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    • 1. 发明申请
    • COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF
    • 抑制甘油运输机及其用途的化合物
    • WO2007113309A3
    • 2008-09-12
    • PCT/EP2007053275
    • 2007-04-03
    • GLAXO GROUP LTDCOULTON STEVENGILPIN MARTINPORTER RODERICK ALAN
    • COULTON STEVENGILPIN MARTINPORTER RODERICK ALAN
    • C07C211/27A61K31/166A61K31/40A61K31/445A61P25/28C07C233/78C07D213/40C07D295/13
    • C07C211/27C07C233/78C07D213/40C07D295/13
    • Compounds of formula (I) and salts and solvates are provided wherein R 2 is selected from phenyl substituted with n R 1 groups, and pyridyl substituted with n R 1 groups; n = 0, 1 or 2; each R 1 is independently selected from the group consisting of halo, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkyl, haloC 1-4 alkoxy and cyano; R 3 is selected from hydrogen and C 1-2 alkyl; R 4 is selected from the group consisting of ethyl, n- propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R 3 and R 4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C 1-4 alkyl, and haloC 1-4 alkyl; R 12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R 13 is selected from hydrogen, chloro and trifluoromethyl; R 14 is selected from hydrogen, trifluoromethyl and chloro; R 15 is selected from hydrogen, chloro and trifluoromethyl; R 16 is selected from hydrogen, methyl, fluoro and chloro; R 12 , R 13 , R 14 , R 15 and R 16 not all simultaneously being hydrogen. Processes for the preparation and uses of the compounds as medicaments for treating disorders such as psychoses, dementia or attention deficit disorder are also disclosed.
    • 提供式(I)化合物及其盐和溶剂合物,其中R 2选自被n R 1基团取代的苯基,和被n R 1取代的吡啶基 组 n = 0,1或2; 每个R 1独立地选自卤素,C 1-4烷基,C 1-4烷氧基,卤代C 1 -C 4烷基, 1-4个C 1-4烷基,卤代C 1-4烷氧基和氰基; R 3选自氢和C 1-12烷基; R 4选自乙基,正丙基,异丙基,正丁基,异丁基和叔丁基; 或R 3和R 4与它们所连接的氮原子一起形成任选被一个或多个基团X取代的饱和5或6元杂环; 每个X独立地选自C 1-4烷基和卤代C 1-4烷基; R 12选自氢,氟,氯,溴,甲基和甲硫基; R 13选自氢,氯和三氟甲基; R 14选自氢,三氟甲基和氯; R 15选自氢,氯和三氟甲基; R 16选自氢,甲基,氟和氯; R 12,R 13,R 14,R 15和R 16不是 全部同时为氢。 还公开了用于制备和使用化合物作为治疗诸如精神病,痴呆或注意力缺陷障碍之类疾病的药物的方法。