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RU2013148728A - Комбинации соединений, ингибирующих акт, и эрлотиниба и способы их применения - Google Patents

Комбинации соединений, ингибирующих акт, и эрлотиниба и способы их применения Download PDF

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RU2013148728A
RU2013148728A RU2013148728/04A RU2013148728A RU2013148728A RU 2013148728 A RU2013148728 A RU 2013148728A RU 2013148728/04 A RU2013148728/04 A RU 2013148728/04A RU 2013148728 A RU2013148728 A RU 2013148728A RU 2013148728 A RU2013148728 A RU 2013148728A
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pharmaceutically acceptable
acceptable salt
cancer
combination
combination according
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Мишель НАННИНИ
Дипак САМПАТХ
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Дженентек, Инк.
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Abstract

1. Комбинация a) соединения формулы Ia:или его фармацевтически приемлемой соли; и b) эрлотиниба или его фармацевтически приемлемой соли для профилактики или терапевтического лечения гиперпролиферативного нарушения.2. Комбинация по п.1, где гиперпролиферативным нарушением является злокачественное новообразование.3. Комбинация по п.2, где злокачественное новообразование связано с мутацией PTEN.4. Комбинация по п.2, где злокачественное новообразование связано с мутацией AKT, сверхэкспрессией или амплификацией.5. Комбинация по п.2, где злокачественное новообразование связано с мутацией PI3K.6. Комбинация по п.2, где злокачественное новообразование связано с амплификацией Her2/ErbB2.7. Комбинация по любому из пп.2-6, где злокачественное новообразование выбрано из рака молочной железы, рака легких, рака яичников, рака предстательной железы, меланомы, рака желудка, рака толстой кишки, рака почек, рака головы и рака шеи, и глиомы.8. Комбинация по любому из пп.1-6, где комбинация обеспечивает синергетический эффект при лечении гиперпролиферативного нарушения.9. Комбинация по п.8, где значение комбинаторного индекса синергетического эффекта меньше, чем около 0,8.10. Комбинация по п.7, где комбинация обеспечивает синергетический эффект при лечении гиперпролиферативного нарушения.11. Соединение формулы Ia или его фармацевтически приемлемая соль, как определено в п.1, для терапевтического применения для улучшения качества жизни пациента, которого лечат от гиперпролиферативного нарушения эрлотинибом или его фармацевтически приемлемой солью.12. Способ лечения гиперпролиферативного заболевания у млекопитающего, включающее введение млекопитающе

Claims (16)

1. Комбинация a) соединения формулы Ia:
Figure 00000001
или его фармацевтически приемлемой соли; и b) эрлотиниба или его фармацевтически приемлемой соли для профилактики или терапевтического лечения гиперпролиферативного нарушения.
2. Комбинация по п.1, где гиперпролиферативным нарушением является злокачественное новообразование.
3. Комбинация по п.2, где злокачественное новообразование связано с мутацией PTEN.
4. Комбинация по п.2, где злокачественное новообразование связано с мутацией AKT, сверхэкспрессией или амплификацией.
5. Комбинация по п.2, где злокачественное новообразование связано с мутацией PI3K.
6. Комбинация по п.2, где злокачественное новообразование связано с амплификацией Her2/ErbB2.
7. Комбинация по любому из пп.2-6, где злокачественное новообразование выбрано из рака молочной железы, рака легких, рака яичников, рака предстательной железы, меланомы, рака желудка, рака толстой кишки, рака почек, рака головы и рака шеи, и глиомы.
8. Комбинация по любому из пп.1-6, где комбинация обеспечивает синергетический эффект при лечении гиперпролиферативного нарушения.
9. Комбинация по п.8, где значение комбинаторного индекса синергетического эффекта меньше, чем около 0,8.
10. Комбинация по п.7, где комбинация обеспечивает синергетический эффект при лечении гиперпролиферативного нарушения.
11. Соединение формулы Ia или его фармацевтически приемлемая соль, как определено в п.1, для терапевтического применения для улучшения качества жизни пациента, которого лечат от гиперпролиферативного нарушения эрлотинибом или его фармацевтически приемлемой солью.
12. Способ лечения гиперпролиферативного заболевания у млекопитающего, включающее введение млекопитающему комбинации a) соединения формулы Ia:
Figure 00000001
или его фармацевтически приемлемой соли; и b) эрлотиниба или его фармацевтически приемлемой соли.
13. Комбинация a) соединения формулы Ia или его фармацевтически приемлемой соли, как определено в п.1; и b) эрлотиниба или его фармацевтически приемлемой соли для лечения нарушения или состояния, модулированного киназой AKT.
14. Применение соединения формулы Ia или его фармацевтически приемлемой соли, как определено в п.1, при получении лекарственного средства для лечения гиперпролиферативного нарушения у млекопитающего, при котором млекопитающему вводят эрлотиниб или его фармацевтически приемлемую соль.
15. Набор, содержащий соединение формулы Ia или его фармацевтически приемлемую соль, как определено в п.1, контейнер и вкладыш для упаковки или этикетку с указанием порядка приема соединения формулы Ia с эрлотинибом или его фармацевтически приемлемой соли при лечении гиперпролиферативного нарушения.
16. Продукт, содержащий соединение, имеющее формулу Ia, или его фармацевтически приемлемую соль, как определено в п.1, и эрлотиниб или его фармацевтически приемлемую соль, в виде комбинированного препарата для раздельного, одновременного или последовательного применения при лечении гиперпролиферативного нарушения.
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