RU2466127C2 - Бензилпиперидиновое производное - Google Patents

Бензилпиперидиновое производное Download PDF

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RU2466127C2
RU2466127C2 RU2010136952/04A RU2010136952A RU2466127C2 RU 2466127 C2 RU2466127 C2 RU 2466127C2 RU 2010136952/04 A RU2010136952/04 A RU 2010136952/04A RU 2010136952 A RU2010136952 A RU 2010136952A RU 2466127 C2 RU2466127 C2 RU 2466127C2
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piperidin
ethyl
benzyl
dihydro
bromo
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Томохиро ТОЙОДА (JP)
Томохиро ТОЙОДА
Хидефуми ЙОСИНАГА (JP)
Хидефуми ЙОСИНАГА
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ДАЙНИППОН СУМИТОМО ФАРМА Ко., ЛТД.
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Abstract

Раскрываются бензилпиперидиновое производное, представленное формулой (1), или его фармацевтически приемлемая соль, которые применимы в качестве лекарственного средства, такого как антидепрессант. В формуле (1) R1 представляет собой атом водорода или метильную группу; R2 представляет собой группу, присоединенную в пара- или мета-положении относительно метиленовой группы, и представляет собой атом хлора, присоединенный в пара-положении, атом брома, присоединенный в пара-положении, метильную группу, присоединенную в пара-положении, атом хлора, присоединенный в мета-положении, или атом брома, присоединенный в мета-положении; Х представляет собой метиленовую группу или атом кислорода; n равен целому числу от 1 до 3. 4 н. и 7 з.п. ф-лы, 34 пр., 14 табл., 7 ил.

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Claims (11)

1. Соединение, представленное формулой (1), или его фармацевтически приемлемая соль,
Формула 1
Figure 00000145

где в указанной формуле R1 представляет собой атом водорода или метильную группу; R2 представляет собой группу, присоединенную в пара- или мета-положении относительно метиленовой группы, связанной с пиперидиновым циклом, конкретно атом хлора, присоединенный в пара-положении, атом брома, присоединенный в пара-положении, метильную группу, присоединенную в пара-положении, атом хлора, присоединенный в мета-положении, или атом брома, присоединенный в мета-положении; X представляет собой метиленовую группу или атом кислорода; и n равен целому числу от 1 до 3.
2. Соединение по п.1 или его фармацевтически приемлемая соль, где X представляет собой метиленовую группу, и n равен целому числу 1 или 2, или где X представляет собой атом кислорода, и n равен целому числу 2 или 3.
3. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R1 представляет собой метильную группу.
4. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R2 представляет собой атом брома, присоединенный в пара-положении.
5. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где X представляет собой атом кислорода, и n равен целому числу 2.
6. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R1 представляет собой метильную группу, R2 представляет собой атом брома, присоединенный в пара-положении; Х представляет собой атом кислорода; и n равен целому числу 2.
7. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R1 представляет собой атом водорода, R2 представляет собой атом брома, присоединенный в пара-положении; X представляет собой атом кислорода; и n равен целому числу 2.
8. Соединение по п.1 или его фармацевтически приемлемая соль, где соединение, представленное формулой (1), выбрано из группы, включающей следующие соединения (01)-(15):
(01) 6-(2-{4-[4-бром-3-(2-гидроксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-1Н-инден-1-он,
(02) 7-(2-{4-[4-бром-3-(2-гидроксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидронафталин-1(2Н)-он,
(03) 6-(2-{4-[4-бром-3-(2-гидроксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он,
(04) 7-(2-{4-[4-бром-3-(2-гидроксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидро-1-бензоксепин-5(2Н)-он,
(05) 6-(2-{4-[4-хлор-3-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он,
(06) 6-(2-{4-[4-бром-3-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-1Н-инден-1-он,
(07) 7-(2-{4-[4-бром-3-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидронафталин-1(2Н)-он,
(08) 6-(2-{4-[4-бром-3-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он,
(09) 7-(2-{4-[4-бром-3-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидро-1-бензоксепин-5(2Н)-он,
(10) 6-(2-{4-[3-(2-метоксиэтокси)-4-метилбензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он,
(11) 6-(2-{4-[3-хлор-5-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он,
(12) 6-(2-{4-[3-бром-5-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-1Н-инден-1-он,
(13) 7-(2-{4-[3-бром-5-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидронафталин-1(2Н)-он,
(14) 6-(2-{4-[3-бром-5-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-2,3-дигидро-4Н-хромен-4-он и
(15) 7-(2-{4-[3-бром-5-(2-метоксиэтокси)бензил]пиперидин-1-ил}этил)-3,4-дигидро-1-бензоксепин-5(2Н)-он.
9. Фармацевтическая композиция, ингибирующая повторное поглощение серотонина, включающая соединение по любому из пп.1-8 или его фармацевтически приемлемую соль в качестве активного ингредиента.
10. Ингибитор повторного поглощения серотонина, включающий соединение по любому из пп.1-8 или его фармацевтически приемлемую соль в качестве активного ингредиента.
11. Антидепрессант или анксиолитическое лекарственное средство, включающее соединение по любому из пп.1-8 или его фармацевтически приемлемую соль в качестве активного ингредиента.
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