RU2008122779A - Соединения для ингибирования фермента - Google Patents
Соединения для ингибирования фермента Download PDFInfo
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- RU2008122779A RU2008122779A RU2008122779/04A RU2008122779A RU2008122779A RU 2008122779 A RU2008122779 A RU 2008122779A RU 2008122779/04 A RU2008122779/04 A RU 2008122779/04A RU 2008122779 A RU2008122779 A RU 2008122779A RU 2008122779 A RU2008122779 A RU 2008122779A
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- 0 CC(C)CC(C(C1(C)OC1)=O)NC([C@](COC)NC(C(COC)NC(c1n[o]*(C)c1)=O)=O)=O Chemical compound CC(C)CC(C(C1(C)OC1)=O)NC([C@](COC)NC(C(COC)NC(c1n[o]*(C)c1)=O)=O)=O 0.000 description 2
- LGAOYYYWTTXCEX-OJVMJSSBSA-N CC(C)CC(C(C1(C)OC1)=O)NC([C@H](C)NC(C(COC)NC(c1n[o]c(C)c1)=O)=O)=O Chemical compound CC(C)CC(C(C1(C)OC1)=O)NC([C@H](C)NC(C(COC)NC(c1n[o]c(C)c1)=O)=O)=O LGAOYYYWTTXCEX-OJVMJSSBSA-N 0.000 description 1
- OMFJGXMPSYXWCE-BFGVMEHQSA-N CC(C)CC(C(C1(C)OC1)=O)NC([C@H](Cc1c[s]cn1)NC(C(COC)NC(c1n[o]c(C)c1)=O)=O)=O Chemical compound CC(C)CC(C(C1(C)OC1)=O)NC([C@H](Cc1c[s]cn1)NC(C(COC)NC(c1n[o]c(C)c1)=O)=O)=O OMFJGXMPSYXWCE-BFGVMEHQSA-N 0.000 description 1
- WHBBNXVJTBOKBT-DREYXHSYSA-N CC(C)CC(C([C@]1(C)OC1)=O)NC(C(Cc1ccccc1)NC(C(COC)NC(c1ccn[o]1)=O)=O)=O Chemical compound CC(C)CC(C([C@]1(C)OC1)=O)NC(C(Cc1ccccc1)NC(C(COC)NC(c1ccn[o]1)=O)=O)=O WHBBNXVJTBOKBT-DREYXHSYSA-N 0.000 description 1
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Abstract
1. Соединение, имеющее структуру формулы (I) или его фармацевтически приемлемая соль ! ! в которой L выбран из С=О, C=S и SO2; ! Х выбран из О, S, NH и N-C1-6-алкила; ! Z отсутствует или представляет собой С1-6-алкил или С1-6-алкоксигруппу; ! каждый из R1, R2 и R3 независимо друг от друга выбран из водорода, С1-6-алкила, ! С1-6-алкенила, С1-6-алкинила, С1-6-гидроксиалкила, С1-6-алкоксиалкила, арила, С1-6-аралкила, гетероарила, гетероциклила, С1-6-гетероциклоалкила, С1-6-гетероаралкила, карбоциклила и С1-6-карбоциклоалкила; ! R4 выбран из водорода, С1-6-аралкила и С1-6-алкила; ! R5 представляет собой гетероарил и ! R6 и R7 независимо друг от друга выбраны из водорода, С1-6-алкила и С1-6-аралкила. ! 2. Соединение по п.1, в котором Z отсутствует. ! 3. Соединение по п.1, в котором R4, R6 и R7 независимо друг от друга выбраны из водорода и метила. ! 4. Соединение по п.1, в котором L представляет собой С=О. ! 5. Соединение по п.1, в котором L представляет собой SO2. ! 6. Соединение по п.1, в котором R1, R2 и R3 независимо друг от друга выбраны из водорода, С1-6-алкила, С1-6-алкенила, С1-6-алкинила, С1-6-гидроксиалкила, С1-6-алкоксиалкила, С1-6-аралкила, С1-6-гетероциклоалкила, С1-6-гетероаралкила и С1-6-карбоциклоалкила. ! 7. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-алкил. ! 8. Соединение по п.7, в котором любой из R1, R2 и R3 независимо друг от друга выбран из метила, этила, пропила, изопропила, бутила, втор-бутила и изобутила. ! 9. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой пропаргил. ! 10. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-гидроксиалкил. ! 11. Соединение по п.10, в котором любой из R1, R2 и R3 неза�
Claims (52)
1. Соединение, имеющее структуру формулы (I) или его фармацевтически приемлемая соль
в которой L выбран из С=О, C=S и SO2;
Х выбран из О, S, NH и N-C1-6-алкила;
Z отсутствует или представляет собой С1-6-алкил или С1-6-алкоксигруппу;
каждый из R1, R2 и R3 независимо друг от друга выбран из водорода, С1-6-алкила,
С1-6-алкенила, С1-6-алкинила, С1-6-гидроксиалкила, С1-6-алкоксиалкила, арила, С1-6-аралкила, гетероарила, гетероциклила, С1-6-гетероциклоалкила, С1-6-гетероаралкила, карбоциклила и С1-6-карбоциклоалкила;
R4 выбран из водорода, С1-6-аралкила и С1-6-алкила;
R5 представляет собой гетероарил и
R6 и R7 независимо друг от друга выбраны из водорода, С1-6-алкила и С1-6-аралкила.
2. Соединение по п.1, в котором Z отсутствует.
3. Соединение по п.1, в котором R4, R6 и R7 независимо друг от друга выбраны из водорода и метила.
4. Соединение по п.1, в котором L представляет собой С=О.
5. Соединение по п.1, в котором L представляет собой SO2.
6. Соединение по п.1, в котором R1, R2 и R3 независимо друг от друга выбраны из водорода, С1-6-алкила, С1-6-алкенила, С1-6-алкинила, С1-6-гидроксиалкила, С1-6-алкоксиалкила, С1-6-аралкила, С1-6-гетероциклоалкила, С1-6-гетероаралкила и С1-6-карбоциклоалкила.
7. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-алкил.
8. Соединение по п.7, в котором любой из R1, R2 и R3 независимо друг от друга выбран из метила, этила, пропила, изопропила, бутила, втор-бутила и изобутила.
9. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой пропаргил.
10. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-гидроксиалкил.
11. Соединение по п.10, в котором любой из R1, R2 и R3 независимо друг от друга выбран из гидроксиметила и гидроксиэтила.
12. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-алкоксиалкил.
13. Соединение по п.12, в котором любой из R1, R2 и R3 независимо друг от друга выбран из метоксиметила и метоксиэтила.
14. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой С1-6-гетероаралкил.
15. Соединение по п.14, в котором любой из R1, R2 и R3 независимо друг от друга выбран из имидазолилметила, пиразолилметила и тиазолилметила и пиридилметила.
16. Соединение по п.6, в котором любой из R1, R2 и R3 независимо друг от друга представляет собой циклогексилметил.
17. Соединение по п.1, в котором все R1, R2 и R3 различны.
18. Соединение по п.1, в котором по меньшей мере один из R1 и R2 выбран из С1-6-гидроксиалкила и С1-6-алкоксиалкила.
19. Соединение по п.18, в котором по меньшей мере один из R1 и R2 представляет собой С1-6-алкоксиалкил.
20. Соединение по п.19, в котором по меньшей мере один из R1 и R2 выбран из метоксиметила и метоксиэтила.
21. Соединение по п.1 или 18, в котором R3 выбран из С1-6-алкила и С1-6-аралкила.
22. Соединение по п.21, в котором R3 представляет собой С1-6алкил.
23. Соединение по п.22, в котором R3 выбран из метила, этила, изопропила, втор-бутила и изобутила.
24. Соединение по п.23, в котором R3 представляет собой изобутил.
25. Соединение по п.21, в котором R3 представляет собой С1-6-аралкил.
26. Соединение по п.25, в котором R3 представляет собой фенилметил.
27. Соединение по п.1, в котором R5 представляет собой 5- или 6-членный гетероарил.
28. Соединение по п.27, в котором R5 выбран из изоксазола, изотиазола, фурана, тиофена, оксазола, тиазола, пиразола или имидазола.
29. Соединение по п.28, в котором R5 выбран из изоксазола, фурана или тиофена.
30. Соединение по п.29, в котором R5 представляет собой фуран или тиофен.
31. Соединение по п.30, в котором R5 представляет собой незамещенный фуран-3-ил или тиен-2-ил.
32. Соединение по п.29, в котором R5 представляет собой изоксазол-3-ил или изоксазол-5-ил.
33. Соединение по п.32, в котором R5 представляет собой изоксазол-3-ил, содержащий заместитель в 5-положении.
34. Соединение по п.32, в котором R5 представляет собой изоксазол-5-ил, содержащий заместитель в 3-положении.
35. Соединение по п.33 или 34, в котором заместитель выбран из С1-6-алкила, С1-6-алкоксигруппы, С1-6-алкоксиалкила, С1-6-гидроксиалкила, остатка карбоновой кислоты, аминокарбоксилата, С1-6-алкиламинокарбоксилата, (С1-6-алкил)2аминокарбоксилата, С1-6-алкилкарбоксилата, С1-6-гетероаралкила, С1-6-аралкила, С1-6-гетероциклоалкила и С1-6-карбоциклоалкила.
36. Соединение по п.35, в котором заместитель выбран из метила, этила, изопропила и циклопропилметила.
37. Соединение по п.35, в котором заместитель выбран из С1-6-гетероаралкила и
С1-6-гетероциклоалкила.
38. Соединение по п.37, в котором заместитель представляет собой 1,2,4-триазол-5-илметил.
39. Соединение по п.37, в котором заместитель представляет собой азетидин-1-илметил.
41. Соединение по п.40, в котором W представляет собой О.
42. Соединение по п.37, в котором заместитель выбран из С1-6-алкоксигруппы и С1-6-алкоксиалкила.
43. Соединение по п.42, в котором заместитель выбран из метоксигруппы, этоксигруппы, метоксиметила и метоксиэтила.
44. Соединение по п.37, в котором заместитель выбран из карбоновой кислоты, аминокарбоксилата, С1-6-алкиламинокарбоксилата, (С1-6-алкил)2-аминокарбоксилата или С1-6-алкилкарбоксилата.
45. Соединение по п.44, в котором заместитель представляет собой метилкарбоксилат.
47. Фармацевтическая композиция, содержащая соединение по любому из пп.1-46 и фармацевтически приемлемый разбавитель или носитель.
48. Фармацевтическая композиция по п.47, которая биодоступна перорально.
49. Способ лечения воспаления, нейродегенеративного заболевания, мышечной дистрофии, рака, хронических инфекционных заболеваний, гиперпролиферативного состояния, атрофии мышц и иммунно-зависимых состояний, предусматривающий введение терапевтически эффективного количества фармацевтической композиции по п.48.
50. Способ ингибирования или уменьшения ВИЧ-инфекции, предусматривающий введение терапевтически эффективного количества фармацевтической композиции по п.48.
51. Способ воздействия на уровень экспрессии генов вируса у субъекта, предусматривающий введение терапевтически эффективного количества фармацевтической композиции по п.48.
52. Способ изменения варьирования антигенных пептидов, продуцированных протеасомой в организме, предусматривающий введение терапевтически эффективного количества фармацевтической композиции по п.48.
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Publication number | Priority date | Publication date | Assignee | Title |
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RU2450016C2 (ru) * | 2006-06-19 | 2012-05-10 | Протеоликс, Инк. | Пептидные эпоксикетоны для ингибирования протеасомы |
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