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RU2009138602A - Новые производные бензазепина - Google Patents

Новые производные бензазепина Download PDF

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RU2009138602A
RU2009138602A RU2009138602/04A RU2009138602A RU2009138602A RU 2009138602 A RU2009138602 A RU 2009138602A RU 2009138602/04 A RU2009138602/04 A RU 2009138602/04A RU 2009138602 A RU2009138602 A RU 2009138602A RU 2009138602 A RU2009138602 A RU 2009138602A
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pharmaceutically acceptable
disease
acceptable salt
cyclobutyl
azepin
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RU2009138602/04A
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RU2423353C1 (ru
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Марк Джеймс БАМФОРД (GB)
Марк Джеймс Бамфорд
Дэвид Кеннет ДИН (GB)
Дэвид Кеннет Дин
Санджит Сингх СЕХМИ (GB)
Санджит Сингх СЕХМИ
Дэвид Мэттью УИЛСОН (GB)
Дэвид Мэттью Уилсон
Джейсон ВИЗЕРИНГТОН (GB)
Джейсон Визерингтон
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Глэксо Груп Лимитед (GB)
Глэксо Груп Лимитед
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Abstract

1. Соединение общей формулы (I), которое представляет собой 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид !! или его фармацевтически приемлемая соль. ! 2. Фармацевтически приемлемая соль соединения по п.1, которая представляет собой кислотно-аддитивную соль, образованную 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамидом и кислотой. ! 3. Фармацевтически приемлемая соль соединения по п.2, где кислота представляет собой малеиновую, хлористоводородную, бромистоводородную, фосфорную, уксусную, фумаровую, салициловую, серную, лимонную, молочную, миндальную, винно-каменную и метансульфоновую кислоту. ! 4. Фармацевтическая композиция, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид ! ! или его фармацевтически приемлемую соль, и фармацевтически приемлемый носитель или эксцепиент. ! 5. Соединение по п.1, используемое в терапии. ! 6. Применение 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемой соли в получении лекарственного средства для лечения нейрологического заболевания или психиатрического расстройства. ! 7. Применение по п.6, где лекарственное средство предназначено для лечения: нейрологического заболевания, такого как болезнь Альцгеймера, деменцию, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических расстройств, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания

Claims (18)

1. Соединение общей формулы (I), которое представляет собой 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид
Figure 00000001
или его фармацевтически приемлемая соль.
2. Фармацевтически приемлемая соль соединения по п.1, которая представляет собой кислотно-аддитивную соль, образованную 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамидом и кислотой.
3. Фармацевтически приемлемая соль соединения по п.2, где кислота представляет собой малеиновую, хлористоводородную, бромистоводородную, фосфорную, уксусную, фумаровую, салициловую, серную, лимонную, молочную, миндальную, винно-каменную и метансульфоновую кислоту.
4. Фармацевтическая композиция, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид
Figure 00000001
или его фармацевтически приемлемую соль, и фармацевтически приемлемый носитель или эксцепиент.
5. Соединение по п.1, используемое в терапии.
6. Применение 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемой соли в получении лекарственного средства для лечения нейрологического заболевания или психиатрического расстройства.
7. Применение по п.6, где лекарственное средство предназначено для лечения: нейрологического заболевания, такого как болезнь Альцгеймера, деменцию, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических расстройств, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания с гиперактивностью, депрессию или привыкание.
8. Применение по п.6, где лекарственное средство используют для лечения ухудшения познавательной способности, вызванной заболеванием.
9. Применение по п.8, где лекарственное средство используют для лечения ухудшения познавательской способности, вызванной болезнью Альцгеймера, или родственного нейродегенеративного нарушения.
10. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль в качестве терапевтического вещества, используемого при лечении нейрологического заболевания или психиатрического расстройства.
11. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль по п.10 в качестве терапевтического вещества, используемого при лечении: нейрологического заболевания, такого как болезнь Альцгеймера, деменция, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсию, невропатическую боль, болезнь Паркинсона, рассеянный склероз или удар; или психиатрических заболеваний, таких как нарушение познавательной способности при шизофрении, синдром дефицита внимания с гиперактивностью, депрессию и привыкание.
12. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид или его фармацевтически приемлемая соль по п.10 в качестве терапевтического вещества, используемого для лечения ухудшения нарушения познавательной способности, вызванной заболеванием.
13. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид по п.12 или его фармацевтически приемлемая соль в качестве терапевтического вещества, используемого для лечения ухудшения познавательной способности, вызванной болезнью Альцгеймера или родственным нейродегенеративным нарушением.
14. 6-(3-Циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метилникотинамид по п.13 или его фармацевтически приемлемая соль в качестве терапевтического вещества используемого для лечения ухудшения познавательной способности, вызванной болезнью Альцгеймера.
15. Фармацевтическая композиция, предназначенная для лечения неврологического заболевания, включающая 6-(3-циклобутил-2,3,4,5-тетрагидро-1H-бензо[d]азепин-7-илокси)-N-метил-никотинамид или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель или эксцепиент.
16. Фармацевтическая композиция по п.15, где неврологическим заболеванием является болезнь Альцгеймера, деменция, старческое расстройство памяти, легкое ухудшение познавательной способности, нарушение познавательной способности, эпилепсия, невропатическая боль, болезнь Паркинсона, рассеянный склероз или удар.
17. Способ получения соединения формулы (I) по п.1 или его фармацевтически приемлемой соли
Figure 00000002
I
где R1 представляет собой незамещенный циклобутил;
R2 представляет собой 2-пиридинил, замещенный СОN(H)(Me), и представляет собой 4-метиламинокарбонилпиридин-2-ил, который включает
а) взаимодействие соединения формулы (II)
Figure 00000003
где R1 определен выше,
с соединением формулы R2'-L1, где R2' такой, как определен выше для R2 или группа, превращаемая в него, a L1 обозначает подходящую уходящую группу, или
в) взаимодействие соединения формулы (III)
Figure 00000004
где R2 такой, как определено выше,
с соединением формулы R1'-L2, где R1' такой, как определено выше для R1 или группа, превращаемая в него, a L2 обозначает подходящую уходящую группу, или
с) взаимодействие соединения формулы (III), как определено выше, с кетоном формулы R1'=O, где R1' такой, как определен для R1 или группа, превращаемая в него, или
d) удаление защитной группы с защищенного соединения формулы (I).
18. Способ по п.17, где
на стадии а) R2' определен выше для R2 и L1 обозначает подходящую уходящую группу, такую как атом галогена или активированная гидроксильная группа, и
на стадии в) R1' определен выше для R1 и L2 обозначает подходящую уходящую группу, такую как атом галогена.
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ATE441417T1 (de) 2009-09-15
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