RU2006126978A - Производные 3-(4-бензилоксифенил)пропановой кислоты - Google Patents

Производные 3-(4-бензилоксифенил)пропановой кислоты Download PDF

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RU2006126978A
RU2006126978A RU2006126978/04A RU2006126978A RU2006126978A RU 2006126978 A RU2006126978 A RU 2006126978A RU 2006126978/04 A RU2006126978/04 A RU 2006126978/04A RU 2006126978 A RU2006126978 A RU 2006126978A RU 2006126978 A RU2006126978 A RU 2006126978A
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salt
optionally substituted
methoxy
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Цунео ЯСУМА (JP)
Цунео Ясума
Судзи КИТАМУРА (JP)
Судзи КИТАМУРА
Нобуюки НЕГОРО (JP)
Нобуюки Негоро
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Такеда Фармасьютикал Компани Лимитед (Jp)
Такеда Фармасьютикал Компани Лимитед
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Claims (20)

1. Соединение, представленное формулой (I)
Figure 00000001
где R1, R3, R4 и R5 являются одинаковыми или разными и каждый представляет атом водорода, атом галогена, необязательно замещенную углеводородную группу или необязательно замещенную гидроксильную группу;
R2 представляет атом галогена, нитрогруппу, необязательно замещенную углеводородную группу, необязательно замещенную гидроксильную группу, необязательно замещенную аминогруппу, необязательно замещенную меркаптогруппу, необязательно замещенную ацильную группу или необязательно замещенную гетероциклическую группу;
R10 и R11 являются одинаковыми или разными и каждый представляет атом водорода, атом галогена или С1-6-алкоксигруппу;
Е представляет связь, необязательно замещенную С1-4 алкиленовую группу, -W1-О-W2-, -W1-S-W2- или -W1-N(R6)-W2- (где W1 и W2 являются одинаковыми или разными и каждый представляет связь или необязательно замещенную С1-3-алкиленовую группу, и R6 представляет атом водорода, необязательно замещенную ацильную группу или необязательно замещенную углеводородную группу);
цикл S1 представляет бензольное кольцо, необязательно дополнительно имеющее заместитель(лей), выбранный(ых) из атома галогена, необязательно замещенной гидроксильной группы и необязательно замещенной аминогруппы; и
R представляет необязательно замещенную гидроксильную группу или необязательно замещенную аминогруппу;
при условии, что R1 и R2 не являются одновременно атомами водорода,
или его соль.
2. Соединение по п.1, в котором R2 представляет атом галогена, необязательно замещенную углеводородную группу, необязательно замещенную гидроксильную группу, необязательно замещенную аминогруппу, необязательно замещенную меркаптогруппу или необязательно замещенную гетероциклическую группу, и R10 и R11 оба являются атомами водорода, или его соль.
3. Пролекарство соединения по п.1 или его соль.
4. Соединение по п.1, у которого R4 и R5 являются одинаковыми или разными и каждый представляет собой атом водорода или атом галогена, или его соль.
5. Соединение по п.1, у которого Е является связью, или его соль.
6. Соединение по п.1, у которого R является гидроксильной группой, или его соль.
7. Соединение по п.1, у которого R1 и R3 являются одинаковыми или разными и каждый является С1-6-алкильной группой, или его соль.
8. Соединение по п.1, у которого R2 является необязательно замещенной гидроксильной группой, или его соль.
9. Соединение по п.1, у которого R10 и R11, оба являются атомами водорода, или его соль.
10. Соединение по п.1, у которого цикл S1 является бензольным кольцом, необязательно дополнительно имеющим С1-6-алкоксигруппу, или его соль.
11. 3-[4-[[4'-(бензилокси)-2',6'-диметилбифенил-3-ил]-метокси]фенил]пропановая кислота;
3-(4-{[4'-(2-этоксиэтокси)-2',6'-диметилбифенил-3-ил]-метокси}фенил)-2,2-дифторпропановая кислота;
3-[4-({4'-[2-(этилсульфонил)этокси]-2',6'-диметилбифенил-3-ил]-метокси)-2-фторфенил]пропановая кислота;
3-[4-({2',6'-диметил-4'-[3-(2-оксопирролидин-1-ил)-пропокси]бифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-[4-({2',6'-диметил-4'-[(6-метилпиридин-2-ил)метокси]-бифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-[2-фтор-4-({4'-[(4-гидрокси-1,1-диоксидтетрагидро-2Н-тиопиран-4-ил)метокси]-2',6'-диметилбифенил-3-ил}метокси)-фенил]пропановая кислота;
3-[4-({2',6'-диметил-4'-[(метилсульфонил)окси]бифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-[4-({4'-[(1,1-диоксидтетрагидро-2Н-тиопиран-4-ил)окси]-2',6'-диметилбифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-[4-({2',6'-диметил-4'-[(3-метилоксетан-3-ил)метокси]-бифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-(4-{[2',6'-диметил-4'-(тетрагидро-2Н-пиран-4-илокси)-бифенил-3-ил]метокси}-2-фторфенил)пропановая кислота;
3-[4-({4'-[3-(диэтоксифосфорил)пропокси]-2',6'-диметилбифенил-3-ил}метокси)-2-фторфенил]пропановая кислота;
3-[2-фтор-4-({6-изопропокси-2',6'-диметил-4'-[(3-метилоксетан-3-ил)метокси]бифенил-3-ил}метокси)фенил]пропановая кислота
или их соли.
12. Модулятор функции рецепторов GРR40, содержащий соединение по п.1, или его соль, или его пролекарство.
13. Фармацевтическое средство, содержащее соединение по п.1, или его соль, или его пролекарство.
14. Фармацевтическое средство по п.13, которое является средством для профилактики или лечения диабета.
15. Применение соединения по п.1, или его соли, или его пролекарства для производства модулятора функции рецепторов GРR40.
16. Применение соединения по п.1, или его соли, или его пролекарства для производства средства для профилактики или лечения диабета.
17. Способ модификации функции рецепторов GРR40 у млекопитающего, который включает введение эффективного количества соединения по п.1, или его соли, или его пролекарства млекопитающему.
18. Способ профилактики или лечения диабета у млекопитающего, который включает введение эффективного количества соединения по п.1, или его соли, или его пролекарства млекопитающему.
19. Способ получения соединения, представленного формулой (Ib)
Figure 00000002
где R1, R2, R3, R4, R5, R10, R11, Е и цикл S1 имеют значения, представленные в п.1,
или его соли, который включает взаимодействие соединения, представляемого формулой (Х)
Figure 00000003
где каждый символ имеет значение, представленное выше,
или его соли и соединения, представляемого формулой (II)
Figure 00000004
где R4, R5, R10 и R11 имеют значения, представленные выше, и R' представляет необязательно замещенную С1-6-алкоксигруппу,
или его соли с получением соединения, представленного формулой (Ib')
Figure 00000005
где каждый символ имеет значение, представленное выше,
или его соли и проведение реакции гидролиза данного соединения или его соли.
20. Способ получения соединения, представляемого формулой (Id)
Figure 00000006
где R1, R3, R4, R5, R10, R11, Е и цикл S1 имеют значения, представленные в п.1, Y представляет -О- или -S- и R2' является заместителем,
или его соли, который включает взаимодействие соединения, представляемого формулой (Ie')
Figure 00000007
где R1, R3, R4, R5, R10, R11, Е, Y и цикл S1 имеют значения, представленные выше, R' имеет значение, представленное в п.19,
или его соли и соединения, представляемого формулой
R 2 '-ОН,
где R2' имеет значение, представленное выше,
или его соли с получением соединения, представляемого формулой (If')
Figure 00000008
где каждый символ имеет значение, представленное выше,
или его соли и проведение реакции гидролиза данного соединения или его соли.
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AU2004309271A1 (en) 2005-07-14
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BRPI0418148A (pt) 2007-04-17
CO5721002A2 (es) 2007-01-31
US7456218B2 (en) 2008-11-25
US20070149608A1 (en) 2007-06-28
IL176189A0 (en) 2006-10-05
CA2551610A1 (en) 2005-07-14
TW200523247A (en) 2005-07-16

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