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

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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 8924. Отображено 200.
19-03-2020 дата публикации

Трис{ [1-(6-метилбензо[d]тиазол-2-ил)амино-1,4-диоксо-4-(п-толил)бут-2-ен-2-ил]окси} железо, обладающее противовоспалительным действием

Номер: RU2717242C2

Изобретение относится к области органической химии, к новым биологически активным веществам класса комплексных соединений N-гетариламидов 4-(гет)арил-2-гидрокси-4-оксобут-2-еновых кислот, а именно к соединению трис{[1-(6-метилбензо[d]тиазол-2-ил)амино-1,4-диоксо-4-(п-толил)бут-2-ен-2-ил]окси}железо формулы 1.Предложенное соединение обладает высоким противовоспалительным действием, а также низкой острой токсичностью и может быть использовано в качестве противовоспалительного средства. 1 табл., 1 пр.

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14-08-2017 дата публикации

НОВОЕ ПРОИЗВОДНОЕ 3-(4-(БЕНЗИЛОКСИ)ФЕНИЛ)ГЕКС-4-ИНОВОЙ КИСЛОТЫ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ПРОФИЛАКТИКИ И ЛЕЧЕНИЯ МЕТАБОЛИЧЕСКОГО ЗАБОЛЕВАНИЯ, ВКЛЮЧАЮЩАЯ ЕГО В КАЧЕСТВЕ ЭФФЕКТИВНОГО ИНГРЕДИЕНТА

Номер: RU2628077C2
Принадлежит: ХЕНДЭ ФАРМ КО., ЛТД (KR)

Изобретение относится к соединению, представленному формулой 1, его оптическому изомеру или его фармацевтически приемлемой соли:[Формула 1], а также к способам его получения и фармацевтической композиции на его основе. Технический результат: получены новые соединения, обладающие способностью активировать фермент GPR40, пригодные для применения для профилактики или лечения метаболического заболевания. 7 н. и 3 з.п. ф-лы, 7 табл., 77 пр., 2 ил.

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20-09-2012 дата публикации

НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ СОЛИ

Номер: RU2461542C2
Принадлежит: САНДОЗ АГ (CH)

Изобретение относится к новому способу получения одной кристаллической полиморфной формы гидрогалогенида органического амина предпочтительно в сравнении с другой кристаллической полиморфной формой гидрогалогенида органического амина. Способ включает добавление триалкилсилилгалогенида к органическому амину в растворителе, где триалкилсилилгалогенид добавляется в условиях, в которых одна полиморфная форма кристаллизуется предпочтительно в сравнении с другой полиморфной формой, и где органический амин находится в форме свободного основания или кислотно-аддитивной соли. Причем, если органический амин находится в форме кислотно-аддитивной соли, сопряженная кислота кислотно-аддитивной соли является более слабой, чем гидрогалогеновая кислота, и растворитель представляет собой апротонный растворитель, а если органический амин находится в форме свободного основания, то он растворяется в апротонном растворителе, а триалкилсилилгалогенид добавляется в протонном растворителе. Органический амин представляет ...

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20-05-2007 дата публикации

7-АМИНОБЕНЗОТИАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ЛИГАНДОВ АДЕНОЗИНОВОГО РЕЦЕПТОРА

Номер: RU2299203C2

Изобретение относится к соединениям, которые обладают сродством к аденозиновому рецептору А2А и представляют собой соединения общей формулы в которой R1, R2 независимо друг от друга представляют собой водород, низший алкил, тетрагидропиран-2,3- или 4-ил, -(СН2)n-О-низший алкил, -С(O)-низший алкил, -(СН2)n-С(O)-низший алкил, -(CH2)n-C(O)-NR'R", -(СН2)n-фенил, необязательно замещенные низшим алкилом, низшим алкокси или -(СН2)n-пиридинил, -(СН2)n-тетрагидропиран-2,3- или 4-ил, -С(O)-пиперидин-1-ил или R1 и R2 вместе с атомом N, к которому они присоединены, образуют кольцо 2-окса-5-азабицикло[2,2,1]гепт-5-ил; R3 представляет собой низший алкокси, фенил, необязательно замещенный галогеном, -(CH2)n-галогеном или -(CH2)n-N(R')-(CH2)n+1-O-низшим алкилом, или представляет собой пиридинил, необязательно замещенный низшим алкилом, галогеном или морфолинилом, n обозначает 1 или 2; R'/R" независимо друг от друга представляют собой водород или низший алкил, и их фармацевтически приемлемые кислотные аддитивные ...

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10-07-2009 дата публикации

НОВЫЕ ПРОИЗВОДНЫЕ 3-ФЕНИЛПРОПИОНОВОЙ КИСЛОТЫ ДЛЯ ЛЕЧЕНИЯ ДИАБЕТА

Номер: RU2360906C2
Принадлежит: АДАМЕД СП.З О.О. (PL)

Изобретение относится к производным 3-фенилпропионовой кислоты формулы (I) в качестве лиганда гамма-рецептора пролифератора-активатора пероксисом (PPARγ), к их фармацевтически приемлемым солям, а также к их применению, способу лечения и фармацевтической композиции на их основе. Соединения могут найти примененение для лечения и профилактики заболеваний, опосредованных гамма-рецептором пролифератора-активатора пероксисом (PPARγ), например диабета типа 2, резистентности к инсулину, метаболического синдрома, осложнений, являющихся результатом или связанных с диабетом, сердечно-сосудистых расстройств, атеросклероза, ожирения, когнитивных расстройств и расстройств метаболизма липидов. В общей формуле (I) ! ! W представляет СООН или -СОО-С1-С4-алкильную группу; Y представляет NH; Z представляет S или О; Х представляет О; R1-R8 каждый независимо представляет атом водорода или атом галогена; А представляет моно-, би- или трициклический 5-13-членный гетероарил с 1 или 2 гетероатомами, выбранными ...

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10-06-2009 дата публикации

ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ АРИЛАЛКИЛЬНЫХ ПРОИЗВОДНЫХ КИСЛОТ ДЛЯ ЛЕЧЕНИЯ ОЖИРЕНИЯ

Номер: RU2357959C2

Изобретение относится к новым соединениям формулы (I) и его фармацевтически приемлемым солям и эфирам. Соединения настоящего изобретения обладают свойствами ингибитора DGAT-1. В общей формуле (I) ! ! Q представляет собой О, S или NR5; А представляет собой линкер, выбранный из , где p равно 1 или 2 и , где m равно 0 и n равно 1, 2, 3 или 4, или m равно 1 и n равно 1, 2 или 3, где указанный линкер необязательно замещен одной или двумя группами R8; R1 и R2 независимо выбирают из водорода, галоида; R3 выбирают из водорода, (С1-С6)алкила, необязательно замещенного гидроксилом, и фенила, необязательно замещенного галоидом; R4 выбирают из водорода, нитро- и (С1-С6)алкила; или R3 и R4 вместе с атомами углерода, к которым они присоединены, могут образовывать бензольное кольцо, необязательно замещенное 1-2 заместителями. Изобретение также относится к соединениям формул (Ia) и (Ib), структурные формулы которых представлены в формуле изобретения, а также к фармацевтической композиции, лекарственному ...

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27-06-2012 дата публикации

СИНТЕЗ ХИРАЛЬНО ОЧИЩЕННЫХ ЗАМЕЩЕННЫХ БЕНЗОТИАЗОЛДИАМИНОВ

Номер: RU2454409C2

В изобретении представлены способы получения хирально очищенных замещенных 4,5,6,7-тетрагидробензотиазолдиаминов, таких как, например, (6R)-2-амино-4.5,6,7-тетрагидро-6-(пропиламино)бензотиазол, и их солей, а также очистка преобладающего энантиомера замещенных 4,5,6,7-тетрагидробензотиазолдиаминов из энантиомерно обогащенных смесей замещенных 4,5,6,7-тетрагидробензотиазолдиаминов. 2 н. и 21 з.п. ф-лы, 6 табл., 7 ил., 25 пр.

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27-07-2010 дата публикации

ПРОИЗВОДНЫЕ ФЕНИЛ-ПИПЕРАЗИН МЕТАНОНА

Номер: RU2395502C2

Изобретение относится к новым соединениям общей формулы ! ! где R1 представляет собой группу ! или или ! или ! R2 представляет собой морфолин или представляет собой OR' или N(R'')2; R' представляет собой низший алкил, низший алкил, замещенный галогеном, или -(СН2)n-циклоалкил; R'' представляет собой низший алкил; R3 представляет собой NO2 или SO2R'; R4 представляет собой водород, гидрокси, галоген, NO2, низший алкокси, SO2R' или C(O)OR''; R5/R6/R7 представляют собой водород, галоген, низший алкил; Х1/Х1' представляют собой СН или N при условии, что Х1/Х1' одновременно не являются СН; X2 представляет собой О или S; n представляет собой 0 или 1; и к их фармацевтически активным кислотно-аддитивным солям. Изобретение также относится к лекарству. Технический результат - получение новых биологически активных соединений, обладающих активностью в качестве ингибиторов переносчика глицина 1. 2 н. и 9 з.п. ф-лы, 1 табл.

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02-02-2021 дата публикации

МОЛЕКУЛЫ С ПЕСТИЦИДНОЙ ФУНКЦИЕЙ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, КОМПОЗИЦИИ И СПОСОБЫ, СВЯЗАННЫЕ С НИМИ

Номер: RU2742119C2

Изобретение относится к молекулам, имеющих пестицидную функцию в отношении вредителей типов членистоногие, моллюски и нематоды. Предложено соединение формулы (1), где R1и R5выбраны из H, F, Cl, Br и I; R2и R4выбраны из H, F, Cl, Br, I, CN, (C1-C4)алкила, (C1-C4)алкокси и (C1-C4)галогеналкила; R3выбран из H, F, Cl, Br, I, NO2и (C1-C4)галогеналкокси; R6и R15выбраны из H и (C1-C4)алкила; R7и R8выбраны из группы, состоящей из F, Cl, Br и I; R9, R10,R11, R12и R14представляют собой H; R13выбран из H, F, Cl, Br, I и (C1-C4)галогеналкила; R16выбран из группы, состоящей из (C3-C8)циклоалкила, азетидинила, изоксазолидинонила, морфолинила, оксазолидинонила, оксетанила, тетрагидрофуранила, тетрагидропиранила, тетрагидротиофенила, тетрагидротиофенил-оксида, тетрагидротиофенил-диоксида, который может быть необязательно замещен одним или более заместителями, выбранными из группы, состоящей из H, F, Cl, Br, I, CN, оксо, (C1-C4)алкила, (C1-C4)галогеналкила, C(=O)O(C1-C4)алкила, (C=O)NH(C1-C4)алкила, (C= ...

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20-02-2012 дата публикации

АРИЛСУЛЬФОНИЛМЕТИЛЬНЫЕ ИЛИ АРИЛСУЛЬФОНАМИДНЫЕ ПРОИЗВОДНЫЕ АРОМАТИЧЕСКИХ СОЕДИНЕНИЙ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ РАССТРОЙСТВ, ВОСПРИИМЧИВЫХ К ЛЕЧЕНИЮ ЛИГАНДАМИ ДОФАМИНОВЫХ D3 РЕЦЕПТОРОВ, С ИХ ПОМОЩЬЮ

Номер: RU2442781C2

Настоящее изобретение относится к соединениям формулы I и физиологически переносимым солям присоединения кислот указанных соединений. Соединения формулы I или их фармацевтически приемлемые соли могут быть использованы для приготовления фармацевтических композиций с целью лечения медицинских расстройств, восприимчивых к лечению лигандами дофаминовых рецепторов D3. 3 н. и 44 з.п. ф-лы, 2 табл., 81 пр.

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20-11-2003 дата публикации

ГЕТЕРОАРИЛ-1-ПИПЕРИДИНЫ И ПИПЕРАЗИНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБ ЛЕЧЕНИЯ ПСИХОЗОВ И ОСЛАБЛЕНИЯ БОЛИ

Номер: RU2216545C2

Описываются гетероарил-1-пиперидины и пиперазины общей формулы (I), где Х представляет собой О, S, NH или М(R2), R2 выбран из группы: бензоил, (С2-С18)алканоил и алкоксикарбонил, р = 1, Y - водород, хлор, фтор, Q - пиперидинил или пиперазинил, замещенный в 1 положении Y2, Y2 выбирают из 21 группы. Описываются также фармацевтическая композиция на основе этих соединений, способ ослабления боли и лечения психозов с использованием соединений, а также 1-[4-(3-хлорпропокси)-3-метоксифенил]-2-гидроксиэтанон, являющийся исходным соединением в синтезе соединений формулы (I). Технический результат - антипсихотические и анальгетические свойства соединений позволяют использовать их для ослабления боли и лечения психозов. 13 с. и 112 з. п. ф-лы, 2 табл.

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24-03-2022 дата публикации

НОВОЕ СОЕДИНЕНИЕ, ПРОЯВЛЯЮЩЕЕ ИНГИБИРУЮЩУЮ АКТИВНОСТЬ В ОТНОШЕНИИ ЭНТЕРОПЕПТИДАЗЫ

Номер: RU2768755C1
Принадлежит: ЭлДжи КЕМ, ЛТД. (KR)

Изобретение относится к новым гетероароматическим соединениям. Предложено соединение, имеющее химическую формулу (1a) или (1b), или его фармацевтически приемлемая соль, где каждый из A1, A2, A3, A4 и A5 независимо представляет собой С; Q представляет собой O или N; каждый из R1 и R6 независимо представляет собой H или незамещенный или замещенный C1-C6 алкил, или R1 и R6 вместе с атомом азота, к которому они присоединены, образуют незамещенное или замещенное 5-6-членное гетероциклическое кольцо, содержащее от 1 до 2 атомов N; каждый из R3 и R4 независимо представляет собой Н или галоген; и R5 представляет собой амидин или гуанидин, или где каждый из A1, A2, A3, A4, A5, A6, A7 и A8 независимо представляет собой C; Q представляет собой O; каждый из R1 и R6 независимо представляет собой H, незамещенный или замещенный C1-C6 алкил, или R1 и R6 вместе с атомом азота, к которому они присоединены, образуют незамещенное или замещенное 5-6-членное гетероциклическое кольцо, содержащее от 1 до 2 атомов ...

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29-01-2021 дата публикации

Номер: RU2019114961A3
Автор:
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22-11-2019 дата публикации

ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Номер: RU2707067C2

Изобретение относится к способу получения соединения формулы (IVa):или его фармацевтически приемлемой соли или стереоизомера. Способ включает обработку гидроксиалкилтиофена формулы (i):(i),аминоальдегид ацеталем и кислотой с получением соединения формулы (IVa), где m равно 0, n равно 1, Rи Rявляются, каждый независимо, водородом или Салкилом, Rи Rявляются, каждый независимо, водородом или Салкилом, Rпредставляет собой водород, и Rи Rявляются, каждый независимо, водородом, галогеном или Салкилом. Также предложены способы получения конкретных соединений формулы (IVa). Изобретение позволяет получить соединения, которые применятся для предотвращения и/или проведения лечения неврологических нарушений. 3 н. и 25 з.п. ф-лы, 2 табл.

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10-03-1999 дата публикации

ПРОИЗВОДНЫЕ БЕНЗОЛА

Номер: RU2127254C1

Соединения, представленные формулой I, в которой R1 - водород, гидроксил, С1-9 - ацилокси группа или низший алкоксил; R2 и R3 - Н, галоген, низший алкил, алкоксил; R4 - Н или низший алкил; А - фрагмент, представленный формулой II; R5 - Н, алкил, алкоксил, фенил, пиролидин, 5-членное кольцо, содержащее два атома кислорода, в случае которого атом углерода, к которому оно присоединено, является спироатомом; или фрагмент представленный формулами III - XVI; R6 и R7 - Н, алкил, арил или гетероциклическая группа; n = 2,3,4,5 или 6, или их возможные стереоизомеры или оптические изомеры, или их фармацевтически приемлемые соли. Соединения формулы I оказывают ингибирующее действие на перегрузку кальция в дополнение к их сосудорасширяющей активности и ингибирующее действие на липидное переокисление и полезны в качестве профилактических или лечебных средств в случаях ишемичееких болезней и гипертонии. 30 з.п. ф-лы, 37 табл.

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19-06-1995 дата публикации

ПРОИЗВОДНЫЕ 2-ИМИНО-БЕНЗОТИАЗОЛИНОВ, ИХ ЭНАНТИОМЕРЫ ПРИ НАЛИЧИИ АСИММЕТРИЧНОГО ЦЕНТРА И ИХ КИСЛОТНО-АДДИТИВНЫЕ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Номер: RU2037489C1
Принадлежит: Рон-Пуленк Санте (FR)

Сущность изобретения: производные 2-иминобензотиазолинов ф-лы I, где R1 -полифтор C1-C4 алкил или полифтор C1-C4 алкоксигруппа, R2 -группа ф-лы CH2[CH(R4)]n-R3, где R3-qu-(C1-C4) алкиламиногруппа, 1-пиперидинил, 1-пирролидинил, меркаптогруппа, C1-C4 ацилтиогруппа, C1-C4 алкилтиогруппа, C1-C4 алкилсульфинил- или C1-C4 алкилсульфонилгруппа: R4 -атом водорода или C1-C4 алкил и n=0 или 1: или R2 -группа ф-лы II, их энантиомеры при наличии асимметричного центра, их кислотно-аддитивные фармацевтически приемлемые соли и фармацевтическая композиция на их основе. Структура соединения ф-лы I и II (см. чертеж). 2 с.п. ф-лы, 1 ил.

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27-02-2006 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 2, 6-ДИАМИНО-4, 5, 6, 7-ТЕТРАГИДРОБЕНЗОТИАЗОЛА

Номер: RU2005117364A
Принадлежит:

... 1. Способ получения 2,6-диамино-4,5,6,7-тетрагидробензотиазола, включающий следующие последовательные стадии: (i) взаимодействие брома с водным раствором 4-ацетамидоциклогексанона с получением 2-бром-4-ацетамидоциклогексанона; (ii) добавление тиомочевины с получением 6-ацетиламино-2-амино-4,5,6,7-тетрагидробензотиазола; (iii) добавление водного раствора бромоводородной кислоты с получением 2,6-диамино-4,5,6,7-тетрагидробензотиазола; и (iv) выделение 2,6-диамино-4, 5,6,7-тетрагидробензотиазола. 2. Способ по п.1, отличающийся тем, что стадию (iii) проводят без выделения 6-ацетиламино-2-амино-4,5,6,7-тетрагидробензотиазола, полученного на стадии (ii). 3. Способ по п.1 или 2, отличающийся тем, что любые три последовательных стадии (i)-(iv) проводят в одном реакционном сосуде. 4. Способ по п.1, отличающийся тем, что стадии (i)-(iv) проводят в одном реакционном сосуде. 5. Способ по п.1, дополнительно включающий перед стадией (i) стадию окисления 4-ацетамидоциклогексанола с получением 4-ацетамидоциклогексанона ...

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27-07-2006 дата публикации

ПРОИЗВОДНЫЕ БЕНЗОТИАЗОЛА И ИХ ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АДЕНОЗИНОВЫМИ А2А-РЕЦЕПТОРАМИ

Номер: RU2005141307A
Принадлежит:

... 1. Соединения общей формулы в которой R1 представляет собой С5-С6-циклоалкил, замещенный группой CF3, низший алкил, -(СН2)nОН или -(СН2)n-O-низший алкил, или означает 1-бицикло[2,2,1]гепт-2-ил, 1-(7-окса-бицикло[2,2,1]гепт-2-ил, 1-(5-экзо-гидроксибицикло[2,2,1]гепт-2-экзо-ил, 1-(5-экзо-гидроксибицикло[2,2,1]гепт-2-эндо-ил, или означает 1-адамантан-1-ил; R2 представляет собой низший алкил; или R1 и R2 вместе с атомом N образуют группу 8-окса-3-аза-бицикло [3,2,1 ] октан; n означает 0 или 1, и фармацевтически приемлемые соли этих соединений. 2. Соединения формулы I по п.1, где R1 представляет собой С5-С6 циклоалкил, замещенный группой CF3, низший алкил, -(CH2)nOH или -(CH2)nO-низший алкил. 3. Соединения формулы I по п.2, которые представляют собой следующие соединения: 3-(4-метокси-7-морфолин-4-ил-бензотиазол-2-ил)-1-метил-1-(4-трифторметилциклогексил)мочевина, (транс)-3-(4-метокси-7-морфолин-4-ил-бензотиазол-2-ил)-1-метил-1-(4-метилциклогексил)мочевина, (транс)-1-(4-гидроксиметилциклогексил ...

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20-02-2008 дата публикации

ГЕТЕРОАРОМАТИЧЕСКИЕ ПРОИЗВОДНЫЕ МОЧЕВИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ АКТИВАТОРОВ ГЛЮКОКИНАЗЫ

Номер: RU2006122209A
Принадлежит:

... 1. Соединение общей формулы (I) где R1 представляет собой С3-8-циклоалкил, С3-8-циклоалкенил, С3-8-гетероциклил, С3-8-гетероциклоалкенил, конденсированный арил-С3-8-циклоалкил или конденсированный гетероарил-С3-8-циклоалкил, каждый из которых возможно замещен одним или более чем одним заместителем R3, R4, R5 и R6; R2 представляет собой С3-8-циклоалкил, С3-8 -циклоалкенил, С3-8-гетероциклил, С3-8-гетероциклоалкенил, конденсированный арил-С3-8-циклоалкил или конденсированный гетероарил-С3-8-циклоалкил, каждый из которых возможно замещен одним или более чем одним заместителем R30, R31, R32 и R33, и R3, R4, R5, R6, R30, R31, R32 и R33 независимо выбраны из группы, состоящей из галогена, нитро, циано, гидрокси, оксо, карбокси, -CF3; либо - NR10R11; либо С1-6-алкила, С2-6-алкенила, С2-6-алкинила, С3-8-циклоалкила, С3-8-циклоалкил-С1-6-алкила, арила, арил-С1-6-алкила, гетероарил-С1-6-алкила, С1-6-алкокси, С3-6-циклоалкил-С1-6-алкокси, арил-С1-6-алкокси, гетероарила, гетероарил-С1-6-алкокси, арилокси ...

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27-07-2011 дата публикации

НОВОЕ СУЛЬФОНАМИДНОЕ ПРОИЗВОДНОЕ МАЛОНОВОЙ КИСЛОТЫ И ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

Номер: RU2010101633A
Принадлежит:

... 1. Производное сульфонилмалонамида, представленное следующей формулой (I) ! ! где R1 представляет собой необязательно замещенный C1-8 алкил, необязательно замещенный C2-6 алкенил, необязательно замещенный C2-6 алкинил, необязательно замещенный C3-10 циклоалкил, необязательно замещенный C3-10 циклоалкил C1-6 алкил, необязательно замещенный гетероцикл, необязательно замещенный арил, необязательно замещенный арил C1-6 алкил, необязательно замещенный арилокси C1-6 алкил, необязательно замещенный арил C2-6 алкенил, необязательно замещенный гетероарил, необязательно замещенный гетероарил C1-6 алкил, необязательно замещенный гетероарилокси C1-6 алкил или необязательно замещенный гетероарил C2-6 алкенил; ! один из R2 и R3 представляет собой атом водорода или атом галогена, а другой представляет собой атом галогена, необязательно замещенный C1-6 алкил, необязательно замещенный C1-6 алкокси, необязательно замещенный C2-6 алкенил, необязательно замещенный C2-6 алкинил, -(CH2)n-С(O)-NR5R6 (где n представляет ...

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10-07-2010 дата публикации

НОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ЛИГАНДОВ КАННАБИНОИДНЫХ РЕЦЕПТОРОВ И ИХ ПРИМЕНЕНИЕ

Номер: RU2008152788A
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... 1. Соединение формулы (I) !! или его фармацевтически приемлемая соль, пролекарство, соль пролекарства или их комбинация, где ! R1 представляет собой алкоксиалкил, алкоксиалкоксиалкил, гидроксиалкил, A или A-алкилен; ! R2 представляет собой атом водорода, алкокси, алкоксиалкил, алкоксикарбонил, алкоксикарбонилалкил, алкил, алкил-S(O)2-, арил, арилалкил, арилалкенил, азидоалкил, циано, циклоалкил, галоген, галогеналкил, гетероарил, гетероцикл, -(CR21R22)m-OH, RaRbN-, RaRbN-алкил-, RcRdNC(О)- или R8-R7-; ! R3 представляет собой атом водорода, алкокси, алкоксиалкил, алкил, алкилкарбонил, алкил-S(О)2-, арил, арилалкил, арилалкенил, циано, циклоалкил, галоген, галогеналкил, гетероарил, гетероцикл, -(CR31R32)m-OH, RaRbN-, RaRbN-алкил- или R8-R7; или ! R2 и R3 вместе с атомами углерода, к которым они присоединены, образуют 4-, 5-, 6- или 7-членное моноциклическое кольцо, необязательно конденсированное с бензольным кольцом или моноциклическим гетероарилом, причем указанное моноциклическое кольцо ...

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27-01-2009 дата публикации

НОВЫЕ ПРОИЗВОДНЫЕ 3-ФЕНИЛПРОПИНОВОЙ КИСЛОТЫ ДЛЯ ЛЕЧЕНИЯ ДИАБЕТА

Номер: RU2007127724A
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... 1. Производные 3-фенилпропионовой кислоты формулы (I) где W представляет COOH или -COO-C1-C4-алкильную группу; Y представляет NH, N-C1-C10-алкил; Z представляет NH, N-C1-C10-алкил, N-арил, N-гетероарил, S или O; X представляет O; R1-R8 каждый независимо представляет атом водорода или заместитель, выбранный из группы, включающей C1-C4-алкил, C1-C4-алкокси, C3-C7-циклоалкил, C3-C7-циклоалкокси, C1-C4-тиоалкокси, C3-C7-циклотиоалкокси, атом галогена, замещенный галогеном C3-C7-циклоалкил, арил, гетероарил, -NO2, -CN, -SO2-NH2, -SO2-NH-C1-C4-алкил, -SO2-N(C1-C4-алкил)2, -CO-C1-C4-алкил, -O-CO-C1-C4-алкил, -CO-O-C1-C4-алкил, -CO-арил, -CO-NH2, -CO-NH-C1-C4-алкил, -CO-N(C1-C4-алкил)2; А представляет C1-C4-алкил, C3-C7-циклоалкил, замещенный галогеном C3-C7-циклоалкил, арил, гетероарил, гетероциклил, -NH-CO-C1-C4-алкил, N(C1-C4-алкил)-CO-C1-C4-алкил, -NH-CO-арил, -N(C1-C4-алкил)-CO-арил, N(C1-C4-алкил)-CO-гетероарил, -N(C1-C4-алкил)-CO-C3-C7-циклоалкил, -NH-CO-NH2, -NH-CO-NH-C1-C4-алкил, -NH-CS-NH-C1 ...

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10-12-1996 дата публикации

ГИДРОКСИЭТИЛАМИНОСУЛЬФОНАМИДЫ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ИНГИБИРОВАНИЯ РЕТРОВИРУСНЫХ ПРОТЕАЗ, СПОСОБ ЛЕЧЕНИЯ РЕТРОВИРУСНЫХ ИНФЕКЦИЙ, СПОСОБ ЛЕЧЕНИЯ СПИДА

Номер: RU95106624A
Принадлежит:

В изобретении предлагаются гидроксиэтиламиносульфонамидные соединения α- и b-аминокислот, эффективные в качестве ингибиторов ретровирусных протеаз и, в частности, в качестве ингибиторов протеазы ВИЧ, а также фармацевтические композиции.

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10-06-2012 дата публикации

ПРОИЗВОДНОЕ ЦИКЛОПЕНТИЛАКРИЛАМИДА

Номер: RU2010142229A
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... 1. Соединение, представленное общей формулой (1) или его фармацевтически приемлемая соль ! [химическая формула 1] ! ! (в которой R1 и R2 независимо представляют атом водорода, атом галогена, аминогруппу, гидроксильнуную группу, гидроксиаминогруппу, нитрогруппу, цианогруппу, сульфамоильную группу, C1-С6 алкильную группу, С1-С6 алкоксигруппу C1-С6 алкилсульфанильную группу, C1-С6 алкилсульфинильную группу, С1-С6 алкилсульфонильную группу или С1-С6алкокси-С1-С6 алкилсульфонильную группу, а А - замещенную или незамещенную гетероарильную группу). ! 2. Соединение по п.1 или его фармацевтически приемлемая соль, отличающееся тем, что R1 и R2 независимо представляют собой атом водорода, атом галогена или С1-С6 алкилсульфонильную группу. ! 3. Соединение по п.1 или его фармацевтически приемлемая соль, отличающееся тем, что R1 представляет собой атом водорода или атом галогена, a R2 представляет собой С1-С6 алкилсульфонильную группу. ! 4. Соединение по п.1 или его фармацевтически приемлемая соль, отличающееся ...

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10-11-2009 дата публикации

ПРОИЗВОДНЫЕ 3-ЦИКЛИЛ-2-(4-СУЛЬФАМОИЛФЕНИЛ)-N-ЦИКЛИЛПРОПИОНАМИДА, ПРИМЕНИМЫЕ ДЛЯ ЛЕЧЕНИЯ НАРУШЕННОЙ ПЕРЕНОСИМОСТИ ГЛЮКОЗЫ И ДИАБЕТА

Номер: RU2008116575A
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... 1. Соединение формулы ! ! в которой ! Q совместно с атомами углерода и азота, к которым он присоединен, образует 5-6-членное моноциклическое гетероароматическое кольцо; или ! Q совместно с атомами углерода и азота, к которым он присоединен, образует 9-10-членный бициклический гетероцикл; ! R1 и R2 независимо друг от друга обозначают водород, галоген, цианогруппу, нитрогруппу, необязательно замещенный алкил, алкоксигруппу, алкилтиогруппу, алкилтионогруппу, сульфонил, свободную или этерифицированную карбоксигруппу, карбамоил, сульфамоил, необязательно замещенную аминогруппу, арил или гетероциклил; или ! R2 отсутствует; ! R3 обозначает С3-С6циклоалкил или С3-С6гетероциклил; ! R4 обозначает водород, галоген, цианогруппу, низш. алкил или низш. алкоксигруппу; ! R5 обозначает водород, необязательно замещенный алкил или циклоалкил; ! R6 обозначает -(CR7R8)m-W-R9, в котором ! R7 и R8 независимо друг от друга обозначают водород, необязательно замещенный алкил или циклоалкил; или ! R7 и R8 вместе ...

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20-11-2014 дата публикации

ЛЕЧЕНИЕ РАКА/ИНГИБИРОВАНИЕ МЕТАСТАЗИРОВАНИЯ

Номер: RU2013121744A
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... 1. Композиция для применения в(а) способе уменьшения метастатического поведения или(б) способе предотвращения метастатического поведения у пациента, страдающего от ракового заболевания, связанного с экспрессией потенциалзависимых натриевых каналов (VGSC), причем указанную композицию применяют в дозировке, которая по меньшей мере уменьшает незатухающую часть тока VGSC без устранения переходной части.2. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, обладающая указанным эффектом без уничтожения клеток.3. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, обладающая указанным эффектом без существенного влияния на пролиферацию.4. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, отличающаяся тем, что метастатическое поведение представляет собой по меньшей мере одно из следующих:(i) адгезивность, причем композиция увеличивает адгезивность ...

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10-01-2014 дата публикации

ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Номер: RU2012127770A
Принадлежит:

... 1. Соединение формулы (I):или его фармацевтически приемлемая соль или стереоизомер, гдеодин из Х и Y является O, а другой является CH; или оба, и Х, и Y, являются CH;один из Z, Zи Zявляется S; и (i) два из Z, Zи Zявляются C; или (ii) один из Z, Zи Zявляется C, и один из Z, Zи Zявляется N;Rи Rявляются, каждый независимо, (i) водородом, алкилом, алкоксилом, аминоалкилом, алкенилом, алкинилом, циклоалкилом, циклоалкилалкилом, арилом или аралкилом, каждый из которых является необязательно замещенным; или (ii) -(CH)-R, где Rявляется SOалкилом или SOарилом, каждый из которых является необязательно замещенным; или (iii) Rи Rвместе с атомом азота, к которому они присоединены, образуют необязательно замещенный гетероциклил или гетероарил;Rи Rявляются, каждый независимо, (i) водородом, алкилом, алкоксилом, аминоалкилом, алкенилом, алкинилом, циклоалкилом, циклоалкилалкилом, арилом или аралкилом, каждый из которых является необязательно замещенным; или (ii) -(CH)-R, где Rявляется CF, CN, нитро, амино ...

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15-07-1989 дата публикации

Способ получения 2-(4-метоксифенилпропионил)-амино-6-н-пропиламино-4,5,6,7-тетрагидробензотиазола в виде рацемата или (-)-энантиомера или его кислотно-аддитивной соли

Номер: SU1494867A3

Изобретение касается гетероциклических соединений ,в частности, способа получения 2-(4-метоксифенилпропионил) -амино-6-н -пропиламино-4,5,6,7-тетрагидробензотиазола в виде рацемата или (-) -энантиомера или его кислотно-аддитивной соли, который может быть использован в медицине для лечения болезни Паркинсона. Цель - создание нового активного более длительно действующего соединения указанного класса. Процесс ведут взаимодействием 2-(4-метоксифенилпропионил)амино-6-оксо-тетрагидробензотиазола с н-пропиламином в присутствии восстановителя с последующим выделением целевого продукта в виде рацемата или (-)-энантиомера или их кислотно-аддитивной соли. Выход рацемата 63%, для основания т.пл. 105-106°С, для дигидрохлорида т.пл. 259-261°С. Испытания показывают, что новые соединения в дозе 50 мкг/кг имеют продолжительность действия 20 ч при низкой токсичности против 6 ч для известного соединения в той же дозе.

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06-09-2007 дата публикации

CYKLISIERUNGSVERFAHREN FÜR BENZOTHIAZOLDERIVATE

Номер: DE0060307682T2
Автор: SPURR PAUL, SPURR, PAUL
Принадлежит: HOFFMANN LA ROCHE, F. HOFFMANN-LA ROCHE AG

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08-01-1976 дата публикации

Номер: DE0002405289B2
Принадлежит: NIPPON SODA CO., LTD., TOKIO

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02-11-1978 дата публикации

VERFAHREN ZUR HERSTELLUNG VON HARNSTOFFDERIVATEN

Номер: DE0002818947A1
Принадлежит:

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10-08-2006 дата публикации

New thiazolo-indazole derivatives useful as PI3 kinase inhibitors, for treating e.g. cancer and other proliferative diseases, viral infections and inflammatory, autoimmune, skin and bone diseases

Номер: DE102005005813A1
Принадлежит:

Thiazolo[4,5-g]indazole derivatives (I) are new. Thiazolo[4,5-g]indazole derivatives (I) of formula (1) and their tautomers, isomers and acid addition salts are new: R 1> : NHRc, NHCORc, NHCOORc, NHCONRcRd or NHCOSRc; R 2> : 1-6C alkyl, 3-8C cycloalkyl, 3- to 8-membered heterocycloalkyl, 6-10C aryl or 5- to 10-membered heteroaryl, all optionally substituted with R 4>; R 3> : 6-10C aryl or 5- to 10-membered heteroaryl, all optionally substituted with Re and/or Rf; R 4> : Ra (optionally substituted with Rc and/or Rb) or Rb; Ra : 1-6C alkyl, 3-8C cycloalkyl, 4-11C cycloalkylalkyl, 6-10C aryl, 7-16C arylalkyl, 2- to 6-membered heteroalkyl, 3- to 8-membered heterocycloalkyl, 4- to 14-membered heterocycloalkylalkyl, 5- to 10-membered heteroaryl or 6- to 16-membered heteroarylalkyl; Rb : =O, ORc, 1-3C haloalkoxy, OCF 3, =S, SRc, =NRc, =NORc, NRcRc, halo, CF 3, CN, NC, OCN, SCN, NO, NO 2, =N 2, N 3, SORc, SO 2Rc, SO 2ORc, SONRcRc, SO 2NRcRc, OSORc, OSO 2Rc, OSO 2ORc, OSO 2NRcRc, CORc, COORc, CONRcRc ...

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06-05-1970 дата публикации

Mikrobizide Mittel

Номер: DE0001953149A1
Автор: STEFAN JANIAK DR
Принадлежит:

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26-05-1976 дата публикации

BENZENESULPHONYL-UREAS AND PROCESSES FOR PREPARING THEM

Номер: GB0001437036A
Автор:
Принадлежит:

... 1437036 Benzene sulphonyl ureas HOECHST AG 7 Aug 1973 [7 Aug 1972] 37341/73 Heading C2C [Also in Division A5] The invention comprises compounds having the general formula in which X is a 5- or 6-membered aromatic nitrogen-containing heterocyclic ring which may be substituted by one or two methyl groups and/or fused with a benzene ring, which ring may contain a further nitrogen, oxygen, or sulphur atom and which is linked to the rest of the molecule via the atom adjacent to the nitrogen atom; R represents an alkyl group of up to 3 carbon atoms; and R1 is C 3 to C 6 alkyl, C 5 to C 9 cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, or alkylcycloalkenyl or a cyclohexenylmethyl, chlorocyclohexyl, bicycloheptenylmethyl, bicycloheptylmethyl, bicycloheptenyl, bicycloheptyl, nortricyclyl, adamantyl or benzyl group. They may be prepared by (a) reacting a benzenesulphonylisocyanate, benzenesulphonyl-carbamate, thiocarbamate, sulphonyl-urea, sulphonyl-semicarbazide or semicarbazone ...

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13-03-1985 дата публикации

CHEMICAL COMPOUNDS

Номер: GB0008503541D0
Автор:
Принадлежит:

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19-04-1967 дата публикации

3-(2-benzthiazolyl)-1-ethylureas and their application as fungicides

Номер: GB0001065589A
Автор:
Принадлежит:

The invention comprises the compounds of formula wherein R is H or C2H5. The compounds are used in fungicidal compositions (see Division A5). In examples: (1) 3-(2-benzthiazolyl)-1-ethylurea is prepared by condensing 2-aminobenzothiazole with ethyl isocyanate; (2) 3 - (2 - benzthiazolyl) - 1,1 - diethylurea is prepared by reacting 2-aminothiophenol with diethylcarbamoyl isothiocyanate.ALSO:Fungicidal compositions comprise a biologically inert carrier and a fungitoxic quantity of a compound of formula wherein R is H or C2H5. The compositions may be in spray emulsion, vapour, wettable powder or dust form. Specified solid carriers are fullers earth, pyrophyllite, talc, bentonite, Kieselguhr or diatomaceous earth. Specified liquid carriers are water, kerosene, fuel and lubricating oils and soy bean oil, linseed, castor, sperm and cod liver oils. Specified wetting agents are fatty alcohol sulphates, aliphatic or aromatic sulphonates and alkyl polyglycol ...

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05-11-1980 дата публикации

Tetrahydrobenzothiazolylimidazolidinones process for their preparation, and their use as herbicides

Номер: GB0002045754A
Автор: Stach, Leonard J
Принадлежит:

Novel compounds of the general formula wherein X is an alkyl, alkoxy, alkylthio, halogen, dialkylamino or cyano group; n is 0 or an integer of from 1 to 4; and R is an alkyl, alkenyl or haloalkyl group are used as herbicides.

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08-10-1969 дата публикации

Improved Photographic Colour Process and Light-Sensitive Elements

Номер: GB0001166655A
Принадлежит:

... 1,166,655. Benzothiazoles. GEVAERTAGFA N.V. 24 Aug., 1967 [19 Sept., 1966], No. 41637/66. Heading C2C. [Also in Division G2] Compounds of the formula wherein D is hexadecyl, R 2 is hydrogen, R 1 is methyl or phenyl and Z is a benz ring which is unsubstituted or is substituted by chloro, fluoro, sulpho, trifluoro - methyl, difluoromethylsulphonyl, sulphamoyl or p - chlorophenylsulphamoyl, are made by heating an appropriately substituted 2 - methylmercapto - 3- methyl (or phenyl) - benzothiazolium quaternary salt with a carboxy-alkoxy-benzene sulphonyl hydrazide in pyridine. A compound of the above formula where D and R 2 are as above, R 1 is methyl and Z represents the 4: 6-dichlorobenz radical is made by heating 3-methyl-4: 6- dichloro - benzothiazolone - 2 - hydrazone with 2 - hexadecyloxy - 5 - carboxy - benzene sulphonyl chloride in the presence of zinc oxide and N-methyl-pyrrolidone; and a compound of the above formula where D is hexadecyl, R 2 is ethyl, R 1 is methyl and Z is the benz ...

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21-07-1976 дата публикации

AGENT FOR THE SELECTIVE COMBATING OF WEEDS IN CEREALS

Номер: GB0001443138A
Автор:
Принадлежит:

... 1443138 Synergistic herbicide composition BAYER AG 31 Jan 1975 [1 Feb 1974] 4296/75 Heading A5E A herbicidal composition containing as active ingredients (1) 3-(benzthiazo]-2-yl)-1, 3- dimethyl-urea of the formula: and (2) 3-(5-n-butylsulphonyl-1, 3, 4-thiadiazol- 2-yl)-1, 3-dimethyl-urea of the formula: alone or in admixture with a solid or liquid or liquefied gaseous diluent or carrier. The compositions find application in combating weeds in cereals.

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25-10-2023 дата публикации

Benzothiazole and benzimidazole derivatives, pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising

Номер: GB0002618017A
Принадлежит:

The present invention relates to a benzothiazole or benzimidazole derivative, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same as an active ingredient for prevention or treatment of SIRTUIN 7 protein-related diseases. With excellent inhibitory activity against SIRTUIN 7 protein, the derivative can be used for preventing or treating SIRTUIN 7 protein-related diseases.

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30-06-2008 дата публикации

Composition and sythesis of new reagents for inhibition of HIV replication

Номер: AP0200804459A0
Автор: RANA TARIG N
Принадлежит:

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30-09-2003 дата публикации

Broadspectrum 2-(substitutted-amino)-benzothiazolesulphonamide HIV protease inhibitors.

Номер: AP0200302856D0
Автор:
Принадлежит:

Подробнее
31-05-2015 дата публикации

Anthelminitic compounds and compositions and method of using thereof

Номер: AP0201508449D0
Принадлежит:

Подробнее
31-12-2001 дата публикации

Substituted phenoxyacetic acids

Номер: AP0200102377D0
Автор:
Принадлежит:

Подробнее
15-05-1995 дата публикации

Inhibition of the replication of HIV and related viruses using thiourea derivative compounds or salts thereof.

Номер: AP0000000384A
Принадлежит:

Method of aids, inhibition of the replication of hiv by contacting hiv with a compound of the formula-(see file) ...

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10-12-2005 дата публикации

Broadspectrum 2- (substituted-amino) -benzothiazole sulfonamide HIV protease inhibitors

Номер: AP0000001504A
Принадлежит:

The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6 alkyl, C2-6alkenyl, C3-7cycloaJkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11a.R11b) NC (R10Ar10b) CR9-; t is 0, 1 or 2; R2 is H or Cl.6alkyl; L is -C(=O)-, -O-C(=O>, -NR8-C(=O)-, -O-C1.6alkanediyl-C(=O)-, -NRg-Cr6?alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2., -NR8-S(=O)2; R3 is C1-6alkyl, aryl, C3.7cycloalkyl, C3.7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6salkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O), -C(=S), -S(=O)2., C1.6alkanediyl-C(=O), C1-6alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2.; R5 is H, OH, C1-6alkyl, HetlCl.6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het10, Het2 ...

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30-06-2003 дата публикации

Pesticidal 1- Aryl -3- Iminopyrazoles.

Номер: AP0000001158A
Принадлежит:

... 1-aryl-3-iminopyrazoles of formula (i)wherein r31, r32, r33, r4, r5, r12, r13, r14, r15 and z are as defined in the specification, are useful as pesticides or as intermediates to other pesticides. Compositions comprising the compounds of formula (i)and methods for their use, particularly in agriculture or for animal protection, as pesticides, especially for controlling arthropods, are described.

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31-07-1992 дата публикации

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Номер: AP0009200412A0
Автор:
Принадлежит:

Подробнее
30-04-1995 дата публикации

Inhihition of the replication of hiv and related viruses using thiourea derivative compounds or salts thereof

Номер: AP0009500723A0
Автор:
Принадлежит:

Подробнее
30-09-1999 дата публикации

Pesticidal 1-ary -3-imnnopyrazoles

Номер: AP0009901645A0
Автор:
Принадлежит:

Подробнее
31-12-2001 дата публикации

Substituted phenoxyacetic acids.

Номер: AP2001002377A0
Принадлежит:

Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.

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30-06-2008 дата публикации

Composition and sythesis of new reagents for inhibition of HIV replication

Номер: AP2008004459A0
Автор: RANA TARIG N
Принадлежит:

Подробнее
30-06-2005 дата публикации

Process for preparing 2,6-diamino - 4,5,6,7-tetrahydro-benzothiazole

Номер: AP2005003306A0
Принадлежит:

Подробнее
30-06-2010 дата публикации

Amide compounds as boosters of antivirals

Номер: AP2010005285A0
Принадлежит:

Подробнее
30-09-2003 дата публикации

Broadspectrum 2-(substitutted-amino)-benzothiazolesulphonamide HIV protease inhibitors.

Номер: AP2003002856A0
Автор:
Принадлежит:

Подробнее
30-06-2005 дата публикации

Thiazole compounds for the treatment of neurodegenerative disorders

Номер: AP2005003274A0
Принадлежит:

Подробнее
31-12-2004 дата публикации

Substituted benzazoles and use thereof as raf kinase inhibitors.

Номер: AP2004003161A0
Автор:
Принадлежит:

Подробнее
30-06-2004 дата публикации

N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.

Номер: AP2004003049A0
Принадлежит:

Disclosed are compounds of the formula (0, wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasec-retase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

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30-11-2013 дата публикации

Benzothiazole compounds and their pharmaceutical use

Номер: AP2013007249A0
Принадлежит:

Подробнее
31-05-2015 дата публикации

Anthelminitic compounds and compositions and method of using thereof

Номер: AP2015008449A0
Принадлежит:

Подробнее
30-06-2015 дата публикации

Antibacterial compounds

Номер: AP2015008503A0
Принадлежит:

Подробнее
31-12-2015 дата публикации

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Номер: AP2015008931A0
Принадлежит:

Подробнее
31-12-2012 дата публикации

New compounds

Номер: AP2012006641A0
Принадлежит:

Подробнее
30-09-2003 дата публикации

Broadspectrum 2-(substitutted-amino)-benzothiazolesulphonamide HIV protease inhibitors.

Номер: AP0200302856A0
Автор:
Принадлежит:

Подробнее
31-12-2001 дата публикации

Substituted phenoxyacetic acids

Номер: AP0200102377A0
Автор:
Принадлежит:

Подробнее
31-10-2008 дата публикации

Substituted benzazoles and use thereof as Raf kinase inhibitors

Номер: AP0000001913A
Принадлежит:

New substituted benz-azole compounds of formula (I), compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

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04-02-1970 дата публикации

New fungicidal products derived from salicylic aldehyde.

Номер: OA0000001881A
Автор:
Принадлежит:

Подробнее
31-07-1981 дата публикации

Derived from benzothiazole, their method of preparation and their applications into therapeutic.

Номер: OA0000006504A
Автор:
Принадлежит:

Подробнее
30-11-1990 дата публикации

Use of derived from the malonic acid to improve the output of the cultures.

Номер: OA0000008946A
Автор:
Принадлежит:

Подробнее
13-10-2006 дата публикации

Thiazole compounds for the treatment of neurodegenerative disorders.

Номер: OA0000012937A
Принадлежит:

Подробнее
15-12-1970 дата публикации

New agents biocides.

Номер: OA0000002904A
Автор:
Принадлежит:

Подробнее
18-04-2006 дата публикации

Substituted phenoxyacetic acids.

Номер: OA0000011972A
Автор: ZANDT VAN MICHAEL C
Принадлежит:

Подробнее
15-08-1994 дата публикации

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Номер: OA0000009914A
Принадлежит:

Подробнее
30-06-2005 дата публикации

Thiazole compounds for the treatment of neurodegenerative disorders

Номер: AP0200503274A0
Принадлежит:

Подробнее
30-06-2015 дата публикации

Antibacterial compounds

Номер: AP0201508503A0
Принадлежит:

Подробнее
05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

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05-01-2012 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20120004216A1
Принадлежит: Vertex Pharmaceuticals Inc

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

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28-03-2013 дата публикации

Synthesis of Chirally Purified Substituted Benzothiazole Diamines

Номер: US20130079526A1
Принадлежит: Knopp Neurosciences Inc.

Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro--(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein. 2. The process of claim 1 , wherein the alkyl sulfonate is a propyl sulfonate selected from n-propyl tosylate claim 1 , n-propyl methoxysulfonate and combinations thereof.3. The process of claim 1 , wherein the chirally purified substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is at least greater than about 97% chirally pure.4. The process of claim 1 , wherein the chirally purified substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is at least greater than about 99% chirally pure.5. The process of claim 1 , wherein the chirally purified substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is at least about 99.9% chirally pure.6. The process of claim 1 , wherein the chemical purity of the substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is greater than about 98%.7. The process of claim 1 , wherein the chemical purity of the substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is greater than about 99.9%.8. The process of claim 1 , wherein the chemical purity of the substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is greater than about 99.99%.9. The process of claim 1 , wherein the chemical purity of the substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is 100%.10. The process of claim 1 , wherein the substituted 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-benzothiazole diamine is substantially free of achiral salts.11. The process of claim 1 , wherein the substituted 4 claim 1 ,5 ...

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16-05-2013 дата публикации

Compounds having trpv1 antagonistic activity and uses thereof

Номер: US20130123239A1
Автор: Noriyuki Kurose
Принадлежит: Shionogi and Co Ltd

The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.

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18-07-2013 дата публикации

METHOD FOR PROMOTING DIFFERENTIATION OF PLURIPOTENT STEM CELLS INTO CARDIAC MUSCLE CELLS

Номер: US20130183753A1
Принадлежит: KYOTO UNIVERSITY

The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells. 2. The method according to claim 1 , wherein{'sub': 6', '9', '12', '11', '12', '13', '6', '9', '2', '2', '2, 'Rto Rare each independently a hydrogen atom; a halogen atom; a hydroxyl group; a linear or branched alkoxy group having 1 to 5 carbon atoms; a linear or branched alkyl group having 1 to 5 carbon atoms which is unsubstituted or substituted with a halogen atom; or a group —NRR, wherein Rand Rare each independently a hydrogen atom, an oxygen atom, or a linear or branched alkyl group having 1 to 5 carbon atoms which is unsubstituted or substituted with a halogen atom; wherein two adjacent groups among Rto Rmay join together to form —O—CH—O— or —O—(CH)—O—.'}3. The method according to claim 2 , wherein{'sub': 1', '5', '1', '5', '2', '2', '2, 'Rto Rare each independently a hydrogen atom; a halogen atom; a hydroxyl group; a linear or branched alkoxy group having 1 to 5 carbon atoms; or a linear or branched alkyl group having 1 to 5 carbon atoms which is unsubstituted or substituted with a halogen atom; wherein two adjacent groups among Rto Rmay join together to form —O—CH—O— or —O—(CH)—O—, and'}{'sub': 15', '15, 'X is an oxygen atom; a sulfur atom; or a group —NR, wherein Ris a hydrogen atom, a linear or branched alkyl group having 1 to 5 carbon atoms, or a linear or branched acyl group having 1 to 5 carbon atoms.'}4. The method according to claim 3 , wherein{'sub': 2', '3', '2', '3', '2', '2', '2, 'Rand Rare a linear or branched alkoxy group having 1 to 5 carbon atoms, or Rand Rjoin together to form —O—CH—O— or —O—(CH)—O—,'}{'sub': 6', '9, 'Rand Rare each independently, a hydrogen atom; a halogen atom; a hydroxyl group; a linear or branched alkoxy group having 1 to 5 carbon atoms; or a linear or ...

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08-08-2013 дата публикации

BENZOTHIAZOLES AS GHRELIN RECEPTOR MODULATORS

Номер: US20130203730A1
Принадлежит: AstraZeneca AB

A compound of formula I 113-. (canceled)15. The compound as claimed in in which Ris chloro.16. The compound as claimed in selected from one or more of the following:2-Chloro-5-(3-(dimethylamino)pyrrolidin-1-yl)-N-(6-(methylsulfonyl)benzothiazol-2-ylcarbamoyl)benzamide;2-Chloro-N-(6-(3-(4-methylpiperazin-1-yl)propylsulfonyl)benzothiazol-2-ylcarbamoyl)-5-(pyrrolidin-1-yl)benzamide;2-Chloro-N-(6-(3-(4-methylpiperazin-1-yl)propylsulfonyl)benzothiazol-2-ylcarbamoyl)-5-morpholinobenzamide;2-Chloro-5-(5-methyl-1H-pyrazol-1-yl)-N-(6-(3-(4-methylpiperazin-1-yl)propylsulfonyl)benzothiazol-2-ylcarbamoyl)benzamide;2-Chloro-5-ethoxy-N-(6-(3-(4-methylpiperazin-1-yl)propylsulfonyl)benzothiazol-2-ylcarbamoyl)benzamide;2-Chloro-N-(6-(1-methylpiperidin-4-ylsulfonyl)benzothiazol-2-ylcarbamoyl)-5-morpholinobenzamide;2-Chloro-5-ethynyl-N-[[6-[3-(4-methylpiperazin-1-yl)propylsulfonyl]benzothiazol-2-yl]carbamoyl]benzamide;2-chloro-5-ethyl-N-(6-(3-(4-methylpiperazin-1-yl)propylsulfonyl)benzo[d]thiazol-2-ylcarbamoyl)benzamide;2-chloro-N-(6-(2-methyl-1-(pyrrolidin-1-yl)propan-2-ylsulfonyl)benzo[d]thiazol-2-ylcarbamoyl)-5-morpholinobenzamide;2-chloro-4-fluoro-N-(6-(1-methylpiperidin-4-ylsulfonyl)benzo[d]thiazol-2-ylcarbamoyl)-5-(1H-pyrazol-1-yl)benzamide; and2-chloro-4-methoxy-N-(6-(1-methylpiperidin-4-ylsulfonyl)benzo[d]thiazol-2-ylcarbamoyl)-5-morpholinobenzamide;and pharmaceutically acceptable salts thereof.17. A method for the treatment of obesity or being overweight claim 14 , for the prevention of weight gain claim 14 , for the modulation of appetite and/or satiety claim 14 , eating disorders claim 14 , for the treatment of diabetes claim 14 , for the treatment of metabolic syndrome claim 14 , for the treatment of the Prader-Willi syndrome claim 14 , for the treatment of cachexia resulting from cancer or congestive heart failure claim 14 , for the treatment of wasting due to ageing or AIDS or chronic liver failure or chronic obstructive pulmonary disease claim 14 , comprising ...

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08-08-2013 дата публикации

TREATMENT OF CANCER/INHIBITION OF METASTASIS

Номер: US20130203764A1
Принадлежит:

Substances and methods are disclosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole. 1. Ranolazine for reducing or preventing metastatic behaviour in VGSC expressing cancer.2. Ranolazine according to claim 1 , wherein the cancer is breast cancer.3. Ranolazine according to claim 1 , wherein the cancer is prostate cancer.4. Riluzole for reducing or preventing metastatic behaviour in VGSC expressing cancer without directly killing the cancer cells.5. Riluzole according to claim 4 , wherein the cancer is breast cancer.6. Riluzole according to claim 4 , wherein the cancer is prostate cancer.7. A substance for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part.8. A substance according to claim 7 , having said effect in breast cancer.9. A substance according to claim 7 , having said effect in prostate cancer.10. A substance according to claim 7 , having said effect without killing the cells.11. A substance according to claim 7 , having said effect without substantially affecting proliferation.12. Ranolazine according to claim 1 , in a dosage level corresponding to the range 1 μmol to 10 μmol.13. Riluzole according to claim 4 , in a dosage level corresponding to the range 1 μmol of 10 μmol.14. A method of reducing or preventing metastatic behaviour in VGSC expressing cancer comprising administering ranolazine.15. A method according to claim 14 , wherein the cancer is breast cancer.16. A method according to claim 14 , wherein the cancer is prostate cancer.17. A method of reducing ...

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24-10-2013 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20130281434A1
Принадлежит: Gilead Sciences, Inc.

Compounds of formula I′: 2. The compound of wherein A is phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.3. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.4. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.5. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.6. The compound of wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , pyrimidinyl claim 1 , indazolyl claim 1 , pyrazolopyridine or benzimidazolyl claim 1 , wherein any phenyl claim ...

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28-11-2013 дата публикации

Amidobenzothiazoles And Process For The Preparation Thereof

Номер: US20130317231A1
Принадлежит: Individual

The present invention provides a compound of general formulae A useful as potential anti-cancer agents against human cancer cell lines and a process for the preparation thereof. Where in R, R 1 , R 2 ═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G= Where in R, R 1 , R 2 ═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G=

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05-12-2013 дата публикации

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

Номер: US20130324537A1
Принадлежит:

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': [{'sub': 1', '6', '2', '6, 'each optionally substituted C-C-alkyl or C-C-alkenyl,'}, {'sub': 2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}], 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': W', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of ...

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13-02-2014 дата публикации

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Номер: US20140045818A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I. 2. The compound wherein:{'sup': 1', '2', '1', '2', '5, 'Gis S, Gis N, the dashed bond connected to Gis a single bond, the dashed bond connected to Gis a double bond, and the wavy bond connected to Ris a single bond; or'}{'sup': 1', '2', '6', '1', '2', '5', '5, 'Gis S, Gis NR, the dashed bond connected to Gis a single bond, the dashed bond connected to Gis a single bond, the wavy bond connected to Ris a double bond and Ris oxygen.'}3. The compound of or wherein Ris H or halo.43. The compound of any one of - wherein R is H.65. The compound of any one of - wherein Ris (C-C)alkyl claims 1 , (C-C)alkenyl or —O(C-C)alkyl claims 1 , wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claims 1 , halo claims 1 , oxo and —CN.75. The compound of any one of - wherein Ris —OC(CH).87. The compound of any one of - wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —(C-C)alkyl-(C-C)cycloalkyl, —OH, —O(C-C)allyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo; and'}{'sup': 7', '1, 'b) aryl, heteroaryl, spiro-heterocycle, fused- ...

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20-03-2014 дата публикации

Modulators of ATP-binding cassette transporters

Номер: US20140080825A1
Принадлежит: Vertex Pharmaceuticals Inc

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

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20-03-2014 дата публикации

METHODS FOR INHIBITING FASCIN

Номер: US20140080843A1
Принадлежит:

Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof. 6. The method of claim 1 , wherein Ris phenyl optionally substituted with one claim 1 , two claim 1 , or three groups chosen from halo and lower alkyl.7. The method of claim 1 , wherein Ris triazole.8. The method of claim 2 , wherein m is 0.9. The method of claim 1 , wherein Lis —N(R)S(O)—.10. The method of claim 1 , wherein Lis —S—.11. The method of claim 1 , wherein Xis OH and Xis O.12. The method of claim 1 , wherein Ris independently selected from the group consisting of OH claim 1 , halo claim 1 , lower alkyl claim 1 , and —OR.13. The method of claim 1 , wherein the compound is selected from5-(3,4-dichlorobenzyl)-1-(S,S,-dioxo-tetrahydrothiophen-3-yl)-1H-pyrazolo-[3,4-d]pyrimidin-4(5H)-one;N-(1-(4-(trifluoromethyl)benzyl)-1H-indazol-3-yl)furan-2-carboxamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-2,5-dimethylbenzenesulfonamide;N-(3(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-ethoxybenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-methoxybenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-ethylbenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-trimethylbenzenesulfonamide;(Z)—N-(3-(1H-1,2,4-triazol-3-ylthio)-4-oxonaphthalen-1(4H)-ylidene)benzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-4-bromobenzenesulfonamide;N-(3-(1H-1,2,4-triazol-3-ylthio)-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide;5-(3-chlorobenzyl)-1-(2-hydroxyethyl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one;2-(4-oxo-1-(S,S,-dioxo-tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-d]-pyrimidin-5(4H)-yl)-N-(3-( ...

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10-04-2014 дата публикации

SYNTHESIS OF CHIRALLY PURIFIED SUBSTITUTED BENZOTHIAZOLE DIAMINES

Номер: US20140100372A1
Принадлежит: Knopp Neurosciences, Inc.

Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein. 228-. (canceled)29. Chirally purified 2-amino-4 ,5 ,6 ,7-tetrahydro-6-(propylamino)benzothiazole prepared by a process comprising:heating a solution comprising entantiomerically enriched 2,6 diamino-4,5,6,7-tetrahydro-benzothiazole and a propyl halide or a propyl sulfonate to form a reaction mixture;reacting the reaction mixture; andrecovering the chirally purified 2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole.3052-. (canceled)53. A process for preparing a chirally purified 2-amino-4 ,5 ,6 ,7-tetrahydro-6-(propylamino)benzothiazole comprising:heating a solution comprising 2,6 diamino-4,5,6,7-tetrahydro-benzothiazole in an organic solvent;adding to the heated solution propyl sulfonate or a propyl halide to form a reaction mixture; andreacting the reaction mixture for up to about 12 hours.5479-. (canceled)80. A process for preparing chirally purified 2-amino-4 ,5 ,6 ,7-tetrahydro-6-(propylamino)benzothiazole comprising:heating a solution comprising 2,6 diamino-4,5,6,7-tetrahydro-benzothiazole;adding a propyl halide or a propyl sulfonate to the heated solution slowly over from about 0.5 hours to about 2 hours to form a reaction mixture;reacting the reaction mixture; andrecovering the chirally purified 2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole.81101-. (canceled)102. Chirally purified 2-amino-4 ,5 ,6 ,7-tetrahydro-6-(propylamino)benzothiazole prepared by a process comprising:heating a solution comprising 2,6 diamino-4,5,6,7-tetrahydro-benzothiazole;adding a propyl halide or a propyl sulfonate to the heated solution slowly over from about 0.5 hours to about 2 hours to ...

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06-01-2022 дата публикации

SULFUR (VI) FLUORIDE COMPOUNDS AND METHODS FOR THE PREPARATION THEREOF

Номер: US20220000799A1
Принадлежит: The Scripps Research Institute

This application describes modified amino acids and polypeptides comprising a SOF or CHCHSOF group bound to the side chain of an amono acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptot sites of receptor proteins are also described herein. 1. A modified amino acid comprising an amino acid core group bound to a SOF or CHCHSOF group; wherein the amino acid core group has a side chain comprising a hydroxyl or amino substituent , and the SOF or CHCHSOF group is bound to the side chain in place of a hydrogen of the hydroxyl or amino substituent thereof.2. The modified amino acid of claim 1 , wherein the amino acid core group is tyrosine.3. The modified amino acid of claim 1 , wherein the amino acid core group is 2 claim 1 ,6-dimethyltyrosine.4. The modified amino acid of claim 1 , wherein the amino acid core group is histidine.5. The modified amino acid of claim 1 , wherein the amino acid core group is lysine.6. The modified amino acid of claim 1 , wherein the amino acid core group is arginine.7. A polypeptide comprising a modified amino acid residue bearing a SOF or CHCHSOF group; wherein the a modified amino acid residue comprises an amino acid residue core group having a side chain comprising a hydroxyl or amino substituent claim 1 , and the SOF or CHCHSOF group is bound to the side chain in place of a hydrogen of the hydroxyl or amino substituent thereof.8. The polypeptide of claim 7 , wherein the amino acid residue core group is a tyrosine residue.9. The polypeptide of claim 7 , wherein the amino acid residue core group is a 2 claim 7 ,6-dimethyltyrosine residue.10. The polypeptide of claim 7 , wherein the amino acid residue core group is a histidine residue.11. The polypeptide of claim 7 , wherein the amino acid residue core group is a lysine residue.12. The polypeptide of claim 7 , wherein the amino acid residue core group is an arginine residue. ...

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04-01-2018 дата публикации

ZINC COMPLEXES OF HYDRAZONES AND (THIO)SEMICARBAZONES AND THEIR USE FOR THE TREATMENT OF CANCER

Номер: US20180000772A1
Принадлежит:

The invention provides complexes of Zn2+ of formulae (la) and (IIa) that are useful for treating cancer, as well as compositions and kits comprising such complexes. 3. The complex of or or a solvate thereof , which comprises Znand a compound of formula (Ia).4. The complex of or a solvate thereof claim 1 , which comprises Znand a compound of formula (IIa).5. The complex of any one of - or a solvate thereof claim 1 , wherein the compound and the Znare present in a ratio of about 1:1.6. The complex of any one of - or a solvate thereof claim 1 , wherein the compound and the Znare present in a ratio of about 2:1.7. The complex or solvate of any one of - which is charge neutral.12. The complex of any one of - or a solvate thereof wherein Ris selected from the group consisting of H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , tert-butyl claim 1 , allyl claim 1 , cyclopropyl claim 1 , phenyl claim 1 , benzyl claim 1 , CHCHOCH claim 1 , and CHCH—N(CH).15. A pharmaceutical composition claim 1 , comprising a complex of any one of - or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.16. An injectable pharmaceutical formulation comprising claim 1 , a complex of any one of - or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.17. A method of inhibiting cancer cell growth in vivo or in vitro claim 1 , comprising contacting a cancer cell with a complex of any one of - or a solvate thereof.18. A method of treating cancer in an animal comprising administering a complex of any one of - or a solvate thereof to the animal.19. The method of claim 18 , further comprising administering zinc to the animal.20. The method of any one of - claim 18 , wherein the cancer is caused by mutations affecting zinc binding proteins.21. The method of any one of - claim 18 , wherein the cancer is associated with a zinc binding p53 mutation.22. The method of any one of - claim 18 , wherein the cancer is associated ...

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03-01-2019 дата публикации

Inhibitors of N-Linked Glycosylation and Methods Using Same

Номер: US20190000858A1
Принадлежит:

The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compound of the invention. 45-. (canceled)711-. (canceled)13. The composition of claim 12 , further comprising at least one additional therapeutic compound that treats or prevents cancer.15. (canceled)16. The method of claim 14 , wherein the cell is a receptor tyrosine kinase-dependent cancer cell.17. The method of claim 16 , wherein the cancer is selected from the group consisting of non-small cell lung cancer claim 16 , small cell lung cancer claim 16 , head and neck squamous cell carcinoma claim 16 , breast cancer claim 16 , gastric cancer claim 16 , cervical cancer claim 16 , colon cancer claim 16 , and glioma.18. (canceled)19. The method of claim 14 , wherein the cell is in vivo in a mammal and wherein the agent is administered to the mammal.20. (canceled)22. (canceled)23. The method of claim 21 , wherein the cancer is receptor tyrosine kinase-dependent.24. The method of claim 23 , wherein the agent blocks or inhibits cell surface expression of the receptor tyrosine kinase in a cell from the cancer.25. (canceled)26. The method of claim 21 , further comprising administering to the subject at least one additional therapeutic compound that treats or prevents cancer.27. The method of claim 26 , wherein the agent and the at least one additional therapeutic compound are co-administered to the subject.28. The method of claim 27 , wherein the agent and the at least one additional therapeutic compound are coformulated.29. (canceled)30. The method of claim 21 , wherein the cancer is selected from the group consisting of squamous cell cancer claim 21 , small cell lung cancer claim 21 , non-small cell lung cancer claim 21 , vulval cancer claim 21 , thyroid cancer claim 21 , adenocarcinoma of the lung and squamous carcinoma of ...

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05-01-2017 дата публикации

4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase

Номер: US20170001955A1
Принадлежит:

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder. 2. The compound of claim 1 , wherein Ris selected from the group consisting of methoxy and Cl when Ris H;{'sub': 2', '1, 'Ris selected from the group consisting of Br, and Cl when Ris H; and'}{'sub': '3', 'Ris selected from the group consisting of thiazole, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 4-methyl-2-benzothiazole, thiophene, 4-methyl-2-thiazole, 5-methyl-2-thiazole, 4, 5-methyl-2-thiazole, phenyl, 1-naphthalene, 2-naphthalene, 1, 4-bi-phenyl, 3-piperazine-phenyl, 4-piperidine-phenyl, 4-piperazine-3-pyridine, 6-methyl-3-pyridine, 3-quinoline, 8-isoquinoline, 2-pyridine, 3-pyridine, 3-tertbutyl-phenyl, 6-methoxy-2-benzothiazole, 6-fluro-2-benzothiazole, 4-phenyl-2-thiazole, 3-morpholine-phenyl, 4N-boc-piperidine-3-phenyl, 3-piperidine-phenyl, 3-isopropyl-phenyl, and 4-bi-phenyl;'}or a pharmaceutically acceptable salt thereof, enantiomers ...

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04-01-2018 дата публикации

POLYMERIZABLE COMPOUND AND OPTICALLY ANISOTROPIC BODY

Номер: US20180002276A1
Принадлежит: DIC CORPORATION

In light of requests to reduce or reverse the wavelength dispersion of the birefringence of a phase-retardation film in order to increase the viewing angle of a liquid crystal display, the present invention provides a polymerizable compound that reduces, for example, the likelihood of crystals precipitating in a polymerizable composition including the polymerizable compound and enables the polymerizable composition to have high preservation stability and a polymerizable composition including the polymerizable compound which reduces the likelihood of inconsistencies being formed in a film-like polymer produced by polymerizing the polymerizable composition. Another object of the present invention is to provide a polymer produced by polymerizing the polymerizable composition and an optically anisotropic body including the polymer. 3. The compound according to claim 1 , wherein Sp claim 1 , Sp claim 1 , Sp claim 1 , and Spthat are present in General Formula (I) each independently represent an alkylene group having 1 to 20 carbon atoms in which one —CH— group or two or more —CH— groups that are not adjacent to one another may be each independently replaced with —O— claim 1 , —COO— claim 1 , —OCO— claim 1 , —OCO—O— claim 1 , —CO—NH— claim 1 , —NH—CO— claim 1 , —CH═CH— claim 1 , or —C≡C—.4. The compound according to claim 1 , wherein claim 1 , in General Formula (I) claim 1 , the total number of π electrons included in Wand Wis 4 to 24.6. A composition comprising the compound according to .7. A liquid crystal composition comprising the compound according to .8. A polymer produced by polymerizing the composition according to .9. An optically anisotropic body comprising the polymer according to .10. A resin claim 1 , a resin additive claim 1 , an oil claim 1 , a filter claim 1 , a bonding agent claim 1 , an adhesive claim 1 , a fat claim 1 , an ink claim 1 , a drug claim 1 , a cosmetic claim 1 , a detergent claim 1 , a building material claim 1 , a packaging material claim 1 ...

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07-01-2016 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC BODY

Номер: US20160002374A1
Принадлежит: ZEON CORPORATION

According to the invention, a polymerizable compound, a polymerizable composition, and a polymer that have a low melting point at a practical level, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that exhibits excellent transparency, and achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article can be provided. In formula (I), Yto Yare, —O—, —O—C(═O)—, —C(═O)—O—, etc., Gand Gare a divalent linear aliphatic group of 1-20 carbon atoms, Zand Zare an alkenyl group of 2-10 carbon atoms that is substituted with a halogen atom, or unsubstituted, Ais an organic group of 2-30 carbon atoms that includes at least one aromatic ring, Ais a hydrogen atom, an alkyl group of 1-20 carbon atoms, etc., Ais a trivalent aromatic group, Aand Aare a substituted or unsubstituted divalent alicyclic hydrocarbon group of 3-30 carbon atoms, Aand Aare a divalent aromatic group of 6-30 carbon atoms, and Qis a hydrogen atom, or an alkyl group of 1-6 carbon atoms. 2. The polymerizable compound according to claim 1 , wherein a total number of it electrons included in Aand Ais 4 to 24.3. The polymerizable compound according to claim 1 , wherein Ais a substituted or unsubstituted trivalent benzene ring group claim 1 , or a substituted or unsubstituted trivalent naphthalene ring group.4. The polymerizable compound according to claim 1 , wherein Yto Yare independently a chemical single bond claim 1 , —O— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , or —O—C(═O)—O—.5. The polymerizable compound according to claim 1 , wherein Zand Zare independently CH═CH— claim 1 , CH═C(CH)— claim 1 , or CH═C(Cl)—.6. The polymerizable compound according to claim 1 , wherein Gand Gare independently a substituted or unsubstituted divalent aliphatic group having 1 to 12 carbon atoms that optionally includes —O— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , or —C(═O)— claim 1 , provided ...

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03-01-2019 дата публикации

ANTI-VIRAL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Номер: US20190002477A1
Принадлежит: Kineta, Inc.

Disclosed herein are compounds, pharmaceutical compositions, and related methods for the treatment of viral infection, including RNA viral infection in subjects. The compounds, pharmaceutical compositions, and methods can modulate the innate immune antiviral response in vertebrate cells, including activating the RIG-I pathway. 129.-. (canceled)31. The compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , wherein each Ris independently H or SONRRwherein Rand Rform an optionally substituted carbocyclic claim 30 , heterocarbocyclic claim 30 , aryl or heteroaryl ring.32. The compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , wherein each Ris independently H or SONRRwherein Rand Rform an optionally substituted heterocyclic ring selected from pyrrolidine claim 30 , piperidine claim 30 , morpholine claim 30 , and piperazine.33. The a pharmaceutical composition comprising the compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and a pharmaceutically acceptable carrier.34. A method of modulating the innate immune response in a eukaryotic cell claim 30 , comprising administering to the cell a compound of claim 30 , or a pharmaceutically acceptable salt thereof.35. The method of wherein the cell is in vivo.36. The method of wherein the cell is in vitro. This application claims the benefit of U.S. Provisional Patent Application No. 61/991,418 filed on May 9, 2014, and U.S. Provisional Application No. 62/177,900, filed on Mar. 25, 2015, each of which is incorporated by reference herein in their entirety.Compounds, pharmaceutical compositions, and methods disclosed herein are useful for treating viral infection, including RNA viral infection, in subjects.As a group, RNA viruses represent an enormous public health problem in the U.S. and worldwide. Well-known RNA viruses include influenza virus (including the avian and swine isolates; also referred to herein as flu), Hepatitis C virus (HCV), Dengue ...

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07-01-2021 дата публикации

Novel Antimycobacterial Heterocyclic Amides

Номер: US20210002239A1
Принадлежит:

The present invention provides novel heterocylic amide compounds having useful antimycobacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided. 4. A compound selected from the group consisting of: N-(1-benzothiophen-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-(5 ,7-dichloro-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-(5-bromo-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-(5 ,7-difluoro-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , 5-methyl-N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]bicyclo[3.3.1]nonane-1-carboxamide , 1-methyl-N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]cycloheptane-1-carboxamide , N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]adamantane-2-carboxamide , N-(5 ,7-dimethyl-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , 5-methyl-N-(4 ,5 ,6-trifluoro-1 ,3-benzothiazol-2-yl)bicyclo[3.3.1]nonane-1-carboxamide , N-(4 ,6-difluoro-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-(6-bromo-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-(6-chloro-1 ,3-benzothiazol-2-yl)-5-methylbicyclo[3.3.1]nonane-1-carboxamide , N-[6-(difluoromethoxy)-1 ,3-benzothiazol-2-yl]-5-methylbicyclo[3.3.1]nonane-1-carboxamide , (3R ,5S ,7s)-N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]adamantane-1-carboxamide , N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]bicyclo[3.3.1]nonane-3-carboxamide , N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]-decahydronaphthalene-2-carboxamide , (1R ,3S)-1 ,2 ,2 ,3-tetramethyl-N-[6-(trifluoromethoxy)-1 ,3-benzothiazol-2-yl]cyclopentane-1-carboxamide , N-(5 ,7-dichloro-1 ,3-benzothiazol-2-yl)-1-methylcycloheptane-1-carboxamide , N-(1-benzothiophen-2-yl)adamantane-2-carboxamide , N-(5 ,7-dichloro-1 ,3-benzothiazol-2-yl)adamantane-2-carboxamide , 5-methyl-N-[6-(trifluoromethyl)-1 ,3-benzothiazol-2-yl]bicyclo[3.3.1]nonane-1- ...

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12-01-2017 дата публикации

METHOD FOR MANUFACTURING 1,1-DISUBSTITUTED HYDRAZINE COMPOUND

Номер: US20170008862A1
Принадлежит: ZEON CORPORATION

This method for a manufacturing a 1,1-disubstituted hydrazine compound represented by a formula (II) involves reacting a hydrazino compound represented by a formula (I) with a compound represented by a formula: R-Hal in an aprotic polar solvent in the presence of a base selected from an alkali metal hydroxide and alkaline-earth metal hydroxide in an amount of 1.0 to 3.0 equivalents based on the hydrazino compound. In the formulae, X represents an oxygen atom, a sulfur atom, —CH— or the like, and each of Rrepresents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, a cyano group, a nitro group, a fluoroalkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms or the like. An arbitrary C—Rthat forms the ring is optionally substituted with a nitrogen atom. Hal represents a chlorine atom, a bromine atom, or an iodine atom, and R represents a substituted or unsubstituted organic group having 1 to 12 carbon atoms. 2. The method according to claim 1 , further comprising adding a protic solvent to a reaction mixture obtained by the reaction to effect direct crystallization.3. The method according to claim 2 , wherein the protic solvent is water.4. The method according to claim 1 , wherein the compound represented by the formula (I) is the compound represented by the formula (I) in which each of Ris a hydrogen atom.5. The method according to claim 1 , wherein the compound represented by the formula (I) is the compound represented by the formula (I) in which X is a sulfur atom.6. The method according to claim 1 , wherein the compound represented by the formula (III): R-Hal is the compound represented by the formula (III) in which R is a substituted or unsubstituted alkyl group having 1 to 12 carbon atoms.7. The method according to claim 1 , wherein the base is an alkali metal hydroxide.8. The method according to claim 1 , wherein the base is sodium hydroxide or potassium hydroxide.9. The method according to claim 1 , wherein ...

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12-01-2017 дата публикации

NOVEL CYP-EICOSANOID DERIVATIVES

Номер: US20170008918A1
Принадлежит:

The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for C the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias. 2. The compound according to , wherein E is a group represented by the general formula (III); and P , and I are defined as in .4. The compound according to or , wherein P represents a group —(CH)X , —(CH)X , —(CH)X , or —(CH)X; wherein X is defined as in .7. The compound according to , wherein E is a group represented by the general formula (IV); one of Rand Rrepresents a hydrogen atom and the other represents a fluorine atom , hydroxy , —NH , C-Calkyl , C-Calkoxy , —C(═O)-aryl , —C(═O)C-Calkyl , or —SO(C-Calkyl); or —SOaryl; wherein any of the foregoing C-Calkyl , C-Calkoxy , or aryl are optionally substituted with one , two or three substituents independently selected from the group consisting of —NH , —NH(C-C)alkyl , —N(C-C)dialkyl , C-Calkylcarbonyloxy- , C-Calkoxycarbonyloxy- , C-Calkylcarbonylthio- , C-Calkylaminocarbonyl- , di(C-C)alkylaminocarbonyl- , fluorine or chlorine atom , and hydroxy; or Rand Rare taken together to form a 5-membered or 6-membered ring , which ring is optionally substituted with one , two or three substituents independently selected from the group consisting of —NH , —NH(C-C)alkyl , —N(C-C)dialkyl , C-Calkylcarbonyloxy- , C-Calkoxycarbonyloxy- , C-Calkylcarbonylthio- , C-Calkylaminocarbonyl- , di(C-C)alkylaminocarbonyl- , fluorine or chlorine atom , and hydroxy; and P and I are defined as in .8. The compound according to , wherein E is a group represented by the general ...

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08-01-2015 дата публикации

Phenylimide-containing benzothiazole derivative of its salt and pharmaceutical composition comprising the same

Номер: US20150011528A1
Принадлежит: Yuhan Corp

Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.

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19-01-2017 дата публикации

METHOD FOR PRODUCING POLYMERIZABLE COMPOUND

Номер: US20170015639A1
Принадлежит: ZEON CORPORATION

Provided is a method for producing a polymerizable compound represented by a formula (I) comprising: 2. The method according to claim 1 , wherein R included in the compound represented by the formula (IV) is a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkenyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkynyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted aromatic group having 6 to 18 carbon atoms claim 1 , or a substituted or unsubstituted heteroaromatic group having 4 to 18 carbon atoms.3. The method according to claim 1 , wherein each of Rincluded in the compound represented by the formula (IV) is a hydrogen atom.4. The method according to claim 1 , wherein an acid component included in the acidic aqueous solution is an inorganic acid or an organic acid having 1 to 20 carbon atoms.5. The method according to claim 1 , wherein an acid component included in the acidic aqueous solution is at least one acid selected from a group consisting of hydrochloric acid claim 1 , sulfuric acid claim 1 , phosphoric acid claim 1 , boric acid claim 1 , a sulfonic acid claim 1 , a sulfinic acid claim 1 , formic acid claim 1 , acetic acid claim 1 , and oxalic acid. The present invention relates to a method by which a polymerizable compound that can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, can be produced in high purity and high yield.A quarter-wave plate that converts linearly polarized light into circularly polarized light, a half-wave plate that changes (converts) the plane of vibration of linearly polarized light by 90°, and the like are known as a retardation film that is used for a flat panel display (FPD) and the like. These retardation films can achieve accurate conversion of specific monochromatic light so that ¼λ or ½λ retardation occurs. In recent years, various wideband retardation ...

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15-01-2015 дата публикации

METHOD FOR INDUCING CARDIAC DIFFERENTIATION OF PLURIPOTENT STEM CELL

Номер: US20150017718A1
Принадлежит:

The present invention relates to a method for inducing cardiac differentiation of a pluripotent stem cell, which comprises the steps of 1. A method for inducing cardiac differentiation of a pluripotent stem cell , which comprises the steps of(1) culturing a pluripotent stem cell in a medium containing one or more WNT signaling activators, and(2) culturing a cell produced in the step (1) in a medium containing one or more WNT signaling inhibitor.5. The method of claim 1 , wherein the one or more WNT signaling inhibitors comprise a WNT signaling inhibitor selected from XAV939 and IWP-2.6. The method of claim 1 , wherein the one or more WNT signaling activators comprise a GSK3β inhibitor.7. The method of claim 6 , wherein the one or more WNT signaling activators comprise a WNT signaling activator selected from BIO and CHIR99021.8. The method of claim 1 , wherein the medium in the step (1) and the medium in the step (2) do not comprise serum.9. The method of claim 1 , wherein the medium in the step (1) and the medium in the step (2) do not comprise a cytokine.10. The method of claim 1 , wherein the medium in the step (1) and the medium in the step (2) comprise albumin.11. The method of claim 1 , wherein the medium in the step (1) and the medium in the step (2) do not comprise a protein other than albumin.12. The method of claim 1 , which is conducted in the absence of a xenogeneic component.13. The method of claim 1 , wherein the pluripotent stem cell is a monkey or human pluripotent stem cell.14. The method of claim 1 , which is used to prepare a cardiomyocyte.15. A kit for promoting cardiac differentiation comprising one or more WNT signaling activators and/or one or more WNT signaling inhibitors claim 1 , wherein the kit is used for the method of . The present invention relates to a method for inducing cardiac differentiation of a pluripotent stem cell.Human pluripotent stem cells (hPSCs), including embryonic stem cells (hESCs) and induced pluripotent stem cells ( ...

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19-01-2017 дата публикации

Novel azo compound, use thereof and method for preparing same

Номер: US20170016050A1
Принадлежит: Bioneer Corp

The present invention provides a novel azo compound having a quenching ability for the material that exhibits a luminescent phenomenon at an excited energy level, a quencher comprising the novel azo compound, a use of the quencher and a method for preparing the azo compound. The quencher according to the present invention may exhibit excellent characteristics in a wavelength absorption region.

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16-01-2020 дата публикации

Bicyclic heteroaryl derivatives and preparation and uses thereof

Номер: US20200017456A1
Принадлежит: XW Laboratories Inc Cayman Islands

The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.

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16-01-2020 дата публикации

TREATMENT OF CANCER/INHIBITION OF METASTASIS

Номер: US20200017457A1
Автор: Djamgoz Mustafa
Принадлежит: Celex Oncology Ltd.

Substances and methods are dislosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole. 1. A method for inhibiting metastatic and invasive growth of malignant cells in a cancer patient in need thereof , comprisingadministering an effective and pharmaceutically acceptable amount to the patient of an inhibitor of a voltage gated sodium channel (VGSC), is not lethal to the malignant cells,', 'blocks or reduces the persistent part of the VGSC current in the malignant cells, and', 'does not block the transient part of the VGSC current in the malignant cells., 'wherein the effective and pharmaceutically acceptable amount'}2. The method according to claim 1 , wherein the VGSC is Nav1.53. The method according to claim 2 , wherein the VGSC is the neonatal form.4. The method according to claim 2 , wherein the cancer patient suffers from breast cancer.5. The method according to claim 1 , wherein the VGSC is Nav1.7.6. The method according to claim 5 , wherein the cancer patient suffers from prostate cancer.7. A method for inhibiting metastatic and invasive growth of malignant cells in a cancer patient in need thereof claim 5 , comprisingadministering an effective and pharmaceutically acceptable amount to the patient of an inhibitor of a voltage gated sodium channel (VGSC), is not lethal to the malignant cells,', 'blocks or reduces the persistent part of the VGSC current in the malignant cells, and', 'does not block the transient part of the VGSC current in the malignant cells,, 'wherein the effective and pharmaceutically acceptable amount'}and wherein the inhibitor of the VGSC is a drug accepted for use in treatment of arrhythmia or angina ...

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16-01-2020 дата публикации

4-PYRIDONE COMPOUND OR SALT THEREOF, AND PHARMACEUTICAL COMPOSITION AND FORMULATION INCLUDING SAME

Номер: US20200017459A1
Принадлежит: FUJIFILM Corporation

An object of the present invention is to provide a compound or a salt thereof having anti-HBV activity, a pharmaceutical composition, an anti-hepatitis B virus agent, a production inhibitor of DNA of a hepatitis B virus, and a production or secretion inhibitor of a hepatitis B surface antigen. According to the present invention, provided are a compound represented by General Formula [1] or a salt thereof: 3. The compound or a salt thereof according to claim 2 ,{'sup': 'a1', 'sub': 1-6', '1-6, "wherein m R's are each independently the same as or different from each other, and are each a halogen atom, a Calkyl group which may be substituted, or a Calkoxy group which may be substituted; and"}m is an integer of 0 or 1.4. The compound or a salt thereof according to claim 2 ,{'sup': 'b1', 'sub': 1-6', '1-6', '1-6', '1-6, 'wherein Ris a hydrogen atom, a halogen atom, a Calkyl group which may be substituted, a Calkoxy group which may be substituted, a Calkylamino group which may be substituted, a di(Calkyl)amino group which may be substituted, or a heterocyclic group which may be substituted.'}5. The compound or a salt thereof according to claim 1 ,{'sup': '2', 'wherein Ris a phenyl group which may be substituted, a thienyl group which may be substituted, a thiazolyl group which may be substituted, or a benzoxazinyl group which may be substituted.'}7. The compound or a salt thereof according to claim 6 ,{'sub': '1', 'wherein the substituent group Aisa halogen atom,a cyano group,{'sub': 1-6', '2, 'a Calkyl group which may have one or more substituents selected from the substituent group A,'}{'sub': 1-6', '2, 'a Calkoxy group which may have one or more substituents selected from the substituent group A,'}{'sub': 1-6', '2, 'a Calkylamino group which may have one or more substituents selected from the substituent group A,'}{'sub': 1-6', '2, 'a di(Calkyl)amino group which may have one or more substituents selected from the substituent group A, or'}{'sub': '2', 'a heterocyclic ...

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16-01-2020 дата публикации

METHODS FOR INHIBITING FASCIN

Номер: US20200017506A1
Принадлежит:

Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof. 6. The method of claim 1 , wherein Ris phenyl optionally substituted with one claim 1 , two claim 1 , or three groups chosen from halo and lower alkyl.7. The method of claim 1 , wherein Ris triazole.8. The method of claim 2 , wherein m is 0.9. The method of claim 1 , wherein Lis —N(R)S(O)—.10. The method of claim 1 , wherein Lis —S—.11. The method of claim 1 , wherein Xis OH and Xis O.12. The method of claim 1 , wherein Ris independently selected from the group consisting of OH claim 1 , halo claim 1 , lower alkyl claim 1 , and —OR.13. (canceled)16. The method of claim 15 , wherein Wis S.17. The method of claim 14 , wherein Ris phenyl optionally substituted with halo or alkyl.18. The method of claim 14 , wherein Ris phenyl optionally substituted with halo or alkyl.19. The method of claim 14 , wherein Rand Rare phenyl.20. The method of claim 14 , wherein Ris methyl claim 14 , phenyl claim 14 , or benzyl.2122-. (canceled)2467-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/972,649, filed on Aug. 21, 2013, which claims the benefit of U.S. Provisional Patent Application No. 61/692,177, filed on Aug. 22, 2012, and U.S. Provisional Patent Application No. 61/778,015, filed on Mar. 12, 2013. The entire contents of the foregoing applications are hereby incorporated herein by reference in their entireties.The technology described herein was developed with funds from National Institutes of Health Grant No. R01 CA136837. The United States Government has certain rights to the technology.The present technology relates generally to methods for treating or preventing cancer.In recent years, progress has ...

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28-01-2016 дата публикации

Novel 3-(4(benzyloxy)phenyl)hex-4-inoic acid derivative, method of preparing same and pharmaceutical composition for preventing and treating metabolic disease including same as effective ingredient

Номер: US20160024063A1
Принадлежит: Hyundai Pharm Co Ltd

The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.

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17-04-2014 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC BODY

Номер: US20140107247A1
Автор: OKUYAMA Kumi, Sakamoto Kei
Принадлежит: ZEON CORPORATION

The invention provides a polymerizable compound represented by formula (I), a polymerizable composition, and a polymer that have a practical low melting point, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article. In the formula: Y-Yrepresent a single bond, —O—, —O—C(═O)—, —C(═O)—O—, or the like; Gand Grepresent a bivalent aliphatic group, or the like, of C1-20; Zand Zrepresent a C2-10 alkenyl group or the like; Arepresents a C2-30 organic group, or the like, having at least one aromatic ring selected from an aromatic hydrocarbon ring and a hetero-aromatic ring; Arepresents a hydrogen atom, a C1-6 alkyl group, or a C2-30 organic group, or the like, having at least one aromatic ring selected from an aromatic hydrocarbon ring and a hetero-aromatic ring; Arepresents a trivalent aromatic group or the like; Aand Arepresent a bivalent aromatic group or the like; Qrepresents a hydrogen atom, a C1-6 alkyl group, or the like. Aand Amay form a ring together. 2. The polymerizable compound according to claim 1 , wherein a total number of π electrons included in Aand Ais 4 to 24.3. The polymerizable compound according to claim 1 , wherein Ais a substituted or unsubstituted trivalent benzene ring claim 1 , or a substituted or unsubstituted trivalent naphthalene ring claim 1 , and Aand Aare independently a substituted or unsubstituted phenylene group claim 1 , or a substituted or unsubstituted naphthylene group.4. The polymerizable compound according to claim 1 , wherein Yto Yare independently a chemical single bond claim 1 , —O— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , or —O—C(═O)—O—.5. The polymerizable compound according to claim 1 , wherein Zand Zare independently CH═CH— claim 1 , CH═C(CH)— claim 1 , or CH═C(Cl)—.6. The polymerizable compound according to claim 1 , wherein Gand Gare independently a substituted or unsubstituted divalent ...

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25-01-2018 дата публикации

POLYMERIZABLE COMPOUND AND OPTICAL ISOMER

Номер: US20180022716A1
Принадлежит: DIC CORPORATION

The present invention provides a polymerizable compound having high storage stability without causing crystal precipitation when added to a polymerizable composition. The present invention also provides a polymerizable composition containing the compound. When the filmy polymer produced through polymerization of the polymerizable composition is irradiated with UV light, it hardly discolors or peels from substrate. Further, the present invention provides a polymer produced through polymerization of the polymerizable composition and an optically anisotropic body using the polymer. 4. The compound according to claim 2 , wherein in the formula (I-R) claim 2 , Sp each independently represents an alkylene group having 1 to 20 carbon atoms in which one —CH— or two or more of (—CH—)'s which are not adjacent to each other may be each independently substituted with —O— claim 2 , —COO— claim 2 , —OCO— claim 2 , —OCO—O— claim 2 , —CO—NH— claim 2 , —NH—CO— claim 2 , —CH═CH— or —C≡C—.5. A composition containing the compound of .6. A liquid crystal composition containing the compound of .7. A polymer obtained through polymerization of the composition of .8. An optically anisotropic body using the polymer of .9. Resins claim 1 , resin additives claim 1 , oils claim 1 , filters claim 1 , adhesives claim 1 , pressure-sensitive adhesives claim 1 , oils and fats claim 1 , inks claim 1 , medicines claim 1 , cosmetics claim 1 , detergents claim 1 , building materials claim 1 , wrapping or packaging materials claim 1 , liquid crystal materials claim 1 , organic EL materials claim 1 , organic semiconductor materials claim 1 , electronic materials claim 1 , display devices claim 1 , electronic devices claim 1 , communication instruments claim 1 , automobile parts claim 1 , airplane parts claim 1 , machine parts claim 1 , agricultural chemicals and foods using the compound of . The present invention relates to a compound having a polymerizable group, a polymerizable composition containing ...

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22-01-2015 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20150025076A1
Принадлежит:

The present invention relates to modulator of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. 1226-. (canceled)228230-. (canceled)231. The pharmaceutical composition according to claim 227 , wherein Xis CH claim 227 , CF claim 227 , or O.232. The pharmaceutical composition according to claim 227 , wherein Xis CH.233. The pharmaceutical composition according to claim 227 , wherein Ais selected from phenyl claim 227 , triazinyl claim 227 , pyrazinyl claim 227 , pyrimidinyl claim 227 , pyridazinyl claim 227 , pyridyl claim 227 , thiadiazolyl claim 227 , triazolyl claim 227 , oxadiazolyl claim 227 , isothiazolyl claim 227 , pyrazolyl claim 227 , imidazolyl claim 227 , thiazolyl claim 227 , oxazolyl claim 227 , pyrrolyl claim 227 , thienyl claim 227 , furanyl claim 227 , indolizinyl claim 227 , indolyl claim 227 , isoindolyl claim 227 , benzofuranyl claim 227 , benzo[b]thienyl claim 227 , 1H-indazolyl claim 227 , benzimidazolyl claim 227 , benzthiazolyl claim 227 , purinyl claim 227 , quinolinyl claim 227 , isoquinolinyl claim 227 , cinnolinyl claim 227 , phthazinyl claim 227 , quinazolinyl claim 227 , quinoxalinyl claim 227 , 1 claim 227 ,8-naphthyridinyl claim 227 , pteridinyl claim 227 , carbazolyl claim 227 , acridinyl claim 227 , phenazinyl claim 227 , phenothiazinyl claim 227 , phenoxazinyl claim 227 , indenyl claim 227 , naphthyl claim 227 , azulinyl claim 227 , or anthracenyl.234. The pharmaceutical composition according to claim 227 , wherein each Bis independently selected from optionally substituted C6-C10 aryl.235. The pharmaceutical composition according to claim 227 , wherein each Bis independently an optionally substituted phenyl or naphthyl.236. The pharmaceutical composition according to claim 227 , wherein each Bis an unsubstituted ...

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22-01-2015 дата публикации

COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE

Номер: US20150025094A1
Принадлежит:

The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related disorders. 132-. (canceled)34. A compound of claim 33 , wherein at least one of Xto Xis O.35. A compound of claim 33 , wherein at least two of Xto Xare O.36. A compound of claim 33 , wherein least one of Xto Xis CHR.37. A compound of claim 33 , wherein Ris aryl or heretroaryl.38. A compound of claim 33 , wherein Y and Z are identical.39. A compound of claim 33 , wherein Y and Z are S.41. A compound of claim 33 , being used as a medicament.42. A composition comprising a compound according to .43. A method of treating or preventing a condition claim 33 , symptom or disease associate with elevated blood glucose levels in a subject in need thereof claim 33 , said method comprising administering to said subject a compound of .44. A method for the treatment or prevention of at least one condition selected from hyperglycemia claim 33 , diabetes claim 33 , altered insulin secretion claim 33 , ...

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28-01-2021 дата публикации

BINDING FUNCTION 3 (BF3) SITE COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE

Номер: US20210024464A1
Принадлежит:

This invention provides compound having a structure of Formulas: 120-. (canceled)281. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim and a pharmaceutically acceptable excipient.29. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to and a pharmaceutically acceptable excipient.301. A method of modulating AR activity claim 27 , the method comprising (a) administering a compound of claim to a subject in need thereof.31. The method of claim 30 , wherein the modulating AR activity is for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 30 , prostate cancer claim 30 , breast cancer claim 30 , ovarian cancer claim 30 , endometrial cancer claim 30 , bladder cancer claim 30 , Taxene resistant triple negative breast cancer claim 30 , hair loss claim 30 , acne claim 30 , hirsutism claim 30 , ovarian cysts claim 30 , polycystic ovary disease claim 30 , precocious puberty claim 30 , and age-related macular degeneration.32. The method of claim 31 , wherein the modulating AR activity is for the treatment of prostate cancer.33. The method of claim 31 , wherein the modulating AR activity is for the treatment of Taxene resistant triple negative breast cancer.34. The method of claim 31 , wherein the modulating AR activity is for the treatment of ovarian cancer.35. The method of claim 31 , wherein the modulating AR activity is for the treatment of endometrial cancer. This application is a continuation of U.S. application Ser. No. 16/426,406, filed May 30, 2019, which is a divisional application of U.S. application Ser. No. 15/302,363, filed Oct. 6, 2016, now U.S. Pat. No. 10,351,527, which is a National Stage Application of International Patent Application No. PCT/CA2015/000239, filed Apr. 9, 2015; which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/977,445, filed Apr. 9, 2014 and U.S. ...

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24-04-2014 дата публикации

EPOXYEICOSATRIENOIC ACID ANALOGS AND METHODS OF MAKING AND USING THE SAME

Номер: US20140113884A1
Принадлежит:

Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described. 5. A composition comprising a compound of and a pharmaceutically acceptable carrier.6. A method of reducing hypertension in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein hypertension in said subject is reduced.7. (canceled)8. (canceled)9. A method of reducing nephrotoxicity in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein nephrotoxicity in said subject is reduced.10. The method of claim 9 , wherein the nephrotoxicity is drug-induced.11. The method of claim 10 , wherein the nephrotoxicity is cisplatin-induced.12. (canceled)13. (canceled)14. A method of reducing cisplatin nephrotoxicity in a subject claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein cisplatin nephrotoxicity in said subject is reduced.15. (canceled)16. (canceled)17. A composition comprising a compound of and a pharmaceutically acceptable carrier.18. A method of reducing hypertension in a subject claim 4 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 4 , wherein hypertension in said subject is reduced.19. A method of reducing nephrotoxicity in a subject claim 4 , comprising administering to a subject a therapeutically effective amount of a compound according to claim 4 , wherein nephrotoxicity in said subject is reduced.20. The method of claim 19 , wherein the nephrotoxicity is drug-induced.21. The method of claim 20 , wherein the nephrotoxicity is cisplatin-in-induced.22. A method of ...

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02-02-2017 дата публикации

BINDING FUNCTION 3 (BF3) SITE COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE

Номер: US20170029372A1
Принадлежит:

This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide. 2. The compound of claim 1 , wherein the compound is selected from one or more of the compounds in TABLE 2.7. The compound of any one of - claim 1 , for use in the treatment of at least one indication selected from the group consisting of: cancer claim 1 , hair loss claim 1 , acne claim 1 , hirsutism claim 1 , ovarian cysts claim 1 , polycystic ovary disease claim 1 , precocious puberty claim 1 , and age related macular degeneration.8. A pharmaceutical composition for modulating AR activity claim 1 , the composition comprising a compound of any one of - claim 1 , and a pharmaceutically acceptable carrier.9. The compound of any one of - claim 1 , for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 1 , prostate cancer claim 1 , breast cancer claim 1 , ovarian cancer claim 1 , endometrial cancer claim 1 , bladder cancer claim 1 , Taxene resistant triple negative breast cancer claim 1 , hair loss claim 1 , acne claim 1 , hirsutism claim 1 , ovarian cysts claim 1 , polycystic ovary disease claim 1 , precocious puberty claim 1 , and age-related macular degeneration.10. A method of modulating AR activity claim 1 , the method comprising (a) administering a compound of any one of - or a pharmaceutical composition of to a subject in need thereof.11. The method of claim 10 , wherein the modulating AR activity is for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 10 , prostate cancer claim 10 , breast cancer claim 10 , ovarian cancer claim 10 , endometrial cancer claim 10 , bladder cancer claim 10 , Taxene resistant triple negative breast cancer claim 10 , hair loss claim 10 , acne claim 10 , hirsutism claim 10 , ovarian cysts claim 10 , ...

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02-02-2017 дата публикации

POLYMERIZABLE COMPOUND, COMPOSITION, POLYMER, OPTICALLY ANISOTROPIC BODY, LIQUID CRYSTAL DISPLAY DEVICE, AND ORGANIC EL DEVICE

Номер: US20170029655A1
Принадлежит: DIC CORPORATION

It is an object of the present invention to provide a polymerizable compound suitable as a material for optically anisotropic bodies having excellent optical properties, a composition containing the polymerizable compound, a polymer obtained by polymerizing the polymerizable compound, an optically anisotropic body formed of the polymer, and a liquid crystal display device including the optically anisotropic body. 2. The polymerizable compound according to claim 1 , wherein X claim 1 , X claim 1 , X claim 1 , and Xeach independently represent a single bond claim 1 , —CHCH— claim 1 , —CH═CH— claim 1 , —C≡— claim 1 , —CH═CHCOO— claim 1 , —OCO—CH═CH— claim 1 , —(CH)—O—COO— claim 1 , —(CH)—OCO— claim 1 , —(CH)—COO— claim 1 , —(CH)—O— claim 1 , —O—COO—(CH)— claim 1 , —OCO—(CH)— claim 1 , —COO—(CH)— claim 1 , or —O—(CH)— (u represents an integer of 0 to 2).3. A composition comprising the polymerizable compound according to .4. A polymer obtained by polymerizing the composition according to .5. An optically anisotropic body using the polymer according to .6. A liquid crystal display device using the optically anisotropic body according to .7. An organic EL device using the optically anisotropic body according to . The present invention relates to a polymerizable compound, a composition, a polymer, an optically anisotropic body, a liquid crystal display device, and an organic EL device.Optically anisotropic bodies such as retardation films and polarizing plates used in liquid crystal displays can be produced by applying a solution containing a polymerizable liquid crystal material onto a substrate subjected to a rubbing treatment or a substrate having a photo-alignment film formed thereon, drying a solvent, and then performing polymerization using ultraviolet rays or heat. Regarding retardation films, the wavelength dispersion of the birefringence index (Δn) needs to be decreased or reversed in order to improve the viewing angle of liquid crystal displays. To realize such ...

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31-01-2019 дата публикации

SULFUR(VI) FLUORIDE COMPOUNDS AND METHODS FOR THE PREPARATION THEREOF

Номер: US20190029972A1
Принадлежит: The Scripps Research Institute

This application describes a compound represented by Formula (I): 1. A compound represented by Formula (I):{'br': None, 'sup': 1', '2, 'sub': m', 'n, 'Y\ue8a0Z\ue8a0X—S(O)(X)F)]\u2003\u2003(I)'}wherein:Y is a biologically active organic core group comprising one or more unsubstituted or substituted moiety selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, a nonaromatic heterocyclic group, to which each Z independently is covalently bonded;n is 1, 2, 3, 4 or 5;each Z independently is O, NR, or N;{'sup': '1', 'when Z is O, m is 1, Xis a covalent bond, and the Z is covalently bonded to an aryl or heteroaryl moiety of Y;'}{'sup': '1', 'sub': 2', '2, 'when Z is NR, m is 1, Xis a covalent bond or CHCH, and the Z is covalently bonded to a nonaromatic hydrocarbyl, a nonaromatic heterocyclic, an aryl, or heteroaryl moiety of Y;'}{'sup': 1', '1, 'sub': 2', '2', '2', '2, 'when Z is N, either (a) m is 2, Xis CHCHand the Z is covalently bonded to a nonaromatic hydrocarbyl, a nonaromatic heterocyclic, an aryl, or a heteroaryl moiety of Y; or (b) m is 1, Xis a covalent bond or CHCH, and the Z is a nitrogen in an aromatic or non-aromatic heterocyclic ring portion of core group Y;'}{'sup': '2', 'each Xindependently is O or NR; and'}each R independently comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group.2. The compound of claim 1 , wherein each Xis O claim 1 , each Z independently is O claim 1 , NR claim 1 , or N; and at least one Z is O.3. The compound of claim 1 , wherein claim 1 , each Xis O claim 1 , each Z independently is O claim 1 , NR claim 1 , or N; and at least one Z is NR.4. The compound of claim 1 , wherein claim 1 , each Xis O claim 1 , each Z independently is O claim 1 , NR claim 1 , or N; and at least one Z is N.5. The compound of claim 1 , wherein claim 1 , each Xis O claim 1 , each Xis a covalent bond claim 1 ...

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30-01-2020 дата публикации

AGENT FOR REDUCING VISCERAL FAT WEIGHT

Номер: US20200030299A1
Принадлежит: KOWA CO., LTD.

An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): 1. A method for reducing visceral fat weight comprising administering, to a subject in need thereof, a compound represented by the following formula (1):{'sup': 1', '2', '3a', '3b', '4a', '4b', '3a', '3b', '4a', '4b', '5', '5, 'sub': 1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', 'l, 'wherein each of Rand R, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R, R, R, and R, which may be identical to or different from one another, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a Calkyl group, a trifluoromethyl group, a Calkoxy group, a Calkylcarbonyloxy group, a di-Calkylamino group, a Calkylsulfonyloxy group, a Calkylsulfonyl group, a Calkylsulfinyl group, or a Calkylthio group, or Rand Ror Rand Rmay bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R(Rrepresents a hydrogen atom, a Calkyl group, a Calkylsulfonyl group, or a Calkyloxycarbonyl group); Y represents an oxygen atom, an S(O)group (l is a number of from 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, an aminosulfonyl group, or an NH group;'}Z represents CH or N; n is a number of from 1 to 6; and m is a number of from 2 to 6, a salt of the compound, or a solvate of the compound or the salt. This application is a continuation of U.S. application Ser. No. 15/787,049, filed on Oct. 18, 2017, which is a continuation of U.S. application Ser. No. 15/145,090, filed on May 3, 2016, which is a continuation of U.S. application Ser. No. 13/393,164, filed on Feb. 28, 2012, and incorporated herein by reference, which is a National Stage of PCT/JP10/066678 filed Sep. 27, 2010 and claims the benefit of JP 2009-222853 filed on Sep. 28, 2009.The present invention relates to ...

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30-01-2020 дата публикации

Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof

Номер: US20200030325A1
Принадлежит:

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. 121-. (canceled)23. The compound of claim 22 , wherein ring A is phenyl claim 22 , naphthyl claim 22 , anthracenyl claim 22 , pyridinyl claim 22 , pyrimidinyl claim 22 , pyrazinyl claim 22 , indolyl claim 22 , imidazolyl claim 22 , oxazolyl claim 22 , furyl claim 22 , thienyl claim 22 , thiazolyl claim 22 , triazolyl claim 22 , isoxazolyl claim 22 , quinolinyl claim 22 , pyrrolyl claim 22 , pyrazolyl claim 22 , or 5 claim 22 ,6 claim 22 ,7 claim 22 ,8-tetrahydroisoquinoline; each of which may be optionally substituted with halo.24. The compound of claim 22 , wherein Ris H claim 22 , methyl claim 22 , ethyl claim 22 , propyl claim 22 , i-propyl claim 22 , butyl claim 22 , i-butyl claim 22 , t-butyl claim 22 , pentyl claim 22 , hexyl claim 22 , phenyl claim 22 , naphthyl claim 22 , pyridinyl claim 22 , OH or OCH; each of which may be optionally substituted with OH claim 22 , halo claim 22 , alkyl claim 22 , or alkoxy.25. The compound of claim 22 , wherein the carbonyl and the Z group attached to ring A are disposed para to each other.26. The compound of claim 22 , wherein the carbonyl and Z group attached to ring A are disposed meta to each other.27. The compound of claim 22 , wherein the carbonyl and the Z group attached to ring A are disposed ortho to each other.29. The compound of claim 28 , wherein ring B is phenyl claim 28 , pyridinyl claim 28 , pyrimidinyl claim 28 , or pyrazinyl; wherein phenyl claim 28 , pyridinyl claim 28 , pyrimidinyl claim 28 , or pyrazinyl may be optionally substituted with alkyl claim 28 , aryl claim 28 , heteroaryl claim 28 , cycloalkyl claim 28 , heterocycloalkyl claim 28 , aralkyl claim 28 , haloalkyl claim 28 , halo claim 28 , OH claim 28 , NH claim 28 , NHR″ claim 28 , CN claim 28 , N claim 28 , or ...

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30-01-2020 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE LIQUID CRYSTAL MIXTURE, POLYMER, OPTICAL FILM, OPTICALLY ANISOTROPIC BODY, POLARIZING PLATE, DISPLAY DEVICE, ANTIREFLECTION FILM, AND COMPOUND

Номер: US20200031786A1
Принадлежит: ZEON CORPORATION

Disclosed is a polymerizable compound useful for preparing a polymer that enables the production of a film, such as an optical film, which has a good balance of lightness and saturation and which can improve reverse wavelength dispersion on the short wavelength side while achieving reverse wavelength dispersion on the longer wavelength side. The polymerizable compound of the present disclosure is represented by: 4. The polymerizable compound according to claim 3 , wherein Ayand Ayeach independently represent a hydrogen atom claim 3 , an alkyl group having 1 to 20 carbon atoms which may have a substituent claim 3 , an alkenyl group having 2 to 20 carbon atoms which may have a substituent claim 3 , an alkynyl group having 2 to 20 carbon atoms which may have a substituent claim 3 , a cycloalkyl group having 3 to 12 carbon atoms which may have a substituent claim 3 , an aromatic hydrocarbon ring group having 6 to 30 carbon atoms which may have a substituent claim 3 , or claim 3 , an aromatic heterocyclic ring group having 2 to 30 carbon atoms which may have a substituent.7. The polymerizable compound according to claim 1 , wherein p and q are both 0.8. The polymerizable compound according to claim 1 , wherein p and q are both 1 claim 1 , and claim 1 , Band Beach independently represent a cyclic aliphatic group which may have a substituent.11. A polymerizable liquid crystal mixture comprising the polymerizable compound according to as a main component.16. A polymer obtainable by polymerizing the polymerizable liquid crystal mixture according to .17. An optical film composed of the polymer according to as a constituent material.18. An optically anisotropic body comprising a layer composed of the polymer according to as a constituent material.19. A polarizing plate comprising the optically anisotropic body according to and a polarizing film.20. A display device comprising the polarizing plate according to .21. An antireflection film comprising the polarizing plate ...

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30-01-2020 дата публикации

ULTRAVIOLET-STABILIZED CORROSION INHIBITORS

Номер: US20200032401A1
Принадлежит:

According to one embodiment of the present disclosure, a method of forming an ultraviolet-stabilized corrosion inhibitor is provided. The method includes forming a functionalized azole; forming a functionalized photosensitizer; and forming an ultraviolet-stabilized corrosion inhibitor by reacting the functionalized azole with the functionalized photosensitizer. In another embodiment, an ultraviolet-stabilized corrosion inhibitor is provided. The inhibitor includes an azole bonded to a photosensitizer. In another embodiment, an article of manufacture is provided. The article of manufacture includes a material comprising a reaction product of an azole and a photosensitizer. 1. A method of forming an ultraviolet-stabilized corrosion inhibitor , comprising:forming a functionalized azole;forming a functionalized photosensitizer; andforming an ultraviolet-stabilized corrosion inhibitor by reacting the functionalized azole with the functionalized photosensitizer.2. The method of claim 1 , wherein the functionalized azole comprises a benzotriazole claim 1 , a benzothiazole claim 1 , a benzoxazole claim 1 , or a derivative thereof.3. The method of claim 1 , wherein the functionalized azole comprises a bromine atom.4. The method of claim 1 , wherein the functionalized azole comprises a boronic ester.5. The method of claim 1 , wherein the functionalized photosensitizer comprises an avobenzone claim 1 , an oxybenzone claim 1 , an octisalate claim 1 , an octocrylene claim 1 , a homosalate claim 1 , an octinoxate claim 1 , or a derivative thereof.6. The method of claim 1 , wherein the functionalized photosensitizer comprises a bromine.7. The method of claim 1 , wherein the functionalized photosensitizer comprises an alkyne.8. The method of claim 1 , wherein the forming the ultraviolet-stabilized corrosion inhibitor comprises performing a palladium cross-coupling reaction.10. An ultraviolet-stabilized corrosion inhibitor comprising:an azole bonded to a photosensitizer.11. The ...

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08-02-2018 дата публикации

RILUZOLE PRODRUGS AND THEIR USE

Номер: US20180036290A1
Принадлежит:

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. 3. A composition comprising an effective amount of at least one compound according to and at least one excipient.4. A method for treating or preventing cancer claim 1 , said method comprising administering to a subject an effective amount of at least one compound according to .5. The method of claim 4 , wherein the at least one compound is administered in a composition further comprising at least one excipient.6. The method of claim 5 , wherein the at least one compound is administered in a composition further comprising an anticancer agent.7. The method of wherein the anticancer agent is selected from the group consisting of Vemurafenib claim 6 , Ipilimumab claim 6 , Masitinib claim 6 , Sorafenib claim 6 , Lenalidomide claim 6 , Oblimersen claim 6 , Trametinib claim 6 , Dabrafenib claim 6 , RO5185426 claim 6 , Veliparib claim 6 , Bosentan claim 6 , YM155 claim 6 , CNTO 95 claim 6 , CR011-vcMMAE claim 6 , CY503 claim 6 , Lenvatinib claim 6 , Avastin claim 6 , Tasidotin claim 6 , Ramucirumab claim 6 , IPI-504 claim 6 , Tasisulam claim 6 , KW2871 claim 6 , MPC-6827 claim 6 , RAF265 claim 6 , Dovitinib claim 6 , Everolimus claim 6 , MEK162 claim 6 , BKM120 claim 6 , Nilotinib claim 6 , Reolysin claim 6 , 825A claim 6 , Tremelimumab claim 6 , PI-88 claim 6 , Elesclomol claim 6 , STA9090 claim 6 , and Allovectin-7.8. The method of wherein the cancer is selected from the group consisting of melanoma claim 6 , nonmelanoma skin cancer claim 6 , skin cancer claim 6 , ovarian cancer claim 6 , cervical cancer claim ...

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09-02-2017 дата публикации

GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

Номер: US20170037016A1
Принадлежит:

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': {'sub': 1', '6', '2', '6', '2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'each optionally substituted C-C-alkyl or C-C-alkenyl, O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}, 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': w', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of one another ...

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08-02-2018 дата публикации

PRODRUGS RILUZOLE AND THEIR METHOD OF USE

Номер: US20180037557A1
Принадлежит:

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. 18. A compound according to selected from the group consisting of:2-(methylamino)-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) acetamide;(S)—N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)pyrrolidine-2-carboxamide;(R)-2-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;3-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;1-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) cyclopropane-1-carboxamide;(S)—N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)azetidine-2-carboxamide;2-amino-2-methyl-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;(S)-2-(methylamino)-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;(R)-2-(methylamino)-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;(R)-2-amino-3-hydroxy-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) propanamide;(R)-2-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)pent-4-ynamide;(S)-2-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)pent-4-ynamide;(R)—N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)pyrrolidine-2-carboxamide;1-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)cyclobutane-1-carboxamide;(S)-2-amino-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl) pentanamide;(R)-2-amino-3-methyl-N-(2-oxo-2 ...

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08-02-2018 дата публикации

PARTICLES FOR ELECTROPHORETIC DISPLAYS

Номер: US20180037744A1
Принадлежит:

This invention relates to polymer particles preferably with surface functionality for charge retention, a process for their preparation, the use of these particles for the preparation of an electrophoretic device, electrophoretic displays comprising such particle, and new polymerisable dyes. 118.-. (canceled)19. A coloured polymer particle for use in electrophoretic devices comprising at least one A-B diblock copolymer comprising a hydrophobic polymer block A and a hydrophilic polymer block B containing a charge or being chargeable , and monomer units of at least one monomer , of at least one polymerisable dye , optionally of at least one charged co-monomer , and optionally of at least one crosslinking co-monomer.20. The coloured polymer particle according to claim 19 , wherein block A is a polymethylmethacrylate block.21. The coloured polymer particle according to claim 19 , wherein block B comprises amino groups or carboxylic acid groups.22. The coloured polymer particle according to claim 19 , wherein block B is charged with 0.2% to 100% permanent charge based on partially or completely quaternised nitrogen groups or partially or completely neutralised acid groups.23. The coloured polymer particle according to claim 19 , wherein a polymerisable dye comprises a chromophore claim 19 , at least one polymerisable group claim 19 , optionally at least one linker group claim 19 , and optionally at least one charged group is used.24. The coloured polymer particle according to claim 19 , wherein the polymer particles have a diameter of 50-1000 nm.25. The coloured polymer particle according to claim 19 , wherein a water-soluble polymerisable dye is used.27. A process for the preparation of coloured polymer particles for use in electrophoretic devices claim 19 , comprisinga) the reaction of at least one monomer, at least one A-B diblock copolymer comprising a hydrophobic polymer block A and a hydrophilic polymer block B containing a charge or being chargeable, at least one ...

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07-02-2019 дата публикации

Modulators of indoleamine 2,3-dioxygenase

Номер: US20190040023A1

Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.

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12-02-2015 дата публикации

Selective glycosidase inhibitors and uses thereof

Номер: US20150045346A1

The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

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12-02-2015 дата публикации

Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

Номер: US20150045380A1
Принадлежит: Acetylon Pharmaceuticals Inc

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

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12-02-2015 дата публикации

PRODRUGS OF RILUZOLE AND THEIR METHOD OF USE

Номер: US20150045401A1
Принадлежит:

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. 2. (canceled)4. The compound according to that is:2-Amino-N-(6-trifluoromethoxy-benzothiazol-2-yl)-acetamide;(R)-2-Amino-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(R)-2-Amino-3-phenyl-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(R)-2-Amino-3-benzyloxy-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(S)-2-Amino-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(S)-2-Amino-3-methyl-N-(6-trifluoromethoxy-benzothiazol-2-yl)-butyramide;(S)-2-Amino-3-phenyl-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(S)-2-Amino-3-benzyloxy-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propionamide;(S)-2-amino-3-(4-fluorobenzyloxy)-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propanamide;(S)-2-amino-3-(2,4-difluorobenzyloxy)-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propanamide;(S)-2-amino-3-methoxy-N-(6-trifluoromethoxy-benzothiazol-2-yl)-propanamide;(S)-3-tert-butoxy-2-amino-N-(6-(trifluoromethoxy)benzo[d]thiazol-2-yl)propanamide;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid methyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid ethyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid propyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid butyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid isobutyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid hexyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid 2-dimethylamino-ethyl ester;(6-Trifluoromethoxy-benzothiazol-2-yl)-carbamic acid 3-dimethylamino-propyl ester;N-(6- ...

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16-02-2017 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC MATERIAL

Номер: US20170044279A1
Автор: OKUYAMA Kumi, Sakamoto Kei
Принадлежит: ZEON CORPORATION

The present invention relates to: a polymerizable compound (I), wherein Yto Yare a chemical single bond, —O—C(═O)—, —C(═O)—O— or the like, Gand Gare a divalent aliphatic group, Zand Zare an alkenyl group, Ais a fused ring group represented by a formula (II), wherein X is —NR—, an oxygen atom, a sulfur atom or the like, Ris a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and D is a substituted or unsubstituted ring having 1 to 20 carbon atoms that includes at least one nitrogen atom, Ais a hydrogen atom, an alkyl group, Ais a trivalent aromatic group or the like, Aand Aare a divalent aromatic group having 6 to 30 carbon atoms or the like, and Qis a hydrogen atom, or an alkyl group having 1 to 6 carbon atoms. 3. A method for producing an optically anisotropic article , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'reacting the hydrazine compound according to with a carbonyl compound for preparing a polymerizable compound;'}forming a liquid crystal layer including a polymer by polymerizing the polymerizable compound or a polymerizable composition containing the polymerizable compound and an initiator on a substrate having an alignment film.4. A method for producing a polymerizable compound comprising reacting the hydrazine compound according to with a precursor compound of said polymerizable compound.5. The method according to claim 4 , wherein the polymerizable compound is a liquid crystalline compound.7. The method according to claim 6 , wherein the polymerizable compound is a liquid crystalline compound.9. A method for producing an optically anisotropic article claim 6 , comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'reacting the hydrazine compound according to with a carbonyl compound for preparing a polymerizable compound;'}forming a liquid crystal layer including a polymer formed by polymerizing the polymerizable compound or a polymerizable composition containing the polymerizable compound and an initiator on a ...

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08-05-2014 дата публикации

Method for Promoting Differentiation of Pluripotent Stem Cells into Cardiac Muscle Cells

Номер: US20140127807A1
Принадлежит: KYOTO UNIVERSITY

The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells 2. The compound or salt thereof according to claim 1 , wherein Ris a methoxy.3. The compound or salt thereof according to claim 1 , wherein Ris I.4. The compound or salt thereof according to claim 1 , wherein Ris Cl.5. The compound or salt thereof according to claim 1 , wherein Ris Br.8. The method for inducing differentiation of pluripotent stem cells into cardiac muscle cells of claim 7 , further comprisingconfirming differentiation of the pluripotent stem cells into cardiac muscle cells after a prescribed time of culturing the cells.9. The method for inducing differentiation of pluripotent stem cells into cardiac muscle cells of claim 7 , wherein the compound or the salt thereof is added in the final amount of between 0.5 to 20 μM.10. The method for inducing differentiation of pluripotent stem cells into cardiac muscle cells of claim 7 , wherein Ris a methoxy.11. The method for inducing differentiation of pluripotent stem cells into cardiac muscle cells of claim 7 , wherein Ris I claim 7 , Cl claim 7 , or Br. This application is a continuation-in-part of U.S. patent application Ser. No. 13/777,765 filed on Feb. 26, 2013, which is a continuation of International PCT Application No. PCT/JP2011/069054 filed on Aug. 24, 2011 that claims the benefit under 35 U.S.C. 119(d) of Japanese Patent Application No. 2010-189548 filed on Aug. 26, 2010. This application also claims the benefit under 35 U.S.C. 119(d) of Japanese Patent Application No. 2013-190462 filed on Sep. 13, 2013. The contents of the foregoing applications are hereby incorporated by reference in their entireties.This invention relates to the field of regenerative medicine. In particular, the invention relates to a composition for promoting ...

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08-05-2014 дата публикации

Piperazine compound capable of inhibiting prostaglandin d synthase

Номер: US20140128394A1
Принадлежит: Taiho Pharmaceutical Co Ltd

This invention relates to a piperazine compound represented by Formula (I), wherein R 1 is c1-6 alkyl; R 2 is hydroxy, c1-6 alkyl that may have one or more substituents, —(C=0)-N(R 2 )(R 4 ), or —(C=0)-0R 5 ; R 3 and R 4 are the same or different, and each represents hydrogen or c1-6 alkyl that may have one or more substituents, or R 3 and R 4 , taken together with a nitrogen atom to which R 3 and R 4 are attached, may form a saturated heterocyclic group; R 5 is hydrogen or c1-6 alkyl that may have one or more 15 substituents; and n is 1 or 2; or a salt thereof.

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13-02-2020 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, OPTICALLY ANISOTROPIC BODY, AND METHOD FOR PRODUCING POLYMERIZABLE COMPOUND

Номер: US20200048213A1
Принадлежит: ZEON CORPORATION

A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. 2. The carbonyl compound according to claim 1 , wherein Ais a substituted or unsubstituted trivalent benzene ring group claim 1 , or a substituted or unsubstituted trivalent naphthalene ring group.3. The carbonyl compound according to claim 1 , wherein Aand Aare independently a substituted or unsubstituted divalent cyclohexyl group.4. The carbonyl compound according to claim 1 , wherein Zand Zare independently CH═CH— claim 1 , CH═C(CH)— claim 1 , or CH═C(Cl)—. This application is a Divisional of U.S. application Ser. No. 16/176,325 filed Oct. 31, 2018, which is a Divisional of U.S. application Ser. No. 15/179,145 filed Jun. 10, 2016, which is a Divisional of U.S. application Ser. No. 14/413,787 filed Jan. 9, 2015, which in turn is a National Stage Application of PCT/JP2013/065040 filed May 30, 2013, which claims the benefit of Japanese Application No. 2013-075379 (filed Mar. 29, 2013), Japanese Application No. 2013-064874 (filed Mar. 26, 2013), Japanese Application No. 2012-232316 (filed Oct. 19, 2012), and Japanese Application No. 2012-153914 (filed Jul. 9, 2012). The disclosures of the prior applications are hereby incorporated by reference herein in their entireties.The invention relates to a polymerizable compound, a polymerizable composition, and a polymer that may produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article, a carbonyl compound that is useful as a raw material for producing the polymerizable compound, a method for producing the polymerizable compound using the carbonyl compound, and a method for using the carbonyl compound as a raw material for producing the ...

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01-03-2018 дата публикации

AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS

Номер: US20180057444A1
Принадлежит: William Marsh Rice University

In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions. 1. A method of preparing an aminoaromatic group or a hydroxyaromatic group comprising:(A) admixing a metal aromatic compound with an oxaziridine compound to form a first reaction mixture under conditions sufficient to cause a reaction to obtain an anionic intermediate;(B) admixing a weak acid with the anionic intermediate and the first reaction mixture to obtain a second reaction mixture under conditions sufficient to obtain an aminoaromatic group or a hydroxyaromatic group.2. The method of claim 1 , wherein the metal of the metal aromatic compound is attached to one of the carbon atoms of the aromatic ring.3. The method of claim 1 , wherein the metal of the metal aromatic compound is a magnesium halide or lithium.48-. (canceled)9. The method of claim 1 , wherein the metal aromatic compound is substituted.10. (canceled)11. The method of claim 9 , wherein the metal aromatic compound is substituted with a substituent wherein the substituent is amino claim 9 , aminosulfonyl claim 9 , carboxy claim 9 , cyano claim 9 , halo claim 9 , hydroxy claim 9 , hydroxyamino claim 9 , hydroxysulfonyl claim 9 , mercapto claim 9 , nitro claim 9 , oxo claim 9 , or thio; or acyl claim 9 , alkoxy claim 9 , cycloalkoxy claim 9 , alkenyloxy claim 9 , aryloxy claim 9 , aralkoxy claim 9 , acyloxy claim 9 , cycloalkylalkoxy claim 9 , heterocycloalkylalkoxy claim 9 , heterocycloalkoxy claim 9 , alkylthio claim 9 , cycloalkylthio claim 9 , amido claim 9 , alkylamino claim 9 , dialkylamino claim 9 , alkylsulfonyl claim 9 , arylsulfonyl claim 9 , or a substituted version of these groups ...

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02-03-2017 дата публикации

ANTI-VIRAL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Номер: US20170057978A1
Принадлежит: Kineta, Inc.

Disclosed herein are compounds, pharmaceutical compositions, and related methods for the treatment of viral infection, including RNA viral infection in subjects. The compounds, pharmaceutical compositions, and methods can modulate the innate immune antiviral response in vertebrate cells, including activating the RIG-I pathway. 4. A compound of claim 1 , wherein Ris CF claim 1 , OR claim 1 , or a phenyl group substituted by at least one OCHgroup.9. A compound of or wherein Ris H; and V is C═O.10. A compound of any one of claim 1 , claim 1 , or wherein Ris optionally substituted phenyl or optionally substituted naphthyl.11. A compound of any one of - claim 1 , wherein W is S and X is N.12. A compound of any one of - claim 1 , wherein W is O and X is N.19. A pharmaceutical composition comprising a compound of any one of to .20. A method of treating a viral infection in a subject comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition of thereby treating the viral infection in the subject.21. A method of preventing a viral infection in a subject comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition of .22. A method of or wherein the viral infection is caused by a virus from one or more of the following families: Arenaviridae claim 19 , Arterivirus claim 19 , Astroviridae claim 19 , Birnaviridae claim 19 , Bromoviridae claim 19 , Bunyaviridae claim 19 , Caliciviridae claim 19 , Closteroviridae claim 19 , Comoviridae claim 19 , Coronaviridae claim 19 , Cystoviridae claim 19 , Filoviridae claim 19 , Flaviviridae claim 19 , Flexiviridae claim 19 , Hepadnaviridae claim 19 , Hepevirus claim 19 , Herpesviridae claim 19 , Leviviridae claim 19 , Luteoviridae claim 19 , Mesoniviridae claim 19 , Mononegavirales claim 19 , Mosaic Viruses claim 19 , Nidovirales claim 19 , Nodaviridae claim 19 , Orthomyxoviridae claim 19 , Papillomaviridae claim 19 , Paramyxoviridae claim 19 , ...

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28-02-2019 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, OPTICALLY ANISOTROPIC BODY, AND METHOD FOR PRODUCING POLYMERIZABLE COMPOUND

Номер: US20190062289A1
Принадлежит: ZEON CORPORATION

A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. 2. The carbonyl compound according to claim 1 , wherein Ais a substituted or unsubstituted trivalent benzene ring group claim 1 , or a substituted or unsubstituted trivalent naphthalene ring group.3. The carbonyl compound according to claim 1 , wherein Aand Aare independently a substituted or unsubstituted divalent cyclohexyl group.4. The carbonyl compound according to claim 1 , wherein Zand Zare independently CH═CH— claim 1 , CH═C(CH)— claim 1 , or CH═C(Cl)—. This Application is a Divisional of U.S. application Ser. No. 15/179,145 filed Jun. 10, 2016, which is a Divisional of U.S. application Ser. No. 14/413,787 filed Jan. 9, 2015, which in turn is a National Stage Application of PCT/JP2013/065040 filed May 30, 2013, which claims the benefit of Japanese Application No. 2013-075379 (filed Mar. 29, 2013), Japanese Application No. 2013-064874 (filed Mar. 26, 2013), Japanese Application No. 2012-232316 (filed Oct. 19, 2012), and Japanese Application No. 2012-153914 (filed Jul. 9, 2012). The disclosures of the prior applications are hereby incorporated by reference herein in their entireties.The invention relates to a polymerizable compound, a polymerizable composition, and a polymer that may produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article, a carbonyl compound that is useful as a raw material for producing the polymerizable compound, a method for producing the polymerizable compound using the carbonyl compound, and a method for using the carbonyl compound as a raw material for producing the polymerizable compound.A flat panel display (FPD) that utilizes an optical film (e.g., ...

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18-03-2021 дата публикации

PRODRUGS OF RILUZOLE AND THEIR METHOD OF USE

Номер: US20210078962A1
Принадлежит:

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. 130-. (canceled)32. The method of claim 31 , wherein the at least one compound is administered in a composition further comprising at least one excipient and an anticancer agent.34. The method of claim 33 , wherein the at least one compound is administered in a composition further comprising at least one excipient. This application claims the benefit of the filing date of U.S. Provisional Patent Application No. 61/612,210, filed Mar. 16, 2012, the disclosure of which is incorporated by reference herein in its entirety.The U.S. Government has a paid-up license in this invention and the right in limited circumstances to require the patent owner to license others on reasonable terms as provided for by the terms of grant number R43 CA156781-01 awarded by the National Cancer Institute.The present invention describes compounds and methods useful as prodrug agents, useful for the treatment of cancers including melanoma through the release of riluzole.A recently conducted Phase 0 human clinical trial of riluzole (Rilutek™) demonstrated dramatic efficacy in certain melanoma patients after only 14 days of treatment. Riluzole, the only FDA approved drug to treat amyotrophic lateral sclerosis (ALS), showed clinical or radiologic evidence of tumor response in four of 12 patients with Stage III and IV melanoma, cancer with a poor prognosis and severely limited treatment options.It is clear that the repositioned use of riluzole for melanoma or other cancers will be significantly constrained due to high levels of ...

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22-03-2018 дата публикации

AGENT FOR REDUCING VISCERAL FAT WEIGHT

Номер: US20180078530A1
Принадлежит: KOWA CO., LTD.

An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): 2. The method of claim 1 , wherein the (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid or a salt thereof is administered in a divided dose from one to three times daily.3. The method of claim 1 , wherein the (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid or a salt thereof is administered in a daily dose of 0.1 to 100 mg.4. The method of claim 2 , wherein the (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid or a salt thereof is administered in a daily dose of 0.1 to 100 mg.5. The method of claim 2 , wherein the (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid or a salt thereof is administered 0.1 to 1 mg/day. This application is a continuation of U.S. application Ser. No. 13/393,164 filed Feb. 28, 2012, pending and incorporated herein by reference, which is a National Stage of PCT/JP10/066678 filed Sep. 27, 2010 and claims the benefit of JP 2009-222853 filed Sep. 28, 2009.The present invention relates to an agent for promoting production of FGF21 (hereinafter may be referred to as an “FGF21 production promoting agent”), an agent for reducing visceral fat weight (hereinafter may be referred to as a “visceral fat weight reducing agent”), and a preventive and/or therapeutic agent for obesity or metabolic syndrome, each of the agents containing, as an active ingredient, compound (1) which selectively activates α-type peroxisome proliferator-activated receptor (PPARα).PPAR is a receptor belonging to the nuclear receptor family. PPAR binds to specific sites (peroxisome proliferator response elements, PPREs) of a target gene, and positively or negatively regulates transcription of the gene. As has been known, this receptor has three subtypes (α, γ, and δ) (Non-Patent ...

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12-03-2020 дата публикации

METHODS USING HDAC11 INHIBITORS

Номер: US20200079744A1
Принадлежит:

The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases. 3. The compound according to claim 2 , wherein L is selected from a bond claim 2 , —CH— claim 2 , —(CH)— claim 2 , —(CH)— claim 2 , —C(O)— claim 2 , —S(O)— claim 2 , —C(O)NR— claim 2 , or —C(O)CH—.4. The compound according to claim 2 , wherein L is selected from —CH— or —C(O)—.5. The compound according to claim 2 , wherein R is hydrogen or an optionally substituted group selected from C-Calkyl claim 2 , aryl claim 2 , C-Ccycloalkyl claim 2 , heterocyclyl claim 2 , or heteroaryl containing 1-5 heteroatoms selected from the group consisting of N claim 2 , S claim 2 , P claim 2 , or O.6. The compound according to claim 2 , wherein R is hydrogen or an optionally substituted group selected from phenyl claim 2 , C-Calkyl claim 2 , cyclopropyl claim 2 , cyclobutyl claim 2 , cyclopentyl claim 2 , cyclohexyl claim 2 , pyridyl claim 2 , or morpholinyl.7. The compound according to claim 2 , wherein R is phenyl optionally substituted with one or more independent occurrences of halogen claim 2 , CF claim 2 , —SOCH claim 2 , phenyl claim 2 , C-Calkyl claim 2 , C-Calkoxy claim 2 , pyridyl claim 2 , —OCFor —OCHphenyl.8. The compound according to claim 4 , wherein R is hydrogen or an optionally substituted group selected from phenyl claim 4 , C-Calkyl claim 4 , cyclopropyl claim 4 , cyclobutyl claim 4 , cyclopentyl claim 4 , cyclohexyl claim 4 , pyridyl claim 4 , or morpholinyl.9. The compound according to claim 4 , wherein R is phenyl optionally substituted with one or more independent occurrences of halogen claim 4 , CF claim 4 , —SOCH claim 4 , phenyl claim 4 , C-Calkyl claim 4 , C-Calkoxy claim 4 , pyridyl claim 4 , —OCFor —OCHphenyl.11. The compound according to claim 2 , wherein L is selected from a bond claim 2 , —CH— claim 2 , —(CH)— claim 2 , —(CH)— claim 2 , —C(O)— claim 2 , —S(O)— ...

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29-03-2018 дата публикации

INHIBITORS OF VIRUSES

Номер: US20180086749A1
Принадлежит:

The present technology is directed to compounds, compositions, and methods to treat a viral infection. The compound is according to Formula I or a solvate and/or pharmaceutically acceptable salt thereof. The technology is especially suited to treat Chikungunya virus, Zika virus, Venezuelan equine encephalitis virus, and/or respiratory syncytial virus infection. 2. The compound of claim 1 , wherein Xis N or CH.3. The compound of claim 1 , wherein Ris H claim 1 , or Rand Rtaken together are a substituted or unsubstituted C-Calkylenyl group.4. The compound of claim 1 , wherein Rand Rtaken together form a substituted or unsubstituted aryl or Rand Rtaken together are a substituted or unsubstituted C-Calkylenyl.6. The compound of claim 1 , wherein Ris a substituted or unsubstituted alkyl claim 1 , a substituted or unsubstituted phenyl claim 1 , or an unsubstituted heterocyclyl group.7. The compound of claim 1 , wherein Ris a substituted or unsubstituted alkyl claim 1 , a substituted or unsubstituted phenyl claim 1 , or an unsubstituted saturated heterocyclyl group.8. The compound of claim 1 , wherein when Xis —C(R)═C(R)— claim 1 , then Ris not trifluoromethyl and is not alkoxy.10. The compound of claim 9 , wherein Xis S or O.11. The compound of claim 9 , wherein Xis S.12. The compound of claim 1 , wherein when Xis S; Xis CH; Xis S; R claim 1 , R claim 1 , Rand Rare each independently H; and Rand Rtaken together form a unsubstituted cyclohexyl group; then Ris not H.13. The compound of claim 1 , wherein when Xis S; Xis CH; Xis S; R claim 1 , R claim 1 , R claim 1 , and Rare each independently H; and Rand Rtaken together form a unsubstituted cyclohexyl group; then Ris not phenyl.14. The compound of claim 1 , wherein when Xis S claim 1 , then R claim 1 , R claim 1 , and Rare each not trifluoromethyl.15. A composition comprising a compound of and a pharmaceutically acceptable carrier.16. A pharmaceutical composition for treating a viral infection claim 1 , the composition ...

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21-03-2019 дата публикации

METHODS USING HDAC11 INHIBITORS

Номер: US20190084945A1
Принадлежит:

The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases. 3. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , and Xare each CR.4. The compound of claim 3 , wherein each Ris independently H claim 3 , halogen claim 3 , —CF claim 3 , —OH claim 3 , —CN claim 3 , —SO(C-Calkyl) claim 3 , phenyl claim 3 , C-Calkyl claim 3 , C-Calkoxy claim 3 , pyridyl claim 3 , —C(O)C-Calkyl claim 3 , —OC-Calkyl claim 3 , —(C-Calkyl)O(C-Calkyl) claim 3 , —OCFor —OCHphenyl.5. The compound of claim 4 , wherein each Ris independently H or halogen.6. The compound of claim 2 , wherein Ris H claim 2 , —(CHR)NRR claim 2 , or —C-Calkyl optionally substituted with one or more substituents selected from —OH claim 2 , halogen claim 2 , —NO claim 2 , oxo claim 2 , —CN claim 2 , —R claim 2 , —O(C-C)alkyl claim 2 , —NH(C-C)alkyl claim 2 , —N(C-Calkyl) claim 2 , —S(O)N(C-Calkyl) claim 2 , —S(O)NHC-Calkyl claim 2 , —C(O)C-Calkyl claim 2 , —C(O)OC-Calkyl claim 2 , —N(C-Calkyl)S(O)C-Calkyl claim 2 , —S(O)R claim 2 , —S(O)N(C-Calkyl) claim 2 , or —N(C-Calkyl)S(O)R.7. The compound of claim 6 , wherein Ris H. This application claims the benefit of U.S. Provisional Application Ser. No. 62/410,766 filed Oct. 20, 2016, 62/410,767 filed Oct. 20, 2016, and 62/410,768 filed Oct. 20, 2016, the contents of all of which are hereby incorporated by reference in their entirety.This application contains a Sequence Listing which has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety. Said ASCII copy, created, Oct. 19, 2017, is named FOTH039_ST25.txt and is 10.6 KB in size.The present invention relates to inhibitors of histone deacetylase 11 (HDAC11) useful in the treatment of certain diseases and/or disorders, including diseases and disorders associated with cell proliferation (e.g., cancers) and/or diseases and ...

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21-03-2019 дата публикации

METHODS USING HDAC11 INHIBITORS

Номер: US20190084946A1
Принадлежит:

The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases. 1. A method of inhibiting or reducing proliferation of cancer cells in a patient in need thereof , comprising administering a HDAC11 inhibitor to the patient.2. The method of claim 1 , wherein at least some of the cancer cells express one or more stem cell markers.3. The method of claim 2 , wherein the stem cell marker is a gene amplification of SOX2 and/or activation of STAT3.4. The method of any one of - claim 2 , wherein the cancer is a lung cancer claim 2 , a hematological cancer claim 2 , a breast cancer claim 2 , a squamous cell carcinoma claim 2 , esophageal cancer claim 2 , gastric cancer claim 2 , breast cancer or adenocarcinoma of the lung.5. The method of any one of - claim 2 , wherein the HDAC11 inhibitor is a siRNA claim 2 , a shRNA claim 2 , an antibody agent claim 2 , or a chemical compound.6. The method of wherein the chemical compound is a small molecule that is at least 10-fold selective for the inhibition of HDAC11 over one or more other histone deacetylase isoforms.7. A method of treating cancer in a patient in need thereof claim 5 , comprising administering to a patient an effective amount of a HDAC11 inhibitor claim 5 , wherein one or more cancer cells in the patient exhibit stem cell-like properties.8. The method of claim 7 , wherein the one or more cancer cells is associated with gene amplification of a marker for a cancer stem cell.9. The method of or claim 7 , wherein the one or more cancer cells is associated with a gene amplification of SOX2.10. The method of any one of - claim 7 , wherein the cancer is esophageal squamous cell carcinoma claim 7 , oral squamous cell carcinoma claim 7 , lung claim 7 , squamous cell carcinoma claim 7 , lung adenocarcinoma claim 7 , non-small cell lung cancer claim 7 , small cell lung cancer or sinonasal cancer.11. ...

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30-03-2017 дата публикации

ANTIBACTERIAL AGENTS

Номер: US20170088549A1
Принадлежит:

Antibacterial compounds of formula (I) are provided: 2. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,{'sup': 3G', '3G, '(3) —CR═CR—C≡C—, and'}{'sup': 3G', '3G, '(4) —C≡C—CR═CR—.'}3. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,(3) —CH═CH—C≡C—, and(4) —C≡C—CH═CH—.4. A compound of wherein G is —C≡C—.5. A compound of wherein G is —C≡C—C≡C—.6. A compound of wherein G is —CH═CH—C≡C—.8. A compound of wherein G is —C≡C—CH═CH—.10. A compound of any one of - wherein X is —(C═O)NR—.11. A compound of wherein X is —(C═O)NH—.12. A compound of any one of - wherein Q is —(C═O)N(R claim 10 ,R).13. A compound of wherein Q is —(C═O)NHOH.14. A compound of any one of - wherein n is 0.15. A compound of any one of - wherein Ris H.16. A compound of any one of - wherein Y is substituted or unsubstituted aryl.17. A compound of wherein Y is substituted or unsubstituted phenyl.18. A compound of wherein Y is unsubstituted phenyl.19. A compound of any one of - wherein A is selected from the group consisting of:{'sub': 2', '0-4', '2', '0-4, 'sup': 1a', '2a', '3a, '(1) —(CH)C(R,R)(CH)OR,'}{'sub': 2', '0-4, 'sup': 1a', '2a', '4a', '5a, '(2) —(CH)C(R,R)N(R,R), and'}{'sup': 1a', '2a, '(3) —CH(R,R).'}20. A compound of wherein A is selected from the group consisting of —CH(CH) claim 19 , —CHOH claim 19 , —CHNH claim 19 , —CHCHOH claim 19 , —CHCHNHand —C(CH)OH.21. A compound of wherein A is —C(CH)NH.22. A compound of any one of - wherein A is selected from the group consisting of:{'sub': 3', '10, '(1) substituted or unsubstituted C-C-cycloalkyl,'}(2) substituted or unsubstituted aryl,(3) substituted or unsubstituted heterocyclyl, and(4) substituted or unsubstituted heteroaryl.26. A compound of any one of - wherein D is present.27. A compound of wherein D is substituted or unsubstituted heteroaryl.29. A compound of wherein D is substituted or unsubstituted aryl.30. A compound of wherein D is substituted or ...

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19-03-2020 дата публикации

RILUZOLE PRODRUGS AND THEIR USE

Номер: US20200085794A1
Принадлежит: Biohaven Therapeutics Ltd.

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. 2. The method according to claim 1 , wherein Ris H.3. The method according to claim 1 , wherein the compound is selected from the group consisting of(S)-2-amino-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)propanamide;(R)-2-amino-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)propanamide;(S)-2-amino-3-methyl-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)butanamide;(R)-2-amino-3-methyl-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)butanamide;(S)-2-amino-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)-3-phenylpropanamide;(R)-2-amino-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)-3-phenylpropanamide;(S)-2-amino-4-methyl-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)pentanamide;(R)-2-amino-4-methyl-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)pentanamide;(S)-2-amino-3-hydroxy-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)propanamide;(R)-2-amino-3-hydroxy-N-(2-(methyl(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)amino)-2-oxoethyl)propanamide;2-(2-aminoacetamido)-N-methyl-N-(2-oxo-2-((6-(trifluoromethoxy)benzo[d]thiazol-2-yl)amino)ethyl)acetamide;or a pharmaceutically ...

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19-06-2014 дата публикации

Hybrid Compounds And Methods Of Making And Using The Same

Номер: US20140171438A1
Автор: Haizhong Tang, Wenxi Pan
Принадлежит: Cellceutix Corp

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

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07-04-2016 дата публикации

TREATMENT OF CANCER/INHIBITION OF METASTASIS

Номер: US20160096812A1
Принадлежит:

Substances and methods are disclosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole. 1. Ranolazine for reducing or preventing metastatic behaviour in VGSC expressing cancer.2. Ranolazine according to claim 1 , wherein the cancer is breast cancer.3. Ranolazine according to claim 1 , wherein the cancer is prostate cancer.4. Riluzole for reducing or preventing metastatic behaviour in VGSC expressing cancer without directly killing the cancer cells.5. Riluzole according to claim 4 , wherein the cancer is breast cancer.6. Riluzole according to claim 4 , wherein the cancer is prostate cancer.7. A substance for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part.8. A substance according to claim 7 , having said effect in breast cancer.9. A substance according to claim 7 , having said effect in prostate cancer.10. A substance according to claim 7 , having said effect without killing the cells.11. A substance according to claim 7 , having said effect without substantially affecting proliferation.12. Ranolazine according to claim 1 , in a dosage level corresponding to the range 1 μmol to 10 μmol.13. Riluzole according to claim 4 , in a dosage level corresponding to the range 1 μmol of 10 μmol.14. A method of reducing or preventing metastatic behaviour in VGSC expressing cancer comprising administering ranolazine.15. A method according to claim 14 , wherein the cancer is breast cancer.16. A method according to claim 14 , wherein the cancer is prostate cancer.17. A method of reducing ...

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01-04-2021 дата публикации

BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF

Номер: US20210094925A1
Принадлежит:

The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans. 3. The method of claim 1 , wherein administering comprises orally administering.4. The method of claim 1 , wherein administering comprises transdermally administering.5. The method of claim 1 , wherein administering comprises administering a therapeutically effective amount of a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof.6. The method of claim 5 , wherein claim 5 ,the pharmaceutical composition is an oral pharmaceutical formulation; andadministering comprises orally administering.7. The method of claim 5 , wherein claim 5 ,the pharmaceutical composition is a transdermal pharmaceutical formulation; andadministering comprises transdermally administering.8. The method of claim 1 , wherein the disease or disorder is anxiety.9. The method of claim 1 , wherein the disease or disorder is ataxia.10. The method of claim 1 , wherein the disease or disorder is attention deficit disorder.11. The method of claim 1 , wherein the disease or disorder is cancer.12. The method of claim 1 , wherein the disease or disorder is bipolar disorder.13. The method of claim 1 , wherein the disease or disorder is dementia.14. The method of claim 1 , wherein the disease or disorder is depression.15. The method of claim 1 , wherein the disease or disorder is drug addiction.16. The method of claim 1 , wherein the disease or disorder is eating disorder.17. The method of claim 1 , wherein the disease or disorder is Huntington's disease.18. The method of claim 1 , wherein the disease or disorder is obsessive- ...

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05-04-2018 дата публикации

POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC PRODUCT

Номер: US20180093958A1
Автор: OKUYAMA Kumi, Sakamoto Kei
Принадлежит: ZEON CORPORATION

A compound represented by a formula (IIa) is provided. In formula (IIa), Yto Yrepresent —O—, —S—, —O—C(═O)—, —C(═O)—O— or the like, Gand Grepresent a divalent linear aliphatic group having 1 to 20 carbon atoms or the like, Zand Zrepresent an alkenyl group having 2 to 10 carbon atoms or the like, Arepresents a group represented by a formula (II), wherein X represents an oxygen atom, a sulfur atom or the like, D represents an alkylene group having 1 to 20 carbon atoms or the like, Arepresents a trivalent aromatic group or the like, Aand Arepresent a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms or the like, Aand Arepresent a divalent aromatic group having 4 to 30 carbon atoms or the like, Qrepresents an alkyl group having 1 to 6 carbon atoms or the like, and m and n are 0 or 1. 2. The compound according to claim 1 , wherein D is a substituted or unsubstituted alkylene group having 1 to 20 carbon atoms that optionally includes —O— claim 1 , —S— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , —O—C(═O)—O— claim 1 , or —C(═O)— claim 1 , provided that a case where the alkylene group includes two or more contiguous —O— or —S— is excluded.3. The compound according to claim 1 , wherein Ais a substituted or unsubstituted trivalent benzene ring group claim 1 , or a substituted or unsubstituted trivalent naphthalene ring group.4. The compound according to claim 1 , wherein each of Yto Yis independently a chemical single bond claim 1 , —O— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , or —O—C(═O)—O—.5. The compound according to claim 1 , wherein each of Zand Zis independently CH═CH— claim 1 , CH═C(CH)— claim 1 , or CH═C(Cl)—.6. The compound according to claim 1 , wherein each of Gand Gis independently a substituted or unsubstituted divalent aliphatic group having 1 to 12 carbon atoms that optionally includes —O— claim 1 , —O—C(═O)— claim 1 , —C(═O)—O— claim 1 , or —C(═O)— claim 1 , provided that a case where the aliphatic group includes two or more ...

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14-04-2016 дата публикации

BENZOTHIAZOLE DERIVATIVE AND ANTI-TUMOR USE THEREOF

Номер: US20160102066A1
Принадлежит: YANTAI UNIVERSITY

The present invention relates to a benzothiazole derivative of formula 1 or a pharmaceutically acceptable salt thereof and a process for preparation thereof. The present invention also relates to a pharmaceutical composition comprising the compounds and the use of the compounds in the preparation of an anti-tumor medicament. 17-. (canceled)9. The method according to claim 8 , wherein the cancer is selected from breast cancer claim 8 , lung cancer claim 8 , prostate cancer and oral epithelium carcinoma. The present invention belongs to the field of organic synthesis, and relates to an anti-tumor drug benzothiazole derivative and use thereof.With the extension of human life, cancer emerged as the leading cause of death in recent years. “2012 Chinese Cancer Registry Annual Report” shows that about 3.5 million of new cancer cases occur and about 2.5 million of persons die of cancer each year in China. Lung cancer has a highest incidence among malignant tumors in China, followed by stomach cancer, colorectal cancer, liver cancer and esophageal cancer. Cancer has become the leading cause of human death in China.With regard to treatment of cancers, scientists have carried out a tot of research work. New anticancer drugs are discovered continuously Currently, there are more than 20 kinds of cancers, cure rates of which are above 30%. The research of drug action mechanism at sub-cellular and molecular level largely expands the research in the application of anti-cancer drugs. The rapid development of cell kinetics, pharmacokinetics and immunological research makes the drug screening, dose titeration, and determination of route of administration become more and more mature. Now treatments of malignant tumors have achieved very good therapeutic effects by means of combination therapy, high-dose intermittent therapy, adjuvant chemotherapy, and therapy in combination with traditional Chinese medicine. Nowadays the means for treatment of cancer are mainly surgery therapy, ...

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16-04-2015 дата публикации

Cyclopentylacrylamide derivative

Номер: US20150105581A1

A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R 1 and R 2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C 1 to C 6 alkyl group, a C 1 to C 6 alkoxy group, a C 1 to C 6 alkylsulfanyl group, a C 1 to C 6 alkylsulfinyl group, a C 1 to C 6 alkylsulfonyl group, or a C 1 to C 6 alkoxy-C 1 to C 6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).

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12-04-2018 дата публикации

Mixture of polymerizable compound and method of producing the same

Номер: US20180099921A1
Принадлежит: Zeon Corp

Disclosed is a mixture containing compound (I) and polymerizable compound (II) wherein compound (I) accounts for 50 mol % or more of the entire mixture and 1,4-cyclohexanedicarboxylic acid accounts for less than 5 mol % of the entire mixture; a method of producing the mixture which includes reacting in a water-immiscible organic solvent 1,4-cyclohexanedicarboxylic acid dichloride with compound (IV) in the presence of a base, and washing the obtained reaction solution with a weakly acidic buffer solution; etc. The disclosure provides mixtures useful for low-cost production of polymerizable compounds which have low melting points suitable for practical use, show superior solubility to general-purpose solvents, can be produced at low costs, and allow for provision of optical films capable of uniform polarized light conversion over a wide wavelength range, and methods of producing the mixtures. where A represents hydrogen, methyl group or chlorine, and n represents an integer of 1 to 20.

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04-04-2019 дата публикации

BENZOTHIAZOL COMPOUNDS AND METHODS USING THE SAME FOR TREATING NEURODEGENERATIVE DISORDERS

Номер: US20190100500A1
Принадлежит:

The present disclosure provides a compound of general Formula (I) having c-abl kinase inhibitory activity or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound, and a method useful to treat or prevent neurodegenerative diseases using the compound. 2. The compound of claim 1 , wherein{'sup': 1', '1, 'sub': 1', '3', '1', '3', '1', '3, 'Ris cyclopropyl, cyclobutyl, or 3- or 4-membered heterocyclyl, wherein Ris optionally substituted with one or more groups selected from the group consisting of halo, C-Calkyl, C-Chydroxyalkyl and C-Chaloalkyl;'}{'sup': 2', '3, 'sub': 1', '3', '1', '3', '3', '3, 'Rand Rare independently —H, halo, C-Calkyl, C-Calkoxy, —CF, or —OCF;'}{'sup': 4', '4, 'sub': 1', '3', '2', '3', '2', '3', '1', '3', '1', '3', '1', '3', '2', 'a', 'b', 'a', 'b', 'a', 'a', 'b', 'a', 'b', 'a', 'a', 'a', 'a', 'b', 'a', 'a', 'a', 'b', 'a, 'Ris aryl, heteroaryl, cycloalkyl, heterocyclyl, or heteroalkyl, wherein Ris optionally substituted with one or more groups selected from the group consisting of halo, hydroxyl, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Chaloalkyl, mono-C-Calkylamino, di-C-Calkylamino, —NO, —NRR, —NRC(═O)R, —NRC(═O)NRR, —NRC(═O)OR, —OR, —CN, —C(═O)R, —C(═O)OR, —C(═O)NRR, —OC(═O)R, —OC(═O)OR, —OC(═O)NRR, —SR, azetidinyl, oxetanyl, tetrahydrofuranyl, furanyl, pyrrolidinyl, pyrrolyl, pyrazolyl, thiophenyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, furazanyl, oxadiazolyl, thiadiazolyl, phenyl, tetrahydropyranyl, pyranyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, piperidinyl, piperazinyl, morpholinyl and thiomorpholinyl, and'}{'sub': a', 'b', '1', '3', '1', '3, 'Rand Rare independently —H, halo, amino, C-Calkyl, or C-Chaloalkyl.'}3. The compound of claim 1 , wherein{'sub': 1', '1', '3', '1', '3', '1', '3, 'Ris cyclopropyl or cyclobutyl, optionally substituted with one or more selected from the group consisting of fluoro, C-Calkyl, C-Chydroxyalkyl and C-Cfluoroalkyl,'}{'sup': 2', '3, 'sub': 1', '3', '3, 'Rand ...

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23-04-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DEGENERATIVE DISORDERS

Номер: US20150111932A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing neurological degenerative disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of Parkinson's disease (PD), restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, sexual dysfunction, amyotrophic lateral sclerosis (ALS), also known as Lou Gehrig's disease and depression. 3. A Pharmaceutical composition comprising claim 1 , a compound of and a pharmaceutically acceptable carrier.4. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 3 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 3 , delayed release or sustained release claim 3 , transmucosal claim 3 , syrup claim 3 , topical claim 3 , parenteral administration claim 3 , injection claim 3 , subdermal claim 3 , oral solution claim 3 , rectal administration claim 3 , buccal administration or transdermal administration.6. The pharmaceutical composition of claim 4 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration or transdermal administration.7. Compounds and compositions of are formulated for the treatment of ...

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19-04-2018 дата публикации

NOVEL INHIBITORS OF TRANSFORMING GROWTH FACTOR KINASE AND METHODS OF USE THEREOF

Номер: US20180105500A1
Принадлежит:

The present invention provides novel inhibitors of TAK1 and methods of using such compounds to treat various diseases. 117-. (canceled)19. The compound according to claim 18 , or a tautomer or salt thereof claim 18 , wherein X is NRand Ris propyl.20. The compound according to claim 18 , or a tautomer or salt thereof claim 18 , wherein Ris OCHor Br.21. The compound according to claim 18 , or a tautomer or salt thereof claim 18 , wherein Ris OCHor NHCH.22. The compound according to claim 18 , or a tautomer or salt thereof claim 18 , wherein Ris H claim 18 , CH claim 18 , OCHor Cl.24. A pharmaceutical composition comprising the compound according to claim 18 , or a tautomer or pharmaceutically acceptable salt thereof claim 18 , and a pharmaceutically acceptable carrier.29. The method of claim 27 , wherein the disease is selected from inflammatory conditions claim 27 , autoimmune conditions claim 27 , and cancer.30. The method of claim 29 , wherein the disease is selected from breast cancer claim 29 , colorectal cancer claim 29 , leukemia claim 29 , neurofibrodomas claim 29 , or non-small cell lung cancer.31. The method of claim 29 , wherein the disease is selected from rheumatoid arthritis claim 29 , osteoarthritis claim 29 , gout claim 29 , psoriatic arthritis claim 29 , ankylosing spondylitis claim 29 , diabetes claim 29 , Sjogren's syndrome claim 29 , lupus claim 29 , inflammatory bowel disease claim 29 , and psoriasis.32. The method of claim 31 , wherein the inflammatory bowel disease is Crohn's disease or ulcerative colitis.33. The method of claim 27 , wherein the disease is malaria.34. (canceled)35. (canceled)36. (canceled)37. A kit comprising the compound of claim 18 , or tautomer or a pharmaceutically acceptable salt thereof claim 18 , and instructions for treating a disease modulated by transforming growth factor β activated kinase 1 (TAK1).38. A kit comprising the pharmaceutical composition of claim 25 , and instructions for treating a disease modulated by ...

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27-04-2017 дата публикации

WATER-SOLUBLE TRIAZABUTADIENES

Номер: US20170114033A1
Принадлежит:

Water-soluble triazabutadiene molecules and methods for producing and using such compounds. The triazabutadiene molecules may be more labile at pH levels below physiological pH, such as pH 7, pH 6, pH 5, etc. The triazabutadiene molecules and compounds may be used for depositing diazonium salt and/or cargo in a pH-sensitive manner. The triazabutadiene molecules may alternatively be cleaved in reducing conditions or as a light-catalyzed reaction. The compounds herein may be used for delivery of drugs, as part of detection systems, or for other applications such as underwater adhesive applications. 2. The triazabutadiene molecule of claim 1 , wherein the tri-substituted aryl group of Ycomprises a NHS-ester moiety; an oligonucleotide; a peptide; a fluorescence quencher; a pro-fluorophore; an alkyne; a triazene; or a combination thereof; and the optionally substituted aryl of Zcomprises a NHS-ester moiety; an oligonucleotide; a peptide; a fluorescence quencher; a pro-fluorophore; an alkyne; a triazene; a biologically active acid labile compound; a prodrug comprising a phenolic functional group; an aldehyde; an amine; an aminooxy; a halogen; or a combination thereof.3. The triazabutadiene molecule of claim 1 , wherein Xcomprises a moiety of the formula —R-Q claim 1 , wherein Rcomprises Calkylene claim 1 , and Qcomprises sulfate claim 1 , phosphate claim 1 , or a quaternary ammonium cation.4. The triazabutadiene molecule of claim 1 , wherein the molecule has half-life of at least 12 hours in a pH 7.4 buffer.56-. (canceled)7. The triazabutadiene molecule of claim 1 , wherein the triazabutadiene molecule is adapted to undergo an irreversible reaction yielding a diazonium species and a cyclic guanidine species.8. The triazabutadiene molecule of claim 7 , wherein the reaction occurs at a reaction rate claim 7 , and said reaction rate is increased when the triazabutadiene molecule is subjected to a lowered pH.9. The triazabutadiene molecule of claim 8 , wherein the lowered pH ...

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03-05-2018 дата публикации

APELIN RECEPTOR AGONISTS AND METHODS OF USE THEREOF

Номер: US20180118698A1
Принадлежит:

Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions. 3. The compound of claim 2 , wherein A and B are taken together and joined to form cyclopropyl claim 2 , cyclopentyl or cyclohexyl.5. A compound selected from the group consisting of: methyl 4-{[N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)carbamoyl]methyl}benzoate claim 2 , methyl 3-{[N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)carbamoyl]methyl}benzoate claim 2 , 3-{[N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)carbamoyl]methyl}benzoic acid claim 2 , 4-{[N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)carbamoyl]methyl}benzoic acid claim 2 , 2-{[N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)carbamoyl]methyl}benzoic acid claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]propanamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]butanamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]-3-methylbutanamide claim 2 , N-(5 claim 2 ,6-di methoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]-2-(4-methoxyphenoxy)acetamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[3-(N claim 2 ,N-dimethylcarbamoyl)phenyl]acetamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(N claim 2 ,N-dimethylcarbamoyl)phenyl]acetamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-{4-[(dimethylamino)sulfonyl]phenyl}acetamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]-4-methoxybutanamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-3-cyclopropyl-2-[4-(ethylsulfonyl)phenyl]propanamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[4-(ethylsulfonyl)phenyl]-3-phenylpropanamide claim 2 , N-(5 claim 2 ,6-dimethoxybenzothiazol-2-yl)-2-[2-(N claim 2 ,N-dimethylcarbamoyl)phenyl]acetamide claim 2 , N-(5 claim 2 ,6- ...

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07-05-2015 дата публикации

SYNTHESIS OF AMINE SUBSTITUTED 4,5,6,7-TETRAHYDROBENZOTHIAZOLE COMPOUNDS

Номер: US20150126745A1
Принадлежит:

The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process. 2. The process of claim 1 , further comprising the steps of:{'sub': '(HOTs)', 'a) forming a mixture comprising the compound of formula I, IPA and water, and heating the mixture to about 78° C.;'}b) cooling the mixture to about 5° C.; and{'sub': '(HOTs)', 'c) isolating the solid compound of formula Iformed during step b.'}3. The process of claim 1 , wherein Ris hydrogen.4. The process of claim 1 , wherein Ris Calkyl.5. The process of claim 4 , wherein Ris n-propyl.6. The process of claim 1 , wherein the solvent is a mixture of acetonitrile and water claim 1 , a mixture of IPA and water claim 1 , a mixture of acetonitrile and IPA claim 1 , or a mixture of acetonitrile claim 1 , IPA and water.7. The process of claim 6 , wherein the solvent is a mixture of acetonitrile and water.8. The process of claim 7 , wherein water is present from about 0% to about 10% by weight in the mixture of acetonitrile and water.9. The process of claim 8 , wherein the ratio of the mixture of acetonitrile to water is about 39:1 wt/wt.10. The process of claim 6 , wherein the solvent is a mixture of acetonitrile claim 6 , IPA and water.11. The process of claim 10 , wherein water is present in an amount from about 0% to about 10% by weight of the mixture claim 10 , acetonitrile is present in an amount from about 0% to about 50% by weight of the mixture claim 10 , and IPA is present in an amount from about 0% to about 50% by weight of the mixture.12. The process of claim 1 , wherein the stereochemistry of the carbon atom to which the —NR(R) moiety is ...

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16-04-2020 дата публикации

TETRALIN AND INDANE DERIVATIVES AND USES THEREOF

Номер: US20200115333A1
Принадлежит: Roche Palo Alto LLC

The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, RR, Rand Rare as defined herein. 2. The method of wherein m is 0 claim 1 , s is 1 claim 1 , Ris 3-fluoro claim 1 , Ris hydrogen and Ris acetyl claim 1 , aminocarbonyl or methylsulfonyl or a pharmaceutically acceptable salt.3. The method of wherein the compound is (R)-[6-(3-fluoro-benzenesulfonyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-naphthalen-1-ylmethyl]-urea or a pharmaceutically acceptable salt.4. The method of claim 3 , wherein the central nervous system disease state is depression.5. The method of claim 3 , wherein the central nervous system disease state is a memory disorder.6. The method of claim 3 , wherein the central nervous system disease state is Parkinson's disease. This Application is a Continuation of U.S. application Ser. No. 15/597,478, filed May 17, 2017, which is a Continuation of U.S. application Ser. No. 14/531,465, filed Nov. 3, 2014, which is a Continuation U.S. application Ser. No. 13/314,525, filed on Dec. 8, 2011, which is a Continuation of U.S. application Ser. No. 11/985,459, filed on Nov. 15, 2007, which is a continuation of U.S. patent application Ser. No. 11/315,706, filed Dec. 21, 2005, which claims the benefit under Title 35 U.S.C. 119(e) of U.S. Provisional Patent Application Ser. No. 60/638,030, filed Dec. 21, 2004, the disclosure of which is incorporated herein by reference in its entirety.This invention relates to substituted indane and tetralin compounds, and associated compositions, methods for use as therapeutic agents, and methods of preparation thereof.The actions of 5-hydroxytryptamine (5-HT) as a major modulatory neurotransmitter in the brain are mediated through a number of receptor families termed 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HTS, 5-HT6, and 5-HT7. Based on a high level of 5-HT6 receptor mRNA in the brain, it has been stated that the 5-HT6 receptor may play a role in the pathology and treatment of ...

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16-04-2020 дата публикации

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

Номер: US20200115374A1
Принадлежит:

Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases such as chronic viral infection, chronic bacterial infections, cancer, sepsis or a neurological disorder. 2. A compound or salt according to wherein one of Rand Ris H and the other is CH.3. A compound or salt according to wherein Ris COH.4. A compound or salt according to wherein Ris a 5 or 6-membered heterocycle or heteroaryl containing 1 to 3 heteroatoms selected from N claim 1 , and S.5. A compound or salt according to wherein Ris a pyridine claim 4 , thiadiazole claim 4 , pyrimidine claim 4 , pyrazine claim 4 , pyridazine claim 4 , triazol claim 4 , or thiazol.6. A compound or salt according to wherein Ris unsubstituted or substituted with 1 or 2 substituents selected from the group consisting of F claim 5 , Cl claim 5 , CN claim 5 , OCH claim 5 , CF claim 5 , cyclopropyl claim 5 , CONH claim 5 , CHCHOCH claim 5 , and CHOCH.7. A compound or salt according to wherein Ris a 6-membered heterocycle containing an O or a N.8. A compound or salt according to wherein Ris unsubstituted or substituted on the heteroatom by a substituent selected from the group consisting of halogen claim 7 , OH claim 7 , Calkyl; OCalkyl claim 7 , C(O)Ccycloalkyl claim 7 , C(O)Calkyl-O—Calkyl; C(O)Calkyl; C(O)—O—Calkyl claim 7 , and a 4 to 6-membered heterocycle or heteroaryl containing 1 to 4 heteroatoms selected from N claim 7 , S claim 7 , and O claim 7 , wherein said heterocycle or heteroaryl may optionally be substituted by 1 substituent selected from the group consisting of halogen claim 7 , Ccycloalkyl claim 7 , CHOH claim 7 , C(O)NH claim 7 , CN claim 7 , CHOCalkyl claim 7 , Calkyl optionally substituted by 1-3 halogens.9. A compound or salt according to wherein Ris unsubstituted or substituted on the heteroatom with OH or OCH.11. A pharmaceutical ...

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10-05-2018 дата публикации

METHODS USING HDAC11 INHIBITORS

Номер: US20180127386A1
Принадлежит:

The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases. 149.-. (canceled)50. A method of treating cancer in a patient in need thereof , comprising administering to a patient an effective amount of a HDAC11 inhibitor.51. The method of claim 50 , wherein one or more cancer cells in the patient exhibit stem cell-like properties.52. The method of claim 50 , wherein the cancer is a hematological cancer.53. A method of treating a patient having a myeloproliferative disorder claim 50 , comprising administering to the patient a HDAC11 inhibitor and a second therapeutic agent.54. The method of claim 53 , wherein the second therapeutic agent is a JAK2 inhibitor.55. The method of claim 53 , wherein the myeloproliferative disorder is resistant to a JAK2 inhibitor.56. The method of claim 53 , wherein the second therapeutic agent is a hedgehog pathway inhibitor.57. The method of claim 50 , wherein the patient has received a first line therapy claim 50 , and any cancer cells surviving from the first line therapy are reduced or eliminated after treatment with the HDAC11 inhibitor. This application claims the benefit of U.S. Provisional Application Ser. No. 62/410,766 filed Oct. 20, 2016, 62/410,767 filed Oct. 20, 2016, and 62/410,768 filed Oct. 20, 2016, the contents of all of which are hereby incorporated by reference in their entirety.This application contains a Sequence Listing which has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety. Said ASCII copy, created, Oct. 19, 2017, is named FOTH039_ST25.txt and is 10.6 KB in size.The present invention relates to inhibitors of histone deacetylase 11 (HDAC11) useful in the treatment of certain diseases and/or disorders, including diseases and disorders associated with cell proliferation (e.g., cancers) and/or diseases and disorders associated with ...

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10-05-2018 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20180127388A1
Принадлежит:

Compounds disclosed herein including compounds of formula I′: 2. The compound of wherein the configuration of the —OC(CH)group as shown in formula I′ is the (S) stereochemistry.3. The compound of wherein Ris selected from aryl claim 1 , heterocycle and heteroaryl claim 1 , wherein any aryl claim 1 , heterocycle and heteroaryl of Ris optionally substituted with one or more halo or (C-C)alkyl.4. The compound wherein Ris selected from aryl and heterocycle claim 1 , wherein any aryl and heterocycle of Ris optionally substituted with one or more chloro claim 1 , fluoro or methyl.7. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle claim 1 , wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.8. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.9. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl or pyrazinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.10. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.11. The compound of wherein A and B together form a ...

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23-04-2020 дата публикации

REMOVAL OF SENESCENCE-ASSOCIATED MACROPHAGES

Номер: US20200123127A1
Принадлежит:

In various aspects and embodiments provided are compounds, compositions and methods relating to aging, senescent cells (SCs) and/or senescence associate macrophages (SAMs). In certain aspects and embodiments provided are compounds and compositions that selectively kill or reprogram senescent cells (SCs) and or senescence associate macrophages (SAMs) and associated methods. In some embodiments, the compounds compositions and methods treat or reverse aging organism Normal tissue and/or age-related diseases. 48-. (canceled)9. A method for removing senescence-associated macrophages (SAMs) in a mixed population of cells comprising SAMs , the method comprising selectively inducing SAM cell death in said mixed population of cells.10. The method of claim 9 , wherein SAM cell death is selectively induced by delivering to said mixed population of cells an agent which is selectively ingested by SAMs such that SAMs are removed from said mixed population.1118-. (canceled)19. A method of treating or preventing an age-related disease in a mammal claim 9 , the method comprising administering an agent capable of reducing claim 9 , eradicating claim 9 , or reprogramming senescence-associated macrophages (SAMs) in a mammal claim 9 , thereby treating said disease.20. The method of claim 19 , wherein said disease is cancer claim 19 , age-related disease claim 19 , tobacco-related disease claim 19 , or skin wrinkles.21. (canceled)22. A method for identifying an agent that selectively removes SAMs from a mixed population of cells comprising SAMs claim 19 , said method comprising (a) contacting a plurality of candidate agents with a mixed population of SAMs and senescent cells; and (b) determining selective removal of SAMs from said mixed population claim 19 , thereby identifying said agent.23. (canceled)24. A method of reprogramming senescence-associated macrophages (SAMs) in a mixed population of cells claim 19 , the method comprising selectively reversing or reducing the SAM phenotype ...

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07-08-2014 дата публикации

2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient

Номер: US20140221411A1

The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.

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07-08-2014 дата публикации

ALPHA HELIX MIMETIC COMPOSITIONS FOR TREATING CANCER AND OTHER CBP/CATENIN-MEDIATED DISEASES AND CONDITIONS

Номер: US20140221657A1
Принадлежит: Prism BioLab Corporation

Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. 136.-. (canceled)38. (canceled) This application is a divisional of U.S. patent application Ser. No. 13/124,104, filed May 20, 2011 and entitled ALPHA HELIX MIMETIC COMPOSITIONS FOR TREATING CANCER AND OTHER CBP/CATENIN-MEDIATED DISEASES AND CONDITIONS (which will issue on Apr. 8, 2014 as U.S. Pat. No. 8,691,819), which is the United States national phase of PCT/JP2009/06085, filed Oct. 14, 2009 and entitled ALPHA HELIX MIMETICS IN THE TREATMENT OF CANCER, which claims the benefit of Provisional U.S. Patent Application No. 60/105,088, filed Oct. 14, 2008 and entitled ALPHA HELIX MIMETICS IN THE TREATMENT OF CANCER, all of which are incorporated herein by reference in their entirety.The present invention relates generally to alpha-helix mimetic structures and to a compound relating thereto. The invention also relates to applications in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics.Recently, non-peptide compounds have been developed which more closely mimic the secondary structure of reverse-turns found in biologically active proteins or peptides. For example, U.S. Pat. No. 5,440,013 to Kahn and published PCT applications nos. WO94/03494, WO01/00210A1, and WO01/16135A2 to Kahn each disclose conformationally constrained, non-peptidic compounds, which mimic the three-dimensional structure of reverse-turns. In addition, U.S. Pat. No. 5,929,237 and its continuation-in-part U.S. Pat. No. 6,013,458, both to Kahn, disclose conformationally constrained ...

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26-05-2016 дата публикации

Polymerizable compound, polymerizable composition, polymer, and optically anisotropic material

Номер: US20160145363A1
Автор: Kei Sakamoto, Kumi Okuyama
Принадлежит: Zeon Corp

The present invention relates to a polymerizable compound represented by a formula (I). The present invention provides a polymerizable compound, a polymerizable composition, a polymer, and an optically anisotropic article that are capable of obtaining an optical film having a low melting point, having excellent solubility, capable of being manufactured at low cost, and capable of uniform polarized light conversion across a broad wavelength region. [In formula: Y 1 to Y 6 are independently a chemical single bond, —O—, —O—C(═O)—, —C(═O)—O— etc.; G 1 and G 2 are independently a divalent C1-C20 aliphatic group etc.; Z 1 and Z 2 are independently C2-C10 alkenyl group that is substituted with a halogen atom etc.; A x is a C2-C30 organic group that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring; A y is a hydrogen atom, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C3-C12 cycloalkyl group etc.; A 1 is a trivalent aromatic group etc.; A 2 and A 3 are independently a divalent C6-C30 aromatic group etc.; and Q 1 is a hydrogen atom, or a C1-C6 alkyl group etc.]

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10-06-2021 дата публикации

NOVEL COMPOUND FOR INHIBITING NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE AND COMPOSITION CONTAINING SAME

Номер: US20210171513A1
Принадлежит:

The present invention relates to a novel compounds for inhibiting nicotinamide phosphoribosyltransferase (NamPT), a composition comprising the same, and various uses thereof. 130.-. (canceled)32. The method of claim 31 , wherein the compound is selected from the group of following compounds:1) N-(4-(benzo[d]oxazol-2-yl)benzyl)nicotinamide;2) N-(4-(6-methylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;3) N-(4-(6-methylbenzo[d]oxazol-2-yl)benzyl)benzamide;4) N-(4-(5-methylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;5) N-(4-(5-ethylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;6) N-(4-(6-ethylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;7) N-(4-(5-isopropylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;8) N-(4-(6-(tert-butyl)benzo[d]oxazol-2-yl)benzyl)nicotinamide;9) N-(4-(5-methoxybenzo[d]oxazol-2-yl)benzyl)nicotinamide;10) N-(4-(6-chlorobenzo[d]oxazol-2-yl)benzyl)nicotinamide;11) N-(4-(6-nitrobenzo[d]oxazol-2-yl)benzyl)nicotinamide;12) N-(4-(5-phenylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;13) N-(4-(naphtho[2,3-d]oxazol-2-yl)benzyl)nicotinamide;14) N-(4-(oxazolo[5,4-b]pyridin-2-yl)benzyl)nicotinamide;15) N-(4-(oxazolo[4,5-c]pyridin-2-yl)benzyl)nicotinamide;16) N-(4-(oxazolo[4,5-b]pyridin-2-yl)benzyl)nicotinamide;17) N-(4-(benzo[d]thiazol-2-yl)benzyl)nicotinamide; and18) N-(4-(5-isopropylbenzo[d]oxazol-2-yl)phenyl)nicotinamide. The present invention relates to novel compounds for inhibiting nicotinamide phosphorbosyltransferase (NamPT) and a composition comprising the same and various uses thereof.NAD+ (nicotinamide adenine dinucleotide) is a coenzyme that plays an important role in many physiologically essential processes (Ziegkel, M. 267, 1550-1564, 2000). NAD is essential for several signaling pathways including mono-ADP-ribosylation in both the immune system and G-protein-coupled receptor signaling among other poly ADP-ribosylation in DNA repair, and is also essential for the activity of Sirtuin deacetylase (Garten, A. et al., 20, 130-138, 2008).Nicotinamide phosphoribosyltransferase (NamPT) ...

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02-06-2016 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20160152582A1
Принадлежит:

Compounds of formula I′: 2. The compound of wherein A is phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.3. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.4. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.5. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.6. The compound of wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , pyrimidinyl claim 1 , indazolyl claim 1 , pyrazolopyridine or benzimidazolyl claim 1 , wherein any ...

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21-08-2014 дата публикации

INTERMEDIATE FOR MANUFACTURE OF POLYMERIZABLE COMPOUND AND PROCESS FOR MANUFACTURE THEREOF

Номер: US20140235857A1
Принадлежит: ZEON CORPORATION

The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ais an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ais a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Aand Aoptionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.). According to the invention, provided are a novel compound that makes it possible to produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band can be inexpensively produced in high yield by utilizing the compound according to one aspect of the invention as an intermediate for producing the polymerizable compound, and a method for producing thereof. 2. The compound according to claim 1 , wherein a total number of aromatic ring π-electrons included in Aand Ais 24 or less.3. The compound according to claim 1 , wherein Q is a hydrogen atom.4. The compound according to claim 1 , wherein Ais a hydrogen atom claim 1 , or a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms.6. The method according to claim 5 , wherein the solvent is an alcohol-based solvent.7. The method according to claim 6 , wherein the alcohol-based solvent is an alcohol-based solvent having 1 to 4 carbon atoms.8. The compound according to claim 2 , wherein Q is a hydrogen atom.9. The compound according to claim 2 , wherein Ais a hydrogen atom claim 2 , or a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms.10. The compound according to claim 3 , wherein Ais a hydrogen ...

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28-08-2014 дата публикации

ZWITTERIONIC AZO DYESTUFFS FOR COLOURING KERATIN-INCLUDING FIBRES

Номер: US20140237735A1
Принадлежит: Henkel AG & Co. KGaa

The invention relates to agents for coloring keratinic fibers, in particular human hair, including in a cosmetic carrier at least one compound of the formula (I). The structures the of the general formula (I) have a heterocycle A which bears a quaternary nitrogen atom and thus a positive charge. The invention furthermore relates to the use of these novel azo dyes in agents for coloring hair and to the dyes themselves. 2. The agent of claim 1 , wherein the agent comprises at least one compound of the formula (I) claim 1 , in which A denotes one of structures (II) claim 1 , (III) claim 1 , (IV) claim 1 , (VI) claim 1 , (VII) claim 1 , (IX) claim 1 , (X) claim 1 , (XII) or (XIII).3. The agent of claim 1 , further comprising at least one compound of the formula (I) claim 1 , in which X denotes N—R3 and Y denotes (CH)with n equal to 2 or 3.4. The agent of claim 1 , further comprising at least one compound of the formula (I) claim 1 , in which X denotes N—R3 and R3 denotes a C-Calkyl group claim 1 , a C-Calkenyl group claim 1 , a methyl claim 1 , or an ethyl group.5. The agent of claim 1 , further comprising at least one compound of the formula (I) claim 1 , in which R1 and R2 mutually independently denote hydrogen claim 1 , a C-Calkyl group claim 1 , a C-Calkoxy group claim 1 , a halogen claim 1 , or a hydrogen.6. The agent of claim 1 , further comprising at least one compound of the formula (I) selected from:2-(methyl{4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)ethyl sulfate;2-(ethyl{4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)ethyl sulfate;3-(methyl{4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)propyl sulfate;3-(ethyl{4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)propyl sulfate;2-(methyl{3-methyl-4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)-ethyl sulfate;3-(ethyl{3-methyl-4-[(3-methyl-1,3-thiazol-3-ium-2-yl)diazenyl]phenyl}amino)propyl sulfate;2-[{4-[(1,3-dimethyl-1H-imidazol-3-ium-2-yl)diazenyl]phenyl}( ...

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22-09-2022 дата публикации

BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF

Номер: US20220298127A1
Принадлежит:

The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans. 6. The method of claim 1 , wherein administering comprises orally administering.7. The method of claim 1 , wherein administering comprises transdermally administering.8. The method of claim 1 , wherein administering comprises administering a therapeutically effective amount of a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof.9. The method of claim 8 , wherein claim 8 ,the pharmaceutical composition is an oral pharmaceutical formulation; andadministering comprises orally administering.10. The method of claim 8 , wherein claim 8 ,the pharmaceutical composition is a transdermal pharmaceutical formulation; andadministering comprises transdermally administering.11. The method of claim 1 , wherein the disease or disorder is anxiety.12. The method of claim 1 , wherein the disease or disorder is Parkinson's disease.13. The method of claim 1 , wherein the disease or disorder is Alzheimer's disease. This application is a continuation of U.S. application Ser. No. 17/083,877 filed on Oct. 29, 2020, now allowed, which is a continuation of U.S. application Ser. No. 16/791,243, filed on Feb. 14, 2020, which issued as U.S. Pat. No. 10,882,832, which is divisional of U.S. application Ser. No. 16/587,571, filed on Sep. 30, 2019, which issued as U.S. Pat. No. 10,640,476, which claims the benefit under 35 U.S.C. § 111(a) of PCT International Application No. PCT/CN2017/078873, filed on Mar. 30, 2017, which is incorporated by reference in its entirety.The present invention relates to the field of ...

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23-05-2019 дата публикации

METHOD OF PRODUCING POLYMERIZABLE COMPOUND, HALOGENATED COMPOUND, AND MIXTURE

Номер: US20190152934A1
Принадлежит: ZEON CORPORATION

Provided is a method of producing a high-purity polymerizable compound in an industrially advantageous manner. The production method is a method of producing a polymerizable compound indicated by the following formula (I). The method includes subjecting a composition containing a halogenated compound indicated by the following formula (II) to a dehydrohalogenation reaction in an organic solvent in the presence of an aqueous layer containing a basic compound. 3. The method according to claim 2 , wherein{'sup': 1', '2, 'Xand Xare each a chlorine atom.'}5. The method according to claim 4 , wherein{'sup': '1', 'Xis a chlorine atom.'}6. The method according to claim 4 , wherein{'sup': '1', 'FGis a hydroxy group.'}8. The method according to claim 7 , whereinthe halogenated compound indicated by formula (IV) constitutes a proportion of at least 0.01 mass % and not more than 5 mass % among a total of the halogenated compound indicated by formula (IV) and the compound indicated by formula (V).10. The method according to claim 9 , wherein{'sup': '1', 'Xis a chlorine atom.'}11. The method according to claim 9 , wherein{'sup': '2', 'FGis a carboxyl group, and'}b is 1.13. The method according to claim 12 , whereinthe halogenated compound indicated by formula (VI) constitutes a proportion of at least 0.01 mass % and not more than 5 mass % among a total of the halogenated compound indicated by formula (VI) and the compound indicated by formula (VII).1627-. (canceled) The present disclosure relates to a method of producing a polymerizable compound that can be used in production of an optical film that enables uniform polarized light conversion over a wide wavelength region, and also to a halogenated compound and a mixture that can be used in this production method.Examples of retardation plates used in various devices such as flat panel displays include quarter-wave plates that convert linearly polarized light to circularly polarized light and half-wave plates that perform 90° ...

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08-06-2017 дата публикации

SYNTHESIS OF AMINE SUBSTITUTED 4,5,6,7-TETRAHYDROBENZOTHIAZOLE COMPOUNDS

Номер: US20170158648A1
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The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process. 154-. (canceled)56. The process of claim 55 , wherein Ris hydrogen.57. The process of claim 55 , wherein Ris Calkyl.58. The process of claim 57 , wherein Ris n-propyl.59. The process of claim 55 , wherein the solvent is a mixture of acetonitrile and water claim 55 , a mixture of IPA and water claim 55 , a mixture of acetonitrile and IPA claim 55 , or a mixture of acetonitrile claim 55 , IPA and water.60. The process of claim 59 , wherein the solvent is a mixture of acetonitrile and water.61. The process of claim 60 , wherein water present is about 0% to about 10% by weight in the mixture of acetonitrile and water.62. The process of claim 61 , wherein the ratio of the mixture of acetonitrile to water is about 37:1 wt/wt.63. The process of claim 59 , wherein the solvent is a mixture of acetonitrile claim 59 , IPA and water64. The process of claim 63 , wherein the water present is about 0% to about 10% by weight of the mixture claim 63 , the acetonitrile present is about 0% to about 50% by weight of the mixture claim 63 , and the IPA present is about 0% to about 50% by weight of the mixture.65. The process of claim 55 , wherein the stereochemistry of the carbon atom to which the —NR(R) moiety is attached is in the (R) configuration.66. The process of claim 55 , wherein the base is triethylamine claim 55 , DIPEA claim 55 , pyridine or DBU.67. The process of claim 66 , wherein the base is DIPEA.68. The process of claim 55 , wherein the ratio of IPA to water in step a) is about 2.3:1 v/v to about 4.25:1 v/v.69. The process of ...

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08-06-2017 дата публикации

SYNTHESIS OF CHIRALLY PURIFIED SUBSTITUTED BENZOTHIAZOLE DIAMINES

Номер: US20170158649A1
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Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzotiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzotiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzotiazole diamines are provided herein. 1134-. (canceled)136. The process of claim 135 , wherein the steps of heating in step a. claim 135 , and reacting in step b. claim 135 , are carried out from about 55° C. to about 100° C.137. The process of claim 135 , wherein the steps of heating in step a. claim 135 , and reacting in step b. claim 135 , are carried out from about 60° C. to about 95° C.138. The process of claim 135 , wherein the alkyl halide is a propyl halide selected from an n-propyl bromide claim 135 , n-propyl chloride claim 135 , n-propyl iodide claim 135 , and combinations thereof.139. The process of claim 138 , wherein the propyl chloride is n-propyl chloride.140. The process of claim 135 , wherein the alkyl sulfonate is n-propyl tosylate.141. The process of claim 135 , wherein the chirally purified substituted 4 claim 135 ,5 claim 135 ,6 claim 135 ,7-tetrahydro-benzothiazole diamine is at least greater than about 97% chirally pure.142. The process of claim 135 , wherein the chirally purified substituted 4 claim 135 ,5 claim 135 ,6 claim 135 ,7-tetrahydro-benzothiazole diamine is at least greater than about 99% chirally pure.143. The process of claim 135 , wherein the chirally purified substituted 4 claim 135 ,5 claim 135 ,6 claim 135 ,7-tetrahydro-benzothiazole diamine is at least about 99.9% chirally pure.144. The process of claim 135 , wherein the chemical purity of the substituted 4 claim 135 ,5 claim 135 ,6 claim 135 ,7-tetrahydro-benzothiazole diamine is greater than about 98%.145. The process of claim 135 , wherein the chemical purity of the substituted 4 claim 135 ,5 claim 135 ,6 claim 135 ,7-tetrahydro- ...

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08-06-2017 дата публикации

ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME

Номер: US20170158707A1
Принадлежит:

The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject. 2. The compound of claim 1 , wherein Gis N.3. The compound of claim 1 , wherein Gis NH.4. The compound of claim 1 , wherein Gis CH claim 1 , Gis NH claim 1 , and Gand Gare CH.5. The compound of claim 1 , wherein Gis N and G claim 1 , G claim 1 , and Gare CH.6. The compound of claim 1 , wherein Gis N claim 1 , Gand Gare CH claim 1 , and Gis NH.7. The compound of claim 1 , wherein Gis N claim 1 , Gand Gare CH claim 1 , and Gis NH.8. The compound of claim 1 , wherein Gis CH claim 1 , Gand Gare NH claim 1 , and Gis CH.11. The compound of any one of - claim 1 , wherein Xis present and selected from the group consisting of halogen claim 1 , —CN claim 1 , or —OMe.12. The compound of any one of - claim 1 , wherein Xis —OMe.13. The compound of any one of - claim 1 , wherein Xis present and selected from the group consisting of H claim 1 , halogen claim 1 , —OH claim 1 , —CN claim 1 , Calkoxy claim 1 , and CF.14. The compound of any one of - claim 1 , wherein Xis CFand n is 1.17. The compound of claim 16 , wherein Xis selected from the group consisting of H claim 16 , —OMe claim 16 , ethyl claim 16 , —OH claim 16 , and —OCHPh.18. The compound of or claim 16 , wherein Ris selected from the group consisting of H claim 16 , acetyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , isobutyl claim 16 , tert-butyl claim 16 , pentyl claim 16 , isopentyl claim 16 , and —COCHPh.19. The compound of any one of - claim 16 , wherein Xis present and independently for each occurrence H claim 16 , —OMe claim 16 , —NO claim 16 , —COMe claim 16 , methyl claim 16 , —OC(O)Me claim ...

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14-05-2020 дата публикации

MIXTURE OF POLYMERIZABLE COMPOUND AND METHOD OF PRODUCING THE SAME

Номер: US20200148622A1
Принадлежит: ZEON CORPORATION

Disclosed is a mixture containing compound (I) and polymerizable compound (II) wherein compound (I) accounts for 50 mol % or more of the entire mixture and 1,4-cyclohexanedicarboxylic acid accounts for less than 5 mol % of the entire mixture; a method of producing the mixture which includes reacting in a water-immiscible organic solvent 1,4-cyclohexanedicarboxylic acid dichloride with compound (IV) in the presence of a base, and washing the obtained reaction solution with a weakly acidic buffer solution; etc. The disclosure provides mixtures useful for low-cost production of polymerizable compounds which have low melting points suitable for practical use, show superior solubility to general-purpose solvents, can be produced at low costs, and allow for provision of optical films capable of uniform polarized light conversion over a wide wavelength range, and methods of producing the mixtures. 5. The method of claim 3 , wherein the buffer solution is a buffer solution having a pH of 5.0 to 6.0.6. The method of claim 3 , wherein the buffer solution is a mixed buffer solution of acetic acid and sodium acetate claim 3 , or a mixed buffer solution of potassium hydrogen phthalate and sodium hydroxide.7. The method of claim 3 , wherein the water-immiscible organic solvent is an organic solvent having a Hildebrand solubility parameter of 14.0 to 22.0 (MPa).8. The method of claim 3 , further comprising claim 3 , after washing with the weakly acid buffer solution claim 3 , cooling an obtained organic layer to 5° C. or lower to precipitate polymerizable compound (II) claim 3 , and removing the precipitate. This application is a divisional application of U.S. application Ser. No. 15/560,646 filed Sep. 22, 2017, which is a National Stage Application of PCT/JP2016/060580 filed Mar. 30, 2016, which claims priority based on Japanese Patent Application No. 2015-072950 filed Mar. 31, 2015. The disclosures of the prior applications are hereby incorporated by reference herein in their ...

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