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    • 1. 发明授权
    • Phenyl-and phenylalkyl-substituted ethanolamines and ethylenediamines
    • 苯基和苯基烷基取代的乙醇胺和乙二胺
    • US06770636B2
    • 2004-08-03
    • US09912163
    • 2001-07-24
    • Klaus FuchsWerner StranskyMatthias GrauertAdrian CarterWolfram GaidaThomas WeiserHelmut Ensinger
    • Klaus FuchsWerner StranskyMatthias GrauertAdrian CarterWolfram GaidaThomas WeiserHelmut Ensinger
    • A61K3133
    • C07D295/125C07C211/35C07C217/48C07C2601/02C07C2601/14C07C2601/16C07D231/12C07D233/56C07D249/08C07D295/092
    • Compounds of formula 1, wherein: R1 is hydrogen, hydroxy, CF3, NO2, CN, halogen, C1-C8-alkyl, or C1-C8-alkoxy; R2, R3, and R4 independently of one another are hydrogen, C1-C8-alkyl, hydroxy, NO2, CN, C1-C8-alkoxyl, CF3, or halogen; R5 and R6 independently of one another are hydrogen or a group consisting of C1-C8-alkyl, C2-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkylene, C5-C8-cycloalkenyl, C5-C8-cycloalkenyl-C1-C6-alkylene, C6-C10-aryl, and C6-C10-aryl-C1-C6-alkylene, each optionally substituted by a group consisting of C1-C6-alkyl, C2-C6-alkenyl, halogen, C1-C6-alkyloxy, —NH2, —NH(C1-C4-alkyl), —N(C1-C4-alkyl)2, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, and CF3, or R5 and R6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, oxygen, and nitrogen, and optionally mono-, di-, or trisubstituted by a group consisting of C1-C4-alkyl, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, halogen, and benzyl; X is oxygen, —NH—, —N(CHO)—, —N(CO—C1-C6-alkyl), —N(C1-C6-alkyl), or —N(C3-C6-cycloalkyl-C1-C4-alkylene); and A is a group consisting of C1-C6-alkylene, C2-C6-alkenylene, and C3-C6-alkynylene, each optionally substituted by a group consisting of halogen, ═O, and hydroxy, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing certain diseases.
    • 式1的化合物,其中:R 1是氢,羟基,CF 3,NO 2,CN,卤素,C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基; R 2,R 3, 4>彼此独立地是氢,C 1 -C 8 - 烷基,羟基,NO 2,CN,C 1 -C 8 - 烷氧基,CF 3或卤素; R 5和R 6彼此独立地是氢或基团 由C 1 -C 8 - 烷基,C 2 -C 8 - 烯基,C 3 -C 8 - 炔基,C 3 -C 8 - 环烷基,C 3 -C 8 - 环烷基-C 1 -C 6亚烷基,C 5 -C 8 - 环烯基,C 5 -C 8 - 环烯基 - C 1 -C 6 - 亚烷基,C 6 -C 10 - 芳基和C 6 -C 10 - 芳基-C 1 -C 6亚烷基,各自任选被C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,卤素,C 1 -C 6 - 烷氧基,-NH 2,-NH(C 1 -C 4 - 烷基),-N(C 1 -C 4 - 烷基)2,羟基,= O,-COOH,-CO-OC 1 -C 4烷基,-CONH 2,-CONH C 1 -C 4烷基),-CON(C 1 -C 4 - 烷基)2和CF 3或R 5和R 6与氮原子一起为饱和或不饱和的5-,6-,7-或 任选地含有一个或两个由硫,氧和氮组成的另外的杂原子的8-元杂环基,以及任选的单 - ,二 - ,或被由C 1 -C 4 - 烷基,羟基,O,-COOH,-CO-OC 1 -C 4烷基,-CONH 2,-CONH(C 1 -C 4 - 烷基),-CON(C 1 -C 4) - 烷基)2,卤素和苄基; X是氧,-NH-,-N(CHO) - , - N(CO-C 1 -C 6烷基), - N(C 1 -C 6 - 烷基) (C 3 -C 6 - 环烷基-C 1 -C 4 - 亚烷基); 并且A是由C 1 -C 6亚烷基,C 2 -C 6亚烯基和C 3 -C 6亚炔基组成的基团,各自任选地被卤素,= O和羟基取代,或光学异构体,对映体,互变异构体, 游离碱或其药理学上可接受的酸加成盐; 制备此类化合物的方法; 其药物组合物及其在治疗或预防某些疾病中的用途。