RU2015116112A - Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7 - Google Patents
Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7 Download PDFInfo
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Abstract
1. Соединение формулы Iгде Rпредставляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил, 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими Салкилами, галогенами, гидрокси, Сфторалкилами, Сциклоалкилами, Салкокси, Cфторалкокси, циано или -SOR;где Rи Rобъединяются с азотом, к которому они присоединены, образуя пиперазинил, пиперидинил, морфолинил, пирролидинил, пирроло, имидазо, азетидинил, 6-10-членный спиро(гетороциклил), гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими Салкилами, Салкенилами, С-циклоалкилами, Салкокси, оксо, -NRRили атомами фтора;где Rпредставляет собой галоген, Сфторалкил, циано, циклопропил, Cалкилокси, Сфторалкилокси, -SOR, -NRRили Cалкил;где Rпредставляет собой галоген, Салкил, Сфторалкил, циано, -SOR, -NRR, Салкокси, Сфторалкокси или С-циклоалкил;где Rи Rнезависимо друг от друга представляют собой водород или Cалкил;где Rпредставляет собой Салкил, Сциклоалкил, Сфторалкил и где n равно 0-3; или его фармацевтически приемлемая соль.2. Соединение по п. 1, где Rпредставляет собой необязательно замещенный фенил.3. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиридил.4. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиразинил.5. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиримидил.6. Соединение по п. 1, где Rпредставляет собой необязательно замещенный 5-членный гетероарил.7. Соединение по любому из пп. 1-6, где Rи Rобъединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперазинил.8. Соединение по любому из пп. 1-6, где Rи Rобъединяются с азотом, к которому они присоединены, образуя
Claims (24)
1. Соединение формулы I
где R1 представляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил, 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими С1-6алкилами, галогенами, гидрокси, С1-4фторалкилами, С3-6циклоалкилами, С1-6алкокси, C1-6фторалкокси, циано или -SO2R7;
где R2a и R2b объединяются с азотом, к которому они присоединены, образуя пиперазинил, пиперидинил, морфолинил, пирролидинил, пирроло, имидазо, азетидинил, 6-10-членный спиро(гетороциклил), гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими С1-6алкилами, С1-6алкенилами, С3-6-циклоалкилами, С1-6алкокси, оксо, -NR5R6 или атомами фтора;
где R3 представляет собой галоген, С1-4фторалкил, циано, циклопропил, C1-4алкилокси, С1-4фторалкилокси, -SO2R7, -NR5R6 или C1-6алкил;
где R4 представляет собой галоген, С1-6алкил, С1-4фторалкил, циано, -SO2R8, -NR5R6, С1-6алкокси, С1-4фторалкокси или С3-6-циклоалкил;
где R5 и R6 независимо друг от друга представляют собой водород или C1-6алкил;
где R7 представляет собой С1-6алкил, С3-6циклоалкил, С1-4фторалкил и где n равно 0-3; или его фармацевтически приемлемая соль.
2. Соединение по п. 1, где R1 представляет собой необязательно замещенный фенил.
3. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиридил.
4. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиразинил.
5. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиримидил.
6. Соединение по п. 1, где R1 представляет собой необязательно замещенный 5-членный гетероарил.
7. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперазинил.
8. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперидинил.
9. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный морфолинил.
10. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пирролидинил.
11. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пирроло.
12. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный имидазо.
13. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный 6-10-членный спиро(гетероциклил).
14. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомоморфолинил.
15. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперидинил.
16. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперазинил.
17. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный азетидинил.
18. Соединение по любому из пп. 1-6, где R3 представляет собой хлор, метил или трифторметил.
19. Соединение по любому из пп. 1-6, где n равно 0.
20. Соединение по любому из пп. 1-6, где n равно 1.
21. Соединение по любому из пп. 1-6, где n равно 2.
22. Соединение по любому из пп. 1-6, где R4 представляет собой фтор, хлор, С1-3алкил, С1-4фторалкил, циано-, C1-3алкокси- или С1-4фторалкокси.
23. Соединение, представленное в Таблице 1.
24. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-23.
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