RU2009105496A - Аминоиндановое производное или его соль - Google Patents
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Abstract
1. Соединение общей формулы (I) или его соль: ! [Химическая структура 8] ! ! где радикалы в формуле (I) имеют следующие значения в указанном порядке: ! кольцо A представляет собой 5- или 6-членное гетероциклическое кольцо или бензольное кольцо, ! X представляет собой C(R4)(R5), O, S или N(R12), ! R1 представляет собой низший алкил, циклоалкил, -низший алкиленарил, арил, который может быть замещенным, гетероарил, который может быть замещенным, или низший алкил, замещенный одним или несколькими атомами галогена, ! R2 и R3 являются одинаковыми или различными, каждый представляет собой низший алкил или арил, ! R4 и R5 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -О-низший алкил, -OH, -низший алкилен-OH или -низший алкилен-O-низший алкил, ! R6-R9 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -O-низший алкил, атом галогена, низший алкил, замещенный одним или несколькими атомами галогена, OH, CN, низший алкенил или азотсодержащую гетероциклическую группу, ! R10 и R11 являются одинаковыми или различными, каждый представляет собой атом водорода или низший алкил, и ! R12 представляет собой атом водорода или низший алкил, ! при условии, что R2 и R3 могут быть взяты вместе со смежным атомом углерода, с образованием циклоалкила. ! 2. Соединение общей формулы (Ia) или его соль: ! [Химическая структура 9] ! ! где радикалы в формуле (Ia), представленной выше, имеют следующие значения в указанном порядке: ! R1 представляет собой низший алкил, циклоалкил, -низший алкиленарил, арил, который может быть замещенным, гетероарил, который может быть замещенным, или низший алкил, замещенный одним ил
Claims (10)
1. Соединение общей формулы (I) или его соль:
[Химическая структура 8]
где радикалы в формуле (I) имеют следующие значения в указанном порядке:
кольцо A представляет собой 5- или 6-членное гетероциклическое кольцо или бензольное кольцо,
X представляет собой C(R4)(R5), O, S или N(R12),
R1 представляет собой низший алкил, циклоалкил, -низший алкиленарил, арил, который может быть замещенным, гетероарил, который может быть замещенным, или низший алкил, замещенный одним или несколькими атомами галогена,
R2 и R3 являются одинаковыми или различными, каждый представляет собой низший алкил или арил,
R4 и R5 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -О-низший алкил, -OH, -низший алкилен-OH или -низший алкилен-O-низший алкил,
R6-R9 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -O-низший алкил, атом галогена, низший алкил, замещенный одним или несколькими атомами галогена, OH, CN, низший алкенил или азотсодержащую гетероциклическую группу,
R10 и R11 являются одинаковыми или различными, каждый представляет собой атом водорода или низший алкил, и
R12 представляет собой атом водорода или низший алкил,
при условии, что R2 и R3 могут быть взяты вместе со смежным атомом углерода, с образованием циклоалкила.
2. Соединение общей формулы (Ia) или его соль:
[Химическая структура 9]
где радикалы в формуле (Ia), представленной выше, имеют следующие значения в указанном порядке:
R1 представляет собой низший алкил, циклоалкил, -низший алкиленарил, арил, который может быть замещенным, гетероарил, который может быть замещенным, или низший алкил, замещенный одним или несколькими атомами галогена,
R2 и R3 являются одинаковыми или различными, каждый представляет собой низший алкил или арил,
R4 и R5 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -O-низший алкил, -OH, -низший алкилен-OH или -низший алкилен-O-низший алкил,
R6-R9 являются одинаковыми или различными, каждый представляет собой атом водорода, низший алкил, -O-низший алкил, атом галогена, низший алкил, замещенный одним или несколькими атомами галогена, OH, CN, низший алкенил или азотсодержащую гетероциклическую группу,
R10 и R11 являются одинаковыми или различными, каждый представляет собой атом водорода или низший алкил,
при условии, что R2 и R3 могут быть взяты вместе со смежным атомом углерода с образованием циклоалкила.
3. Соединение или его соль по п.2, где каждый R4, R5, R10 и R11 в формуле (Ia), указанной выше, представляет собой атом водорода.
4. Соединение или его соль по п.3, где R2 и R3 в формуле (Ia), указанной выше, являются одинаковыми или различными, и каждый представляет собой низший алкил или циклоалкил, образованный в комбинации с соседним атомом углерода.
5. Соединение или его соль по п.1, которое выбрано из 2,2-диметил-1-фенилиндан-1-амина, 1-(4-фторфенил)-2,2-диметилиндан-1-амина, 1-(2-метоксифенил)-2,2-диметилиндан-1-амина, 1-(3-метоксифенил)-2,2-диметилиндан-1-амина, 1,2,2-триметилиндан-1-амина, 1,2,2,5-тетраметилиндан-1-амина, 1,2,2,6-тетраметилиндан-1-амина, 4-фтор-1,2,2-триметилиндан-1-амина, 5-фтор-1,2,2-триметилиндан-1-амина, 7-фтор-1,2,2-триметилиндан-1-амина, 5-метокси-1,2,2-триметилиндан-1-амина, 6-метокси-1,2,2-триметилиндан-1-амина, 6-изопропокси-1,2,2-триметилиндан-1-амина, 1-этил-2,2-диметилиндан-1-амина, 1-изопропил-2,2-диметилиндан-1-амина, 1′-метил-1′,3′-дигидроспиро[циклопропан-1,2′-индин]-1′-амина, 2,4,5,5-тетраметил-5,5-дигидро-4H-циклопента[b]тиофен-4-амина.
6. Фармацевтическая композиция, содержащая соединение или его соль по п.1 или 2.
7. Фармацевтическая композиция по п.6, которая представляет собой антагонист NMDA рецептора.
8. Фармацевтическая композиция по п.6, которая представляет собой терапевтический агент для лечения деменции.
9. Применение соединения или его соли по п.1 или 2 для получения антагониста NMDA рецептора или терапевтического агента для лечения деменции.
10. Способ лечения деменции, включающий введение пациенту терапевтически эффективного количества соединения или его соли по п.1 или 2.
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EP2042480A4 (en) | 2011-11-23 |
NO341827B1 (no) | 2018-01-29 |
WO2008010481A1 (fr) | 2008-01-24 |
ES2412384T3 (es) | 2013-07-11 |
CN101489984A (zh) | 2009-07-22 |
MX2009000648A (es) | 2009-01-30 |
AU2007274420B2 (en) | 2011-12-08 |
SI2042480T1 (sl) | 2013-08-30 |
TWI391385B (zh) | 2013-04-01 |
CY1115373T1 (el) | 2017-01-04 |
BRPI0714142A2 (pt) | 2012-12-25 |
CA2657106C (en) | 2011-09-20 |
JPWO2008010481A1 (ja) | 2009-12-17 |
PT2042480E (pt) | 2013-06-24 |
KR101389209B1 (ko) | 2014-04-24 |
CA2657106A1 (en) | 2008-01-24 |
PL2042480T3 (pl) | 2013-09-30 |
IL196136A (en) | 2014-11-30 |
EP2042480B1 (en) | 2013-05-01 |
JP5109974B2 (ja) | 2012-12-26 |
AU2007274420A1 (en) | 2008-01-24 |
CN101489984B (zh) | 2013-04-03 |
TW200817351A (en) | 2008-04-16 |
KR20090031945A (ko) | 2009-03-30 |
EP2042480A1 (en) | 2009-04-01 |
US8013018B2 (en) | 2011-09-06 |
IL196136A0 (en) | 2009-09-22 |
NO20090762L (no) | 2009-03-16 |
US20090186916A1 (en) | 2009-07-23 |
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