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    • 6. 发明申请
    • 2-アミノブタノール化合物及びその医薬用途
    • 2-氨基丁醇化合物及其用于医疗用途的方法
    • WO2007126042A1
    • 2007-11-08
    • PCT/JP2007/059150
    • 2007-04-27
    • 三菱ウェルファーマ株式会社城内 正壽中村 光治濱田 真以子菅原 邦夫
    • 城内 正壽中村 光治濱田 真以子菅原 邦夫
    • C07C217/64A61K31/135A61K31/145A61K31/381A61K31/661A61P37/06C07C225/10C07C323/32C07C323/38C07D333/22C07D333/34C07F9/09
    • C07F9/653C07C217/64C07C225/16C07C309/65C07C323/32C07C323/38C07C323/41C07D333/22C07D333/34C07F9/091
    • [PROBLEMS] To provide a novel compound having few adverse side-effects such as bradycardia and also having an excellent effect of reducing the number of lymphocytes in the peripheral blood. [MEANS FOR SOLVING PROBLEMS] Disclosed is a 2-aminobutanol compound represented by the general formula (I) shown below, a pharmaceutically acceptable acid addition salt thereof, or a hydrate or solvate of the compound or the acid addition salt. Also disclosed is a process for production of the 2-aminobutanol compound. (I) wherein R 1 represents a hydrogen atom or P(=O)(OH) 2 ; R 2 represents an alkyl having 1 to 4 carbon atoms which may be substituted by a hydroxyl group or a halogen atom; R 3 represents a hydrogen atom, a halogen atom, a cyano, an alkyl having 1 to 4 carbon atoms which may be substituted by a halogen atom, or an acyl having 2 to 5 carbon atoms which may be subsituted by a halogen atom; X represents an oxygen atom, a sulfur atom, a carbonyl or NR 4 (wherein R 4 represents a hydrogen atom or an alkyl having 1 to 4 carbon atoms; Ar 1 represents an arylene which may be substituted or a heteroarylene which may be substituted; and Ar 2 represents an aryl which may be substituted or a hateroaryl which may be subsituted, provided that, when X represents an oxygen atom, Ar 1 represents a phenylene and Ar 2 represents a phenyl group, the phenyl group corresponding to Ar 2 is substituted.
    • [问题]提供一种具有很少不良副作用的新型化合物,例如心动过缓,并且还具有减少外周血中淋巴细胞数量的优异效果。 解决问题的手段公开了由下述通式(I)表示的2-氨基丁醇化合物,其药学上可接受的酸加成盐或化合物或酸加成盐的水合物或溶剂合物。 还公开了2-氨基丁醇化合物的制备方法。 (I)其中R 1代表氢原子或P(= O)(OH)2; R 2表示可以被羟基或卤素原子取代的碳原子数1〜4的烷基, R 3表示氢原子,卤素原子,氰基,可以被卤素原子取代的具有1〜4个碳原子的烷基,或者可以具有2〜5个碳原子的酰基, 由卤素原子取代; X表示氧原子,硫原子,羰基或NR 4(其中R 4表示氢原子或具有1至4个碳原子的烷基; Ar 1 表示可以被取代的亚芳基或可被取代的亚杂芳基; Ar 2代表可以被取代的芳基或可以被取代的杂芳基,条件是当 X表示氧原子,Ar 1表示亚苯基,Ar 2表示苯基,对应于Ar 2的苯基被取代。