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RU2010139577A - Ингибиторы 11бета-гидроксистероиддегидрогеназы - Google Patents

Ингибиторы 11бета-гидроксистероиддегидрогеназы Download PDF

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Publication number
RU2010139577A
RU2010139577A RU2010139577/04A RU2010139577A RU2010139577A RU 2010139577 A RU2010139577 A RU 2010139577A RU 2010139577/04 A RU2010139577/04 A RU 2010139577/04A RU 2010139577 A RU2010139577 A RU 2010139577A RU 2010139577 A RU2010139577 A RU 2010139577A
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RU2010139577/04A
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Найджел ВИКЕР (GB)
Найджел ВИКЕР
Сяндон СУ (GB)
Сяндон СУ
Фабьенн ПРАДО-КАГГИАНО (GB)
Фабьенн ПРАДО-КАГГИАНО
Барри Виктор Ллойд ПОТТЕР (GB)
Барри Виктор Ллойд Поттер
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Стерикс Лимитед (Gb)
Стерикс Лимитед
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Publication of RU2010139577A publication Critical patent/RU2010139577A/ru

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Abstract

1. Соединение формулы ! R1-CO-X-Y-Z-R2, ! в которой ! Х и Z каждый представляет собой необязательные группы, независимо выбранные из насыщенных или ненасыщенных углеродных цепей, имеющих 1-3 атома углерода в длину, ! Y представляет собой SO, S, SO2, CH=CH, CH2CH2 или О, ! R1 выбран из следующих групп ! ! ! где линия обозначает точку присоединения, ! R2 представляет собой гетероарильную группу, включающую 15 необязательно замещенное 5- или 6-членное кольцо, где кольцо содержит только углерод и по крайней мере один азот, или содержит только углерод и по крайней мере два азота и по крайней мере одну серу, ! и где (i) когда R1 представляет собой , и группа -CO-X-Y-Z-представляет собой CO-CH2-SO, СО-СН2-S или CO-CH2-SO2, то R2 является отличным от , и ! (ii) когда R1 представляет собой, , и группа -CO-X-Y-Z- представляет собой -СО-СН2-О-, то R2 является отличным от . ! 2. Соединение по п.1, где R1 представляет собой . ! 3. Соединение по п.1, где R1 представляет собой . ! 4. Соединение по п.1, где R1 выбран из следующих групп ! . ! 5. Соединение по любому из пп.1-4 формулы ! R1-CO-X-Y-Z-R2, ! где Х и Z независимо выбраны из насыщенных или ненасыщенных углеродных цепей, имеющих 1-3 атома углерода в длину, и Y представляет собой SO, S, SO2, CH=CH, CH2CH2 или О. ! 6. Соединение по любому из пп.1-4 формулы ! R1-CO-X-Y-R2, ! где Х выбран из насыщенных или ненасыщенных углеродных цепей, имеющих в длину 1-3 атома углерода, и Y представляет собой SO, S, SO2, СН=СН, СН2СН2 или О. ! 7. Соединение по любому из пп.1-4 формулы ! R1-CO-Y-Z-R2, ! где Z выбран из насыщенных или ненасыщенных углеродных цепей, имеющих в длину 1-3 атомов углерода, и Y представляет собой SO, S, SO2, СН=СН, СН2СН2 или О. ! 8. Соединение по любому из пп.1-4 формулы ! R1-CO-Y-R2, ! где Y представляет собой SO,

Claims (45)

1. Соединение формулы
R1-CO-X-Y-Z-R2,
в которой
Х и Z каждый представляет собой необязательные группы, независимо выбранные из насыщенных или ненасыщенных углеродных цепей, имеющих 1-3 атома углерода в длину,
Y представляет собой SO, S, SO2, CH=CH, CH2CH2 или О,
R1 выбран из следующих групп
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
где линия
Figure 00000008
обозначает точку присоединения,
R2 представляет собой гетероарильную группу, включающую 15 необязательно замещенное 5- или 6-членное кольцо, где кольцо содержит только углерод и по крайней мере один азот, или содержит только углерод и по крайней мере два азота и по крайней мере одну серу,
и где (i) когда R1 представляет собой
Figure 00000001
, и группа -CO-X-Y-Z-представляет собой CO-CH2-SO, СО-СН2-S или CO-CH2-SO2, то R2 является отличным от
Figure 00000009
, и
(ii) когда R1 представляет собой,
Figure 00000001
, и группа -CO-X-Y-Z- представляет собой -СО-СН2-О-, то R2 является отличным от
Figure 00000010
.
2. Соединение по п.1, где R1 представляет собой
Figure 00000001
.
3. Соединение по п.1, где R1 представляет собой
Figure 00000011
.
4. Соединение по п.1, где R1 выбран из следующих групп
Figure 00000003
Figure 00000012
Figure 00000005
Figure 00000006
Figure 00000007
.
5. Соединение по любому из пп.1-4 формулы
R1-CO-X-Y-Z-R2,
где Х и Z независимо выбраны из насыщенных или ненасыщенных углеродных цепей, имеющих 1-3 атома углерода в длину, и Y представляет собой SO, S, SO2, CH=CH, CH2CH2 или О.
6. Соединение по любому из пп.1-4 формулы
R1-CO-X-Y-R2,
где Х выбран из насыщенных или ненасыщенных углеродных цепей, имеющих в длину 1-3 атома углерода, и Y представляет собой SO, S, SO2, СН=СН, СН2СН2 или О.
7. Соединение по любому из пп.1-4 формулы
R1-CO-Y-Z-R2,
где Z выбран из насыщенных или ненасыщенных углеродных цепей, имеющих в длину 1-3 атомов углерода, и Y представляет собой SO, S, SO2, СН=СН, СН2СН2 или О.
8. Соединение по любому из пп.1-4 формулы
R1-CO-Y-R2,
где Y представляет собой SO, S, SO2, CH=CH, CH2CH2 или О.
9. Соединение по п.1, где Х представляет собой C1-3алкилен.
10. Соединение по п.1, где Х выбран из СН2 и С(CH3)2.
11. Соединение по п.1, где Z представляет собой С1-3алкилен.
12. Соединение по п.1, где Z представляет собой СН2.
13. Соединение по п.1, где Х представляет собой С1-3алкилен и Z представляет собой С1-3алкилен.
14. Соединение по п.1, где Х выбран из СН2 и С(СН3)2, и Z представляет собой СН2.
15. Соединение по п.1 формулы
R1-CO-X-Y-Z-R2,
где Х представляет собой С1-3алкилен;
Z является необязательной группой, представляющей собой С1-3алкилен, и Y представляет собой SO, S или SO2.
16. Соединение по п.15, где Х выбран из СН2 и С(СН3)2, и Z является необязательной группой CH2.
17. Соединение по п.1 формулы
R1-CO-X-Y-Z-R2,
где Х представляет собой C1-3алкилен;
Z является необязательной группой, выбранной из C1-3алкилена.
18. Соединение по п.17, где Х представляет собой CH2 и Z является необязательной группой СН2.
19. Соединение по п.1 формулы
R1-CO-Y-R2,
где Y представляет собой СН=СН или СН2СН2.
20. Соединение по п.1, где группа -CO-X-Y-Z- выбрана из COCH2S, COCH2SO, COCH2SO2, COCH2SCH2, COCH2SOCH2, COCH2SO2CH2, СОС(СН3)2SO, СОСН2O, СОСН2OСН2, СОСН=СН и СОСН2СН2.
21. Соединение по п.1, где R2 является гетероарильной группой, включающей необязательно замещенное 5- или 6-членное кольцо, где кольцо содержит только углерод и по крайней мере один азот.
22. Соединение по п.1, где R2 является гетероарильной группой, включающей необязательно замещенное 5-членное кольцо, где кольцо содержит только углерод и по крайней мере один азот.
23. Соединение по п.1, где R2 является гетероарильной группой, включающей необязательно замещенное 6-членное кольцо, где кольцо содержит только углерод и по крайней мере один азот.
24. Соединение по п.1, где необязательные заместители группы R2 вместе образуют дополнительное кольцо, сконденсированное с 5- или 6-членным гетероарильным кольцом.
25. Соединение по п.1, где R2 является гетероарильной группой, включающей необязательно замещенное 5- или 6-членное кольцо, где кольцо содержит только углерод и по крайней мере два азота и по крайней мере одну серу.
26. Соединение по п.1, где группа R2 представляет собой необязательно замещенное 5- или 6-членное гетероарильное кольцо, выбранное из
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
.
27. Соединение по п.1, где группа R2 представляет собой необязательно замещенное 5- или 6-членное гетероарильное кольцо, выбранное из
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
где линия
Figure 00000025
обозначает точку присоединения.
28. Соединение по п.1, где группа R2 необязательно замещена заместителями, независимо выбранными из гидрокарбильных групп, галогенов, гидроксильных групп, карбонила, аминов и амидов.
29. Соединение по п.1, где один или каждый необязательный заместитель группы R2 независимо выбран из оксигрупп, простых эфирных групп, тиоэфирных групп, арильных групп, арильных групп, замещенных одной или несколькими алкильными группами или галогенами, алкильных групп, алкоксигрупп, галогеналкильных групп, галогенов, амидов и карбонильных групп, или вместе образуют арильную группу, сконденсированную с 5- или 6-членным гетероарильным кольцом.
30. Соединение по п.1, где один или каждый необязательный заместитель группы R2 независимо выбран из C1-5алкильных групп, С3-6циклоалкильных групп, простых эфирных групп, содержащих от 1 до 5 атомов углерода, тиоэфирных групп, содержащих от 1 до 5 атомов углерода, C1-5алкоксигрупп, C1-5галогеналкильных групп, галогенов, оксигрупп, аминов, фенила, фурана, тиофена, -(C1-5алкил)фенильных групп, замещенных одним или несколькими галогенами, амидами, алкиламидами, диалкиламидами, ациламидами, или вместе образуют фенильную группу, сконденсированную с 5- или 6-членным гетероарильным кольцом.
31. Соединение по п.1, где один или каждый необязательный заместитель группы R2 независимо выбран из метила, метоксигруппы, оксигруппы, хлора, СН(СН3)2, -S-Me, -СН2-O-Ме, СF3, NMe2, COOH, C=ONH2, C=ONHMe, C=ONMe2, С=ОNНСН2СН3, -NH2, фенила, фурана, тиофена, -NH-C=OMe, -NH-С=O-циклопропана, циклопропана, СН2-4-хлорфенила, или вместе образуют фенильную группу, сконденсированную с 5- или 6-членным гетероарильным кольцом.
32. Соединение по п.1, где группа R2 выбрана из
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
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
.
33. Соединение по п.1, где группа R2 выбрана из
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
    
где линия
Figure 00000097
обозначает точку присоединения.
34. Соединение по п.1, выбранное из следующих соединений
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
Figure 00000118
Figure 00000119
Figure 00000120
Figure 00000121
Figure 00000120
Figure 00000122
Figure 00000123
Figure 00000124
Figure 00000125
Figure 00000126
Figure 00000127
Figure 00000128
Figure 00000129
Figure 00000130
Figure 00000131
Figure 00000132
Figure 00000133
Figure 00000134
Figure 00000135
Figure 00000136
Figure 00000137
Figure 00000138
Figure 00000139
Figure 00000140
Figure 00000141
Figure 00000142
Figure 00000143
Figure 00000144
Figure 00000145
Figure 00000146
Figure 00000147
Figure 00000148
Figure 00000149
Figure 00000150
Figure 00000151
Figure 00000152
Figure 00000153
Figure 00000154
Figure 00000155
Figure 00000156
Figure 00000157
Figure 00000158
Figure 00000159
Figure 00000160
Figure 00000161
Figure 00000162
Figure 00000163
Figure 00000164
Figure 00000165
Figure 00000166
Figure 00000167
Figure 00000168
Figure 00000169
Figure 00000170
Figure 00000171
Figure 00000172
Figure 00000173
Figure 00000174
Figure 00000175
Figure 00000176
Figure 00000177
Figure 00000178
Figure 00000179
Figure 00000180
Figure 00000181
  
Figure 00000182
Figure 00000183
Figure 00000184
Figure 00000185
Figure 00000186
Figure 00000187
Figure 00000188
Figure 00000189
Figure 00000190
Figure 00000191
Figure 00000192
Figure 00000193
Figure 00000194
Figure 00000195
Figure 00000196
Figure 00000197
Figure 00000198
Figure 00000199
Figure 00000200
Figure 00000201
Figure 00000202
Figure 00000203
Figure 00000204
Figure 00000205
.
35. Фармацевтическая композиция, включающая соединение по любому из пп.1-34, необязательно в смеси с фармацевтически приемлемым носителем, разбавителем, эксципиентом или адьювантом.
36. Соединение по любому из пп.1-34 для применения в медицине.
37. Применение соединения по любому из пп.1-34 для изготовления лекарственного средства, предназначенного для применения в терапии состояния или заболевания, связанного с 11β-HSD.
38. Соединение по любому из пп.1-34 для применения в терапии состояния или заболевания, связанного с 11β-HSD.
39. Применение или соединение по п.37 или 38, где состояние или заболевание выбрано из группы, состоящей из метаболических нарушений, таких как диабет и ожирение; сердечно-сосудистых заболеваний, такого как гипертония; глаукомы; воспалительных заболеваний, таких как артрит или астма; иммунных заболеваний; заболеваний костной ткани, такого как остеопороз; рака; задержки внутриутробного развития; синдрома явного избытка минералокортикоидов (АМЕ); синдрома поликистозных яичников (PCOS); гирсутизма; акне; олиго- или аменорреи; адренокортикальной аденомы и карциномы; синдрома Кушинга; гипофизарных опухолей; инвазивных карцином; рака молочной железы и рака эндометрия.
40. Применение соединения по любому из пп.1-34 для изготовления лекарственного средства, предназначенного для применения в терапии состояния или заболевания, связанного с нежелательными уровнями 11β-HSD.
41. Соединение по любому из пп.1-34 для применения в терапии состояния или заболевания, связанного с нежелательными уровнями 11β-HSD.
42. Применение соединения по любому из пп.1-34 для изготовления фармацевтического средства для модулирования активности 11β-HSD.
43. Соединение по любому из пп.1-34 для модулирования активности 11β-HSD.
44. Применение соединения по любому из пп.1-34 для изготовления фармацевтического средства для ингибирования активности 11β-HSD.
45. Соединение по любому из пп.1-34 для ингибирования активности 11β-HSD.
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