RU2015131137A - Производное амида коричной кислоты - Google Patents

Производное амида коричной кислоты Download PDF

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RU2015131137A
RU2015131137A RU2015131137A RU2015131137A RU2015131137A RU 2015131137 A RU2015131137 A RU 2015131137A RU 2015131137 A RU2015131137 A RU 2015131137A RU 2015131137 A RU2015131137 A RU 2015131137A RU 2015131137 A RU2015131137 A RU 2015131137A
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substituted
carbon atoms
compound
propenamide
fluorophenyl
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RU2015131137A
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Томохиро ООКУБО
Ко НАКАМУРА
Йоситака НАКАДЗАВА
Хиройоси НАНБА
Хироюки ЙОСИДА
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Ниппон Дзоки Фармасьютикал Ко., Лтд.
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Claims (56)

1. Соединение или его фармацевтически приемлемая соль или гидрат, где соединение представлено следующей общей формулой (I):
Figure 00000001
,
где n означает целое число от 0 до 4;
X1 и X2, являющиеся одинаковыми или различными, означают водород, фтор, трифторметил или карбокси, и один из X1 и X2 означает заместитель, иной чем водород;
R1 означает:
имидазолил, замещенный алкилом с 1-6 атомами углерода или фенилом;
пирролил, который может быть замещен алкилом с 1-4 атомами углерода;
фенил, замещенный амино, изоксазолилом или морфолино;
фенил, замещенный тиоморфолино, который может быть замещен оксо;
пиперазино, замещенный алкилом с 1-4 атомами углерода или циклогексилом;
тиоморфолино, который может быть замещен одним или двумя оксо; или
любой из заместителей, выбираемых из гуанидино, индазолила и циклогексиламино; и
R2 означает водород, циано или алкил с 1-4 атомами углерода, при условии, что в случае n=0, R1 означает заместитель, иной чем фенил, замещенный морфолино.
2. Соединение или его фармацевтически приемлемая соль или гидрат по п. 1, где R2 означает водород и где один из X1 и X2 означает водород, а другой означает фтор.
3. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает имидазолил, замещенный алкилом с 1-6 атомами углерода или фенилом.
4. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает пирролил, который может быть замещен алкилом с 1-4 атомами углерода.
5. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает фенил, замещенный амино, изоксазолилом или морфолино.
6. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает фенил, замещенный тиоморфолино, который может быть замещен оксо.
7. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает пиперазино, замещенный алкилом с 1-4 атомами углерода или циклогексилом.
8. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает тиоморфолино, который может быть замещен одним или двумя оксо.
9. Соединение или его фармацевтически приемлемая соль или гидрат по п. 2, где R1 означает любой из заместителей, выбираемых из гуанидино, индазолила и циклогексиламино.
10. Соединение или его фармацевтически приемлемая соль или гидрат по п. 1, которые выбирают из группы, состоящей из (E)-N-[2-(4-циклогексилпиперазин-1-ил)этил]-3-(2-фторфенил)-2-пропенамида, (E)-N-[3-(4-циклогексилпиперазин-1-ил)пропил]-3-(2-фторфенил)-2-пропенамида, (E)-3-(2-фторфенил)-N-[3-(4-метилпиперазин-1-ил)пропил]-2-пропенамида, (E)-3-(2-фторфенил)-N-[3-(изоксазол-5-ил)фенил]-2-пропенамида, (E)-3-(4-фторфенил)-N-(3-тиоморфолинопропил)-2-пропенамида, (E)-3-(2-фторфенил)-N-(3-тиоморфолинопропил)-2-пропенамида, (E)-N-[3-(1,1-диоксо-1,4-тиазинан-4-ил)пропил]-3-(2-фторфенил)-2-пропенамида, (E)-N-[3-(1,1-диоксо-1,4-тиазинан-4-ил)пропил]-3-(4-фторфенил)-2-пропенамида, (E)-3-(4-фторфенил)-N-[3-(1-оксо-1,4-тиазинан-4-ил)пропил]-2-пропенамида и (E)-3-(2-фторфенил)-N-[3-(1-оксо-1,4-тиазинан-4-ил)пропил]-2-пропенамида.
11. Соединение или его фармацевтически приемлемая соль или гидрат по п. 1, которые выбирают из группы, состоящей из (E)-3-(4-фторфенил)-N-(3-тиоморфолинопропил)-2-пропенамида, (E)-3-(2-фторфенил)-N-(3-тиоморфолинопропил)-2-пропенамида, (E)-3-(4-фторфенил)-N-[3-(1-оксо-1,4-тиазинан-4-ил)пропил]-2-пропенамида и (E)-3-(2-фторфенил)-N-[3-(1-оксо-1,4-тиазинан-4-ил)пропил]-2-пропенамида.
12. Фармацевтическое средство, включающее в качестве активного ингредиента, по меньшей мере одно соединение или его фармацевтически приемлимую соль или гидрат, где соединение представлено следующей общей формулой (I):
Figure 00000002
,
где n означает целое число от 0 до 4;
X1 и X2, являющиеся одинаковыми или различными, означают водород, фтор, трифторметил или карбокси, и один из X1 и X2 означает заместитель, иной чем водород;
R1 означает:
имидазолил, который может быть замещен алкилом с 1-6 атомами углерода или фенилом;
пирролил, который может быть замещен алкилом с 1-4 атомами углерода;
фенил, замещенный амино, алкокси с 1-4 атомами углерода, пиразолилом, изоксазолилом или морфолино;
фенил, замещенный тиоморфолино, который может быть замещен оксо;
пиперазино, который может быть замещен алкилом с 1-4 атомами углерода или циклогексилом;
тиоморфолино, который может быть замещен одним или двумя оксо; или
любой из заместителей, выбираемых из амино, карбокси, гуанидино, индолила, бензоимидазолила, индазолила, пиразолила, триазолила, пиридила, пирролидинила, пиперидино, гексаметиленимино, морфолино и циклогексиламино; и
R2 означает водород, циано или алкил с 1-4 атомами углерода.
13. Фармацевтическое средство по п. 12, которое представляет собой аналгетик.
14. Фармацевтическое средство по п. 13, где аналгетик представляет собой терапевтическое средство для лечения хронических болей.
15. Фармацевтическое средство по п. 14, где терапевтическое средство для лечения хронических болей представляет собой терапевтическое средство для лечения люмбаго, артралгии или невропатических болей.
16. Фармацевтическое средство по п. 13, где аналгетик представляет собой терапевтическое средство для лечения невропатических болей.
17. Фармацевтическое средство по любому из пп. 12-16, которое представляет собой пероральный препарат.
18. Фармацевтическое средство по любому из пп. 12-16, которое представляет собой инъекционный препарат.
19. Применение соединения или его фармацевтически приемлемой соли или гидрата в качестве фармацевтического средства, где соединение представлено следующей общей формулой (I):
Figure 00000003
,
где n означает целое число от 0 до 4;
X1 и X2, являющиеся одинаковыми или различными, означают водород, фтор, трифторметил или карбокси, и один из X1 и X2 означает заместитель, иной чем водород;
R1 означает:
имидазолил, который может быть замещен алкилом с 1-6 атомами углерода или фенилом;
пирролил, который может быть замещен алкилом с 1-4 атомами углерода;
фенил, замещенный амино, алкокси с 1-4 атомами углерода, пиразолилом, изоксазолилом или морфолино;
фенил, замещенный тиоморфолино, который может быть замещен оксо;
пиперазино, который может быть замещен алкилом с 1-4 атомами углерода или циклогексилом;
тиоморфолино, который может быть замещен одним или двумя оксо; или
любой из заместителей, выбираемых из амино, карбокси, гуанидино, индолила, бензоимидазолила, индазолила, пиразолила, триазолила, пиридила, пирролидинила, пиперидино, гексаметиленимино, морфолино и циклогексиламино; и
R2 означает водород, циано или алкил с 1-4 атомами углерода.
20. Применение по п. 19, где фармацевтическое средство представляет собой аналгетик.
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