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    • 3. 发明申请
    • 新規ウラシル誘導体及びその医薬用途
    • 新型尿嘧啶衍生物及其药物用途
    • WO2004026842A1
    • 2004-04-01
    • PCT/JP2003/011859
    • 2003-09-17
    • 住友製薬株式会社井上 善文磯部 義明戸辺 雅則磯部 真一
    • 磯部 義明戸辺 雅則磯部 真一
    • C07D239/54
    • C07D239/545A61K31/513C07D405/06C07D405/12C07D405/14
    • It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R represents hydrogen or optionally substituted C1-6 alkyl; R represents a group of the following general formula (II) or (III): (II) (III) (wherein m is 0 or 1; n is an integer of from 1 to 3; Y represents OH or NH2; and a dotted line shows a binding position), provided that when R is a group of the general formula (III), X represents NHCO or NHCH2; R and R independently represent each hydrogen or C1-6 alkyl; and Ar represents phenyl substituted by C1-6 alkyl at the o- and m-positions, optionally substituted heteroaryl or a bicyclic aromatic group; its pharmaceutically acceptable salt, and a remedy containing the above uracil derivative or its pharmaceutically acceptable salt as the active ingredient for, in particular, allergic diseases relating to a type IV allergic reaction, i.e., a novel compound useful in treating diseases in which a type IV allergic reaction participates and a remedy for allergic diseases containing the same as the active ingredient.
    • 旨在提供由以下通式(I)表示的尿嘧啶衍生物:(I)其中X表示选自NHCO,NHCH 2,CO,CONH和CH 2 NH的基团; R 1表示氢或任选取代的C 1-6烷基; R 2表示以下通式(II)或(III)的基团:(II)(III)(其中m为0或1; n为1至3的整数; Y表示OH或NH 2; 并且虚线表示结合位置),条件是当R 2为通式(III)的基团时,X表示NHCO或NHCH 2; R 3和R 4独立地表示每个氢或C 1-6烷基; 并且Ar表示在O和m位被C 1-6烷基取代的苯基,任选取代的杂芳基或双环芳基; 其药学上可接受的盐,以及含有上述尿嘧啶衍生物或其药学上可接受的盐作为特别是与IV型过敏反应有关的过敏性疾病的有效成分的药物,即用于治疗类型 IV过敏反应参与了与活性成分相同的过敏性疾病的补救措施。