RU2017135950A - Композиции для лечения фиброза и связанных с фиброзом состояний - Google Patents

Композиции для лечения фиброза и связанных с фиброзом состояний

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RU2017135950A
RU2017135950A RU2017135950A RU2017135950A RU2017135950A RU 2017135950 A RU2017135950 A RU 2017135950A RU 2017135950 A RU2017135950 A RU 2017135950A RU 2017135950 A RU2017135950 A RU 2017135950A RU 2017135950 A RU2017135950 A RU 2017135950A
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fibrosis
optionally substituted
compound according
subject
alkyl
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RU2017135950A
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RU2017135950A3 (ru
RU2712140C2 (ru
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Карен Аннетт ДАГГЭН
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Вектус Байосистемс Лимитед
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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Claims (43)

1. Соединение формулы:
Figure 00000001
или
Figure 00000002
где
А выбран из необязательно замещенного насыщенного, частично насыщенного или ненасыщенного 5- или 6-членного гетероциклила; необязательно замещенного C1-6алкоксиламина; необязательно замещенного C1-6алкиламина; необязательно замещенной С0-6алкил-карбоновой кислоты; необязательно замещенного C1-6алкилгидроксила; необязательно замещенного насыщенного или ненасыщенного C0-6алкил-бициклического-гетероциклила и необязательно замещенного насыщенного или ненасыщенного C1-6алкоксил-бициклического-гетероциклила, или его фармакологически приемлемая соль, стереоизомер, диастереомер, энантиомер, рацемат, гидрат и/или сольват.
2. Соединение по п. 1, где насыщенный, частично насыщенный или ненасыщенный 5- или 6-членный гетероциклил содержит один или несколько атомов N, S или О, необязательно замещенных одним или несколькими заместителями, представляющими собой оксо, C1-6алкил, амино, гидроксил или галоген.
3. Соединение по п. 1, где насыщенный, частично насыщенный или ненасыщенный 5- или 6-членный гетероциклил выбран из пирролила, пиразолила, имидазолила, триазолила, имидазолидинила, пирролидинила, пирролидинилидена, дигидропирролила, изоксазолил-дигидрооксазолила, изоксазолидинила, оксазолидинила и оксазолила, необязательно замещенных одним или несколькими заместителями, представляющими собой оксо, C1-6алкил, амино, гидроксил или галоген.
4. Соединение по п. 1, где C1-6алкоксиламин представляет собой аминооксиметил.
5. Соединение по п. 1, где C1-6алкиламин необязательно замещен одним или несколькими из C1-6алкила, C1-6галогеналкила, гидроксила или галогена, предпочтительно моно-, ди- или тризамещенного галогеналкила, наиболее предпочтительно трифторметана.
6. Соединение по п. 1, где С0-6алкил-карбоновая кислота представляет собой карбоновую кислоту.
7. Соединение по п. 1, где C1-6алкилгидроксил представляет собой метилгидроксил.
8. Соединение по п. 1, где C0-6алкил-бициклический-гетероциклил выбран из индолила, изоиндолила, индолинила и изоиндолинила, необязательно замещенных одним или несколькими оксо, предпочтительно диоксо.
9. Соединение по п. 1, где C1-6алкоксил-бициклический-гетероциклил выбран из индолила, изоиндолила, индолинила и изоиндолинила, необязательно замещенных одним или несколькими оксо, и где C1-6алкоксил представляет собой метокси или этокси.
10. Соединение по п. 1, где А выбран из:
Figure 00000003
Figure 00000004
Figure 00000005
и
Figure 00000006
11. Соединение по любому из пп. 1-10, где соединение выбрано из группы, состоящей из:
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
и
Figure 00000012
или его фармакологически приемлемая соль, стереоизомер, диастереомер, энантиомер, рацемат, гидрат и/или сольват.
12. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-11 и фармацевтически приемлемое вспомогательное вещество.
13. Способ профилактического или терапевтического лечения фиброза у субъекта, включающий введение субъекту соединения по любому из пп. 1-11 или фармацевтической композиции по п. 12.
14. Способ по п. 13, где лечение предотвращает, ослабляет или замедляет прогрессирование фиброза.
15. Способ по п. 13, где лечение уменьшает развившийся фиброз.
16. Способ по п. 13, где лечение восстанавливает нормальную структуру ткани.
17. Способ по любому из пп. 13-15, где фиброз представляет собой фиброз миокарда, фиброз почек и/или фиброз печени.
18. Применение соединения по любому из пп. 1-11 для изготовления лекарственного препарата для лечения фиброза.
19. Применение по п. 18, где лекарственный препарат предотвращает, ослабляет или замедляет прогрессирование фиброза.
20. Применение по п. 18, где лекарственный препарат уменьшает развившийся фиброз.
21. Применение по п. 18, где лекарственный препарат восстанавливает нормальную структуру ткани.
22. Применение по любому из пп. 18-20, где фиброз представляет собой фиброз миокарда, фиброз почек и/или фиброз печени.
23. Способ предотвращения, снижения степени или замедления накопления жира в печени субъекта, включающий введение субъекту соединения по любому из пп. 1-11 или фармацевтической композиции по п. 12.
24. Способ предотвращения, снижения степени или замедления отмирания клеток почечных канальцев у субъекта, включающий введение субъекту соединения по любому из пп. 1-11 или фармацевтической композиции по п. 12.
25. Способ восстановления нормальной структуры ткани у субъекта, включающий введение субъекту соединения по любому из пп. 1-11 или фармацевтической композиции по п. 12.
26. Применение соединения по любому из пп. 1-11 для изготовления лекарственного препарата для предотвращения, снижения степени или замедления накопления жира в печени.
27. Применение соединения по любому из пп. 1-11 для изготовления лекарственного препарата для предотвращения, снижения степени или замедления отмирания клеток почечных канальцев.
28. Применение соединения по любому из пп. 1-11 для изготовления лекарственного препарата для восстановления нормальной структуры ткани.
29. Соединение формулы:
Figure 00000013
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