公开(公告)号：EP1473289A1

公开(公告)日：2004-11-03

申请号：EP02783612.1

申请日：2002-11-25

申请人： Sankyo Company, Limited

发明人： Meguro, Masaki, c/o SANKYO COMPANY, Ltd. ,  Oda, Tomiichiro, c/o SANKYO COMPANY, Ltd. ,  Nakagami, Yasuhiro, c/o SANKYO COMPANY, Ltd. ,  Marumoto, Shinji, c/o SANKYO COMPANY, Ltd. ,  Koyama, Kazuo, c/o SANKYO COMPANY, Ltd. ,  Kaneko, Isao, c/o SANKYO COMPANY, Ltd.

IPC分类号： C07D237/20 ,  C07D239/48 ,  C07D239/50 ,  C07D251/18 ,  C07D251/52 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D239/48 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  C07D237/20 ,  C07D237/22 ,  C07D239/50 ,  C07D241/20 ,  C07D251/18 ,  C07D251/48 ,  C07D251/52 ,  C07D251/70

摘要： The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors:
(where, R 1 and R 2 are H or alkyl; Z 1 and Z 2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z 3 is alkoxy, SH, alkylthio, NH 2 , mono- or di-alkylamino, OH or halogeno; Z 4 and Z 5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

摘要翻译： 本发明涉及预防或治疗药用于治疗阿尔茨海默氏病，或淀粉样蛋白纤丝的形成抑制剂，其包括通式（I）的化合物作为活性成分低于或其药理学上允许的盐; 并因此具有特定的取代基，或它们的药理学上允许的盐，其是作为预防或治疗药用于治疗阿尔茨海默病有价值的，或作为淀粉样蛋白纤丝的形成抑制剂含氮杂芳基衍生物：（其中R <1>和R <2>是H或烷基; Z <1>和Z <2>为H，烷基，烷氧基，卤代烷基或卤代; Z <3>为烷氧基，SH，烷硫基，NH 2，单 - 或二 - 烷基氨基，OH或 卤代; Z <4>和Z <5>是H或卤代;并且A是4,6-嘧啶-1,3-二基，1,3,5-三嗪-2,6-二基等）。