RU2009117388A - Моногидрат 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил})амино)-3-фторфенокси]-n-метилпиридин-2-карбоксамида - Google Patents

Моногидрат 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил})амино)-3-фторфенокси]-n-метилпиридин-2-карбоксамида Download PDF

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RU2009117388A
RU2009117388A RU2009117388/04A RU2009117388A RU2009117388A RU 2009117388 A RU2009117388 A RU 2009117388A RU 2009117388/04 A RU2009117388/04 A RU 2009117388/04A RU 2009117388 A RU2009117388 A RU 2009117388A RU 2009117388 A RU2009117388 A RU 2009117388A
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Альфонс ГРУНЕНБЕРГ (DE)
Альфонс Груненберг
Юрген ШТИЛЬ (DE)
Юрген ШТИЛЬ
Катарина ТЕНБИГ (DE)
Катарина Тенбиг
Биргит КАЙЛЬ (DE)
Биргит Кайль
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Байер Шеринг Фарма Акциенгезельшафт (DE)
Байер Шеринг Фарма Акциенгезельшафт
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Abstract

1. Соединение формулы (II) ! ! 2. Соединение по п.1, которое демонстрирует при рентгеновской дифрактометрии пиковое максимальное значение угла 2 тэта 21.2. ! 3. Соединение по п.1, которое демонстрирует в дальнем ИК-спектре пиковое максимальное значение, равное 353 см-1. ! 4. Способ получения соединения формулы (II) по любому из пп.1-3, включающий растворение 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил)амино)-3-фторфенокси]-N-метилпиридин-2-карбоксамида и добавление воды до выпадения осадка. ! 5. Способ получения соединения формулы (II) по любому из пп.1-3, включающий суспендирование 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил}амино)-3-фторфенокси]-N-метилпиридин-2-карбоксамида в водном растворителе, а затем перемешивание или встряхивание до преобразования в соединение формулы (II). ! 6. Соединение формулы (II) по любому из пп.1-3 для лечения гаперпролиферативных заболеваний. ! 7. Соединение формулы (II) по любому из пп.1-3 для лечения солидных опухолей, лимфом, сарком, лейкемий, раков молочной железы, дыхательных путей, мозга, репродуктивных органов, пищеварительного тракта, мочевых путей, глаза, печени, кожи, головы и шеи, щитовидной и/или паращитовидной железы. ! 8. Применение соединения формулы (II) по любому из пп.1-3 для получения фармацевтической композиции для лечения гиперпролиферативных заболеваний. ! 9. Применение по п.8 для лечения солидных опухолей, лимфом, сарком, лейкемий, раков молочной железы, дыхательных путей, мозга, репродуктивных органов, пищеварительного тракта, мочевых путей, глаза, печени, кожи, головы и шеи, щитовидной и/или паращитовидной железы. ! 10. Фармацевтическая композиция, включающая в основном соединение формулы (II) по любому и

Claims (17)

1. Соединение формулы (II)
Figure 00000001
2. Соединение по п.1, которое демонстрирует при рентгеновской дифрактометрии пиковое максимальное значение угла 2 тэта 21.2.
3. Соединение по п.1, которое демонстрирует в дальнем ИК-спектре пиковое максимальное значение, равное 353 см-1.
4. Способ получения соединения формулы (II) по любому из пп.1-3, включающий растворение 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил)амино)-3-фторфенокси]-N-метилпиридин-2-карбоксамида и добавление воды до выпадения осадка.
5. Способ получения соединения формулы (II) по любому из пп.1-3, включающий суспендирование 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил}амино)-3-фторфенокси]-N-метилпиридин-2-карбоксамида в водном растворителе, а затем перемешивание или встряхивание до преобразования в соединение формулы (II).
6. Соединение формулы (II) по любому из пп.1-3 для лечения гаперпролиферативных заболеваний.
7. Соединение формулы (II) по любому из пп.1-3 для лечения солидных опухолей, лимфом, сарком, лейкемий, раков молочной железы, дыхательных путей, мозга, репродуктивных органов, пищеварительного тракта, мочевых путей, глаза, печени, кожи, головы и шеи, щитовидной и/или паращитовидной железы.
8. Применение соединения формулы (II) по любому из пп.1-3 для получения фармацевтической композиции для лечения гиперпролиферативных заболеваний.
9. Применение по п.8 для лечения солидных опухолей, лимфом, сарком, лейкемий, раков молочной железы, дыхательных путей, мозга, репродуктивных органов, пищеварительного тракта, мочевых путей, глаза, печени, кожи, головы и шеи, щитовидной и/или паращитовидной железы.
10. Фармацевтическая композиция, включающая в основном соединение формулы (II) по любому из пп.1-3, никаких значительных частей другой формы 4-[4-({[4-хлор-3-(трифторметил)фенил]карбамоил}амино)-3-фторфенокси]-N-метилпиридин-2-карбоксамида и один или более инертных, нетоксичных, фармацевтически приемлемых наполнителей.
11. Фармацевтическая композиция по п.10, содержащая более 90 мас.% соединения формулы (II) по любому из пп.1-3 относительно общего количества соединения формулы (II), присутствующего в композиции.
12. Фармацевтическая композиция по п.10 для лечения заболеваний.
13. Фармацевтическая композиция по любому из пп.10-12, включающая один или более других фармацевтических веществ.
14. Фармацевтическая композиция по п.13, где одно или более других фармацевтических веществ являются аптигиперпролиферативными веществами, цитотоксическими веществами, ингибиторами трансдукции сигнала, противораковыми веществами и/или противорвотными средствами.
15. Способ лечения гиперпролиферативных заболеваний при помощи эффективного количества соединения формулы (II) по любому из пп.1-3 или фармацевтической композиции по одному из пп.10-12.
16. Комбинация, включающая соединение формулы (II) по любому из пп.1-3 и одно или более других фармацевтических веществ.
17. Комбинация по п.16, где одно или более других фармацевтических веществ являются цитотоксическими веществами, ингибиторами трансдукции сигнала, противораковыми веществами или противорвотными средствами.
RU2009117388/04A 2006-10-11 2007-09-29 Моногидрат 4-[4-({[4-хлор -3(трифторметил)фенил]карбамоил}амино)-3-фторфенокси]-n-метилпиридин-2-карбоксамида RU2466992C2 (ru)

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