RU2005138049A - Новые биоизостеры актинонина - Google Patents

Новые биоизостеры актинонина Download PDF

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RU2005138049A
RU2005138049A RU2005138049/04A RU2005138049A RU2005138049A RU 2005138049 A RU2005138049 A RU 2005138049A RU 2005138049/04 A RU2005138049/04 A RU 2005138049/04A RU 2005138049 A RU2005138049 A RU 2005138049A RU 2005138049 A RU2005138049 A RU 2005138049A
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hydrogen atom
heteroalkyl
heterocycloalkyl
cycloalkyl
heteroalkylcycloalkyl
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RU2005138049/04A
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RU2379284C2 (ru
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Михаэль ТОРМАНН (DE)
Михаэль Торманн
Михаэль АЛЬМШТЕТТЕР (DE)
Михаэль Альмштеттер
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Новартис АГ (CH)
Новартис Аг
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Claims (11)

1. Соединения формулы (I)
Figure 00000001
в которой R1 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток,
R2 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток,
R3 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток,
R4 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток,
R5 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток,
R6 представляет собой атом водорода, алкильный, алкенильный, алкинильный, гетероалкильный, арильный, гетероарильный, циклоалкильный, алкилциклоалкильный, гетероалкилциклоалкильный, гетероциклоалкильный, аралкильный или гетероаралкильный остаток или два из остатков R1, R2, R3, R4 и R6 совместно являются фрагментом необязательно замещенного циклоалкильного либо гетероциклоалкильного кольца и
n обозначает 1, 2 или 3,
или фармацевтически приемлемая соль, сольват, гидрат или фармацевтически приемлемая композиция указанных соединений.
2. Соединения по п.1, в которых R1 представляет собой атом водорода.
3. Соединения по п.2, в которых R2 представляет собой атом водорода.
4. Соединения по п.1, в которых n обозначает 1.
5. Соединения по п.1, в которых R3 представляет собой атом водорода.
6. Соединения по п.6, в которых R6 представляет собой атом водорода.
7. Фармацевтическая композиция, содержащая соединение по одному из пп.1-6 и необязательно носители и/или вспомогательные вещества.
8. Применение соединения или фармацевтической композиции по одному из пп.1-8 для ингибирования металлопротеиназ.
9. Применение соединения или фармацевтической композиции по одному из пп.1-8 для ингибирования пептид-деформилазы (PDF).
10. Применение соединения или фармацевтической композиции по одному из пп.1-8 для лечения и/или предупреждения заболеваний, опосредуемых активностью металлопротеиназ.
11. Применение соединения или фармацевтической композиции по одному из пп.1-8 для лечения и/или предупреждения заболеваний, опосредуемых активностью пептид-деформилазы (PDF).
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