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RU2435759C2 - Производные бензимидазолов и их применение для модуляции гамка-рецепторного комплекса - Google Patents

Производные бензимидазолов и их применение для модуляции гамка-рецепторного комплекса Download PDF

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RU2435759C2
RU2435759C2 RU2008129868/04A RU2008129868A RU2435759C2 RU 2435759 C2 RU2435759 C2 RU 2435759C2 RU 2008129868/04 A RU2008129868/04 A RU 2008129868/04A RU 2008129868 A RU2008129868 A RU 2008129868A RU 2435759 C2 RU2435759 C2 RU 2435759C2
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Янус С. ЛАРСЕН (DK)
Янус С. Ларсен
Лене ТЕУБЕР (DK)
Лене Теубер
Филип К. АРИНГ (DK)
Филип К. АРИНГ
Эльсебет Эстергорд НИЛЬСЕН (DK)
Эльсебет Эстергорд Нильсен
Нахид МИРЗА (DK)
Нахид Мирза
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Abstract

Настоящее изобретение относится к новым производным бензимидазолов формулы (I), к любому из его изомеров или любой смеси его изомеров; или к его фармацевтически приемлемой соли, где R представляет собой -(CR'R'')n-Rc, где Rc представляет собой С1-6-алкил, R' представляет собой водород или C1-6-алкил, и R" представляет собой гидрокси; n равно 1; Х представляет собой N; и Y, Z и W представляют собой CRd, где каждый Rd представляет собой водород; Ro представляет собой галогено. Также изобретение относится к фармацевтической композиции, содержащей соединение формулы I, применению соединения формулы I и способу модулирования ГАМКА-рецепторного комплекса. Технический результат: получены новые производные бензимидазола, чувствительные к модуляции ГАМКА-рецепторного комплекса. 4 н. и 4 з.п. ф-лы, табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (8)

1. Соединение общей формулы I
Figure 00000093

любой из его изомеров или любая смесь его изомеров,
или его фармацевтически приемлемая соль,
где R представляет собой -(CR'R'')n-Rc, где Rc представляет собой C1-6-алкил, R' представляет собой водород или С1-6-алкил, и R" представляет собой гидрокси;
n равно 1;
Х представляет собой N; и
Y, Z и W представляют собой CRd, где каждый Rd представляет собой водород;
Ro представляет собой галогено.
2. Соединение по п.1, где R представляет собой 1-гидрокси-этил или 1-гидрокси-1-метил-этил.
3. Соединение по п.1, где Ro представляет собой хлоро или фторо.
4. Соединение по п.1, представляющее собой
(R)-1-{1-[3-(2-фтор-пиридин-3-ил)-фенил]-1Н-бензимидазол-5-ил}-этанол;
(S)-1-{1-[3-(2-фтор-пиридин-3-ил)-фенил]-1Н-бензимидазол-5-ил}-этанол;
2-{1-[3-(2-фтор-пиридин-3-ил)-фенил]-1Н-бензимидазол-5-ил}-пропан-2-ол;
2-{1-[3-(2-хлор-пиридин-3-ил)-фенил]-1Н-бензимидазол-5-ил}-пропан-2-ол;
любой из его изомеров или любую смесь его изомеров, или его фармацевтически приемлемую соль.
5. Фармацевтическая композиция, обладающая активностью модулятора ГАМК(гамма-аминомасляная кислота)А-рецепторного комплекса, содержащая терапевтически эффективное количество соединения по любому из пп.1-4, любого из его изомеров, или любой смеси его изомеров, или его фармацевтически приемлемой соли, вместе с по меньшей мере одним фармацевтически приемлемым носителем, эксципиентом или разбавителем.
6. Применение химического соединения по любому из пп.1-4, любого из его изомеров или любой смеси его изомеров, или его фармацевтически приемлемой соли, для изготовления лекарственного средства, обладающего активностью модулятора ГАМКА-рецепторного комплекса.
7. Применение по п.6 для изготовления фармацевтической композиции для лечения, предупреждения или облегчения заболевания, или расстройства, или состояния млекопитающего, где заболевание, расстройство или состояние чувствительно к модулированию ГАМКА-рецепторного комплекса.
8. Способ модулирования ГАМКА-рецепторного комплекса, включающий стадию введение терапевтически эффективного количества соединения по любому из пп.1-4, любого из его изомеров, или любой смеси его изомеров, или его фармацевтически приемлемой соли.
RU2008129868/04A 2006-03-24 2007-03-22 Производные бензимидазолов и их применение для модуляции гамка-рецепторного комплекса RU2435759C2 (ru)

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