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RU2007101685A - Модуляторы никотиновых ацетилхолиновых рецепторов альфа 7 и их терапевтические применения - Google Patents

Модуляторы никотиновых ацетилхолиновых рецепторов альфа 7 и их терапевтические применения Download PDF

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RU2007101685A
RU2007101685A RU2007101685/04A RU2007101685A RU2007101685A RU 2007101685 A RU2007101685 A RU 2007101685A RU 2007101685/04 A RU2007101685/04 A RU 2007101685/04A RU 2007101685 A RU2007101685 A RU 2007101685A RU 2007101685 A RU2007101685 A RU 2007101685A
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RU2007101685/04A
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RU2403247C2 (ru
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Джованни ГАВИРАГИ (IT)
Джованни ГАВИРАГИ
Кь ра ГИРОН (IT)
Кьяра Гирон
Хендрик БОТМАНН (IT)
Хендрик Ботманн
Ренца РОНКАРАТИ (IT)
Ренца РОНКАРАТИ
Георг Кристиан ТЕРСТАППЕНН (IT)
Георг Кристиан ТЕРСТАППЕНН
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СЬЕНА БИОТЕК С.п.А. (IT)
СЬЕНА БИОТЕК С.п.А.
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Claims (8)

1. Соединение общей формулы (I):
Figure 00000001
где Y представляет собой группу -CONH(Q)- или -NHCONH(Q)-;
Q представляет собой 5-10-членное ароматическое или гетероароматическое кольцо;
R представляет собой водород; галоген; линейный, разветвленный или циклический (С1-С6)алкил, галогеноалкил, алкокси или ацил; гидрокси; циано; нитро; моно- или ди-(С1-С6)алкиламино, ациламино или алкиламинокарбонил; карбамоил; (С6-С10)арил- или (С1-С6)алкилсульфониламино; (С6-С10)арил- или (С1-С6)алкилсульфамоил; 5-10-членное ароматическое или гетероароматическое кольцо, возможно замещенное: галогеном; линейным, разветвленным или циклическим (С1-С3)алкилом, галогеноалкилом, алкокси или ацилом; гидрокси; циано; нитро; амино; моно- или ди-(С1-С6)алкиламино, ациламино или алкиламинокарбонильной группами; карбамоилом; (С6-С10)арил- или (С1-С6)алкилсульфониламино; (С6-С10)арил- или (С1-С6)алкилсульфамоилом;
Х представляет собой группу
Figure 00000002
;
где Z представляет собой СН2, N или О;
m представляет собой целое число от 1 до 4;
р равен 0, 1 или 2;
R'', независимо друг от друга для р равного 2, выбран из группы, состоящей из водорода; моно- или ди-[линейного, разветвленного или циклического (С1-С6)алкил]аминокарбонила; линейного, разветвленного или циклического (С1-С6)алкила, алкокси, ацила;
его соли, изомеры, диастереомеры или рацемические смеси,
за исключением следующих соединений:
N-[4-(диметиламино)фенил]-1-пиперидинпентанамида,
N-(4-ацетилфенил)-1-пиперидинпентанамида,
N-(4-метоксифенил)-1-пиперидинпентанамида,
N-(4-нитрофенил)-1-пиперидинпентанамида,
N-фенил-1-пиперидинпентанамида,
N-(4-метилфенил)-1-пиперидинпентанамида,
N-(4-хлорфенил)-1-пиперидинпентанамида.
2. Соединение по п.1, где Y представляет собой -CONH(Q)-;
Q представляет собой 5-10-членное ароматическое или гетероароматическое кольцо;
R выбран из группы, состоящей из фенила; нафтила; пиридила; пиримидинила; хинолинила; изохинолинила; индолила; тиенила; бензотиенила; фуранила; бензофуранила; имидазолила; бензоимидазолила; пирролила; возможно замещенных, как указано в п.1;
Х представляет собой группу
Figure 00000002
;
где Z представляет собой CH2, N или О;
m представляет собой целое число от 1 до 4;
р равен 0, 1 или 2;
R'', независимо друг от друга, когда р равен 2, выбран из группы, состоящей из водорода; моно- или ди-[линейного, разветвленного или циклического (С1-С6)алкил]аминокарбонила; линейного, разветвленного или циклического (С1-С6)алкила, алкокси, ацила.
3. Соединение по п.1, где Y представляет собой -NHCONH(Q)-;
Q представляет собой 5-10-членное ароматическое или гетероароматическое кольцо;
R выбран из группы, состоящей из галогена; линейного, разветвленного или циклического (С1-С6)алкила, алкокси или алкиламино; галогеноалкила; фенила; нафтила; пиридила; пиримидинила; хинолинила; изохинолинила; индолила; тиенила; бензотиенила; фуранила; бензофуранила; имидазолила; бензоимидазолила; пирролила; возможно замещенных, как указано в п.1;
Х представляет собой группу
Figure 00000002
;
Z представляет собой CH2, N или О;
m представляет собой целое число от 1 до 4;
р равен 0, 1 или 2;
R'', независимо друг от друга, когда р равен 2, выбран из группы, состоящей из водорода; моно- или ди-[линейного, разветвленного или циклического (С1-С6)алкил]аминокарбонила; линейного, разветвленного или циклического (С1-С6)алкила, алкокси, ацила.
4. Фармацевтическая композиция, содержащая соединение по любому из пп.1-3 в комбинации с фармацевтически приемлемым носителем или эксципиентом.
5. Применение соединения по любому из пп.1-3 для получения лекарства для лечения неврологических, психиатрических, когнитивных, иммунологических и воспалительных расстройств.
6. Применение по п.5 для лечения болезни Альцгеймера.
7. Способ предупреждения или лечения заболеваний, состояний или дисфункций, связанных с никотиновыми ацетилхолиновыми рецепторами (nAChR) альфа 7, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения по любому из пп.1-3.
8. Способ по п.7 для предупреждения или лечения нейродегенеративного заболевания, в частности болезни Альцгеймера и шизофрении.
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