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    • 1. 发明公开
    • PYRIMIDINE DERIVATIVES
    • 嘧啶衍生物
    • EP1595869A1
    • 2005-11-16
    • EP04713192.5
    • 2004-02-20
    • KYOWA HAKKO KOGYO CO., LTD.
    • OHSHIMA, EtsuoMIYAMA, MotokiYANAGAWA, KojiARATAKE, SeijiMIKI, IchiroKOBAYASHI, KatsuyaSATO, TakashiKAWABE, AriTAGAYA, Miho
    • C07D239/42C07D401/04C07D401/14C07D405/14C07D409/14C07D417/14A61K31/506A61P29/00A61P37/06A61P37/08A61P43/00
    • C07D401/04
    • The present invention provides a pyrimidine derivative represented by Formula (I)
      [wherein Ar represents substituted or unsubstituted aryl, etc., R 1 represents -NR 2 R 3 (wherein R 2 represents a hydrogen atom or substituted or unsubstituted lower alkyl and R 3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, etc.), etc. A represents a single bond, Formula (III)
      (wherein m 1 represents an integer of 0 to 2, n 1 represents an integer of 0 to 4, a 1 represents a number ranging from 0 to a substitutable number, R 5 represents substituted or unsubstituted lower alkyl, etc. and each R 5 may be the same or different when a 1 is 2 or more), etc. and Q represents -NR 6 R 7 (wherein R 6 and R 7 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted heteroalicyclic group, etc.), a substituted or unsubstituted heteroalicyclic group, substituted or unsubstituted piperidin-4-ylamino, etc.], or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof which have anti-inflammatory activities, modulating activities on TARC and/or MDC functions and the like, and are useful for treating and/or preventing diseases which is related to T cells such as allergic diseases, autoimmune diseases, transplant rejection, etc.
    • 本发明提供由式(I)表示的嘧啶衍生物[其中Ar表示取代或未取代的芳基等,R 1表示-NR 2 R 3(其中R 2表示氢原子或取代或未取代的低级烷基,并且R 3表示取代或未取代的低级烷基 ,取代或未取代的芳烷基等)等.A表示单键,式(III)(式中,m1表示0〜2的整数,n1表示0〜4的整数,a1表示0〜 可取代的数,R5表示取代或未取代的低级烷基等,并且当a1为2或更大时,每个R5可以相同或不同),并且Q表示-NR6R7(其中R6和R7可以相同或不同,并且 各自表示氢原子,取代或未取代的杂脂环基等),取代或未取代的杂脂环基,取代或未取代的哌啶-4-基氨基等]或它们的季铵盐,或 其具有抗炎活性,调节对TARC和/或MDC功能等的活性,并且可用于治疗和/或预防与T细胞有关的疾病,例如变应性疾病,自身免疫疾病,移植排斥 等等