RU2384576C2 - Сульфонил-замещенные бициклические соединения в качестве модуляторов ppar - Google Patents

Сульфонил-замещенные бициклические соединения в качестве модуляторов ppar Download PDF

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RU2384576C2
RU2384576C2 RU2007116039/04A RU2007116039A RU2384576C2 RU 2384576 C2 RU2384576 C2 RU 2384576C2 RU 2007116039/04 A RU2007116039/04 A RU 2007116039/04A RU 2007116039 A RU2007116039 A RU 2007116039A RU 2384576 C2 RU2384576 C2 RU 2384576C2
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group
optionally substituted
hydrogen
lower alkyl
sulfonyl
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RU2007116039A (ru
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Стюарт А. НОБЛ (US)
Стюарт А. НОБЛ
Гай ОШИРО (US)
Гай ОШИРО
Джеймс В. МАЛЕЧА (US)
Джеймс В. МАЛЕЧА
Кунсян ЖАО (US)
Кунсян ЖАО
Кармен К. М. РОБИНСОН (US)
Кармен К. М. РОБИНСОН
Серджио Дж. ДЮРОН (US)
Серджио Дж. ДЮРОН
Майкл СЕРТИЧ (US)
Майкл СЕРТИЧ
Эндрю ЛИНДСТРОМ (US)
Эндрю ЛИНДСТРОМ
Эндрю ШИАУ (US)
Эндрю ШИАУ
Кристофер Д. БЭЙН (US)
Кристофер Д. БЭЙН
Стивен П. ГОВЕК (US)
Стивен П. Говек
Мехмет КАРАМАН (US)
Мехмет Караман
Болян ЛУ (US)
Болян ЛУ
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Калипсис, Инк
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Abstract

Описывается соединение, выбранное из группы, состоящей из Формулы II, Формулы III и Формулы IV: ! и ! или его соль, или сложный эфир, где G1 выбран из группы, включающей - (CR1R2)n-, n равно 0 или 1; R1 и R2 независимо выбраны из группы, включающей водород; X1, Х2 и Х3 независимо выбраны из группы, состоящей из водорода, необязательно замещенного низшего алкила, галогена, необязательно замещенного низшего алкокси; G2 - гетероциклоалкильный линкер, необязательно замещенный Х4 и Х5, при этом гетероциклоалкильный линкер выбран из группы, состоящей из пиперазинила, 3,6-дигидро-2Н-пиридинила, [1,4]диазепанила, 3,9-дазабицикло[3,3,1]нонила; Х4 и Х5 независимо выбраны из группы, состоящей из водорода и необязательно замещенного низшего алкила; CO2R; R выбран из группы, состоящей из необязательно замещенного низшего алкила и водорода; G3 - связь; G4 выбран из группы, состоящей из водорода, арила, выбранного из фенила необязательно замещенного низшим алкилом, галогеном, низшим галоалкилом, или низшим галоалкокси; гетероарила, выбранного из пиридинила, необязательно замещенного галогеном или низшим галоалкилом; и необязательно замещенного циклогетероалкила, выбранного из 1,3-бензодиоксолида. Описываются также конкретные соединения и фармацевтическая композиция. Представленные соединения используются в качестве модуляторов рецепторов, активируемых пероксисомальным пролифератором (PPAR). 5 н.з.п. ф-лы, 2 табл.

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Claims (5)

1. Соединение, имеющее структурную формулу, выбранную из группы, состоящей из Формулы II, Формулы III и Формулы IV:
Figure 00000146
,
Figure 00000147
, и
Figure 00000148

или его соль, или сложный эфир, где:
G1 выбран из группы, включающей -(CR1R2)n-,
n равно 0 или 1;
R1 и R2 независимо выбраны из группы, включающей водород.
X1, X2 и X3 независимо выбраны из группы, состоящей из водорода, необязательно замещенного низшего алкила, галогена, необязательно замещенного низшего алкокси;
G2 - гетероциклоалкильный линкер, необязательно замещенный Х4 и Х5, при этом гетероциклоалкильный линкер выбран из группы, состоящей из пиперазинила, 3,6-дигидро-2Н-пиридинила, [1,4]диазепанила, 3,9-дазабицикло [3,3,1]нонила;
Х4 и Х5 независимо выбраны из группы, состоящей из водорода и необязательно замещенного низшего алкила; CO2R;
R выбран из группы, состоящей из необязательно замещенного низшего алкила и водорода;
G3 - связь;
G4 выбран из группы, состоящей из водорода, арила, выбранного из фенила, необязательно замещенного низшим алкилом, галогеном, низшим галоалкилом, или низшим галоалкокси; гетероарила, выбранного из пиридинила, необязательно замещенного галогеном или низшим галоалкилом; и необязательно замещенного циклогетероалкила, выбранного их 1,3-бензодиоксолида.
2. Соединение, выбранное из группы, состоящей из соединений:
Figure 00000149

Figure 00000150

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Рацематы:
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3. Соединение, выбранное из группы, состоящей из (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-фенил)-пиперазин-1-сульфонил]-индан-2-карбоновой кислоты и (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-бензил)-пиперазин-1-сульфонил]-индан-2-карбоновой кислоты, или его соль.
4. Соль, выбранная из группы, состоящей из тозилата (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-фенил)-пиперазин-1-сульфонил]-индан-2-карбоновой кислоты и тозилата (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-бензил)-пиперазин-1-сульфонил]-индан-2-карбоновой кислоты.
5. Фармацевтическая композиция, модулирующая функцию рецептора, активируемого пероксисомальным пролифератором, включающая соединение по любому из пп.1-4 и фармацевтически приемлемый носитель.
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