RU2011102363A - Сульфонамидные соединения или их соли - Google Patents

Сульфонамидные соединения или их соли Download PDF

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RU2011102363A
RU2011102363A RU2011102363/04A RU2011102363A RU2011102363A RU 2011102363 A RU2011102363 A RU 2011102363A RU 2011102363/04 A RU2011102363/04 A RU 2011102363/04A RU 2011102363 A RU2011102363 A RU 2011102363A RU 2011102363 A RU2011102363 A RU 2011102363A
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methyl
ylsulfonyl
pyridin
amino
fluoropropyl
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RU2011102363/04A
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RU2481329C2 (ru
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Хидеки КУБОТО (JP)
Хидеки КУБОТО
Иссеи ЦУКАМОТО (JP)
Иссеи ЦУКАМОТО
Кадзунори КАМИДЗЕ (JP)
Кадзунори КАМИДЗЕ
Кодзи КАТО (JP)
Кодзи Като
Юта ФУКУДА (JP)
Юта ФУКУДА
Хиденори АЗАМИ (JP)
Хиденори АЗАМИ
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Астеллас Фарма Инк. (Jp)
Астеллас Фарма Инк.
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
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Abstract

1. Соединение формулы (I) или его соль ! [химическая формула 8] ! ! где R1 и R2 являются одинаковыми или различными и представляют собой Н, галоген, R0, галоген-низший алкил, -ОН или -О-R0, либо R1 и R2, взятые вместе с двумя смежными атомами углерода, с которыми они связаны, могут образовывать 5-8-членное циклоалкеновое кольцо; ! R3 представляет собой 2-фторпропил, 2-фторбутил, 2,2-дифторэтил или 3-фтор-2-метилпропил; ! L представляет собой низший алкилен; ! А представляет собой фенил, который может быть замещенным, или моноциклический гетероарил, который может быть замещенным; ! В представляет собой фенилен, который может быть замещенным, или моноциклический гетероарилен, который может быть замещенным; ! Х представляет собой -CO2R0, -СО2Н, -СО-NH-SO2-R0, и ! R0 представляет собой низший алкил. ! 2. Соединение или его соль по п.1, где L представляет собой метилен. ! 3. Соединение или его соль по п.2, где А представляет собой фенил, замещенный галогеном(ами), фурил, замещенный метилом(ами), тиазолил, замещенный метилом(ами), 2-пиридил или 3-пиридил. ! 4. Соединение или его соль по п.3, где Х представляет собой -СО2Н или -СО-NH-SO2-R0. ! 5. Соединение или его соль по п.4, где R3 представляет собой 2-фторпропил, 2-фторбутил или 3-фтор-2-метилпропил. ! 6. Соединение или его соль по п.5, где В представляет собой тиофендиил, пиридиндиил, пиримидиндиил или фенилен, который может быть замещен одной группой, выбранной из группы, состоящей из метила, F и метокси. ! 7. Соединение по п.1, выбранное из группы, состоящей из: ! 4-[(2-{[(2S)-2-фторпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты, ! 4-[(2-{[(2R)-2-фторпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензой

Claims (15)

1. Соединение формулы (I) или его соль
[химическая формула 8]
Figure 00000001
где R1 и R2 являются одинаковыми или различными и представляют собой Н, галоген, R0, галоген-низший алкил, -ОН или -О-R0, либо R1 и R2, взятые вместе с двумя смежными атомами углерода, с которыми они связаны, могут образовывать 5-8-членное циклоалкеновое кольцо;
R3 представляет собой 2-фторпропил, 2-фторбутил, 2,2-дифторэтил или 3-фтор-2-метилпропил;
L представляет собой низший алкилен;
А представляет собой фенил, который может быть замещенным, или моноциклический гетероарил, который может быть замещенным;
В представляет собой фенилен, который может быть замещенным, или моноциклический гетероарилен, который может быть замещенным;
Х представляет собой -CO2R0, -СО2Н, -СО-NH-SO2-R0, и
R0 представляет собой низший алкил.
2. Соединение или его соль по п.1, где L представляет собой метилен.
3. Соединение или его соль по п.2, где А представляет собой фенил, замещенный галогеном(ами), фурил, замещенный метилом(ами), тиазолил, замещенный метилом(ами), 2-пиридил или 3-пиридил.
4. Соединение или его соль по п.3, где Х представляет собой -СО2Н или -СО-NH-SO2-R0.
5. Соединение или его соль по п.4, где R3 представляет собой 2-фторпропил, 2-фторбутил или 3-фтор-2-метилпропил.
6. Соединение или его соль по п.5, где В представляет собой тиофендиил, пиридиндиил, пиримидиндиил или фенилен, который может быть замещен одной группой, выбранной из группы, состоящей из метила, F и метокси.
7. Соединение по п.1, выбранное из группы, состоящей из:
4-[(2-{[(2S)-2-фторпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-[(2-{[(2R)-2-фторпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-{[(6-{[(2R)-2-фторпропил](пиридин-2-илсульфонил)амино}-2,3-дигидро-1Н-инден-5-ил)окси)метил}бензойной кислоты,
4-[(5-хлор-2-{[(2S)-2-фторпропил](пиридин-2-илсульфонил)амино}-4-метилфенокси)метил]бензойной кислоты,
4-[(5-хлор-2-{[(2R)-2-фторпропил](пиридин-2-илсульфонил)амино}-4-метилфенокси)метил]бензойной кислоты,
4-[(2-{[(2R)-3-фтор-2-метилпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-[(2-{[(2S)-3-фтор-2-метилпропил](пиридин-2-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-{[(6-{[(2R)-2-фторбутил](пиридин-2-илсульфонил)амино}-2,3-дигидро-1Н-инден-5-ил)окси)метил}бензойной кислоты,
4-{[(6-{[(2S)-2-фторбутил](пиридин-2-илсульфонил)амино}-2,3-дигидро-1Н-инден-5-ил)окси)метил}бензойной кислоты,
4-[(5-хлор-2-{[(2R)-2-фторпропил](пиридин-3-илсульфонил)амино}-4-метилфенокси)метил]бензойной кислоты,
4-[(5-хлор-2-{[(2S)-2-фторпропил](пиридин-3-илсульфонил)амино}-4-метилфенокси)метил]бензойной кислоты,
4-[(2-{[(2S)-2-фторпропил](пиридин-3-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-[(2-{[(2R)-2-фторпропил](пиридин-3-илсульфонил)амино}-4,5-диметилфенокси)метил]бензойной кислоты,
4-{[(6-{[(2S)-2-фторпропил](пиридин-3-илсульфонил)амино}-2,3-дигидро-1Н-инден-5-ил)окси)метил}бензойной кислоты и
4-{[(6-{[(2R)-2-фторпропил](пиридин-3-илсульфонил)амино}-2,3-дигидро-1Н-инден-5-ил)окси)метил}бензойной кислоты,
или их соли.
8. Фармацевтическая композиция, содержащая соединение или его соль по п.1 и наполнитель.
9. Фармацевтическая композиция по п.8, которая представляет собой антагонист рецептора ЕР1.
10. Фармацевтическая композиция по п.8, которая представляет собой средство для лечения дисфункции нижних мочевых путей.
11. Фармацевтическая композиция по п.10, где указанными заболеваниями, вызывающими дисфункцию нижних мочевых путей, являются гиперактивный мочевой пузырь, доброкачественная гиперплазия предстательной железы, спазм шейки мочевого пузыря, цистит или простатит.
12. Применение соединения или его соли по п.1 для получения средства для лечения дисфункции нижних мочевых путей.
13. Применение по п.12, где указанными заболеваниями, вызывающими дисфункцию нижних мочевых путей, являются гиперактивный мочевой пузырь, доброкачественная гиперплазия предстательной железы, спазм шейки мочевого пузыря, цистит или простатит.
14. Способ лечения дисфункции нижних мочевых путей, включающий введение пациенту терапевтически эффективного количества соединения или его соли по п.1.
15. Способ по п.14, где указанными заболеваниями, вызывающими дисфункцию нижних мочевых путей, являются гиперактивный мочевой пузырь, доброкачественная гиперплазия предстательной железы, спазм шейки мочевого пузыря, цистит или простатит.
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