RU2016144410A - Позитивные аллостерические модуляторы никотинового рецептора ацетилхолина - Google Patents

Позитивные аллостерические модуляторы никотинового рецептора ацетилхолина Download PDF

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RU2016144410A
RU2016144410A RU2016144410A RU2016144410A RU2016144410A RU 2016144410 A RU2016144410 A RU 2016144410A RU 2016144410 A RU2016144410 A RU 2016144410A RU 2016144410 A RU2016144410 A RU 2016144410A RU 2016144410 A RU2016144410 A RU 2016144410A
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Йерген Эскилдсен
Анетте Гравен Самс
Аск Пюшль
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Х. Лундбекк А/С
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Claims (33)

1. Соединение согласно формуле [I]:
Figure 00000001
где R1, R2, R3, R4 и R5 означают Н;
R6 означает метоксиметил;
А7 означает C-R7, А8 означает N и А9 означает C-R9;
R7, R9, R10 и R11 выбирают, независимо друг от друга, из Н, C1-6-алкила, С2-6-алкенила, С2-6-алкинила, C1-6-алкокси и OR12, где
R12 означает моноциклический насыщенный остаток, имеющий 4-6 атомов в кольце, где один из вышеуказанных атомов кольца представляет собой О, а другие представляют собой С;
и его фармацевтически приемлемые соли.
2. Соединение по п. 1, где R7, R10 и R11 представляют собой Н.
3. Соединение по п. 1, где R9 представляет собой C1-4-алкокси.
4. Соединение по п. 1, где R9 представляет собой OR12, где R12 означает моноциклический насыщенный остаток, имеющий 4-6 атомов в кольце, где один из вышеуказанных атомов кольца представляет собой О, а другие представляют собой С.
5. Соединение по п. 1, обладающее диастереомерным избытком, по меньшей мере, 80%, таким как, по меньшей мере, 85%, таким как, по меньшей мере, 90%, таким как, по меньшей мере, 95%.
6. Соединение по п. 1, выбираемое из:
46: [(R)-1-(6-этоксипиридин-3-ил)-2-метоксиэтил]амида (1S,2S)-2-фенилциклопропанкарбоновой кислоты;
47: (1S,2S)-N-[(1R)-2-метокси-1-[6-[(3R)-тетрагидрофуран-3-ил]окси-3-пиридил]этил]-2-фенилциклопропанкарбоксамида;
48: (1S,2S)-N-[(1R)-2-метокси-1-[6-[(3S)-тетрагидрофуран-3-ил]окси-3-пиридил]этил]-2-фенилциклопропанкарбоксамида;
49: {(R)-2-метокси-1-[6-(тетрагидропиран-4-илокси)пиридин-3-ил]этил}амида (1S,2S)-2-фенилциклопропанкарбоновой кислоты;
и фармацевтически приемлемые соли любого из этих соединений.
7. Соединение по п. 1, представляющее собой
46: [(R)-1-(6-этоксипиридин-3-ил)-2-метоксиэтил]амида (1S,2S)-2-фенилциклопропанкарбоновой кислоты;
или его фармацевтически приемлемую соль.
8. Соединение по п. 1, представляющее собой
47: (1S,2S)-N-[(1R)-2-метокси-1-[6-[(3R)-тетрагидрофуран-3-ил]окси-3-пиридил]этил]-2-фенилциклопропанкарбоксамида;
или его фармацевтически приемлемую соль.
9. Соединение по п. 1, представляющее собой
48: (1S,2S)-N-[(1R)-2-метокси-1-[6-[(3S)-тетрагидрофуран-3-ил]окси-3-пиридил]этил]-2-фенилциклопропанкарбоксамида;
или его фармацевтически приемлемую соль.
10. Соединение по п. 1, представляющее собой
49: {(R)-2-метокси-1-[6-(тетрагидропиран-4-илокси)пиридин-3-ил]этил}амида (1S,2S)-2-фенилциклопропанкарбоновой кислоты или его фармацевтически приемлемую соль.
11. Соединение по любому из пп. 1-10 для применения в качестве лекарственного средства.
12. Соединение по любому из пп. 1-10 для применения в лечении заболевания или нарушения, выбираемого из психоза; шизофрении; когнитивных нарушений; когнитивного ухудшения, ассоциированного с шизофренией; синдрома гиперактивности с дефицитом внимания (ADHD); нарушений спектра аутизма; болезни Альцгеймера (AD); слабого когнитивного ухудшения (MCI); ухудшения памяти, ассоциированного с возрастом (AAMI); сенильной деменции; ассоциированной со СПИДом деменции; болезни Пика; деменции, ассоциированной с тельцами Леви; деменции, ассоциированной с синдромом Дауна; болезни Гентингтона; болезни Паркинсона (PD); обсессивно-компульсивного расстройства (OCD); травматического повреждения головного мозга; эпилепсии; посттравматического стресса; синдрома Вернике-Корсакова (WKS); посттравматической амнезии; когнитивного дефицита, ассоциированного с депрессией; диабетом, контролем массы, воспалительными нарушениями, ослабленным ангиогенезом; бокового амиотрофического склероза и боли.
13. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-10 и один или более фармацевтически приемлемых носителей или эксципиентов.
14. Набор, включающий соединение по любому из пп. 1-10 вместе со вторым соединением, выбираемым из перечня, состоящего из ингибиторов ацетилхолинэстеразы; антагонистов глутаматного рецептора глутамата; ингибиторов транспорта допамина; ингибиторов транспорта норадреналина; D2-антагонистов; частичных D2-агонистов; PDE10-антагонистов; 5-НТ2А-антагонистов; 5-НТ6-антагонистов; KCNQ-антагонистов; блокаторов литиевого, натриевого канала и энхансеров передачи сигнала GABA.
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