RU2017112518A - Пиридоновые и азапиридоновые соединения и способы применения - Google Patents
Пиридоновые и азапиридоновые соединения и способы применения Download PDFInfo
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- RU2017112518A RU2017112518A RU2017112518A RU2017112518A RU2017112518A RU 2017112518 A RU2017112518 A RU 2017112518A RU 2017112518 A RU2017112518 A RU 2017112518A RU 2017112518 A RU2017112518 A RU 2017112518A RU 2017112518 A RU2017112518 A RU 2017112518A
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- Prior art keywords
- compound according
- compound
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- heterocyclyl
- methyl
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- 150000001875 compounds Chemical class 0.000 title claims 30
- -1 (1-methylazetidin-3-yl) oxy, N -methyl-N-oxetan-3-ylamino Chemical group 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000004452 carbocyclyl group Chemical group 0.000 claims 6
- 125000002393 azetidinyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000003566 oxetanyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- JBXGNKZFIOAVNY-UHFFFAOYSA-N 2h-thieno[2,3-d]pyridazin-4-one Chemical compound O=C1N=NC=C2SCC=C12 JBXGNKZFIOAVNY-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
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Claims (65)
1. Соединение, выбранное из формулы I:
или его стереоизомеры, таутомеры, или фармацевтически приемлемые соли, где:
R1 представляет собой Н, D, F, Cl, CN, -NH2, -NHCH3, -N(CH3)2, -OH, -OCH3, -ОСН2СН3, -ОСН2СН2ОН, гетероарил, выбранный из имидазолила и пиразолила, гетероциклил, выбранный из оксетанила и азетидинила, и С1-С3 алкил;
R2, R3 и R4 независимо выбраны из Н, D, F, Cl, -NH2, -NHCH3, -N(CH3)2, -ОН, -ОСН3, -ОСН2СН3, -ОСН2СН2ОН, и С1-С3 алкила;
R5 представляет собой необязательно замещенный С6-С20 арил, C3-C12 карбоциклил, С2-С20 гетероциклил, С1-С20 гетероарил, -(С6-С20 арил)-(С2-С20 гетероциклил), -(С1-С20 гетероарил)-(С2-С20 гетероциклил), -(C1-C20 гетероарил)-(С1-С6 алкил), или -(C1-C20 гетероарил)-С(=O)-(С2-С20 гетероциклил);
R6 представляет собой Н, F, -NH2, -ОН, или необязательно замещенный C1-C3 алкил;
X представляет собой S, S(=O), S(=O)2, N, NR6, О, или CR7;
R7 независимо выбран из Н, D, F, Cl, -СН3, -СН2СН3, -CN, -CH2F, -CHF2, -CF3, -NH2, -ОН, и -ОСН3;
Y1 и Y2 независимо выбраны из CR6 и N;
Z1, Z2, Z3, и Z4 независимо выбраны из С, CR7 и N;
Z5 представляет собой -CR3=N-;
один из Z1 и Z2, или X и Z1, где X не представляет собой S, S(=O), или S(=O)2, образуют пяти, шести, или семичленное арильное, карбоциклильное, гетероциклильное или гетероарильное кольцо;
где алкил, карбоциклил, гетероциклил, арил, и гетероарил необязательно замещены одной или более группой, независимо выбранной из D, F, Cl, Br, I, -СН3, -СН2СН3, -СН2СН(СН3)2, -СН2ОН, -СН2СН2ОН, -С(СН3)2ОН, -СН(ОН)СН(СН3)2, -С(СН3)2СН2ОН, -CH2CH2SO2CH3, -СН2ОР(O)(ОН)2, -CN, -CH2F, -CHF2, -CF3, -CO2H, -COCH3, -CO2CH3, -CO2C(СН3)3, -СОСН(ОН)СН3, -CONH2, -CONHCH3, -CON(CH3)2, -C(CH3)2CONH2, -NO2, -NH2, -NHCH3, -N(CH3)2, -NHCOCH3, -N(CH3)COCH3, -NHS(O)2CH3, -N(CH3)C(CH3)2CONH2, -N(CH3)CH2CH2S(O)2CH3, =O, -OH, -OCH3, -OCH2CH2N(CH3)2, -OP(O)(OH)2, -S(O)2N(CH3)2, -SCH3, -CH2OCH3, -S(O)2CH3, циклопропила, азетидинила, (1-метилазетидин-3-ил)окси, N-метил-N-оксетан-3-иламино, азетидин-1-илметила, оксетанила, и морфолино.
2. Соединение по п. 1, выбранное из формул Ia-c:
3. Соединение по п. 1, выбранное из формул Id-f:
4. Соединение по п. 1, выбранное из формул Ig-n:
5. Соединение по п. 1, выбранное из формул Io-t:
6. Соединение по п. 1, отличающееся тем, что Z1 и Z2 образуют пяти, шести, или семичленное арильное, карбоциклильное, гетероциклильное или гетероарильное кольцо, и выбрано из формул Iaa-ap:
7. Соединение по п. 1, отличающееся тем, что X и Z1, и X не представляет собой S, образуют пяти, шести, или семичленное арильное, карбоциклильное, гетероциклильное или гетероарильное кольцо, и выбрано из формул Iaq-bf:
8. Соединение по п. 1, отличающееся тем, что группа:
образует структуры:
при этом волнистая линия указывает на место присоединения.
9. Соединение по любому из пп. 1-8, отличающееся тем, что каждый из R1, R2, R3, и R4 представляет собой Н.
10. Соединение по п. 1, отличающееся тем, что R1 выбран из F, -СН3, -CH2F, -CHF2, и -CF3.
11. Соединение по п. 1, отличающееся тем, что R1 представляет собой -СН2ОН.
12. Соединение по п. 1, отличающееся тем, что R3 представляет собой F.
13. Соединение по п. 1, отличающееся тем, что R1 представляет собой -СН2ОН, каждый из R2 и R4 представляет собой Н, и R3 представляет собой F.
14. Соединение по п. 1, отличающееся тем, что R5 представляет собой необязательно замещенный С6-С20 арил, выбранный из фенила и нафтила.
15. Соединение по п. 1, отличающееся тем, что R5 представляет собой необязательно замещенный С3-С12 карбоциклил, выбранный из циклопропила, циклобутила, циклопентила, циклогексила, и циклогептила.
16. Соединение по п. 1, отличающееся тем, что R5 представляет собой необязательно замещенный С2-С20 гетероциклил, выбранный из оксетанила, азетидинила, пирролидинила, тетрагидрофурила, пиперидинила, пиперазинила, морфолинила, и тетрагидропиранила.
17. Соединение по п. 1, отличающееся тем, что R5 представляет собой необязательно замещенный C1-C20 гетероарил, выбранный из пиразолила, пиридинила, пиримидинила, 5-метил-4,5,6,7-тетрагидропиразоло[1,5-а]пиразин-2-ила, 5-ацетил-4,5,6,7-тетрагидропиразоло[1,5-а]пиразин-2-ила, 6,7-дигидро-4Н-пиразоло[5,1-с][1,4]оксазин-2-ила, и 1-метил-5-(5-(4-метилпиперазин-1-ил)пиридин-2-ила.
18. Соединение по п. 1, отличающееся тем, что R5 замещен одной или более группой, выбранной из F, Cl, -СН3, циклопропила, азетидинила, оксетанила, и морфолино.
19. Соединение по п. 1, отличающееся тем, что R5 выбран из структур:
при этом волнистая линия указывает на место присоединения.
20. Соединение по п. 1, отличающееся тем, что R6 представляет собой Н.
21. Соединение по п. 1, отличающееся тем, что X представляет собой S.
22. Соединение по п. 1, отличающееся тем, что X представляет собой N.
23. Соединение по п. 1, отличающееся тем, что X представляет собой CR7.
24. Соединение по п. 1, отличающееся тем, что Y1 представляет собой CR6 и Y2 представляет собой N.
25. Соединение по п. 1, отличающееся тем, что Y1 представляет собой N и Y2 представляет собой CR6.
26. Соединение по п. 1, отличающееся тем, что каждый из Y1 и Y2 представляет собой CR6.
27. Фармацевтическая композиция, содержащая соединение по п. 1 и фармацевтически приемлемый носитель, скользящее вещество, разбавитель, или наполнитель.
28. Фармацевтическая композиция по п. 27, дополнительно содержащая второй терапевтический агент.
29. Способ получения фармацевтической композиции, включающий объединение соединения по п. 1 с фармацевтически приемлемым носителем.
30. Соединение по п. 1, выбранное из
5-[5-фтор-2-(гидроксиметил)-3-(1-метил-5-{[5-(4-(оксетан-3-ил)пиперазин-1-ил)пиридин-2-ил]амино}-6-оксо-1,6-дигидропиридин-3-ил)фенил]-8-тиа-4,5-диазатрицикло[7.4.0.02,7]тридека-1(9),2(7),3-триен-6-он,
5-[5-фтор-2-(гидроксиметил)-3-(1-метил-5-{[5-(4-метилпиперазин-1-ил)пиридин-2-ил]амино}-6-оксо-1,6-дигидропиридин-3-ил)фенил]-8-тиа-4,5-диазатрицикло[7.4.0.02,7]тридека-1(9),2(7),3(4)-триен-6-он,
3-(5-фтор-2-гидроксиметил-3-{1-метил-5-[6-(4-метилпиперазин-1-ил)-пиридазин-3-иламино]-6-оксо-1,6-дигидропиридин-3-ил}-фенил)-6,7,8,9-тетрагидро-3Н-бензо[4,5]тиено[2,3-d]пиридазин-4-он,
3-(5-фтор-2-гидроксиметил-3-{1-метил-5-[6-(4-оксетан-3-ил-пиперазин-1-ил)-пиридазин-3-иламино]-6-оксо-1,6-дигидропиридин-3-ил}-фенил)-6,7,8,9-тетрагидро-3Н-бензо[4,5]тиено[2,3-d]пиридазин-4-он,
2-(5-фтор-2-(гидроксиметил)-3-(1-метил-5-(5-(4-(оксетан-3-ил)пиперазин-1-ил)пиридин-2-иламино)-6-оксо-1,6-дигидропиридин-3-ил)фенил)-6,7,8,9-тетрагидро-[1,2,4]триазино[4,5-а]индол-1(2Н)-он, и
2-(5-фтор-2-(гидроксиметил)-3-(1-метил-5-(5-(4-метилпиперазин-1-ил)пиридин-2-иламино)-6-оксо-1,6-дигидропиридин-3-ил)фенил)-6,7,8,9-тетрагидро-[1,2,4]триазино[4,5-а]индол-1(2Н)-он.
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