RU2016141934A - Ингибиторы циклин-зависимой киназы 7 (cdk7) - Google Patents

Ингибиторы циклин-зависимой киназы 7 (cdk7) Download PDF

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RU2016141934A
RU2016141934A RU2016141934A RU2016141934A RU2016141934A RU 2016141934 A RU2016141934 A RU 2016141934A RU 2016141934 A RU2016141934 A RU 2016141934A RU 2016141934 A RU2016141934 A RU 2016141934A RU 2016141934 A RU2016141934 A RU 2016141934A
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Кевин Спротт
Джейсон Дж. МАРИНО
Дарби Шмидт
М. Аршад СИДДИКИ
Стефан КИБЛАТ
Стефани РОЙ
Дана К. ВИНТЕР
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Сирос Фармасьютикалз, Инк.
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    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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Claims (35)

1. Соединение структурной Формулы (Ic):
Figure 00000001
(Ic);
или его фармацевтически приемлемая соль, сольват, гидрат, таутомер, стереоизомер или его изотопно меченое производное, где:
кольцо Aʺ выбрано из
Figure 00000002
,
Figure 00000003
,
Figure 00000004
,
Figure 00000005
и
Figure 00000006
;
каждый из R7, R8 и R10 независимо выбран из водорода и метила;
R21a выбран из Cl, CN, CF3, CH3 и CH2CH3; и
каждый R12, если он присутствует, представляет собой галоген; и o равно 0, 1, 2 или 3.
2. Соединение по п. 1, имеющее структурную Формулу (Ic'):
Figure 00000007
(Ic'),
где кольцо A'', R7, R8, R10, R21a, R12 и o являются такими, как определено в п. 1.
3. Соединение по п. 1 или 2, где каждый R12, если он присутствует, представляет собой фтор.
4. Соединение по любому из пп. 1-3, где o представляет собой 0.
5. Соединение по п. 1, выбранное из любого из Соединений, представленных ниже:
Figure 00000008
,
Figure 00000009
,
Figure 00000010
,
Figure 00000011
,
Figure 00000012
,
Figure 00000013
,
Figure 00000014
,
Figure 00000015
,
Figure 00000016
, и
Figure 00000017
.
6. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-5 или 16 и фармацевтически приемлемое вспомогательное вещество.
7. Композиция по п. 6 для применения при лечении субъекта, страдающего от заболевания или состояния, связанного с аберрантной активностью CDK.
8. Композиция для применения по п. 7, отличающаяся тем, что субъект страдает от заболевания или состояния, связанного с аберрантной активностью CDK7.
9. Композиция по п. 6 для применения в лечении заболевания или состояния, которое выбрано из рака, доброкачественного новообразования, ангиогенеза, воспалительного заболевания, аутовоспалительного заболевания, аутоиммунного заболевания или инфекционного заболевания.
10. Композиция для применения по п. 9, отличающаяся тем, что субъект является человеком.
11. Композиция для применения по любому из пп. 9 и 10, отличающаяся тем, что заболевание представляет собой рак.
12. Композиция для применения по п. 11, отличающаяся тем, что рак выбран из рака крови, меланомы, рака кости, рака молочной железы, рака мозга или рака легкого.
13. Композиция для применения по п. 12, отличающаяся тем, что рак представляет собой рак крови, выбранный из хронического лимфоцитарного лейкоза (ХЛЛ), острого лимфобластного лейкоза (ОЛЛ), T клеточного острого лимфобластного лейкоза (T ОЛЛ), хронического миелогенного лейкоза (ХМЛ), острого миелогенного лейкоза (ОМЛ), лимфомы и множественной миеломы.
14. Композиция для применения по п. 12, отличающаяся тем, что рак выбран из остеосаркомы, саркомы Юинга, трижды негативного рака молочной железы (ТНРМЖ), нейробластомы и мелкоклеточного рака легкого (МКРЛ).
15. Композиция для применения по любому из пп. 9-14, отличающаяся тем, что композицию применяют в сочетании с одним или более дополнительными агентами, независимо выбранными из антипролиферативных агентов, противораковых агентов, иммуносупрессивных агентов и облегчающих боль агентов.
16. Соединение, выбранное из любого из соединений, представленных ниже:
Figure 00000018
,
Figure 00000019
,
Figure 00000020
,
Figure 00000021
,
Figure 00000022
,
Figure 00000023
,
Figure 00000024
,
Figure 00000025
, и
Figure 00000026
.
RU2016141934A 2014-04-04 2015-04-03 Ингибиторы циклин-зависимой киназы 7 (cdk7) RU2016141934A (ru)

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US201461975457P 2014-04-04 2014-04-04
US61/975,457 2014-04-04
US201462053741P 2014-09-22 2014-09-22
US62/053,741 2014-09-22
PCT/US2015/024357 WO2015154038A1 (en) 2014-04-04 2015-04-03 Inhibitors of cyclin-dependent kinase 7 (cdk7)

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