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Небесная энциклопедия

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

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Применить Всего найдено 3296. Отображено 195.
10-07-2011 дата публикации

НОВЫЕ БИОЛОГИЧЕСКИ АКТИВНЫЕ ПЕПТИДЫ И ИХ НОВОЕ ПРИМЕНЕНИЕ

Номер: RU2423375C2

Изобретение относится к применению биологически активного пептида, который представляет собой аминокислотную последовательность SEQ ID No.1, для получения лекарственного средства для модуляции, по меньшей мере, одного из следующих состояний: усталости, уровня запаса гликогена в печени и уровня молочной кислоты в крови. 30 табл.

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11-08-2020 дата публикации

ПЕПТИДНЫЕ МАКРОЦИКЛЫ ПРОТИВ ACINETOBACTER BAUMANNII

Номер: RU2729609C2

Изобретение относится к новым соединениям формулы (I), а также к фармацевтическим композициям на их основе и применению. Технический результат: получены новые соединения, которые могут быть применимы в качестве лекарственных средств для лечения заболеваний и инфекций, вызванных. 8 н. и 14 з.п. ф-лы, 5 табл., 255 пр.(I) ...

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27-04-2007 дата публикации

ИНГИБИТОРЫ ВИРУСА ГЕПАТИТА С

Номер: RU2298001C2

FIELD: organic chemistry, biochemistry, virology. SUBSTANCE: invention relates to inhibitors of hepatitis C virus of the general formula (I): wherein R 1 means (C 1 -C 8 )-alkyl, (C 3 -C 7 )-cycloalkyl; m means 2; n means 1; R 2 means hydrogen atom (H), (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl wherein each of them is optionally substituted with halogen atom; R 3 means (C 1 -C 8 )-alkyl optionally having the following substitute: (C 6 -C 10 )-aryl, (C 7 -C 14 )-alkylaryl, (C 1 -C 6 )-alkoxy-, carboxy-, hydroxy-, (C 7 -C 14 )-alkylaryloxy-group, (C 2 -C 6 )-alkyl ester, (C 8 -C 15 )-alkylaryl ester, (C 3 -C 7 )-alkenyl, (C 3 -C 7 )-cycloalkyl or (C 4 -C 10 )-alkylcycloalkyl wherein cycloalkyl or alkylcycloalkyl have optionally (C 1 -C 6 )-alkyl as a substitute; Y means H or (C 1 -C 6 )-alkyl under condition that if R 4 and R 5 means H then Y means H; B means H, R 4 -(C=O)-, R 4 O(C=O)-, R 4 -N(R 5 )-C(=O)- wherein R 4 means: (i) (C 1 -C 10 )-alkyl optionally having the following substitute: phenyl, 1-3 halogen atoms, hydroxy-group, -OC(O)-(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-group; (ii) (C 3 -C 7 )-cycloalkyl, (C 3 -C 7 )-cycloalkoxy-group or (C 4 -C 10 )-alkylcycloalkyl; (iii) (C 6 -C 10 )-aryl or (C 7 -C 16 )-arylalkyl wherein each of them is optionally substituted with halogen atom; (iv) Het; (v) bicyclo[1.1.1]pentane, or (vi) -C(O)O-(C 1 -C 6 )-alkyl; R 5 means H, (C 1 -C 6 )-alkyl optionally substituted with (C 1 -C 6 )-alkoxy-group under condition that R 4 means (C 1 -C 10 )-alkyl; X means oxygen atom (O), sulfur atom (S), -SO 2 , -CH 2 O or -NH; R' means Het or (C 6 -C 10 )-aryl optionally substituted with R a wherein R a means (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-group, (C 3 -C 7 )-cycloalkyl, halogen atom, (C 1 -C 6 )-alkyl, -CF 3 , dihalogen-(C 1 -C 6 )-alkoxy-, cyano-group, halogen atom, thioalkyl, hydroxy-group, di-(C 1 -C 6 )-alkyl-(alkoxy)-amine, (C 6 -C 10 )-aryl, (C 7 -C 14 )-alkylaryl or 5-7-membered monocyclic heterocycle under condition that X-R ...

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20-10-2010 дата публикации

ИНГИБИТОРЫ IAP

Номер: RU2401840C2
Принадлежит: ДЖЕНЕНТЕК, ИНК. (US)

Настоящее изобретение относится к новым ингибиторам IAP, которые могут использоваться в качестве терапевтических агентов для лечения злокачественных опухолей, где соединения имеют общую формулу I, ! в которой X, Y, A, R1, R2, R3, R4, R4', R5, R5', R6 и R6' имеют такие же значения, которые указаны в описании изобретения. 2 н. и 14 з.п. ф-лы. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 401 840 (13) C2 (51) МПК C07K 5/08 (2006.01) A61K 38/06 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2007104028/04, 05.07.2005 (24) Дата начала отсчета срока действия патента: 05.07.2005 (43) Дата публикации заявки: 10.08.2008 C 2 2 4 0 1 8 4 0 R U (85) Дата перевода заявки PCT на национальную фазу: 02.02.2007 (86) Заявка PCT: US 2005/023564 (05.07.2005) (87) Публикация PCT: WO 2006/014361 (09.02.2006) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) ИНГИБИТОРЫ IAP (57) Реферат: Настоящее изобретение относится к новым ингибиторам IAP, которые могут использоваться в качестве терапевтических агентов для лечения злокачественных опухолей, где соединения имеют общую формулу I, в которой X, Y, A, R1, R2, R3, R4, R4', R5, R5', R6 и R6' имеют такие же значения, которые указаны в описании изобретения. 2 н. и 14 з.п. ф-лы. Ñòð.: 1 ru C 2 (56) Список документов, цитированных в отчете о поиске: RU 2000126298 А, 27.10.2002. CHAI JIJIE ET AL "STRUCTURAL AND BIOCHEMICAL BASIS OF. APOPTOTIC ACTIVATION BY SMAC/DIABLO", NATURE, NATURE. PUBLISHING GROUP, 2000, v.406, no 6798, 855-862. LIU Z ET AL "STUCTURAL BASIS FOR BINDING OF SMAC/DIABLO TO THE XIAP BIR3 DOMAIN", NATURE, NATURE PUBLISHING GROUP, 2000, v.408,пo 6815, 1004-1008. (73) Патентообладатель(и): ДЖЕНЕНТЕК, ИНК. (US) 2 4 0 1 8 4 0 (45) Опубликовано: 20.10.2010 Бюл. № 29 R U (30) Конвенционный приоритет: 02.07.2004 US 60/585,501 (72) ...

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27-08-1999 дата публикации

ПРОИЗВОДНЫЕ 1,5-БЕНЗОДИАЗЕПИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЙ ИХ ФАРМАЦЕВТИЧЕСКИЙ СОСТАВ

Номер: RU2135486C1

Производные 1,5-бензодиазепина формулы I, где Х=Н, R1 - радикал формулы II или NR4R5; R2 - индол, бензофуран, тиофен, бензотиофен, индолин, хинолин или 4-оксобензопиран; фенил, возможно замещенный галогеном, карбокси, амино или диметиламино, лобо NHR11, R11 - 7-индазолил; R3- Н, C1-6-алкил, С3-6-циклоалкил или фенил (значения других радикалов см. в п.1 формулы изобретения), а также их физиологически приемлемые соли и сольваты проявляют агонистическую активность по отношению к рецепторам ХЦК-А, что позволяет указанным соединениям регулировать функционирование гормонов гастрина и холецисткинина (ХЦК) у млекопитающих. 3 с. и 8 з.п. ф-лы, 9 табл.

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10-06-2005 дата публикации

ЛИГАНДЫ МЕЛАНОКОРТИНОВЫХ РЕЦЕПТОРОВ

Номер: RU2003134019A
Принадлежит:

... 1. Соединение, включая все его энантиомерные и диастереомерные формы и фармацевтически приемлемые соли, причем указанное соединение имеет формулу: где А представляет конформационно ограниченную кольцевую систему, выбранную из группы, включающей: a) неароматические карбоциклические кольца; b) ароматические карбоциклические кольца; c) неароматические гетероциклические кольца; d) ароматические гетероциклические кольца; где указанные кольца содержат от 5 до 8 атомов; W представляет боковой фрагмент, имеющий формулу: где R выбран из группы, включающей: a) неароматические карбоциклические кольца; b) ароматические карбоциклические кольца; c) неароматические гетероциклические кольца; d) ароматические гетероциклические кольца; указанные кольца содержат от 3 до 12 атомов; J выбран из группы, включающей: i) -[C(R”)d]k-, где каждый R” независимо представляет водород, C1-C12 линейный или разветвленный алкил, -SUB, два фрагмента R”, взятые вместе с атомом кислорода, могут образовывать карбонильный фрагмент ...

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10-08-2005 дата публикации

ИНГИБИТОРЫ ВИРУСА ГЕПАТИТА С

Номер: RU2004137480A
Принадлежит:

... 1. Соединение, имеющее формулу где (a) R1 обозначает C1-8 алкил, C3-7 циклоалкил или C4-10 алкилциклоалкил; (b) m обозначает 1 или 2; (c) n обозначает 1 или 2; (d) R2 обозначает Н, C1-6 алкил, C2-6 алкенил или C3-7 циклоалкил, каждый из которых, необязательно, замещен галогеном; (e) R3 обозначает C1-8 алкил, необязательно имеющий следующий заместитель: галоген, циано, амино, C1-6 диалкиламино, C6-10 арил, C7-14 алкиларил, C1-6 алкокси, карбокси, гидрокси, арилокси, C7-14 алкиларилокси, C2-6 алкиловый сложный эфир, C8-15 алкилариловый сложный эфир; C3-12 алкенил, C3-7 циклоалкил или C4-10алкилциклоалкил, где циклоалкил или алкилциклоалкил, необязательно, имеют заместитель: гидрокси, C1-6 алкил, C2-6 алкенил или C1-6 алкокси; или R3, вместе с углеродным атомом, к которому он присоединен, образует C3-7 циклоалкильную группу, необязательно замещенную C2-6 алкенилом; (f) Y обозначает Н, фенил, замещенный нитрогруппой, пиридил, замещенный нитрогруппой или C1-6 алкил, необязательно имеющий в качестве ...

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10-05-2011 дата публикации

НОВЫЕ ПЕПТИДЫ КАК ИНГИБИТОРЫ NS3-СЕРИНПРОТЕАЗЫ ВИРУСА ГЕПАТИТА C

Номер: RU2404189C9

FIELD: medicine. SUBSTANCE: invention relates to novel peptide compounds, which possess ability to inhibit protease of hepatitis C virus (HCV), their pharmaceutical compositions and application of compounds for obtaining medication for diseases associated with HCV. EFFECT: improvement of compound properties. 48 cl, 6 tbl, 65 ex 2404189 С9 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ С07К С07К ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (11) < аа зд (13) (51) МПК 5/02 (2006.01) 7/02 (2006.01) АбТК 38/55 АбЙР 31/14 (2006.01) (2006.01) 12) СКОРРЕКТИРОВАННОЕ ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ Примечание: библиография отражает состояние при переиздании (21)(22) Заявка: 2004125279/04, 16.01.2003 (24) Дата начала отсчета срока действия патента: 16.01.2003 Приоритет(ы): (30) Конвенционный приоритет: 18.01.2002 05 10/052,386 (43) Дата публикации заявки: 19.01.2006 Бюл. № 1 (45) Опубликовано: 20.11.2010 (15) Информация о коррекции: Версия коррекции №1 (ТС2) (48) Коррекция опубликована: 10.05.2011 Бюл. № 13 (56) Список документов, цитированных в отчете о поиске: ВО 93036735 А, 27.04.1996. \О 01/40262 АТ, 07.06.2001. \О 01/74768 АТ, 11.11.2001. \О 02/08244 АТ, 31.01.2002. (85) Дата начала рассмотрения заявки РСТ на национальной фазе: 18.08.2004 (86) Заявка РСТ: 0$ 03/01430 (16.01.2003) (87) Публикация заявки РСТ: УГО 03/062265 (31.07.2003) Адрес для переписки: 105064, Москва, а/я 88, пат.пов. В.П.Квашнину (72) Автор(ы): САКСЕНА Энил К. (05), ГИРИЯВАЛЛАБХН Вийюр М. (0$), ЛАВИ Реймонд Дж. (05$), ЯО Эдвин (05), БЕННЕТТ Френк (05), МАК КОРМИК Джинпинг Л. (0$), ВАНГ Хейян (05), ПАЙК Рассел И. (0$). БОУДЖЕН Стефани Л. (05), ЧАН Тин-Яу (05), ЛИУ Ю-Тсунг (05), ЖУ Жаонинг (05), НИОРОУДЖ Джордж Ф. (0$), ЭРЕСЕППЕН Эшок (0$), ПЕРИК Тиял (0$), ГЕНГЮЛИ Эшит К. (05), ЧЕН Кевин Кс. (05), ВЕНКЕТРЕМЕН Срикент (05), ВЕККЕЙРО Хенри А. (0$), ПИНТО Патрик А. (05), СЕНТХЕНЕМ Бама (05), КЕМП Скотт Джефри (05), ЛЕВИ Одайл Эстер (05), ЛИМ-УИЛБИ Маргарит (03), ТЕЙМУРА Сьюзан И. (0$), ...

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10-01-2006 дата публикации

ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ ДЛЯ СИНТЕЗА АНТАГОНИСТА РИЛИЗИНГ-ФАКТОРА ЛЮТЕИНИЗИРУЮЩЕГО ГОРМОНА (LHRH), СПОСОБ ИХ ПОЛУЧЕНИЯ И СПОСОБ ПОЛУЧЕНИЯ АНТАГОНИСТА LHRH

Номер: RU2004119964A
Принадлежит:

... 1. Способ получения трипептида, включая его соль, формулы (I) или (IX) при котором осуществляют следующие последовательные стадии получения (I), на которых: (а) осуществляют взаимодействие Boc-D-4ClPhe-OH с HONSu с образованием Boc-D-4ClPhe-OSu (VII); (б) осуществляют взаимодействие Boc-D-4ClPhe-OSu (VII) с H-D-3Pal-ОН с образованием Boc-D-4ClPhe-D-3Pal-OH (VIII); (в) осуществляют взаимодействие Boc-D-4ClPhe-D-3Pal-OH (VIII) с Boc-D-2Nal-OSu, полученным путем осуществления взаимодействия Boc-D-2Nal-OH с HONSu, с образованием Boc-D-2Nal-D-4ClPhe-D-3Pal-OH (IX); (г) осуществляют взаимодействие Boc-D-2Nal-D-4ClPhe-D-3Pal-OH (IX) с уксусной кислотой с образованием Ac-D-2Nal-4ClPhe-D-3Pal-OH (I); или последовательные стадии с (а) по (в) для получения (IX). 2. Способ получения антагониста рилизинг - фактора лютеинизирующего гормона (luteinizing hormone-releasing hormone, LHRH) или его фармацевтически приемлемой соли, при котором осуществляют сочетание трипептида Ac-D-2Nal-D-4ClPhe-D-3Pal-OH ( ...

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10-04-2008 дата публикации

НОВЫЕ СОЕДИНЕНИЯ, ДЕЙСТВУЮЩИЕ КАК ИНГИБИТОРЫ СЕРИНОВОЙ ПРОТЕАЗЫ NS3 ВИРУСА ГЕПАТИТА С

Номер: RU2006134002A

1. Соединение или энантиомеры, стереоизомеры, ротамеры, таутомеры или рацематы указанного соединения или фармацевтически приемлемая соль, сольват или сложный эфир указанного соединения, причем указанное соединение имеет общую структуру, представленную формулой Iформула Iгде Rпредставляет собой Н, OR, NRRили CHRR, где R, Rи Rмогут быть одинаковыми или различными, причем каждый из них независимо выбран из группы, состоящей из Н, алкил-, алкенил-, алкинил-, арил-, гетероалкил-, гетероарил-, циклоалкил-, гетероцикпил-, арилалкил- и гетероарилалкил;А и М могут быть одинаковыми или различными, причем каждый из них независимо выбран из R, OR, NHR, NRR', SR, SOR и галогена; или А и М связаны друг с другом таким образом, что радикал,приведенный выше в формуле I, образует либо трех-, четырех-, шести-, семи- или восьмичленный циклоалкил, либо четырех-восьмичленный гетероциклил, либо шести-десятичленный арил, либо пяти-десятичленный гетероарил;Е представляет собой С(Н) или C(R);L представляет собой С(Н), C(R), СНC(R) или C(R)CH;R, R', Rи Rмогут быть одинаковыми или различными, причем каждый из них независимо выбран из группы, состоящей из Н, алкил-, алкенил-, алкинил-, циклоалкил-, гетероалкил-, гетероциклил-, арил-, гетероарил-, (циклоалкил)алкил-, (гетероциклил)алкил-, арил-алкил- и гетероарил-алкил-; или альтернативно R и R' в NRR' связаны друг с другом таким образом, что NRR' образует четырех-восьми-членный гетероциклил;a Y выбран из следующих радикалов:илигде G представляет собой NH или О; и R, R, R, Rи Rмогут быть одинаковыми или различными, причем каждый из них независимо выбран из группы, состоящей из Н, алкила, гетероалкила, алкенила, гетероалкенила, алкинила, гетероалкинила, цикло� ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2006 134 002 (13) A (51) ÌÏÊ C07K 5/06 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006134002/04, 24.02.2005 (71) Çà âèòåëü(è): ØÅÐÈÍà ...

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27-04-2008 дата публикации

СПОСОБ ПОЛУЧЕНИЯ МИКРОЦИКЛИЧЕСКИХ СОЕДИНЕНИЙ

Номер: RU2006136084A
Принадлежит:

... 1. Способ получения соединения формулы (I) в которой Q обозначает заместитель формулы олефиновая группа, присоединенная к циклопропильному кольцу, находится в син-конфигурации относительно группы А как это представлено приведенной структурой, W обозначает N; L0 выбирают из Н, -ОН, -ОСН3 и -N(СН3)2; один из L1 и L2 обозначает -СН3, -F, -Cl или -Br, а другой из L1 и L2 обозначает Н или оба L1 и L2 обозначают Н; R2 обозначает ; или где R6 обозначает NH-R7 или NH-C(O)-R7, где R7 независимо обозначает С1-С6алкил или С3-С6циклоалкил; R3 обозначает NH-C(O)-OR10, где R10 обозначает C1-С6алкил или С3 -С6циклоалкил; R4 обозначает Н или C1-С6алкил; D обозначает 5-атомную насыщенную алкиленовую цепь; а А обозначает карбоновую кислоту или ее фармацевтически приемлемую соль или эфир; который включает циклизацию диенового соединения формулы (IX) в присутствии приемлемого катализатора с получением соединения формулы (I) и, когда А обозначает защищенную карбоксильную группу, необязательное удаление защитной ...

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20-05-2010 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ЛИЗОБАКТИНА

Номер: RU2008144662A
Принадлежит:

... 1. Способ получения циклических депсипептидов следующей формулы (I) ! ! в которой R1 обозначает Н или CH3, ! в которой R2 обозначает водород, C3-C6-циклоалкил, C5-C6-циклоалкенил, C3-C6-циклоалкилметил, 5-7-членный гетероциклилметил, метил, этил, н-пропил, изопропил, 1-метилпроп-1-ил, 2-метилпроп-1-ил, 2,2-диметилпроп-1-ил, 1,1-диметилпроп-1-ил, 1-этилпроп-1-ил, 1-этил-1-метилпроп-1-ил, н-бутил, 2-метилбут-1-ил, 3-метилбут-1-ил, 1-этилбут-1-ил, трет-бутил, 4-метилпент-1-ил, н-гексил, алкенил или арил, ! в которой R2 могут содержать 0, 1, 2 или 3 заместителя, независимо друг от друга выбранных из группы, включающей галоген, гидроксигруппу, аминогруппу, цианогруппу, триметилсилил, алкил, алкоксигруппу, бензилоксигруппу, C3-C6-циклоалкил, арил, 5-10-членный гетероарил, алкиламиногруппу, ариламиногруппу, алкилкарбониламиногруппу, арилкарбониламиногруппу, алкилкарбонил, алкоксикарбонил, арилкарбонил и бензилоксикарбониламиногруппу, ! где арил и гетероарил, в свою очередь, могут содержать 0, ...

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10-06-2011 дата публикации

ПРОИЗВОДНЫЕ ТЕТРАГИДРОКАРБАЗОЛА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И НАБОР НА ИХ ОСНОВЕ, СПОСОБ ЛЕЧЕНИЯ И/ИЛИ ПРОФИЛАКТИКИ ФИЗИОЛОГИЧЕСКИХ И/ИЛИ ПАТОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ, ОПОСРЕДОВАННЫХ РЕЦЕПТОРАМИ, СОПРЯЖЕННЫМИ С G-БЕЛКОМ, ИЛИ ФИЗИОЛОГИЧЕСКИХ И/ИЛИ ПАТОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ, НА КОТОРЫЕ МОЖНО ВОЗДЕЙСТВОВАТЬ МОДУЛЯЦИЕЙ ЭТИХ РЕЦЕПТОРОВ ПОСРЕДСТВОМ ВЫШЕНАЗВАННЫХ ПРОИЗВОДНЫХ

Номер: RU2009143990A
Принадлежит:

... 1. Производные тетрагидрокарбазола, охватываемые общей структурной формулой (I) ! ! (А) V, W независимо друг от друга выбраны из группы, состоящей из =O, =S, =S+-O-, геминально связанные Н2; ! R1, R1* - когда присутствуют - вместе независимо образуют =O, =S или =S+-O- или независимо оба представляют собой водород; ! R2, R3 независимо друг от друга выбраны из группы, состоящей из ! (i) водорода, алкила, (С9-С30)алкила, циклоалкила, циклоалкилалкила, гетероциклила, гетероциклилалкила, арила, арилалкила, гетероарила, гетероарилалкила, -F, -Cl, -Вr, -I, - CN, -СF3, -N3, -NH2, -NHX1, -NX2X3, -NO2, -ОН, =O, -ОСF3, -SH, -O-SO3Н, -ОР(O)(ОН)2, -СНО, -СООН, -C(O)NH2, -SО3Н, -Р(O)(ОН)2, -С(O)-Х4, -С(O)O-Х5, -C(O)NH-X6, -C(O)NX7X8, -O-Х9, -O(-Х10-O)а-Н (а=1, 2, 3, 4, 5), -O(-Х11-O)b-Х12 (b=1, 2, 3, 4, 5), -OC(O)-X13, -OC(O)-O-X14,-OC(O)-NHX15, -O-C(O)-NX16X17, -OP(O)(OX18)(OX19), -OSi(X20)(X21)(X22), -OS(O2)-X23, -NHC(O)-NH2, -NHC(O)-X24, -NX25C(O)-X26, -NH-C(O)-O-X27, -NH-C(O)-NH-X28, -NH-C(O)-NX29X30 ...

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09-08-1989 дата публикации

Healing wounds in horses

Номер: GB0002213060A
Принадлежит:

The healing of a variety of wounds in horses is enhanced by administering to the wound a therapeutically effective amount of a composition comprising Glycyl-L-Histidyl-L-Lysine: Copper (II) or a derivative thereof in combination with a physiologically acceptable carrier or diluent. The derivatives are of the formula: [X-L-Histidyl-L-Lysine-CO-R]: Cu (II) where R is C 1-18 alkyl, C 6-12 aryl, C 1-18 alkoxy, L-Prolyl-L-Valyl-L-Phenylalany-L-Valine or L-Valyl-L-Phenylalanyl-L-Valine, and where X is Glycyl, Glycyl-L-Alanyl, Glycyl-L-Seryl, Glycyl-L-Valyl or Glycyl-Glycyl.

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10-03-2010 дата публикации

Theraputic compounds and their use

Номер: GB0201001070D0
Автор:
Принадлежит:

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17-04-1996 дата публикации

Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use

Номер: GB0009603227D0
Автор:
Принадлежит:

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28-02-2007 дата публикации

Antiviral compounds

Номер: AP0200703895A0
Принадлежит:

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19-02-1996 дата публикации

1,5 Benzodiazepine derivatives.

Номер: AP0000000462A
Принадлежит:

Compounds of the general formula ...

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14-09-2012 дата публикации

Antiviral compounds

Номер: AP0000002461A
Принадлежит:

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30-04-1994 дата публикации

1,5 Benzodiaze pine derivatives

Номер: AP0009400635A0
Автор:
Принадлежит:

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30-04-1994 дата публикации

1,5 Benzodiaze pine derivatives

Номер: AP0009400634A0
Автор:
Принадлежит:

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31-08-2007 дата публикации

Peptidic compounds

Номер: AP2007004093A0
Принадлежит:

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18-03-2013 дата публикации

Peptidic compounds

Номер: AP0000002616A
Принадлежит:

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28-02-2007 дата публикации

Antiviral compounds

Номер: AP2007003895A0
Принадлежит:

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31-12-2014 дата публикации

Inhibitors of hepatitis C virus

Номер: AP2014008166A0
Принадлежит:

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07-10-1997 дата публикации

1,5 Benzodiazepine derivatives having cck and/or gastrin antagonistic activity

Номер: OA0000010236A
Принадлежит:

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31-12-2014 дата публикации

Inhibitors of hepatitis C virus

Номер: AP0201408166A0
Принадлежит:

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28-02-2007 дата публикации

Antiviral compounds

Номер: AP0200703895D0
Принадлежит:

Подробнее
31-08-2007 дата публикации

Peptidic compounds

Номер: AP0200704093D0
Принадлежит:

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30-04-1994 дата публикации

1,5 Benzodiaze pine derivatives

Номер: AP0009400635D0
Автор:
Принадлежит:

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31-12-2014 дата публикации

Inhibitors of hepatitis C virus

Номер: AP0201408166D0
Принадлежит:

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30-04-1994 дата публикации

1,5 Benzodiaze pine derivatives

Номер: AP0009400634D0
Автор:
Принадлежит:

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31-08-2007 дата публикации

Peptidic compounds

Номер: AP0200704093A0
Принадлежит:

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25-01-1979 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW PEPTID DERIVATIVES

Номер: AT0000354655B
Автор:
Принадлежит:

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15-03-2011 дата публикации

FORMULATIONS OF BORIC ACID CONNECTIONS

Номер: AT0000501157T
Принадлежит:

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15-06-1979 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN PEPTID- DERIVATEN

Номер: ATA500877A
Автор:
Принадлежит:

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15-08-1979 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW PEPTID DERIVATIVES

Номер: AT0000345877A
Автор:
Принадлежит:

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15-01-1982 дата публикации

PROCEDURE FOR THE PROTECTION OF GROUPS OF CARBOXYLS

Номер: AT0000109777A
Автор:
Принадлежит:

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15-05-1981 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW PEPTIDDERIVATEN AND THEIR SALTS

Номер: AT0000918478A
Автор:
Принадлежит:

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15-06-2006 дата публикации

HEPATITIS C TRIPEPTID INHIBITORS

Номер: AT0000327246T
Принадлежит:

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15-02-1997 дата публикации

NEW ORAL EFFECTIVE ELASTASE INHIBITORS

Номер: AT0000147756T
Принадлежит:

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15-08-1996 дата публикации

AMINO ACID DERIVATIVES OF CHINOLIN AND NAPHTHYRIDIN

Номер: AT0000141271T
Принадлежит:

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15-08-1995 дата публикации

HIV PROTEASE HEMMER.

Номер: AT0000125547T
Принадлежит:

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15-04-1994 дата публикации

CHEMICAL DERIVATIVES OF GHL-CU.

Номер: AT0000103608T
Принадлежит:

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15-09-1994 дата публикации

USE OF GHL-CU DERIVATIVES FOR THE PRODUCTION OF A MEDICINE FOR THE STIMULATION OF HAIR GROWTH.

Номер: AT0000110255T
Принадлежит:

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15-01-2000 дата публикации

MIXTURES TO THE PROTECTION AND REGENIERUNG OF FABRICS

Номер: AT0000188383T
Принадлежит:

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10-09-1992 дата публикации

NOVEL PEPTIDASE INHIBITORS

Номер: AU0000628075B2
Принадлежит:

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09-01-2014 дата публикации

Hepatitis C virus inhibitors

Номер: AU2012250920A1
Принадлежит:

Hepatitis C virus inhibitors having the following general formula (I); are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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23-02-2012 дата публикации

Compounds for enzyme inhibition

Номер: AU2005243168B2
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

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04-08-2011 дата публикации

HCV NS3 protease inhibitors

Номер: AU2009335904A1
Принадлежит:

The present invention relates to macrocyclic compounds of formula (Ia) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

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01-10-2015 дата публикации

Small molecule modulators of PCSK9 and methods of use thereof

Номер: AU2014231330A1
Принадлежит:

A compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or racemic mixture or stereoisomer thereof, and methods for preventing or treating an LDL-cholesterol-related disease or disorder using such compound(s), and kits and compositions comprising such compound(s).

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22-12-2016 дата публикации

Crystal forms

Номер: AU2015269306A1
Принадлежит: Spruson & Ferguson

The present invention features crystalline forms of Compound I. In one embodiment, a crystalline form of Compound I has characteristic peaks in the PXRD pattern as shown in any one of Figures 1-4.

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03-09-1998 дата публикации

Acylated enol derivatives as prodrugs of elastase inhibitors

Номер: AU0000696292B2
Принадлежит:

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10-05-1973 дата публикации

OLIGOPEPTIDES CONTAINING M-%D1-%2-CHLORETHYL<AMINOL-L- PHENYLALANINE

Номер: AU0003532171A
Принадлежит:

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26-04-1990 дата публикации

AMINO ACID QUINOLINE AND NAPHTHYRIDINE DERIVATIVES

Номер: AU0004172489A
Автор: NAME NOT GIVEN
Принадлежит:

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18-08-2005 дата публикации

METHOD OF REMOVING TRANSITION METALS FROM REACTION SOLUTIONS COMPRISING TRANSITION METAL BYPRODUCTS

Номер: CA0002544886A1
Принадлежит:

A method of diminishing the concentration of a transition metal complex from a first solution by adding a solubility-enhancing compound that enhances the solubility of said complex in a second solution and extracting the first solution with the second solution. The solubility-enhancing compound is a compound of formula (A) wherein, Ra is SH, SO3H, OH or COOH; Rb is SH, OH or COOH; Rc each independently is H, SH, OH or COOH; Rd each independently is H or COOH; n is 1, 2, 3, 4 or 5; or a salt or an activated form thereof.

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02-09-2004 дата публикации

PEPTIDOMIMETIC INHIBITORS OF STAT3 ACTIVITY AND THEIR MEDICAL USES

Номер: CA0002516685A1
Принадлежит:

The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include dipeptides of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position and L=Leu, Val, Ala or a non-polar amino acid. R is preferably aryl or heteroaryl, eventually substituted with halogens, amino and nitro groups. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.

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23-06-1981 дата публикации

CARBOXYLIC ACID ESTERS

Номер: CA0001103660A1
Автор: SIEBER PETER
Принадлежит:

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24-08-2010 дата публикации

HETEROCYCLIC TRIPEPTIDES AS HEPATITIS C INHIBITORS

Номер: CA0002474031C
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or -CH2-C(CH3)3 or -CH2-cyclopentyl; R3is t-butyl or cyclohexil and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.

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17-07-2008 дата публикации

MACROCYCLIC HEPATITIS C PROTEASE INHIBITORS

Номер: CA0002679563A1
Принадлежит:

The present invention provides novel macrocyclic compounds that mimic pep tide substrates of the hepatitis C viral protease and inhibit the viral prot ease, more particularly as inhibitors of the NS3 serine protease from hepati tis C virus. Methods for synthesis of the compounds are also provided. The c ompounds find utility as antiviral agents directed at hepatitis C. The inven tion further provides methods of employing such inhibitors, alone or in comb ination with other therapeutic agents, to treat hepatitis C infection in a s ubject in need of such treatment.

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20-06-2000 дата публикации

PEPTIDASE INHIBITORS

Номер: CA0001341029C

This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

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09-05-1989 дата публикации

PEPTIDES RENFERMENT UN GROUPE ACIDE (ALPHA)-AMINOBORIQUE

Номер: CA0001253999A1
Принадлежит:

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19-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120094930A1
Принадлежит: Onyx Therapeutics Inc

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

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05-07-2012 дата публикации

Novel Biologically Active Peptides and their New Uses

Номер: US20120171234A1
Автор: Kong Lam, Wai Ming Wong
Принадлежит: CMS Peptides Patent Holding Co Ltd

Novel peptides are disclosed with their use as a pharmaceutical composition. A method is also disclosed for making pharmaceutical compositions and treatment of an individual.

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21-03-2013 дата публикации

COMPOUNDS FOR IMMUNOPROTEASOME INHIBITION

Номер: US20130072422A1
Принадлежит:

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention. 2. A compound of claim 1 , wherein Ris —Calkyl-Y.3. A compound of claim 2 , wherein Y is absent and Ris selected from methyl claim 2 , ethyl claim 2 , isopropyl claim 2 , carboxymethyl claim 2 , and benzyl.4. A compound of claim 3 , wherein Ris methyl.5. A compound of claim 1 , wherein Ris selected from Caralkyl and Cheteroaralkyl.6. A compound of claim 5 , wherein Ris selected from Calkyl-phenyl claim 5 , Calkyl-indolyl claim 5 , Calkyl-thienyl claim 5 , Calkyl-thiazolyl claim 5 , and Calkyl-isothiazolyl.7. A compound of claim 6 , wherein Ris selected from Calkyl-phenyl and Calkyl-indolyl optionally substituted with alkyl claim 6 , trihaloalkyl claim 6 , alkoxy claim 6 , hydroxy claim 6 , or cyano.8. A compound of claim 1 , wherein Ris selected from Caralkyl and Calkyl.9. A compound of claim 8 , wherein Ris Caralkyl.10. A compound of claim 9 , wherein Ris Calkyl-phenyl.11. A compound of claim 1 , wherein Rand Rare independently selected from hydrogen and Calkyl.12. A compound of claim 11 , wherein Rand Rare both hydrogen.13. A compound of claim 11 , wherein Rand Rtogether are Calkyl claim 11 , thereby forming a ring.14. A compound of claim 13 , wherein Rand Rtogether with the two adjacent oxygen atoms and the boron form a pinacol boronate ester.15. A compound of claim 1 , wherein Ris selected from carbocyclyl claim 1 , aryl claim 1 , and heterocyclylM-.16. A compound of claim 15 , wherein Ris carbocyclyl or aryl.17. A compound of claim 16 , wherein Ris an indene.18. A compound of claim 17 , wherein Ris 3-methylindene.19. A compound of claim 15 , wherein Ris ...

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06-06-2013 дата публикации

QUINOXALINE-CONTAINING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS

Номер: US20130144036A1
Принадлежит: Enanta Pharmaceuticals, Inc.

The present invention discloses compounds of formula I and II or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1. A compound of Formula I or II:wherein{'sub': 2', '1, 'A is absent or selected from —(C═O)—, —S(O), —C═N—ORor —C(═N—CN);'}{'sub': 201', '1', '8', '2', '8', '2', '8', '1', '8', '2', '8', '2', '8', '3', '12', '3', '12', '3', '12', '3', '12, 'Lis absent or selected from —C-Calkylene, —C-Calkenylene, or —C-Calkynylene each containing 0, 1, 2, or 3 heteroatoms selected from O, S, or N; substituted —C-Calkylene, substituted —C-Calkenylene, or substituted —C-Calkynylene each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N; —C-Ccycloalkylene, or substituted —C-Ccycloalkylene each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N; —C-Ccycloalkenylene, or substituted —C-Ccycloalkenylene each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N;'}{'sub': 2', '1', '1, 'M is absent or selected from O, S, SO, SOor NR; wherein Ris selected at each occurrence from the group consisting of(i) hydrogen;(ii) aryl; substituted aryl; heteroaryl; substituted heteroaryl;(iii) heterocycloalkyl or substituted heterocycloalkyl;{'sub': 1', '8', '2', '8', '2', '8', '3', '8', '2', '8', '2', '8', '3', '12', '3', '12', '3', '12', '3', '12, '(iv) —C-Calkyl, —C-Calkenyl, or —C-Calkynyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S, or N; substituted —C-Calkyl, substituted —C-Calkenyl, or substituted —C-Calkynyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N; —C-Ccycloalkyl, or substituted —C-Ccycloalkyl; —C-Ccycloalkenyl, or substituted —C-Ccycloalkenyl;'}{'sub': 101', '1', '8', '2', '8', '2', '8', '1', '8', '2', '8', '2', '8', '3', '12', '3', '12', '3', '12', '3', '12, 'Lis absent or selected from —C-Calkylene, —C-Calkenylene, or —C-Calkynylene each containing 0, 1, 2, or 3 heteroatoms selected from O, S, or N; substituted —C-Calkylene, substituted —C-Calkenylene, or substituted —C-Calkynylene each ...

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27-06-2013 дата публикации

Methods and Systems for Preparing Irreversible Inhibitors of Protein Tyrosine Phosphatases

Номер: US20130165333A1

Described herein are the preparation and use of novel bromo-phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples. 2. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (I) of claim 1 , wherein R is hydrogen and each Ris hydrogen.3. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (I) of claim 1 , wherein R is Fmoc claim 1 , Boc claim 1 , or Cbz and Ris methyl claim 1 , ethyl claim 1 , benzyl claim 1 , dimethylamino (—N(CH)) claim 1 , propylamino (—NHCHCHCH) claim 1 , isopropylamino (—NHCH(CH)) or allyl.423-. (canceled)24. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (I) of claim 1 , which is an L-amino acid derivative.25. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (I) of which is a D-amino acid derivative.2628-. (canceled)29. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (II) of claim 1 , wherein Ris hydrogen claim 1 , Ris the side chain of aspartic acid claim 1 , nis 1 claim 1 , each Ris hydrogen claim 1 , Ris the side chain of leucine claim 1 , Ris hydroxyl claim 1 , and nis 1.30. The bromo-phosphonomethylphenylalanine amino acid derivative of the Formula (II) of claim 1 , wherein ...

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14-01-2021 дата публикации

PEPTIDOMIMETICS FOR THE TREATMENT OF CORONAVIRUS AND PICORNAVIRUS INFECTIONS

Номер: US20210008150A1
Принадлежит:

Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV-2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus.

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10-01-2019 дата публикации

INHIBITORS OF HEPATITIS C VIRUS

Номер: US20190008858A1
Принадлежит:

Compounds of Formula I are disclosed 184.-. (canceled) This application claims the benefit under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 61/667,806, filed on Jul. 3, 2012, and U.S. Provisional Application Ser. No. 61/798,524, filed on Mar. 15, 2013. The entirety of both applications is incorporated herein by reference.Novel small molecule inhibitors of viral replication are disclosed, compositions containing such compounds, and therapeutic methods comprising the administration of such compounds are also disclosed.The hepatitis C virus (HCV), a member of the hepacivirus genera within the Flaviviridae family, is the leading cause of chronic liver disease worldwide (Boyer, N. et al. 2000, 32, 98-112). Consequently, a significant focus of current antiviral research is directed toward the development of improved methods for the treatment of chronic HCV infections in humans (Ciesek, S., von Hahn T., and Manns, M P., 2011, 15, 597-609, Soriano, V. et al, 2011, 66, 1573-1686; Brody, H., Nature Outlook, 2011, 474, S1-S7; Gordon. C. P., et al., 2005, 48. 1-20; Maradpour, D., et al., 2007, 5, 453-463).Virologic cures of patients with chronic HCV infection are difficult to achieve because of the prodigious amount of daily virus production in chronically infected patients and the high spontaneous mutability of HCV (Neumann, et al., 1998, 282, 103-7; Fukimoto, et al., 1996, 24, 1351-4; Domingo, et al., 1985, 40, 1-8; Martell. et al., 1992, 66, 3225-9). HCV treatment is further complicated by the fact that HCV is genetically diverse and expressed as several different genotypes and numerous subtypes. For example, HCV is currently classified into six major genotypes (designated 1-6), many subtypes (designated a, b, c, and so on), and about 100 different strains (numbered 1, 2, 3, and so on).HCV is distributed worldwide with genotypes 1, 2, and 3 predominate within the United States, Europe, Australia, and East Asia (Japan, Taiwan, Thailand, and China). Genotype 4 ...

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04-02-2016 дата публикации

SMALL MOLECULE MODULATORS OF PCSK9 AND METHODS OF USE THEREOF

Номер: US20160031935A1
Принадлежит:

A compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or racemic mixture or stereoisomer thereof, and methods for preventing or treating an LDL-cholesterol-related disease or disorder using such compound(s), and kits and compositions comprising such compound(s). 2. The compound of claim 1 , wherein:(A){'sub': b', 'c', 'a, 'a. R1 is —B(OR)(OR), or —CH(OH)R;'}{'sub': 2', '2', 'm', 'j, 'b. R2 is H or —CH(CH)C(O)R;'}c. R3 is H or C1-6 alkyl substituted or not;d. R4 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not or cycloalkyl substituted or not;e. R5 is H;f. R6 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not, or cycloalkyl substituted or not;g. R7 is H;h. R8 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not, or cycloalkyl substituted or not; and/or{'sub': m', 'i', 'm', 'i', 'i', 'n, 'i. R9 is RiOC(O)—, RiC(O)—, RORC(O)—, RC(O)RC(O)— or RS(O)—; or'}(B){'sub': b', 'c', 'a, 'a. R1 is —B(OR)(OR) or —CH(OH)R;'}{'sub': 2', '2', 'j, 'b. R2 is H or —CH(CH)C(O)R;'}c. R3 is H or C1-6 alkyl substituted or not;d. R4 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not or cycloalkyl substituted or not;e. R5 is H;f. R6 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not, or cycloalkyl substituted or not;g. R7 is H;h. R8 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl substituted or not, or cycloalkyl substituted or not; and{'sub': m', 'i', 'm', 'i', 'i', 'n, 'i. R9 is RiOC(O)—, RiC(O)—, RORC(O)—, RC(O)RC(O)—, RS(O)—.'}3. (canceled)4. The compound of claim 1 , wherein:{'sub': b', 'c', 'a, 'a. R1 is —B(OR)(OR) or —CH(OH)R;'}{'sub': 2', '2', 'm', 'j, 'b. R2 is H or —CH(CH)C(O)R;'}c. R3 is H or C1-6 alkyl substituted or not;d. R4 is H, C1-6 alkyl substituted or not, C1-6 thioalkyl substituted or not, aryl ...

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01-03-2018 дата публикации

INDOLINE COMPOUNDS AS GRANZYME B INHIBITORS

Номер: US20180057528A1
Автор: Cameron Dale R.
Принадлежит: viDA Therapeutics Inc.

Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B. 811-. (canceled)12. A pharmaceutical composition claim 1 , comprising a compound of and a pharmaceutically acceptable carrier.13. A method for inhibiting Granzyme B in a subject claim 1 , comprising administering an effective amount of a compound of to a subject in need thereof.14. A method for treating a disease claim 1 , disorder claim 1 , or condition treatable by inhibiting Granzyme B claim 1 , comprising administering a therapeutically effective amount of a compound of to a subject in need thereof.15. The method of claim 14 , wherein the disease claim 14 , disorder claim 14 , or condition treatable by inhibiting Granzyme B is selected from treating dissection claim 14 , aneurysm claim 14 , and atherosclerosis.16. The method of claim 14 , wherein the condition treatable by inhibiting Granzyme B is a wound and administering the compound or composition promotes wound healing.17. The method of claim 13 , wherein administering the compound comprises topical administration claim 13 , oral administration claim 13 , and administration by injection. This application is a continuation of U.S. patent application Ser. No. 14/869,750, filed Sep. 29, 2015 (now U.S. Pat. No. 9,605,021), which is a continuation-in-part of International Application No. PCT/CA2014/050317, filed Mar. 28, 2014, which claims the benefit of U.S. Patent Application No. 61/806,767, filed Mar. 29, 2013, and U.S. Patent Application No. 61/941,358, filed Feb. 18, 2014, and is a continuation-in-part of International Application No. PCT/CA2014/050318, filed Mar. 28, 2014, which claims the benefit of U.S. Patent Application No. 61/806,767, filed Mar. 29, 2013, and U.S. Patent Application No. 61/941,358, filed Feb. 18, 2014, each expressly incorporated herein by reference in its entirety.The present ...

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05-03-2020 дата публикации

COMPOUNDS FOR PROTEASOME

Номер: US20200071356A1
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. 2. A compound of claim 1 , wherein X is O.3. A compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare independently selected from Calkyl claim 2 , Chydroxyalkyl claim 2 , and Caralkyl; and Ris hydrogen.4. A compound of claim 3 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.5. A compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , and Rare all hydrogen.6. A compound of claim 5 , wherein Y is selected from N-alkyl claim 5 , O claim 5 , and CH.7. A compound of claim 6 , wherein Z is CH claim 6 , and m and n are both 0.8. A compound of claim 6 , wherein Z is CH claim 6 , m is 0 claim 6 , and n is 2 or 3.9. A compound of claim 6 , wherein Z is O claim 6 , m is 1 claim 6 , and n is 2.17. A compound of claim 16 , wherein X is O.18. A compound of claim 17 , wherein R claim 17 , R claim 17 , R claim 17 , and Rare independently selected from Calkyl claim 17 , Chydroxyalkyl claim 17 , and Caralkyl.19. A compound of claim 18 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.21. A compound of claim 20 , wherein X is O.22. A compound of claim 21 , wherein Rand Rare independently selected from Calkyl claim 21 , Chydroxyalkyl claim 21 , and Caralkyl.23. A compound of claim 22 , wherein Rand Rare independently Calkyl.24. A compound ...

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30-03-2017 дата публикации

Macrocyclic proline derived hcv serine protease inhibitors

Номер: US20170088583A1
Принадлежит: Enanta Pharmaceuticals Inc

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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25-08-2022 дата публикации

COMPOUNDS FOR PROTEASOME ENZYME INHIBITION

Номер: US20220267372A1
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Nn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. 149.-. (canceled)51. The method of claim 50 , wherein compound (B) is admixed as a salt.52. The method of claim 51 , wherein compound (B) is admixed as the trifluoroacetate salt.53. The method of claim 50 , wherein step (a) is performed in the presence of a peptide coupling agent.54. The method of claim 53 , wherein the peptide coupling agent comprises PyBOP.55. The method of claim 50 , wherein compound (E) is admixed as a trifluoroacetate salt.56. The method of claim 50 , wherein step (c) is performed in the presence of a peptide coupling agent.57. The method of claim 56 , wherein the peptide coupling agent comprises PyBOP claim 56 , HOBT claim 56 , or both.58. The method of claim 50 , further comprising (d) isolating compound 8 via filtration. This application claims the benefit of priority of U.S. Provisional Patent Application Ser. No. 60/599,401 filed on Aug. 6, 2004 and U.S. Provisional Patent Application Ser. No. 60/610,001 filed Sep. 14, 2004 and is a continuation-in-part of U.S. patent application Ser. No. 11/106,879 filed Apr. 14, 2005. The teachings of all of the referenced applications are incorporated by reference in their entirety.This invention relates to compounds and methods for enzyme inhibition. In particular, the invention relates to therapeutic methods based on enzyme inhibition.In ...

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01-09-2022 дата публикации

PEPTIDOMIMETICS FOR THE TREATMENT OF CORONAVIRUS AND PICORNAVIRUS INFECTIONS

Номер: US20220273753A1
Принадлежит:

Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV-2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus. 130-. (anceled)32. The method of claim 31 , wherein Ris C(O)H.33. The method of claim 31 , wherein Ris alkylaryl or alkylheteroaryl.35. The method of claim 31 , wherein Ris thiophene.36. The method of claim 31 , wherein X is O claim 31 , Rand R′ are H claim 31 , and Ris an optionally substituted phenyl.37. The method of claim 31 , wherein X=a covalent bond claim 31 , p=0 claim 31 , and Ris an optionally substituted aryl or heteroaryl.3824. The method of claim claim 31 , wherein the heteroaryl ring is a pyrazine claim 31 , thiophene claim 31 , isoxazole claim 31 , or oxazole ring.39. The method of claim 31 , wherein Ris phenyl claim 31 , halo-substituted phenyl claim 31 , or naphthyl.40. The method of claim 31 , wherein the Hepeviridae virus is the hepatitis E virus.41. The method of claim 31 , wherein the picornavirus is an enterovirus.42. The method of claim 31 , wherein the virus is a causative agent for multiple sclerosis claim 31 , SARS claim 31 , MERS claim 31 , or COVID-19.43. The method of claim 31 , wherein the virus is a causative agent for a respiratory infection.44. The method of claim 31 , wherein the method further comprising administering another anti-coronavirus or picornavirus virus agent in combination or alternation with the compound of any of Formulas I-VI.45. The method of claim 31 , wherein the patient is co-infected with norovirus claim 31 , and the ...

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02-05-2019 дата публикации

NEUROPEPTIDE S RECEPTOR (NPSR) AGONISTS

Номер: US20190127419A1
Принадлежит:

Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling. 2. The compound according to Formula IA of .3. The compound according to claim 2 , wherein Ris CH(NH)CHOH claim 2 , Ris a phenylalanine side chain claim 2 , R is an alkylated lysine side chain claim 2 , and Ris an asparagine side chain.4. The compound according to claim 2 , wherein Ris CH(NH)CHOH claim 2 , Ris a alkylcycloalkyl claim 2 , R is an alkylated lysine side chain claim 2 , and Ris an asparagine side chain.5. The compound according to claim 2 , wherein Ris an alkyl group claim 2 , Ris a phenylalanine side chain claim 2 , R is a lysine side chain claim 2 , and Ris an asparagine side chain.6. The compound according to claim 2 , wherein Ris phenyl claim 2 , Ris a phenylalanine side chain claim 2 , R is a lysine side chain claim 2 , and Ris an asparagine side chain.7. The compound according to claim 2 , wherein Ris phenyl claim 2 , Ris a benzyl substituted with halo claim 2 , R is a lysine side chain claim 2 , and Ris an asparagine side chain.8. The compound according to claim 2 , wherein Ris phenyl claim 2 , Ris a phenylalanine side chain claim 2 , R is an alkylated lysine side chain claim 2 , and Ris an asparagine side chain.9. The compound according to claim 2 , wherein Ris phenyl claim 2 , Ris a phenylalanine side chain claim 2 , R is a lysine side chain claim 2 , Ris an asparagine ...

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17-06-2021 дата публикации

COMPOUNDS FOR PROTEASOME ENZYME INHIBITION

Номер: US20210179663A1
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. 2. A compound of claim 1 , wherein X is O.3. A compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare independently selected from Calkyl claim 2 , Chydroxyalkyl claim 2 , and Caralkyl; and Ris hydrogen.4. A compound of claim 3 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.5. A compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , and Rare all hydrogen.6. A compound of claim 5 , wherein Y is selected from N-alkyl claim 5 , O claim 5 , and CH.7. A compound of claim 6 , wherein Z is CH claim 6 , and m and n are both 0.8. A compound of claim 6 , wherein Z is CH claim 6 , m is 0 claim 6 , and n is 2 or 3.9. A compound of claim 6 , wherein Z is O claim 6 ,m is 1 claim 6 , and n is 2.17. A compound of claim 16 , wherein Xis O.18. A compound of claim 17 , wherein R claim 17 , R claim 17 , R claim 17 , and Rare independently selected from Calkyl claim 17 , Chydroxyalkyl claim 17 , and Caralkyl.19. A compound of claim 18 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.21. A compound of claim 20 , wherein X is O.22. A compound of claim 21 , wherein Rand Rare independently selected from Callyl claim 21 , Chydroxyalkyl claim 21 , and Caralkyl.23. A compound of claim 22 , wherein Rand Rare independently Calkyl.24. A compound ...

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08-06-2017 дата публикации

Antimicrobial Compounds

Номер: US20170158720A1
Принадлежит: bioMerieux SA

An antimicrobial compound, as well as the salts, derivatives and analogues thereof, said compound being represented by the general formula (I): wherein R 1 represents a peptide part P1 or a peptide part P2.

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14-06-2018 дата публикации

MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS

Номер: US20180162905A1
Принадлежит:

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: 226-. (canceled) This application is a continuation application of U.S. application Ser. No. 15/287,042, filed on Oct. 6, 2016, which is a continuation application of U.S. application Ser. No. 14/946,866, filed Nov. 20, 2015, now abandoned, which is a continuation application of U.S. application Ser. No. 14/146,161, filed Jan. 2, 2014, now U.S. Pat. No. 9,220,748, issued on Dec. 29, 2015, which is a continuation application of U.S. application Ser. No. 13/237,120, filed on Sep. 20, 2011, now U.S. Pat. No. 8,648,037, issued on Feb. 11, 2014, which claims the benefit of U.S. Provisional Application No. 61/385,058, filed on Sep. 21, 2010, U.S. Provisional Application No. 61/499,994, filed on Jun. 22, 2011, and U.S. Provisional Application No. 61/504,616, filed on Jul. 5, 2011. The entire teachings of the above applications are incorporated herein by reference.Inventions described in this application were made by or on behalf of Enanta Pharmaceuticals, Inc. and Abbott Laboratories who are parties to a joint research agreement, that was in effect on or before the date such inventions were made and such inventions were made as a result of activities undertaken within the scope of the joint research agreement.The present invention relates to novel hepatitis C virus (HCV) protease inhibitor compounds, methods for using the same to treat HCV infection, as well as processes for making such compounds.HCV is the principal cause of non-A, non-B hepatitis and is an increasingly severe public health problem both in the developed and developing world. It is estimated that the virus infects over 200 million people worldwide, surpassing the number of individuals infected with the human immunodeficiency virus (HIV) by nearly five fold. HCV infected patients, due to the high percentage of individuals inflicted with chronic infections, are at an elevated risk of ...

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25-06-2015 дата публикации

Peptoids Useful for the Mineralization of Apatite

Номер: US20150174197A1

The present invention provides for a bio-mimetic polymer capable of catalyzing or mineralizing calcium ion and phosphate ions into an apatite.

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23-07-2015 дата публикации

FLUORINATED EPOXYKETONE-BASED COMPOUNDS AND USES THEREOF AS PROTEASOME INHIBITORS

Номер: US20150203534A1
Принадлежит: FLUORINOV PHARMA INC.

The present application relates to novel fluorinated epoxyketone-based compounds, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions mediated by proteasome inhibition, in particular, the present application includes compounds of Formula I, and compositions and uses thereof: 35.-. (canceled)8. (canceled)9. The compound of claim 2 , wherein Ris Cheterocycloalkyl and X is Calkylene.10. The compound of claim 9 , wherein Ris selected from morpholinyl claim 9 , 1 claim 9 ,4-oxazepanyl claim 9 , thiomorpholinyl claim 9 , 1 claim 9 ,4-thiazepanyl claim 9 , 1 claim 9 ,4-thiazepanyl-1-oxide claim 9 , 1 claim 9 ,4-thiazepanyl-1 claim 9 ,1-dioxide claim 9 , 1 claim 9 ,4-thiazinanyl-1-oxide claim 9 , 1 claim 9 ,4-thiazinanyl-1 claim 9 ,1-dioxide claim 9 , aziridinyl claim 9 , azetidinyl claim 9 , pyrrolidinyl claim 9 , piperazinyl and 1 claim 9 ,4-diazepanyl.11. (canceled)12. The compound of claim 10 , wherein X is —CH—.13. The compound of claim 1 , wherein Rand Rare each independently selected from the group consisting of Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Calkylene-O—Calkyl claim 1 , Calkylene-O—Chaloalkyl claim 1 , Calkenylene-O—Chaloalkyl and Calkynylene-O—Chaloalkyl claim 1 , wherein at least one of Rand Ris C-alkylene-O—Chaloalkyl.14. The compound of claim 13 , wherein Rand Rare each independently selected from the group consisting of isobutyl claim 13 , —CH—O—CHand —CH—O—CHF claim 13 , wherein at least one of Rand Ris —CH—O—CHF.15. (canceled)16. The compound of claim 13 , wherein Ris selected from the group consisting of Calkyl claim 13 , Calkenyl claim 13 , Calkynyl claim 13 , CalkyleneCcycloalkyl and CalkyleneCaryl.17. (canceled)18. The compound of claim 1 , wherein Ris selected from the group consisting of H and Calkyl.20. The compound of claim 1 , or a salt claim 1 , solvate or prodrug thereof claim 1 , selected from:2-Methyl-thiazole-5-carboxylic acid ((S)-1-{(S)-1-[(S)-1- ...

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29-07-2021 дата публикации

OLIGOPEPTIDE LINKER INTERMEDIATE AND PREPARATION METHOD THEREOF

Номер: US20210230218A1
Автор: HUANG Changjiang, LI Lele
Принадлежит: MABPLEX INTERNATIONAL, LTD.

The invention provides a new oligopeptide linker intermediate and a preparation method thereof. The preparation method of the oligopeptide intermediate is easily carried out under mild reaction conditions, and since almost no side reactions occur in the reaction, the method produces a high-purity product with fewer impurities and easy to be purified, achieving unexpected technical effects. 2. The oligopeptide linker intermediate according to claim 1 , wherein the AA claim 1 , AA claim 1 , AA claim 1 , and AAare each independently selected from the group consisting of -valine- (-Val-) claim 1 , -citrulline -(-Cit-) claim 1 , -alanine- (-Ala-) claim 1 , -lysine- (-Lys-) claim 1 , -lysine(trityl)- (-Lys(Trt)-) claim 1 , -lysine(monomethoxytrityl)-(-Lys(Mmt)-) claim 1 , -lysine(fluorenylmethyloxycarbonyl)- (-Lys(Fmoc)-) claim 1 , -arginine- (-Arg-) claim 1 , -phenylalanine- (-Phe-) claim 1 , -glycine- (-Gly-) claim 1 , -leucine- (-Leu-) and -isoleucine- (-Ile-).3. The oligopeptide linker intermediate according to claim 2 , wherein{'sub': 1', '2, 'the -AA-AA- is selected from the group consisting of -valine-citrulline- (-Val-Cit-), -valine-alanine-(-Val-Ala-), -valine-lysine- (-Val-Lys-), -valine-lysine(trityl)- (-Val-Lys(Trt)-), -valine-lysine(monomethoxytrityl)-(-Val-Lys(Mmt)-), -valine-lysine(fluorenylmethyloxycarbonyl)-(-Val-Lys(Fmoc)-), -valine-arginine- (-Val-Arg-), -phenylalanine-citrulline-(-Phe-Cit-), -phenylpropyl-lysine- (-Phe-Lys-), -phenylalanine-lysine(trityl)-(-Phe-Lys(Trt)-), -phenylalanine-lysine(monomethoxytrityl)- (-Phe-Lys (Mmt)-), -phenylalanine-lysine (fluorenylmethyloxycarbonyl)- (-Phe-Lys(Fmoc)-), leucine-citrulline- (-Leu-Cit-), isoleucine-citrulline- (-Ile-Cit-) and -phenylalanine-arginine- (-Phe-Arg-);'}{'sub': 1', '2', '3, 'the -AA-AA-AA- is -phenylalanine-arginine-arginine-(-Ala-Arg-Arg-); and'}{'sub': 1', '2', '3', '4, 'the -AA-AA-AA-AA- is selected from the group consisting of -glycine-glycine-phenylalanine-glycine-(-Gly-Gly-Phe-Gly-), - ...

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04-08-2016 дата публикации

Intermediates for macrocyclic compounds

Номер: US20160221927A1
Принадлежит: Ocera Therapeutics Inc

The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n 1 , m, p Z 1 , Z 2 , and Z 3 are as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

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11-07-2019 дата публикации

COMPOUNDS FOR PROTEASOME ENZYME INHIBITION

Номер: US20190211058A1
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. 2. A compound of claim 1 , wherein X is O.3. A compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare independently selected from Calkyl claim 2 , Chydroxyalkyl claim 2 , and Caralkyl; and Ris hydrogen.4. A compound of claim 3 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.5. A compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , and Rare all hydrogen.6. A compound of claim 5 , wherein Y is selected from N-alkyl claim 5 , O claim 5 , and CH.7. A compound of claim 6 , wherein Z is CH claim 6 , and m and n are both 0.8. A compound of claim 6 , wherein Z is CH claim 6 , m is O claim 6 , and n is 2 or 3.9. A compound of claim 6 , wherein Z is O claim 6 , m is 1 claim 6 , and n is 2.17. A compound of claim 16 , wherein X is O.18. A compound of claim 17 , wherein R claim 17 , R claim 17 , R claim 17 , and Rare independently selected from Calkyl claim 17 , Chydroxyalkyl claim 17 , and Caralkyl.19. A compound of claim 18 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.21. A compound of claim 20 , wherein X is O.22. A compound of claim 21 , wherein Rand Rare independently selected from Calkyl claim 21 , Chydroxyalkyl claim 21 , and Caralkyl.23. A compound of claim 22 , wherein Rand Rare independently Calkyl.24. A compound ...

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25-07-2019 дата публикации

18f labeled amino acids, derivatives thereof and method of making same

Номер: US20190223814A1
Принадлежит: SIMON FRASER UNIVERSITY

The present invention provides 18 F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging:

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17-08-2017 дата публикации

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

Номер: US20170233437A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention provides compounds of formula (I) 3. The compound according to any of or , wherein:{'sup': 1', '1, 'Xis CRor N,'}{'sup': 2', '12, 'Xis CRor N,'}{'sup': 3', '13, 'Xis CRor N,'}{'sup': 4', '14', '1', '2', '3', '4, 'Xis CRor N, with the proviso that not more than two of X, X, Xand Xare N;'}{'sup': 5', '15, 'Xis CRor N,'}{'sup': 6', '16, 'Xis CRor N,'}{'sup': 7', '17, 'Xis CRor N,'}{'sup': 8', '18', '5', '6', '7', '8, 'Xis CRor N, with the proviso that not more than two of X, X, Xand Xare N;'}{'sup': '1', 'sub': 2', 'm', '2', 'm', '1-7', '1-7', '3-7', '1-7, 'Ris —(CH)-heteroaryl or —(CH)— heterocycloalkyl; wherein heteroaryl is optionally substituted with one or more halo, cyano, C-alkyl, C-haloalkyl, C-cycloalkyl or C-alkoxy; and wherein heterocycloalkyl is partly unsaturated;'}{'sup': 2', '4', '6, 'sub': 1-7', '1-7', '3-7, 'R, Rand Rare each individually selected from hydrogen, C-alkyl, C-haloalkyl, and C-cycloalkyl;'}{'sup': 3', '20', '21', '20', '21', '20', '21, 'sub': 1-7', '2', 'n', '2', 'n', '2', 'n', '2', 'q, 'Ris —C-alkyl, —(CH)—NRR, —(CH)—C(O)NRRor —(CH)—O—(CH)—NRR;'}{'sup': 5', '22', '23', '22', '23, 'sub': 1-7', '1-7', '2', 'o', '2', 'o, 'claim-text': [{'sub': 2', 'o', '2', 'q', '2', 'o', '2', 'o, 'sup': 20', '21', '22', '23', '22', '23, '—(CH)—O—(CH)NRR, —(CH)—NH—C(NH)—NRR, —(CH)—NH—C(O)—NRR,'}, {'sub': 2', 'o', '2', 'o', '2', 'o', '2', 'o, 'sup': '26', '—(CH)—NH—C(O)—OR, —(CH)-heterocycloalkyl, —(CH)-heteroaryl, —(CH)-aryl,'}, {'sub': 1-7', '1-7', '1-7, 'wherein cycloalkyl, heterocycloalkyl, heteroaryl and aryl are optionally substituted by halo, cyano, C-alkyl, C-haloalkyl, C-alkoxy or aryl;'}], 'Ris hydrogen, C-alkyl, hydroxy-C-alkyl, —(CH)—NRR, —(CH)—C(O)—NRR,'}{'sup': 7', '8, 'sub': 1-7', '1-7', '3-7', '1-7, 'Rand Rare each individually selected from hydrogen, C-alkyl, C-haloalkyl, C-cycloalkyl and C-alkoxy;'}{'sup': 11', '12', '13', '14', '15', '16', '24', '25', '24', '25, 'sub': 1-7', '1-7', '1-7', '1-7', '1-7', '2', '3-7, ' ...

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29-09-2016 дата публикации

ALKOXYSILANE DERIVATIVES OF N-ACYL AMINO ACIDS, N-ACYL DIPEPTIDES, AND N-ACYL TRIPEPTIDES, AND PARTICLES AND STABLE OIL-IN-WATER FORMULATIONS USING THE SAME

Номер: US20160280737A1
Принадлежит:

Hydrophilic N-acylamino acid, N-acyl dipeptide, and N-acyl tripeptide substituted silanes are prepared which can be utilized as reactive surface treatments for particles of pigments, minerals, and fillers. These treated particles form stable dispersions in the aqueous phase of oil-in-water mixtures that are suitable for cosmetic applications. The treated particles may also be used in pressed powder and color cosmetic formulations. 1. A hydrophilic alkoxysilane derivative of an N-acyl dipeptide or N-acyl tripeptide , wherein the acyl group is acetyl.2. The hydrophilic alkoxysilane derivative according to claim 1 , wherein the alkoxy group is selected from the group consisting of methoxy and ethoxy.3. The hydrophilic alkoxysilane derivative according to claim 1 , wherein the derivative is a propyltrialkoxysilane derivative.4. The hydrophilic alkoxysilane derivative according to claim 1 , wherein the derivative is (N-acetylglycylpropyl)triethoxysilane.5. The hydrophilic alkoxysilane derivative according to claim 1 , wherein the derivative is (N-acetylglycinamidepropyl) trimethoxysilane.6. The hydrophilic alkoxysilane derivative according to claim 1 , wherein the derivative is (N-acetylleucinamidepropyl)triethoxysilane.7. (N-acetylhydroxyprolyl)propyltriethoxysilane.8. The hydrophilic alkoxysilane derivative according to claim 1 , comprising an amino acid residue selected from glycine and hydroxyproline. This application is a continuation of co-pending U.S. patent application Ser. No. 13/241,860, filed Sep. 23, 2011, which claims the benefit of U.S. provisional patent Application No. 61/385,790, filed on Sep. 23, 2010, the disclosures of which are incorporated herein by reference.Surface treated pigments have been used to improve the wetting and dispersion of pigments and fillers in inks, coatings, resins and cosmetics. Passivation of the pigment and filler surfaces to reduce chemical interaction with the vehicle is another application of surface modifications. In ...

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29-08-2019 дата публикации

MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS

Номер: US20190263860A1
Принадлежит:

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: 226-. (canceled) This application is a continuation application of U.S. application Ser. No. 15/839,249, filed Dec. 12, 2017, which is a continuation application of U.S. application Ser. No. 15/287,042, filed on Oct. 6, 2016, now abandoned, which is a continuation application of U.S. application Ser. No. 14/946,866, filed Nov. 20, 2015, now abandoned, which is a continuation application of U.S. application Ser. No. 14/146,161, filed Jan. 2, 2014, now U.S. Pat. No. 9,220,748, issued on Dec. 29, 2015, which is a continuation application of U.S. application Ser. No. 13/237,120, filed on Sep. 20, 2011, now U.S. Pat. No. 8,648,037, issued on Feb. 11, 2014, which claims the benefit of U.S. Provisional Application No. 61/385,058, filed on Sep. 21, 2010, U.S. Provisional Application No. 61/499,994, filed on Jun. 22, 2011, and U.S. Provisional Application No. 61/504,616, filed on Jul. 5, 2011. The entire teachings of the above applications are incorporated herein by reference.Inventions described in this application were made by or on behalf of Enanta Pharmaceuticals, Inc. and Abbott Laboratories who are parties to a joint research agreement, that was in effect on or before the date such inventions were made and such inventions were made as a result of activities undertaken within the scope of the joint research agreement.The present invention relates to novel hepatitis C virus (HCV) protease inhibitor compounds, methods for using the same to treat HCV infection, as well as processes for making such compounds.HCV is the principal cause of non-A, non-B hepatitis and is an increasingly severe public health problem both in the developed and developing world. It is estimated that the virus infects over 200 million people worldwide, surpassing the number of individuals infected with the human immunodeficiency virus (HIV) by nearly five fold. HCV infected ...

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27-08-2020 дата публикации

MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS

Номер: US20200270303A1
Принадлежит:

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: 126-. (canceled) This application is a is a continuation application of U.S. application Ser. No. 16/142,087, filed on Sep. 26, 2018, which is a continuation application of U.S. application Ser. No. 15/839,249, filed Dec. 12, 2017, now abandoned, which is a continuation application of U.S. application Ser. No. 15/287,042, filed on Oct. 6, 2016, now abandoned, which is a continuation application of U.S. application Ser. No. 14/946,866, filed Nov. 20, 2015, now abandoned, which is a continuation application of U.S. application Ser. No. 14/146,161, filed Jan. 2, 2014, now U.S. Pat. No. 9,220,748, issued on Dec. 29, 2015, which is a continuation application of U.S. application Ser. No. 13/237,120, filed on Sep. 20, 2011, now U.S. Pat. No. 8,648,037, issued on Feb. 11, 2014, which claims the benefit of U.S. Provisional Application No. 61/385,058, filed on Sep. 21, 2010, U.S. Provisional Application No. 61/499,994, filed on Jun. 22, 2011, and U.S. Provisional Application No. 61/504,616, filed on Jul. 5, 2011. The entire teachings of the above applications are incorporated herein by reference.Inventions described in this application were made by or on behalf of Enanta Pharmaceuticals, Inc. and Abbott Laboratories who are parties to a joint research agreement, that was in effect on or before the date such inventions were made and such inventions were made as a result of activities undertaken within the scope of the joint research agreement.The present invention relates to novel hepatitis C virus (HCV) protease inhibitor compounds, methods for using the same to treat HCV infection, as well as processes for making such compounds.HCV is the principal cause of non-A, non-B hepatitis and is an increasingly severe public health problem both in the developed and developing world. It is estimated that the virus infects over 200 million people worldwide, ...

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08-11-2018 дата публикации

GELATINASE INHIBITORS AND USE THEREOF

Номер: US20180319839A1
Принадлежит: Iproteos S.L

New gelatinase inhibitors, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy and/or prophylaxis of conditions wherein inhibition of gelatinases is useful such as epilepsy, schizophrenia, Alzheimer disease, autism (in particular associated to fragile X syndrome), mental retardation, mood disorders such as bipolar disorders, depression, vascular diseases such as ischemic stroke and atherosclerosis, inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease, drug addiction, neuropathic pain, lung diseases such as asthma and chronic obstructive pulmonary disease, cancer and sepsis. 2. A compound according to claim 1 , wherein AAand AAare absent.3. A compound according to claim 1 , wherein G is selected from the group consisting of —CH— claim 1 , —(CH)— claim 1 , —(CH)— claim 1 , —CH—CH(CH)—CH— claim 1 , —(CH)— claim 1 , —CH—CH—CH—CH(CH—CH—CH)— claim 1 , —O—(CH)— claim 1 , —(CH)— and —CH—O—(CH)—O—CH—.4. A compound according to claim 3 , wherein R-G is selected from the group consisting of CH—(CH)— claim 3 , CH—CH(CH)—CH— claim 3 , phenyl-O—(CH)— claim 3 , CH—(CH)— claim 3 , CH—(CH)— and CH—CH—CH—CH(CH—CH—CH)—.5. A compound according to claim 1 , wherein one of R claim 1 , Rand Ris hydrogen.6. A compound according to claim 5 , wherein one of R claim 5 , Rand Ris hydrogen and the other two are fluorine atoms.7. A compound according to claim 6 , wherein the phenyl group substituted by R claim 6 , Rand Ris a 3 claim 6 ,5-difluorophenyl.8. A compound according to claim 1 , wherein Rand Rare both hydrogen.10. A compound according to selected from the group consisting of:(2S)-1-acetyl-N-[(1 S)-1-[[(1S)-3-[(4-fluorobenzoyl)amino]-1-(hydroxycarbamoyl)propyl]carbamoyl]-2-methyl-butyl]-N-methyl-pyrrolidine-2-carboxamide(2S)-1-acetyl-N-[(1S)-1-[[(1S)-3-[(3,5-difluorobenzoyl)amino]-1-(hydroxycarbamoyl)propyl]carbamoyl]-2-methyl-butyl]-N-methyl-pyrrolidine-2-carboxamide(2S)—N-[(1S)-1-[[(1S ...

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15-10-2020 дата публикации

Compounds for proteasome enzyme inhibition

Номер: US20200325172A1
Принадлежит:

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. 2. A compound of claim 1 , wherein X is O.3. A compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare independently selected from Calkyl claim 2 , Chydroxyalkyl claim 2 , and Caralkyl; and Ris hydrogen.4. A compound of claim 3 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.5. A compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , and Rare all hydrogen.6. A compound of claim 5 , wherein Y is selected from N-alkyl claim 5 , O claim 5 , and CH.7. A compound of claim 6 , wherein Z is CH claim 6 , and m and n are both 0.8. A compound of claim 6 , wherein Z is CH claim 6 , m is 0 claim 6 , and n is 2 or 3.9. A compound of claim 6 , wherein Z is O claim 6 , m is 1 claim 6 , and n is 2.17. A compound of claim 16 , wherein X is O.18. A compound of claim 17 , wherein R claim 17 , R claim 17 , R claim 17 , and Rare independently selected from Calkyl claim 17 , Chydroxyalkyl claim 17 , and Caralkyl.19. A compound of claim 18 , wherein Rand Rare independently Caralkyl and Rand Rare independently Calkyl.21. A compound of claim 20 , wherein X is O.22. A compound of claim 21 , wherein Rand Rare independently selected from Calkyl claim 21 , Chydroxyalkyl claim 21 , and Caralkyl.23. A compound of claim 22 , wherein Rand Rare independently Calkyl.24. A compound ...

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01-12-2016 дата публикации

FLUORINATED EPOXYKETONE-BASED COMPOUNDS AND USES THEREOF AS PROTEASOME INHIBITORS

Номер: US20160347792A1
Принадлежит: TRILLIUM THERAPEUTICS INC.

The present application relates to novel fluorinated epoxyketone-based compounds, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions mediated by proteasome inhibition. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: 5. The compound of claim 2 , wherein Ris Cheterocycloalkyl and X is Calkylene.6. The compound of claim 5 , wherein Ris selected from morpholinyl claim 5 , 1 claim 5 ,4-oxazepanyl claim 5 , thiomorpholinyl claim 5 , 1 claim 5 ,4-thiazepanyl claim 5 , 1 claim 5 ,4-thiazepanyl-1-oxide claim 5 , 1 claim 5 ,4-thiazepanyl-1 claim 5 ,1-dioxide claim 5 , 1 claim 5 ,4-thiazinanyl-1-oxide claim 5 , 1 claim 5 ,4-thiazinanyl-1 claim 5 ,1-dioxide claim 5 , aziridinyl claim 5 , azetidinyl claim 5 , pyrrolidinyl claim 5 , piperazinyl and 1 claim 5 ,4-diazepanyl.7. The compound of claim 6 , wherein X is —CH—.8. The compound of claim 1 , wherein Rand Rare each independently selected from the group consisting of Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Calkylene-O—Calkyl claim 1 , Calkylene-O—Chaloalkyl claim 1 , Calkenylene-O—Chaloalkyl and Calkynylene-O—Chaloalkyl claim 1 , wherein at least one of Rand Ris C-alkylene-O—Chaloalkyl.9. The compound of claim 8 , wherein Rand Rare each independently selected from the group consisting of isobutyl claim 8 , —CH—O—CHand —CH—O—CHF claim 8 , wherein at least one of Rand Ris —CH—O—CHF.10. The compound of claim 8 , wherein Ris selected from the group consisting of Calkyl claim 8 , Calkenyl claim 8 , Calkynyl claim 8 , CalkyleneCcycloalkyl and CalkyleneCaryl.11. The compound of claim 1 , wherein Ris selected from the group consisting of H and Calkyl.13. The compound of claim 1 , or a salt or solvate thereof claim 1 , selected from:2-Methyl-thiazole-5-carboxylic acid ((S)-1-{(S)-1-[(S)-1-benzyl-2-((R)-2-methyloxiranyl)-2-oxo-ethylcarbamoyl]-2-difluoromethoxyethylcarbamoyl}-2- ...

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17-12-2015 дата публикации

Compounds for proteasome enzyme inhibition

Номер: US20150361134A1
Принадлежит: Onyx Therapeutics Inc

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

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15-12-2016 дата публикации

Inhibitors of hepatitis c virus

Номер: US20160361375A1
Принадлежит: Gilead Sciences Inc

Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

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20-12-2018 дата публикации

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

Номер: US20180362578A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention provides compounds of formula (I) 151.-. (canceled)5357.-. (canceled)59. (canceled)64. The method of claim 58 , wherein Ris —(CH)-heteroaryl or —(CH)— heterocycloalkyl claim 58 , wherein heteroaryl is monocyclic or bicyclic and is optionally substituted with one or more halo claim 58 , cyano claim 58 , C-alkyl claim 58 , C-haloalkyl claim 58 , C-cycloalkyl or C-alkoxy; and wherein heterocycloalkyl is partly unsaturated.6513. The method of claim 58 , wherein Ris hydrogen claim 58 , C-alkyl claim 58 , hydroxy-C-alkyl claim 58 , —(CH)—NRR claim 58 , —(CH)—C(O)—NRR claim 58 , —(CH)—O—(CH)—NRR claim 58 , —(CH)—NH—C(NH)—NRR claim 58 , —(CH)—NH—C(O)—NRR claim 58 , —(CH)—NH—C(O)—OR claim 58 , —(CH)-heterocycloalkyl claim 58 , —(CH)-heteroaryl claim 58 , —(CH)-aryl claim 58 , wherein heterocycloalkyl claim 58 , heteroaryl and aryl are optionally substituted by halo claim 58 , cyano claim 58 , C-alkyl claim 58 , C-haloalkyl claim 58 , C-alkoxy or aryl; and wherein o claim 58 , q claim 58 , R-Rand Rare as defined in any of claims to .66. The method of claim 58 , wherein Ris hydrogen claim 58 , halo claim 58 , C-alkyl claim 58 , halo-C-alkyl claim 58 , heterocycloalkyl claim 58 , aryl or heteroaryl claim 58 , wherein heteroaryl is optionally substituted with one C-haloalkyl or C-alkoxy.67. The method of claim 58 , wherein Ris hydrogen claim 58 , halo claim 58 , C-alkyl claim 58 , halo-C-alkyl claim 58 , heterocycloalkyl or aryl.68. The method of claim 58 , wherein Ris hydrogen claim 58 , halogen claim 58 , cyano claim 58 , C-alkyl claim 58 , C-haloalkyl claim 58 , —NRR claim 58 , C-alkyl-NRR claim 58 , hydroxy claim 58 , C-alkoxy claim 58 , —B(OH) claim 58 , benzyloxy-propynyl claim 58 , heterocycloalkyl claim 58 , aryl or heteroaryl claim 58 , wherein heterocycloalkyl is optionally substituted with one amino claim 58 , wherein aryl is optionally substituted with one halo claim 58 , cyano claim 58 , —SO—C-alkyl claim 58 , or —SO—NRR claim 58 , and wherein ...

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27-12-2018 дата публикации

NEW DIFLUOROKETAMIDE DERIVATIVES AS HTRA1 INHIBITORS

Номер: US20180371015A1
Принадлежит: Hoffmann-La Roche Inc.

The invention provides novel compounds having the general formula (I) 2. A compound according to claim 1 , wherein{'sup': '1', 'sub': '1-6', 'Ris halo-C-alkyl;'}{'sup': '2', 'claim-text': [{'sub': '1-6', 'i) C-alkyl, and'}, {'sub': '3-8', 'ii) C-cycloalkyl;'}], 'Ris selected from'}{'sup': 3', '4', '6', '7', '9', '10', '23, 'R, R, R, R, R, Rand Rare H;'}{'sup': 5', '12', '13', '14, 'Ris phenyl substituted with R, Rand R;'}{'sup': '8', 'claim-text': i) H,', 'ii) hydroxy,', {'sup': 15', '16', '17, 'iii) phenyl substituted with R, Rand R;'}], 'Ris selected from'}{'sup': '11', 'claim-text': [{'sub': '1-6', 'sup': 21', '22, 'i) amino-Cs-alkyl substituted on the nitrogen atom by Rand R,'}, {'sup': 18', '19', '20, 'ii) phenyl substituted with R, Rand R,'}, {'sub': '1-6', 'sup': 18', '19', '20, 'iii) phenyl-C-alkyl substituted with R, Rand R,'}, {'sub': '3-8', 'sup': 18', '19', '20, 'iv) phenyl-C-cycloalkyl substituted with R, Rand R,'}, {'sub': '1-6', 'sup': 18', '19', '20, 'v) phenyl(halo)-C-alkyl substituted with R, Rand R,'}, {'sup': 18', '19', '20, 'vi) heteroaryl substituted with R, Rand R, wherein heteroaryl is selected from pyrazinyl, pyridinyl, pyrimidinyl and thiophenyl,'}], 'Ris selected rom'}{'sup': '12', 'claim-text': i) H, and', {'sub': '1-6', 'ii) C-alkoxy;'}], 'Ris selected from'}{'sup': 13', '14', '17', '20, 'R, R, Rand Rare H;'}{'sup': '15', 'claim-text': [{'sub': '1-6', 'i) C-alkyl,'}, 'ii) cyano,', 'iii) halogen, and', {'sub': '1-6', 'iv) carboxy-C-alkoxy;'}], 'Ris selected from'}{'sup': '16', 'claim-text': i) H, and', 'ii) halogen;, 'Ris selected from'}{'sup': '18', 'claim-text': i) H,', 'ii) halogen,', {'sub': '1-6', 'iii) halo-C-alkoxy,'}, 'iv) cyano,', {'sub': '1-6', 'v) amino substituted on the nitrogen atom by two C-alkyl,'}, {'sub': 1-6', '1-6, 'vi) C-alkoxycarbonyl-C-alkoxy,'}, {'sub': '1-6', 'vii) carboxy-C-alkoxy, and'}, 'viii) morpholinyl;, 'Ris selected from'}{'sup': '19', 'claim-text': i) H and', 'ii) halogen;, 'Ris selected from'}{'sup': '21 ...

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27-12-2018 дата публикации

TRIFLUOROMETHYLPROPANAMIDE DERIVATIVES AS HTRA1 INHIBITORS

Номер: US20180371016A1
Принадлежит: Hoffmann-La Roche Inc.

The invention provides novel compounds having the general formula (I) 2. A compound according to claim 1 , wherein{'sup': 2', '3', '4', '6', '7', '10', '23, 'claim-text': i) H,', {'sub': '1-6', 'ii) C-alkyl, and'}, {'sub': '3-8', 'iii) C-cycloalkyl;'}], 'R, R, R, R, R, Rand Rare independently selected from'}{'sup': '5', 'claim-text': [{'sup': 12', '13', '14, 'i) aryl substituted with R, Rand R,'}, {'sub': '1-6', 'sup': 12', '13', '14, 'ii) aryl-C-alkyl substituted with R, Rand R,'}, {'sup': 12', '13', '14, 'iii) heteroaryl substituted with R, Rand R, and'}, {'sub': '1-6', 'sup': 12', '13', '14, 'iv) heteroaryl-C-alkyl substituted with R, Rand R;'}], 'Ris selected from'}{'sup': '8', 'claim-text': i) H,', 'ii) hydroxy,', {'sub': 1-6', '1-6', '1-6', '1-6, 'sup': 15', '16', '17, 'iii) amino-C-alkyl substituted on the nitrogen atom by one or two substituents selected from H, C-alkylcarbonyl, C-alkoxycarbonyl, C-alkyl, arylcarbonyl and heteroarylcarbonyl, wherein arylcarbonyl and heteroarylcarbonyl are substituted with R, Rand R,'}, {'sub': 1-6', '1-6', '1-6, 'sup': 15', '16', '17, 'iv) aminocarbonyl substituted on the nitrogen atom by one or two substituents selected from H, C-alkylcarbonyl, C-alkoxycarbonyl, C-alkyl, arylcarbonyl and heteroarylcarbonyl, wherein arylcarbonyl and heteroarylcarbonyl are substituted with R, Rand R,'}, {'sub': 1-6', '1-6', '1-6', '1-6, 'sup': 15', '16', '17, 'v) aminocarbonyl-C-alkyl substituted on the nitrogen atom by one or two substituents selected from H, C-alkylcarbonyl, C-alkoxycarbonyl, C-alkyl, arylcarbonyl and heteroarylcarbonyl, wherein arylcarbonyl and heteroarylcarbonyl are substituted with R, Rand R,'}, 'vi) carboxy,', {'sub': '1-6', 'vii) carboxy-C-alkyl,'}, {'sub': '1-6', 'viii) C-alkoxy,'}, {'sub': '1-6', 'ix) C-haloalkoxy,'}, {'sub': '1-6', 'x) C-alkoxycarbonyl,'}, {'sub': 1', '1-6, 'xi) C-s-alkoxycarbonyl-C-alkyl,'}, {'sub': '3-8', 'xii) C-cycloalkyl,'}, {'sup': 15', '16', '17, 'xiii) aryl substituted with R, Rand R,'}, {' ...

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05-12-2019 дата публикации

Inhibitors of hepatitis c virus

Номер: US20190365748A1
Принадлежит: GILEAD PHARMASSET LLC

Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

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26-12-2019 дата публикации

Glycopeptide Derivatives For Use In The Treatment And/Or Prevention And/Or Attenuation of Fibrosis Diseases

Номер: US20190388501A1
Принадлежит: Tfchem SARL

The present invention relates to a compound of the following formula (I), as well as to a pharmaceutical composition comprising at least one compound of following formula (I) and at least one pharmaceutically acceptable excipient, for use in the treatment and/or prevention and/or attenuation of fibrosis diseases, in particular excessive scars such as keloids or hypertrophic scars.

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28-08-2003 дата публикации

Components for producing amphoteric liposomes

Номер: WO2003070735A2
Принадлежит: Novosom Ag

The invention relates to amphoteric lipids. According to the invention, at least one amphoteric group having an isoelectric point between 4 and 9 is substituted on a membranous or membrane-forming amphiphile. The invention also relates to liposomes containing said compounds.

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23-02-2006 дата публикации

Antiviral compounds

Номер: WO2006020276A2
Принадлежит: Gilead Sciences, Inc.

The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

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10-06-2010 дата публикации

Dimeric iap inhibitors

Номер: US20100143499A1
Автор: Stephen M. Condon
Принадлежит: TETRALOGIC PHARMACEUTICALS CORP

Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.

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29-09-2010 дата публикации

Iap의 억제제

Номер: KR100984459B1
Принадлежит: 제넨테크, 인크.

본 발명은 악성종양을 치료하기 위한 치료제로 유용한 하기 화학식 I의 화합물인 IAP의 신규한 억제제를 제공한다. <화학식 I> (식 중, X, Y, A, R 1 , R 2 , R 3 , R 4 , R 4 ', R 5 , R 5 ', R 6 및 R 6 '는 본원에 정의된 바와 같음). IAP 억제제, 카스파제, 아폽토시스 유도.

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20-03-2010 дата публикации

Enzyme inhibiting compounds

Номер: RU2384585C2
Принадлежит: Протеоликс, Инк.

FIELD: chemistry. SUBSTANCE: invention relates to α',β'-epoxides of peptides of formulae (III) and (IV) which inhibit chymotrypsin-like activity of 20S proteasome. EFFECT: increased effectiveness of the compounds. 19 cl, 29 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 384 585 (13) C2 (51) МПК ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ C07K C07K C07K A61K A61K A61K A61P 5/065 5/083 5/107 38/05 38/06 38/07 25/00 ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2006143664/04, 09.05.2005 (24) Дата начала отсчета срока действия патента: 09.05.2005 (73) Патентообладатель(и): ПРОТЕОЛИКС, ИНК. (US) 2 3 8 4 5 8 5 R U (56) Список документов, цитированных в отчете о поиске: RU 2192429 C2, 10.11.2002. ЕР 0411660 А, 06.02.1991. WO 01/28579 A2, 26.04.2001. US 6204257 B1, 20.03.2001. ELOFSSON M; ET AL "Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α',β'epoxyketones.", CHEMISTRY AND BIOLOGY, 1995 Vol:6, Nr:11, Page(s): 811-822. Kim К.В.; Myung J.; Sin N.; Crews С.М. (см. прод.) (85) Дата перевода заявки PCT на национальную фазу: 11.12.2006 (86) Заявка PCT: US 2005/016335 (09.05.2005) (87) Публикация PCT: WO 2005/111008 (24.11.2005) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ ФЕРМЕНТОВ (57) Реферат: Изобретение относится к α',β'-эпоксидам пептидов формулы (III) и (IV), которые ингибируют химотрипсино-подобную активность 20S протеасомы. 2 н. и 17 з.п. ф-лы. Ñòð.: 1 C 2 C 2 (45) Опубликовано: 20.03.2010 Бюл. № 8 2 3 8 4 5 8 5 (43) Дата публикации заявки: 20.06.2008 (72) Автор(ы): СМИТ Марк С. (US), ЛЭЙДИГ Гай Дж. (US), БОРЧАРДТ Рональд Т. (US), БЬЮНИН Барри А. (US), КРУЗ Крейг М. (US), МАССЕР Джон Х. (US), ШЕНК Кевин Д. (US), РЭЙДЕЛ Пегги А. (US) R U (30) Конвенционный приоритет: 10.05.2004 US 60/569,885 14.09.2004 US 60/610,040 07.12.2004 US 60/634,366 ru (2006.01) (2006.01) (2006 ...

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29-07-2010 дата публикации

Hcv protease inhibitors and uses thereof

Номер: WO2009082701A8
Принадлежит: AVILA THERAPEUTICS, INC.

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

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27-05-2011 дата публикации

Compounds and compositions as canal activating protease inhibitors

Номер: RU2419626C2
Принадлежит: Айрм Ллк

FIELD: medicine, pharmaceutics. ^ SUBSTANCE: present invention refers to compounds of formula ^ and to pharmaceutically acceptable salts, stereoisomers and to pharmaceutical compositions containing them which are effective for canal activating protease modulation, such as prostasin or trypsin. ^ EFFECT: preparing new compounds and applying such compounds for prostasin or trypsin inhibition. ^ 17 cl, 1 tbl, 258 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 419 626 (13) C2 (51) МПК C07K 5/08 (2006.01) A61K 38/06 (2006.01) A61P 11/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (24) Дата начала отсчета срока действия патента: 16.05.2007 Приоритет(ы): (30) Конвенционный приоритет: 23.05.2006 US 60/802,983 22.11.2006 US 60/860,604 (73) Патентообладатель(и): АЙРМ ЛЛК (BM) 2 4 1 9 6 2 6 R U (56) Список документов, цитированных в отчете о поиске: WO 00/44733 A1, 03.08.2000. WO 2005/023 804 A1, 17.03.2005. EP 0291234 A2, 17.11.1988. COSTANZO M J ET AL: "Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone" JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY 2003, vol.46, (см. прод.) C 2 C 2 (45) Опубликовано: 27.05.2011 Бюл. № 15 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.12.2008 (86) Заявка PCT: US 2007/069059 (16.05.2007) (87) Публикация заявки РСТ: WO 2007/137080 (29.11.2007) Адрес для переписки: 101000, Москва, М.Златоустинский пер., 10, кв.15, "ЕВРОМАРКПАТ", пат.пов. М.Б.Веселицкому (54) СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕАЗЫ, АКТИВИРУЮЩЕЙ КАНАЛЫ (57) Реферат: Настоящее изобретение относится к соединениям формулы (1) и фармацевтически приемлемым солям, стереоизомерам и содержащим их фармацевтическим композициям, которые являются полезными для модулирования протеазы, активирующей каналы, такой как простазин и трипсин, а также и к способам ...

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12-03-2007 дата публикации

Stabilized vitamin c derivatives with a peptide molecule, preparation method thereof, and composition containing the same

Номер: KR100691540B1
Принадлежит: 주식회사 펩트론

A vitamin C derivative is provided to show excellent stability and skin permeation by introducing a phosphoric acid derivative and a collagen generating peptide thereinto. The vitamin C derivative is represented by the formula(1), where each R1 and R2 is independently OH or a group represented by the structural formula(1-1)(where X is -OC(O)(CH2)mC(O)-, a group represented by the structural formula(1-2) is a peptide where at least one amino acid residue selected from the group consisting of glycine, lysine, histidine, serine, proline, hydroxyproline, threonine, glutamic acid, methionine, glutamine and arginine is amide-coupled, R is a side branch of the amino acid residue, n is an integer from 3 to 10, and m is an integer from 2 to 5), and W is a group represented by the structural formula(1-3) or glucose(where R3 is -N(CH3)2, -N(CH2CH3)2, -NHCH2CH2CH3, -NHCH2C6H5 or -OH). The skin whitening composition comprises at least one of the vitamin C derivative or a pharmaceutically acceptable salt thereof.

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30-09-2015 дата публикации

HEPATITIS C VIRUS INHIBITORS

Номер: EA201590770A1

Описаны ингибиторы вируса гепатита С, имеющие общую формулу (I)Также описаны композиции, содержащие эти соединения, и способы применения этих соединений для ингибирования HCV. Hepatitis C virus inhibitors are described having the general formula (I) Compositions containing these compounds and methods for using these compounds to inhibit HCV are also described.

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27-07-2014 дата публикации

Inhibitors of protease of hepatitis c virus and their application

Номер: RU2523790C2

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to compounds, which can be used as inhibitors of protease of hepatitis C virus, pharmaceutical compositions, containing the said compounds, and methods of their application. EFFECT: obtaining compounds which can be used as inhibitors of protease of hepatitis C virus. 41 cl, 10 dwg, 7 tbl, 26 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07K 5/06 C07K 5/08 A61K 38/06 A61K 38/08 A61P 31/14 (13) 2 523 790 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2010125120/04, 19.12.2008 (21)(22) Заявка: (24) Дата начала отсчета срока действия патента: 19.12.2008 Приоритет(ы): (30) Конвенционный приоритет: US US US US 61/016,110; 61/016,473; 61/075,001; 61/098,675 (73) Патентообладатель(и): АВИЛА ТЕРАПЬЮТИКС, ИНК. (US) (45) Опубликовано: 27.07.2014 Бюл. № 21 (56) Список документов, цитированных в отчете о поиске: RU 2298001 С2, 27.04.2007 . WO (85) Дата начала рассмотрения заявки PCT на национальной фазе: 21.07.2010 C 2 C 2 2005037214 A2, 28.04.2005. US 6869964 B2, 22.03.2005. US 2004180815 A1, 16.09.2004 . US 2004162318 A1, 19.08.2004 . US 2003/064499 A1, 03.04.2003. US 2006/121563 A1, 08.06.2006 (86) Заявка PCT: 2 5 2 3 7 9 0 US 2008/087736 (19.12.2008) R U 2 5 2 3 7 9 0 (43) Дата публикации заявки: 27.01.2012 Бюл. № 3 R U 21.12.2007 23.12.2007 23.06.2008 19.09.2008 (72) Автор(ы): НИУ Декианг (US), ПЕТТЕР Рассел (US), СИНГХ Джасвиндер (US), КЛЮГ Артур Ф. (US), КЬЯО Ликсин (US) (87) Публикация заявки PCT: WO 2009/082701 (02.07.2009) Адрес для переписки: 190000, Санкт-Петербург, ул. Малая Морская, 15, офис 5, ВОХ 1125, ООО "ПАТЕНТИКА", М.И.Ниловой (54) ИНГИБИТОРЫ ПРОТЕАЗЫ ВИРУСА ГЕПАТИТА С И ИХ ПРИМЕНЕНИЕ (57) Реферат: Изобретение относится к соединениям, содержат указанные соединения, и способам их которые могут использоваться в качестве применения. 9 н. и 32 з.п. ф-лы, 10 ил., 7 табл., 26 ингибиторов протеазы вируса ...

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27-07-2009 дата публикации

Новые производные 2-азетидинона, полезные в лечении гиперлипидемических состояний

Номер: RU2007147339A

1. Соединение формулы (I) ! ! где X представляет собой -СН2-, -СН2СН2- или -СН2СН2СН2-; ! Y представляет собой -СН2- или -O-; ! Y1 представляет собой -СН2- или -O-; ! где по меньшей мере один из Y и Y1 представляет собой -СН2-; ! R1 представляет собой водород, C1-6алкил, С3-6-циклоалкил или арил; ! R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный C1-6алкил, С3-6циклоалкил или арил; где указанный С1-6алкил возможно может быть замещен одним или более чем одним гидрокси, амино, гуанидино, циано, карбамоилом, карбокси, C1-6алкокси, арил С1-6алкокси, (С1-С4алкил)3Si, N-(С1-6алкил)амино, N,N-(С1-6алкил)2амино, С1-6алкилS(O)а, С3-6циклоалкилом, арилом или арилС1-6алкилS(O)а, где а равно 0-2; и где любая арильная группа возможно может быть замещена одним или двумя заместителями, выбранными из галогено, гидрокси, C1-6алкила, С1-6алкокси или циано; ! R4 представляет собой водород, C1-6алкил, галогено или C1-6алкокси; ! R6 и R9 представляют собой водород, C1-6алкил или арилС1-6алкил; ! где R5 и R2 могут образовывать кольцо с 2-7 атомами углерода, и где R6 и R2 могут образовывать кольцо с 3-6 атомами углерода; ! или его фармацевтически приемлемые соль, сольват, сольват такой соли или пролекарство. ! 2. Соединение формулы (I2) ! ! где X представляет собой -СН2-, -СН2СН2- или -СН2СН2СН2-; ! Y представляет собой -СН2- или -O-; ! Y1 представляет собой -СН2- или -O-; ! где по меньшей мере один из Y и Y1 представляет собой -СН2-; ! R1 представляет собой водород, С1-6алкил, С3-6циклоалкил или арил; ! R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный C1-6алкил, С3-6циклоалкил или арил; где указанный С1-6алкил возможно может быть замещен одним или более чем одним гидрокси, амино, гуанидино, циа (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2007 147 339 (13) A (51) МПК C07D 405/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: ...

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10-01-2010 дата публикации

PEPTIDE DERIVATIVES

Номер: RU2008126266A
Автор: Анил К. САКСЕНА, Анил К. САКСЕНА (US), Ашит К. ГАНГУЛИ, Ашит К. ГАНГУЛИ (US), Ашок АРАСАППАН, Ашок АРАСАППАН (US), Бама САНТАНАМ, Бама САНТАНАМ (US), Ванли ВУ, Ванли ВУ (US), Вийур Мупил ГИРИЯВАЛЛАБХАН, Вийур Мупил ГИРИЯВАЛЛАБХАН (US), Жаонинг ЖУ, Жаонинг ЖУ (US), Йи-Тсунг ЛИУ, Йи-Тсунг ЛИУ (US), Кевин Кс ЧЕН, Кевин Кс ЧЕН (US), КОРМИК Джинпинг Л. МАК, КОРМИК Джинпинг Л. МАК (US), Маргерита ЛИМ-ВИЛБИ, Маргерита ЛИМ-ВИЛБИ (US), Одил Эстер ЛЕВИ, Одил Эстер ЛЕВИ (US), Патрик Э. ПИНТО, Патрик Э. ПИНТО (US), Рассел И. ПАЙК, Рассел И. ПАЙК (US), Реймонд Дж. ЛАВИ, Реймонд Дж. ЛАВИ (US), Сиска ХЕНДРАТА, Сиска ХЕНДРАТА (US), Скотт Джеффри КЕМП, Скотт Джеффри КЕМП (US), Срикант ВЕНКАТРАМАН, Срикант ВЕНКАТРАМАН (US), Стефан Л. БОГЕН, Стефан Л. БОГЕН (US), Сьюзан Й. ТАМУРА, Сьюзан Й. ТАМУРА (US), Тейал Н. ПАРЕХ, Тейал Н. ПАРЕХ (US), Тин-Яу ЧЭН, Тин-Яу ЧЭН (US), Ф. Джордж НЬЕРОГЕ, Ф. Джордж НЬЕРОГЕ (US), Фрэнк БЕННЕТ, Фрэнк БЕННЕТ (US), Хайян ВАНГ, Хайян ВАНГ (US), Хенри Э. ВАККАРО, Хенри Э. ВАККАРО (US), Эдвин И. ДЖАО, Эдвин И. ДЖАО (US), Юхуа ХУАНГ, Юхуа ХУАНГ (US)

1. Производное пептида общей структуры, представленной формулой I ! ! где ! Y выбран из группы, включающей следующие фрагменты: алкил, алкиларил, гетероалкил, гетероарил, арилгетероарил, алкилгетероарил, циклоалкил, алкилоксил, алкиларилоксил, арилоксил, гетероарилоксил, гетероциклоалкилоксил, циклоалкилоксил, алкиламинную, ариламинную, алкилариламинную, гетероариламинную, циклоалкиламинную и гетероциклоалкиламинную группы при условии, что Y может необязательно содержать X11 или X12 в качестве заместителей; ! X11 означает алкил, алкенил, алкинил, циклоалкил, циклоалкилалкил, гетероциклический остаток, гетероциклоалкил, арил, алкиларил, арилалкил, гетероарил, алкилгетероарил или гетероарилалкил при условии, что Х может необязательно содержать X11 в качестве заместителя; ! X12 означает гидроксил, алкоксил, арилоксил, тиоил, алкилтиоил, арилтиоил, амино-, алкиламино-, ариламиногруппу, алкилсульфонил, арилсульфонил, алкилсульфонамидную, арилсульфонамидную группу, карбоксил, карбалкоксил, карбоксамидную, алкоксикарбониламиногруппу, алкоксикарбонилоксил, алкилуреидную, арилуреидную группу, галоген, циано- или нитрогруппу при условии, что указанные алкил, алкоксил и арил могут дополнительно необязательно содержать в качестве заместителей фрагменты, независимо выбранные из группы значений для ! X12; ! R1 означает COR5, где R5 означает COOR8, CONR9R10, СF3, С2F5, С3F7, CF2R6, или R6, где R6, R8, R9 и R10 независимо выбраны из группы, включающей Н, алкил, арил, гетероалкил, гетероарил, циклоалкил, арилалкил, гетероарилалкил, [CH(R1')]pCOOR11, [CH(R1')]pCONR12R13, [CH(R1')]pSO2R11, [CH(R1')]pCOR11, [CH(R1')]pCH(OH)R11, CH(R1')CONHCH(R2')COOR11, CH(R1')CONHCH(R2')CONR12R13, CH(R1')CONHCH(R2')R', CH(R1')CONHCH(R2')CONHCH(R3')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONR РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 126 266 (13) A (51) МПК C07K 7/02 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ...

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19-05-1987 дата публикации

Intravenous or intraperitoneal administration of a tripeptide compound for treating cancer

Номер: US4666887A
Автор: Augusto De Barbieri
Принадлежит: Proter SpA

A pharmaceutical composition for use in the treatment of malignant tumor cells in laboratory animals is disclosed. The pharmaceutical composition uses a pharmaceutically acceptable excipient with a tripeptide compound as the active ingredient. The tripeptide compound is formed from dichlorodiethylaminophenylalanine, parafluorophenylalanine, and methione.

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22-07-2009 дата публикации

Diamine derivatives

Номер: KR100908966B1

화학식 1 Formula 1 [식 중, R 1 및 R 2 는 수소원자 등을, Q 1 은 치환기를 갖거나 갖지 않는 포화 또는 불포화 5~6원의 고리형상 탄화수소기 등을, Q 2 는 단일결합 등을, Q 3 는 하기의 기 [Wherein, R 1 and R 2 represent a hydrogen atom, Q 1 represents a saturated or unsaturated 5-6 membered cyclic hydrocarbon group with or without a substituent, Q 2 represents a single bond and Q 3 represents The following flag (기 중, Q 5 는 탄소수 1~8의 알킬렌기 등을 나타낸다.)를, T 0 및 T 1 은 카르보닐기 등을 나타낸다.]로 표시되는 화합물, 그의 염, 그들의 용매화물 또는 그들의 N-옥시드. (Wherein, Q 5 represents an alkylene group having 1 to 8 carbon atoms, etc.), and T 0 and T 1 represent a carbonyl group or the like.], A compound thereof, a salt thereof, a solvate thereof or an N-oxide thereof . 뇌경색, 뇌색전, 심근경색, 협심증, 폐경색, 폐색전, 버거씨병, 심부 정맥 혈전증, 범발성 혈관내 응고증후군, 인공밸브/관절 치환 후의 혈전형성, 혈행 재건 후의 혈전형성 및 재폐색, 전신성 염증성 반응증후군(SIRS), 다장기부전(MODS), 체외 순환시의 혈전형성 또는 채혈시 혈액응고의 예방제 및/또는 치료제로서 유용하다. Cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Burger's disease, deep vein thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve / joint replacement, thrombus formation and reclosure after thrombolysis, systemic inflammatory response It is useful as a prophylactic and / or therapeutic agent for syndrome (SIRS), multi-organ failure (MODS), thrombus formation in extracorporeal circulation or blood coagulation in blood collection.

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27-07-2009 дата публикации

NEW 2-AZETIDINONE DERIVATIVES FOR THE TREATMENT OF HYPERLIPIDEMIC DISEASES

Номер: RU2007147344A

1. Соединение формулы (I): ! ! где R1 представляет собой водород, С1-6алкил, C3-6циклоалкил или арил; ! R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный С1-6алкил, C3-6циклоалкил или арил; где указанный С1-6алкил возможно может быть замещен одним или более чем одним гидрокси, амино, гуанидино, циано, карбамоилом, карбокси, С1-6алкокси, арилС1-6алкокси, (С1-С4алкил)3Si, N-(С1-6алкил)амино, N,N-(С1-6алкил)2амино, С1-6алкилS(O)а, С3-6циклоалкилом, арилом или арилС1-6алкилS(O)а, где а равно 0-2; и где любая арильная группа возможно может быть замещена одним или двумя заместителями, выбранными из галогено, гидрокси, С1-6алкила, С1-6алкокси или циано; ! R3 представляет собой водород, алкил, галогено, С1-6алкокси или С1-6алкилS-; ! R4 представляет собой водород, С1-6алкил, галогено или С1-6алкокси; ! R6 и R9 представляют собой водород, С1-6алкил или арилС1-6алкил; ! где R5 и R2 могут образовывать кольцо с 2-7 атомами углерода, и где R6 и R2 могут образовывать кольцо с 3-6 атомами углерода; ! или его фармацевтически приемлемые соль, сольват, сольват такой соли или пролекарство. ! 2. Соединение формулы (I2): ! ! где R1 представляет собой водород, С1-6алкил, С3-6циклоалкил или арил; ! R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный С1-6алкил, гидрокси, амино, гуанидино, циано, карбамоил, карбокси, С1-6алкокси, арилС1-6алкокси, (С1-С4алкил)3Si, N-(С1-6алкил)амино, N,N-(С1-6алкил)2амино, С1-6алкилS(O)а, C3-6циклоалкил, арил или арилС1-6алкилS(O)а, где а равно 0-2; и где любая арильная группа возможно может быть замещена одним или двумя заместителями, выбранными из галогено, гидрокси, С1-6алкила, С1-6алкокси или циано; ! R3 представляет собой водород, алкил, галогено, (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2007 147 344 (13) A (51) МПК C07D 205/08 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2007147344/04, 21.06. ...

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20-05-2009 дата публикации

Novel peptides as inhibitors of hepatitis c virus ns3 serine protease

Номер: RU2355700C2

FIELD: chemistry. SUBSTANCE: invention claims novel compounds with inhibition effect on HCV (hepatitis C virus) protease, and methods of obtaining the claimed compounds. EFFECT: pharmaceutical compositions including these compounds, and methods of compound application in treatment of HCV protease related diseases. 23 cl, 5 tbl, 39 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 355 700 (13) C2 (51) МПК C07K 7/02 (2006.01) C07K 5/02 (2006.01) C07K 5/08 (2006.01) A61K 38/55 (2006.01) A61K 38/08 (2006.01) A61P 31/14 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2003105217/04, 19.07.2001 (24) Дата начала отсчета срока действия патента: 19.07.2001 (43) Дата публикации заявки: 10.09.2004 2 3 5 5 7 0 0 R U (85) Дата перевода заявки PCT на национальную фазу: 21.02.2003 (86) Заявка PCT: US 01/22678 (19.07.2001) (87) Публикация PCT: WO 02/08244 (31.01.2002) Адрес для переписки: 105064, Москва, а/я 88, В.П.Квашнину (73) Патентообладатель(и): ШЕРИНГ КОРПОРЕЙШН (US), ДЕНДРЕОН КОРПОРЕЙШН (US) (54) НОВЫЕ ПЕПТИДЫ КАК ИНГИБИТОРЫ NS3-СЕРИНПРОТЕАЗЫ ВИРУСА ГЕПАТИТА С (57) Реферат: В настоящем изобретении раскрыты новые соединения, которые обладают способностью ингибировать протеазу HCV (вируса гепатита С), а также способы получения таких соединений. В другом варианте осуществления в настоящем изобретении раскрыты фармацевтические композиции, включающие такие соединения, а также способы их применения для лечения заболеваний, связанных с протеазой HCV. 6 н. и 17 з.п. ф-лы, 5 табл. (56) (продолжение): the hepatitis С virus serine protease." BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, v.8, № 19, p.2719-2724. Ñòðàíèöà: 1 ru C 2 C 2 (56) Список документов, цитированных в отчете о поиске: RU 2104284 C1, 10.02.1998. WO 9907734 A3, 18.02.1999. WO 9817679 A1, 30.04.1998. HAN; WEI; et al. "α-Ketoanides, α-ketoesters and diketones as HCV NS3 protease inhibitors." BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ...

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29-09-2011 дата публикации

Compounds and compositions as channel activating protease inhibitors

Номер: KR101069051B1
Принадлежит: 아이알엠 엘엘씨

본 발명은 채널 활성화 프로테아제를 조절하는데 유용한 화학식 1의 화합물, 및 그의 제약상 허용되는 염, 수화물, 용매화물, 입체이성질체 및 제약 조성물, 및 비제한적으로 프로스타신, PRSS22, TMPRSS11 (예를 들어, TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), 매트립타제 (MTSP-1), CAP2, CAP3, 트립신, 카텝신 A 또는 호중구 엘라스타제를 비롯한 채널 활성화 프로테아제와 관련된 증상의 치료, 개선 또는 예방을 위한 이러한 화합물의 사용 방법을 제공한다. The present invention provides compounds of formula (1) useful for modulating channel activating proteases, and pharmaceutically acceptable salts, hydrates, solvates, stereoisomers and pharmaceutical compositions thereof, and, without limitation, prostine, PRSS22, TMPRSS11 (eg, Treatment of symptoms associated with channel activation protease, including TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), Matriptase (MTSP-1), CAP2, CAP3, Trypsin, Cathepsin A or Neutrophil elastase, Provided are methods of using these compounds for improvement or prevention. 채널 활성화 프로테아제 억제제, 프로스타신, 기관지 상피 세포 Channel activated protease inhibitors, prostacins, bronchial epithelial cells

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10-01-2008 дата публикации

Diamine derivatives

Номер: RU2314303C2

FIELD: organic chemistry, medicine, hematology. SUBSTANCE: invention relates to novel compounds or their salts that inhibit blood coagulation activated factor X and elicit strong anti-coagulating effect. Compounds are represented by one of the following formulae: Also, invention relates to a medicinal agent, inhibitor of blood coagulation activated factor X, anti-coagulating agent, medicinal composition comprising indicated compounds, to their using for preparing a medicinal agent, inhibitors and anti-coagulating agent. EFFECT: valuable medicinal properties of compounds. 9 cl, 1 tbl, 794 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 314 303 (13) C2 (51) ÌÏÊ C07D 401/12 C07D 417/12 C07D 487/04 C07D 495/04 C07D 498/04 C07D 513/04 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,A61K 31/428 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ A61P 7/02 A61P 9/10 A61P 29/00 (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2004106625/04, 08.08.2002 (30) Êîíâåíöèîííûé ïðèîðèòåò: 09.08.2001 JP 2001-243046 20.06.2002 JP PCT/JP02/06141 2 3 1 4 3 0 3 R U (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: WO 9845262 A1, 15.10.1998. WO 9204017 A1, 19.03.1992. WO 8607257 A2,18.12.1986. WO 0009480 A1, 24.02.2000. WO 0064902 A2, 02.11.2000. ÅÐ 0947510 Â1, 06.10.1999. WO 9932225 A2, 01.07.1999. WO 9710853 A2, 27.03.1997. FRANCESCO GASPARRINI et al. Enantioselective chromatography on brush-type chiral stationary phases containing totally synthetic (ñì. ïðîä.) (73) Ïàòåíòîîáëàäàòåëü(è): ÄÀÉÈÒÈ ÔÀÐÌÀÑÜÞÒÈÊÀË ÊÎ., ËÒÄ. (JP) C 2 C 2 (45) Îïóáëèêîâàíî: 10.01.2008 Áþë. ¹ 1 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 09.03.2004 (86) Çà âêà PCT: JP 02/08119 (08.08.2002) (87) Ïóáëèêàöè PCT: WO 03/016302 (27.02.2003) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) ÏÐÎÈÇÂÎÄÍÛÅ ÄÈÀÌÈÍÀ (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê íîâûì ñîåäèíåíè ì èëè èõ ñîë ì, êîòîðûå èíãèáèðóþò àêòèâèðîâàííûé 2 3 1 4 3 0 3 (43) ...

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20-07-2009 дата публикации

ORGANIC COMPOUNDS

Номер: RU2007147959A

1. Соединение формулы (I): ! ! где ! R1 представляет собой Н или C1-C4 алкил; ! R2 представляет собой Н или C1-C4 алкил, который является незамещенным или замещенным одним или несколькими заместителями, выбранными из галогена, -ОН, -SH, -ОСН3, -SСН3, -CN, -SCN и нитро; ! R3 представляет собой Н, C1-C4 алкил, -СF3, -C2F5, -(СН2)-Z, или R2 и R3 вместе с атомом азота образуют С3-С6 гетероалифатическое кольцо; ! Z представляет собой Н, -ОН, F, Cl, -СН3; -СF3, -CH2Cl, -CH2F или -(СН2)OН; ! Х представляет собой моноциклическую или бициклическую структуру, ! выбранную из группы, состоящей из: ! ! где ! А представляет собой -(СН2), -СН-, N, О или S; ! X1 представляет собой О, S или NRa; ! R4, Ra и Rb независимо представляют собой Н; C1-C16 линейный или разветвленный алкил; C1-C16 алкенил; C1-C16 алкинил или C1-C16 циклоалкил; -(СН2)0-6-фенил; (СН2)0-6-гет; -O-C1-C16 линейный или разветвленный алкил, -S-C1-C16 линейный или разветвленный алкил; -N-C1-С16 линейный или разветвленный алкил; -O-C1-C16 алкенил; -S-C1-C16 алкенил; -N-C1-C16 алкенил -O-C1-C16 циклоалкил; -N-C1-C16 циклоалкил; -S-C1-С16 циклоалкил; -O-(СН2)0-6-фенил; -Н-(СН2)0-6-фенил; -S-(CH2)0-6-фенил; -O-(СН2)0-6-гет; -N-(CH2)0-6-гeт или -S-(СН2)0-6-гет, где алкил, циклоалкил и фенил являются незамещенными или замещенными; или R4 и Ra могут образовывать кольцо; ! U представляет собой -R5; -СН(R5)(R6); -СО-Н(R5)(R6); -CO-O(R5); -CO-S(R5); ! CS-N(R5)(R6); -N(R5)-CO-N(R5)(R6); -C1-C5 алкил-N(R5)(R6);-С1-С5-алкил-O(R6) или или -C1-C5 алкил-S(O)n(R6), где n обозначает 0, 1 или 2; ! R5 представляет собой Н; C1-С10 алкил; С3-С7 циклоалкил; -(СН2)1-6-С3-С7 циклоалкил; -C1-С10алкиларил; -(СН2)0-6-фенил; -(СН2)0-6-С3-С7 циклоалкил-(СН2)0-6-фенил; -(СН2)0-4СН-((СН2)1-4-фенил)2; -(СН2)0-6-СН(фенил)2; -C(O)-C1-C10 алкил; -С(O)-(СН2)1-6-С3-С7 циклоалкил; -С(O)-(СН2)0-6-фенил; -(СН2)1-6-гет; -С(O)-(СН2)1-6-гет; -(СR7R8)0-2-арил-V-арил; CHR6C(O)N(R12)(R13); C(O)-NH-CH(R11)(R14), или R5 представля� (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11 ...

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07-06-1995 дата публикации

Novel biologically active compounds and compositions,their use and derivation

Номер: GB9508195D0
Автор:

This invention relates to derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by general formula I, wherein Y, n, R1, R2, R3, R6, R7, R70, R71, R72, R74, and R75 are as defined in the specification.

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30-09-2009 дата публикации

Diamine derivative

Номер: CN100545160C
Принадлежит: Daiichi Pharmaceutical Co Ltd

由通式(1)表示的化合物,其盐,溶剂化物或N-氧化物:Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -N(R 2 )-T 1 -Q 4 (1)其中,R 1 和R 2 是氢原子等;Q 1 是可被取代的饱和或不饱和的5-或6-元环烃基等;Q 2 是单键等;Q 3 下面基团,其中,Q 5 是有1-8个碳原子的亚烷基等;T 0 和T 1 是羰基等。该化合物可用作预防和/或治疗脑梗死、脑栓塞、心肌梗死、心绞痛、肺梗塞形成、肺栓塞、伯格氏疾病、重度静脉血栓形成、弥漫性血管内凝血综合症、瓣膜替换术或关节置换后的血栓形成、血管形成术的血栓形成和再闭合、系统炎性响应并发症(SIRS)、多器官功能紊乱并发症(MODS)、体外循环期间的血栓形成、或在血液采集时血凝的药剂。

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21-03-2007 дата публикации

Boronic ester and acid compounds, synthesis and uses

Номер: CN1305475C
Принадлежит: Millennium Pharmaceuticals Inc

本发明公开了一种降低动物中蛋白质降解速率的方法,包括使所述动物的细胞与特定的硼酸酯和硼酸化合物接触。还公开了新的硼酸酯和硼酸化合物,其制备和用途。

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17-02-2009 дата публикации

Methods of using macrocyclic modulators of the ghrelin receptor

Номер: US7491695B2
Принадлежит: Tranzyme Pharma Inc

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

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20-01-2008 дата публикации

Hepatitis c virus inhibitors

Номер: RU2315039C1

FIELD: organic chemistry, virology. SUBSTANCE: invention relates to heterocyclic compounds comprising five- and six-membered heterocycles with one or two nitrogen atoms and representing inhibitors of hepatitis C virus. Invention provides synthesis of novel compounds possessing valuable biological properties. EFFECT: valuable biological and medicinal properties of compounds. 12 cl, 2 tbl, 472 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 315 039 (13) C1 (51) ÌÏÊ C07D 207/08 (2006.01) A61K 31/40 (2006.01) A61P 1/16 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2006134702/04, 20.05.2003 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 20.05.2003 (45) Îïóáëèêîâàíî: 20.01.2008 Áþë. ¹ 2 (73) Ïàòåíòîîáëàäàòåëü(è): ÁÐÈÑÒÎË-ÌÀÅÐÑ ÑÊÂÈÁÁ ÊÎÌÏÀÍÈ (US) (62) Íîìåð è äàòà ïîäà÷è ïåðâîíà÷àëüíîé çà âêè, èç êîòîðîé äàííà çà âêà âûäåëåíà: 2004137480 20.05.2003 (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê ãåòåðîöèêëè÷åñêèì ñîåäèíåíè ì, ñîäåðæàùèì ï òè- è øåñòè÷ëåííûå ãåòåðîöèêëû ñ îäíèì èëè äâóì àòîìàìè àçîòà, âë þùèìñ èíãèáèòîðàìè âèðóñà ãåïàòèòà Ñ. Òåõíè÷åñêèé ðåçóëüòàò - ïîëó÷åíû íîâûå ñîåäèíåíè , îáëàäàþùèå ïîëåçíûìè áèîëîãè÷åñêèìè ñâîéñòâàìè. 12 í.ï. ô-ëû, 2 òàáë. R U 2 3 1 5 0 3 9 (54) ÈÍÃÈÁÈÒÎÐÛ ÂÈÐÓÑÀ ÃÅÏÀÒÈÒÀ Ñ Ñòðàíèöà: 1 RU C 1 C 1 Àäðåñ äë ïåðåïèñêè: 119034, Ìîñêâà, Ïðå÷èñòåíñêèé ïåð., 14, ñòð. 1, 4-é ýòàæ, "Ãîóëèíãç Èíòåðíýøíë Èíê.", ïàò.ïîâ. Þ.Â.Äåìåíòüåâîé, ðåã.¹ 560 2 3 1 5 0 3 9 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: WO 00/09543 A, 24.02.2000. RU 93056617 A, 27.12.1997. R U (30) Êîíâåíöèîííûé ïðèîðèòåò: 20.05.2002 (ïï.1-12) US 60/382,055 (72) Àâòîð(û): ÂÀÍà Êñèàíã-äîíã Ýëàí (US), ÑÀÍ Ëè-Êâàíã (US), ÑÈÒ Ñèíã-Þåí (US), ÑÈÍ Íàé (US), ÑÊÎËÀ Ïîë Ìàéêë (US), ÕÅÂÀÂÀÑÀÌ Ïè ñåíà (US), ÃÓÄ Ýíäðþ ×àðëç (US), ×ÅÍ ßí (US), ÊÝÌÏÁÅËË Äæåôôðè Ýëëåí (US) RUSSIAN FEDERATION (19) RU (11) 2 315 039 (13) C1 (51) Int. Cl. C07D 207/08 (2006.01) A61K 31/40 (2006.01) A61P 1/16 (2006.01) ...

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NEW 2-ASETHIDINONE DERIVATIVES AS CHOLESTEROL SUCTION INHIBITORS FOR TREATMENT OF HYPERLIPIDEMIC CONDITIONS

Номер: RU2007147346A

1. Соединение формулы (I) ! ! где: R1 представляет собой водород, С1-6алкил, С3-6циклоалкил или арил; ! R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный C1-6алкил, С3-6циклоалкил или арил; где указанный С1-6алкил возможно может быть замещен одним или более чем одним гидрокси, амино, гуанидино, циано, карбамоилом, карбокси, С1-6алкокси, арилС1-6алкокси, (С1-С4алкил)3Si, N-(С1-6алкил)амино, N,N-(С1-6алкил)2амино, С1-6алкилS(O)а, С3-6циклоалкилом, арилом или арилС1-6алкилS(O)а, где а равно 0-2; и где любая арильная группа возможно может быть замещена одним или двумя заместителями, выбранными из галогено, гидрокси, С1-6алкила, С1-6алкокси или циано; ! R4 представляет собой водород, С1-6алкил, галогено или C1-6алкокси; ! R6 и R9 представляют собой водород, C1-6алкил или арилС1-6алкил; ! где R5 и R2 могут образовывать кольцо с 2-7 атомами углерода, и где R6 и R2 могут образовывать кольцо с 3-6 атомами углерода; ! или его фармацевтически приемлемые соль, сольват, сольват такой соли или пролекарство. ! 2. Соединение формулы (I2) ! ! где R1 представляет собой водород, С1-6алкил, С3-6циклоалкил или арил; R2, R5, R7 и R8 независимо представляют собой водород, разветвленный или неразветвленный С1-6алкил, где указанный С1-6алкил возможно может быть замещен одним или более чем одним гидрокси, амино, гуанидино, циано, карбамоилом, карбокси, C1-6алкокси, арилС1-6алкокси, (С1-С4алкил)3Si, N-(С1-6алкил)амино, N,N-(С1-6алкил)2амино, С1-6алкилS(O)а, С3-6циклоалкилом, арилом или арилС1-6алкилS(O)а, где а равно 0-2; и где любая арильная группа возможно может быть замещена одним или двумя заместителями, выбранными из галогено, гидрокси, С1-6алкила, C1-6алкокси или циано; ! R4 представляет собой водород, C1-6алкил (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2007 147 346 (13) A (51) МПК C07D 405/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2007147346/04, 21.06.2006 ( ...

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MACROCYCLIC PEPTIDES AS HCV NS3-PROTEASE INHIBITORS

Номер: RU2008107972A

1. Соединение формулы (I): ! ! в которой: ! n равно 1 или 2; ! R1 представляет собой CO2R10, CONR10SO2R6, CONR10SO2NR8R9 или тетразолил; ! R2 представляет собой C1-C6алкил, C2-C6алкенил или C3-C8циклоалкил, где упомянутые алкил, алкенил или циклоалкил необязательно замещены 1-3 галогенами; ! R3 представляет собой C1-C8алкил, C3-C8циклоалкил, C3-C8циклоалкил(C1-C8)алкил, арил(C1-C8)алкил или Het, где арил представляет собой фенил или нафтил, и упомянутые алкил, циклоалкил или арил необязательно замещены 1-3 заместителями, выбранными из группы, состоящей из галогена, OR10, SR10, N(R10)2, N(C1-C6алкил)O(C1-C6алкил), C1-C6алкила, C1-C6галогеналкила, галоген(C1-C6алкокси), NO2, CN, CF3, SO2(C1-C6алкил), S(O)(C1-C6алкил), NR10SO2R6, SO2N(R6)2, NHCOOR6, NHCOR6, NHCONHR6, CO2R10, C(O)R10 и CON(R10)2; ! Het представляет собой 5-6-членное насыщенное циклическое кольцо, содержащее 1, 2 или 3 гетероатома, выбранных из N, O и S, где упомянутое кольцо необязательно замещено 1-3 заместителями, выбранными из группы, состоящей из галогена, OR10, SR10, N(R10)2, N(C1-C6алкил)O(C1-C6алкил), C1-C6алкила, C1-C6галогеналкила, галоген(C1-C6алкокси), NO2, CN, CF3, SO2(C1-C6алкил), S(O)(C1-C6алкил), NR10SO2R6, SO2N(R6)2, NHCOOR6, NHCOR6, NHCONHR6, CO2R10, C(O)R10 и CON(R10)2; ! R4 представляет собой H, C1-C8алкил, C3-C8циклоалкил(C1-C8)алкил или арил(C1-C8)алкил; где арил представляет собой фенил или нафтил, и упомянутые алкил, циклоалкил или арил необязательно замещены 1-3 заместителями, выбранными из группы, состоящей из галогена, OR10, SR10, N(R10)2, N(C1-C6алкил)O(C1-C6алкил), C1-C6алкила, C1-C6галогеналкила, галоген(C1-C6алкокси), NO2, CN, CF3, SO2(C1-C6алкил), S(O)(C1-C6алкил), NR10SO2R6, SO2N(R6)2, NHCOOR6, NHCOR6, NHCONHR6, CO2R10, C(O)R10 и CON(R10)2; ! R5 представляет собой H, галоген, OH, C1-C6алкокси, C1-C6алкил, CN, CF3, SR10, SO2(C1-C6алкил), C3-C8циклоалкил, C3-C8циклоалкокси, C1-C6галогеналкил, N(R7)2, арил, гетероарил или гетероциклил; где арил предст� (19) РОССИЙСКАЯ ...

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Номер: WO1998016240A1
Принадлежит: The Liposome Company, Inc.

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NEUROTROPHIN RECEPTOR AGONISTS AND THEIR APPLICATION AS MEDICINES

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Номер: RU2497806C2
Принадлежит: Этерна Центарис ГмбХ

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to tetrahydrocarbazole derivatives of formula: , wherein the values W, V, R1-R22, R1*, R4 m , R5 m , n, m are presented in clause 1 of the patent claim. EFFECT: compounds may be used in a pharmaceutical composition for treating and/or preventing the physiological and/or pathological conditions mediated by LHRH receptors. 13 cl, 2 dwg, 5 tbl, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 497 806 (13) C2 (51) МПК C07D 209/82 (2006.01) A61K 31/403 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (24) Дата начала отсчета срока действия патента: 25.04.2008 Приоритет(ы): (30) Конвенционный приоритет: 27.04.2007 EP 07107094.0 27.04.2007 US 60/914,424 (43) Дата публикации заявки: 10.06.2011 Бюл. № 16 (45) Опубликовано: 10.11.2013 Бюл. № 31 (56) Список документов, цитированных в отчете о поиске: WO 2006/005484 А, 19.01.2006. WO 2003/051837 A2, 26.06.2003. EA 2347 B1, 25.04.2002. RU 2207340 C2, 27.06.2003. (86) Заявка PCT: EP 2008/055039 (25.04.2008) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 27.11.2009 R U 2 4 9 7 8 0 6 (87) Публикация заявки РСТ: WO 2008/132153 (06.11.2008) Адрес для переписки: 127055, Москва, а/я 11, пат.пов. Н.К.Попеленскому, рег. № 31 (54) ПРОИЗВОДНЫЕ ТЕТРАГИДРОКАРБАЗОЛА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ЛЕКАРСТВЕННОЕ СРЕДСТВО НА ИХ ОСНОВЕ, СПОСОБ ЛЕЧЕНИЯ И/ИЛИ ПРОФИЛАКТИКИ ФИЗИОЛОГИЧЕСКИХ И/ИЛИ ПАТОЛОГИЧЕСКИХ СОСТОЯНИЙ, ОПОСРЕДОВАННЫХ LHRH РЕЦЕПТОРОМ, ПОСРЕДСТВОМ ВЫШЕНАЗВАННЫХ ПРОИЗВОДНЫХ (57) Реферат: Изобретение относится к тетрагидрокарбазола формулы: производным где значения W, V, R1-R22, R1 *, R4m, R5m, n, Ñòð.: 1 ru 2 4 9 7 8 0 6 (73) Патентообладатель(и): Этерна Центарис ГмбХ (DE) R U (72) Автор(ы): БААСНЕР Сильке (DE), ГЮНТЕР Экхард (DE), ПАУЛИНИ Клаус (DE), ПОЛИМЕРОПУЛОС Эммануэль (DE), ТАЙФЕЛ Михаэль (DE), ШМИДТ Петер (DE), ШУСТЕР Тильман (DE) (21)(22) Заявка: 2009143990/04, 25.04.2008 m ...

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15-01-2010 дата публикации

Hepatitis c virus inhibitors

Номер: MY140680A
Принадлежит: Bristol Myers Squibb Co

HEPATITIS C VIRUS INHIBITORS ARE DISCLOSED HAVING THE GENERAL FORMULA:(I) WHEREIN R1,R2, R3, R',B,Y AND X ARE DESCRIBED IN THE DESCRIPTION.COMPOSITIONS COMPRISING THE COMPOUNDS AND METHODS FOR USING THE COMPOUNDS TO INHIBIT HCV ARE ALSO DISCLOSED.

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02-12-2004 дата публикации

Diamine derivative

Номер: JPWO2003016302A1
Принадлежит: 第一製薬株式会社

一般式(1)Q1−Q2−T0−N(R1)−Q3−N(R2)−T1−Q4(1)[式中、R1およびR2は水素原子などを、Q1は置換基を有することもある飽和もしくは不飽和の5〜6員の環状炭化水素基などを、Q2は単結合などを、Q3は下記の基(基中、Q5は炭素数1〜8のアルキレン基などを示す。)を、T0及びT1はカルボニル基などを示す。]で表される化合物、その塩、それらの溶媒和物またはそれらのN−オキシド。脳梗塞、脳塞栓、心筋梗塞、狭心症、肺梗塞、肺塞栓、バージャー病、深部静脈血栓症、汎発性血管内凝固症候群、人工弁/関節置換後の血栓形成、血行再建後の血栓形成および再閉塞、全身性炎症性反応症候群(SIRS)、多臓器不全(MODS)、体外循環時の血栓形成または採血時の血液凝固の予防剤および/または治療剤として有用である。 General formula (1) Q1-Q2-T0-N (R1) -Q3-N (R2) -T1-Q4 (1) [wherein R1 and R2 may be a hydrogen atom or the like, and Q1 may have a substituent. A saturated or unsaturated 5- to 6-membered cyclic hydrocarbon group or the like, Q2 represents a single bond or the like, and Q3 represents the following group (in the group, Q5 represents an alkylene group having 1 to 8 carbon atoms). , T0 and T1 represent a carbonyl group or the like. A salt thereof, a solvate thereof or an N-oxide thereof. Cerebral infarction, cerebral embolism, myocardial infarction, angina, pulmonary infarction, pulmonary embolism, Burger's disease, deep vein thrombosis, generalized intravascular coagulation, thrombus formation after artificial valve / joint replacement, thrombus after revascularization It is useful as a prophylactic and / or therapeutic agent for formation and reocclusion, systemic inflammatory response syndrome (SIRS), multiple organ failure (MODS), thrombus formation during extracorporeal circulation or blood coagulation during blood collection.

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05-01-2010 дата публикации

Macrocyclic peptides active against the hepatitis C virus

Номер: US7642235B2
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula I: wherein D, R 4 , R 3 , L 0 , L 1 , L 2 , R 2 and R C are defined herein; or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.

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06-07-2010 дата публикации

Macrocyclic peptides active against the hepatitis C virus

Номер: US7749961B2
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I): wherein R 1 , R 2 , X, R 3 , D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.

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15-05-2012 дата публикации

Macrocyclic compounds as antiviral agents

Номер: US8178520B2

The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R 1 , R a , R b , R 3 , R 4 , M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.

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10-07-2012 дата публикации

HCV NS3 protease inhibitors

Номер: US8216999B2
Принадлежит: Individual

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

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02-10-2012 дата публикации

HCV NS3 protease inhibitors

Номер: US8278322B2
Принадлежит: Individual

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

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20-11-2012 дата публикации

Macrocyclic compounds as antiviral agents

Номер: US8314062B2

The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R 1 , R 2 , R 3 , R 4 , R 5 , R a , M, Z and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.

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18-05-2016 дата публикации

Macrocyclic proline derived hcv serine protease inhibitors

Номер: EP3020723A1
Принадлежит: Enanta Pharmaceuticals Inc

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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12-04-2005 дата публикации

Substituted cycloalkyl P1′ hepatitis C virus inhibitors

Номер: US6878722B2
Принадлежит: Bristol Myers Squibb Co

The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.

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07-02-2006 дата публикации

Hepatitis C virus inhibitors

Номер: US6995174B2
Принадлежит: Bristol Myers Squibb Co

Hepatitis C virus inhibitors are disclosed having the general formula: wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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14-11-2006 дата публикации

Hepatitis C virus inhibitors

Номер: US7135462B2
Принадлежит: Bristol Myers Squibb Co

Hepatitis C virus inhibitors are disclosed having the general formula: wherein A, R 2 , R 3 , R′, B and Y are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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