RU2005131838A - С-гликозидные производные и их соли - Google Patents

С-гликозидные производные и их соли Download PDF

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RU2005131838A
RU2005131838A RU2005131838/04A RU2005131838A RU2005131838A RU 2005131838 A RU2005131838 A RU 2005131838A RU 2005131838/04 A RU2005131838/04 A RU 2005131838/04A RU 2005131838 A RU2005131838 A RU 2005131838A RU 2005131838 A RU2005131838 A RU 2005131838A
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lower alkyl
ring
lower alkylene
glucite
benzothien
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RU2005131838/04A
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RU2317288C3 (ru
RU2317288C2 (ru
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Масаказу ИМАМУРА (JP)
Масаказу ИМАМУРА
Такеси МУРАКАМИ (JP)
Такеси Мураками
Риота СИРАКИ (JP)
Риота СИРАКИ
Казухиро ИКЕГАЙ (JP)
Казухиро ИКЕГАЙ
Такаси СУГАНЕ (JP)
Такаси Сугане
Фумийоси ИВАСАКИ (JP)
Фумийоси Ивасаки
Эйдзи КУРОСАКИ (JP)
Эйдзи КУРОСАКИ
Хироси ТОМИЯМА (JP)
Хироси ТОМИЯМА
Ацуси НОДА (JP)
Ацуси НОДА
Кайоко КИТТА (JP)
Кайоко КИТТА
Йосинори КОБАЯСИ (JP)
Йосинори КОБАЯСИ
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Астеллас Фарма Инк. (Jp)
Астеллас Фарма Инк.
Котобуки Фармасьютикал Ко., Лтд. (Jp)
Котобуки Фармасьютикал Ко., Лтд.
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Claims (12)

1. Производное С-гликозида формулы (I) или его соль
Figure 00000001
где кольцо А представляет собой (1) бензольное кольцо, (2) пяти- или шестичленное моноциклическое гетероарильное кольцо, содержащее от 1 до 4 гетероатомов, выбранных из N, S и О, за исключением триазолов и тетразолов, или (3) насыщенный или ненасыщенный восьми-десятичленный бициклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О;
кольцо В представляет собой (1) насыщенный или ненасыщенный восьми-десятичленный бициклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О, (2) насыщенный или ненасыщенный пяти- или шестичленный моноциклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О, (3) ненасыщенный восьми- или девятичленный бициклический карбоцикл, или (4) бензольное кольцо;
Х представляет собой связь или низший алкилен;
где значения кольца А, кольца В и Х соотносятся таким образом, что (1) когда кольцо А представляет собой бензольное кольцо, кольцо В не является бензольным кольцом, или (2) когда кольцо А представляет собой бензольное кольцо, кольцо В представляет собой насыщенный или ненасыщенный восьми-десятичленный бициклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О, включающий бензольное кольцо, или насыщенный или ненасыщенный восьми-десятичленный бициклический карбоцикл, включающий бензольное кольцо, Х присоединен к кольцу В в части, отличной от бензольного кольца, включенного в кольцо В;
R1-R4 каждый отдельно представляет собой атом водорода, низший алкил, -С(=О)-низший алкил или -низший алкилен-арил; и
R5-R11 каждый отдельно представляет собой атом водорода, низший алкил, циклоалкил, галоген, галоген-замещенный низший алкил, -ОН, =О, -NH2, низший алкил-сульфонил-, галоген-замещенный низший алкил-сульфонил-, арилсульфонил-, арил, насыщенный или ненасыщенный пяти- или шестичленный моноциклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О, -низший алкилен-ОН, -низший алкилен-О-низший алкил, -низший алкилен-О-С(=О)-низший алкил, -низший алкил, -низший алкилен-О-низший алкилен-СООН, -низший алкилен-О-низший алкилен-С(=О)-О-низший алкил, -низший алкилен-NH2, -низший алкилен-NH-низший алкил, -низший алкилен-N(низший алкил)2, -низший алкилен-NH-C(=O)-низший алкил, -СООН, -CN, -C(=O)-O-низший алкил, -С(=О)-NH2, -C(=O)-NH-низший алкил, -С(=О)-N(низший алкил)2, -О-низший алкил, -О-циклоалкил, -О-низший алкилен-ОН, -О-низший алкилен-О-низший алкил, -О-низший алкилен-СООН, -О-низший алкилен-С(=О)-О-низший алкил, -О-низший алкилен-С(=О)-NH2, -О-низший алкилен-С(=О)-NH-низший алкил, -О-низший алкилен-С(=О)-N(низший алкил)2, -О-низший алкилен-СН(ОН)-СН2(ОН), -О-низший алкилен-NH2, -O-низший алкилен-NH-низший алкил, -О-низший алкилен-N(низший алкил)2, -О-низший алкилен-NH-C(=O)-низший алкил, -NH-низший алкил, -N(низший алкил)2, -NH-SO2-низший алкил, -NH-SO2-галоген-замещенный низший алкил, -NH-низший алкилен-ОН, -NH-C(=O)-низший алкил, -NH-C(=O)-NH2, -NH-C(=O)-NH-низший алкил, -NH-C(=O)-N(низший алкил)2 или -NH-C(=O)-O-низший алкил.
2. Производное С-гликозида и его соль по п.1, где кольцо А в формуле (I) представляет собой (1) бензольное кольцо или (2) пяти- или шестичленное моноциклическое гетероарильное кольцо, содержащее от 1 до 4 гетероатомов, выбранных из N, S и О, за исключением триазолов и тетразолов.
3. Производное С-гликозида и его соль по п.2, где кольцо В в формуле (I) представляет собой (1) насыщенный или ненасыщенный восьми-десятичленный бициклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О, или (2) насыщенный или ненасыщенный пяти- или шестичленный моноциклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О.
4. Производное С-гликозида и его соль по п.3, где кольцо А в формуле (I) представляет собой бензольное кольцо и кольцо В представляет собой насыщенный или ненасыщенный восьми-десятичленный бициклический гетероцикл, содержащий от 1 до 4 гетероатомов, выбранных из N, S и О.
5. Производное С-гликозида и его соль по п.4, где Х в формуле (I) представляет собой метилен.
6. Производное С-гликозида и его соль по п.5, где R1-R4 в формуле (I) представляют собой атомы водорода.
7. Производное С-гликозида и его соль по п.1, где производное С-гликозида формулы (I) представляет собой, по меньшей мере, одно соединение, выбранное из группы, включающей
(1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)фенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-2-гидроксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-2-метоксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-2-(2-гидроксиэтокси)фенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-2-(метиламино)фенил]-D-глюцит,
(1S)-1,5-ангидро-1-{[5-(1-бензотиен-2-илметил)-2-[(2-гидроксиэтокси)амино]фенил}-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-метоксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-хлорфенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-фторфенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-2,4-диметоксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-хлор-2-метоксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-хлор-2-гидроксифенил]-D-глюцит,
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-фтор-2-гидроксифенил]-D-глюцит и
(1S)-1,5-ангидро-1-[5-(1-бензотиен-2-илметил)-4-фтор-2-метоксифенил]-D-глюцит.
8. Фармацевтическая композиция, содержащая производное С-гликозида или его соль по любому из пп.1-7.
9. Фармацевтическая композиция по п.8, где композиция представляет собой ингибитор сотранспортера Na+-глюкозы.
10. Фармацевтическая композиция по п.8, где композиция представляет собой противодиабетический агент.
11. Применение производного С-гликозида и его соли по любому из пп.1-7 для получения ингибитора сотранспортера Na+-глюкозы или противодиабетического агента.
12. Способ лечения диабета, включающий введение пациенту эффективного количества производного С-гликозида и его соли по любому из пп.1-7.
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