RU2499795C2 - Антагонисты гистаминовых н3-рецепторов - Google Patents

Антагонисты гистаминовых н3-рецепторов Download PDF

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RU2499795C2
RU2499795C2 RU2011142654/04A RU2011142654A RU2499795C2 RU 2499795 C2 RU2499795 C2 RU 2499795C2 RU 2011142654/04 A RU2011142654/04 A RU 2011142654/04A RU 2011142654 A RU2011142654 A RU 2011142654A RU 2499795 C2 RU2499795 C2 RU 2499795C2
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pyridin
isopropylpiperazin
phenyl
pharmaceutically acceptable
acceptable salt
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RU2011142654A (ru
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Рольф Хольвег
Кнуд Эрик Андерсен
Ян Линди СЁРЕНСЕН
Жан Мари ЛУНДБЕК
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Хай Пойнт Фармасьютикалс, ЛЛС
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Abstract

Изобретение относится к новым соединениям, которые взаимодействуют с Н3-гистаминовым рецептором и содержат в своей структуре пиридиновое кольцо. Кроме того, изобретение относится к фармацевтической композиции для модуляции Н3-гистаминовых рецепторов, содержащей соединения, описанные выше. Технический результат: описанные соединения являются полезными в лечении ряда заболеваний или состояний, при которых взаимодействия с Н3-гистаминовым рецептором являются благоприятными, таким образом, данные соединения могут найти применение, например, в лечении заболеваний центральной нервной системы, периферической нервной системы, сердечно-сосудистой системы, пульмональной системы, желудочно-кишечного тракта и эндокринной системы. 2 н. и 7 з.п. ф-лы, 216 пр.

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Claims (9)

1. Соединение, которое выбрано из группы, включающей в себя:
N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}ацетамид;
N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}ацетамид;
4-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}морфолин;
N,N-Диизопропил-4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]бензамид;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперидин-1-ил)метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}морфолин-4-илметанон;
4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]-N,N-диметилбензамид;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}пиперидин-1-илметанон;
(4-Гидроксиметилпиперидин-1-ил)-{4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперазин-1-ил)метанон;
{4-[6-(4-Циклопропилпиперазин-1-ил)пиридин-3-ил]фенил}пиперидин-1-илметанон;
{4-[6-(4-Циклопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперазин-1-ил)метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метоксиметилпиперидин-1-ил)-метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}диметиламин;
1-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}-4-метилпиперазин;
(1-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}пиперидин-4-ил)метанол;
1-Изопропил-4-[5-(4-пиперидин-1-илметилфенил)пиридин-2-ил]пиперазин;
1-Циклопропил-4-[5-(4-пиперидин-1-илметилфенил)пиридин-2-ил]пиперазин;
или его фармацевтически приемлемая соль.
2. Соединение по п.1, которое представляет собой N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}ацетамид или его фармацевтически приемлемую соль.
3. Соединение по п.1, которое представляет собой N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}ацетамид или его фармацевтически приемлемую соль.
4. Соединение по п.1, которое представляет собой 4-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}морфолин или его фармацевтически приемлемую соль.
5. Соединение по п.1, которое представляет собой N,N-Диизопропил-4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]бензамид или его фармацевтически приемлемую соль.
6. Соединение по п.1, которое представляет собой {4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперидин-1-ил)метанон или его фармацевтически приемлемую соль.
7. Соединение по п.1, которое представляет собой {4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}морфолин-4-илметанон или его фармацевтически приемлемую соль.
8. Соединение по п.1, которое представляет собой 4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]-N,N-диметилбензамид или его фармацевтически приемлемую соль.
9. Фармацевтическая композиция для модуляции Н3-гистаминовых рецепторов, содержащая соединение по любому из пп.1-8 и фармацевтически приемлемый носитель или эксципиент.
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