RU2015113320A - Бензамиды - Google Patents
Бензамиды Download PDFInfo
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- RU2015113320A RU2015113320A RU2015113320A RU2015113320A RU2015113320A RU 2015113320 A RU2015113320 A RU 2015113320A RU 2015113320 A RU2015113320 A RU 2015113320A RU 2015113320 A RU2015113320 A RU 2015113320A RU 2015113320 A RU2015113320 A RU 2015113320A
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Abstract
1. Соединение формулы Iгде Rпредставляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил или 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими Cалкилами, галогенами, гидроксигруппами, Cгидроксиалкилами, Cфторалкилами, Cциклоалкилами, Cалкокси, Cфторалкокси, циано или -SOR;где Rпредставляет собой Cциклоалкил, Cциклогетероалкил, Cфторалкил, Cфторалкоксигруппу, Cалкокси, Cалкенил, Cалкинил, 6-членный гетероарил, фенил или Cалкил, необязательно замещенный одним или несколькими R;где Rпредставляет собой водород, фтор, Cалкил или Cфторалкил; илигде Rи Rобъединяются с углеродом, к которому они присоединены, образуя циклогексил, тетрагидропиранил, пиперазинил, пиреридинил, морфолинил, пирролидинил, азетидинил, гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими Cалкилами, Cалкенилами, C-циклоалкилами, Cалкокси, оксо, NRRили фтором;где Rпредставляет собой галоген, Cфторалкил, циано, циклопропил, Cалкилокси, Cфторалкилокси, -SOR, -NRRили Cалкил;где Rпредставляет собой галоген, Cалкил, Cфторалкил, циано, -SOR, -NRR, Cалкокси, Cфторалкокси или C-циклоалкил;где Rи Rнезависимо друг от друга представляют собой водород или Cалкил;где Rпредставляет собой Cалкил, Cциклоалкил или Cфторалкил;где Rпредставляет собой Cалкил, Cциклоалкил, -NRR, Cфторалкил или 3-7-членный гетероциклил, который необязательно замещен одним или несколькими Cалкилами, галогенами, гидрокси, Cфторалкилами, Cциклоалкилами, Cалкокси, Cфторалкокси или циано;где Rи Rнезависимо друг от друга представляют собой водород или Cалкил; илигде Rи Rобъединяются с азотом, к которому они присоединены, образуя пиперазинил, пиреридинил, морфолинил, пирролидинил,
Claims (23)
1. Соединение формулы I
где R1 представляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил или 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими C1-6алкилами, галогенами, гидроксигруппами, C1-6гидроксиалкилами, C1-4фторалкилами, C3-6циклоалкилами, C1-4алкокси, C1-4фторалкокси, циано или -SO2R8;
где R2 представляет собой C3-6циклоалкил, C3-6циклогетероалкил, C1-4фторалкил, C1-4фторалкоксигруппу, C1-4алкокси, C1-6алкенил, C1-6алкинил, 6-членный гетероарил, фенил или C1-4алкил, необязательно замещенный одним или несколькими R9;
где R3 представляет собой водород, фтор, C1-4алкил или C1-4фторалкил; или
где R2 и R3 объединяются с углеродом, к которому они присоединены, образуя циклогексил, тетрагидропиранил, пиперазинил, пиреридинил, морфолинил, пирролидинил, азетидинил, гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими C1-6алкилами, C1-6алкенилами, C3-6-циклоалкилами, C1-6алкокси, оксо, NR6R7 или фтором;
где R4 представляет собой галоген, C1-4фторалкил, циано, циклопропил, C1-4алкилокси, C1-4фторалкилокси, -SO2R8, -NR6R7 или C1-6алкил;
где R5 представляет собой галоген, C1-6алкил, C1-4фторалкил, циано, -SO2R8, -NR6R7, C1-6алкокси, C1-4фторалкокси или C3-6-циклоалкил;
где R6 и R7 независимо друг от друга представляют собой водород или C1-6алкил;
где R8 представляет собой C1-6алкил, C3-6циклоалкил или C1-4фторалкил;
где R9 представляет собой C1-6алкил, C3-6циклоалкил, -NR10R11, C1-4фторалкил или 3-7-членный гетероциклил, который необязательно замещен одним или несколькими C1-6алкилами, галогенами, гидрокси, C1-4фторалкилами, C3-6циклоалкилами, C1-4алкокси, C1-4фторалкокси или циано;
где R10 и R11 независимо друг от друга представляют собой водород или C1-6алкил; или
где R10 и R11 объединяются с азотом, к которому они присоединены, образуя пиперазинил, пиреридинил, морфолинил, пирролидинил, азетидинил, гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими C1-6алкилами, C1-6алкокси, оксо, или фтором; 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 R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперазинил.
8. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперидинил.
9. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный морфолинил.
10. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пирролидинил.
11. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиррольный фрагмент.
12. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный имидазольный фрагмент.
13. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомоморфолинил.
14. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперидинил.
15. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперазинил.
16. Соединение по любому из пп. 1-6, где R2 и R3 объединяются с азотом, к которому они присоединены, образуя необязательно замещенный азетидинил.
17. Соединение по любому из пп. 1-6, где R4 представляет собой хлор, метил или трифторметил.
18. Соединение по любому из пп. 1-6, где n равно 0.
19. Соединение по любому из пп. 1-6, где n равно 1.
20. Соединение по любому из пп. 1-6, где n равно 2.
21. Соединение по любому из пп. 1-6, где R5 представляет собой фтор, хлор, C1-3алкил, C1-4фторалкил, циано, C1-3алкокси или C1-4фторалкокси.
22. Соединение, представленное в Таблице 1.
23. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-22.
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