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RU2008129667A - Соединения с медицинскими эффектами, обусловленными взаимодействием с рецептором глюкокортикоидов - Google Patents

Соединения с медицинскими эффектами, обусловленными взаимодействием с рецептором глюкокортикоидов Download PDF

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RU2008129667A
RU2008129667A RU2008129667/04A RU2008129667A RU2008129667A RU 2008129667 A RU2008129667 A RU 2008129667A RU 2008129667/04 A RU2008129667/04 A RU 2008129667/04A RU 2008129667 A RU2008129667 A RU 2008129667A RU 2008129667 A RU2008129667 A RU 2008129667A
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alkoxy
halogen
hydrogen
optionally halogenated
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RU2430086C2 (ru
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Нилл Мортон ХЭМИЛТОН (GB)
Нилл Мортон ХЭМИЛТОН
Саймон Джеймс Энтони ГРОУВ (GB)
Саймон Джеймс Энтони ГРОУВ
Майкл Джон КИЦУН (GB)
Майкл Джон КИЦУН
Джон Ричард МОРФИ (GB)
Джон Ричард Морфи
Брэд ШЕРБОРН (GB)
Брэд ШЕРБОРН
Питер Томас Алберт ЛИТТЛВУД (GB)
Питер Томас Алберт Литтлвуд
Ангус Ричард БРАУН (GB)
Ангус Ричард БРАУН
Селия КИНГСБЕРИ (US)
Селия КИНГСБЕРИ
Майкл ОЛЬМЕЙЕР (US)
Майкл Ольмейер
Кок-Кан ХО (US)
Кок-Кан Хо
Стивен Дж КАЛТДЖЕН (US)
Стивен Дж КАЛТДЖЕН
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Н.В. Органон (Nl)
Н.В. Органон
Фармакопия, Инк. (Us)
Фармакопия, Инк.
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Abstract

1. Соединение, имеющее строение согласно формуле I ! ! где X представляет собой атом азота или углерода; ! Ar представляет собой фенил или гетероароматический цикл; ! R1 представляет собой водород, галоген, CN или (C1-C4)алкил; ! R2 представляет собой водород, галоген или необязательно фторированный (C1-C3)алкокси; ! R3 и R5 независимо представляют собой водород, необязательно галогенированный (C1-C4)алкил, необязательно галогенированный (C1-C4)алкокси, необязательно галогенированный арил(C1-C4)алкокси, необязательно галогенированный (C1-C4)алкенил или гидроксилметил; ! R4 представляет собой водород, галоген, необязательно галогенированный (C1-C4)алкокси или необязательно галогенированный арил(C1-C4)алкокси; ! R6 представляет собой водород, бензил, необязательно замещенный одним и более галогеном, или (C1-C4)алкилом, или R6 необязательно является галогенированным (C1-C4)алкилом; ! каждый R7 независимо представляет собой водород, галоген, необязательно галогенированный (C1-C4)алкил или необязательно галогенированный (C1-C4)алкокси; ! или его фармацевтически приемлемая кислотно-аддитивная соль. ! 2. Соединение по п.1, где ! X представляет собой атом азота или углерода; ! Ar представляет собой бензольный или гетероароматический цикл; ! R2 представляет собой галоген или необязательно фторированный (C1-C3)алкокси; ! по меньшей мере один из R3, R4 или R5 представляет собой водород; ! R6 представляет собой водород или метил; ! или его фармацевтически приемлемая аддитивная соль. ! 3. Соединение по п.1, где ! Ar представляет собой тиазол, тиофен, изоксазол, фуран или 1H-пиразол; ! R1 представляет собой водород, галоген, CN или метил; ! R2 представляет собой водород, галоген или необязательн�

Claims (6)

1. Соединение, имеющее строение согласно формуле I
Figure 00000001
где X представляет собой атом азота или углерода;
Ar представляет собой фенил или гетероароматический цикл;
R1 представляет собой водород, галоген, CN или (C1-C4)алкил;
R2 представляет собой водород, галоген или необязательно фторированный (C1-C3)алкокси;
R3 и R5 независимо представляют собой водород, необязательно галогенированный (C1-C4)алкил, необязательно галогенированный (C1-C4)алкокси, необязательно галогенированный арил(C1-C4)алкокси, необязательно галогенированный (C1-C4)алкенил или гидроксилметил;
R4 представляет собой водород, галоген, необязательно галогенированный (C1-C4)алкокси или необязательно галогенированный арил(C1-C4)алкокси;
R6 представляет собой водород, бензил, необязательно замещенный одним и более галогеном, или (C1-C4)алкилом, или R6 необязательно является галогенированным (C1-C4)алкилом;
каждый R7 независимо представляет собой водород, галоген, необязательно галогенированный (C1-C4)алкил или необязательно галогенированный (C1-C4)алкокси;
или его фармацевтически приемлемая кислотно-аддитивная соль.
2. Соединение по п.1, где
X представляет собой атом азота или углерода;
Ar представляет собой бензольный или гетероароматический цикл;
R2 представляет собой галоген или необязательно фторированный (C1-C3)алкокси;
по меньшей мере один из R3, R4 или R5 представляет собой водород;
R6 представляет собой водород или метил;
или его фармацевтически приемлемая аддитивная соль.
3. Соединение по п.1, где
Ar представляет собой тиазол, тиофен, изоксазол, фуран или 1H-пиразол;
R1 представляет собой водород, галоген, CN или метил;
R2 представляет собой водород, галоген или необязательно фторированный (C1-C2)алкокси;
R3 и R5 независимо представляют собой водород, (C1-C3)алкил, бензилокси, (C2-C3)алкенил, гидроксилметил или необязательно фторированный метокси;
R4 представляет собой водород, F, Cl или метокси, и по меньшей мере один из R3, R4 и R5 является водородом;
R6 представляет собой водород или метил;
каждый R7 независимо представляет собой водород, необязательно фторированный метил, необязательно фторированный метокси, F, Cl, бром или циано;
или его фармацевтически приемлемая аддитивная соль.
4. Применение соединения по любому из пп.1-3 в способе лечения, цель которого состоит в изменении уровня активности вторичного сигнала после активации рецептора глюкокортикоидов.
5. Применение по п.4, где лечение направлено на депрессию, тревогу или заболевания, отражающие высокие уровни кортизола в плазме.
6. Применение по п.5, где лечение направлено на посттравматическое стрессовое расстройство.
RU2008129667/04A 2005-12-21 2006-12-18 Соединения с медицинскими эффектами, обусловленными взаимодействием с рецептором глюкокортикоидов RU2430086C2 (ru)

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CA2716136A1 (en) * 2008-03-06 2009-09-11 William P. Dankulich Hexahydrocyclopentyl[f]indazole sulfonamides and derivatives thereof as selective glucocorticoid receptor modulators
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US20130190356A1 (en) * 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
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AU2006328550A1 (en) 2007-06-28
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BRPI0620184A2 (pt) 2011-11-01
WO2007071638A1 (en) 2007-06-28
JP5319299B2 (ja) 2013-10-16
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CN101534811A (zh) 2009-09-16
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US20070149577A1 (en) 2007-06-28
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