公开(公告)号：EP1486501A4

公开(公告)日：2006-03-22

申请号：EP03710430

申请日：2003-03-19

申请人： ASTELLAS PHARMA INC

发明人： ITAHANA HIROTSUNE ,  FUJIYASU JIRO ,  HAYASHIBE SATOSHI ,  WATANABE TOSHIHIRO ,  OKADA MASAMICHI ,  TOYA TAKASHI

IPC分类号： A61K31/429 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D513/04

CPC分类号： A61K31/429 ,  A61K31/5377 ,  C07D513/04

摘要： A novel aminomethyl-substituted thiazolobenzimidazole derivative represented by the following general formula (I) or a salt thereof. The derivative or salt has metabotropic glutamate receptor activity, has excellent oral activity, and is useful as a medicine. (I) (In the formula, R1 represents oxygenic saturated heterocycle, etc.; Alk1 represents lower alkylene; m is 0 or 1; Alk2 represents lower alkylene optionally substituted by oxo; n is 0 or 1; X represents a bond, oxygen, sulfur, or NR5; R3 represents hydrogen, etc.; and R2, R4, R5, R6, and R7 are the same or different and each represents hydrogen, etc.; provided that when X is a bond and n is 1, then R3 represents neither lower alkyl nor lower halogenoalkyl, and when m is 1, R1 is OH or OMe, Alk1 is C1-3 alkylene, and either 1) X is a bond, n is 1, and R3 is hydrogen or 2) X is a bond, n is 0, and R3 is cyclohexane, then R4 represents a group other than Me.)