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RU2435760C2 - 1н-хиназолин-2,4-дионы - Google Patents

1н-хиназолин-2,4-дионы Download PDF

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RU2435760C2
RU2435760C2 RU2007141566/04A RU2007141566A RU2435760C2 RU 2435760 C2 RU2435760 C2 RU 2435760C2 RU 2007141566/04 A RU2007141566/04 A RU 2007141566/04A RU 2007141566 A RU2007141566 A RU 2007141566A RU 2435760 C2 RU2435760 C2 RU 2435760C2
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Russia
Prior art keywords
alkyl
alkylamino
isopropyl
ampa receptor
pharmaceutically acceptable
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RU2007141566/04A
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RU2007141566A (ru
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Ханс АЛЛЬГАЙЕР (DE)
Ханс Алльгайер
Ив ОБЕРСОН (CH)
Ив Оберсон
Давид КАРКАШ (CH)
Давид КАРКАШ
Филипп ФЛЁРШАЙМ (CH)
Филипп ФЛЁРШАЙМ
Кристель ГИБУРДЕНШ (CH)
Кристель ГИБУРДЕНШ
Вольфганг ФРЁШТЛЬ (CH)
Вольфганг ФРЁШТЛЬ
Йерг КАЛЛЕН (CH)
Йерг КАЛЛЕН
Мануэль КОЛЛЕР (CH)
Мануэль КОЛЛЕР
Анри МАТТЕ (FR)
Анри Матте
Йоахим НОЦУЛАК (DE)
Йоахим Ноцулак
Давид ОРЕН (FR)
Давид Орен
Жоанне РЕНО (CH)
Жоанне РЕНО
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Новартис Аг
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Abstract

Изобретение относится к 1Н-хиназолин-2,4-дионам формулы (I) и их фармацевтически приемлемым солям, где R1 и R2 имеют значения, указанные в п.1 формулы изобретения. Указанные соединения обладают антагонистической активностью в отношении рецептора АМРА. Изобретение также относится к содержащей их фармацевтической композиции, а также к их применению для получения лекрственнонго средства, предназначенного для лечсения состояния, опосредованного рецептором АМРА и прежде всего для лечения эпилепсии или шизофрении. 5 н. и 3 з.п. ф-лы.

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Claims (8)

1. Соединения формулы (I)
Figure 00000212

где R1 означает СF3 или изопропил, и
R2 означает гетероциклил, необязательно замещенный одним-тремя заместителями, выбранными из группы, включающей галоген, гидрокси, амино, нитро, циано, (С14)алкил, гидрокси-(С14)алкил, (C14)алкоксиалкил, амино-(С14)алкил, (С14)алкиламино-(С14)алкил, ди-(С14)алкиламино-(С14)алкил, НСО, (С14)алкилкарбонил, (C14)алкокси, ацилокси, (С14)алкоксикарбонилокси, (С14)алкиламино, ди-(С14)алкиламино, ациламино, (С14)алкоксикарбониламино; гетероциклил состоит из 3-11 кольцевых атомов, из которых 1-3 кольцевых атома представляют собой гетероатомы, выбранные из азота, кислорода и серы, и где гетероцикл присоединен к фенильному кольцу через атом углерода,
и их фармацевтически приемлемые соли.
2. N-[7-изопропил-6-(2-метил-2Н-пиразол-3-ил)-2,4-диоксо-1,4-дигидро-2Н-хиназолин-3-ил]метансульфонамид и его фармацевтически приемлемые соли.
3. N-[-[7-изопропил-6-(2-метил-2Н-пиразол-3-ил)-2,4-диоксо-1,4-дигидро-2Н-хиназолин-3-ил]метансульфонамид по п.2 в виде его фармацевтически приемлемых солей.
4. N-[7-изопропил-6-(2-метил-2Н-пиразол-3-ил)-2,4-диоксо-1,4-дигидро-2Н-хиназолин-3-ил]метансульфонамид по п.2 в свободной форме.
5. Соединения по любому из пп.1-4 для применения в качестве фармацевтического средства, обладающего антагонистической активностью в отношении рецептора АМРА.
6. Фармацевтическая композиция, обладающая антагонистической активностью в отношении рецептора АМРА, включающая соединение по любому из пп.1-4.
7. Применение соединения по любому из пп.1-4 для получения лекарственного средства, предназначенного для лечения состояния, опосредованного рецептором АМРА.
8. Применение соединения по любому из пп.1-4 для получения лекарственного средства, предназначенного для лечения эпилепсии или шизофрении.
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