公开(公告)号：EP1595869A1

公开(公告)日：2005-11-16

申请号：EP04713192.5

申请日：2004-02-20

申请人： KYOWA HAKKO KOGYO CO., LTD.

发明人： OHSHIMA, Etsuo ,  MIYAMA, Motoki ,  YANAGAWA, Koji ,  ARATAKE, Seiji ,  MIKI, Ichiro ,  KOBAYASHI, Katsuya ,  SATO, Takashi ,  KAWABE, Ari ,  TAGAYA, Miho

IPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/506 ,  A61P29/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

CPC分类号： C07D401/04

摘要： 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.

摘要翻译： 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