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COMPOUNDS HAVING MUSCARINIC RECEPTOR AGONIST AND BETA-2-ADRENERGIC RECEPTOR AGONIST ACTIVITY

机译:具有肌肉受体激动剂和BETA-2-肾上腺素受体激动剂活性的化合物

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to organic chemistry and specifically to a compound of formula I ; and pharmaceutically acceptable salts and solvates thereof. In the compounds of formula I: Y is selected from Y2 and Y1, which are divalent groups of formula or , where A1 and A2 independently absent or selected from a group consisting of (C1-C12)alkylene, (C3-C8)cycloalkylene; B is absent or selected from a group consisting of phenylene, optionally substituted with one group selected (C1-C6)alkoxy; C is absent or selected from a group consisting of -O-, -N(R7) - or represents one of the following groups C1-C2 , where R7 in each case independently represents H or is selected from a group consisting of a straight or branched (C1-C8)alkyl, (C3-C8)cycloalkyl, phenyl, phenyl(C1-C6)alkyl, (C1-C8)alkylcarbonyl, (C3-C8)cycloalkylcarbonyl, phenylcarbonyl, (C1-C8)alkoxycarbonyl, (C1-C8)alkylaminocarbonyl, (C1-C10)alkylsulphanyl and phenylsulphonyl; and where R7 can optionally be further substituted with one group selected from halogen, -CN, (C1-C8)alkyl, halogen (C1-C8)alkyl, phenyl, phenyl (C1-C6)alkyl, (C1-C8)alkoxy, phenyl(C1-C8)alkoxy, (C3-C8)cycloalkyl, which is a saturated monocyclic group, D is absent or is selected from a group consisting of (C1-C12)alkylene and phenylene; n, n', n'' and n''' in each case independently equal to 0 or integer from 1 to 3; E is absent or is selected from -O-, -NR7-, -NR7-C(O)-, -C(O)-NR7-; G is absent or is phenylene or thienylene, optionally substituted with one or two substitutes selected from a group consisting of halogen atoms, (C1-C10)alkyl, phenyl, halophenyl, thienyl and (C1-C10)alkoxy; L is absent or is a divalent group selected from -C(O)-, (C1-C8)alkylcarbonylen and (C2-C8) alkenylcarbonylene; i is 1 or 2; i' is equal to 1 or 2; R1 in each case is independently selected from hydrogen and halogen; s is equal to 0. Also disclosed are a pharmaceutical composition, use of the compound of formula I and a device.;EFFECT: technical result is obtaining novel compounds acting as both muscarinic receptor antagonists and beta-2-adrenergic receptor agonists.;14 cl, 2 tbl, 31 ex
机译:技术领域本发明涉及有机化学,尤其涉及式I的化合物。 及其药学上可接受的盐和溶剂化物。在式I的化合物中:Y选自Y 2和Y 1,它们是式<图像文件=“ 00000225.JPG” he =“ 17” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 71” />或,其中A 1 和A 2 独立地不存在或选自由(C 1 -C 12 )亚烷基,(C 3 -C < Sub> 8 )亚环烷基; B不存在或选自由亚苯基组成的组,其任选地被一个选自(C 1 -C 6 )烷氧基的基团取代; C不存在或选自-O-,-N(R 7 )-或代表以下组之一C1-C2 <图像文件=“ 00000227.JPG” he =“ 28“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 95“ />,其中R 7 分别独立表示H或选自直链或支链(C 1 -C 8 )烷基,(C 3 -C 8 )环烷基,苯基,苯基(C < Sub> 1 -C 6 )烷基,(C 1 -C 8 )烷基羰基,(C 3 < / Sub> -C 8 )环烷基羰基,苯基羰基,(C 1 -C 8 )烷氧基羰基,(C 1 -C 8 )烷基氨基羰基,(C 1 -C 10 )烷基磺酰基和苯基磺酰基;并且其中R 7 可以任选地被选自卤素,-CN,(C 1 -C 8 )烷基,卤素中的一个基团进一步取代(C 1 -C 8 )烷基,苯基,苯基(C 1 -C 6 )烷基,( C 1 -C 8 )烷氧基,苯基(C 1 -C 8 )烷氧基,(C 3 -C 8 )环烷基,是饱和的单环基团,D不存在或选自(C 1 -C < Sub> 12 )亚烷基和亚苯基; n,n',n''和n'''分别独立地等于0或1到3的整数; E不存在或从-O-,-NR 7 -,-NR 7 -C(O)-,-C(O)-NR 中选择7 -;; G不存在或为亚苯基或亚噻吩基,任选地被一个或两个选自卤素原子,(C 1 -C 10 )烷基,苯基,卤代苯基,噻吩基和(C 1 -C 10 )烷氧基; L不存在或为选自-C(O)-,(C 1 -C 8 )烷基羰基和(C 2 -C 8 )烯基羰基;我是1或2;我等于1或2; R 1 分别独立地选自氢和卤素; s等于0。还公开了药物组合物,式I化合物的用途和装置。效果:技术结果是获得了同时用作毒蕈碱受体拮抗剂和β-2-肾上腺素能受体激动剂的新型化合物; 14 cl,2 tbl,31前

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