RU2006142331A - Комбинации, содержащие антимускариновые агенты и ингибиторы pde4 - Google Patents
Комбинации, содержащие антимускариновые агенты и ингибиторы pde4 Download PDFInfo
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Abstract
1. Комбинация, содержащая (а) ингибитор PDE4 и (b) антагонист мускариновых рецепторов М3, который представляет собой 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октан в форме соли с анионом X, который является фармацевтически приемлемым анионом моно- или поливалентной кислоты.2. Комбинация по п.1, где антагонист мускариновых рецепторов М3 (b) представляет собой бромид 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октана.3. Комбинация по п.1 или 2, где ингибитор PDE4 выбран из группы, содержащей теофиллин, дротаверина гидрохлорид, циломиласт, рофлумиласт, денбуфиллин, ролипрам, тетомиласт, энпрофиллин, арофиллин, ципамфиллин, тофимиласт, филаминаст, пикламиласт, (R)-(+)-4-[2-(3-циклопентилокси-4-метоксифенил)-2-фенилэтил]пиридин, мезопрам, N-(3,5-дихлор-4-пиридинил)-2-[1-(4-фторбензил)-5-гидрокси-1Н-индол-3-ил]-2-оксоацетамид, CDC-801 (например, Celgene), СС-1088 (например, Celgene), лиримиласт, ONO-6126 (например, Опо), СС-10004 (например, Celgene) и MN-001 (например, Kyorin), необязательно в форме их рацематов, их энантиомеров, их диастереомеров и их смесей и необязательно их фармакологически совместимых кислотно-аддитивных солей.4. Комбинация по п.3, где ингибитор PDE4 выбран из группы, включающей циломиласт, рофлумиласт, денбуфиллин и тетомиласт, необязательно в форме их рацематов, их энантиомеров, их диастереомеров и их смесей и необязательно их фармакологически совместимых кислотно-аддитивных солей.5. Комбинация по п.4, где ингибитор PDE4 представляет собой рофлумиласт.6. Комбинация по п.4, где ингибитор PDE4 представляет собой циломиласт.7. Комбинация по п.3, отличающаяся тем, что активные ингредиенты (а) и (b) образуют часть едино
Claims (19)
1. Комбинация, содержащая (а) ингибитор PDE4 и (b) антагонист мускариновых рецепторов М3, который представляет собой 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октан в форме соли с анионом X, который является фармацевтически приемлемым анионом моно- или поливалентной кислоты.
2. Комбинация по п.1, где антагонист мускариновых рецепторов М3 (b) представляет собой бромид 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октана.
3. Комбинация по п.1 или 2, где ингибитор PDE4 выбран из группы, содержащей теофиллин, дротаверина гидрохлорид, циломиласт, рофлумиласт, денбуфиллин, ролипрам, тетомиласт, энпрофиллин, арофиллин, ципамфиллин, тофимиласт, филаминаст, пикламиласт, (R)-(+)-4-[2-(3-циклопентилокси-4-метоксифенил)-2-фенилэтил]пиридин, мезопрам, N-(3,5-дихлор-4-пиридинил)-2-[1-(4-фторбензил)-5-гидрокси-1Н-индол-3-ил]-2-оксоацетамид, CDC-801 (например, Celgene), СС-1088 (например, Celgene), лиримиласт, ONO-6126 (например, Опо), СС-10004 (например, Celgene) и MN-001 (например, Kyorin), необязательно в форме их рацематов, их энантиомеров, их диастереомеров и их смесей и необязательно их фармакологически совместимых кислотно-аддитивных солей.
4. Комбинация по п.3, где ингибитор PDE4 выбран из группы, включающей циломиласт, рофлумиласт, денбуфиллин и тетомиласт, необязательно в форме их рацематов, их энантиомеров, их диастереомеров и их смесей и необязательно их фармакологически совместимых кислотно-аддитивных солей.
5. Комбинация по п.4, где ингибитор PDE4 представляет собой рофлумиласт.
6. Комбинация по п.4, где ингибитор PDE4 представляет собой циломиласт.
7. Комбинация по п.3, отличающаяся тем, что активные ингредиенты (а) и (b) образуют часть единой фармацевтической композиции.
8. Комбинация по п.3, дополнительно включающая (с) другое активное соединение, выбранное из: (а) β2-агонистов, (b) кортикостероидов, (с) антагонистов лейкотриена D4, (d) ингибиторов киназы egfr, (e) ингибиторов киназы р38 и (f) агонистов рецептора NK1.
9. Комбинация по п.8, где активное соединение (с) выбрано из группы, состоящей из (а) β2-агонистов и (b) кортикостероидов.
10. Применение (а) ингибитора PDE4 по любому из пп.1, 3-6 и (b) антагониста мускариновых рецепторов МЗ по п.1 или 2 для приготовления лекарственного средства для совместного, раздельного или последовательного применения для лечения пациента, страдающего респираторным заболеванием, реагирующим на М3 антагонистическое воздействие.
11. Применение по п.10, где респираторное заболевание представляет собой астму или хроническое обструктивное заболевание легких (COPD).
12. Продукт, содержащий (а) ингибитор PDE4 по любому из пп.1, 3-6 и (b) антагонист мускариновых рецепторов М3 по п.1 или 2, в виде комбинированного препарата для совместного, раздельного или последовательного применения для лечения пациента, страдающего респираторным заболеванием, реагирующим на М3 антагонистическое воздействие.
13. Продукт по п.12, дополнительно включающий с) другое активное соединение, определенное в п.8 или 9.
14. Набор, содержащий (b) антагонист мускариновых рецепторов М3 по п.1 или 2 совместно с инструкциями для совместного, раздельного или последовательного применения в комбинации с (а) ингибитором PDE4 по любому из пп.1, 3-6, предназначенный для лечения пациента, страдающего респираторным заболеванием, определенным в п.10 или 11.
15. Набор по п.14, дополнительно включающий с) другое активное соединение, определенное в п.8 или 9.
16. Упаковка, содержащая (b) антагонист мускариновых рецепторов М3 по п.1 или 2 и (а) ингибитор PDE4 по любому из пп.1, 3-6, предназначенные для совместного, раздельного или последовательного применения для лечения респираторного заболевания, определенного в п.10 или 11.
17. Упаковка по п.16, дополнительно включающая с) другое активное соединение, определенное в п.8 или 9.
18. Применение (b) антагониста мускариновых рецепторов М3 по п.1 или 2 для приготовления лекарственного средства для совместного, раздельного или последовательного применения в комбинации с (а) ингибитором PDE4 по любому из пп.1, 3-6 для лечения пациента, страдающего респираторным заболеванием, определенным в п.10 или 11.
19. Применение (а) ингибитора PDE4 по любому из пп.1, 3-6 для приготовления лекарственного средства для совместного, раздельного или последовательного применения в комбинации с (b) антагонистом мускариновых рецепторов М3 по п.1 или 2 для лечения пациента, страдающего респираторным заболеванием, определенным в п.10 или 11.
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- 2014-11-20 US US14/549,347 patent/US20150080359A1/en not_active Abandoned
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2015
- 2015-02-19 NL NL300720C patent/NL300720I1/nl unknown
- 2015-02-27 HU HUS1500011C patent/HUS1500011I1/hu unknown
- 2015-02-27 NO NO2015007C patent/NO2015007I2/no not_active IP Right Cessation
- 2015-03-02 LT LTPA2015010C patent/LTC1763368I2/lt unknown
- 2015-03-03 CY CY2015006C patent/CY2015006I2/el unknown
- 2015-07-09 US US14/795,194 patent/US20150306079A1/en not_active Abandoned
- 2015-10-22 US US14/920,519 patent/US20160038470A1/en not_active Abandoned
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2016
- 2016-03-24 US US15/080,475 patent/US20170049756A1/en not_active Abandoned
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2017
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2019
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