RU2008148325A - Полиморфные формы(2s)-(4е)-n-метил-5-(3-изопропоксипиридин)ил) 4-пентен-2амина для лечения расстройств центральной нервной системы - Google Patents
Полиморфные формы(2s)-(4е)-n-метил-5-(3-изопропоксипиридин)ил) 4-пентен-2амина для лечения расстройств центральной нервной системы Download PDFInfo
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Abstract
1. Кристаллический полиморф А (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, показывающий порошковую рентгенограмму с характеристическими пиками, выраженными в градусах (2-θ°): приблизительно 7,6 и 15,2 и 19,7. ! 2. Кристаллический полиморф В (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, показывающий порошковую рентгенограмму с характеристическими пиками, выраженными в градусах (2-θ°): приблизительно 8,0, 9,6 и 16,1. ! 3. Смесь полиморфов, содержащая полиморфы А по п.1 и B по п.2 в соотношениях 5:95-95:5. ! 4. Полиморф (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, где полиморф отделяют перекристаллизацией из этанола, метанола, изопропилового спирта, ацетона, этилацетата и/или ацетонитрила. ! 5. Кристаллический полиморф А, имеющий порошковую рентгенограмму, по существу, такую же, что показана в таблице 1. ! 6. Кристаллический полиморф В, имеющий порошковую рентгенограмму, по существу, такую же, что показана в таблице 2. ! 7. Полиоморф по любому одному из пп.1-6 для применения в терапии. ! 8. Применение полиморфа по любому одному из пп.1-6 в приготовлении лекарственного средства для лечения расстройств центральной нервной системы. ! 9. Способ лечения расстройств центральной нервной системы, включающий введение млекопитающему, нуждающемуся в таком лечении, терапевтически эффективного количества полиморфа по любому одному из пп.1-6. ! 10. Способ по п.9, где расстройство выбирают из группы, включающей возрастное нарушение памяти, умеренные когнитивные нарушения, предстарческое слабоумие (раннее начало болезни Альцгеймера), старческое слабоумие (слабоумие Альцгей
Claims (14)
1. Кристаллический полиморф А (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, показывающий порошковую рентгенограмму с характеристическими пиками, выраженными в градусах (2-θ°): приблизительно 7,6 и 15,2 и 19,7.
2. Кристаллический полиморф В (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, показывающий порошковую рентгенограмму с характеристическими пиками, выраженными в градусах (2-θ°): приблизительно 8,0, 9,6 и 16,1.
3. Смесь полиморфов, содержащая полиморфы А по п.1 и B по п.2 в соотношениях 5:95-95:5.
4. Полиморф (2S)-(4E)-N-метил-5-[3-(5-изопропоксипиридин)ил]-4-пентен-2-амина п-гидроксибензоата, где полиморф отделяют перекристаллизацией из этанола, метанола, изопропилового спирта, ацетона, этилацетата и/или ацетонитрила.
5. Кристаллический полиморф А, имеющий порошковую рентгенограмму, по существу, такую же, что показана в таблице 1.
6. Кристаллический полиморф В, имеющий порошковую рентгенограмму, по существу, такую же, что показана в таблице 2.
7. Полиоморф по любому одному из пп.1-6 для применения в терапии.
8. Применение полиморфа по любому одному из пп.1-6 в приготовлении лекарственного средства для лечения расстройств центральной нервной системы.
9. Способ лечения расстройств центральной нервной системы, включающий введение млекопитающему, нуждающемуся в таком лечении, терапевтически эффективного количества полиморфа по любому одному из пп.1-6.
10. Способ по п.9, где расстройство выбирают из группы, включающей возрастное нарушение памяти, умеренные когнитивные нарушения, предстарческое слабоумие (раннее начало болезни Альцгеймера), старческое слабоумие (слабоумие Альцгеймеровского типа), деменцию с тельцами Леви, сосудистую деменцию, болезнь Альцгеймера, удар, комплекс СПИД-деменции, синдром дефицита внимания, синдром дефицита внимания с гиперактивностью, дислексию, шизофрению, шизофреноподобное расстройство и шизоаффективное расстройство.
11. Способ по п.9, где расстройство выбирают из группы, включающей лечение от легкого до среднего слабоумия Альцгеймеровского типа, синдрома дефицита внимания, умеренного когнитивного нарушения и возрастного нарушения памяти.
12. Фармацевтическая композиция, содержащая в качестве активного компонента терапевтически эффективное количество полиморфа по любому одному из пп.1-6 вместе с одним или более фармацевтически пригодными разбавителями, наполнителями и/или инертными носителями.
13. Фармацевтическая композиция по п.12, предназначенная для лечения расстройств центральной нервной системы.
14. Агент для лечения расстройств центральной нервной системы, который содержит в качестве активного компонента полиморф по любому одному из пп.1-6.
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| SG185497A1 (en) * | 2010-05-20 | 2012-12-28 | Astrazeneca Ab | New process for the preparation of aryl substituted olefinic amines |
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