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    • 17. 发明授权
    • Long acting beta-2-agonists and their use as medicaments
    • 长效β-2-激动剂及其用作药物
    • US07632834B2
    • 2009-12-15
    • US12101462
    • 2008-04-11
    • Thierry BouyssouIngo KonetzkiPhilipp LustenbergerJuergen MackAndreas SchnappDieter WiedenmayerChristoph HoenkeKlaus Rudolf
    • Thierry BouyssouIngo KonetzkiPhilipp LustenbergerJuergen MackAndreas SchnappDieter WiedenmayerChristoph HoenkeKlaus Rudolf
    • A61K31/538A61K31/536C07D413/12C07D413/14
    • C07D265/36C07D413/12
    • A compound of formula 1′″ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R2′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
    • 式1“'的化合物,其中:V是-CH 2 - , - NH-或-O-; R a和R b各自独立地为氢,C 1-4 - 烷基或卤素-C 1-4 - 烷基,或者R a和R b一起是C 2-5亚烷基桥,其中一个或多个氢原子任选被卤素取代; R 1和R 1'各自独立地为氢,C 1-6 - 烷基,C 3-6 - 环烷基,卤素-C 1-6 - 烷基,卤素-C 3-6环烷基或C 1-6亚烷基-C 3-6环烷基, 或者R1和R1'一起是C2-5亚烷基桥,其中一个或多个氢原子任选地被卤素取代; R 2,R 2',R 2“和R 2”各自独立地为氢,C 1-6 - 烷基,卤素-C 1-6亚烷基,OH,HO-C 1-6 - 亚烷基,-O-C 1-6 - 烷基,C 6-10 - 芳基,C 6-10 - 芳基-C 1-4 - 亚烷基,C 6-10 - 芳基-C 1-6 - 亚烷基-O,COOH,COOC 1-6 - 烷基,O-C 1-6亚烷基 - COOH,O-C 1-6亚烷基-COOC 1-6 - 烷基,NHSO 2 -C 1-6 - 烷基,CN,NH 2,NH-C 1-6 - 烷基,N(C 1-6 - 烷基)2,NO 2, C 1-6 - 烷基,SO 2 -C 1-6 - 烷基,SO-C 1-6 - 烷基,O(CO)C 1-6 - 烷基,CO C 1-6 - 烷基,NHCOC 1-6 - 烷基或卤素; 和n为0,1或2,或其光学异构体或其与药理学上可接受的酸的相应的酸加成盐,以及其作为药物组合物的用途,特别是用于治疗炎性和阻塞性呼吸道疾病。