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RU2012127334A - Производные 5-замещенного хиназолинона, содержащие их композиции и способы их применения - Google Patents

Производные 5-замещенного хиназолинона, содержащие их композиции и способы их применения Download PDF

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Publication number
RU2012127334A
RU2012127334A RU2012127334/04A RU2012127334A RU2012127334A RU 2012127334 A RU2012127334 A RU 2012127334A RU 2012127334/04 A RU2012127334/04 A RU 2012127334/04A RU 2012127334 A RU2012127334 A RU 2012127334A RU 2012127334 A RU2012127334 A RU 2012127334A
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optionally substituted
halogen atoms
alkyl
hydrogen atom
halogen
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RU2012127334/04A
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RU2617989C2 (ru
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Джордж В. Мюллер
Хон-Ва МЭН
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Селджин Корпорейшн
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Abstract

1. Способ лечения или регулирования заболевания или нарушения, включающий введение пациенту соединения формулы (I):или его фармацевтически приемлемой соли, сольвата или стереоизомера, где:Rпредставляет собой атом водорода; атом галогена; -(CH)OH; (С-С)алкил, необязательно замещенный одним или несколькими атомами галогена; (С-С)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена; или-(СН)NHR, где Rпредставляет собойатом водорода;(С-С)алкил, необязательно замещенный одним или несколькими атомами галогена;-(СН)-(6-10-членный арил);-С(О)-(СН)-(6-10-членный арил) или -С(О)-(СН)-(6-10-членный гетероарил), где арил или гетероарил необязательно замещены одним или несколькими заместителями из атома галогена; -SCF; (С-С)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С-С)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена;-С(О)-(С-С)алкил, где алкил необязательно замещен одним или несколькими атомами галогена;-С(О)-(СН)-(С-С-циклоалкил);-С(О)-(СН)-NRR, где Rи Rкаждый независимо друг от друга представляет собойатом водорода;(С-С)алкил, необязательно замещенный одним или несколькими атомами галогена;(С-С)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена; или6-10-членный арил, необязательно замещенный одним или несколькими заместителями из атома галогена; (С-С)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С-С)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена;-С(О)-(СН)-О-(С-С)алкил; или-С(О)-(СН)-О-(СН)-(6-10-членный арил);Rпредставляет собой: атом водорода; -(СН)OH; �

Claims (16)

1. Способ лечения или регулирования заболевания или нарушения, включающий введение пациенту соединения формулы (I):
Figure 00000001
или его фармацевтически приемлемой соли, сольвата или стереоизомера, где:
R1 представляет собой атом водорода; атом галогена; -(CH2)nOH; (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; (С1-С6)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена; или
-(СН2)nNHRa, где Ra представляет собой
атом водорода;
(С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
-(СН2)n-(6-10-членный арил);
-С(О)-(СН2)n-(6-10-членный арил) или -С(О)-(СН2)n-(6-10-членный гетероарил), где арил или гетероарил необязательно замещены одним или несколькими заместителями из атома галогена; -SCF3; (С1-С6)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С1-С6)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена;
-С(О)-(С1-С8)алкил, где алкил необязательно замещен одним или несколькими атомами галогена;
-С(О)-(СН2)n-(С3-С10-циклоалкил);
-С(О)-(СН2)n-NRbRc, где Rb и Rc каждый независимо друг от друга представляет собой
атом водорода;
(С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
(С1-С6)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена; или
6-10-членный арил, необязательно замещенный одним или несколькими заместителями из атома галогена; (С1-С6)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С1-С6)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена;
-С(О)-(СН2)n-О-(С1-С6)алкил; или
-С(О)-(СН2)n-О-(СН2)n-(6-10-членный арил);
R2 представляет собой: атом водорода; -(СН2)nOH; фенил; -О(С1-С6)алкил; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
R3 представляет собой атом водорода; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; и
n принимает значения 0, 1 или 2; и где заболевание или нарушение представляет собой рак, нарушение, связанное с ангиогенезом, боль, дегенерацию желтого пятна и сопутствующий синдром, кожное заболевание, легочное заболевание, связанное с асбестом нарушение, паразитное заболевание, иммунодефицитное расстройство, расстройство ЦНС, поражение ЦНС, атеросклероз и сопутствующее нарушение, дисфункциональный сон или сопутствующее нарушение, гемоглобинопатия или сопутствующее нарушение, TNFα-связанные нарушения.
2. Способ по п.1, где соединение имеет структуру формулы (II):
Figure 00000002
или его фармацевтически приемлемая соль, сольват или стереоизомер, где:
R4 представляет собой атом водорода; атом галогена; -(CH2)nOH; (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; (С1-С6)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена;
R5 представляет собой атом водорода; -(СН2)nOH; фенил; -О(С1-С6)алкил; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
R6 представляет собой атом водорода; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; и
n принимает значения 0, 1 или 2.
3. Способ по п.2, где R4 представляет собой метил или метокси-группу.
4. Способ по п.2, где R4 представляет собой F или Cl.
5. Способ по п.2, где R4 представляет собой -CF3.
6. Способ по п.2, где соединение представляет собой:
Figure 00000003
Figure 00000004
или его фармацевтически приемлемая соль, сольват или стереоизомер.
7. Способ по п.1, где соединение представляет собой соединение формулы (III):
Figure 00000005
или его фармацевтически приемлемая соль, сольват или стереоизомер, где:
Rd представляет собой
атом водорода;
(С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
-С(О)-(С1-С8)алкил, где алкил необязательно замещен одним или несколькими атомами галогена;
-С(О)-(СН2)n-(С3-С10-циклоалкил);
-С(О)-(СН2)n-NReRf, где Re и Rf каждый независимо друг от друга представляет собой
атом водорода;
(С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; или
(С1-С6)алкокси-группу, необязательно замещенную одним или несколькими атомами галогена; или
-С(О)-(СН2)n-О-(С1-С6)алкил;
R7 представляет собой атом водорода; -(СН2)nOH; фенил; -О-(С1-С6)алкил; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
R8 представляет собой атом водорода; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; и
n принимает значения 0, 1 или 2.
8. Способ по п.7, где R7 представляет собой метил.
9. Способ по п.7, где Rd представляет собой -С(О)-(С1-С6)алкил.
10. Способ по п.7, где Rd представляет собой -С(О)-СН2-О-(С1-С6)алкил.
11. Способ по п.7, где соединение представляет собой:
Figure 00000006
или его фармацевтически приемлемая соль, сольват или стереоизомер.
12. Способ по п.1, где соединение представляет собой соединение формулы (IV):
Figure 00000007
или его фармацевтически приемлемая соль, сольват или стереоизомер, где:
Rg представляет собой
-(СН2)n-(6-10-членный арил);
-С(О)-(СН2)n-(6-10-членный арил) или -С(О)-(СН2)n-(6-10-членный гетероарил), где арил или гетероарил необязательно замещены одним или несколькими заместителями из атома галогена; -SCF3; (С1-С6)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С1-С6)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена;
-С(О)-(СН2)n-NHRh, где Rh представляет собой
6-10-членный арил, необязательно замещенный одним или несколькими заместителями из атома галогена; (С1-С6)алкила, самого необязательно замещенного одним или несколькими атомами галогена; или (С1-С6)алкокси-группы, самой необязательно замещенной одним или несколькими атомами галогена; или
-С(О)-(СН2)n-O-(CH2)n-(6-10 членный арил);
R9 представляет собой атом водорода; -(СН2)nOH; фенил; -О-(С1-С6)алкил; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена;
R10 представляет собой атом водорода; или (С1-С6)алкил, необязательно замещенный одним или несколькими атомами галогена; и
n принимает значения 0, 1 или 2.
13. Способ по п.12, где R9 представляет собой метил.
14. Способ по п.12, где Rg представляет собой -С(О)-фенил, -С(О)-СН2-фенил или -С(О)-NH-фенил.
15. Способ по п.14, где фенил замещен одним или несколькими заместителями из метила, -CF3 или атома галогена.
16. Способ по п.12, где соединение представляет собой:
Figure 00000008
Figure 00000009
или его фармацевтически приемлемая соль, сольват или стереоизомер.
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EP2066656A2 (en) 2009-06-10
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IL228017A0 (en) 2013-09-30
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