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RU2439068C2 - Модуляторы mglur5 - Google Patents

Модуляторы mglur5 Download PDF

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RU2439068C2
RU2439068C2 RU2009111113/04A RU2009111113A RU2439068C2 RU 2439068 C2 RU2439068 C2 RU 2439068C2 RU 2009111113/04 A RU2009111113/04 A RU 2009111113/04A RU 2009111113 A RU2009111113 A RU 2009111113A RU 2439068 C2 RU2439068 C2 RU 2439068C2
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methyl
triazol
ethoxy
chlorophenyl
compound according
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RU2009111113/04A
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RU2009111113A (ru
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Метвин ИСААК (CA)
Метвин Исаак
Абдельмалик СЛАССИ (CA)
Абдельмалик Сласси
Луиза ЭДВАРДС (CA)
Луиза Эдвардс
Питер ДАВ (CA)
Питер Дав
Тао КСИН (CA)
Тао Ксин
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Томислав Стефанак
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Астразенека Аб
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Abstract

Описываются новые соединения общей формулы I: ! , ! (где значения R1-R5, X и Z определены в описании изобретения) фармацевтическая композиция, их содержащая, и применение данных соединений в качестве модуляторов MGLUR5 для ингибирования транзиторных релаксаций нижнего пищеводного сфинктера или для лечения или предупреждения гастроэзофагеальной рефлюксной болезни. ! 3 н. и 11 з.п. ф-лы.

Description

Текст описания приведен в факсимильном виде.
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Claims (14)

1. Соединение формулы (I)
Figure 00000078
,
где R1 выбран из группы, состоящей из метила, галогена и циано;
R2 выбран из группы, состоящей из водорода и фторо;
R3 представляет собой метил;
R4 выбран из группы, состоящей из водорода и С1-С3алкила;
R5 представляет собой метил;
Х выбран из группы, состоящей из:
Figure 00000079
;
Figure 00000080
или
Figure 00000081
;
и Z выбран из группы, состоящей из:
Figure 00000082
и
Figure 00000083

где R6 выбран из группы, состоящей из водорода, C1-С3алкила, C1-С3галогеноалкила, C1-С3алкокси, C1-С3галогеноалкокси и галогена;
R7 выбран из группы, состоящей из водорода, C1-С3алкила, C1-С3галогеноалкила, C1-С3алкокси, C1-С3галогеноалкокси и галогена;
или его фармацевтически приемлемые соль, гидрат, таутомер или энантиомер.
2. Соединение по п.1, где R1 выбран из метила и хлоро;
R2 представляет собой водород;
R3 представляет собой метил;
R4 представляет собой водород; и
R5 представляет собой метил.
3. Соединение по п.1, где R6 выбран из группы, состоящей из водорода и C1-С3алкила; и
R7 выбран из группы, состоящей из водорода и C1-С3алкила.
4. Соединение по п.1, где R6 представляет собой водород или метил; и R7 представляет собой водород.
5. Соединение по любому из пп.1-4, где R6 представляет собой водород, и R7 представляет собой водород.
6. Соединение по любому из пп.1-4, где R6 представляет собой метил, и R7 представляет собой водород.
7. Соединение по п.1, выбранное из группы, состоящей из:
4-(5-{(1R)-1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)-1-метилпиридин-2(1Н)-она,
4-(5-{(1R)-1-[5-(3-хлорфенил)-1,2,4-оксадиазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)-1-метилпиридин-2(1Н)-она,
4-(5-{1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридин-2(1Н)-она,
4-(5-{[5-(3-хлорфенил)изоксазол-3-ил]метокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридин-2(1Н)-она,
4-(5-{(1R)-1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридин-2(1Н)-она,
4-(5-{(1R)-1-[5-(3-хлорфенил)-1,2,4-оксадиазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридин-2(1Н)-она,
4-(5-{(1R)-1-[2-(3-хлорфенил)-2Н-тетразол-5-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридин-2(1Н)-она,
5-(5-{(1R)-1-[2-(3-хлорфенил)-2Н-тетразол-5-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она,
5-(5-{(1R)-1-[5-(3-хлорфенил)-1,2,4-оксадиазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она,
5-(5-{(1R)-1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она,
5-(4-метил-5-{(1R)-1-[2-(3-метилфенил)-2Н-тетразол-5-ил]этокси}-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она и
5-(4-метил-5-{(1R)-1-[5-(3-метилфенил)изоксазол-3-ил]этокси}-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она.
8. Соединение по п.1, выбранное из группы, состоящей из:
5-(5-{(1R)-1-[2-(3-хлорфенил)-2Н-тетразол-5-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она,
5-(4-метил-5-{(1R)-1-[2-(3-метилфенил)-2Н-тетразол-5-ил]этокси}-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она и
5-(5-{(1R)-1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-она.
9. Соединение по п.1, представляющее собой 5-(5-{(1R)-1-[2-(3-хлорфенил)-2Н-тетразол-5-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-он или его фармацевтически приемлемые соль, гидрат, таутомер или энантиомер.
10. Соединение по п.1, представляющее собой 5-(4-метил-5-{(1R)-1-[2-(3-метилфенил)-2Н-тетразол-5-ил]этокси}-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-он или его фармацевтически приемлемые соль, гидрат, таутомер или энантиомер.
11. Соединение по п.1, представляющее собой 5-(5-{(1R)-1-[5-(3-хлорфенил)изоксазол-3-ил]этокси}-4-метил-4Н-1,2,4-триазол-3-ил)пиридазин-3(2Н)-он или его фармацевтически приемлемые соль, гидрат, таутомер или энантиомер.
12. Соединение по любому из пп.1-4, обладающее активностью модулятора метаботропных глутаматных рецепторов.
13. Фармацевтическая композиция, обладающая активностью модулятора метаботропных глутаматных рецепторов, содержащая соединение по любому из пп.1-4 в качестве активного ингредиента вместе с фармакологически и фармацевтически приемлемым носителем.
14. Применение соединения по любому из пп.1-4 или его фармацевтически приемлемой соли или оптического изомера для изготовления лекарственного средства для ингибирования транзиторных релаксаций нижнего пищеводного сфинктера или для лечения или предупреждения гастроэзофагеальной рефлюксной болезни.
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