RU2013148721A - Комбинации соединений, ингибирующих акт и вемурафениба и способы их применения - Google Patents

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

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RU2013148721A
RU2013148721A RU2013148721/04A RU2013148721A RU2013148721A RU 2013148721 A RU2013148721 A RU 2013148721A RU 2013148721/04 A RU2013148721/04 A RU 2013148721/04A RU 2013148721 A RU2013148721 A RU 2013148721A RU 2013148721 A RU2013148721 A RU 2013148721A
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combination
cancer
vemurafenib
pharmaceutically acceptable
acceptable salt
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Клаус ХИФЛИЧ
Марк МЕРЧАНТ
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Дженентек, Инк.
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Abstract

1. Комбинация a) соединения формулы Ia:или его фармацевтически приемлемой соли, и b) вемурафениба или его фармацевтически приемлемой соли для профилактики или терапевтического лечения гиперпролиферативного расстройства.2. Комбинация по п.1, где гиперпролиферативное расстройство представляет собой рак.3. Комбинация по п.2, где рак включает BRAF V600E мутацию.4. Комбинация по п.2 или 3, где рак связан с высокими уровнями экспрессии или активации pAKT.5. Комбинация по п.2, где рак представляет собой лимфому, рак толстой кишки, меланому, рак щитовидной железы или рак легких.6. Комбинация по п.5, где рак является резистентным к монотерапии вемурафенибом.7. Комбинация по п.6, где рак представляет собой метастатическую или нерезектабельную меланому.8. Комбинация по п.1, где комбинация обеспечивает синергический эффект при лечении расстройства.9. Комбинация по п.1, где соединение формулы Ia или его соль вводят одновременно с вемурафенибом или его солью.10. Комбинация по п.1, где соединение формулы Ia или его соль и вемурафениб или его соль вводят последовательно.11. Соединение формулы Ia или его фармацевтически приемлемая соль по п.1 для терапевтического применения для улучшения качества жизни пациента, подвергаемого лечению по поводу гиперпролиферативного расстройства вемурафенибом или его фармацевтически приемлемой солью.12. Способ лечения заболевание или состояния, модулируемого BRAF V600E мутацией или высокими уровнями pAKT у млекопитающего, включающий введение млекопитающему a) соединения формулы Ia или его фармацевтически приемлемой соли по п.1 и b) вемурафениба или его фармацевтически приемлемой соли.13. Способ по п.12, где пациент ранее получал

Claims (15)

1. Комбинация a) соединения формулы Ia:
Figure 00000001
или его фармацевтически приемлемой соли, и b) вемурафениба или его фармацевтически приемлемой соли для профилактики или терапевтического лечения гиперпролиферативного расстройства.
2. Комбинация по п.1, где гиперпролиферативное расстройство представляет собой рак.
3. Комбинация по п.2, где рак включает BRAF V600E мутацию.
4. Комбинация по п.2 или 3, где рак связан с высокими уровнями экспрессии или активации pAKT.
5. Комбинация по п.2, где рак представляет собой лимфому, рак толстой кишки, меланому, рак щитовидной железы или рак легких.
6. Комбинация по п.5, где рак является резистентным к монотерапии вемурафенибом.
7. Комбинация по п.6, где рак представляет собой метастатическую или нерезектабельную меланому.
8. Комбинация по п.1, где комбинация обеспечивает синергический эффект при лечении расстройства.
9. Комбинация по п.1, где соединение формулы Ia или его соль вводят одновременно с вемурафенибом или его солью.
10. Комбинация по п.1, где соединение формулы Ia или его соль и вемурафениб или его соль вводят последовательно.
11. Соединение формулы Ia или его фармацевтически приемлемая соль по п.1 для терапевтического применения для улучшения качества жизни пациента, подвергаемого лечению по поводу гиперпролиферативного расстройства вемурафенибом или его фармацевтически приемлемой солью.
12. Способ лечения заболевание или состояния, модулируемого BRAF V600E мутацией или высокими уровнями pAKT у млекопитающего, включающий введение млекопитающему a) соединения формулы Ia или его фармацевтически приемлемой соли по п.1 и b) вемурафениба или его фармацевтически приемлемой соли.
13. Способ по п.12, где пациент ранее получал монотерапию вемурафенибом.
14. Применение соединения формулы Ia или его фармацевтически приемлемой соли по п.1 в получении лекарственного средства для лечения гиперпролиферативного расстройства у млекопитающего, где млекопитающему вводят вемурафениб.
15. Применение соединения формулы Ia или его фармацевтически приемлемой соли по п.1 в получении лекарственного средства для лечения заболевания или состояния, модулируемого AKT-киназой у млекопитающего, где млекопитающему вводят вемурафениб.
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