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RU2005131735A - Химические соединения - Google Patents

Химические соединения Download PDF

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RU2005131735A
RU2005131735A RU2005131735/04A RU2005131735A RU2005131735A RU 2005131735 A RU2005131735 A RU 2005131735A RU 2005131735/04 A RU2005131735/04 A RU 2005131735/04A RU 2005131735 A RU2005131735 A RU 2005131735A RU 2005131735 A RU2005131735 A RU 2005131735A
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alkyl
nhc
phenyl
heteroaryl
nhs
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Джон КАММИНГ (GB)
Джон Камминг
Алан ФОЛЛ (GB)
Алан Фолл
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Астразенека Аб (Se)
Астразенека Аб
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Claims (12)

1. Соединение формулы (I)
Figure 00000001
где А отсутствует или представляет собой СН2СН2;
R1 представляет собой галогено, гидрокси, нитро, (СН2)2S(O)k(С1-6алкил), (CH2)nS(O)2NH2, (СН2)nS(O)2NH(С1-6алкил), (CH2)nS(O)2NHCHO, (CH2)nS(O)2N(C1-6алкил)2, OS(O)2(С1-6алкил), циано, С1-6алкил, С1-6алкокси, NH2, NH(С1-6алкил), N(С1-6алкил)2, C(O)NH2, С(O)NH(С1-6алкил), С(O)N(С1-6алкил)2, С(O)[N-связанный гетероциклил], CO2Н, CO2(С1-6алкил), NHC(O)(С1-6алкил), NHC(O)O(С1-6алкил), (СН2)nNHS(O)2(С1-6алкил), С(O)(С1-6алкил), CF3, OCF3, фенил, гетероарил, (С1-4алкил)фенил, (С1-4алкил)гетероарил, NHC(O)фенил, NHC(O)гетероарил, NHC(O)(С1-4алкил)фенил, NHC(O)(С1-4алкил)гетероарил, NHS(O)2фенил, NHS(O)2 гетероарил, NHS(O)2(С1-4алкил)фенил, NHS(O)2(С1-4алкил)гетероарил, NHC(O)NH(С1-6алкил), NHC(O)NH(С3-7циклоалкил), NHC(O)NHфенил, NHC(O)NHгетероарил, NHC(O)NH(С1-4алкил)фенил или NHC(O)NH(С1-4алкил)гетероарил; где вышеуказанные фенильные и гетероарильные группы возможно замещены галогено, гидрокси, нитро, S(O)m(С1-4алкил), S(O)2NH2, S(O)2NH(С1-4алкил), S(O)2N(С1-4алкил)2, циано, С1-4алкилом, С1-4алкокси, C(O)NH2, С(O)NH(С1-4алкил), С(O)N(С1-4алкил)2, CO2Н, CO2(С1-4алкил), NHC(O)(С1-4алкил),NHS(O)2(С1-4алкил), С(O)(С1-4алкил), CF3 или OCF3;
R2 представляет собой фенил, галогенофенил, тиенил или галогенотиенил;
R3 представляют собой водород или метил;
R4 представляет собой пятичленный гетероцикл, содержащий по меньшей мере один атом углерода, от одного до четырех атомов азота и возможно один атом кислорода или серы, где указанный гетероцикл возможно замещен оксо, С1-6алкилом, H2NC(O), (фенилС1-2алкил)NHC(O), С1-2алкил(фенил) (который возможно замещен галогеном, С1-4алкилом, С1-4алкокси, CF3, OCF3, S(С1-4алкил), S(O)(С1-4алкил) или S(O)2(С1-4алкил)), S(С1-4алкил), S(С1-2алкил(фенил)), NH2 или фенилом; причем этот пятичленный гетероцикл возможно конденсирован с циклогексановым, пиперидиновым, бензольным, пиридиновым, пиридазиновым, пиримидиновым или пиразиновым кольцом, где кольцевые атомы углерода указанного конденсированного циклогексанового, пиперидинового, бензольного, пиридинового, пиридазинового, пиримидинового или пиразинового кольца возможно замещены галогеном, циано, С1-4алкилом, С1-4алкокси, CF3, OCF3, NH2, S(С1-4алкил), S(O)(С1-4алкил) или S(O)2(С1-4алкил); и где атом азота конденсированного пиперидинового кольца возможно замещен С1-4алкилом (который возможно замещен оксо, галогеном, ОН, С1-4алкокси, OCF3, C(O)O(С1-4алкил), CN, C(O)NH2, С(O)NH(С1-4алкил), С(O)N(С1-4алкил)2, NH2, NH(С1-4алкил) или N(С1-4алкил)2), С(O)(С1-4алкил) (где алкил возможно замещен С1-4алкокси или фторо), С(O)O(С1-4алкил), C(O)NH2, С(O)NH(С1-4алкил), С(O)N(С1-4алкил)2 или S(O)2(С1-4алкил) (где алкил возможно замещен фторо);
k, m и n независимо равны 0, 1 или 2,
или его фармацевтически приемлемая соль или его сольват.
2. Соединение формулы (I) по п.1, где А отсутствует.
3. Соединение формулы (I) по п.1, где R1 представляет собой галогено, циано, S(O)2(С1-6алкил), OS(O)2(С1-6алкил), CO2(С1-6алкил), NHC(O)(С1-6алкил), NHS(O)2(С1-6алкил), NHC(O)фенил, NHC(O)гетероарил, NHC(O)(С1-4алкил)фенил, NHC(O)(С1-4алкил)гетероарил, NHS(O)2фенил, NHS(O)2 гетероарил, NHS(O)2(С1-4алкил)фенил или NHS(O)2(С1-4алкил) гетероарил, где вышеуказанные фенильные и гетероарильные группы возможно замещены галогено, гидрокси, нитро, S(O)2(С1-4алкил), S(O)2NH2, S(O)2NH(С1-4алкил), S(O)2N(С1-4алкил)2, циано, С1-4алкилом, С1-4алкокси, C(O)NH2, С(O)NH(С1-4алкил), С(O)N(С1-4алкил)2, CO2Н, CO2(С1-4алкил), NHC(O)(С1-4алкил), NHS(O)2(С1-4алкил), С(O)(С1-4алкил), CF3 или OCF3.
4. Соединение формулы (I) по п.1, где R1 представляет собой галогено, циано, S(O)2(С1-6алкил), OS(O)2(С1-6алкил), CO2(С1-6алкил), NHC(O)(С1-6алкил) или NHS(O)2(С1-6алкил).
5. Соединение формулы (I) по п.1, где R2 представляет собой фенил или галогенофенил.
6. Соединение формулы (I) по п.1, где R3 представляет собой водород.
7. Соединение формулы (I) по любому из пп.1-6, где R4 представляет собой имидазолил, 1,2,4-триазолил, 1,2,4-оксадиазолил, тетразолил, пиразолил или 1,3-тиазолил, изоксазолил, возможно замещенные, как описано в п.1.
8. Способ получения соединения формулы (I) по п.1, включающий восстановительное аминирование соединения формулы (II)
Figure 00000002
соединением формулы (III)
Figure 00000003
в присутствии NaBH(ОАс)3 (где Ас представляет собой С(О)СН3) и уксусной кислоты в подходящем растворителе при комнатной температуре.
9. Фармацевтическая композиция, которая содержит соединение по п.1 или его фармацевтически приемлемую соль или его сольват и фармацевтически приемлемый адъювант, разбавитель или носитель.
10. Соединение по п.1 или его фармацевтически приемлемая соль или его сольват для применения в качестве лекарства.
11. Соединение по п.1 или его фармацевтически приемлемая соль или его сольват для применения в изготовлении лекарства для использования в терапии.
12. Способ лечения болезненного состояния, опосредованного CCR5, включающий введение нуждающемуся в таком лечении пациенту эффективного количества соединения по п.1.
RU2005131735/04A 2003-05-09 2004-05-06 Химические соединения RU2005131735A (ru)

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