RU2011113443A - Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов - Google Patents

Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов Download PDF

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RU2011113443A
RU2011113443A RU2011113443/04A RU2011113443A RU2011113443A RU 2011113443 A RU2011113443 A RU 2011113443A RU 2011113443/04 A RU2011113443/04 A RU 2011113443/04A RU 2011113443 A RU2011113443 A RU 2011113443A RU 2011113443 A RU2011113443 A RU 2011113443A
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Хосе Мария Сид-Нуньес
Андрес Авелино Трабанко-Суарес
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Орто-Макнейл-Янссен Фармасьютикалз, Инк.
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Abstract

1. Соединение формулы (I)или его стереохимически изомерная форма, гдеRпредставляет собой Cалкил или Cалкил, замещенный Сциклоалкилом, галогено, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;Rпредставляет собой галогено, трифторметил, Cалкил или циклопропил;Rпредставляет собой водород, галогено или трифторметил;n равно 1 или 2;Х представляет собой -СНСН-O, -СН=СН- или -CHCH-;Y представляет собой -О- или -CR(OH)-;Rпредставляет собой водород или Cалкил;или его фармацевтически приемлемые соль или сольват.2. Соединение по п.1, гдеRпредставляет собой Cалкил или Cалкил, замещенный Сциклоалкилом, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;Rпредставляет собой галогено, трифторметил, Cалкил или циклопропил;Rпредставляет собой водород, галогено или трифторметил;n равно 1 или 2;Х представляет собой -СНСН-O-, -СН=СН- или -СНСН-;Y представляет собой -О- или -CR(OH)-;Rпредставляет собой водород или Cалкил;или его фармацевтически приемлемые соль или сольват.3. Соединение по п.1, гдеRпредставляет собой 1-бутил, 2-метил-1-пропил, 3-метил-1-бутил, (циклопропил)метил или 2-(циклопропил)-1-этил;Rпредставляет собой хлоро, бромо, циклопропил или трифторметил;Rпредставляет собой водород, или хлоро, или трифторметил;n равно 2;Х представляет собой -CHCH-O- или -СН=СН-;Y представляет собой -О- или -CR(OH)-;Rпредставляет собой водород или Cалкил;или его фармацевтически приемлемые соль или сольват.4. Соединение по п.1, представляющее собойтранс-1-бутил-3-хлор-4-[1-(4-гидрокси-циклогексил)-1Н-индол-5-ил]-1Н-пиридин-2-он (Е3) илитранс-1-бутил-3-хлор-4-[1-(4-гидрокси-4-метил-циклогексил)-1Н-индол-5-ил]-1H-пиридин-2-он (Е5).5. Фармацевтическая композиция,

Claims (16)

1. Соединение формулы (I)
Figure 00000001
или его стереохимически изомерная форма, где
R1 представляет собой C1-6алкил или C1-3алкил, замещенный С3-7циклоалкилом, галогено, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;
R2 представляет собой галогено, трифторметил, C1-3алкил или циклопропил;
R3 представляет собой водород, галогено или трифторметил;
n равно 1 или 2;
Х представляет собой -СН2СН2-O, -СН=СН- или -CH2CH2-;
Y представляет собой -О- или -CR4(OH)-;
R4 представляет собой водород или C1-3алкил;
или его фармацевтически приемлемые соль или сольват.
2. Соединение по п.1, где
R1 представляет собой C1-6алкил или C1-3алкил, замещенный С3-7циклоалкилом, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;
R2 представляет собой галогено, трифторметил, C1-3алкил или циклопропил;
R3 представляет собой водород, галогено или трифторметил;
n равно 1 или 2;
Х представляет собой -СН2СН2-O-, -СН=СН- или -СН2СН2-;
Y представляет собой -О- или -CR4(OH)-;
R4 представляет собой водород или C1-3алкил;
или его фармацевтически приемлемые соль или сольват.
3. Соединение по п.1, где
R1 представляет собой 1-бутил, 2-метил-1-пропил, 3-метил-1-бутил, (циклопропил)метил или 2-(циклопропил)-1-этил;
R2 представляет собой хлоро, бромо, циклопропил или трифторметил;
R3 представляет собой водород, или хлоро, или трифторметил;
n равно 2;
Х представляет собой -CH2CH2-O- или -СН=СН-;
Y представляет собой -О- или -CR4(OH)-;
R4 представляет собой водород или C1-3алкил;
или его фармацевтически приемлемые соль или сольват.
4. Соединение по п.1, представляющее собой
транс-1-бутил-3-хлор-4-[1-(4-гидрокси-циклогексил)-1Н-индол-5-ил]-1Н-пиридин-2-он (Е3) или
транс-1-бутил-3-хлор-4-[1-(4-гидрокси-4-метил-циклогексил)-1Н-индол-5-ил]-1H-пиридин-2-он (Е5).
5. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по любому из пп.1-4 и фармацевтически приемлемый носитель или эксципиент.
6. Соединение по любому из пп.1-4 для применения в качестве лекарственного средства.
7. Соединение по любому из пп.1-4 или фармацевтическая композиция по п.5 для применения в лечении или предупреждении заболевания или состояния у млекопитающего, включая человека, на лечение или предупреждение которого влияет или лечению или предупреждению которого способствует нейромодуляторный эффект положительных аллостерических модуляторов метаботропного глутаматного рецептора mGluR2.
8. Соединение по любому из пп.1-4 или фармацевтическая композиция по п.5 для применения в лечении или предупреждении расстройства центральной нервной системы, выбранного из тревожных расстройств, психотических расстройств, расстройств личности, расстройств, связанных с приемом веществ, расстройств приема пищи, расстройств настроения, мигрени, эпилепсии или конвульсивных расстройств, расстройств детского возраста, когнитивных расстройств, нейродегенерации, нейротоксичности и ишемии.
9. Соединение или фармацевтическая композиция по п.8, где расстройство центральной нервной системы представляет собой тревожное расстройство, выбранное из агорафобии, генерализованного тревожного расстройства (GAD), обсессивно-компульсивного расстройства (OCD), панического расстройства, посттравматического стрессового расстройства (PTSD), социальной фобии и других фобий.
10. Соединение или фармацевтическая композиция по п.8, где расстройство центральной нервной системы представляет собой психотическое расстройство, выбранное из шизофрении, бредового расстройства, шизоаффективного расстройства, шизофреноформного расстройства и вызванного приемом веществ психотического расстройства.
11. Соединение или фармацевтическая композиция по п.8, где расстройство центральной нервной системы представляет собой расстройство настроения, выбранное из группы биполярных расстройств (I и II), циклотимического расстройства, депрессии, дистимического расстройства, большого депрессивного расстройства и вызванного приемом веществ расстройства настроения.
12. Соединение или фармацевтическая композиция по п.8, где расстройство центральной нервной системы представляет собой эпилепсию или конвульсивное расстройство, выбранное из группы генерализованной неконвульсивной эпилепсии, генерализованной конвульсивной эпилепсии, эпилептического статуса petit mal (малых припадков), эпилептического статуса grand mal (судорожных припадков), парциальной эпилепсии с нарушением или без нарушения сознания, младенческих судорог, парциальной непрерывной эпилепсии (epilepsia partialis continua) и других форм эпилепсии.
13. Соединение или фармацевтическая композиция по п.8, где расстройство детского возраста представляет собой дефицит внимания с гиперактивностью.
14. Соединение или фармацевтическая композиция по п.8, где расстройство центральной нервной системы представляет собой когнитивное расстройство, выбранное из группы делирия, вызванного приемом веществ персистирующего делирия, деменции, деменции при болезни, вызванной ВИЧ-инфекцией, деменции при болезни Гентингтона, деменции при болезни Паркинсона, деменции при болезни Альцгеймера, вызванной приемом веществ персистирующей деменции и легкого когнитивного расстройства.
15. Соединение по любому из пп.1-4 и ортостерический агонист mGluR2 в виде комбинированного препарата для одновременного, раздельного или последовательного применения в лечении или предупреждении состояния, указанного в любом из пп.7-14.
16. Способ лечения или предупреждения заболевания или состояния у пациента, на лечение или предупреждение которого влияет или лечению или предупреждению которого способствует нейромодуляторный эффект положительных аллостерических модуляторов mGluR2, включающий введение пациенту, нуждающемуся в этом, эффективного количества соединения по любому из пп.1-4.
RU2011113443/04A 2008-10-16 2009-10-15 Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов RU2517181C2 (ru)

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JP2012505846A (ja) 2012-03-08
CA2738849C (en) 2016-06-28
RU2517181C2 (ru) 2014-05-27
US20110275624A1 (en) 2011-11-10
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CA2738849A1 (en) 2010-04-22
AU2009304293A1 (en) 2010-04-22
CN102186477B (zh) 2013-07-17
EP2346505B1 (en) 2014-04-23
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WO2010043396A1 (en) 2010-04-22
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