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RU2014114466A - ИНДАЗОЛ-3-КАРБОКСАМИДЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ СИГНАЛЬНОГО ПУТИ WNT/β-КАТЕНИНА - Google Patents

ИНДАЗОЛ-3-КАРБОКСАМИДЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ СИГНАЛЬНОГО ПУТИ WNT/β-КАТЕНИНА Download PDF

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RU2014114466A
RU2014114466A RU2014114466/04A RU2014114466A RU2014114466A RU 2014114466 A RU2014114466 A RU 2014114466A RU 2014114466/04 A RU2014114466/04 A RU 2014114466/04A RU 2014114466 A RU2014114466 A RU 2014114466A RU 2014114466 A RU2014114466 A RU 2014114466A
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alkyl
group
pyridyl
heteroaryl
compound
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RU2014114466/04A
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RU2627693C2 (ru
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Джон ХУД
Сунил Кумар КС
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СЭМЬЮМЕД, ЭлЭлСи
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

1. Соединение или его фармацевтически приемлемая соль или пролекарство, имеющее структуру формулы I:где:R, Rи Rнезависимо выбраны из группы, включающей H, Cалкил, галоген, -N(R), -XR, CN, -OCFи -CF;Rвыбран из группы, включающей карбоциклилR, гетероциклилR, арилRи гетероарилR;при условии, что, когда Rпредставляет собой гетероарил, гетероарил не выбран из группы, включающей изохинолин, 1H-пирроло[2,3-c]пиридин и тетразол;Rвыбран из группы, включающей -(Cалкил)карбоциклилR, -(Cалкил)гетероциклилR, -(Cалкил)арилRи -(Cалкил)гетероарилR;при условии, что Rне представляет собой 4-пиридилR, когда R, Rи Rпредставляют собой H, Rвыбран из группы, включающей 3-пиридилR, 4-пиридилR, 2-пиридилR, фенилR, тиазолR, имидазолR, пиримидинR, оксазолR,и Rи Rоба представляют собой H;при условии, что Rне представляет собой -(CH)(3-пиридил)R, когда R, Rи Rпредставляют собой H, Rвыбран из группы, включающей 3-пиридилR, 4-пиридилRи тиазолR, и Rи Rоба представляют собой H;при условии, что Rне представляет собой фенилR, когда R, Rи Rпредставляют собой H, Rпредставляет собой 4-пиридилRи Rи Rоба представляют собой H;при условии, что Rне представляет собой 3-пиридилR, когда R, Rи Rпредставляют собой H, Rвыбран из группы, включающей фенилR,и Rи Rоба представляют собой H;при условии, что Rне представляет собой оксазолR, когда R, Rи Rпредставляют собой H, Rвыбран из группы, включающейи Rпредставляет собой H;при условии, что Rне представляет собой тиазолR, когда R, Rи Rпредставляют собой H, Rвыбран из группы, включающейи Rпредставляет собой H;каждый Rобозначает 1-5 заместителей, каждый из которых выбран из группы, включающей H, Cалкил, галоген, амино, -OCF, -CF, -CN, -XR, -(Cалкил)карбоциклилR, -(Cалкил)гетероциклилR, -(Cалкил)арилR, -(Cалкил)гетероарилR

Claims (24)

1. Соединение или его фармацевтически приемлемая соль или пролекарство, имеющее структуру формулы I:
Figure 00000001
где:
R1, R2 и R4 независимо выбраны из группы, включающей H, C1-9 алкил, галоген, -N(R10)2, -XR10, CN, -OCF3 и -CF3;
R3 выбран из группы, включающей карбоциклилR6, гетероциклилR6, арилR6 и гетероарилR6;
при условии, что, когда R3 представляет собой гетероарил, гетероарил не выбран из группы, включающей изохинолин, 1H-пирроло[2,3-c]пиридин и тетразол;
R5 выбран из группы, включающей -(C1-9 алкил)nкарбоциклилR7, -(C1-9 алкил)nгетероциклилR7, -(C1-9 алкил)nарилR7 и -(C1-9 алкил)nгетероарилR7;
при условии, что R5 не представляет собой 4-пиридилR7, когда R1, R2 и R4 представляют собой H, R3 выбран из группы, включающей 3-пиридилR6, 4-пиридилR6, 2-пиридилR6, фенилR6, тиазолR6, имидазолR6, пиримидинR6, оксазолR6,
Figure 00000002
Figure 00000003
Figure 00000004
и R6 и R7 оба представляют собой H;
при условии, что R5 не представляет собой -(CH2)(3-пиридил)R7, когда R1, R2 и R4 представляют собой H, R3 выбран из группы, включающей 3-пиридилR6, 4-пиридилR6 и тиазолR6, и R6 и R7 оба представляют собой H;
при условии, что R5 не представляет собой фенилR7, когда R1, R2 и R4 представляют собой H, R3 представляет собой 4-пиридилR6 и R6 и R7 оба представляют собой H;
при условии, что R3 не представляет собой 3-пиридилR6, когда R1, R2 и R4 представляют собой H, R5 выбран из группы, включающей фенилR7,
Figure 00000005
Figure 00000006
Figure 00000007
и R6 и R7 оба представляют собой H;
при условии, что R3 не представляет собой оксазолR6, когда R1, R2 и R4 представляют собой H, R5 выбран из группы, включающей
Figure 00000008
и R6 представляет собой H;
при условии, что R3 не представляет собой тиазолR6, когда R1, R2 и R4 представляют собой H, R5 выбран из группы, включающей
Figure 00000009
и R6 представляет собой H;
каждый R6 обозначает 1-5 заместителей, каждый из которых выбран из группы, включающей H, C1-9 алкил, галоген, амино, -OCF3, -CF3, -CN, -XR10, -(C1-9 алкил)nкарбоциклилR8, -(C1-9 алкил)nгетероциклилR8, -(C1-9 алкил)nарилR8, -(C1-9 алкил)nгетероарилR8, -C(=O)R11, -N(R10)C(=O)R11, -(C1-9 алкил)nN(R10)2, -(C1-9 алкил)nN(R10)SO2R11 и -SO2R11;
каждый R7 обозначает 1-5 заместителей, каждый из которых выбран из группы, включающей H, C1-9 алкил, галоген, амино, -OCF3, -CF3, -CN, -XR10, -(C1-9 алкил)nкарбоциклилR9, -(C1-9 алкил)nгетероциклилR9, -(C1-9 алкил)nарилR9, -(C1-9 алкил)nгетероарилR9, -C(=O)R11, -N(R10)C(=O)R11, -(C1-9 алкил)nN(R10)2, -(C1-9 алкил)nN(R10)SO2R11 и -SO2R11;
каждый R8 обозначает 1-5 заместителей, каждый из которых выбран из группы, включающей H, C1-3 алкил, галоген, амино, OCF3, -CF3 -CN, -XR12, -C(=O)R13, -N(R12)C(=O)R13, -(C1-9 алкил)nN(R12)2, -(C1-9 алкил)nN(R12)SO2R13 и -SO2R13;
каждый R9 обозначает 1-5 заместителей, каждый из которых выбран из группы, включающей H, C1-3 алкил, галоген, амино, -OCF3, -CF3 -CN, -XR12, -C(=O)R13, -N(R12)C(=O)R13, -(C1-9 алкил)nN(R12)2, -(C1-9 алкил)nN(R12)SO2R13 и -SO2R13;
каждый R10 независимо выбран из группы, включающей H, C1-9 алкил, -(C1-9 алкил)nN(R14)2, -(C1-9 алкил)nкарбоциклилR8, -(C1-9 алкил)nгетероциклилR8, -(C1-9 алкил)nарилR8 и -(C1-9
алкил)nгетероарилR8;
каждый R11 независимо выбран из группы, включающей C1-9 алкил, -N(R14)2, -(C1-9 алкил)nкарбоциклилR8, -(C1-9 алкил)nгетероциклилR8, -(C1-9 алкил)nарилR8 и -(C1-9 алкил)nгетероарилR8;
каждый R12 независимо выбран из группы, включающей H, C1-9 алкил, -(C1-9 алкил)nN(R14)2, -(C1-9 алкил)nкарбоциклил, -(C1-9 алкил)nгетероциклил, -(C1-9 алкил)nарил и -(C1-9 алкил)nгетероарил;
каждый R13 независимо выбран из группы, включающей C1-9 алкил, -N(R14)2, -(C1-9 алкил)nкарбоциклил, -(C1-9 алкил)nгетероциклил, -(C1-9 алкил)nарил и -(C1-9 алкил)nгетероарил;
каждый R14 независимо выбран из группы, включающей H, C1-3 алкил, карбоциклил и арил;
каждый X выбран из группы, включающей связь, -O- и -S-; и
каждый n равен 0 или 1.
2. Соединение по п. 1, где n равен 0.
3. Соединение по п. 1, где n равен 1.
4. Соединение по п. 1, где X представляет собой O.
5. Соединение по п. 1, где R1, R2 и R4 представляют собой H.
6. Соединение по п. 1, где R3 представляет собой гетероарилR6.
7. Соединение по п. 6, где гетероарил представляет собой 3-пиридил.
8. Соединение по п. 6, где гетероарил представляет собой 5-пиримидинил.
9. Соединение по п. 6, где гетероарил представляет собой 4-пиридазинил.
10. Соединение по п. 6, где R6 обозначает один заместитель и выбран из группы, включающей H и -N(R9)C(=O)R10.
11. Соединение по п. 1, где R5 представляет собой гетероарилR7.
12. Соединение по п. 11, где гетероарил представляет собой 3-пиридил.
13. Соединение по п. 11, где гетероарил представляет собой 5-пиримидинил.
14. Соединение по п. 11, где гетероарил представляет собой 4-пиридазинил.
15. Соединение по п. 11, где R7 обозначает один заместитель и выбран из группы, включающей H, галоген, -OCF3, -CF3, -(C1-9 алкил)nгетероциклилR9, -(C1-9 алкил)nN(R10)2, -(C1-9 алкил)nN(R10)SO2R11 и -N(R10)C(=O)R11.
16. Соединение или его фармацевтически приемлемая соль или пролекарство, имеющее структуру формулы Ia:
Figure 00000010
где:
R3 выбран из группы, включающей арилR6 и гетероарилR6;
при условии, что, когда R3 представляет собой гетероарил, гетероарил не выбран из группы, включающей изохинолин, 1H-пирроло[2,3-c]пиридин и тетразол;
R5 выбран из группы, включающей -карбоциклилR7, -
гетероциклилR7, -арилR7, -гетероарилR7 и -(C1-2 алкил)гетероарилR7;
при условии, что R5 не представляет собой 4-пиридилR7, когда R3 выбран из группы, включающей 3-пиридилR6, 4-пиридилR6, 2-пиридилR6, фенилR6, тиазолR6, имидазолR6, пиримидинR6, оксазолR6,
Figure 00000011
Figure 00000012
и R6 и R7 оба представляют собой H;
при условии, что R5 не представляет собой -(CH2)(3-пиридил)R7, когда R3 выбран из группы, включающей 3-пиридилR6, 4-пиридилR6 и тиазолR6, и R6 и R7 оба представляют собой H;
при условии, что R5 не представляет собой фенилR7, когда R3 представляет собой 4-пиридилR6, и R6 и R7 оба представляют собой H;
при условии, что R3 не представляет собой 3-пиридилR6, когда R5 выбран из группы, включающей фенилR7,
Figure 00000013
Figure 00000014
Figure 00000015
и R6 и R7 оба представляют собой H;
при условии, что R3 не представляет собой оксазолR6, когда R5 выбран из группы, включающей
Figure 00000016
и R6 представляет собой H;
при условии, что R3 не представляет собой тиазолR6, когда R5 выбран из группы, включающей
Figure 00000017
и R6 представляет собой H;
каждый R6 обозначает 1-2 заместителя, каждый выбран из группы, включающей H, C1-3 алкил, галоген, амино, -OCF3, -CF3, -CN, -OR10, -(C1-2 алкил)гетероциклилR8, -гетероциклилR8, -(C1-2 алкил)арилR8, -C(=O)R11, -N(R10)C(=O)R11 и -(C1-2 алкил)N(R10)2;
каждый R7 обозначает 1-2 заместителя, каждый выбран из группы, включающей H, C1-3 алкил, галоген, амино, -OCF3, -CF3, -CN, -OR10, -(C1-2 алкил)гетероциклилR9, -гетероциклилR9, -арилR9, -(C1-2 алкил)арилR9, -C(=O)R11, -N(R10)C(=O)R11, -N(R10)2, -(C1-2 алкил)N(R10)2, -N(R10)SO2R11 и -SO2R11;
каждый R8 обозначает 1-2 заместителя, каждый выбран из группы, включающей H, C1-3 алкил, галоген, амино, OCF3, -CF3 -CN и -OR12;
каждый R9 обозначает 1-2 заместителя, каждый выбран из группы, включающей H, C1-3 алкил, галоген, амино, -OCF3, -CF3 -CN и -OR12;
каждый R10 независимо выбран из группы, включающей H, C1-3 алкил, -(C1-3 алкил)N(R14)2 и -арилR8;
каждый R11 независимо выбран из группы, включающей C1-3 алкил, -N(R14)2, -карбоциклилR8 и -гетероциклилR8;
каждый R12 независимо выбран из группы, включающей H и C1-3 алкил;
каждый R14 независимо выбран из группы, включающей H, C1-3 алкил и карбоциклил.
17. Соединение по п. 1, имеющее структуру, выбранную из группы, включающей:
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
18. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
19. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
20. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
21. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
22. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
23. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
24. Соединение по п. 17, имеющее структуру, выбранную из группы, включающей:
Figure 00000073
Figure 00000074
Figure 00000075
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