RU2007134901A - Метаболиты антагонистов nk-1 против рвоты - Google Patents

Метаболиты антагонистов nk-1 против рвоты Download PDF

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RU2007134901A
RU2007134901A RU2007134901/04A RU2007134901A RU2007134901A RU 2007134901 A RU2007134901 A RU 2007134901A RU 2007134901/04 A RU2007134901/04 A RU 2007134901/04A RU 2007134901 A RU2007134901 A RU 2007134901A RU 2007134901 A RU2007134901 A RU 2007134901A
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methyl
compound
hydroxypiperazin
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Кристоф ФУНК (CH)
Кристоф ФУНК
Торстен ХОФФМАНН (DE)
Торстен Хоффманн
Андреас КОБЛЕ (CH)
Андреас КОБЛЕ
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Ф. Хоффманн-Ля Рош Аг (Ch)
Ф. Хоффманн-Ля Рош Аг
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Abstract

1. Соединения формулы ! ! где ! R представляет собой метил и ! R1 представляет собой 4-метил-4-оксипиперазин-1-ил; или ! R представляет собой CH2OH и ! R1 представляет собой 4-метилпиперазин-1-ил или представляет собой 4-метил-4-оксипиперазин-1-ил; ! и их фармацевтически приемлемые кислотно-аддитивные соли. ! 2. Соединение по п.1, которое представляет собой 2-(3,5-бис-трифторметилфенил)-N-метил-N-[6-(4-метил-4-оксипиперазин-1-ил)-4-орто-толилпиридин-3-ил]-изобутирамид (соединение 1-1) или 2-(3,5-бис-трифторметилфенил)-N-[4-(2-гидроксиметилфенил)-6-(4-метилпиперазин-1-ил)-пиридин-3-ил]-N-метилизобутирамид (соединение 1-2). ! 3. Лекарство, содержащее одно или более соединений по п.1 или 2 и фармацевтически приемлемые эксципиенты. ! 4. Лекарство по п.3 для лечения заболеваний, относящихся к антагонистам рецептора NK-1. ! 5. Лекарство по пп.3 и 4 для лечения воспалительных состояний, включающих мигрень, ревматоидный артрит и астму, рвоты, болезни Паркинсона, боли, головной боли, особенно мигрени, болезни Альцгеймера, тревоги, депрессии, рассеянного склероза, смягчения отмены морфина, сердечно-сосудистых изменений, отека, аллергического ринита, болезни Крона, психоза, морской болезни и тошноты. ! 6. Применение соединения по п.1 или 2 для лечения заболеваний, относящихся к антагонистам рецептора NK-1. ! 7. Применение соединения по п.1 или 2 для изготовления лекарств для лечения заболеваний, относящихся к антагонистам рецептора NK-1. ! 8. Применение соединения по п.1 или 2 для изготовления лекарств для лечения воспалительных состояний, включающих мигрень, ревматоидный артрит и астму, рвоты, болезни Паркинсона, боли, головной боли, особенно мигрени, болезни Альцгеймера, тревоги, депресси

Claims (9)

1. Соединения формулы
Figure 00000001
где
R представляет собой метил и
R1 представляет собой 4-метил-4-оксипиперазин-1-ил; или
R представляет собой CH2OH и
R1 представляет собой 4-метилпиперазин-1-ил или представляет собой 4-метил-4-оксипиперазин-1-ил;
и их фармацевтически приемлемые кислотно-аддитивные соли.
2. Соединение по п.1, которое представляет собой 2-(3,5-бис-трифторметилфенил)-N-метил-N-[6-(4-метил-4-оксипиперазин-1-ил)-4-орто-толилпиридин-3-ил]-изобутирамид (соединение 1-1) или 2-(3,5-бис-трифторметилфенил)-N-[4-(2-гидроксиметилфенил)-6-(4-метилпиперазин-1-ил)-пиридин-3-ил]-N-метилизобутирамид (соединение 1-2).
3. Лекарство, содержащее одно или более соединений по п.1 или 2 и фармацевтически приемлемые эксципиенты.
4. Лекарство по п.3 для лечения заболеваний, относящихся к антагонистам рецептора NK-1.
5. Лекарство по пп.3 и 4 для лечения воспалительных состояний, включающих мигрень, ревматоидный артрит и астму, рвоты, болезни Паркинсона, боли, головной боли, особенно мигрени, болезни Альцгеймера, тревоги, депрессии, рассеянного склероза, смягчения отмены морфина, сердечно-сосудистых изменений, отека, аллергического ринита, болезни Крона, психоза, морской болезни и тошноты.
6. Применение соединения по п.1 или 2 для лечения заболеваний, относящихся к антагонистам рецептора NK-1.
7. Применение соединения по п.1 или 2 для изготовления лекарств для лечения заболеваний, относящихся к антагонистам рецептора NK-1.
8. Применение соединения по п.1 или 2 для изготовления лекарств для лечения воспалительных состояний, включающих мигрень, ревматоидный артрит и астму, рвоты, болезни Паркинсона, боли, головной боли, особенно мигрени, болезни Альцгеймера, тревоги, депрессии, рассеянного склероза, смягчения отмены морфина, сердечно-сосудистых изменений, отека, аллергического ринита, болезни Крона, психоза, морской болезни и тошноты.
9. Применение соединения по п.1 или 2 для изготовления лекарств для лечения рвоты.
RU2007134901/04A 2005-03-23 2006-03-14 Метаболиты антагонистов nk-1 против рвоты RU2404969C2 (ru)

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CN112174881B (zh) * 2019-07-04 2022-06-21 上海森辉医药有限公司 一种奈妥匹坦的衍生物及其制备方法

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MX2007011489A (es) 2007-10-11
IL185689A0 (en) 2008-01-06
CN101146775B (zh) 2012-07-18
EP1863767A1 (en) 2007-12-12
US7211579B2 (en) 2007-05-01
BRPI0609699A2 (pt) 2010-04-20
PT1863767E (pt) 2009-03-27
DE602006005624D1 (de) 2009-04-23
ATE425144T1 (de) 2009-03-15
KR20070107146A (ko) 2007-11-06
PL1863767T3 (pl) 2009-08-31
US20060217393A1 (en) 2006-09-28

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