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RU2008129623A - Ингибиторы ccr9 активности - Google Patents

Ингибиторы ccr9 активности Download PDF

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RU2008129623A
RU2008129623A RU2008129623/04A RU2008129623A RU2008129623A RU 2008129623 A RU2008129623 A RU 2008129623A RU 2008129623/04 A RU2008129623/04 A RU 2008129623/04A RU 2008129623 A RU2008129623 A RU 2008129623A RU 2008129623 A RU2008129623 A RU 2008129623A
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compound according
indole
dihydro
tert
alkyl
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RU2008129623/04A
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Хосе М. КАРБАЛЬИДО-ЭРРЕРА (AT)
Хосе М. КАРБАЛЬИДО-ЭРРЕРА
Герберт ЯКШЕ (AT)
Герберт ЯКШЕ
Филипп ЛЕР (AT)
Филипп Лер
Гудрун ВЕРНЕР (AT)
Гудрун ВЕРНЕР
Антони УИНИСКИ (AT)
Антони УИНИСКИ
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Новартис АГ (CH)
Новартис Аг
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Abstract

1. Соединение формулы ! ! в которой ! R1 означает водород, (С1-С6)алкил, гало(С1-С4)алкил, (С1-С4)алкокси, галоалкилокси, или галоид, ! R2 означает фенил, замещенный одним или более заместителями: ! - C1-С6алкилом, ! - галоС1-С4алкилом, ! - С1-С4алкокси, ! - галоС1-С4алкокси, или ! - галоидом; и ! R3 означает карбокси, С1-С4алкоксикарбонил или циано. ! 2. Соединение по п.1, в котором ! R1 означает C1-С6алкил, ! R2 означает незамещенный фенил или фенил, замещенный галоидом, и ! R3 означает С1-С4алкокеикарбонил. ! 3. Соединение по п.1, выбранное из группы, состоящей из ! метилового эфира 1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты, ! 1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты, ! метилового эфира 5-бром-1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты, и ! 5-бром-1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты. ! 4. Соединение по п.1 в форме соли. ! 5. Соединение по п.3 в виде соли. ! 6. Соединение по любому из пп.1-5 для применения в качестве лекарства. ! 7. Фармацевтическая композиция, включающая соединение по любому из пп.1-5 в сочетании с по крайней мере одним фармацевтически приемлемым наполнителем. ! 8. Применение соединения по любому из пп.1-5 для получения лекарства для лечения нарушений, опосредованных CCR9 активностью. ! 9. Фармацевтическая комбинация, включающая соединение по любому из пп.1-5, включающая, кроме того, вторую лекарственную субстанцию. ! 10. Фармацевтическая комбинация, включающая фармацевтическую композицию по п.7 и дополнительно включающая второе лекарственное вещество. ! 11. Способ лечения нарушений, опосредованных CCR9 активностью, включающий введение субъекту, нуждающе�

Claims (11)

1. Соединение формулы
Figure 00000001
в которой
R1 означает водород, (С16)алкил, гало(С14)алкил, (С14)алкокси, галоалкилокси, или галоид,
R2 означает фенил, замещенный одним или более заместителями:
- C16алкилом,
- галоС14алкилом,
- С14алкокси,
- галоС14алкокси, или
- галоидом; и
R3 означает карбокси, С14алкоксикарбонил или циано.
2. Соединение по п.1, в котором
R1 означает C16алкил,
R2 означает незамещенный фенил или фенил, замещенный галоидом, и
R3 означает С14алкокеикарбонил.
3. Соединение по п.1, выбранное из группы, состоящей из
метилового эфира 1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты,
1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты,
метилового эфира 5-бром-1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты, и
5-бром-1-(4-трет-бутилбензенсульфонил)-2,3-дигидро-1Н-индол-2-карбоновой кислоты.
4. Соединение по п.1 в форме соли.
5. Соединение по п.3 в виде соли.
6. Соединение по любому из пп.1-5 для применения в качестве лекарства.
7. Фармацевтическая композиция, включающая соединение по любому из пп.1-5 в сочетании с по крайней мере одним фармацевтически приемлемым наполнителем.
8. Применение соединения по любому из пп.1-5 для получения лекарства для лечения нарушений, опосредованных CCR9 активностью.
9. Фармацевтическая комбинация, включающая соединение по любому из пп.1-5, включающая, кроме того, вторую лекарственную субстанцию.
10. Фармацевтическая комбинация, включающая фармацевтическую композицию по п.7 и дополнительно включающая второе лекарственное вещество.
11. Способ лечения нарушений, опосредованных CCR9 активностью, включающий введение субъекту, нуждающемуся в таком лечении, терапевтически эффективного количества соединения по любому из пп.1-5 необязательно в комбинации со второй лекарственной субстанцией.
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