公开(公告)号：EP1552842A1

公开(公告)日：2005-07-13

申请号：EP03733302.8

申请日：2003-06-06

申请人： KYOWA HAKKO KOGYO CO., LTD.

发明人： ARAI, Hitoshi Kyowa Hakko Kogyo Co., Ltd. ,  MATSUMURA, Tsutomu Kyowa Hakko Kogyo Co., Ltd. ,  ISHIDA, Hiroshi Kyowa Hakko Kogyo Co., Ltd. ,  YAMAURA, Yosuke Kyowa Hakko Kogyo Co., Ltd. ,  ARATAKE, Seiji Kyowa Hakko Kogyo Co., Ltd. ,  OHSHIMA, Etsuo Kyowa Hakko Kogyo Co., Ltd. ,  YANAGAWA, Koji Kyowa Hakko Kogyo Co., Ltd. ,  MIYAMA, Motoki Kyowa Hakko Kogyo Co., Ltd. ,  SUZUKI, Koji Hakko Kogyo Co., Ltd ,  KAWABE, Ari Kyowa Hakko Kogyo Co., Ltd. ,  NAKANISHI, Satoshi Kyowa Hakko Kogyo Co., Ltd. ,  KOBAYASHI, Katsuya ,  SATO, Takashi Kyowa Hakko Kogyo Co., Ltd. ,  MIKI, Ichiro Kyowa Hakko Kogyo Co., Ltd. ,  UENO, Kimihisa Kyowa Hakko Kogyo Co., Ltd. ,  FUJII, Shinya Kyowa Hakko Kogyo Co., Ltd. ,  IWASE, Miho Kyowa Hakko Kogyo Co., Ltd.

IPC分类号： A61K35/00

CPC分类号： C07D263/58 ,  C07D471/04 ,  C07D487/04

摘要： [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m + n is 4 or less; R 1 represents NR 4 R 5 (wherein R 4 and R 5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R 2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, -C(=O)-, -SO 2 -, -OC(=O)- or the like; and R 3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like]
Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.

摘要翻译： 其中m和n可以相同或不同，各自表示1〜3的整数，其中m + n为4以下; R 1表示NR 4 R 5（其中R 4和R 5可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳烷基等 ）; R 2表示上述式（II），式（IV）等; A表示单键，-C（= O） - ，-SO 2 - ， - OC（= O） - 等; 和R 3表示取代或未取代的低级烷基，取代或未取代的环烷基，取代或未取代的芳烷基等。上式（I）表示的双环嘧啶衍生物或其季铵盐或其药学上可接受的盐 或其类似物。 它们具有对TARC和/或MDC的功能的抗炎活性或调节活性，并且可用于治疗和/或预防与T细胞相关的疾病，例如过敏性疾病，自身免疫疾病或移植排斥反应。