RU2009101319A - Пептидные эпоксикетоны для ингибирования протеасомы - Google Patents
Пептидные эпоксикетоны для ингибирования протеасомы Download PDFInfo
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- RU2009101319A RU2009101319A RU2009101319/04A RU2009101319A RU2009101319A RU 2009101319 A RU2009101319 A RU 2009101319A RU 2009101319/04 A RU2009101319/04 A RU 2009101319/04A RU 2009101319 A RU2009101319 A RU 2009101319A RU 2009101319 A RU2009101319 A RU 2009101319A
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- alkyl
- compound according
- compound
- hydrogen
- zaz
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Abstract
1. Соединение, имеющее структуру формулы (I), или его фармацевтически приемлемая соль, ! ! где каждый Ar независимо представляет собой ароматическую или гетероароматическую группу, необязательно замещенную 1-4 заместителями; ! каждый А независимо выбран из С=О, C=S и SO2; или ! А необязательно представляет собой ковалентную связь, когда является смежным по отношению к присутствующему Z; ! В отсутствует или представляет собой N(R9)R10; ! L отсутствует или выбран из С=О, C=S и SO2; ! М отсутствует или представляет собой С1-12алкил; ! Q отсутствует или выбран из О, NH и N-С1-6алкила; ! Х выбран из О, S, NH и N-С1-6алкила; ! Y отсутствует или выбран из С=О и SO2; ! каждый Z независимо выбран из О, S, NH и N-С1-6алкила; или ! Z необязательно представляет собой ковалентную связь, когда является смежным по отношению к присутствующему А; ! R1 выбран из Н, -С1-6алкил-В, С1-6гидроксиалкила, С1-6алкоксиалкила, арила и С1-6арилалкила; ! R2 и R3, каждый независимо, выбран из арила, С1-6арилалкила, гетероарила и С1-6гетероарилалкила; ! R4 представляет собой N(R5)L-Q-R6; ! R5 выбран из водорода, ОН, С1-6арилалкила и С1-6алкила; ! R6 выбран из водорода, С1-6алкила, С2-6алкенила, С2-6алкинила, Ar-Y-, карбоциклила, гетероциклила, N-концевой защитной группы, арила, С1-6арилалкила, гетероарила, С1-6гетероарилалкила, R11ZAZ-C1-8алкила-, R14Z-C1-8алкила-, (R11O)(R12O)P(=O)O-C1-8алкил-ZAZ-С1-8алкила-, R11ZAZ-C1-8алкил-ZAZ-C1-8алкила-, гетероциклилМZAZ-C1-8алкила-, (R11O)(R12O)P(=O)O-C1-8алкила-, (R13)2N-C1-12алкила-, (R13)3N+-C1-12алкила-, гетероциклилМ-, карбоциклилМ-, R14SO2C1-8алкила- и R14SO2NH, или ! R5 и R6, вместе представляют собой С1-6алкил-Y-С1-6алкил, С1-6алкил-ZAZ-С1-6алкил, ZAZ-C1-6алкил-ZAZ-С1-6алкил, ZAZ-С1-6алкил-ZAZ или С1-6алкил-А, тем самым образуя кольцо; ! R7 и R8 независимо выбраны из водорода
Claims (38)
1. Соединение, имеющее структуру формулы (I), или его фармацевтически приемлемая соль,
где каждый Ar независимо представляет собой ароматическую или гетероароматическую группу, необязательно замещенную 1-4 заместителями;
каждый А независимо выбран из С=О, C=S и SO2; или
А необязательно представляет собой ковалентную связь, когда является смежным по отношению к присутствующему Z;
В отсутствует или представляет собой N(R9)R10;
L отсутствует или выбран из С=О, C=S и SO2;
М отсутствует или представляет собой С1-12алкил;
Q отсутствует или выбран из О, NH и N-С1-6алкила;
Х выбран из О, S, NH и N-С1-6алкила;
Y отсутствует или выбран из С=О и SO2;
каждый Z независимо выбран из О, S, NH и N-С1-6алкила; или
Z необязательно представляет собой ковалентную связь, когда является смежным по отношению к присутствующему А;
R1 выбран из Н, -С1-6алкил-В, С1-6гидроксиалкила, С1-6алкоксиалкила, арила и С1-6арилалкила;
R2 и R3, каждый независимо, выбран из арила, С1-6арилалкила, гетероарила и С1-6гетероарилалкила;
R4 представляет собой N(R5)L-Q-R6;
R5 выбран из водорода, ОН, С1-6арилалкила и С1-6алкила;
R6 выбран из водорода, С1-6алкила, С2-6алкенила, С2-6алкинила, Ar-Y-, карбоциклила, гетероциклила, N-концевой защитной группы, арила, С1-6арилалкила, гетероарила, С1-6гетероарилалкила, R11ZAZ-C1-8алкила-, R14Z-C1-8алкила-, (R11O)(R12O)P(=O)O-C1-8алкил-ZAZ-С1-8алкила-, R11ZAZ-C1-8алкил-ZAZ-C1-8алкила-, гетероциклилМZAZ-C1-8алкила-, (R11O)(R12O)P(=O)O-C1-8алкила-, (R13)2N-C1-12алкила-, (R13)3N+-C1-12алкила-, гетероциклилМ-, карбоциклилМ-, R14SO2C1-8алкила- и R14SO2NH, или
R5 и R6, вместе представляют собой С1-6алкил-Y-С1-6алкил, С1-6алкил-ZAZ-С1-6алкил, ZAZ-C1-6алкил-ZAZ-С1-6алкил, ZAZ-С1-6алкил-ZAZ или С1-6алкил-А, тем самым образуя кольцо;
R7 и R8 независимо выбраны из водорода, С1-6алкила и С1-6арилалкила;
R9 выбран из водорода, ОН и С1-6алкила; и
R10 представляет собой N-концевую защитную группу;
R11 и R12 независимо выбраны из водорода, катиона металла, С1-6алкила, С2-6алкенила, С2-6алкинила, арила, гетероарила, С1-6арилалкила и С1-6гетероарилалкила;
каждый R13 независимо выбран из водорода и С1-6алкила; и
R14 независимо выбран из водорода, С1-6алкила, С2-6алкенила, С2-6алкинила, карбоциклила, гетероциклила, арила, гетероарила, С1-6арилалкила и С1-6гетероарилалкила;
R15 выбран из водорода, С1-6алкила, С1-6гидроксиалкила, С1-6алкокси, -С(О)ОС1-6алкила, -С(О)NHC1-6алкила и С1-6арилалкила;
при условии, что в любом случае присутствия последовательности ZAZ, по меньшей мере один член последовательности должен быть другим, чем ковалентная связь.
2. Соединение по п.1, где R7 и R8 независимо выбраны из водорода и С1-6алкила.
3. Соединение по п.2, где R7 и R8, оба представляют собой водород.
4. Соединение по п.1, где R15 выбран из С1-6алкила и С1-6гидроксиалкила.
5. Соединение по п.4, где R15 выбран из метила, этила, гидроксиметила и 2-гидроксиэтила.
6. Соединение по п.1, где R5 представляет собой водород.
7. Соединение по п.1, где L и Q отсутствуют.
8. Соединение по п.1, где R6 представляет собой N-концевую защитную группу.
9. Соединение по п.8, где R6 выбран из трет-бутоксикарбонила и бензилоксикарбонила.
10. Соединение по п.1, где углерод, имеющий заместитель R1, имеет стереохимическую конфигурацию D.
11. Соединение по п.1, где R1 выбран из -С1-6алкилВ и С1-6арилалкила.
12. Соединение по п.11, где R1 выбран из метила, этила, изопропила, карбоксиметила и бензила.
13. Соединение по п.1, где R2 выбран из С1-6арилалкила и С1-6гетероарилалкила.
14. Соединение по п.13, где R2 выбран из С1-6алкилфенила, С1-6алкилиндолила, С1-6алкилтиенила, С1-6алкилтиазолила и С1-6алкилизотиазолила.
16. Соединение по п.1, где R3 выбран из С1-6арилалкила и С1-6гетероарилалкила.
17. Соединение по п.16, где R3 выбран из С1-6алкилфенила и С1-6алкилиндолила.
19. Соединение по п.1, где R6 выбран из гетероарила и С1-6гетероарилалкила.
20. Соединение по п.19, где R6 представляет собой гетероарил.
21. Соединение по п.20, где R6 выбран из пиррола, фурана, тиофена, имидазола, изоксазола, оксазола, оксадиазола, тиазола, тиадиазола, триазола, пиразола, пиридина, пиразина, пиридазина и пиримидина.
22. Соединение по п.19, где R6 представляет собой С1-6гетероарилалкил.
23. Соединение по п.22, где R6 выбран из пирролилметила, фуранилметила, тиенилметила, имидазолилметила, изоксазолилметила, оксазолилметила, оксадиазолилметила, тиазолилметила, тиадиазолилметила, триазолилметила, пиразолилметила, пиридилметила, пиразинилметила, пиридазинилметила и пиримидинилметила.
24. Способ лечения относящегося к иммунному заболевания, включающий введение соединения по любому из пп.1-23.
25. Способ лечения рака, включающий введение соединения по любому из пп.1-23.
26. Способ лечения воспаления, включающий введение соединения по любому пп.1-23.
27. Способ лечения инфекции, включающий введение соединения по любому из пп.1-23.
28. Способ лечения пролиферативного заболевания, включающий введение соединения по любому из пп.1-23.
29. Способ лечения нейродегенеративного заболевания, включающий введение соединения по любому из пп.1-23.
30. Соединение по п.1, где отношение ЕС50 соединения в испытании на активность конститутивной протеасомы, по сравнению с ЕС50 соединения в испытании на активность иммунопротеасомы выше, чем 1,0.
31. Соединение по п.30, где отношение ЕС50 выше, чем 3,0.
32. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель или разбавитель и соединение по любому из пп.1-23.
33. Соединение по п.1, где R6 выбирают из карбоциклила, гетероциклила, гетероциклилМZAZ-C1-8алкила-, гетероциклилМ- и карбоциклилМ-.
34. Соединение по п.33, где R6 выбирают из гетероциклила, гетероциклилМZAZ-C1-8алкила- и гетероциклилМ-.
35. Соединение по п.34, где R6 представляет собой гетероциклилМ-, а гетероциклильный фрагмент выбирают из морфолино, пиперидино, пиперазино и пирролидино.
36. Соединение по п.35, где R6 представляет собой гетероциклилМ-, а гетероциклильный фрагмент представляет собой морфолино.
37. Соединение по п.36, где L представляет собой C=O, Q отсутствует и М представляет собой С1-12алкил.
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