RU2021111037A - Производные аминопиридина и их применение в качестве селективных ингибиторов alk-2 - Google Patents

Производные аминопиридина и их применение в качестве селективных ингибиторов alk-2 Download PDF

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RU2021111037A
RU2021111037A RU2021111037A RU2021111037A RU2021111037A RU 2021111037 A RU2021111037 A RU 2021111037A RU 2021111037 A RU2021111037 A RU 2021111037A RU 2021111037 A RU2021111037 A RU 2021111037A RU 2021111037 A RU2021111037 A RU 2021111037A
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disease
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heterotopic ossification
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RU2021111037A3 (ru
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Цзялян Ли
Лука Ариста
Срихари Бабу
Цзяньвэй Бянь
Кай Цуй
Майкл Патрик Диллон
Рене Латтманн
Лв Ляо
Димитриос Лизос
Рита Рамос
Николаус Йоханнес Штифль
Томас Улльрих
Пегги Уссельманн
Сяоян Ван
Лиладхар Мурлидхар Вайколе
Свен Вайлер
Юйбо Чжан
Ицзун Чжоу
Тинин Чжу
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Новартис Аг
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    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Claims (14)

1. Соединение, представляющее собой дигидрат фумарата 2-амино-N-(4-гидрокси-бицикло[2.2.2]октан-1-ил)-5-(4-((1R,5S)-3-(тетрагидро-2H-пиран-4-ил)-3-азабицикло[3.1.0]гексан-1-ил)фенил)никотинамида.
2. Соединение по п.1 в кристаллической форме, характеризующейся диаграммой XRPD (порошковая рентгеновская дифракция) с пиками при углах 2-тета (±2 градуса) 7,0, 14,2, 15,6, 16,2, 18,0, 19,2 и 25.5.
3. Соединение по п.2, обладающее термограммой DSC, которая характеризуется эндотермическим пиком при температуре около 160°C.
4. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по любому из пп.1-3 и один или несколько фармацевтически приемлемых носителей.
5. Способ подавления активности рецептора активиновой рецепторподобной киназы 2 (ALK-2) у субъекта, включающий введение субъекту терапевтически эффективного количества соединения по любому из пп.1-3 или фармацевтической композиции по п.4.
6. Способ лечения расстройства или заболевания, выбранного из гетеротопической оссификации или прогрессирующей оссифицирующей фибродисплазии, включающий введение субъекту терапевтически эффективного количества соединения по любому из пп.1-3 или фармацевтической композиции по п.4.
7. Способ по п.6, где расстройство представляет собой гетеротопическую оссификацию.
8. Способ по п.6, где расстройство представляет собой прогрессирующую оссифицирующую фибродисплазию.
9. Соединение по любому из пп.1-3 для применения в качестве лекарственного средства для лечения расстройства или заболевания, выбранного из гетеротопической оссификации или прогрессирующей оссифицирующей фибродисплазии.
10. Соединение для применения по п.9, где расстройство или заболевание представляет собой гетеротопическую оссификацию.
11. Соединение для применения по п.9, где расстройство или заболевание представляет собой оссифицирующую фибродисплазию.
12. Применение соединения по любому из пп.1-3 для получения лекарственного средства для лечения расстройства или заболевания, выбранного из гетеротопической оссификации или прогрессирующей оссифицирующей фибродисплазии.
13. Применение по п.12, где расстройство или заболевание представляет собой гетеротопическую оссификацию.
14. Применение по п.12, где расстройство или заболевание представляет собой оссифицирующую фибродисплазию.
RU2021111037A 2016-07-20 2017-07-18 Производные аминопиридина и их применение в качестве селективных ингибиторов alk-2 RU2777979C2 (ru)

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