RU2007111957A - Пиперидиновое производное или его фармацевтически приемлемая соль - Google Patents

Пиперидиновое производное или его фармацевтически приемлемая соль Download PDF

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RU2007111957A
RU2007111957A RU2007111957/04A RU2007111957A RU2007111957A RU 2007111957 A RU2007111957 A RU 2007111957A RU 2007111957/04 A RU2007111957/04 A RU 2007111957/04A RU 2007111957 A RU2007111957 A RU 2007111957A RU 2007111957 A RU2007111957 A RU 2007111957A
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lower alkyl
substituted
pharmaceutically acceptable
acceptable salt
piperidine derivative
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RU2347775C2 (ru
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Казуми КИКУТИ (JP)
Казуми КИКУТИ
Дзиро ФУДЗИЯСУ (JP)
Дзиро ФУДЗИЯСУ
Тосихиро ВАТАНАБЕ (JP)
Тосихиро ВАТАНАБЕ
Юкинори НАГАКУРА (JP)
Юкинори НАГАКУРА
Хироси ТОМИЯМА (JP)
Хироси ТОМИЯМА
Мотохару СОНЕГАВА (JP)
Мотохару СОНЕГАВА
Казуо ТОКУЗАКИ (JP)
Казуо ТОКУЗАКИ
Йосинори ИВАИ (JP)
Йосинори ИВАИ
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Астеллас Фарма Инк. (Jp)
Астеллас Фарма Инк.
Котобуки Фармасьютикал Ко., Лтд. (Jp)
Котобуки Фармасьютикал Ко., Лтд.
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Claims (9)

1. Пиперидиновое производное, представленное следующей формулой (I):
Формула 1
Figure 00000001
где символы R1 - R4 каждый представляет собой любую из одновалентных групп, указанных ниже:
R1 представляет собой атом водорода, атом галогена, низший алкил, который может быть замещенным, -O-низший алкил, который может быть замещенным, -O-арил, арил, циклоалкил, -C(=O)-низший алкил, COOH, -C(=O)-O-низший алкил, -C(=O)-NH2, -C(=O)NH-низший алкил, -C(=O)N-(низший алкил)2, OH, -O-C(=O)-низший алкил, NH2, -NH-низший алкил, -N-(низший алкил)2, -NH-C(=O)-низший алкил, CN или NO2;
R2 и R3 могут быть одинаковыми или отличными друг от друга и каждый представляет собой атом водорода, низший алкил или атом галогена; и
R4 представляет собой низший алкил, который может быть замещенным, -O-низший алкил, который может быть замещенным, азотсодержащую гетероциклическую кольцевую группу, которая может быть замещенной, арил, который может быть замещенным, NH2, -NH-низший алкил, который может быть замещенным, или -N-(низший алкил, который может быть замещенным)2,
или его фармацевтически приемлемая соль.
2. Пиперидиновое производное или его фармацевтически приемлемая соль по п.1, где в формуле (I) одновалентная группа, представленная символом R4, представляет собой любую из одновалентных групп (a), (b) и (c), показанных ниже:
Формула 2
Figure 00000002
где в указанных выше группах (a), (b) и (c), символы A и B каждый представляет собой кольцо, показанное ниже, и символы R5 - R11 каждый представляет собой любую из одновалентных групп, показанных ниже.
A и B каждый представляет собой азотсодержащее гетероциклическое кольцо;
R5 и R8-R11 могут быть одинаковыми или отличными друг от друга и каждый представляет собой атом водорода, низший алкил, -C(=O)-O-низший алкил, который может быть замещенным, низший алкилен-O-низший алкил, циклоалкил или насыщенную или ненасыщенную 5- или 6-членную гетероциклическую кольцевую группу, имеющую 1-3 гетероатома, выбранных из N, S и О;
R6 представляет собой атом водорода, низший алкил, -O-низший алкил, -O-низший алкилен-O-, который связывается с одним атомом углерода из кольца A с образованием кольца, -C(=O)-O-низший алкил, который может быть замещенным, OH, -низший алкилен-OH или -C(=O)-гетероарил; и
R7 представляет собой атом водорода, низший алкил, -O-низший алкил, -C(=O)-O-низший алкил, OH, -низший алкилен-OH, или -C(=O)-гетероарил.
3. Пиперидиновое производное или его фармацевтически приемлемая соль по п.2, где символ R4 представляет собой одновалентную группу (a) и азотсодержащее гетероциклическое кольцо, представленное символом A, представляет собой пирролидиновое, пиперидиновое, морфолиновое, пиперазиновое или оксазепамовое кольцо.
4. Пиперидиновое производное или его фармацевтически приемлемая соль по п.2, где символ R4 представляет собой одновалентную группу (b) и азотсодержащее гетероциклическое кольцо, представленное символом B, представляет собой пирролидиновое или пиперидиновое кольцо.
5. Пиперидиновое производное или его фармацевтически приемлемая соль по п.2, где символ R4 представляет собой одновалентную группу (c) и R9 - R11 в группе (c) могут быть одинаковыми или отличными друг от друга и представляют собой, каждый, атом водорода, низший алкил, -C(=O)-O-низший алкил, который может быть замещенным, низший алкилен-O-низший алкил, циклоалкил или насыщенную или ненасыщенную 5- или 6-членную гетероциклическую кольцевую группу, имеющую 1-3 гетероатома, выбранных из N, S и O.
6. Пиперидиновое производное или его фармацевтически приемлемая соль по п.5, где, по меньшей мере, один из R9 - R11 в группе (c) представляет собой циклоалкил, а другой (другие) может быть таким же или отличным и представляет собой (представляют собой, каждый) атом водорода, низший алкил, -C(=O)-O-низший алкил, который может быть замещенным, низший алкилен-O-низший алкил, циклоалкил или насыщенную или ненасыщенную 5- или 6-членную гетероциклическую кольцевую группу, имеющую 1-3 гетероатома, выбранных из N, S и О.
7. Пиперидиновое производное или его фармацевтически приемлемая соль по любому из пп.1-6, где пиперидиновое производное, представленное формулой (I), представляет собой, по меньшей мере, одно соединение, выбранное из группы, состоящей из
4-(2-{4-[(E)-2-(2-метилфенил)винил]пиперидин-1-ил}-2-оксоэтил)морфолина,
4-(2-{4-[(E)-2-(4-изопропилфенил)винил]пиперидин-1-ил}-2-оксоэтил)морфолина,
4-(2-{4-[(E)-2-(4-хлорфенил)винил]пиперидин-1-ил}-2-оксоэтил)морфолина,
N-(2-{4-[(E)-2-(4-хлорфенил)винил]пиперидин-1-ил}-2-оксоэтил)циклогексанамина и
N-(2-{4-[(E)-2-(4-хлорфенил)винил]пиперидин-1-ил}-2-оксоэтил)-N-метилциклогексанамина.
8. Медицинская композиция, содержащая пиперидиновое производное или его фармацевтически приемлемую соль по любому из пп.1-7 и фармацевтически приемлемый носитель.
9. Медицинская композиция по п.8, которая представляет собой ингибитор натриевого канала.
RU2007111957/04A 2004-09-01 2005-08-31 Пиперидиновое производное или его фармацевтически приемлемая соль RU2347775C2 (ru)

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US8809380B2 (en) 2009-08-04 2014-08-19 Raqualia Pharma Inc. Picolinamide derivatives as TTX-S blockers

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GB2092569B (en) * 1981-02-05 1984-09-19 Farmos Oy Substituted imidazole derivatives and their preparation and use
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JPH0631230B2 (ja) * 1987-02-20 1994-04-27 山之内製薬株式会社 飽和ヘテロ環カルボン酸アミド誘導体
JPH0696532B2 (ja) * 1988-08-11 1994-11-30 山之内製薬株式会社 血小板活性化因子拮抗剤
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JP5025266B2 (ja) 2012-09-12
US20080070898A1 (en) 2008-03-20
MX2007002541A (es) 2007-05-09
IL181621A0 (en) 2007-07-04
EP1785415A4 (en) 2009-08-05
JPWO2006025471A1 (ja) 2008-05-08
BRPI0514812A (pt) 2008-06-24
ES2384574T3 (es) 2012-07-09
EP1785415B1 (en) 2012-05-02
ATE556052T1 (de) 2012-05-15
CA2578604A1 (en) 2006-03-09
CN101014570A (zh) 2007-08-08
EP1785415A1 (en) 2007-05-16
WO2006025471A1 (ja) 2006-03-09
NO20071480L (no) 2007-05-10
ZA200702379B (en) 2008-07-30
AU2005278469A1 (en) 2006-03-09
RU2347775C2 (ru) 2009-02-27

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