RU2472783C2 - Аминные производные и их применение в бета-2-адренорецептор-опосредованных заболеваниях - Google Patents

Аминные производные и их применение в бета-2-адренорецептор-опосредованных заболеваниях Download PDF

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RU2472783C2
RU2472783C2 RU2009119912/04A RU2009119912A RU2472783C2 RU 2472783 C2 RU2472783 C2 RU 2472783C2 RU 2009119912/04 A RU2009119912/04 A RU 2009119912/04A RU 2009119912 A RU2009119912 A RU 2009119912A RU 2472783 C2 RU2472783 C2 RU 2472783C2
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Лилиан Алькараз
Роджер Виктор Боннерт
Стивен Коннолли
Энтони Рональд Кук
Эдриан ФИШЕР
Александр ХАМФРИЗ
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Abstract

Изобретение относится к соединению формулы (I), где Аr представляет собой каждый из R2, R3, R4, R5; R4' и R5' представляет собой водород; А представляет собой С(O); D представляет собой кислород или NR8; Е представляет собой CR63R64CR65R66; R63 и R64 представляют собой водород; R65 и R66 независимо представляют собой водород или С1-4алкил; k равно 0; m равно 1; R6 представляет собой группу -(X)p-Y-(Z)q-R10, или R6 представляет собой α- или β-разветвленный С3-6алкил (возможно замещенный С6циклоалкилом); Х и Z независимо представляют собой С1-4алкиленовую группу; р и q независимо равны 0 или 1; Y представляет собой связь; R8 представляет собой водород; R10 представляет собой водород или насыщенную 5-7-членную кольцевую систему; R7 представляет собой 6-членное ароматическое кольцо, возможно замещенное галогеном, карбоксилом, С1-6алкилом, С1-2алкокси или 5-членным гетероароматическим кольцом (которое возможно замещено С1-6алкилом); или его фармацевтически приемлемой соли. Соединения формулы (1) или ею фармацевтически приемлемую соль используют для изготовления лекарственного средства для лечения респираторного дистресс-синдрома (ARDS), эмфиземы легких, бронхита, бронхоэктаза, хронического обструктивного заболевания легких (COPD), астмы или ринита. 3 н. и 4 з.п. ф-лы, 1 табл., 102 пр.
Figure 00000156
где:

Description

Текст описания приведен в факсимильном виде.
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Claims (7)

1. Соединение формулы (I):
Figure 00000154

где Ar представляет собой
Figure 00000155

каждый из R2, R3, R4, R5, R4' и R5' представляет собой водород;
А представляет собой С(O);
D представляет собой кислород или NR8;
Е представляет собой CR63R64CR65R66;
R63 и R64 представляют собой водород;
R65 и R66 независимо представляют собой водород или С1-4алкил;
k равно 0;
m равно 1;
R6 представляет собой группу -(X)p-Y-(Z)q-R10, или R10 представляет собой α- или β-разветвленный С3-6алкил (возможно замещенный С6циклоалкилом);
X и Z независимо представляют собой С1-4алкиленовую группу;
р и q независимо равны 0 или 1;
Y представляет собой связь;
R8 представляет собой водород;
R10 представляет собой водород или насыщенную 5-7-членную кольцевую систему;
R7 представляет собой 6-членное ароматическое кольцо, возможно замещенное галогеном, карбоксилом, С1-6алкилом, С1-2алкокси или 5-членным гетероароматическим кольцом (которое возможно замещено С1-6алкилом);
или его фармацевтически приемлемая соль.
2. Соединение формулы (I) по п.1, где D представляет собой кислород.
3. Соединение формулы (I) по п.1, где Е представляет собой СН2СН2.
4. Соединение формулы (I) по п.1, где R6 представляет собой циклогексил, циклогептил, гексан-2-ил, бутан-2-ил или 3-метилбутан-2-ил.
5. Соединение формулы (I) по п.1, где R7 представляет собой 6-членное ароматическое кольцо, возможно замещенное галогеном, карбоксилом, С1-6алкилом или С1-2алкокси.
6. Фармацевтическая композиция, полезная для лечения респираторного дистресс-синдрома (ARDS), эмфиземы легких, бронхита, бронхоэктаза, хронического обструктивного заболевания легких (COPD), астмы или ринита, содержащая соединение формулы (I) или его фармацевтически приемлемую соль по п.1 вместе с фармацевтически приемлемым адъювантом, разбавителем или носителем.
7. Применение соединения формулы (I) или его фармацевтически приемлемой соли по п.1 в изготовлении лекарственного средства для применения в лечении респираторного дистресс-синдрома взрослых (ARDS), эмфиземы легких, бронхита, бронхоэктаза, хронического обструктивного заболевания легких (COPD), астмы и ринита.
RU2009119912/04A 2006-12-20 2007-12-19 Аминные производные и их применение в бета-2-адренорецептор-опосредованных заболеваниях RU2472783C2 (ru)

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CN102124003A (zh) 2008-06-18 2011-07-13 阿斯利康(瑞典)有限公司 作为治疗呼吸系统疾病的β2肾上腺素受体拮抗剂的苯并噁嗪酮衍生物
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GB0913342D0 (en) * 2009-07-31 2009-09-16 Astrazeneca Ab Compounds - 801
WO2011048409A1 (en) 2009-10-20 2011-04-28 Astrazeneca Ab Cyclic amine derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
US9598381B2 (en) * 2014-07-31 2017-03-21 Abbvie Inc. SMYD2 inhibitors
CN107188865B (zh) * 2016-03-14 2019-08-27 益方生物科技（上海）有限公司 苯并噁嗪化合物及其制备方法和用途

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