.43. The method of claim 37 , wherein Ris heteroaryl optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , lower alkyl claim 37 , and haloalkyl.44. The method of claim 37 , wherein Ris hydrogen claim 37 , alkyl claim 37 , cycloalkyl claim 37 , heterocycloalkyl claim 37 , aryl claim 37 , heteroaryl claim 37 , aralkyl claim 37 , or heteroaralkyl claim 37 , each of which is optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , alkyl claim 37 , cycloalkyl claim 37 , haloalkyl claim 37 , hydroxyl claim 37 , alkoxy claim 37 , and nitrile.45. A method for treating a patient suffering from a neurodegenerative condition claim 37 , cancer claim 37 , amyotrophic lateral sclerosis (ALS) claim 37 , diabetes claim 37 , a cardiovascular condition claim 37 , epilepsy claim 37 , depression claim 37 , viral infection claim 37 , or fungal infection claim 37 , wherein the method comprises administering to the patient a therapeutically effective amount of a compound claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , selected from:(R)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-phenylcyclopent-2-enecarboxamide;(S)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-phenylcyclopent-2-enecarboxamide;(R)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-(o-tolyl)cyclopent-2-enecarboxamide;(S)-1-(3-fluoro-2-methylphenyl)-N-hydroxy ...

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05-11-2015 дата публикации

Quinoxaline Derivative, and Light Emitting Element, Light Emitting Device, and Electronic Device Using the Quinoxaline Derivative

Номер: US20150318492A1

To provide a new bipolar organic compound. In particular, to provide a bipolar organic compound having excellent heat resistance and to provide a bipolar organic compound which is electrochemically stable. Further, to provide a light emitting element and a light emitting device of which a driving voltage and power consumption are reduced by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have excellent heat resistance by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have a long life by using a new bipolar organic compound. 1. (canceled)2. A compound comprises:a quinoxaline skeleton;a carbazole skeleton which is substituted with an aryl group at 9-position of the carbazole skeleton; andan arylene group of carbon number 6 to 25 bonding 2-position of the quinoxaline skeleton and 3-position of the carbazole skeleton.3. The compound according to claim 2 , wherein the aryl group is a phenyl group.4. The compound according to claim 2 ,wherein the arylene group is a phenylene group.5. The compound according to claim 4 ,wherein the 3-position of the carbazole skeleton is bonded to 4-position of the phenylene group.7. A light-emitting element comprises:a first electrodea layer over the first electrode, the layer comprising a light-emitting material and an organic compound; anda second electrode over the layer,wherein the organic compound comprises:a quinoxaline skeleton;a carbazole skeleton which is substituted with an aryl group at 9-position of the carbazole skeleton; andan arylene group of carbon number 6 to 25 bonding 2-position of the quinoxaline skeleton and 3-position of the carbazole skeleton.8. The light-emitting element according to claim 7 , wherein the aryl group is a phenyl group.9. The light-emitting element according to claim 7 ,wherein the arylene group is a phenylene group.10. The light-emitting element according to claim ...

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10-10-2019 дата публикации

SUBSTITUTED BICYCLIC HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS

Номер: US20190308945A1
Принадлежит: Merck Sharp & Dohme Corp.

The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation. 3. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Y is H.4. The compound of according to claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein A is selected from benzoxazolyl claim 3 , quinazolinyl claim 3 , tetrahydrobenzoxazolyl claim 3 , oxazolopyridinyl claim 3 , quinoxalinyl claim 3 , imidazopyridazinyl claim 3 , benzothiazolyl claim 3 , dihydrocyclopentaoxazolyl claim 3 , naphthyridinyl claim 3 , pyrazolopyridinyl claim 3 , cinnolinyl claim 3 , isoquinolyl claim 3 , thienopyridinyl claim 3 , indazolyl claim 3 , tetrahydropyrazolopyridinyl claim 3 , furopyridinyl claim 3 , dihydropyridooxazinyl claim 3 , tetrahydrobenzothiazolyl claim 3 , tetrahydroquinazolinyl claim 3 , benzoxazinyl claim 3 , benzimidazolyl claim 3 , thiazolopyridinyl claim 3 , quinolinyl claim 3 , pyridopyrimidinyl claim 3 , phthalazinyl claim 3 , pyridopyrazinyl claim 3 , thienoxazole claim 3 , and thienothiazole each optionally substituted with 1 to 2 R groups independently selected from halogen claim 3 , CN claim 3 , (C-C)alkyl claim 3 , O(C-C)alkyl claim 3 , NRR claim 3 , (C-C)cycloalkyl claim 3 , aryl claim 3 , heteroaryl and heterocyclyl claim 3 , wherein said alkyl claim 3 , NRR claim 3 , (C-C)cycloalkyl claim 3 , aryl claim 3 , heteroaryl and heterocyclyl are each optionally substituted with one or more substituents independently selected from halogen claim 3 , CN claim 3 , (C-C)alkyl claim 3 , (C═O)O(C-C)alkyl claim 3 , and phenyl.5. The compound according to claim 4 , or a pharmaceutically ...

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01-12-2016 дата публикации

METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUND, AND NOVEL METAL-DIAMINE COMPLEX

Номер: US20160347678A1
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention pertains to a method for producing an optically active compound which includes a step for reducing an imino group of an imine compound or a step for reducing an unsaturated bond of a heterocyclic compound, while in the presence of hydrogen gas as a hydrogen donor and one or more types of complexes selected from a group consisting of a complex represented by general formula (1), a complex represented by general formula (2), a complex represented by general formula (3), and a complex represented by general formula (4) (the general formulas (1)-(4) are as stipulated by claim ). 4. An asymmetric reduction catalyst comprising the complex according to .5. An asymmetric reduction catalyst comprising the complex according to . The present invention relates to a method for selectively producing an optically active compound important as a precursor for synthesis of pharmaceuticals and functional materials, the methods using any of a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex as a catalyst.In the field of production of optically active amines, many asymmetric reactions, including asymmetric reduction, have been developed, and many asymmetric reactions have been reported which use asymmetric metal complexes having optically active phosphine ligands. Meanwhile, for example, there are many documents reporting that complexes in each of which an optically active nitrogen compound is coordinated to a transition metal, such as ruthenium, rhodium, or iridium, have excellent performance as catalysts for asymmetric synthesis reactions (see Chem Rev. (1992), p. 1051, J. Am. Chem. Soc. 117 (1995), p. 7562, J. Am. Chem. Soc. 118 (1996), p. 2521, and J. Am. Chem. Soc. 118 (1996), p. 4916). Especially, synthesis of optically active amines by hydrogenation reaction has been reported recently (see J. Am. Chem. Soc. 133 (2011), p. 9878, and Angew. Chem. Int. Ed 51 (2012), p. 5706).However, the conventional asymmetric synthesis ...

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17-12-2015 дата публикации

Novel Electron Transport Material for Organic Emitting Diodes

Номер: US20150364699A1
Автор: Sisk David T.
Принадлежит:

Some embodiments provide a compound represented by Formula 1, wherein ET, ETand ETare optionally substituted quinolinyl or optionally substituted quinoxalinyl; and wherein R, R, and Rare independently selected from the group consisting of H, Calkyl, and Cperfluoroalkyl. Other embodiments provide an organic electron transmission element and an organic light-emitting diode device comprising a compound of Formula 1. 2. The compound of claim 1 , wherein each substituent of quinolinyl and quinoxalinyl claim 1 , if present claim 1 , is represented by a formula CHONFClBr claim 1 , provided that each substituent has at least one non-hydrogen atom.3. The compound of claim 1 , wherein Ris H.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris H.8. A compound that is optionally substituted 1 claim 1 ,3 claim 1 ,5-tri(quinoxalinyl-5-yl)benzene claim 1 , optionally substituted 1 claim 1 ,3 claim 1 ,5-tri(quinolin-8-yl)benzene claim 1 , or optionally substituted 1 claim 1 ,3 claim 1 ,5-tri(quinolin-5-yl)benzene.9. An electron-transporting element comprising a compound of .10. An organic light-emitting diode device comprising:(1) a cathode;(2) an anode;(3) a light-emitting layer disposed between and electrically connected to the anode and the cathode; and{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '(4) the electron-transporting element of , in the form of an electron-transport layer disposed between and electrically connected to the cathode and the light-emitting layer.'}11. The device of claim 10 , further comprising a hole-transport layer between the anode and the light-emitting layer.12. The device of claim 10 , wherein the light-emitting layer further comprises an emissive component. This application claims priority to U.S. 62/012,098 filed Jun. 13, 2014, the entire disclosure of which is incorporated by reference herein.1. FieldThe present disclosure generally relates to the fields of organic chemistry and organic light emitting diode ...

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31-12-2015 дата публикации

SUBSTITUTED QUINOXALINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR4

Номер: US20150374687A1
Автор: Richardson Thomas E.
Принадлежит:

The present invention relates to novel quinoxaline derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling. 3. Compounds according to claim 1 , wherein{'sub': 1', '2, 'R, Rindependently from each other denote phenyl, furanyl, pyridinyl, thiophenyl, pyrrolidinyl, naphthalenyl, morpholinyl, piperazinyl, azetidinyl, piperidinyl, quinolinyl, indolyl, indazolyl or benzooxazolonyl, which can optionally be substituted by one or more identical or different substituents T;'}and the physiologically acceptable salts, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.4. Compounds according to claim 3 , wherein{'sub': 1', '2, 'R, Rindependently from each other are selected from the group consisting of: phenyl, furan-2-yl, furan-3-yl, 4-dimethylamino-phenyl, 2-fluorophenyl, 4-fluorophenyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, 4-hydroxy-phenyl, thiophen-2-yl, thiophen-3-yl, 4-methoxy-phenyl, 4-ethoxy-phenyl, 4-ethyl-phenyl, 4-fluoro-3-methyl-phenyl, 4-methylsulfanyl-phenyl, 4-trifluoromethoxy-phenyl, 3,4-difluorophenyl, 4-benzaldehyde, 4-tert-butyl-phenyl, 4-isopropyl-phenyl, pyrrolidin-1-yl, 3-chloro-4-methoxy-phenyl, 3-chloro-4-methyl-phenyl, 4-cyanomethyl-phenyl, 2-trifluoromethyl-phenyl, 4-trifluoromethyl-phenyl, 6-methoxy-naphthalen-1-yl, 3,4-dichlorophenyl, morpholin-4-yl, 4-dimethylamino-phenyl, 4-methyl-piperazin-1-yl, azetidin-1-yl, piperidin-1-yl, quinolin-4-yl, quinolin-8-yl, 4-hydroxymethyl-piperidin-1-yl, 4-hydroxy-piperidin-1-yl, indol-4-yl, 4-acetamide, 4-(2,2,2-trifluoro)-acetamide, 4-amino-phenyl, indazol-5-yl, 4-hydroxymethyl-phenyl, benzooxazol-2-one-6-yl;'}and the physiologically acceptable salts, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.5. Compounds according to claim 2 , whereinT denotes independently from each other H, fluoro, chloro, methyl, methoxy, ...

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10-11-2022 дата публикации

ORGANIC COMPOUND AND APPLICATION THEREOF

Номер: US20220359834A1
Автор: DENG Dongyang, Liu Ying
Принадлежит:

Provided are an organic compound and an application thereof. The organic compound has a structure represented by Formula I. Through the design of a molecular structure, the organic compound has suitable HOMO and LUMO energy levels, high singlet energy level, good optoelectronic performance, a high glass transition temperature and good thermal stability, easily forms a good amorphous film, and is suitable for the machining and use of an OLED device. The organic compound, when used in the OLED device, may be used as a light-emitting layer material, an electron transport material or a hole blocking material and especially suitable for use as a host material of the light-emitting layer and can effectively improve the luminescence efficiency of the device, improve the device stability, extend lifetime, and reduce an operating voltage and energy consumption so that the OLED device has significantly improved performance such as luminescence efficiency, lifetime and energy consumption. 2. The organic compound according to claim 1 , wherein the substituted substituents in L claim 1 , A claim 1 , R claim 1 , R claim 1 , Rand Rare each independently selected from at least one of halogen claim 1 , cyano claim 1 , unsubstituted or R′-substituted C1 to C10 linear or branched alkyl claim 1 , C3 to C10 cycloalkyl claim 1 , unsubstituted or R′-substituted C1 to C10 alkoxy claim 1 , unsubstituted or R′-substituted C6 to C20 aryl claim 1 , unsubstituted or R′-substituted C3 to C20 heteroaryl claim 1 , or unsubstituted or R′-substituted C6 to C20 arylamino;wherein R′ is selected from at least one of halogen, cyano, C1 to C6 linear or branched alkyl, C6 to C12 aryl or C3 to C12 heteroaryl.3. The organic compound according to claim 1 , wherein L is selected from any one of a single bond claim 1 , substituted or unsubstituted C6 to C20 arylene claim 1 , or substituted or unsubstituted C3 to C20 heteroarylene; andwherein the substituted substituents in L are each independently selected ...

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05-08-2014 дата публикации

Quinoxaline derivative, light-emitting element, light-emitting device, and electronic appliance

Номер: KR101426513B1

본 발명은, 전자 수송성이 뛰어난 신규 물질, 및 이것을 사용한 발광소자, 및 발광장치를 제공하는 것을 과제로 한다. 아래의 일반식 (G1)로 나타내어지는 퀴녹살린 유도체를 제공한다. 또한, 아래의 일반식 (G1)에서, R 1 내지 R 4 는 각각, 수소, 탄소수 1 내지 4의 알킬기, 탄소수 6 내지 25의 아릴기 중 하나를 나타낸다. 이와 같은 퀴녹살린 유도체는 전자 수송성이 뛰어나고, 발광소자 등에 있어서의 전자 수송 재료로서 매우 유용하다. It is an object of the present invention to provide a novel material having excellent electron transportability, a light emitting device using the same, and a light emitting device. There is provided a quinoxaline derivative represented by the following general formula (G1). In the general formula (G1) shown below, R 1 to R 4 each represent one of hydrogen, an alkyl group having 1 to 4 carbon atoms, and an aryl group having 6 to 25 carbon atoms. Such quinoxaline derivatives are excellent in electron transporting property and are very useful as electron transporting materials in light emitting devices and the like. 발광소자, 퀴녹살린 유도체, 전자 수송성, 전자 수송 재료 A light emitting element, a quinoxaline derivative, an electron transporting material, an electron transporting material

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21-02-2007 дата публикации

Aminoquinoxaline compound, polyaminoquinoxaline compound, and use thereof

Номер: CN1918135A
Автор: 古性均, 笠井干生
Принадлежит: Nissan Chemical Corp

本发明提供一种具有优异的耐热性,可以容易地控制电化学氧化还原电位,而且化合物本身的带隙非常窄,还具有强荧光发光特性的下述式(1a)所示的氨基喹喔啉化合物以及将该化合物聚合而形成的聚氨基喹喔啉化合物 (式中,R 1 和R 2 各自独立地表示氢原子、羟基、C 1 ~C 10 烷基、C 1 ~C 10 烷氧基等,R 3 和R 4 各自独立地表示氢原子、卤原子、氰基、硝基、氨基、C 1 ~C 10 烷基、C 1 ~C 10 烷氧基等,X 1 表示-NH-R 5 -NH 2 或-NH-R 6 )。

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02-01-2013 дата публикации

Heterocyclic bridged biphenyls and their use in oleds

Номер: CN101516856B
Принадлежит: Ciba SC Holding AG

本发明涉及场致发光装置,其包含式(I)的化合物,尤其是作为磷光化合物的主体。该主体可以与磷光材料一起作用来为场致发光装置提供提高的效率、稳定性、制造性或者光谱特性。

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25-08-2017 дата публикации

The method of synthesizing amino quinoxaline mixture

Номер: CN107089954A

本发明公开了一种合成2‑(4‑氨基苯基)‑3‑苯基‑6‑氨基喹喔啉和3‑(4‑氨基苯基)‑2‑苯基‑6‑氨基喹喔啉混合物的方法,它是以4‑硝基苯乙酸为起始原料,先经氯化反应得到4‑硝基苯乙酰氯;然后与苯反应得到2‑(4‑硝基苯基)‑1‑苯乙酮;接着与4‑硝基邻苯二胺反应得到2‑(4‑硝基苯基)‑3‑苯基‑6‑硝基喹喔啉和3‑(4‑硝基苯基)‑2‑苯基‑6‑硝基喹喔啉混合物;最后经催化加氢得到2‑(4‑氨基苯基)‑3‑苯基‑6‑氨基喹喔啉和3‑(4‑氨基苯基)‑2‑苯基‑6‑氨基喹喔啉混合物。本发明的起始原料4‑硝基苯乙酸相比于4‑硝基苯偶酰价廉易得,从而大大降低了生产成本,适合工业化大生产。

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17-07-2007 дата публикации

Quinoxaline derivatives, and light emitting element using thereof

Номер: US7245073B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

It is an object to provide an organic compound that has a bipolar property and also a light emitting property, and further has heat resistance. A quinoxaline derivative represented by a general formula (1) is provided. In the formula, A represents any one of an alkylene chain, silicon (Si), oxygen (O), nitrogen (N), and sulfur (S). R 1 to R 8 , which may be identical or different, individually represent any one of a lower alkyl group, an aryl group, and a heterocyclic group. R 9 to R 24 , which may be identical or different, individually represent any one of a hydrogen atom, a halogen atom, a lower alkyl group, an alkoxy group, an acyl group, a nitro group, a cyano group, an amino group, a dialkylamino group, a diarylamino group, a vinyl group, an aryl group which may have a substituent, and a heterocyclic group

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08-03-2011 дата публикации

Quinoxaline derivative, and light emitting element, light emitting device, and electronic appliance using the same

Номер: US7901792B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R 1 to R 12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar 1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar 2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.)

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09-08-2011 дата публикации

Quinoxaline derivative, and light-emitting element, light-emitting device, and electronic device using the same

Номер: US7993761B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

The present invention provides a quinoxaline derivative represented by a general formula (G1). In the formula, α 1 and α 2 each independently represent an arylene group which has 13 or less carbon atoms forming a ring; Ar represents an aryl group which has 13 or less carbon atoms forming a ring; R 1 and R 6 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an aryl group which has 13 or less carbon atoms forming a ring; and R 2 to R 5 and R 7 to R 10 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or a substituted or unsubstituted biphenyl group.

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15-05-2012 дата публикации

Quinoxaline derivative, and light-emitting element, light-emitting device, and electronic device including quinoxaline derivative

Номер: US8178216B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

An object of the present invention is to provide a quinoxaline derivative represented by a general formula (1). Ar 1 represents one of a substituted or unsubstituted biphenyl group, and a substituted or unsubstituted terphenyl group; Ar 2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, and a substituted or unsubstituted terphenyl group; α 1 represents an arylene group having 6 to 25 carbon atoms; and R 11 to R 15 are the same or different from one another, and each of them represents any one of a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, and a substituted or unsubstituted aryl group having 6 to 25 carbon atoms.

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07-01-2014 дата публикации

Quinoxaline derivative, and light emitting element, light emitting device, and electronic appliance using the same

Номер: US8623523B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R 1 to R 12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar 1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar 2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.)

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08-05-2012 дата публикации

Quinoxaline derivative, and light-emitting element, light-emitting device, and electronic appliance using the same

Номер: US8173277B2
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R 1 to R 12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar 1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar 2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.)

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20-03-2008 дата публикации

Heterocyclic bridged biphenyls and their use in oleds

Номер: WO2008031743A1
Принадлежит: Ciba Holding Inc.

The present invention relates electroluminescent devices, comprising a compound of the formula (I), especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

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02-03-2021 дата публикации

Heterocyclic bridged biphenyls

Номер: US10934262B2
Принадлежит: UDC Ireland Ltd

The present invention relates electroluminescent devices, comprising a compound of the formula especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

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23-03-2006 дата публикации

Aromatic amine derivative and organic electroluminescent element employing the same

Номер: US20060061265A1
Принадлежит: Idemitsu Kosan Co Ltd

Provided are an aromatic amine compound represented by the following Formula (1) and an organic electroluminescent element which has at least one organic thin film layer containing the above aromatic amine derivative in the form of a single component. The organic electroluminescent element described above has a high luminescent efficiency even at a low voltage and a long life. It can emit blue light even at high temperatures. In Formula (1), Ar 1 and Ar 2 each represent naphthyl and the like; Ar 3 to Ar 6 each represent phenyl, naphthyl, phenanthryl and the like; Ar 7 to Ar 10 each represent 1,4-phenylene and the like; L represents a single bond and the like; provided that the conditions of (1) and/or (2) are satisfied: (1) at least one of Ar 3 to Ar 6 is a condensed aryl group having 10 to 50 nuclear carbon atoms and (2) at least one of Ar 1 and Ar 2 is a condensed aryl group having 12 to 50 nuclear carbon atoms.

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01-01-2017 дата публикации

Carrier generation material and organic light emitting diode

Номер: TWI564294B
Принадлежит: 國立清華大學

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12-10-2011 дата публикации

Organic electroluminescence device using anthracene derivative

Номер: JP4790260B2
Принадлежит: Idemitsu Kosan Co Ltd

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03-09-2008 дата публикации

Aromatic amine derivative and organic electroluminescence device using the same

Номер: JP4142404B2
Принадлежит: Idemitsu Kosan Co Ltd

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08-03-2018 дата публикации

1,3-dithiolo[5,6-f]benzo-2,1,3-thiadiazole or 1,3-dithiolo[6,7-g]quinoxaline based organic semiconductors

Номер: WO2018041768A1
Принадлежит: Merck Patent GmBH

The invention relates to novel organic semiconducting (OSC) compounds containing one or more 1,3-dithiolo[5,6-f]benzo-2,1,3-thiadiazole ("DTBTz") or 1,3-dithiolo[6,7-g]quinoxaline ("DTQ") units or derivatives thereof, to methods for their preparation and educts or intermediates used therein, to compositions and formulations containing them, to the use of the compounds and compositions as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices, perovskite-based solar cell (PSC) devices, organic photodetectors (OPD), organic field effect transistors (OFET) and organic light emitting diodes (OLED), and to OE devices comprising these compounds or compositions.

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13-06-2017 дата публикации

A kind of optical activity two(It is miscellaneous)Aryl methyl alcohol and its method of asymmetric synthesis

Номер: CN106831550A
Принадлежит: China Three Gorges University CTGU

本发明涉及一种光学活性二(杂)芳基甲醇的不对称合成方法。该方法以单磺酰手性二胺与金属钌、铑、铱的配合物为催化剂,甲酸钠、或者甲酸/三乙胺、或者异丙醇为氢源,首次实现了对二(杂)芳基甲酮的不对称转移氢化反应,得到光学活性二(杂)芳基甲醇。该方法反应条件温和,操作简便,原料易得、底物适用范围广、对映选择性高,在合成抗组胺手性药物苯海拉明、甲苯海明、卡比沙明、贝他斯汀等方面具有重要的应用前景。

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13-09-2012 дата публикации

Aryl substituted carboxamide derivatives as trpm8 modulators

Номер: WO2012120398A1
Принадлежит: PFIZER LIMITED

The invention provides a compound of the formula (I): wherein A, R 1 , R 2 and R 3 are as defined herein, or a pharmaceutically acceptable salt thereof. Such compounds are small molecule TRPM8 blockers and therefore useful in the propylaxis or treatment of a wide range of diseases, conditions or syndromes, including cold allodynia and Raynaulds syndrome.

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08-06-1994 дата публикации

Derivatives of diamino benzoic and diamino phthalic acid und their use as protein linase inhibitors

Номер: EP0600832A1
Принадлежит: Ciba Geigy AG

The invention relates to compounds of the formula I <IMAGE> in which A1 and A2 denote hydrogen, unsubstituted or substituted lower alkyl, lower alkenyl or lower alkynyl, heterocyclyl-lower alkyl, acyl, lower alkylsulphonyl or arylsulphonyl, or together denote unsubstituted or substituted lower alkylene; Ar1 and Ar2 denote aryl, heteroaryl or unsubstituted or substituted cycloalkyl, X stands for O or S, Y stands for amino, substituted amino, substituted lower alkoxy or unsubstituted or substituted lower alkylthio; or, if X stands for O and Z stands for substituted methyl, for hydroxyl; and Z stands for substituted methyl, carboxyl or esterified or amidated carboxyl or thiocarboxyl; or Y and Z together denote 1-oxamethylene; salts thereof, tautomers thereof, process for preparation, pharmaceutical preparations, and/or these compounds for the therapeutic treatment of the human or animal body or for the production of pharmaceutical preparations. The compounds inhibit protein kinases.

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29-10-2015 дата публикации

Quinoxaline derivative and light-emitting element light-emitting device and electronic device using the same

Номер: KR101564230B1

[과제] 신규한 바이폴라성의 유기 화합물을 제공하는 것을 목적으로 한다. 또한, 캐리어 균형이 우수한 발광 소자를 제공하는 것을 목적으로 한다. 또한, 구동 전압이 낮고, 소비 전력이 작은 발광 소자 및 발광 장치를 제공하는 것을 목적으로 한다. 또한, 소비 전력이 작은 전자 기기를 제공하는 것을 목적으로 한다. [PROBLEMS] To provide a novel bipolar organic compound. Another object of the present invention is to provide a light emitting device having excellent carrier balance. Another object of the present invention is to provide a light emitting device and a light emitting device having a low driving voltage and a low power consumption. It is also an object of the present invention to provide an electronic device with low power consumption. [해결수단] 화학식 1로 나타내지는 퀴녹살린 유도체를 제공한다. [Solution] A quinoxaline derivative represented by the formula (1) is provided. 화학식 1 Formula 1 상기 화학식 1에서, In Formula 1, α 1 및 α 2 는, 각각 독립적으로, 환을 형성하는 탄소수가 13 이하인 아릴렌기를 나타내고, ? 1 and? 2 each independently represent an arylene group having 13 or less carbon atoms forming a ring, Ar은, 환을 형성하는 탄소수가 13 이하인 아릴기를 나타내고, Ar represents an aryl group having 13 or less carbon atoms forming a ring, R 1 및 R 6 은, 각각 독립적으로, 수소 원자, 탄소수 1 내지 6의 알킬기, 또는 환을 형성하는 탄소수가 13 이하인 아릴기 중 어느 하나를 나타내고, R 1 and R 6 each independently represent any one of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an aryl group having 13 or less carbon atoms forming a ring, R 2 내지 R 5 및 R 7 내지 R 10 은, 각각 독립적으로, 수소 원자, 또는 탄소수 1 내지 6의 알킬기, 치환되거나 치환되지 않은 페닐기, 또는 치환되거나 치환되지 않은 비페닐기 중 어느 하나를 나타낸다. Each of R 2 to R 5 and R 7 to R 10 independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or an unsubstituted or substituted biphenyl group. 바이폴라성 유기 화합물, 퀴녹살린 유도체, 캐리어 균형, 발광 소자, 발광 장치, 전자 기기, 구동 전압, 소비 전력. Bipolar organic compound, quinoxaline derivative, carrier balance, light emitting device, light emitting device, electronic device, driving voltage, power consumption.

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02-11-2021 дата публикации

Polymerizable liquid crystal compound, composition, liquid crystal polymer films thereof, method for producing same, and use thereof

Номер: CN107033076B
Автор: 大槻大辅
Принадлежит: JNC Corp, JNC Petrochemical Corp

本发明的目的在于提供一种能够控制波长分散特性的聚合性液晶化合物、组合物、其液晶聚合膜类及其制造方法及它们的用途。聚合性液晶化合物由式(1)所表示。 可例示如下方式:式(1)中,G为包含喹啉骨架、异喹啉骨架、喹噁啉骨架或喹唑啉骨架的基,A 1 为1,4‑亚苯基或1,4‑亚环己基,Z 1 为连结基,m为0~3的整数,R 1 为包含聚合性基的基。

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26-01-2021 дата публикации

Preparation method of tetrahydroquinoxaline compound

Номер: CN112266364A
Принадлежит: Yunnan Minzu University

本发明公开了一种四氢喹喔啉化合物的制备方法,包括以下步骤:1)以喹喔啉为起始原料,将喹喔啉、催化剂及硼烷加入反应管中,再添加一定量的有机溶剂在恒温下进行搅拌反应得到反应液;2)将所述反应液除去挥发性溶剂后通过柱层析纯化即得四氢喹喔啉化合物,所述四氢喹喔啉化合物的结构式为式I, ,其中,R1、R2、R3和R4均独立地选自氢、烷基、烷氧基或卤素。本发明采用有机小分子作为催化剂,以廉价易得的频那醇硼烷为氢源,无需过渡金属、无需氧化剂即可实现喹喔啉化物的氢化,可大大降低生产成本,具有显著的社会效益和经济效益;本发明制备方法操作简单,产率高,采用的催化条件温和且催化体系简单,反应选择性高,绿色环保。

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14-08-2018 дата публикации

Selective kinase inhibitors

Номер: US10045981B2
Автор: Haiching MA
Принадлежит: Jakpharm LLC

The present disclosure relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present disclosure further provides novel compounds and compositions as well as their methods of preparation and use. The disclosed JAK3 inhibitors may be used in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.

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09-06-2022 дата публикации

Tead inhibitors and uses thereof

Номер: WO2022120353A1
Принадлежит: Ikena Oncology, Inc.

The present invention provides compounds, compositions thereof, and methods of using the same.

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02-09-2015 дата публикации

A kind of preparation method of quinoxaline compound

Номер: CN103694182B
Принадлежит: ZHEJIANG ZHONGXIN CHEMICAL CO Ltd

本发明公开了一种喹喔啉类化合物的制备方法,属于化学合成技术领域。本发明以邻苯二胺和硝基烯化合物为原料,以L-脯氨酸为催化剂,以乙醇为溶剂,不需任何气体保护,在室温条件进行反应,制备喹喔啉类化合物,本发明具有原料和催化剂廉价易得,实验程序绿色无污染,实验操作简单有效,产物结构多样等优点。以廉价易得的脯氨酸为催化剂,从而避免了引入金属催化剂,而且反应温度较低易于实现工业化和规模化生产。

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03-07-2019 дата публикации

1,3-dithiolo[5,6-f]benzo-2,1,3-thiadiazole or 1,3-dithiolo[6,7-g]quinoxaline based organic semiconductors

Номер: EP3504216A1
Принадлежит: Merck Patent GmBH

The invention relates to novel organic semiconducting (OSC) compounds containing one or more 1,3-dithiolo[5,6-f]benzo-2,1,3-thiadiazole ("DTBTz") or 1,3-dithiolo[6,7-g]quinoxaline ("DTQ") units or derivatives thereof, to methods for their preparation and educts or intermediates used therein, to compositions and formulations containing them, to the use of the compounds and compositions as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices, perovskite-based solar cell (PSC) devices, organic photodetectors (OPD), organic field effect transistors (OFET) and organic light emitting diodes (OLED), and to OE devices comprising these compounds or compositions.

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10-01-2014 дата публикации

Photosensitive resin composition, photosensitive element utilizing the composition method for formation of resist pattern, and process for production of printed circuit board

Номер: KR101350547B1

바인더 폴리머와, 에틸렌성 불포화 결합을 가지는 광중합성 화합물과, 하기 식 (1), (2), 또는 (3)으로 표시되는 구조를 가지는 화합물로 이루어지는 군으로부터 선택되는 적어도 1종의 피라진 화합물을 함유하는 감광성 수지 조성물. [화학식 1] [화학식 2] [화학식 3] [식 (1)~(3) 중, R 1 ~R1 2 는 각각 독립적으로 알킬기, 시클로 알킬기, 페닐기, 나프틸기 또는 복소환식기를 포함하는 1가의 유기기를 나타내고, R 1 과 R 2 , R 3 와 R 4 , R 5 와 R 6 , R 7 과 R 8 , R 9 와 R 10 , R 11 과 R 12 는, 서로 결합하여 피라진 골격의 2개의 탄소 원자와 함께 환을 형성하고 있어도 된다. 식 (2), 중 X 및 Y는, 각각 독립적으로 피라진 골격의 2개의 탄소와 함께 형성된 단환구조 또는 축합다환구조의 방향족환을 구성하는 원자군을 나타니고, 식 (3) 중, Z는, 피라진 골격의 4개의 탄소와 함께 형성된, 단환구조 혹은 축합다환구조의 방향족환, 또는, 복소환을 구성하는 원자군을 나타낸다.] It contains a binder polymer, a photopolymerizable compound having an ethylenically unsaturated bond, and at least one pyrazine compound selected from the group consisting of a compound having a structure represented by the following formula (1), (2), or (3): The photosensitive resin composition. [Chemical Formula 1] (2) (3) [In formula (1)-(3), R < 1 > -R < 12 > respectively independently represents the monovalent organic group containing an alkyl group, a cycloalkyl group, a phenyl group, a naphthyl group, or a heterocyclic group, and R < 1> , R < 2> , R < 3> And R 4 , R 5 and R 6 , R 7 and R 8 , R 9 and R 10 , R 11 and R 12 may be bonded to each other to form a ring together with two carbon atoms of a pyrazine skeleton. In the formula (2), X and Y each independently represent an atomic group constituting an aromatic ring of a monocyclic structure or a condensed polycyclic structure formed with two carbons of a pyrazine skeleton, and in formula (3), Z is A group of atoms constituting an aromatic ring having a monocyclic structure or a condensed polycyclic structure formed with four carbons of the pyrazine skeleton, or a heterocyclic ring.]

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25-08-2021 дата публикации

Cures, optics, lenses, and compounds

Номер: JP6923744B2
Принадлежит: Fujifilm Corp

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20-08-2015 дата публикации

Use of indanthrene compounds in organic photovoltaics

Номер: AU2011216899B2
Принадлежит: BASF SE

Disclosed is an organic solar cell which comprises at least one photoactive region which comprises at least one indanthrene compound which is in contact with at least one fullerene compound, and the use of indanthrene compounds in organic photovoltaics, especially in the form of a component cell of a tandem cell.

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12-03-2009 дата публикации

Arylsulfonylaminomethylphosphonic acid derivatives, the preparation thereof and the use thereof as pharmaceutical compositions

Номер: CA2698486A1

The invention relates tosubstitutedarylsulphonylaminomethylphosphonic acid derivativesof general formula (I) wherein the groups R a to R f, A and Z are defined as mentioned in the specification and claims, which are suitable for preparinga medicament for the treatmentof metabolic disorders, particularlytype 1 or type 2 diabetesmellitus.

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23-09-2009 дата публикации

Quinoxaline derivative, and light-emitting element, light-emitting device, and electronic device using the same

Номер: CN101538248A
Принадлежит: Semiconductor Energy Laboratory Co Ltd

本发明的目的在于提供一种新的具有双极性的有机化合物。此外,本发明的目的还在于提供一种优越于载流子平衡的发光元件。此外,本发明的目的还在于提供一种驱动电压低且耗电量少的发光元件及发光装置。此外,本发明的目的还在于提供一种耗电量少的电子设备。本发明提供一种通式(G1)所示的喹喔啉衍生物。(在式中,α 1 、α 2 分别表示形成环的碳数为13以下的亚芳基,Ar表示形成环的碳数为13以下的芳基,R 1 、R 6 分别表示氢原子、碳数为1至6的烷基、形成环的碳数为13以下的芳基中的任一种,R 3 至R 5 、R 7 至R 10 分别表示氢原子、碳数为1至6的烷基、取代或没取代的苯基以及取代或没取代的联苯基中的任一种)。

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11-08-2017 дата публикации

Polymerizable liquid crystal compound, composition, its polymerizable mesogenic film class and its manufacture method and their purposes

Номер: CN107033076A
Автор: 大槻大辅
Принадлежит: Chisso Petrochemical Corp, JNC Corp

本发明的目的在于提供一种能够控制波长分散特性的聚合性液晶化合物、组合物、其液晶聚合膜类及其制造方法及它们的用途。聚合性液晶化合物由式(1)所表示。 可例示如下方式:式(1)中,G为包含喹啉骨架、异喹啉骨架、喹噁啉骨架或喹唑啉骨架的基,A 1 为1,4‑亚苯基或1,4‑亚环己基,Z 1 为连结基,m为0~3的整数,R 1 为包含聚合性基的基。

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17-02-2022 дата публикации

Beta adrenergic agonist and methods of using the same

Номер: AU2020300999A1
Принадлежит: Curasen Therapeutics Inc

The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor.

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