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RU2011106374A - Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1 - Google Patents

Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1 Download PDF

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RU2011106374A
RU2011106374A RU2011106374/04A RU2011106374A RU2011106374A RU 2011106374 A RU2011106374 A RU 2011106374A RU 2011106374/04 A RU2011106374/04 A RU 2011106374/04A RU 2011106374 A RU2011106374 A RU 2011106374A RU 2011106374 A RU2011106374 A RU 2011106374A
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pharmaceutically acceptable
formula
compound
acceptable salt
methyl
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RU2539979C2 (ru
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Франк ХИММЕЛЬСБАХ (DE)
Франк Химмельсбах
Дэвид А. КЛЕРМОН (US)
Дэвид А. КЛЕРМОН
Линхан ЧЖУАН (US)
Линхан Чжуан
Катерина ЛЕФТЕРИС (US)
Катерина Лефтерис
Чжэньрон СЮЙ (US)
Чжэньрон СЮЙ
Колин М. ТАЙС (US)
Колин М. ТАЙС
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Берингер Ингельхайм Интернэшнл Гмбх (De)
Берингер Ингельхайм Интернэшнл Гмбх
Вайтаи Фармасьютиклз, Инк. (Us)
Вайтаи Фармасьютиклз, Инк.
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Priority claimed from PCT/US2008/009017 external-priority patent/WO2009017664A1/en
Priority claimed from PCT/US2009/002653 external-priority patent/WO2009134400A1/en
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Abstract

Соединение формулы (Ip3): ! ; ! или его фармацевтически приемлемая соль; ! где G1 представляет собой (C1-C4)алкил, (C1-C4)алкокси, (C1-C4)галогеналкил, (C1-С4)галогеналкокси, галоген, циано или нитро; ! n равен 0, 1 или 2; ! G2a представляет собой (С3-С4)циклоалкил_или (С3-С4)циклоалкил(С1-С2)алкил; ! G2b представляет собой водород, метил или этил; ! R1 представляет собой метил или этил; ! R2 представляет собой фенил или фторфенил; и ! R3 представляет собой 2-гидрокси-2-метилпропил или 2-метил-2-цианопропил. ! 2. Соединение по п.1, в котором n=0. ! 3. Соединение по п.1, имеющее формулу: ! ! или его фармацевтически приемлемая соль. ! 4. Соединение по п.1, имеющее формулу: ! ; ! или его фармацевтически приемлемая соль. ! 5. Соединение по п.1, имеющее формулу: ! ; ! или его фармацевтически приемлемая соль. ! 6. Фармацевтическая композиция, включающая: i) фармацевтически приемлемый носитель или разбавитель; и ii) соединение формулы: ! ; ! или его фармацевтически приемлемую соль, где: ! G1 представляет собой (C1-C4)алкил, (С1-С4)алкокси, (C1-C4)галогеналкил, (C1-С4)галогеналкокси, галоген, циано или нитро; ! n равен 0, 1 или 2; ! G2a представляет собой (С3-С4)циклоалкил или (С3-С4)циклоалкил(С1-С2)алкил; ! G2b представляет собой водород, метил или этил; ! R1 представляет собой метил или этил; ! R2 представляет собой фенил или фторфенил; и ! R3 представляет собой 2-гидрокси-2-метилпропил или 2-циано-2-метилпропил. ! 7. Фармацевтическая композиция по п.6, в которой n равен 0. ! 8. Фармацевтическая композиция по п.6, в которой соединение имеет формулу: !! или представляет собой его фармацевтически приемлемую соль. ! 9. Фармацевтическая композиция по п.6, в которой соединение имеет формулу: ! ; ! или представляет собой �

Claims (1)

  1. Соединение формулы (Ip3):
    Figure 00000001
    ;
    или его фармацевтически приемлемая соль;
    где G1 представляет собой (C1-C4)алкил, (C1-C4)алкокси, (C1-C4)галогеналкил, (C1-С4)галогеналкокси, галоген, циано или нитро;
    n равен 0, 1 или 2;
    G2a представляет собой (С3-С4)циклоалкил_или (С3-С4)циклоалкил(С1-С2)алкил;
    G2b представляет собой водород, метил или этил;
    R1 представляет собой метил или этил;
    R2 представляет собой фенил или фторфенил; и
    R3 представляет собой 2-гидрокси-2-метилпропил или 2-метил-2-цианопропил.
    2. Соединение по п.1, в котором n=0.
    3. Соединение по п.1, имеющее формулу:
    Figure 00000002
    или его фармацевтически приемлемая соль.
    4. Соединение по п.1, имеющее формулу:
    Figure 00000003
    ;
    или его фармацевтически приемлемая соль.
    5. Соединение по п.1, имеющее формулу:
    Figure 00000004
    ;
    или его фармацевтически приемлемая соль.
    6. Фармацевтическая композиция, включающая: i) фармацевтически приемлемый носитель или разбавитель; и ii) соединение формулы:
    Figure 00000005
    ;
    или его фармацевтически приемлемую соль, где:
    G1 представляет собой (C1-C4)алкил, (С1-С4)алкокси, (C1-C4)галогеналкил, (C1-С4)галогеналкокси, галоген, циано или нитро;
    n равен 0, 1 или 2;
    G2a представляет собой (С3-С4)циклоалкил или (С3-С4)циклоалкил(С1-С2)алкил;
    G2b представляет собой водород, метил или этил;
    R1 представляет собой метил или этил;
    R2 представляет собой фенил или фторфенил; и
    R3 представляет собой 2-гидрокси-2-метилпропил или 2-циано-2-метилпропил.
    7. Фармацевтическая композиция по п.6, в которой n равен 0.
    8. Фармацевтическая композиция по п.6, в которой соединение имеет формулу:
    Figure 00000002
    или представляет собой его фармацевтически приемлемую соль.
    9. Фармацевтическая композиция по п.6, в которой соединение имеет формулу:
    Figure 00000003
    ;
    или представляет собой его фармацевтически приемлемую соль.
    10. Фармацевтическая композиция по п.6, в которой соединение имеет формулу:
    Figure 00000004
    ;
    или представляет собой его фармацевтически приемлемую соль.
    11. Способ лечения человека с заболеванием, связанным с активностью или экспрессией 11β-HSD1, включающий стадию введения человеку эффективного количества соединения формулы:
    Figure 00000005
    ;
    или его фармацевтически приемлемой соли, где:
    G1 представляет собой (C1-C4)алкил, (С1-С4)алкокси, (C1-C4)галогеналкил, (С1-С4)галогеналкокси, галоген, циано или нитро;
    n равен 0, 1 или 2;
    G2a представляет собой (С3-С4)циклоалкил или (С3-С4)циклоалкил(С1-С2)алкил;
    C2b представляет водород, метил или этил;
    R1 представляет метил или этил;
    R2 представляет фенил или фторфенил; и
    R3 представляет 2-гидрокси-2-метилпропил или 2-метил-2-цианопропил.
    12. Способ по п.11, при котором n равен 0.
    13. Способ по п.11, при котором соединение имеет формулу:
    Figure 00000002
    или представляет собой его фармацевтически приемлемую соль.
    14. Способ по п.11, при котором соединение имеет формулу:
    Figure 00000003
    ;
    или представляет собой его фармацевтически приемлемую соль.
    15. Способ по п.11, при котором соединение имеет формулу:
    Figure 00000004
    ;
    или представляет собой его фармацевтически приемлемую соль.
    16. Способ по п.11, при котором заболевание представляет собой диабет.
    17. Способ ингибирования активности 11β-HSD1, включающий стадию введения человеку, нуждающемуся в таком лечении, эффективного количества соединения формулы:
    Figure 00000005
    ;
    или его фармацевтически приемлемой соли, где:
    G1 представляет собой (C1-C4)алкил, (C1-C4)алкокси, (C1-C4)галогеналкил, (C1-С4)галогеналкокси, галоген, циано или нитро;
    n равен 0, 1 или 2;
    G2a представляет собой (С3-С4)циклоалкил или (С3-С4)циклоалкил(С1-С2)алкил;
    G2b представляет собой водород, метил или этил;
    R1 представляет собой метил или этил;
    R2 представляет собой фенил или фторфенил; и
    R3 представляет собой 2-гидрокси-2-метилпропил или 2-метил-2-цианопропил.
    Способ по п.17, при котором n равен 0.
    Способ по п.17, при котором соединение имеет формулу:
    Figure 00000002
    или представляет собой его фармацевтически приемлемую соль.
    20. Способ по п.17, при котором соединение имеет формулу:
    Figure 00000003
    ;
    или представляет собой его фармацевтически приемлемую соль.
    21. Способ по п.17, при котором соединение имеет формулу:
    Figure 00000004
    ;
    или представляет собой его фармацевтически приемлемую соль.
    22. Способ по п.17, при котором человек нуждается в лечении диабета.
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