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    • 1. 发明申请
    • GLUCOPYRANOSYL-SUBSTITUTED BENZONITRILE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR MANUFACTURE
    • 含有这些化合物的葡萄糖苷取代的苯并噻吩衍生物,药物组合物,其制备方法及其制备方法
    • WO2007093610A1
    • 2007-08-23
    • PCT/EP2007/051411
    • 2007-02-14
    • BOEHRINGER INGELHEIM INTERNATIONAL GMBHBOEHRINGER INGELHEIM PHARMA GMBH & CO. KGECKHARDT, MatthiasEICKELMANN, PeterHIMMELSBACH, FrankSAUER, AchimTHOMAS, Leo
    • ECKHARDT, MatthiasEICKELMANN, PeterHIMMELSBACH, FrankSAUER, AchimTHOMAS, Leo
    • C07D309/10A61K31/351
    • C07D309/10C07H7/04
    • Glucopyranosyl-substituted benzonitrile derivative of formula (I) are disclosed, wherein R 3 denotes hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, iso-butyl, tert-butyl, 3-methyl-but-1-yl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, difluoromethyl, trifluoromethyl, pentafluoroethyl, 2-hydroxyl-ethyl, hydroxymethyl, 3-hydroxy-propyl, 2-hydroxy-2-methyl-prop-1 -yl, 3- hydroxy-3-methyl-but-1-yl, 1-hydroxy-1-methyl-ethyl, 2,2,2-trifluoro-1-hydroxy-1-methyl-ethyl, 2,2,2-trifluoro-1-hydroxy-1 -trifluoromethyl-ethyl, 2-methoxy-ethyl, 2-ethoxy-ethyl, hydroxy, methyloxy, ethyloxy, isopropyloxy, difluoromethyloxy, trifluoromethyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, (S)-tetrahydrofuran-3-yloxy, (R)-tetrahydrofuran-3-yloxy, tetrahydropyran-4-yloxy, 1-acetyl-piperidin-4-yloxy, 2-methyloxy-ethyloxy, methylsulfanyl, methylsulfinyl, methylsulfonyl, ethylsulfinyl, ethylsulfonyl, trimethylsilyl and cyano, or a derivative thereof wherein one or more hydroxyl groups of the β-D-glucopyranosyl group are acylated with groups selected from (C 1-18 -alkyl)carbonyl, (C 1-18 -alkyl)oxycarbonyl, phenylcarbonyl and phenyl-(C 1-3 -alkyl)-carbonyl; including tautomers, stereoisomers thereof or mixtures thereof; and physiologically acceptable salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
    • 公开了式(I)的吡喃葡糖基取代的苄腈衍生物,其中R 3表示氢,氟,氯,溴,碘,甲基,乙基,丙基,异丙基,丁基,仲丁基, 丁基,叔丁基,3-甲基 - 丁-1-基,环丙基,环丁基,环戊基,环己基,二氟甲基,三氟甲基,五氟乙基,2-羟基 - 乙基,羟甲基,3-羟基丙基,2-羟基-2- 甲基 - 丙-1-基,3-羟基-3-甲基 - 异丙基,1-羟基-1-甲基 - 乙基,2,2,2-三氟-1-羟基-1-甲基 - 乙基, 2,2,2-三氟-1-羟基-1-三氟甲基 - 乙基,2-甲氧基 - 乙基,2-乙氧基 - 乙基,羟基,甲氧基,乙氧基,异丙氧基,二氟甲氧基,三氟甲氧基,环丁氧基,环戊氧基,环己氧基,(S ) - 四氢呋喃-3-基氧基,(R) - 四氢呋喃-3-基氧基,四氢吡喃-4-基氧基,1-乙酰基 - 哌啶-4-基氧基,2-甲氧基 - 乙氧基,甲基硫烷基,甲基亚磺酰基,甲基磺酰基,乙基亚磺酰基,乙基磺酰基, 三甲基甲硅烷基和氰基,或其衍生物 其中所述β-D-吡喃葡糖基的一个或多个羟基用选自(C 1-18烷基)羰基的基团(C 1-18)酰化, - 烷基)氧羰基,苯基羰基和苯基 - (C 1-3 - 烷基) - 羰基; 包括互变异构体,其立体异构体或其混合物; 及其生理上可接受的盐。 根据本发明的化合物适用于治疗代谢性疾病。