公开(公告)号：EP1441732A2

公开(公告)日：2004-08-04

申请号：EP02802729.0

申请日：2002-11-08

申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： TSUTSUMI, Hideo,Fujisawa Pharmaceutic. Co., Ltd. ,  TABUCHI, Seiichiro,Fujisawa Pharmaceuti. Co.Ltd. ,  AKAHANE, Atsushi,Fujisawa Pharmaceutic. Co., Ltd ,  YASUDA, Hironobu,Fujisawa Pharmaceutic. Co.,Ltd. ,  OMORI, Hiroki,Fujisawa Pharmaceutic. Co., Ltd. ,  TEMMARU, KiyoshiFujisawa Pharmaceutic. Co., Ltd. ,  ZANKA, Atsuhiko,Fujisawa Pharmaceutic. Co., Ltd.

IPC分类号： A61K31/501 ,  C07D417/04 ,  C07D417/14 ,  C07D237/16 ,  A61P25/00

CPC分类号： C07D233/56 ,  C07D231/12 ,  C07D249/08 ,  C07D417/04 ,  C07D417/14

摘要： A thiazole derivative of the formula (I):wherein R is 1-optiona lly substituted-6-oxo-1,6-dihydro-3-pyridazinyl, R' is an optionally substituted phenyl, and R2 is hydrogen, a group of the formula (i): wherein R4 is hydrogen, lower alkyl or lower alkenyl, and R5 is hydrogen, optionally substituted lower alkyl, acyl, cyclo(lower)alkyl, lower alkenyl, optionally substituted aryl or heterocyclic, or a group of the formula (ii): wherein X is oxygen or sulfur, R8 is hydrogen or lower alkyl, R9 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, lower alkoxy or mono- or di-lower alkylamino or R?8 and R9¿ may be combine together to form optionally substituted saturated N-containing heterocyclic, or a salt thereof._The compounds are useful as Adenosine antagonists. The application also discloses an improved process for the preparation of pyridazinones (XII-1)