RU2005113238A - Спиросоединения, содержащие их лекарственные композиции и промежуточные соединения указанных соединений - Google Patents

Спиросоединения, содержащие их лекарственные композиции и промежуточные соединения указанных соединений Download PDF

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RU2005113238A
RU2005113238A RU2005113238/04A RU2005113238A RU2005113238A RU 2005113238 A RU2005113238 A RU 2005113238A RU 2005113238/04 A RU2005113238/04 A RU 2005113238/04A RU 2005113238 A RU2005113238 A RU 2005113238A RU 2005113238 A RU2005113238 A RU 2005113238A
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alkyl group
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ring
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Нобухиде ВАТАНАБЕ (JP)
Нобухиде ВАТАНАБЕ
Хироси НАКАГАВА (JP)
Хироси Накагава
Дзун-ити ЦУДЗИ (JP)
Дзун-ити ЦУДЗИ
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Хисао МИНАТО
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Акихиса ИКЕНО
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Тие КОХАЙАКАВА
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Дайниппон Фармасьютикал Ко., Лтд. (JP)
Дайниппон Фармасьютикал Ко., Лтд.
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Claims (14)

1. Спиросоединение, представленное следующей формулой (I)
Figure 00000001
где R1 и R2 являются одинаковыми или разными и каждый представляет собой атом водорода, атом фтора, атом хлора или С1-6-алкильную группу,
n равно 1, 2 или 3,
связь, содержащая пунктирную линию, означает простую связь или двойную связь,
А представляет собой -(СН2)р-N(R3)(R4); -X-(СН2)q-N(R3)(R4); группу, представленную следующей формулой (а)
Figure 00000002
группу, представленную следующей формулой (b)
Figure 00000003
или группу, представленную следующей формулой (с)
Figure 00000004
где р равно 1, 2 или 3,
Х представляет собой атом кислорода или атом серы,
q равно 2 или 3,
R3 и R4 являются одинаковыми или разными и каждый из них представляет собой С1-6-алкильную группу или фенил-С1-4-алкильную группу, или R3 и R4, необязательно, вместе с соседним атомом азота образуют пирролидиновое кольцо, пиперидиновое кольцо, гомопиперидиновое кольцо, пиперазиновое кольцо или морфолиновое кольцо, каждое из которых, необязательно, замещено одной или двумя группами, выбранными из С1-6-алкила, фенила и бензила,
R5 представляет собой С1-6-алкильную группу, С3-8-циклоалкильную группу или С3-8-циклоалкил-С1-4-алкильную группу,
R6 представляет собой атом водорода или С1-4-алкильную группу, и
r, s и t каждый независимо принимают значения один или два, или
его фармацевтически приемлемая кислотно-аддитивная соль.
2. Соединение по п.1, где А представляет собой -Х-(CH2)q-N(R3)(R4) (где Х, R3, R4 и q имеют значения, определенные в п. 1) или его фармацевтически приемлемая кислотно-аддитивная соль.
3. Спиросоединение, представленное следующей формулой (I-1а)
Figure 00000005
где R11 и R21 являются одинаковыми или разными и каждый представляет собой атом водорода, атом фтора или атом хлора,
R31 и R41 вместе с соседним атомом азота образуют пирролидиновое кольцо, пиперидиновое кольцо или гомопиперидиновое кольцо, каждое, необязательно, замещенное одной или двумя метильными группами, или его фармацевтически приемлемая кислотно-аддитивная соль.
4. Спиросоединение, представленное следующей формулой (I-2а)
Figure 00000006
где R11 и R21 являются одинаковыми или разными и каждый представляет собой атом водорода, атом фтора или атом хлора,
R31 и R41 вместе с соседним атомом азота образуют пирролидиновое кольцо, пиперидиновое кольцо или гомопиперидиновое кольцо, каждое, необязательно, замещенное одной или двумя метильными группами, или его фармацевтически приемлемая кислотно-аддитивная соль.
5. (1R*,3S*)-3-[4-(2-Пиперидиноэтокси)фенил]-1,1'-спиробииндан-5,5'-диол или его фармацевтически приемлемая кислотно-аддитивная соль.
6. 3-[4-(2-Пиперидиноэтокси)фенил]спиро[инден-1,1'-индан]-5,5'-диол или его фармацевтически приемлемая кислотно-аддитивная соль.
7. Соединение, выбранное из (+)-3-[4-(2-пиперидиноэтокси)фенил]спиро[инден-1,1'-индан]-5,5'-диола и (-)-3-[4-(2-пиперидиноэтокси)фенил]спиро[инден-1,1'-индан]-5,5'-диола или их фармацевтически приемлемой кислотно-аддитивной соли.
8. Фармацевтическая композиция, содержащая в качестве активного ингредиента соединение по любому из пп.1-7 или его фармацевтически приемлемую кислотно-аддитивную соль.
9. Фармацевтическая композиция по п. 8, которую используют для профилактики и/или лечения остеопороза, климактерического синдрома или рака молочной железы.
10. Применение соединения по любому из пп.1-7 или его фармацевтически приемлемой кислотно-аддитивной соли для профилактики или лечения остеопороза, климактерического синдрома или рака молочной железы.
11. Способ профилактики или лечения остеопороза, климактерического синдрома или рака молочной железы, который включает введение эффективного количества соединения по любому пп.1-7 или его фармацевтически приемлемой кислотно-аддитивной соли пациенту с остеопорозом, климактерическим синдромом или раком молочной железы.
12. Коммерческая упаковка, содержащая фармацевтическую композицию по п.8 или 9 и относящееся к ней описание, причем описание точно определяет, что фармацевтическая композиция может или должна быть использована для профилактики или лечения остеопороза, климактерического синдрома или рака молочной железы.
13. Спиросоединение, представленное следующей формулой (II)
Figure 00000007
где R1 и R2 являются одинаковыми или разными и каждый представляет собой атом водорода, атом фтора, атом хлора или С1-6-алкильную группу,
n равно 1, 2 или 3,
А' представляет собой -ОН, -ОСН2СН=СН2, -OSO2CF3, -(СН2)р-N(R3)(R4); -X-(СН2)q-N(R3)(R4); группу, представленную следующей формулой (а)
Figure 00000008
группу, представленную следующей формулой (b)
Figure 00000003
или группу, представленную следующей формулой (с)
Figure 00000004
где р равно 1, 2 или 3,
Х представляет собой атом кислорода или атом серы,
q равно 2 или 3,
R3 и R4 являются одинаковыми или разными и каждый из них представляет собой С1-6-алкильную группу или фенил-С1-4-алкильную группу, или R3 и R4, необязательно, вместе с соседним атомом азота образуют пирролидиновое кольцо, пиперидиновое кольцо, гомопиперидиновое кольцо, пиперазиновое кольцо или морфолиновое кольцо, каждое из которых, необязательно, замещено одной или двумя группами, выбранными из С1-6-алкила, фенила и бензила,
R5 представляет собой С1-6-алкильную группу, С3-8-циклоалкильную группу или С3-8-циклоалкил-С1-4-алкильную группу,
R6 представляет собой атом водорода или С1-4-алкильную группу, и
r, s и t каждый независимо принимают значения один или два.
14. Спиросоединение, представленное следующей формулой (III)
Figure 00000009
где n равно 1, 2 или 3.
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