RU2409576C2 - Системы, содержащие имидазольное кольцо с заместителями, и способы их получения - Google Patents

Системы, содержащие имидазольное кольцо с заместителями, и способы их получения Download PDF

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RU2409576C2
RU2409576C2 RU2006118033/04A RU2006118033A RU2409576C2 RU 2409576 C2 RU2409576 C2 RU 2409576C2 RU 2006118033/04 A RU2006118033/04 A RU 2006118033/04A RU 2006118033 A RU2006118033 A RU 2006118033A RU 2409576 C2 RU2409576 C2 RU 2409576C2
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alkyl
hydrogen
salt
phenyl
groups
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Ларри Р. КРЕПСКИ (US)
Ларри Р. Крепски
Джозеф Ф. Мл. ДЕЛЛАРИА (US)
Джозеф Ф. Мл. ДЕЛЛАРИА
Дэниел Е. ДАФФИ (US)
Дэниел Е. ДАФФИ
Мэттью Р. РАДМЕР (US)
Мэттью Р. Радмер
Дэвид Т. АМОС (US)
Дэвид Т. АМОС
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3М Инновейтив Пропертиз Компани
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Abstract

Изобретение относится к системам, содержащим имидазольное кольцо, соответствующие веществу формулы (I-1):
Figure 00000190
в которой: Х представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами; Z представляет собой -С(O)-; R1-1 выбирается из группы, включающей: водород, алкил, фенил, -N(СН3)(ОСН3), и фенил, замещенный одним или несколькими галогенами; R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил; RA и RB, взятые вместе, образуют слитое фенильное кольцо или к его фармацевтически приемлемым солям. Изобретение также относится к фармацевтическим композициям для индуцирования биосинтеза цитокина, содержащим такие вещества. Указанные вещества могут найти применение в медицине в качестве иммуномодуляторов, для индукции или подавления биосинтеза цитокинов у животных и при лечении заболеваний, в том числе вирусных и злокачественных болезней. 8 н. и 10 з.п. ф-лы.

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Claims (18)

1. Вещество, соответствующее формуле (I-1):
Figure 00000184

в которой X представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами;
Z представляет собой -С(O)-;
R1-1 выбирается из группы, включающей:
водород,
алкил,
фенил,
-N(СН3)(ОСН3), и
фенил, замещенный одним или несколькими галогенами;
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
RA и RB, взятые вместе, образуют слитое фенильное кольцо или его фармацевтически приемлемая соль.
2. Вещество, соответствующее формуле (I-2):
Figure 00000185

в которой X представляет собой алкилен, факультативно прерываемый одной или
несколькими -О- группами;
n равно 0;
Z представляет собой -С(O)-;
R1-1 выбирается из группы, включающей:
водород,
алкил,
фенил,
-N(СН3)(ОСН3), и
фенил, замещенный одним или несколькими галогенами;
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
или его фармацевтически приемлемая соль.
3. Вещество, соответствующее формуле (I-3):
Figure 00000186

в которой Х представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами;
Z представляет собой -С(O)-, -С(O)O-, или -C(-Q-R1-3)2-;
R1-1 выбирается из группы, включающей:
водород,
алкил,
фенил, и
фенил, замещенный одним или несколькими галогенами;
при условии, что если Z представляет собой -С(O)-, то R1-1 может также быть группой N(СН3)(ОСН3);
при дополнительном условии, что если Z представляет собой - С(O)O-, то R1-1 не является водородом;
при дополнительном условии, что если Z представляет собой - С(O)O-, то Х не включает -О- группы;
Q представляет собой О;
R1-3 представляет собой алкил; и
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
каждая из групп RA' и RB' представляет собой алкил;
или его фармацевтически приемлемая соль.
4. Вещество, соответствующее формуле (Ia):
Figure 00000187

в которой X представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами;
n равно 0;
R1-1 выбирается из группы, включающей:
водород,
алкил,
фенил,
-N(СН3)(ОСН3), и
фенил, замещенный одним или несколькими галогенами; и
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
или его фармацевтически приемлемая соль.
5. Вещество, соответствующее формуле (Id):
Figure 00000188

в которой X представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами;
n равно 0;
R1-1 выбирается из группы, включающей:
водород и алкил;
Q представляет собой О;
R1-3 представляет собой алкил;
или R1-3 группы могут объединяться друг с другом с образованием насыщенного 5-членного кольца;
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
или его фармацевтически приемлемая соль.
6. Вещество, соответствующее формуле (Ie):
Figure 00000189

в которой Х представляет собой алкилен, факультативно прерываемый одной или несколькими -О- группами;
n равно 0;
R2 представляет собой водород; алкил; гидроксиалкил; или алкоксиалкил;
или его фармацевтически приемлемая соль.
7. Вещество по п.3 или его соль, где Z представляет собой - С(O)-.
8. Вещество по п.3 или 5, или его соль, где R1-3 представляет собой алкил или R1-3 группы объединяются друг с другом с образованием 5-членного кольца.
9. Вещество по любому из пп.1-4 и 7, или его соль, где R1-1 выбирается из группы, включающей фенил, алкил и -N(СН3)ОСН3.
10. Вещество по любому из пп.1-4 и 7, или его соль, где R1-1 выбирается из группы, включающей алкил, фенил и водород.
11. Вещество по любому из пп.1-6, или его соль, где Х представляет собой C1-6алкилен или -(CH2)2-4-O-(CH2)1-3-.
12. Вещество по п.11, или его соль, где Х выбирается из группы, включающей -(CH2)1-6-, -СН2-С(СН3)2-, -(СН2)2-O-СН2-, -(CH2)3-О-СН2- и -СН2-С(СН3)2-СН2-.
13. Вещество по любому из пп.1-4 и 7, или его соль, где R1-1 выбирается из группы, включающей алкил и фенил.
14. Вещество по п.13, или его соль, где R1-1 выбирается из группы, включающей метил, этил, н-пропил, изопропил, циклопропил, н-бутил, втор-бутил, изобутил, трет-бутил, н-пентил, циклопентил, н-гексил, циклогексил, фенил, 4-хлорфенил и 2,4-дихлорфенил.
15. Вещество по любому из пп.1-6, или его соль, где R2 выбирается из группы, включающей водород, алкил, гидроксиалкил и алкоксиалкил.
16. Вещество по п.15, или его соль, где R2 выбирается из группы, включающей водород, гидроксиметил, метил; этил, н-пропил, н-бутил, этоксиметил, и 2-метоксиэтил.
17. Фармацевтическая композиция для индуцирования биосинтеза цитокина, содержащая терапевтически эффективное количество вещества по любому из пп.1-6, или его соли в комбинации с фармацевтически приемлемым носителем или наполнителем.
18. Применение вещества по любому из пп.1-6 для производства фармацевтической композиции для индуцирования биосинтеза цитокинов в организме животного.
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