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

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。