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    • 6. 发明申请
    • BENZODIAZEPINE DERIVATIVES AS GABA A RECEPTOR MODULATORS
    • 作为GABA受体调节剂的苯二氮卓衍生物
    • WO0240487A3
    • 2002-09-26
    • PCT/EP0112887
    • 2001-11-08
    • HOFFMANN LA ROCHE
    • MASCIADRI RAFFAELLOTHOMAS ANDREW WILLIAMWICHMANN JUERGEN
    • A61K31/55A61K31/5517A61P25/00A61P25/28A61P43/00C07D487/14
    • C07D487/14
    • The present invention relates to compounds of formula (I), wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, trifluoromethyl, trifluoromethoxy or lower alkylthio; R is -C(O)O-lower alkyl, isoxazol, 1,2,4-oxadiazol-3-yl or 1,2,4-oxadiazol-5-yl, which rings may be substituted by lower alkyl, trifluoromethyl or cycloalkyl; R is hydrogen, lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-halogen, -(CH2)n-pyridin-4-yl, or -(CH2)n-phenyl, wherein the phenyl ring may be substituted by one or two substituents selected from the group consisting of lower alkoxy, halogen, -SO2CH3, phenyl, OCF3, nitro, CF3, -NR2, or is -(CH2)n-indolyl, optionally substituted by lower alkyl or lower alkoxy, or is pyrrolidinyl-5-oxo, -C(O)-NR2, -(CH2)n-OH, -(CH2)n-NR2 or -(CH2)n-benzo[1,3]dioxole; R is hydrogen or lower alkyl; and n is 0, 1, 2 or 3; and to their pharmaceutically acceptable acid addition salts. These compounds have a good affinity to the GABA A alpha 5 receptor and they are therefore useful for the treatment of diseases, related to this receptor.
    • 本发明涉及式(I)化合物,其中R 1是氢,卤素,低级烷基,低级烷氧基,羟基,氰基,三氟甲基,三氟甲氧基或低级烷硫基; R 2是-C(O)O-低级烷基,异恶唑,1,2,4-恶二唑-3-基或1,2,4-恶二唑-5-基,该环可以被低级烷基取代, 三氟甲基或环烷基; (CH 2)n - 卤素, - (CH 2)n - 吡啶-4-基或 - (CH 2)n - 苯基,其中苯基 环可以被一个或两个选自低级烷氧基,卤素,-SO 2 CH 3,苯基,OCF 3,硝基,CF 3,-NR 2或是 - (CH 2)n - 吲哚基的取代基取代,任选被低级烷基或 低级烷氧基或吡咯烷基-5-氧代-C(O)-NR2, - (CH2)n-OH, - (CH2)n-NR2或 - (CH2)n-苯并[1,3] R是氢或低级烷基; 并且n为0,1,2或3; 及其药学上可接受的酸加成盐。 这些化合物对GABA Aα5受体具有良好的亲和力,因此它们可用于治疗与该受体有关的疾病。