RU2007123253A - Производные тетералина и индана и их применения - Google Patents

Производные тетералина и индана и их применения Download PDF

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RU2007123253A
RU2007123253A RU2007123253/04A RU2007123253A RU2007123253A RU 2007123253 A RU2007123253 A RU 2007123253A RU 2007123253/04 A RU2007123253/04 A RU 2007123253/04A RU 2007123253 A RU2007123253 A RU 2007123253A RU 2007123253 A RU2007123253 A RU 2007123253A
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compound
compound according
benzenesulfonyl
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piperazine
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RU2389723C2 (ru
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III Ральф Нью ХАРРИС (US)
III Ральф Нью ХАРРИС
Ненси Элизабет КРАУСС (US)
Ненси Элизабет КРАУСС
Джеймс М. КРЕСС (US)
Джеймс М. КРЕСС
Девид Брюс РЕПКЕ (US)
Девид Брюс РЕПКЕ
Расселл Стефен СТАБЛЕР (US)
Расселл Стефен СТАБЛЕР
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Ф. Хоффманн-Ля Рош Аг (Ch)
Ф. Хоффманн-Ля Рош Аг
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Claims (29)

1. Соединение формулы I
Figure 00000001
;
или его фармацевтически приемлемая соль,
где m имеет значение от 0 до 3;
р имеет значение от 1 до 3;
q имеет значение 0, 1 или 2;
Ar представляет собой возможно замещенный арил или возможно замещенный 5-12-членный гетероарил;
каждый R1 независимо представляет собой галогено, С1-12-алкил, C1-12-галогеноалкил, C1-12-гетероалкил, циано, -S(O)t-Ra, -C(=О)-NRbRc, -SO2-NRbRc, -N(Rd)-C(=O)-Re или -C(=O)-Re, где t имеет значение от 0 до 2, каждый из Ra, Rb, Rc и Rd независимо представляет собой водород или C1-12-алкил и Re представляет собой водород, C1-12-алкил, C1-12-алкокси или гидрокси;
R2 представляет собой
Figure 00000002
;
каждый из n и r независимо имеет значение 1 или 2; и
Х представляет собой -NR3, когда n имеет значение 2, или Х представляет собой -CHNR4R5, когда n имеет значение 1 или 2, где каждый из R3, R4 и R5 независимо представляет собой водород или метил,
при условии, что исключен 4-(4-хлорфенилтио)-1-(метилпиперазино)индан.
2. Соединение по п.1, где р имеет значение 1 или 2.
3. Соединение по п.2, где q имеет значение 2.
4. Соединение по п.1, где n имеет значение 2.
5. Соединение по п.3, где Х представляет собой -NR3.
6. Соединение по п.5, где r имеет значение 1.
7. Соединение по п.6, где Ar представляет собой возможно замещенный арил.
8. Соединение по п.7, где Ar представляет собой возможно замещенный фенил.
9. Соединение по п.8, где R3 представляет собой водород.
10. Соединение по п.8, где R3 представляет собой метил.
11. Соединение по п.5, где R2 представляет собой
Figure 00000003
;
Figure 00000004
или
Figure 00000005
,
где каждый из R3, R4 и R5 независимо представляет собой водород или метил.
12. Соединение по п.1, где указанное соединение представляет собой соединение формулы II
Figure 00000006
;
и где m, p, Ar, R1 и R3 являются такими, как изложено в п.1.
13. Соединение по п.12, где p имеет значение 1 или 2.
14. Соединение по п.13, где q имеет значение 2.
15. Соединение по п.14, где Ar представляет собой возможно замещенный арил.
16. Соединение по п.15, где Ar представляет собой возможно замещенный фенил.
17. Соединение по п.16, где R3 представляет собой водород.
18. Соединение по п.16, где R3 представляет собой метил.
19. Соединение по п.1, где указанное соединение представляет собой соединение формулы IIIа или IIIб
Figure 00000007
;
Figure 00000008
;
где s имеет значение от 0 до 4;
каждый R6 независимо представляет собой галогено, C1-12-алкил, С1-12-галогеноалкил, C1-12-гетероалкил, циано, -S(O)t-Ra, -C(=O)-NRbRc, -SO2-NRbRc, -N(Rd)-C(=O)-Re или -C(=O)-Re, где t имеет значение от 0 до 2, каждый из Ra, Rb, Rc и Rd независимо представляет собой водород или C1-12-алкил и Re представляет собой водород, C1-12-алкил, C1-12-алкокси или гидрокси; и
R3 является таким, как изложено в п.1.
20. Соединение по п.19, где s имеет значение от 0 до 2 и каждый R6 независимо представляет собой галогено, C1-12-алкил, C1-12-алкокси или C1-12-галогеноалкил.
21. Соединение по п.19, где указанное соединение представляет собой соединение формулы IIIа.
22. Соединение по п.21, где R3 представляет собой водород.
23. Соединение по п.21, где R3 представляет собой метил.
24. Соединение по п.21, где s имеет значение 0 или 1 и R6 представляет собой галогено.
25. Соединение по п.1, где указанное соединение выбрано из
1-(5-бензолсульфонил-индан-1-ил)-пиперазина;
1-(5-бензолсульфонил-индан-1-ил)-пирролидин-3-иламина;
1-[5-(4-фтор-бензолсульфонил)-индан-1-ил]-пиперазина;
1-[5-(2-фтор-бензолсульфонил)-индан-1-ил]-пиперазина;
1-[5-(3-хлор-бензолсульфонил)-индан-1-ил]-пиперазина;
1-[5-(3-хлор-бензолсульфонил)-индан-1-ил]-пиперидин-4-иламина;
1-(7-бензолсульфонил-1,2,3,4-тетрагидро-нафталин-1-ил)-пиперазина;
1-(6-бензолсульфонил-1,2,3,4-тетрагидро-нафталин-1-ил)-пиперазина;
1-[6-(4-фтор-бензолсульфонил)-1,2,3,4-тетрагидро-нафталин-1-ил]-пиперазина;
1-(6-бензолсульфонил-1,2,3,4-тетрагидро-нафталин-1-ил)-пиперидин-4-иламина и
1-(6-бензолсульфонил-1,2,3,4-тетрагидро-нафталин-1-ил)-4-метил-пиперазина.
26. Фармацевтическая композиция, содержащая эффективное количество соединения по п.1 в смеси с фармацевтически приемлемым носителем.
27. Применение соединения формулы I по п.1 в приготовлении лекарства, полезного в лечении болезненного состояния центральной нервной системы.
28. Применение по п.27, где болезненное состояние центральной нервной системы выбрано из психозов, шизофрении, маниакальных депрессий, неврологических расстройств, нарушений памяти, синдрома дефицита внимания, болезни Паркинсона, бокового амиотрофического склероза, болезни Альцгеймера, расстройств приема пищи и болезни Хантингтона.
29. Применение соединения формулы I по п.1 в приготовлении лекарства, полезного в лечении расстройства желудочно-кишечного тракта.
RU2007123253/04A 2004-12-21 2005-12-12 Производные тетралина и индана и их применения RU2389723C2 (ru)

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ES2332526T3 (es) 2010-02-08
EP1831189B1 (en) 2009-11-11
ATE448216T1 (de) 2009-11-15
WO2006066745A1 (en) 2006-06-29
KR100899061B1 (ko) 2009-05-25
US7473690B2 (en) 2009-01-06
KR20070088797A (ko) 2007-08-29
CN101124210A (zh) 2008-02-13
MX2007007481A (es) 2007-07-20
RU2389723C2 (ru) 2010-05-20
JP2008524274A (ja) 2008-07-10
BRPI0515835A (pt) 2008-08-12
CA2591793A1 (en) 2006-06-29
AU2005318595B2 (en) 2011-03-03
US20060160825A1 (en) 2006-07-20
DE602005017663D1 (de) 2009-12-24
AU2005318595A1 (en) 2006-06-29
EP1831189A1 (en) 2007-09-12

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