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Применить Всего найдено 33184. Отображено 100.
10-10-2001 дата публикации

СИСТЕМА ДЛЯ НЕПРЕРЫВНОГО ПОЛУЧЕНИЯ ЭТИЛОВОГО СПИРТА (ВАРИАНТЫ)

Номер: RU0000019833U1

1. Система для непрерывного получения этилового спирта, содержащая первую герметичную емкость брожения-отгонки, первый коллектор, вакуум-насос, вход которого через первый коллектор соединен с первой емкостью брожения-отгонки, первый теплообменник, установленный в первой емкости брожения-отгонки, второй коллектор, соединяющий выход вакуум-насоса с входом первого теплообменника, блок разделения сконденсированных водно-спиртовых паров и углекислого газа, третий коллектор, соединяющий выход первого теплообменника с входом блока разделения сконденсированных водно-спиртовых паров и углекислого газа, первый и второй входные вентили, один конец каждого из которых соединен с первой емкостью брожения-отгонки, и выходной вентиль, отличающаяся тем, что в нее дополнительно введены К герметичных емкостей брожения-отгонки (К≥2), через первый коллектор соединенных с входом вакуум-насоса, К теплообменников (К≥2), причем "L"-ый теплообменник (2≤L≤K+1) установлен в "L"-ой емкости брожения-отгонки (2≤L≤K+1), при этом входы этих К теплообменников через второй коллектор соединены с выходом вакуум-насоса, а выходы этих К теплообменников через третий коллектор соединены с входом блока разделения сконденсированных водно-спиртовых паров и углекислого газа, К трубопроводов (К≥2), соединяющих емкость брожения-отгонки последовательно по суслу, причем один конец "М"-го трубопровода (1≤М≤К) соединен с выходом "М"-ой емкости брожения-отгонки (1≤М≤К), а другой конец "М"-го трубопровода соединен с входом "М+1"-ой емкости брожения-отгонки (1≤М≤К), первый насос, четвертый коллектор, соединенный с входом первого насоса, пятый коллектор, соединяющий выход первого насоса с первой емкостью брожения-отгонки, К-1 вентилей, причем один конец "N"-го вентиля (1≤N≤К-1) соединен с "N+1"-ым трубопроводом, а другие концы всех этих К-1 вентилей через четвертый коллектор соединены с входом первого насоса, а один конец выходного вентиля соединен с выходом "К+1"-ой емкости брожения-отгонки. 2. Система по п.1, ...

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20-07-2008 дата публикации

УСТРОЙСТВО ОБЛАГОРАЖИВАНИЯ НЕФТИ

Номер: RU0000074917U1

1. Устройство облагораживания нефти, содержащее емкость, электроды, систему подвода сырья, систему вывода обработанного сырья, блок питания высоковольтного напряжения, отличающееся тем, что электроды образуют конверсированную зону, расположенную в нижней части емкости, и выполнены в виде металлической сетки, скрученной в рулон, ячейки которой имеют отводы в виде острых игл, при этом емкость имеет заземление. 2. Устройство по п.1, отличающееся тем, что содержит две и более конверсированные зоны, соединенные между собой параллельно или последовательно. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 74 917 (13) U1 (51) МПК C10G 15/00 (2006.01) C07C 27/14 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2008110378/22 , 12.03.2008 (24) Дата начала отсчета срока действия патента: 12.03.2008 (45) Опубликовано: 20.07.2008 (73) Патентообладатель(и): Бичевин Александр Вячеславович (RU), Бичевин Алексей Александрович (RU) U 1 7 4 9 1 7 R U Ñòðàíèöà: 1 U 1 Формула полезной модели 1. Устройство облагораживания нефти, содержащее емкость, электроды, систему подвода сырья, систему вывода обработанного сырья, блок питания высоковольтного напряжения, отличающееся тем, что электроды образуют конверсированную зону, расположенную в нижней части емкости, и выполнены в виде металлической сетки, скрученной в рулон, ячейки которой имеют отводы в виде острых игл, при этом емкость имеет заземление. 2. Устройство по п.1, отличающееся тем, что содержит две и более конверсированные зоны, соединенные между собой параллельно или последовательно. 7 4 9 1 7 (54) УСТРОЙСТВО ОБЛАГОРАЖИВАНИЯ НЕФТИ R U Адрес для переписки: 420075, г.Казань, ул. Липатова, 15а, кв.4, А.А. Бичевину (72) Автор(ы): Бичевин Александр Вячеславович (RU), Бичевин Алексей Александрович (RU) U 1 U 1 7 4 9 1 7 7 4 9 1 7 R U R U Ñòðàíèöà: 2 RU 5 10 15 20 25 30 35 40 45 50 74 917 U1 Полезная модель относится к области нефтехимической и ...

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10-08-2009 дата публикации

УСТАНОВКА ДЛЯ ОБРАБОТКИ СЫРЬЯ

Номер: RU0000085478U1

1. Установка для обработки сырья, включающая загрузочный бункер, реакционную камеру, связанную с источником питания и с входным и выходным патрубками, причем реакционная камера выполнена в виде корпуса, в котором установлены электроды, отличающаяся тем, что она снабжена устройством для сбора газообразных оксидов и гидридов с барбатером, а загружающий бункер снабжен ультразвуковым диспергатором, при этом корпус реакционной камеры выполнен в виде плоской емкости, в нижней части которой размещен электрод, предназначенный для ускорения процесса диссоциации воды, а верхняя часть емкости, имеющая на внутренней поверхности материал - источник позитронов, использована в качестве второго электрода. 2. Установка для обработки по п.1, отличающаяся тем, что электрод, предназначенный для ускорения процесса диссоциации воды выполнен из композиционного материала на основе нитрида бора (ВN), армированного ультрадисперсным карбидом кремния SiC и углеродного волокна. 3. Установка для обработки по п.1, отличающаяся тем, что в качестве материала-источника позитронов используют или Zn, или Mn или Fe. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 85 478 U1 (51) МПК C07C 27/14 (2006.01) H05B 7/12 (2006.01) C10G 1/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2009107553/22, 03.03.2009 (24) Дата начала отсчета срока действия патента: 03.03.2009 (45) Опубликовано: 10.08.2009 (72) Автор(ы): Степанов Николай Викторович (RU), Бурлаков Евгений Викторович (RU), Павлов Михаил Андреевич (RU) Адрес для переписки: 105043, Москва, ул. Первомайская, 66, кв.135, Т.К. Широковой U 1 8 5 4 7 8 R U Ñòðàíèöà: 1 ru CL U 1 Формула полезной модели 1. Установка для обработки сырья, включающая загрузочный бункер, реакционную камеру, связанную с источником питания и с входным и выходным патрубками, причем реакционная камера выполнена в виде корпуса, в котором установлены электроды, отличающаяся тем, что она снабжена ...

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10-07-2011 дата публикации

УСТАНОВКА ДЛЯ ПОЛУЧЕНИЯ ЦИКЛОГЕКСАНОНА И ЦИКЛОГЕКСАНОЛА

Номер: RU0000106245U1

1. Установка для получения циклогексанона и циклогексанола, включающая расположенные в технологической последовательности узел подачи реакционной жидкости, узел охлаждения реакционной жидкости, реактор нейтрализации продуктов окисления, разделительный сосуд первого органического и первого водно-щелочного слоя, узел разложения гидроперекиси циклогексила и оснащенный сепаратором узел отделения второго водно-щелочного слоя, связанный с узлом разложения гидроперекиси и реактором нейтрализации, и снабженный выводом второго органического слоя, отличающаяся тем, что между узлом охлаждения реакционной жидкости и реактором нейтрализации установлены узел отмывки, выполненный в виде смесителя охлажденной реакционной жидкости и воды и разделительный сосуд органического и водно-кислого слоев, который связан с экстрактором водно-кислого слоя и, далее, - с устройством очистки рафината, при этом экстрактор водно-кислого слоя и устройство очистки рафината дополнительно связаны с узлом отмывки реакционной жидкости водой, а устройство очистки рафината снабжено узлом отвода водно-кислого стока. 2. Установка по п.1, отличающаяся тем, что устройство очистки рафината связано с узлом отмывки реакционной жидкости водой через узел ее подачи. 3. Установка по п.1, отличающаяся тем, что разделительный сосуд органического и водно-кислого слоев выполнен в виде сепаратора или отстойника. 4. Установка по п.1, отличающаяся тем, что экстрактор водно-кислого слоя выполнен пульсационным или роторно-дисковым, или насадочным. 5. Установка по п.1, отличающаяся тем, что устройство очистки рафината выполнено в виде насадочной или тарельчатой ректификационной колонны. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 106 245 (13) U1 (51) МПК C07C C07C C07C C07C C07C B01J 27/32 (2006.01) 45/53 (2006.01) 29/50 (2006.01) 35/08 (2006.01) 49/403 (2006.01) 10/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21)(22) Заявка: 2010154693/04, 30.12. ...

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22-12-2020 дата публикации

УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА

Номер: RU0000201591U1

Полезная модель относится к узлу концентрации раствора карбамида для установки производства карбамида. Узел содержит две ступени выпаривания, каждая из которых включает вакуумный сепаратор, причем вакуумные сепараторы обеих ступеней соединены между собой трубопроводом для раствора карбамида, и вакуумную систему конденсации сокового пара, соединенную с каждым из вакуумных сепараторов посредством трубопровода для сокового пара, причем в трубопроводе для сокового пара между вакуумным сепаратором первой ступени и вакуумной системой конденсации сокового пара установлен регулирующий клапан, при этом давление во второй ступени узла концентрации ниже давления в первой ступени узла концентрации. Полезная модель обеспечивает упрощение и повышение надежности узла выпаривания раствора карбамида. 7 з.п. ф-лы, 1 ил. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 201 591 U1 (51) МПК C07C 273/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (52) СПК C07C 273/04 (2020.08) (21)(22) Заявка: 2020122793, 09.07.2020 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): Акционерное общество "Аммоний" (RU) Дата регистрации: 22.12.2020 Приоритет(ы): (22) Дата подачи заявки: 09.07.2020 (45) Опубликовано: 22.12.2020 Бюл. № 36 2 0 1 5 9 1 R U (54) УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА (57) Реферат: Полезная модель относится к узлу трубопроводе для сокового пара между концентрации раствора карбамида для установки вакуумным сепаратором первой ступени и производства карбамида. Узел содержит две вакуумной системой конденсации сокового пара ступени выпаривания, каждая из которых установлен регулирующий клапан, при этом включает вакуумный сепаратор, причем давление во второй ступени узла концентрации вакуумные сепараторы обеих ступеней соединены ниже давления в первой ступени узла между собой трубопроводом для раствора концентрации. Полезная модель обеспечивает карбамида, и вакуумную систему конденсации упрощение и повышение ...

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16-04-2021 дата публикации

УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ПАРОВЫМ ОБДУВОМ ВНУТРЕННЕЙ ПОВЕРХНОСТИ ВАКУУМНОГО СЕПАРАТОРА

Номер: RU0000203706U1

Полезная модель относится к производству карбамида (мочевины). Узел концентрации раствора карбамида для установки производства карбамида, включающий в себя две ступени выпаривания, причем каждая из упомянутых ступеней включает в себя вакуумный сепаратор, причем вакуумные сепараторы обеих ступеней соединены между собой трубопроводом для раствора карбамида, отличающийся тем, что вакуумный сепаратор второй ступени выпаривания снабжен паровым обдувом внутренней поверхности. Технический результат заключается в исключении налипания продукта и образования твердых отложений на стенках аппарата, что обеспечивает повышение надежности узла выпаривания раствора карбамида для установки для производства карбамида. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 203 706 U1 (51) МПК C07C 273/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (52) СПК C07C 273/04 (2021.02) (21)(22) Заявка: 2020139920, 04.12.2020 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): Акционерное общество "Аммоний" (RU) Дата регистрации: 16.04.2021 2020122793 09.07.2020 (45) Опубликовано: 16.04.2021 Бюл. № 11 U 1 2 0 3 7 0 6 R U (54) УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ПАРОВЫМ ОБДУВОМ ВНУТРЕННЕЙ ПОВЕРХНОСТИ ВАКУУМНОГО СЕПАРАТОРА (57) Реферат: Полезная модель относится к производству вакуумный сепаратор второй ступени карбамида (мочевины). Узел концентрации выпаривания снабжен паровым обдувом раствора карбамида для установки производства внутренней поверхности. Технический результат карбамида, включающий в себя две ступени заключается в исключении налипания продукта выпаривания, причем каждая из упомянутых и образования твердых отложений на стенках ступеней включает в себя вакуумный сепаратор, аппарата, что обеспечивает повышение причем вакуумные сепараторы обеих ступеней надежности узла выпаривания раствора соединены между собой трубопроводом для карбамида для установки для производства раствора карбамида, отличающийся тем, что ...

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20-04-2021 дата публикации

УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ТЕПЛОИЗОЛЯЦИЕЙ КУПОЛА ВАКУУМНОГО СЕПАРАТОРА

Номер: RU0000203755U1

Полезная модель относится к производству карбамида (мочевины). Узел концентрации раствора карбамида для установки производства карбамида, включающий в себя две ступени выпаривания, причем каждая из упомянутых ступеней включает в себя вакуумный сепаратор, причем вакуумные сепараторы обеих ступеней соединены между собой трубопроводом для раствора карбамида, отличающийся тем, что купол вакуумного сепаратора второй ступени выпаривания снабжен теплоизоляцией. Технический результат заключается в предотвращении потерь тепла и соответственно снижении налипания продукта на внутренней поверхности купола, что обеспечивает повышение надежности узла выпаривания раствора карбамида для установки для производства карбамида. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 203 755 U1 (51) МПК C07C 273/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (52) СПК C07C 273/04 (2021.02) (21)(22) Заявка: 2020139925, 04.12.2020 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): Акционерное общество "Аммоний" (RU) Дата регистрации: 20.04.2021 2020122793 09.07.2020 (45) Опубликовано: 20.04.2021 Бюл. № 11 U 1 2 0 3 7 5 5 R U (54) УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ТЕПЛОИЗОЛЯЦИЕЙ КУПОЛА ВАКУУМНОГО СЕПАРАТОРА (57) Реферат: Полезная модель относится к производству купол вакуумного сепаратора второй ступени карбамида (мочевины). Узел концентрации выпаривания снабжен теплоизоляцией. раствора карбамида для установки производства Технический результат заключается в карбамида, включающий в себя две ступени предотвращении потерь тепла и соответственно выпаривания, причем каждая из упомянутых снижении налипания продукта на внутренней ступеней включает в себя вакуумный сепаратор, поверхности купола, что обеспечивает повышение причем вакуумные сепараторы обеих ступеней надежности узла выпаривания раствора соединены между собой трубопроводом для карбамида для установки для производства раствора карбамида, отличающийся тем, что ...

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31-05-2021 дата публикации

УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ЭЛЕКТРООБОГРЕВОМ КУПОЛА ВАКУУМНОГО СЕПАРАТОРА

Номер: RU0000204557U1

Полезная модель относится к производству карбамида (мочевины). Узел концентрации раствора карбамида для установки производства карбамида, включающий в себя две ступени выпаривания, причем каждая из упомянутых ступеней включает в себя вакуумный сепаратор, причем вакуумные сепараторы обеих ступеней соединены между собой трубопроводом для раствора карбамида, отличающийся тем, что купол вакуумного сепаратора второй ступени выпаривания снабжен электрообогревом. Технический результат заключается в исключении налипания продукта на внутренней поверхности купола, что обеспечивает повышение надежности узла выпаривания раствора карбамида для установки для производства карбамида. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 204 557 U1 (51) МПК C07C 273/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (52) СПК C07C 273/04 (2021.02) (21)(22) Заявка: 2020139921, 04.12.2020 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): Акционерное общество "Аммоний" (RU) Дата регистрации: 31.05.2021 2020122793 09.07.2020 (45) Опубликовано: 31.05.2021 Бюл. № 16 U 1 2 0 4 5 5 7 R U (54) УЗЕЛ КОНЦЕНТРАЦИИ РАСТВОРА КАРБАМИДА С ЭЛЕКТРООБОГРЕВОМ КУПОЛА ВАКУУМНОГО СЕПАРАТОРА (57) Реферат: Полезная модель относится к производству раствора карбамида, отличающийся тем, что карбамида (мочевины). Узел концентрации купол вакуумного сепаратора второй ступени раствора карбамида для установки производства выпаривания снабжен электрообогревом. карбамида, включающий в себя две ступени Технический результат заключается в исключении выпаривания, причем каждая из упомянутых налипания продукта на внутренней поверхности ступеней включает в себя вакуумный сепаратор, купола, что обеспечивает повышение надежности причем вакуумные сепараторы обеих ступеней узла выпаривания раствора карбамида для соединены между собой трубопроводом для установки для производства карбамида. Стр.: 1 U 1 Адрес для переписки: 420015, рес. Татарстан, г. Казань, ул. ...

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12-01-2012 дата публикации

Acetylene derivatives having mglur 5 antagonistic activity

Номер: US20120010263A1
Принадлежит: Individual

The invention provides compounds of formula I wherein n, A, R, R′, R″, R O , X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

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12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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09-02-2012 дата публикации

Plasmalogen compounds, pharmaceutical compositions containing the same and methods for treating diseases of the aging

Номер: US20120035250A1
Принадлежит: Phenomenome Discoveries Inc

Described herein are routes of synthesis and therapeutic uses of 1-alkyl, 2-acyl glycerol derivatives of formula I: which when administered to mammalian biological systems result in increased cellular concentrations of specific sn-2 substituted ethanolamine plasmalogens independent of the ether lipid synthesis capacity of the system. Elevating levels of the specific sn-2 substituted species in this way can cause lowering of membrane cholesterol levels and the lowering of amyloid secretion. These compounds can be used for the treatment or prevention of diseases of aging associated with increased membrane cholesterol, increased amyloid, and decreased plasmalogen levels, such as neurodegeneration (including Alzheimer's disease, Parkinson's disease and age-related macular degeneration), cognitive impairment, dementia, cancer (e.g. prostate, lung, breast, ovarian, and kidney cancers), osteoporosis, bipolar disorder and vascular diseases (such as atherosclerosis, hypercholesterolemia).

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09-02-2012 дата публикации

Sphingo-guanidines and their use as inhibitors of sphingosine kinase

Номер: US20120035268A1

The presently disclosed subject matter provides compounds of the formula: (1) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limit cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.

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16-02-2012 дата публикации

Substituted acylguanidine derivatives (as amended)

Номер: US20120041036A1
Принадлежит: Astellas Pharma Inc

An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT 5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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15-03-2012 дата публикации

Method for analyzing aqueous ammonium carbamate solution, and method for operating unreacted gas absorber

Номер: US20120060931A1
Принадлежит: Toyo Engineering Corp

There are provided a method for analyzing an aqueous ammonium carbamate solution whereby the composition of an unreacted-gas absorber outlet liquid can be specified in real time, and a method for operating an unreacted gas absorber by use of the same. The method for analyzing the composition of an aqueous ammonium carbamate solution includes determining ammonia component concentration, carbon dioxide component concentration, and water concentration of the aqueous ammonium carbamate solution, which is the unreacted-gas absorber outlet liquid in a urea production process, by using a correlation among viscosity, temperature, and carbon dioxide component concentration of the aqueous solution and a correlation among density, temperature, ammonia component concentration, and carbon dioxide component concentration of the aqueous solution, wherein the ammonia component concentration is a concentration of a sum of free ammonia and equivalent ammonia of ammonium carbamate which are contained in the aqueous solution, and the carbon dioxide component concentration is a concentration of equivalent carbon dioxide of ammonium carbamate contained in the aqueous solution.

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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29-03-2012 дата публикации

Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20120077858A1
Принадлежит: Allergan Inc

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R 1 is selected from the group consisting of CO 2 R 7 and CON(R 7 )SO 2 R 7 wherein R 1 , R 2 , R 3 , R 4 , and R 7 are as defined in the specification. The compounds may be administered to treat DP 1 , FP, EP 1 , EP 3 , TP and/or EP 4 receptor mediated diseases or conditions.

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29-03-2012 дата публикации

Method For Improved Bioactivation Of Pharmaceuticals

Номер: US20120077876A1

This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R 1 and R 2 are hydrogen, alkyl, or aryl radicals.

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19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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03-05-2012 дата публикации

Cross-Coupled Peptide Nucleic Acids for Detection of Nucleic Acids of Pathogens

Номер: US20120107794A1

The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

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10-05-2012 дата публикации

N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation

Номер: US20120115915A1
Принадлежит: Harvard College

Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

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17-05-2012 дата публикации

Urethane and urea fluorosurfactants

Номер: US20120122999A1
Принадлежит: EI Du Pont de Nemours and Co

The present invention comprises a compound of a compound of Formula 1 wherein R f is a C 2 to C 12 perfluoroalkyl optionally interrupted by one to four moieties each independently selected from the group consisting of —CH 2 —, —O—, —S—, —S(O)—, and —S(O) 2 —; n is 1 to 6; m is 0 to 2, provided that m is less than or equal to n. X and Y are each independently O or NR, R is hydrogen or C 1 to C 6 alkyl; R 1 , and R 2 are each independently C 1 to C 6 alkyl, optionally containing one or more oxygen atoms and may form a ring selected from the group of piperidine, pyrrolidine, and morpholine; and R 3 is O − , (CH 2 ) p C(O)O − , (CH 2 ) p CH(OH)(CH 2 )SO 3 − , and (CH 2 ) q SO 3 − ; p is 1 to 4; and q is 2 to 4 which is useful as a surfactant.

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31-05-2012 дата публикации

Novel complex for treatment and/or prophylaxis of parasitic infections

Номер: US20120136062A1
Принадлежит: Ipca Laboratories Ltd

Disclosed are complexes of an antipneumocystic compound and an antimalarial compound, processes for their preparation, pharmaceutical compositions and methods of using said complexes or compositions for the treatment and/or prophylaxis of parasitic infections.

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31-05-2012 дата публикации

Modularized System and Method for Urea Production Using Stranded Natural Gas

Номер: US20120136172A1
Принадлежит: 4A TECHNOLOGIES LLC

A modular system and method for producing urea from stranded natural gas includes removal of foreign particulate matter to obtain a substantially homogeneous gas. The gas is processed by controlling the quality of the stranded natural gas to maintain a substantially homogenous mixture The resultant gas stream is further cleaned and compressed to a high pressure of about 3,000 psi. The resultant ammonia stream is processed in a bypass recycling loop system at 30% conversion rate at a high pressure of about 6,000 to 7,000 psi. The equipment associated with each of the process steps may be skid mounted for portability and/or contained within the footprint of a standard 48-foot flatbed trailer.

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07-06-2012 дата публикации

Compositions and methods relating to proliferative diseases

Номер: US20120141578A1
Принадлежит: PENN STATE RESEARCH FOUNDATION

Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

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28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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05-07-2012 дата публикации

In Vivo Polynucleotide Delivery Conjugates Having Enzyme Sensitive Linkages

Номер: US20120172412A1
Принадлежит: Arrowhead Madison Inc

The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.

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05-07-2012 дата публикации

Compositions, Synthesis, and Methods of Using Cycloalkylmethylamine Derivatives

Номер: US20120172426A1
Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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30-08-2012 дата публикации

Process for reduction of alpha-acyloxy sulfide derivatives

Номер: US20120220784A1
Принадлежит: Scinopharm Singapore Pte Ltd

The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding α-acyloxy sulfides.

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06-09-2012 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes and parkinson's disease

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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13-09-2012 дата публикации

Method for the separation of ammonia and carbon dioxide from aqueous solutions

Номер: US20120228225A1
Принадлежит: Saipem Spa

The present invention relates to a method for contemporaneously recovering ammonia and carbon dioxide from an aqueous solution thereof, possibly comprising their condensates, in a synthesis process of urea, characterized in that it comprises a hydrophobic microporous membrane distillation phase of an aqueous solution comprising ammonia, carbon dioxide and their saline compounds or condensates, said distillation being carried out at a temperature ranging from 50 to 250° C. and a pressure ranging from 50 KPa to 20 MPa absolute, with the formation of a residual aqueous solution, possibly comprising urea, and a gaseous permeate stream, comprising ammonia, carbon dioxide and water. The present invention also relates to an apparatus for effecting the above method and a production process of urea which comprises the above method.

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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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18-10-2012 дата публикации

Photocurable compound

Номер: US20120264963A1
Принадлежит: SAMSUNG ELECTRONICS CO LTD

Disclosed is a compound having a photocurable urethane(meth)acrylate group, its manufacturing method, and a photocurable composition including the compound. The compound is represented by Chemical Formulae 1 to 6. Each of Chemical Formulae 1 to 6 includes a urethane(meth)acrylate group represented by Chemical Formula 1-1 or 1-2.

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25-10-2012 дата публикации

Heterodimers of Glutamic Acid

Номер: US20120269726A1
Принадлежит: Molecular Insight Pharmaceuticals Inc

Compounds of Formula (Ia) wherein R is a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl, a C 1 -C 6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O) 2 , C(O) 2 (CH2)p Y is C(O), O, NR′, S, S(O) 2 , C(O) 2 (CH2)p Z is H or C 1 -C 4 alkyl, R′ is H, C(O), S(O) 2 , C(O) 2 , a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl or a C 1 -C 6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C 1 -C 12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

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01-11-2012 дата публикации

Extractive Distillation of Crude Alcohol Product

Номер: US20120277463A1
Принадлежит: Celanese International Corp

Recovery of ethanol from a crude ethanol product obtained from the hydrogenation of acetic acid using an extractive distillation column. The column yields a first residue that comprises ethanol, ethyl acetate, acetic acid, and water. The first residue is separated in a second column to yield a second distillate comprising ethanol and ethyl acetate. The second distillate is then separated in a third column to yield a third distillate comprising ethyl acetate and a third residue comprising ethanol.

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08-11-2012 дата публикации

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

Номер: US20120283445A1
Принадлежит: SANOFI SA

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

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08-11-2012 дата публикации

Process for preparing alkyl hydroperoxide compounds

Номер: US20120283482A1
Принадлежит: Rhodia Operations SAS

A method for making alkyl hydroperoxide compounds, specifically the preparation of cyclohexyl hydroperoxide is described. The preparation of cyclohexyl hydroperoxide by means of the oxidation of cyclohexane by oxygen in a multi-stage reactor or in reactors connected in series is also described. In these methods, the reactor surfaces in contact with the oxidation medium can be protected by a layer of heat-resistant PFA polymer.

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29-11-2012 дата публикации

Urea stripping process for the production of urea

Номер: US20120302789A1
Принадлежит: Stamicarbon BV

The invention relates to a process for producing urea wherein an aqueous urea solution, leaving a urea reaction zone is fed to a stripper, where a part of the non-converted ammonia and carbon dioxide is separated from the aqueous urea solution, which solution leaves the stripper to a first recovery section of one or more serial recovery sections and is subsequently fed to one or more urea concentration sections, wherein the urea solution leaving the stripper is subjected to an adiabatic expansion, thus creating a vapor and a liquid, which are separated before the liquid enters a first recovery section and the vapor is condensed. The invention further relates to a urea plant comprising a stripper and a first recovery section, wherein an adiabatic expansion valve and a liquid/gas separator is provided between the stripper and the first recovery section.

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13-12-2012 дата публикации

Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

Номер: US20120316066A1
Принадлежит: Intrexon Corp

The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.

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27-12-2012 дата публикации

Therapeutic compounds

Номер: US20120329866A1

The invention provides compounds of Formula (I): R 1 ≡R 2   (I) wherein R 1 and R 2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

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24-01-2013 дата публикации

Arachidonic acid analogs and methods for analgesic treatment using same

Номер: US20130023510A1
Принадлежит: Cytometix Inc

The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.

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07-02-2013 дата публикации

Calixarene-Based Peptide Conformation Mimetics, Methods of Use, and Methods of Making

Номер: US20130035394A1
Принадлежит: University of Minnesota

A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

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21-02-2013 дата публикации

Salicylate fatty acid derivatives

Номер: US20130046013A1
Принадлежит: Individual

Fatty acid conjugates of salicylate derivatives and compositions thereof are disclosed. Further disclosed are methods for treating various diseases comprising the administration of an effective amount of at least one compound according to the present disclosure.

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07-03-2013 дата публикации

Therapeutic Compounds

Номер: US20130059919A1
Автор: Thomas E. Jenkins
Принадлежит: Individual

A (−)-stereoisomer of formula (I): [insert formula (I) wherein X is H or F; or a pharmaceutically acceptable salt or prodrug thereof, useful as an anesthetic.

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21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

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21-03-2013 дата публикации

DRUGS, DERIVATIVES AND ANALOGS CONTAINING ADAMANTANE STRUCTURES OF NEW INDICATION APPLICATIONS OF ANTI-TUMOR

Номер: US20130072553A1
Автор: XU LIFENG
Принадлежит:

This invention relates to the drugs, derivatives and analogs containing adamantane structures of new indication applications of anti-tumor. The invention also relates to above compounds to treat tumors and other diseases with FIG. . These drugs, derivatives and analogs are generated by the modification of the parent or fragment structures and formation of pharmaceutically acceptable salts, complex salts or prodrug. The drugs, derivatives and analogs as described are administered alone or together with at least one known anti-tumor and immune chemotherapeutic agent including treatment of viral, bacterial and fungal diseases, neurological diseases, endocrine system diseases, and immune system diseases. 2. The drugs claim 1 , derivatives and analogs according to claim 1 , wherein:compound 1, compound 2, compound 3, compound 4, compound 5 and compound 6, derivatives and analogs are generated by the modification of the parent or fragment structures.3. The drugs claim 2 , derivatives and analogs according to claim 2 , wherein: the derivatives and analogs prepared by direct synthesis or structural modification of the drugs as described compound 1 claim 2 , compound 2 claim 2 , compound 3 claim 2 , compound 4 claim 2 , compound 5 and compound 6 are relevance to the drugs as described compound 1 claim 2 , compound 2 claim 2 , compound 3 claim 2 , compound 4 claim 2 , compound 5 and compound 6 in chemical structures and pharmaceutical activities.4. The drugs claim 3 , derivatives and analogs according to claim 3 , wherein:The drugs, derivatives and analogs are selected from the exemplified examples or pharmaceutically acceptable salts formed by organic acid, inorganic acid, organic base, inorganic base, prodrug or complex salts.5. The drugs claim 3 , derivatives and analogs according to claim 3 , claim 3 , and wherein:This invention relates to the drugs, derivatives and analogs containing adamantane structures of new indication applications of anti-tumor including: the ...

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21-03-2013 дата публикации

ENANTIOMERICALLY PURE AMINES

Номер: US20130072711A1
Принадлежит: NABRIVA THERAPEUTICS AG

A compound of formula 3. A compound according to claim 1 , wherein PROT and PROT′ together with the nitrogen atom to which are attached form phthalimido-N-yl.4. A compound according to claim 1 ,wherein PROT″ is benzoyl or trityl.7. A compound according to claim 1 , selected from the group consisting of:{(1R,2R,4R)-4-[(tert-Butoxycarbonyl)-amino]-2-hydroxy-cyclohexyl}-benzene-carbothioate,{(1R,2R,4R)-4-[(2,2,2-Trifluoro-acetyl)-amino]-2-hydroxy-cyclohexyl}-benzene-carbothioate,tert-Butyl [(1R,3R,4R)-3-hydroxy-4-tritylsulfanyl-cyclohexyl]-carbamate, and2,2,2-Trifluoro-N-((1R,3R,4R)-3-hydroxy-4-tritylsulfanyl-cyclohexyl)-acetamide.10. A compound of formula II claim 9 , II claim 9 , IIor IIaccording to claim 9 , selected from the group consisting oftert-Butyl (1R,3R,6R)-(7-oxa-bicyclo[4.1.0]hept-3-yl)-carbamate, and2,2,2-Trifluoro-N-(1R,3R,6S)-(7-oxa-bicyclo[4.1.0]hept-3-yl)-acetamide.12. A process according to claim 11 , wherein none of the intermediates obtained in a) to d) is isolated.13. A process according to claim 11 , wherein the reaction a) to e) is performed in a single solvent (system).14. (canceled) The present invention relates to enantiomerically pure amines, such as amino and thio protected hydroxy-mercapto-cyclohexyl amines and production processes thereof.Organic compounds, such as cyclohexyl amines containing an asymmetric carbon atom may exist in the form of enantiomers, diastereoisomers and mixtures thereof, e.g. racemates. Such compounds may exist in the (R)-, (S)- or (R,S)-configuration. For pharmaceutical use it is often vital to have an active compound comprising an asymmetric carbon atom in one of the enantiomerically pure forms, since one isomer may differ, e.g. in several aspects from another isomer, e.g. one isomer may be more active than the other isomer. Separation of isomers is often burdensome. Chromatography which, for example, may be useful for isomeric separation, is on technical scale not easy to carry out and often needs sophisticated ...

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28-03-2013 дата публикации

NOVEL AMPHIPHILES

Номер: US20130078283A1
Принадлежит:

Disclosed herein is a compound of structure (A): In this compound, X is either O or S, Ris a rigid group, Ris a hydrophilic group such that (A) is capable of self-assembly in water, and Ris an organic group. 2. The compound of wherein X is S.3. The compound of wherein at least one of Rand Ris oligomeric or polymeric.4. The compound of wherein Rcomprises an oligoether or a polyether chain.5. The compound of wherein the oligoether or polyether chain is an oligo- or poly-oxyethylene chain.6. The compound of wherein Rand Rare the same.7. The compound of wherein Ris a hydrophobic chain.8. The compound of wherein the hydrophobic chain comprises an aliphatic hydrocarbon chain.9. The compound of wherein Rcomprises an aromatic group.10. The compound of wherein the aromatic group is carbocyclic.11. The compound of to wherein R claim 1 , Rand Rare such that the compound has a critical aggregation concentration in water of below about 100 μM.12. The compound of which is non-cytotoxic.14. The process of wherein Rand Rare not the same and the process comprises{'sup': 1', '2', '3', '1, 'sub': 2', '2', '2', '2, 'reacting R(NCX)with one of RNHand RNHin large molar excess of R(NCX);'}{'sup': '1', 'sub': '2', 'separating an intermediate adduct from excess R(NCX); and'}{'sup': 2', '3, 'sub': 2', '2, 'reacting the intermediate adduct with the other of RNHand RNHto produce the compound of structure (A).'}16. The method of wherein Ris a hydrophobic group.18. The method of additionally comprising dialysing the aqueous product so as to remove unencapsulated substance.19. The method of wherein the water soluble substance is a drug.20. The method of wherein the vesicles have a mean diameter of less than about 200 nm.21. The method of wherein Rand Rin the amphiphile are both hydrophilic.22. The method of wherein Rand Rin the amphiphile are the same.24. The method of additionally comprising dialysing the aqueous product so as to remove unencapsulated substance.25. The method of wherein the ...

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28-03-2013 дата публикации

NOVEL DERIVATIVES OF MESALAZINE, PROCESS OF THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF INTESTINAL INFLAMMATORY DISEASES

Номер: US20130079399A1
Автор: LABRUZZO Carla
Принадлежит: SOFAR SPA

The present invention refers to the compounds corresponding to the following general formula (I): 3. 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof , preferably hydrochloride salt.4. Method for treating acute or chronic intestinal inflammatory diseases claim 1 , comprising the administration to a patient in need of such treatment a compound according to claim 1 , wherein said acute or chronic intestinal inflammatory diseases are preferably selected from among IBD claim 1 , IBS claim 1 , ulcerative colitis claim 1 , Crohn's disease claim 1 , diverticular disease claim 1 , more preferably IBD.5. Method for treating according to claim 4 , wherein said acute or chronic intestinal inflammatory diseases are acute intestinal inflammatory diseases.6. Method for treating according to claim 4 , wherein said acute or chronic intestinal inflammatory diseases are chronic intestinal inflammatory diseases.7. Method for treating according to claim 6 , wherein said chronic intestinal inflammatory diseases are in a remission phase.8. A compound according to claim 2 , characterised in that it is administered enterally claim 2 , preferably orally and/or rectally claim 2 , or topically claim 2 , preferably through anal application.9. Pharmaceutical composition containing a compound according to claim 2 , and at least one physiologically acceptable excipient.10. Pharmaceutical composition according to selected from among tablet claim 9 , capsule claim 9 , granule claim 9 , microgranule claim 9 , suspension or aqueous solution claim 9 , enema claim 9 , suppository claim 9 , gel and rectal foam.13. Process according to claim 11 , wherein the step a) is conducted in an aprotic polar solvent and/or in a mixture of said solvent with HO preferably in a molar ratio comprised between 1:1 and 3:1 claim 11 , more preferably 2:1.14. Process according to claim 11 , wherein said mixture is constituted by dioxane and water claim 11 , preferably in a 2:1 molar ratio ...

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11-04-2013 дата публикации

Compositions Comprising Enzyme-Cleavable Phenol-Modified Tapentadol Prodrug

Номер: US20130090379A1
Принадлежит: SIGNATURE THERAPEUTICS, INC.

A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions. 2. The compound of claim 1 , where Ris (1-6C)alkyl.3. (canceled)4. The compound of claim 1 , wherein Ris methyl or ethyl.513-. (canceled)14. The compound of claim 1 , wherein Rand Rare hydrogen.15. The compound of claim 1 , wherein Rand Rwhich are on the same carbon are alkyl.16. (canceled)17. The compound of claim 1 , wherein Rand Rwhich are on the same carbon are methyl.18. The compound of claim 1 , wherein Rand Rwhich are vicinal are both alkyl and Rand Rwhich are vicinal are both hydrogen.1922-. (canceled)23. The compound of claim 1 , wherein one of Rand Ris aminoacyl.2433-. (canceled)34. The compound of claim 1 , wherein n is 2 or 3.35. The compound of claim 1 , wherein Ris a residue of an L-amino acid selected from alanine claim 1 , arginine claim 1 , asparagine claim 1 , aspartic acid claim 1 , cysteine claim 1 , glycine claim 1 , glutamine claim 1 , glutamic acid claim 1 , histidine claim 1 , isoleucine claim 1 , leucine claim 1 , lysine claim 1 , methionine claim 1 , phenylalanine claim 1 , proline claim 1 , serine claim 1 , threonine claim 1 , tryptophan claim 1 , tyrosine and valine claim 1 , or a residue of an N-acyl derivative of any of said amino acids; or a residue of a peptide composed of at least two L-amino acid residues selected independently from alanine claim 1 , arginine claim 1 , asparagine claim 1 , aspartic acid claim 1 , cysteine ...

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11-04-2013 дата публикации

POLYMERIZABLE CARBAMATE AND THIOCARBAMATE COMPOUNDS, POLYMERS DERIVED FROM THEM, AND COMPOSITIONS THEREOF

Номер: US20130090443A1
Автор: Musa Osama M.
Принадлежит: ISP Investments Inc.

Carbamate and thiocarbamate compounds are described that comprise a polymerizable moiety and one or more free hydroxyl and/or thiol groups. Polymers may be obtained by polymerizing these carbamate and/or thiocarbamate compounds. The carbamate and thiocarbamate compounds, as well as the polymers they produce may be formulated into adhesive, agricultural, biocide, cleaning, coating, encapsulation, membrane, oilfield, performance chemical, and personal care compositions. 3. A composition comprising the compound of wherein said composition is an adhesive claim 1 , agricultural claim 1 , biocides claim 1 , cleaning claim 1 , coating claim 1 , encapsulation claim 1 , membrane claim 1 , oilfield claim 1 , performance chemical claim 1 , or personal care composition.5. The polymer according to having a weight-average molecular weight from about 500 Da to about 20 claim 4 ,000 claim 4 ,000 Da.7. The polymer according to wherein said polymer is a non-homopolymer synthesized by the polymerization of the first monomer and at least one second monomer different from said first monomer.8. The polymer according to having a weight-average molecular weight from about 500 Da to about 20 claim 7 ,000 claim 7 ,000 Da.9. The polymer according to wherein the non-homopolymer is an alternating claim 7 , random claim 7 , graft claim 7 , or block non-homopolymer claim 7 , an end-capped derivative thereof claim 7 , or other derivative thereof.10. The polymer according to wherein the molar percentage of said first monomer is from about 0.001 mole percent to about 99.999 mole percent of said non-homopolymer claim 7 , and said second monomer is present from about 0.001 mole percent to about 99.999 mole percent of said non-homopolymer.11. The polymer according to wherein said second monomer is selected from the group consisting of: (meth)acrylamides claim 7 , (meth)acrylates claim 7 , allyls claim 7 , benzoxanes claim 7 , cinnamyls claim 7 , epoxies claim 7 , fumarates claim 7 , maleates claim 7 , ...

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11-04-2013 дата публикации

Epoxidation of glycerol and derivatives therefrom

Номер: US20130090497A1
Принадлежит: AEL Mining Services Ltd

A method producing a surfactant from glycerol by converting glycerol, in a first step, to glycidol, polymerizing glycidol to an aliphatic alcohol and finally substituting a hydroxyl group with a substitute anion.

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18-04-2013 дата публикации

WATER/OIL REPELLENT AGENT AND WATER/OIL REPELLENT COMPOSITION

Номер: US20130092047A1
Автор: HOSHINO Taiki
Принадлежит: Asahi Glass Company, Limited

To provide a water/oil repellent agent and a water/oil repellent composition which are capable of imparting sufficient water/oil repellency to the surface of an article and which have low environmental impact. One comprising a reaction product obtained by reacting a fluorinated alcohol or amine having a polyfluoroalkyl moiety having at most 6 carbon atoms with a polyisocyanate compound, which is, when applied to an article, capable of imparting sufficient water/oil repellency, while presenting little environmental impact. When applied to an article, the water/oil repellent composition of the present invention is capable of imparting a high quality water/oil repellency to the article. 2. The water/oil repellent agent according to claim 1 , wherein the reaction product has no isocyanate group.3. The water/oil repellent agent according to claim 1 , wherein the Rin the fluorinated compound (a) is a Cperfluoroalkyl group.5. The water/oil repellent agent according to claim 1 , wherein the polyisocyanate compound (b) is hexamethylene diisocyanate or its modified product.6. The water/oil repellent agent according to claim 1 , which further contains a reaction product of a polyisocyanate compound (b) with a compound (c) having an active hydrogen group reactive with an isocyanate group claim 1 , or a reaction product of a polyisocyanate (b) with the fluorinated compound (a) and a compound (c) having an active hydrogen group reactive with an isocyanate group.7. A water/oil repellent composition which comprises the water/oil repellent agent as defined in and a solvent.8. The water/oil repellent composition according to claim 7 , which has a solid content concentration of from 0.05 to 10 mass %. The present invention relates to a water/oil repellent agent and a water/oil repellent composition.As a method for imparting water/oil repellency to the surface of an article (such as a fiber product), a method of treating the article by means of a water/oil repellent composition ...

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18-04-2013 дата публикации

Biguanide Compositions and Methods of Treating Metabolic Disorders

Номер: US20130095140A1
Принадлежит: Elcelyx Therapeutics, Inc.

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 2. A composition according to claim 1 , wherein{'sub': 2', '3', '4', '5', '6', '7, 'R, R, R, R, Rand Rare independently selected from H, methyl, ethyl, propyl or isopropyl; and'}{'sub': '1', 'Ris selected fromH,{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkenyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkynyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 3', '7', '2', '6, 'Cto Ccycloalkyl, Cto Cheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N,'}{'sub': 4', '12, 'Cto Calkylcycloalkyl,'}{'sub': 3', '11, 'Cto Calkylheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N and wherein N is present in the heterocyclic ring, the nitrogen atom may be in the form of an amide, carbamate or urea,'}phenyl, substituted phenyl, naphthyl, substituted naphthyl,alkylphenyl, alkylsubstituted phenyl, alkylnaphthyl, alkylsubstituted naphthyl,pyridyl, furanyl, thiophenyl, pyrrollyl, oxazolyl, isoxazolyl, thiazolyl, diazolyl, pyrazolyl ...

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18-04-2013 дата публикации

SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS

Номер: US20130096127A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I′; 3. The compound of wherein:{'sup': '1', 'sub': '1-7', 'Ris H or Calkyl;'}{'sup': 2', 'a', 'b', 'a', 'b, 'sub': 1-7', '3-7', '1-7', '1-7', '6-20', '1-7, 'Rfor each occurrence, is independently Calkyl, halo, Ccycloalkyl, hydroxy, Calkoxy, haloCalkyl, —NRR, Caryl, heteroaryl or heterocyclyl; wherein Rand Rfor each occurrence are independently H or Calkyl;'}{'sup': 3', '1', '1, 'Ris A-C(O)X;'}{'sup': '5', 'Ris H; and'}{'sup': 1', 'a', 'b, 'sub': '1-7', 'X and Xare independently OH, —O—Calkyl or NRR;'}{'sup': '1', 'Bis —C(O)NH— or —NHC(O)—;'}{'sup': '1', 'sub': 1-7', '3-7', '1-7', '3-7, 'Ais a linear or branched Calkylene; which is optionally substituted with one or more substituents independently selected from the group consisting of halo, Ccycloalkyl, Calkoxy, hydroxy and O-acetate; in which two geminal alkyl can optionally combine to form a Ccycloalkyl; or'}and wherein each heteroaryl is a monocyclic or bicyclic aromatic ring comprising 5-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms, and', 'each heterocyclyl is a monocyclic saturated or partially saturated but non-aromatic moiety comprising 4-7 ring atoms selected from carbon atoms and 1-5 heteroatoms, wherein each heteroatom of a heteroaryl or a heterocyclyl is independently selected from O, N and S, or a pharmaceutically acceptable salt thereof., 'n is 0, 1, 2, 3, 4 or 5;'}6. The compound of wherein Ais an optionally substituted linear or branched Calkylene claim 1 , or a pharmaceutically acceptable salt thereof.7. The compounds of wherein Ais CHCH claim 1 , or a pharmaceutically acceptable salt thereof.810-. (canceled)11. The compound of wherein Ris H claim 1 , Ris independently halo claim 1 , Calkoxy claim 1 , hydroxy claim 1 , Calkyl or halo-Calkyl claim 1 , n is 0 claim 1 , 1 or 2 and X and Xare independently OH or —O—Calkyl claim 1 , or a pharmaceutically acceptable salt thereof.12. The compounds of wherein n is 1 or 2; Ris meta-chloro ...

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18-04-2013 дата публикации

NOVEL THIOUREA OR UREA DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING AIDS, CONTAINING SAME AS ACTIVE INGREDIENT

Номер: US20130096138A1
Принадлежит: AVIXGEN INC.

Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS. 3. The thiourea or urea derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein the thiourea or urea derivative is selected from the group consisting of:1-(4-tert-butyl-benzoyl)-3-(5-hydroxy-naphthalen-1-yl)-thiourea1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-propyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-2,2-dimethyl-propyl)-thiourea,4-tert-butyl-N-(4-ethyl-piperazin-1-carbothioyl)-benzoamide,3-(4-tert-butyl-benzoyl)-1-(2-diethylamino-ethyl)-1-methyl-thiourea,3-(4-tert-butyl-benzoyl)-1-(2-dimethylamino-ethyl)-1-methyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-diethylamino-1-methyl-butyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-methyl-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-methyl-benzyl)-thiourea,1(4 tert-butyl-benzoyl)-3-(3-propylamino-propyl)-thiourea,1(4 tert-butyl-benzoyl)-3-phenethyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(naphthalen-2-ylmethyl)-thiourea,4-tert-butyl-N-[4-(4-fluoro-phenyl)-piperazin-1-carbothioyl]-benzamide,1-(4-tert-butyl-benzoyl)-3-cyclohexyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-fluoro-benzyl)-thiourea,1-benzoyl-3-(naphthalen-2-ylmethyl)-thiourea,1-benzoyl-3-[2-(4-chloro-phenyl)-ethyl]-thiourea,1-benzoyl-3-(4-diethylamino-1-methyl-butyl)-thiourea,3-benzoyl-1-(2-diethylamino-ethyl)-1-methyl-thiourea,N-(4-ethyl-piperazin-1-carbothioyl)-4-methyl-benzamide,1-cyclohexyl-3-(4-methyl-benzoyl)-thiourea,1-(4-chloro-benzyl)-3-(4-methyl-benzoyl)-thiourea,1-(3-dimethylamino-propyl)-3-(4-methyl-benzoyl)-thiourea,1-(4- ...

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18-04-2013 дата публикации

Creatine beta-alaninate: a novel salt for increasing athletic performance

Номер: US20130096193A1
Автор: Bruce W. Kneller
Принадлежит: Individual

Disclosed are creatine β-alaninate, compositions and formulations containing same, and methods of use therefor.

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25-04-2013 дата публикации

Curable polysiloxane coating composition

Номер: US20130101840A1
Принадлежит: 3M Innovative Properties Co

A curable composition comprises (a) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydroxysilyl moieties; (b) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydrosilyl moieties; and (c) at least one base selected from amidines, guanidines, phosphazenes, proazaphosphatranes, and combinations thereof; wherein at least one of the components (a) and (b) has an average reactive silane functionality of at least three.

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25-04-2013 дата публикации

PRODRUGS OF GABA ANALOGS, COMPOSITIONS AND USES THEREOF

Номер: US20130102641A1
Принадлежит: XenoPort, Inc.

The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. 141-. (canceled)46. The compound or a pharmaceutically acceptable salt or hydrate thereof according to claim 42 , wherein:{'sup': '13', 'Ris selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; and'}{'sup': '14', 'Ris hydrogen.'}47. The compound or a pharmaceutically acceptable salt or hydrate thereof according to claim 46 , wherein Ris methyl.48. The compound or a pharmaceutically acceptable salt or hydrate thereof according to claim 46 , wherein Ris isopropyl.49. compound or a pharmaceutically acceptable salt or hydrate thereof according to claim 42 , wherein Ris methyl claim 42 , ethyl claim 42 , propyl claim 42 , isopropyl claim 42 , butyl claim 42 , 1 claim 42 ,1-dimethoxyethyl or 1 claim 42 ,1-diethoxyethyl.50. A pharmaceutical composition comprising a compound of claim 42 , or a pharmaceutically acceptable salt or hydrate thereof claim 42 , and a pharmaceutically acceptable vehicle.51. The pharmaceutical composition of claim 50 , which is an oral sustained release dosage form.52. A method of treating preventing epilepsy claim 42 , depression claim 42 , anxiety claim 42 , psychosis claim 42 , faintness attacks claim 42 , hypokinesia claim 42 , cranial disorders claim 42 , neurodegenerative disorders claim 42 , panic claim 42 , pain claim 42 , inflammatory disease claim 42 , insomnia claim 42 , gastrointestinal disorders or ethanol withdrawal syndrome comprising administering a compound of to a patient claim 42 , wherein the compound treats or prevents epilepsy claim 42 , depression claim 42 , anxiety ...

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25-04-2013 дата публикации

Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives

Номер: US20130102794A1
Принадлежит: UCB PHARMA GMBH

The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

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25-04-2013 дата публикации

METHOD FOR SYNTHESIZING RARE EARTH METAL EXTRACTANT

Номер: US20130102806A1
Принадлежит:

A rare earth metal extractant containing, as the extractant component, dialkyldiglycol amide acid which is excellent in breaking down light rare earth elements is reacted in diglycolic acid (X mol) and an esterification agent (Y mol) at a reaction temperature of 70° C. or more and for a reaction time of one hour or more such that the mol ratio of Y/X is 2.5 or more, and is subjected to vacuum concentration. Subsequently, a reaction intermediate product is obtained by removing unreacted products and reaction residue, and an aprotic polar solvent is added as the reaction solvent. Then, the reaction intermediate product is reacted with dialkyl amine (Z mol) such that the mol ratio of Z/X is 0.9 or more and the aprotic polar solvent is removed. As a consequence, a rare earth metal extractant is efficiently synthesized at a low cost and at a high yield without having to use expensive diglycolic acid anhydride and harmful dichloromethane. 2. A method for synthesizing a rare earth metal extractant according to wherein the esterifying agent is selected from acetic anhydride and trifluoroacetic anhydride.3. A method for synthesizing a rare earth metal extractant according to wherein the aprotic polar solvent is selected from the group consisting of acetone claim 1 , acetonitrile claim 1 , tetrahydrofuran claim 1 , N claim 1 ,N-dimethylformamide claim 1 , and dimethyl sulfoxide.4. A method for synthesizing a rare earth metal extractant according to wherein in the step of reacting diglycolic acid with an esterifying agent claim 1 , the molar ratio of Y/X is in the range: 2.5≦Y/X≦6.5.5. A method for synthesizing a rare earth metal extractant according to wherein in the step of reacting the reaction intermediate product between diglycolic acid and esterifying agent with a dialkylamine claim 1 , the molar ratio of Z/X is in the range: 0.9≦Z/X≦1.2. This invention relates to a method for synthesizing a rare earth metal extractant, especially suited for the extraction and separation ...

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02-05-2013 дата публикации

AMINOGUANIDINEPHENYLPHOSPHINATE FLAME RETARDANT COMPOSITIONS

Номер: US20130105745A1
Принадлежит: BASF SE

The present invention relates to flame retardant polymer compositions which comprise aminoguanidine phenylphosphinates and mixtures with additional flame retardants. The compositions are especially useful for the manufacture of flame retardant compounds based on polyfunctional epoxides or polycondensates like polyesters, polyamides and polycarbonates. 2. A composition according to claim 1 , wherein in the aminoguanidine phenylphosphinate salt (I){'sub': 1', '5, 'R-Rrepresent hydrogen;'}{'sub': 6', '10', '1', '4, 'R-Rindependently of one another represent hydrogen or C-Calkyl; and'}x represents a number between 1.0 and 2.0.3. A composition according to claim 1 , wherein in the aminoguanidine phenylphosphinate salt (I){'sub': 1', '5, 'R-Rrepresent hydrogen;'}{'sub': 6', '10, 'R-Rrepresent hydrogen; and'}x represents a number between 1.0 and 2.0.4. A composition according to claim 1 , which comprises as component b) a polymer substrate selected from the group consisting of polyfunctional epoxide compounds claim 1 , hardener compounds and thermoplastic polymers.6. A composition according to claim 4 , which comprises as component b) a polymer substrate selected from the group consisting of polyfunctional epoxide compounds and a hardener compound that contains at least two amino or two hydroxy groups.7. A composition according to claim 1 , which additionally comprises further additives selected from the group consisting of polymer stabilizers and additional flame retardants.8. A composition according to claim 7 , which comprises an additional flame retardant selected from the group consisting of melamine polyphosphate claim 7 , ammonium polyphosphate claim 7 , melamine ammonium phosphate claim 7 , melamine ammonium polyphosphate claim 7 , melamine ammonium pyrophosphate claim 7 , a condensation product of melamine with phosphoric acid claim 7 , other reaction products of melamine with phosphoric acid and mixtures thereof.9. A composition according to claim 1 , which ...

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02-05-2013 дата публикации

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

Номер: US20130109866A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:a is 1 and b is 0.3. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': 5', '14, 'sub': 'n', 'Ris —S(O)R.'}4. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'sub': '3', 'Ris —CF.'}5) A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'Ris halogen.'}6. A compound according to claim 1 , wherein:a is 1 and b is 0;{'sup': 1', '11', '12', '13, 'sub': '1-8', 'Ris optionally substituted Calkyl, —NRRor —OR;'}{'sup': '2', 'sub': '1-8', 'Ris optionally substituted Calkyl;'}{'sup': 3', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 4', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 5', '14, 'sub': 3', 'n, 'Ris halogen, —CFor —S(O)R;'}n is 0, 1 or 2;{'sup': 6', '15', '13', '11', '−12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 7', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': '8', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '6-10, 'Ris hydrogen, optionally substituted Calkyl or optionally substituted Caryl;'}{'sup': '10', 'sub': '1-8', 'Ris hydrogen or optionally substituted C;'}{'sup': '11', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '12', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '13', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '14', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl; ...

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02-05-2013 дата публикации

METHOD FOR PRODUCING TOLUENEDICARBAMATE, METHOD FOR PRODUCING TOLUENEDIISOCYANATE, AND TOLUENEDICARBAMATE

Номер: US20130109881A1
Принадлежит:

A method for producing toluenedicarbamate includes a carbamate production process of producing toluenedicarbamate by reaction between toluenediamine, urea, and/or N-unsubstituted carbamic acid ester, and alcohol; and a benzoyleneurea reduction process of reducing a disubstituted benzoyleneurea and a derivative thereof to 10 mol or less relative to 100 mol of toluenedicarbamate, wherein the disubstituted benzoyleneurea is represented by formula (1) below and has a methyl group and an amino group: 3. The method for producing toluenedicarbamate according to claim 2 , wherein the biuret compound reduction process comprises a first biuret compound reduction process of reducing a first biuret compound represented by formula (2) above where Xand Xare amino groups.4. The method for producing toluenedicarbamate according to claim 3 , further comprising a urea feeding process of feeding urea to the carbamate production process claim 3 ,wherein in the first biuret compound reduction process,when the urea feeding process includes a fluid feeding process, in which urea is melted by heating to be in a fluid state, and to be fed to the carbamate production process, the time after the melting of urea to the completion of its feeding is set to within 2 hours,in the urea feeding process, urea is fed as a slurry to the carbamate production process, orin the urea feeding process, urea is fed in a solid state to the carbamate production process.5. The method for producing toluenedicarbamate according to claim 2 , wherein the biuret compound reduction process comprises a second biuret compound reduction process of reducing a second biuret compound represented by formula (2) above where Xis an amino group or an alkoxy group and Xis an alkoxy group.6. The method for producing toluenedicarbamate according to claim 5 , further comprising an N-unsubstituted carbamic acid ester production process of producing N-unsubstituted carbamic acid ester by reaction between urea and alcohol claim 5 , ...

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09-05-2013 дата публикации

Method for producing biobased chemicals from woody biomass

Номер: US20130115653A1
Принадлежит: Thesis Chemistry LLC

A method for utilizing woody biomass components, namely cellulose, hemicellose, and lignin, and converting them to value-added biobased chemical products is described herein. The present method provides treatments to obtain a plurality of component streams from woody biomass for producing derivative products while minimizing waste products.

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09-05-2013 дата публикации

CLEAN, HIGH-YIELD PREPARATION OF S,S AND R,S AMINO ACID ISOSTERES

Номер: US20130116457A1
Принадлежит: Aerojet Fine Chemicals LLC

The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction methods; (2) inversion methods; and (3) methods involving the epoxidation of alkenes. Using the various methods of the present invention, the R,S-epoxide and the intermediary compounds can be prepared reliably, in high yields and in high purity. 175.-. (canceled)77. The composition in accordance with claim 76 , wherein said non-chelating claim 76 , bulky reducing agent used in said method is a member selected from the group consisting of lithium aluminum t-butoxyhydride (LATBH) and sodium tris-t-butoxyborohydride (STBH).78. The method in accordance with claim 77 , wherein said non-chelating claim 77 , bulky reducing agent is lithium aluminum t-butoxyhydride (LATBH).79. The composition in accordance with claim 76 , wherein Ris a member selected from the group consisting of a benzyl group claim 76 , an S-phenyl group claim 76 , an alkyl group and para-nitrobenzene.80. The composition in accordance with claim 76 , wherein Xis a halogen.81. The composition in accordance with claim 80 , wherein Xis chloro or bromo.82. The composition in accordance with claim 76 , wherein Ris a blocking group selected from the group consisting of BOC claim 76 , MOC and CBZ.83. The composition in accordance with claim 76 , wherein the reduction is carried out in a solvent selected from the group consisting of diethyl ether claim 76 , THF claim 76 , MTBE claim 76 , glyme and diglyme.84. The composition in accordance with claim 83 , wherein said solvent is diethyl ether.85. The composition in accordance with claim 76 , wherein the reduction is carried out at a temperature ranging from about −30° C. to about 25° C.86. The composition in accordance with claim 85 , wherein the reduction is carried out at a temperature ranging from ...

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09-05-2013 дата публикации

PROCESS FOR PREPARING UREA

Номер: US20130116472A1
Автор: Auner Norbert
Принадлежит: SPAWNT PRIVATE S.A.R.L.

A method of producing urea includes reacting SiO/AlOor SiO/AlO-containing material, with addition of a carbon source, with gaseous nitrogen at elevated temperature to produce silicon nitride (SiN)/aluminum nitride (AlN) or silicon nitride/aluminum nitride-containing material; reacting the silicon nitride/aluminum nitride or silicon nitride/aluminum nitride-containing material in the presence of a basic alkali metal compound and/or alkaline-earth metal compound, with water at elevated temperature, to produce ammonia and alkali metal silicates/aluminates and/or alkaline earth metal silicates/aluminates; and reacting the ammonia with carbon dioxide to produce the urea. 1. A method of producing urea comprising:{'sub': 2', '2', '3', '2', '2', '3', '3', '4, 'reacting SiO/AlOor SiO/AlO-containing material, with addition of a carbon source, with gaseous nitrogen at elevated temperature to produce silicon nitride (SiN)/aluminum nitride (AlN) or silicon nitride/aluminum nitride-containing material;'}reacting the silicon nitride/aluminum nitride or silicon nitride/aluminum nitride-containing material in the presence of a basic alkali metal compound and/or alkaline-earth metal compound, with water at elevated temperature, to produce ammonia and alkali metal silicates/aluminates and/or alkaline earth metal silicates/aluminates; andreacting the ammonia with carbon dioxide to produce the urea.2. The method according to claim 1 , wherein the basic alkali metal compound and/or alkaline earth metal compound or a source thereof is added to the silicon nitride/aluminum nitride or silicon nitride/aluminum nitride-containing material before the addition of the water.3. The method according to claim 1 , wherein the basic alkali metal compound and/or alkaline earth metal compound or a source thereof comprises an SiO- or AlO-containing material.4. The method according to claim 1 , further comprising in addition to SiO/AlOor SiO/AlO-containing material as a starting material claim 1 , ...

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16-05-2013 дата публикации

UREA COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS

Номер: US20130123300A1
Принадлежит: CHINESE PLA GENERAL HOSPITAL

A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 2. A compound of Formula I , or an isomer , pharmaceutically acceptable salt or solvate thereof , whereinA represents=O;X represents F, Cl, Br or I;{'sub': 1', '2, 'Rrepresents phenyl, phenyl-C1-C6 alkyl-, wherein said phenyl is unsubstituted or substituted with 1-4 (e.g., 1-2, 1, 2, 3 or 4) substituents independently selected from the group consisting of: halogens, nitro, hydroxyl, amino, cyano, C1-C6 alkyl, C1-C6 alkoxy, and C1-C6 halogenated alkyl, and wherein said alkyl, alkoxy and halogenated alkyl may be optionally substituted with hydroxyl, —O—(C1-C4)-alkyl, oxo, amino, —NH—(C1-C4)-alkyl, or —N—[(C1-C6)-alkyl], or said alkyl, alkoxy and halogenated alkyl can optionally intervened by —O—, —S—, —NH—, —COO—, or —CONH—;'}{'sub': '2', 'thienyl, thiazolyl, wherein said thienyl, thiazolyl is unsubstituted or substituted with 1-3 substituents independently selected from the group consisting of: halogens, nitro, hydroxyl, amino, cyano, C1-C6 alkyl, C1-C6 alkoxy, and C1-C6 halogenated alkyl, and wherein said alkyl, alkoxy and halogenated alkyl may be optionally substituted with hydroxy, —O—(C1-C4)-alkyl, oxo, amino, —NH—(C1-C4)-alkyl, or —N—[(C1-C6)-alkyl], or said alkyl, alkoxy and halogenated alkyl can optionally be intervened by —O—, —S—, —NH—, —COO—;'}{'sub': 2', '3', '2', '3, 'Rand Rrepresent hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl ...

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16-05-2013 дата публикации

NOVEL CATIONIC LIPIDS AND METHODS OF USE THEREOF

Номер: US20130123338A1
Принадлежит: Protiva Biotherapeutics, Inc.

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art. 2. The cationic lipid of claim 1 , wherein Rand Rare independently selected from the group consisting of a methyl group and an ethyl group.3. The cationic lipid of claim 1 , wherein Rand Rare both methyl groups.4. The cationic lipid of claim 1 , wherein Rand Rare joined to form an optionally substituted heterocyclic ring having from 2 to 5 carbon atoms and from 1 to 3 heteroatoms selected from the group consisting of nitrogen (N) claim 1 , oxygen (O) claim 1 , sulfur (S) claim 1 , and combinations thereof.5. The cationic lipid of claim 1 , wherein X is O claim 1 , C(O)O claim 1 , C(O)N(R) claim 1 , N(R)C(O)O claim 1 , or C(O)S.6. The cationic lipid of claim 1 , wherein Ris selected from the group consisting of hydrogen (H) and an optionally substituted methyl group claim 1 , ethyl group claim 1 , or C-Calkyl claim 1 , alkenyl claim 1 , or alkynyl group.7. The cationic lipid of claim 1 , wherein X is an optionally substituted heterocyclic ring having from 2 to 5 carbon atoms and from 1 to 3 heteroatoms selected from the group consisting of nitrogen (N) claim 1 , oxygen (O) claim 1 , sulfur (S) claim 1 , and combinations thereof.8. The cationic lipid of claim 1 , wherein Y is (CH)and n is 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , or 6.9. The cationic lipid of claim 8 , wherein n is 2 claim 8 , ...

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16-05-2013 дата публикации

Aryl urea derivatives as n-formyl peptide receptors like-1 (fprl-1) receptor modulators

Номер: US20130123496A1
Принадлежит: Allergan Inc

The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

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23-05-2013 дата публикации

METHODS AND COMPOSITIONS FOR DELIVERY OF ACTIVE AGENTS

Номер: US20130129785A1
Принадлежит: ALNYLAM PHARMACEUTICALS, INC

A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction. 2. The compound of claim 1 , wherein X are Y are alkyl.3. The compound of claim 3 , wherein X and Y are both methyl.4. The compound of claim 1 , wherein Lis a linear alkylene unit.5. The compound of claim 1 , wherein Lis a linear alkylene unit.6. The compound of claim 5 , wherein Lcontains one or more double bonds and one or more cycloalkylene groups.7. The compound of claim 1 , wherein Rand Rare each claim 1 , independently claim 1 , C-Calkyl or C-Calkenyl.8. The compound of claim 7 , wherein one of Rand Ris a linear C-Calkyl or C-Calkenyl group and the other of Rand Ris a branched C-Calkyl or C-Calkenyl group.9. The compound of claim 1 , wherein Z is —C(O)O— claim 1 , —C(O)N(R)— claim 1 , —O(CO)N(R) claim 1 , —C(O)N(R)C(O)O— claim 1 , or —N(R)C(O)N(R)—.10. The compound of claim 1 , wherein Ris H or alkyl.11. The compound of claim 1 , wherein{'sub': 1', '4, 'X and Y are each, independently, C-Calkyl;'}{'sup': 1', '2, 'sub': 2', '10, 'Land Lare each, independently, an C-Clinear or branched alkylene linking unit, which may optionally contain one or more double bonds and further may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sub': 1', '2', '10', '30, 'Rand Rare each, independently, a C-Caliphatic group, which may optionally contain one or more double bonds, and may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3, 'Z is —C(O)O—, —OC(O)—, —C(O)N(R)—, —N(R)C(O)—, —O(CO)N(R), —N(R)C(O)O—, —C(O)N(R)C(O)O—, —OC(O)N(R)C(O)— or —N(R)C(O)N(R)—;'}{'sup': '3', 'sub': 1', '4, 'each occurrence of Ris independently H or C-Calkyl; and'}{'img': [{'@id': 'CUSTOM-CHARACTER-00003', '@ ...

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23-05-2013 дата публикации

Stabilized phenylcarbamate derivative in solid state

Номер: US20130131164A1
Принадлежит: Medichem Sa

The invention relates to retigabine with improved color quality, and to processes for preparing the same. In addition, the invention relates to a process for drying wet retigabine. Also, the invention relates to stabilized or substantially stabilized retigabine in solid state, or a mixture or pharmaceutical formulation comprising the same. Further, the invention also relates to an improved process for preparing retigabine.

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

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30-05-2013 дата публикации

Antimicrobial Molecules For Treating Multi-Drug Resistant and Extensively Drug Resistant Strains Of Mycobacterium

Номер: US20130137706A1
Принадлежит: POLYMEDIX, INC.

The present invention provides methods of inhibiting the growth of species or treating an animal having a infection (including multi-drug resistance strains and extensively drug resistant strains) by administering a compound of the invention, a salt thereof, or a composition comprising the same. 2. The method of wherein the compound or salt thereof is a compound of Formula I or salt thereof.47-. (canceled)912-. (canceled)13. The method of wherein the compound or salt thereof is a compound of Formula II or salt thereof.1416-. (canceled)17. The method of wherein the compound or salt thereof is a compound of Formula III or salt thereof.1820-. (canceled)22MycobacteriumMycobacterium Tuberculosis.. The method of wherein the species is23Mycobacterium Tuberculosis. The method of wherein the is a multi-drug resistant strain.24Mycobacterium Tuberculosis. The method of wherein the is an extensively drug resistant strain.26. The method of wherein the compound or pharmaceutically acceptable salt thereof is a compound of Formula I or a pharmaceutically acceptable salt thereof.2831-. (canceled)3336-. (canceled)37. The method of wherein the compound or pharmaceutically acceptable salt thereof is a compound of Formula II or pharmaceutically acceptable salt thereof.3840-. (canceled)41. The method of wherein the compound or pharmaceutically acceptable salt thereof is a compound of Formula III or pharmaceutically acceptable salt thereof.4244-. (canceled)46MycobacteriumMycobacterium Tuberculosis.. The method of wherein the infection is47Mycobacterium Tuberculosis. The method of wherein the is a multi-drug resistant strain.48Mycobacterium Tuberculosis. The method of wherein the is an extensively drug resistant strain.49. The method of wherein the compound or salt thereof is present in a composition.5052-. (canceled) The present invention is directed, in part, to methods of treating multi-drug resistant tuberculosis (MDR-TB) and extensively drug resistant tuberculosis (XDR-TB) with ...

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30-05-2013 дата публикации

HISTONE DEMETHYLASE INHIBITORS AND METHODS FOR USING THE SAME

Номер: US20130137720A1
Автор: Wang Xiang, Xu Wenqing

The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an α-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an α-ketoglutarate mimic. 1. A compound of the formula: M-L-K , or a derivative or a prodrug thereof , wherein M is a methyllysine mimic , L is a linker , and K is an α-ketoglutarate mimic.3. The compound according to claim 2 , wherein Ris phenyl claim 2 , naphthyl claim 2 , benzyl claim 2 , or naphthylalkyl claim 2 , each of which is optionally substituted claim 2 , or fluorescein.4. The compound according to claim 2 , wherein X is NH.5. The compound according to claim 2 , wherein Y is O.6. The compound according to claim 2 , wherein Z is O.7. The compound according to claim 2 , wherein Ris C-Calkylene.8. The compound according to claim 2 , wherein Rand Rare methylene.9. The compound according to claim 2 , wherein Aris phenylene.10. The compound according to claim 2 , wherein Ris H or methyl.11. The compound according to claim 2 , wherein Ris alkyl or absent.13. The compound according to claim 12 , wherein Ris hydrogen or C-Calkyl.14. The compound according to claim 12 , wherein Xand Xare O.15. The compound according to claim 12 , wherein Yis —OR.16. The compound according to claim 12 , wherein Lis C-Calkylene or C-Calkenylene.17. A method for treating a clinic condition associated with activity of Jumonji C Domain-Containing Histone Demethylase comprising administering to the subject in need of such a treatment a therapeutically effective amount of a compound of .18. The method of claim 17 , wherein the clinical condition is a cancer or a mental retardation.19. A method for treating a clinic condition associated with overexpression of Jumonji C Domain-Containing Histone ...

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30-05-2013 дата публикации

Treatment of Sleep-Wake Disorders

Номер: US20130137764A1
Принадлежит: SK Biopharmaceuticals Co Ltd

This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R 1 and R 2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R 1 and R 2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.

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06-06-2013 дата публикации

(METH)ACRYLIC ACID ESTER, ACTIVATION ENERGY RAY CURING COMPOSITION, AND INKJET RECORDING INK

Номер: US20130144057A1
Автор: MORITA Mitsunobu
Принадлежит:

(Meth)acrylic acid ester, which contains one or more partial structures each represented by the following formula 1 in a molecule thereof, wherein the partial structure is a urethane structure which does not have a hydrogen atom directly bonded to a nitrogen atom of the following formula 1: 3. The (meth)acrylic acid ester according to claim 2 ,wherein the ring structure A in the formula 3 is a morpholine ring.5. The (meth)acrylic acid ester according to claim 4 , wherein the ring structure B in the formula 4 is a piperidine ring.7. The (meth)acrylic acid ester according to claim 1 , wherein the (meth)acrylic acid ester contains two or more partial structures each represented by the formula 1 in a molecule thereof. 1. Field of the InventionThe present invention relates to novel (meth)acrylic acid ester, and an activation energy ray curing composition using the same, and an inkjet recording ink using the same.2. Description of the Related ArtAs a method for forming an image on a recording medium, such as paper, there are various methods, such as electrophotography, sublimation recording, thermal transfer recording, and inkjet recording. Among them, the inkjet recording has high efficiency in ink consumption, and therefore is excellent in resources saving, and can keep an ink cost per unit recording low. However, there are various problems when an aqueous ink is used. There are inks using organic solvent instead of water, but these inks also have different problems.Because of the reasons as mentioned, attentions have recently been attracted to inkjet recording using an activation energy ray-curing ink. The activation energy ray-curing ink has been described as a UV ray-curing ink composition in various literatures, and documents. Typically, the activation energy ray-curing ink contains a polymerization initiator and monomers as essential components, and optionally contains substances such as a pigment, oligomers, polymers, and a sensitizing agent (Optical Applied ...

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13-06-2013 дата публикации

METHOD FOR PRODUCTION OF F-18 LABELED GLUTAMIC ACID DERIVATIVES

Номер: US20130149243A1
Принадлежит: Bayer Intellectual Property GmbH

This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives. 2. The method according to wherein Step 3 comprises a solid-phase-extraction claim 1 , preferably a cation exchange solid phase.3. The method according to wherein the [F] fluorination reaction described in Step 1 is carried out at 0° C.-160° C.4. The method according to wherein the [F] fluorination agent used in Step 1 is generated from a base and [F]fluoride and the ratio of the base and compound of Formula II is greater than zero (>0) and equal or below 1 (≦1).5. The method according to wherein compound of Formula I has an isomeric purity of greater than 90%.6. The method according to wherein the method is automated and/or remote controlled.12. A method for obtaining a formulation comprising compound of Formula I claim 1 , Formula Ia claim 1 , or Formula Ib claim 1 , or mixture thereof comprises the step of adding one or more physiologically acceptable vehicle or carrier claim 1 , adjuvants or preservatives to a solution of compound of Formula I claim 1 , Formula Ia claim 1 , or Formula Ib claim 1 , or mixture thereof.13. Use of a device for carrying out the method according to for producing compound of Formula I.14. A Kit for producing of compound of Formula I according to comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a predefined quantity of compound of Formula II according to and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or more solid-phase extraction cartridges/columns for the purification of compound of Formula I according to .'} This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.Over the last few years, in vivo scanning using Positron Emission Tomography (PET) has increased. PET is both a medical and research tool. It is used in a variety of medical applications, including imaging of the brain, tumors, and components of cardiovascular system. Radiotracer consisting of a radionuclide ...

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13-06-2013 дата публикации

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

Номер: US20130149244A1
Принадлежит: Lantheus Medical Imaging, Inc.

The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. 4. The composition of claim 3 , wherein X is halide claim 3 , phosphate claim 3 , sulfate claim 3 , trifluoroacetate claim 3 , toluenesulfonate claim 3 , acetate claim 3 , formate claim 3 , citric claim 3 , ascorbate claim 3 , mesylate (methanesulfonate) claim 3 , or benzoate.6. The composition of claim 1 , wherein at least one Ris not hydrogen.921-. (canceled)24. (canceled)2648-. (canceled)49. The method of any one of claims 23 , wherein the step of reacting comprises exposing a compound comprising formula (II) or (IV) to a source of fluoride.50. The method of claim 49 , wherein the source of fluoride is isotopically enriched with F.5158-. (canceled)60. (canceled)62. (canceled)63. The salt of claim 61 , wherein the fluorine is isotopically enriched with F.64. A pharmaceutically acceptable composition comprising a salt of claim 63 , and optionally a pharmaceutically acceptable excipient.65. A kit comprising a salt of and instructions for use66. A method of imaging a subject claim 63 , comprising:{'claim-ref': {'@idref': 'CLM-00063', 'claim 63'}, 'administering a dose of a pharmaceutically acceptable composition comprising a salt of and optionally a pharmaceutically acceptable excipient, to a subject; and'}acquiring at least one image of a portion of the subject.6768-. (canceled)70. The method of ...

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13-06-2013 дата публикации

CLEAVABLE MODIFICATIONS TO REDUCIBLE POLY (AMIDO ETHYLENIMINES)S TO ENHANCE NUCLEOTIDE DELIVERY

Номер: US20130149783A1
Принадлежит:

Polyplex formulations were prepared using p(TETA/CBA), its PEGylated analog, p(TETA/CBA)-g-PEG2k, and mixtures of the two species at 10/90 and 50/50 wt %, respectively. Increasing PEG wt % inhibited polyplex formation. This work demonstrates the feasibility of preparing homogenous polyplexes by altering the PEG wt % using a mixture of p(TETA/CBA) and p(TETA/CBA)-g-PEG2k products. Further, a single-step method of making p(TETA/CBA)-g-PEG2k is disclosed. 1. A composition comprising a graft copolymer of poly(TETA/CBA) and polyethylene glycol.2. The composition of wherein the graft copolymer of poly(TETA/CBA) and polyethylene glycol has a structure as represented in Scheme 2 or Scheme 3.3. A complex comprising a nucleic acid and a graft copolymer of poly(TETA/CBA) and polyethylene glycol.4. The complex of wherein the nucleic acid comprises plasmid DNA.5. The complex of wherein the nucleic acid comprises siRNA.6. The complex of further comprising poly(TETA/CBA) mixed with the graft copolymer.7. A composition comprising a mixture of (a) poly(TETA/CBA) and (b) a graft copolymer of poly(TETA/CBA) and polyethylene glycol.8. A method of transfecting a cell comprising contacting the cell with a complex comprising a nucleic acid and a graft copolymer of poly(TETA/CBA) and polyethylene glycol.9. The method of wherein the nucleic acid comprises plasmid DNA.10. The method of wherein the nucleic acid comprises siRNA.11. The method of further comprising poly(TETA/CBA) mixed with the graft copolymer.12. A method of making a graft copolymer of poly(TETA/CBA) and polyethylene glycol claim 8 , the method comprising:(A) mixing TETA and CBA to form a first mixture and causing the first mixture to react for a first selected period of time to result in poly(TETA/CBA);(B) then adding polyethylene glycol to the first mixture to form a second mixture and causing the second mixture to react for a second selected period of time; and(C) purifying the graft copolymer of poly(TETA/CBA) and ...

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13-06-2013 дата публикации

Glutamate receptor modulators and therapeutic agents

Номер: US20130150416A1
Принадлежит:

The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds. 3. The method of wherein the disease or disorder is selected from the group consisting of cerebral deficits subsequent to cardiac bypass surgery and grafting claim 1 , cerebral ischemia claim 1 , stroke claim 1 , cardiac arrest claim 1 , spinal cord trauma claim 1 , head trauma claim 1 , perinatal hypoxia claim 1 , hypoglycemic neuronal damage claim 1 , AIDS-induced dementia claim 1 , ocular damage claim 1 , retinopathy claim 1 , muscular spasms claim 1 , convulsions claim 1 , migraine headaches claim 1 , urinary incontinence claim 1 , drug tolerance claim 1 , drug withdrawal claim 1 , drug cessation claim 1 , smoking cessation claim 1 , panic attack claim 1 , emesis claim 1 , brain edema claim 1 , neuropathic pain claim 1 , nociceptive pain claim 1 , Tourette's syndrome claim 1 , attention deficit disorder claim 1 , motor disorders claim 1 , tardive dyskinesia claim 1 , eating disorders claim 1 , sexual disorders claim 1 , obesity claim 1 , convulsive disorders claim 1 , circadian disorders claim 1 , neurodegenerative diseases claim 1 , amyelotrophic lateral sclerosis claim 1 , Parkinson's disease claim 1 , and multiple sclerosis claim 1 , ...

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20-06-2013 дата публикации

AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF

Номер: US20130158021A1
Принадлежит: Massachusetts Institute of Technology

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: 2. (canceled)3. The compound of claim 1 , wherein each instance of Q is O.4. The compound of claim 1 , wherein at least one instance of Ris H.5. The compound of claim 1 , wherein Ris a group of formula (iv).6. The compound of claim 1 , wherein L is an optionally substituted alkylene.811-. (canceled)1534-. (canceled)3750-. (canceled)5359-. (canceled)61. (canceled)62. The composition of claim 60 , wherein the composition is a pharmaceutical composition claim 60 , a cosmetic composition claim 60 , a nutraceutical composition claim 60 , or a composition with non-medical application.6377-. (canceled)79. The method of claim 78 , wherein the desired property is solubility in water claim 78 , solubility at different pH claim 78 , ability to bind polynucleotides claim 78 , ability to bind heparin claim 78 , ability to bind small molecules claim 78 , ability to bind protein claim 78 , ability to form microparticles claim 78 , ability to increase transfection efficiency claim 78 , ability to support cell growth claim 78 , ability to support cell attachment claim 78 , ability to support tissue growth claim 78 , and/or intracellular delivery of the APPL and/or an agent complexed or attached thereto to aid in bioprocessing.81. The method of claim 80 , wherein the disease claim 80 , disorder claim 80 , or condition is selected from the group consisting of ...

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20-06-2013 дата публикации

Trpm8 antagonists and their use in treatments

Номер: US20130158034A1
Принадлежит: AMGEN INC

Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

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20-06-2013 дата публикации

TRPV1 Antagonists

Номер: US20130158067A1
Принадлежит: AbbVie Inc.

Disclosed herein are compounds of formula (I): 2. The compound or salt according to claim 1 , wherein A is CH.3. The compound or salt according to claim 1 , wherein Xis O or N(R) claim 1 , and n is 2.4. The compound or salt according to claim 1 , wherein Xis O claim 1 , and n is 2.5. The compound or salt according to claim 1 , wherein Xis CH claim 1 , and n is 1.6. The compound or salt according to claim 1 , wherein L is CH.7. The compound or salt according to claim 1 , wherein L is a bond.8. The compound or salt according to claim 1 , wherein:A is CH;{'sup': 1', 'w, 'Xis O or N(R); and'}n is 2.9. The compound or salt according to claim 8 , wherein L is a bond.10. The compound or salt according to claim 8 , wherein L is CH.11. The compound or salt according to claim 10 , wherein Xis O.12. The compound or salt according to claim 1 , wherein:A is CH;{'sup': '1', 'sub': '2', 'Xis CH;'}n is 1; andLisa bond.14. The compound or salt according to claim 13 , wherein:A is CH;{'sup': 1', 'w, 'Xis O or N(R);'}n is 2; andL is a bond.15. The compound or salt according to claim 13 , wherein:A is CH;{'sup': '1', 'Xis O;'}n is 2; and{'sub': '2', 'L is CH.'}16. The compound or salt according to claim 13 , wherein:A is CH;{'sup': '1', 'sub': '2', 'Xis CH;'}n is 1; andL is a bond.18. The compound or salt according to claim 17 , wherein:A is CH;{'sup': '1', 'Xis O;'}n is 2; andL is a bond.19. The compound or salt according to claim 1 , wherein the compound is selected from the group consisting of:1-[(4R)-6,8-difluoro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-8-chloro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-2,2-dimethyl-7-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-7-chloro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-7-fluoro-2,2- ...

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20-06-2013 дата публикации

PROTEASE INHIBITORS

Номер: US20130158261A1
Принадлежит: TaiMed Biologics, Inc.

The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein Rmay be, for example, 2-pyridyl-CH—, 3-pyridyl-CH—, 4-pyridyl-CH—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R—CO)—, Rbeing selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONRR, CHOH or CHOR. 2. (canceled)3. The compound of claim 1 , wherein Cx is CHOH or CHOR.6. The compound of claim 1 , wherein Ris (CH)CH— claim 1 , 1-naphthyl-CH— claim 1 , or 2-naphthyl-CH—.8. The compound of claim 7 , wherein Cx is selected from the group consisting of COOH claim 7 , and CONRR.18. The compound of claim 16 , wherein Cx is CONRR.19. The compound of claim 18 , wherein Rand Rare H. This application claims priority to U.S. Provisional Application No. 60/846,084, filed Sep. 21, 2006, the entire contents of which are herein incorporated by reference.Inhibitors of the HIV viral protease are presently considered the most effective drugs against HIV infection. Unfortunately, most current proteases inhibitors are relatively large hydrophobic molecules that possess rather low bioavailability. A high pill burden is therefore required to attain the therapeutic dose in a patient. This is a deterrent, which too often results in patient non-compliance and inadequate treatment results. This situation leads to sub-optimal therapeutic drug concentration that in turns leads to the development of HIV resistant strains. Consequently, there is an urgent need to improve the solubility and bioavailability of proteases inhibitors.A unique class of amino acid based HIV protease inhibitors have been described in international application No ...

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20-06-2013 дата публикации

PROCESS FOR THE MANUFACTURE OF DABIGATRAN ETEXILATE

Номер: US20130158270A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

An improved process for preparing dabigatran etexilate, as well as analogous compounds of formula 7, 110-. (canceled)14. The compound according to claim 13 , wherein Ris n-hexyl.16. The compound according to claim 15 , wherein Ris methyl claim 15 , Ris ethyl and Hal is chlorine. Substituted (4-benzimidazol-2-ylmethylamino)-benzamidines, particularly dabigatran etexilate (CAS 593282-20-3), are already known from International Patent Application WO 98/37075 as active substances with a thrombin-inhibiting and thrombin time-prolonging activity. The main indication sectors of the compound of chemical formula I are the postoperative prophylaxis of deep vein thromboses and stroke prevention (prevention of stroke due to atrial fibrillation, SPAF for short).In WO 98/37075 it is proposed to produce the substituted (4-benzimidazol-2-ylmethyl-amino)-benzamidines by reacting corresponding substituted (4-benzimidazol-2-ylmethylamino)-benzonitriles with ammonia. This process is extremely onerous from the manufacturing point of view and results in a large quantity of acids that have to be disposed of (cf. also WO 2007/071743, WO 2007/ 071742).An improved process for preparing dabigatran etexilate and analogous compounds thereof is described hereinafter. By switching to new starting materials, the use of phase transfer catalysis and the formation of the benzimidazole without the use of coupling reagents a significantly more efficient synthesis of dabigatran etexilate is achieved. The high selectivity in the coupling of the intermediates (step 2) contributes significantly to the economy of the new synthesis route.The present invention describes a process for preparing compounds of formula 7:wherein R, Rand Rhere and hereinafter each independently of one another denote C-alkyl and Hal=chlorine or bromine, preferably chlorine, according to the invention haloacetic acid anhydride 5b-1, haloacetic acid 5b-2, ortho-haloacetate 5b-3 or haloacetyl chloride 5b-4 may be used for 5, and ...

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20-06-2013 дата публикации

NEW PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE MANUFACTURE NEP INHIBITORS

Номер: US20130158275A1
Принадлежит: NOVARTIS AG

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof. 2. A process according to wherein the transition metal catalyst comprises Palladium (Pd).5. A process according to claim 4 , wherein the reduction reaction is carried out with hydrogen in the presence of a transition metal catalyst.8. A process according to claim 7 , wherein the reduction reaction is carried out with hydrogen in the presence of a transition metal catalyst.11. The compound according to whereinR1 is hydrogen;R2 is BOC; andR3 is a carboxyl group; orR1 and R2 are hydrogen; andR3 is a carboxyl group13. The use of a compound according to claim 9 , in the synthesis of an NEP-inhibitor or a prodrug thereof claim 9 , such as a NEP inhibitor or prodrug thereof comprising a -amino- -biphenyl- -methylalkanoic acid claim 9 , or acid ester claim 9 , backbone14. The use according to claim 13 , wherein the NEP-inhibitor is N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid or a salt or a prodrug thereof.15. The use according to claim 14 , wherein the NEP-inhibitor prodrug is N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.16. A process for preparing N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester claim 9 , or a salt thereof claim 9 , comprising the manufacture of compound of formula (4) claim 9 , or salt thereof claim 9 , as defined in . The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, ...

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27-06-2013 дата публикации

Substituted saccharide compounds and dental compositions

Номер: US20130164709A1
Принадлежит: 3M Innovative Properties Co

Substituted saccharide compounds, dental compositions comprising substituted saccharide compounds, and methods of using dental compositions are described. In one embodiment, the substituted saccharide amide compound comprises a hydrophobic group and at least one free-radically polymerizable group with the proviso that the hydrophobic group is not bonded to the ethylenically unsaturated carbon atom of the free-radically polymerizable group. The hydrophobic group is typically bonded to a nitrogen atom of a saccharide amine residue or a carbonyl moiety of saccharide amide residue.

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27-06-2013 дата публикации

PHENYL CARBAMATE COMPOUNDS FOR USE IN PREVENTING OR TREATING STROKE

Номер: US20130165410A1
Автор: Choi Yong Moon
Принадлежит: Bio-Pharm Solutions Co., Ltd.

A phenyl carbamate compound; a composition for treating and/or preventing stroke containing the phenyl carbamate compound or a pharmaceutically acceptable salt thereof as an active ingredient; a method of treating and/or preventing stroke comprising administering the phenyl carbamate compound or a pharmaceutically acceptable salt thereof to a patient in need of stroke treatment; and a use of the phenyl carbamate compound or a pharmaceutically acceptable salt thereof in treating and/or preventing stroke, are provided. 3. The method according to claim 1 , wherein the compound is selected from the group consisting of:1-(2-chlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-methylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-propylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-isopropylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-cyclopropylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-cyclohexylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-benzylcarbamate,1-(2-chlorophenyl)-1-hydroxypropyl-2-N-bicyclo[2,2,1]heptanecarbamate,1-(2,4-dichlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxypropyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxybutyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxy-3-methyl-butyl-2-carbamate,1-(2,4-dichlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2,6-dichlorophenyl)-1-hydroxyhexyl-2-carbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-carbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-methylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-propylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-isopropylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-cyclopropylcarbamate,1-(2-chlorophenyl)-2-hydroxypropyl-1-N-cyclohexylcarbamate,1-(2- ...

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27-06-2013 дата публикации

ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF

Номер: US20130165479A1
Принадлежит: ABBVIE, INC.

The present application is directed to compounds that are TRPV1 antagonictc and have formula (I) 2. The compound according to wherein{'sub': 1', 'b, 'Yis —N(R)—;'}{'sub': '2', 'Yis O; and'}{'sub': 3', 'c, 'Yis —N(R)—.'}3. The compound according to claim 2 , wherein Lis cycloalkyl wherein the cycloalkyl is cyclopentyl or cyclohexyl.4. The compound of claim 3 , wherein Aris phenyl.5. The compound according to claim 4 , wherein the phenyl is unsubstituted or substituted with 1 claim 4 , 2 claim 4 , 3 claim 4 , 4 claim 4 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 4 , alkyl claim 4 , arylalkyl claim 4 , halogen claim 4 , haloalkyl claim 4 , or RRN— wherein Rand Rare each independently hydrogen claim 4 , alkyl claim 4 , or haloalkyl.6. The compound according to claim 5 , wherein{'sub': '1', 'Ris hydroxy; and'}{'sub': 2', '3', '4', '5, 'R, R, R, and Rare hydrogen.'}7. The compound according to claim 2 , wherein Lis a bond.8. The compound according to claim 7 , wherein Aris a monocyclic heterocycle fused to a phenyl.9. The compound of claim 8 , wherein{'sub': '1', 'Ris hydroxy;'}{'sub': '2', 'Ris hydrogen, and'}{'sub': '1', 'Aris 3,4-dihydro-2H-chromen-3-yl.'}10. The compound according to wherein Aris optionally substituted with 1 claim 9 , 2 claim 9 , 3 claim 9 , 4 claim 9 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 9 , alkyl claim 9 , arylalkyl claim 9 , halogen claim 9 , haloalkyl claim 9 , or RRN— wherein Rand Rare each independently hydrogen claim 9 , alkyl claim 9 , or haloalkyl.11. The compound according to claim 8 , wherein{'sub': '1', 'Ris hydroxy;'}{'sub': '2', 'Ris hydrogen; and'}{'sub': '1', 'Aris 3,4-dihydro-2H-chromen-4-yl.'}12. The compound according to wherein Aris optionally substituted with 1 claim 11 , 2 claim 11 , 3 claim 11 , 4 claim 11 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 11 , alkyl claim 11 , arylalkyl claim 11 , halogen claim 11 , ...

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27-06-2013 дата публикации

NEW GUANIDINE DERIVATIVES IN CINNAMIC SERIES

Номер: US20130165507A1

The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): 2. Derivatives claim 1 , isomers and salts according to claim 1 , of formula (I) in which the set (R claim 1 , R1 claim 1 , R2 claim 1 , R3 claim 1 , R4) is chosen from the group consisting of (H claim 1 , H claim 1 , H claim 1 , H claim 1 , H) claim 1 , (H claim 1 , NO2 claim 1 , H claim 1 , H claim 1 , H) claim 1 , (C1-C4 alkoxy claim 1 , H claim 1 , H claim 1 , H claim 1 , H) and (H claim 1 , C1-C4 alkoxy claim 1 , OH claim 1 , H claim 1 , H).3. Derivatives claim 1 , isomers and salts according to claim 1 , of formula (I) in which R1 and R2 together form a group OCH2O claim 1 , and R claim 1 , R3 and R4 each represent a hydrogen atom.4. Salt according to claim 1 , which is an addition salt of a mineral acid such as HCl claim 1 , HBr and H2SO4 claim 1 , or an addition salt of an organic acid such as methanesulfonic acid claim 1 , benzoic acid claim 1 , salicylic acid claim 1 , lactic acid claim 1 , citric acid claim 1 , D or L malic acid claim 1 , D glucuronic acid and hyaluronic acid.9. Synthetic intermediates according to claim 8 , of formula (III) in which the set (R claim 8 , R1 claim 8 , R2 claim 8 , R3 claim 8 , R4) is chosen from the group consisting of (H claim 8 , H claim 8 , H claim 8 , H claim 8 , H) claim 8 , (H claim 8 , NO2 claim 8 , H claim 8 , H claim 8 , H) claim 8 , (C1-C4 alkoxy claim 8 , H claim 8 , H claim 8 , H claim 8 , H) and (H claim 8 , C1-C4 alkoxy claim 8 , OH claim 8 , H claim 8 , H).11. Synthetic intermediates according to claim 10 , of formula (V) in which the set (R claim 10 , R1 claim 10 , R2 claim 10 , R3 claim 10 , R4) is chosen from the group consisting of (H claim 10 , H claim 10 , H claim 10 , H claim 10 , H) claim 10 , (H claim 10 , NO2 claim 10 , H claim 10 , H claim 10 , H) claim 10 , (C1-C4 alkoxy claim 10 , H claim 10 , H claim 10 , H claim 10 , H) and (H claim 10 , C1-C4 alkoxy claim 10 , OH claim 10 , H claim 10 , H).1213 ...

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27-06-2013 дата публикации

PHENYL ALKYL CARBAMATE DERIVATIVE COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

Номер: US20130165509A1
Автор: Choi Yong Moon
Принадлежит: Bio-Pharm Solutions Co., Ltd.

A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided. 3. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is in the form of racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , a mixture of enantiomer claim 1 , or a mixture of diastereomer.4. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from the group consisting of:1-(2-chlorophenyl)-2-carbamoyloxypropyl-1-carbamate,1-(2-chlorophenyl)-2-carbamoyloxypropyl-1-N-methylcarbamate,1-(2-chlorophenyl)-2-carbamoyloxypropyl-1-N-propylcarbamate1-(2-chlorophenyl)-2-carbamoyloxybutyl-1-carbamate,1-(2-chlorophenyl)-2-carbamoyloxy-3-methyl-butyl-1-carbamate,1-(2-chlorophenyl)-2-carbamoyloxyhexyl-1-carbamate,1-(2-iodophenyl)-2-carbamoyloxypropyl-1-carbamate,1-(2-iodophenyl)-2-carbamoyloxybutyl-1-carbamate,1-(2-iodophenyl)-2-carbamoyloxy-3-methyl-butyl-1-carbamate,1-(2-iodophenyl)-2-carbamoyloxyhexyl-1-carbamate,1-(2-fluorophenyl)-2-carbamoyloxypropyl-1-carbamate,1-(2-fluorophenyl)-2-carbamoyloxybutyl-1-carbamate,1-(2-fluorophenyl)-2-carbamoyloxy-3-methyl-butyl-1-carbamate,1-(2-fluorophenyl)-2-carbamoyloxyhexyl-1-carbamate,1-(2,4-dichlorophenyl)-2-carbamoyloxypropyl-1-carbamate,1-(2,4-dichlorophenyl)-2-carbamoyloxybutyl-1-carbamate,1-(2,4-dichlorophenyl)-2-carbamoyloxy-3-methyl-butyl-1-carbamate,1-(2,4- ...

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27-06-2013 дата публикации

PROCESS FOR PREPARATION OF OPTICALLY ACTIVE DIAMINE DERIVATIVE SALT

Номер: US20130165657A1
Принадлежит: Daiichi Sankyo Company, Limited

The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group. 3. The preparation process according to claim 1 , wherein the heating is performed at 50 to 80° C.4. The preparation process according to claim 1 , wherein the heating is performed at 70 to 75° C.5. The preparation process according to claim 1 , wherein the stirring step further comprises distilling off the organic solvent by 1/2 to 4/7 of the total volume of the organic solvent under reduced pressure in the range of 40 to 75° C. and then re-adding an organic solvent in an amount corresponding to the amount distilled off.6. The preparation process according to claim 5 , wherein the water content of the organic solvent is kept at less than 0.2% by weight in the distilling off of the organic solvent under reduced pressure and the re-addition.8. The preparation process according to claim 2 , wherein the hydrous organic solvent is a hydrous organic solvent containing 4% or more water.9. The preparation process according to claim 2 , wherein the hydrous organic solvent is a hydrous organic solvent containing 4 to 10% water.10. The preparation process according to claim 2 , wherein the treatment with anhydrous oxalic acid comprises adding dropwise a solution of anhydrous oxalic acid in an organic solvent.11. The preparation process according to claim 10 , wherein the dropwise addition is performed at 50 to 80° C.12. The preparation process ...

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04-07-2013 дата публикации

Cysteine protease inhibitors

Номер: US20130172232A1
Принадлежит: Medivir UK Ltd

Compounds of the formula I wherein R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a C 5 -C 10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; or R 3 is a C 2 -C 4 alkyl chain with at least 2 chloro or 3 fluoro substituents; or R 3 is C 3 -C 7 cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C 1 -C 4 alkyl, halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C 1 -C 6 alkylamino, C 1 -C 6 dialkylamino or; R 4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R 4 is Het, carbocyclyl, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

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04-07-2013 дата публикации

ANTHELMINTICS FOR PREVENTING PARASITIC INFECTIONS IN HUMANS AND ANIMALS

Номер: US20130172385A1
Принадлежит: LANXESS DEUTSCHLAND GMBH

The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths). 2. Compositions for deterring helmintic parasites according to claim 1 , characterized in that they comprise at least one compound of the formula (I) in which{'sub': 1', '6, 'Y represents hydrogen, C-C-alkyl or the radical O—X,'}{'sup': 11', '13, 'X represents hydrogen, CORor R,'}{'sup': '1', 'sub': 3', '7', '3', '7', '1', '2', '3', '7', '1', '2', '3', '7', '1', '6', '1', '6, 'Rrepresents C-C-cycloalkyl, C-C-cycloalkenyl, C-C-alkyl-C-C-cycloalkyl, C-C-alkyl-C-C-cycloalkenyl, where the cycloalkyl or cycloalkenyl rings of the abovementioned radicals are optionally substituted up to three times by C-C-alkyl or by a C-C-dialkylene bridge, or'}{'sup': '1', 'sub': 1', '7', '2', 'r', '2', 'r, 'Rrepresents C-C-alkyl, C-Calkenyl or C-Calkinyl,'}{'sup': 2', '11', '13, 'sub': 1', '6, 'R, R, Rare identical or different and represent C-C-alkyl,'}{'sup': 3', '8', '2', '3', '3', '7', '3', '5', '5', '7, 'sub': 1', '6, 'Rto Rare identical or different and represent hydrogen or C-C-alkyl, where Rand Ror Rand Ror Rand Ror Rand Rtogether with the atoms to which they are attached may also form a 5- or 6- membered monocyclic ring and'}n represents 1 and m represents 0.4. (canceled)5. Process for preparing compositions for deterring helminthic parasites claim 1 , characterized in that compounds of the formula (I) according to are mixed with extenders and/or surfactants.7. The method according to claim 3 , wherein the effective amount is 0.03 to 1 mg of compounds according to formula (I) per cmof skin. This application is a continuation of U.S. patent application Ser. No. 10/311,41 8 filed Jun. 12, 2003, incorporated herein by reference.The present invention relates to compositions comprising certain active compounds which are suitable as ...

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11-07-2013 дата публикации

DELTA CRYSTALLINE FORM OF THE ARGININE SALT OF PERINDOPRIL, A PROCESS FOR ITS PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT

Номер: US20130178464A1
Принадлежит: LES LABORATOIRES SERVIER

Delta crystalline form of the compound of formula (I): 2. The delta crystalline form according to claim 1 , having the following X-ray powder diffraction peaks measured using a diffractometer with a copper anticathode and expressed in terms of Bragg's angle 2 theta: 4.3 claim 1 , 11.0 claim 1 , 11.1 claim 1 , 11.9 claim 1 , 12.5 claim 1 , 13.2 claim 1 , 14.6 claim 1 , 16.0 claim 1 , 19.2 claim 1 , 19.4 claim 1 , 20.0 claim 1 , 21.9 claim 1 , 22.2 and 22.6.5. A process for the preparation of the delta crystalline form according to claim 1 , comprising crystallisation or recrystallisation from a binary mixture of acetonitrile claim 1 , ethyl acetate or methyl tert-butyl ether and dimethyl sulphoxide or a ternary mixture of acetonitrile claim 1 , dimethyl sulphoxide and toluene claim 1 , at a temperature higher than 20° C.6. The process according to claim 5 , wherein the binary mixture of acetonitrile claim 5 , ethyl acetate or methyl tert-butyl ether and dimethyl sulphoxide has a ratio of acetonitrile/dimethyl sulphoxide claim 5 , ethyl acetate/dimethyl sulphoxide or methyl tert-butyl ether/dimethyl sulphoxide ranging from 90/10 w/w to 10/90 w/w.7. The process according to claim 5 , wherein the temperature of the medium is between 25 and 80° C. claim 5 , inclusive.8. The process according to claim 7 , wherein the mixture is heated to a temperature of from 60 to 80° C.9. The process according to claim 5 , wherein the mixture is seeded with the delta crystalline form.10. A pharmaceutical composition comprising claim 1 , as active ingredient claim 1 , the delta crystalline form according to claim 1 , in combination with one or more inert claim 1 , non-toxic claim 1 , pharmaceutically acceptable carriers.11. The pharmaceutical composition according to claim 10 , further comprising a diuretic claim 10 , a calcium antagonist or an If current inhibitor.12. The pharmaceutical composition according to claim 11 , wherein the diuretic is indapamide.13. The pharmaceutical ...

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11-07-2013 дата публикации

PHENYL N-MUSTARD LINKED TO DNA-AFFINIC MOLECULES OR WATER-SOLUBLE ARYL RINGS, METHOD AND THEIR USE AS CANCER THERAPEUTIC AGENTS

Номер: US20130178494A1
Принадлежит: Academia Sinica

The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy. 3. The compound of claim 2 , wherein X and Y are the same.4. The compound of claim 3 , wherein X and Y are Cl.5. The compound of claim 2 , wherein Z is —NH.6. The compound of claim 2 , wherein Z′ is —NH.7. The compound of claim 2 , wherein Z′ is —NHNH.8. The compound of claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris independently hydrogen claim 1 , halogen claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , heterocyclyl claim 1 , aryl claim 1 , —OR claim 1 , —OC(O)R claim 1 , —SR claim 1 , —N(R) claim 1 , —N(R)C(O)R claim 1 , —C(O)N(R) claim 1 , —CN claim 1 , —NO claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , —S(O)R claim 1 , —SOR claim 1 , —SON(R) claim 1 , or —NHSOR.9. The compound of claim 8 , wherein each of R claim 8 , R claim 8 , R claim 8 , R claim 8 , Rand Ris selected from the group consisting of —H claim 8 , —OH claim 8 , —Cl claim 8 , —Br claim 8 , —F claim 8 , methyl claim 8 , ethyl claim 8 , methoxy claim 8 , ethoxy claim 8 , —C≡C-aryl claim 8 , phenyl claim 8 , naphthyl claim 8 , —NO claim 8 , —NH—Calkyl claim 8 , —C(O)CH claim 8 , —COH claim 8 , —COEt claim 8 , —CONH-aryl claim 8 , —CN claim 8 , N-morpholinyl claim 8 , —SO-alkyl claim 8 , and —SO-aryl.10. The compound of claim 2 , wherein Rand Rare taken together with their intervening atoms to form a heterocycle.11. The compound of claim 1 , wherein Rand Rare taken together with their intervening atoms to form a 6-membered aromatic ring claim 1 , wherein the ring is unsubstituted or substituted by one or more R′ group; and R′ is hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , heterocyclyl claim 1 , aryl claim 1 , —OR claim 1 , —OC(O)R claim 1 , —SR claim 1 , —N(R) claim 1 , —N(R)C(O)R claim 1 , —C(O)N(R) claim 1 , —CN claim 1 , —NO claim 1 , — ...

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