公开(公告)号：EP1752452A4

公开(公告)日：2010-07-14

申请号：EP05745730

申请日：2005-06-02

申请人： ASTELLAS PHARMA INC

发明人： HIRANO MASAAKI ,  KAWAMINAMI EIJI ,  KINOYAMA ISAO ,  MATSUMOTO SHUNICHIRO ,  OHNUKI KEI ,  OBITSU KAZUYOSHI ,  KUSAYAMA TOSHIYUKI

IPC分类号： C07D235/12 ,  A61K31/4184 ,  A61K31/4439 ,  A61P5/08 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D409/06

CPC分类号： C07D401/06

公开(公告)号：EP1864976A4

公开(公告)日：2008-05-07

申请号：EP06730589

申请日：2006-03-30

申请人： ASTELLAS PHARMA INC

发明人： MATSUMOTO SHUNICHIRO ,  KINOYAMA ISAO ,  OSODA KAZUHIKO ,  YAMAMOTO HIROFUMI ,  HIRANO MASAAKI ,  OHNUKI KEI ,  KAWAMINAMI EIJI ,  SHIN TAKASHI ,  TAKAHASHI TATSUHISA ,  KUSAYAMA TOSHIYUKI ,  HISAMICHI HIROYUKI ,  SHIMADA ITSURO ,  KOIKE TAKANORI

IPC分类号： C07D235/12 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61P13/08 ,  A61P35/00 ,  C07D403/06 ,  C07D409/14 ,  C07D413/10

CPC分类号： C07D235/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated proane-1,3-dion derivatives and, as a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by -SO2-R3 in a propane-1,3-dion derivative having 2-(1,3-dihydro-2H-benzimidazole-2-ylidene) has an excellent GnRH receptor antagonism and completed the invention. Because the compound of the invention has a potent GnRH receptor antagonism, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the invention has an excellent metabolic stability in human and few drug interactions, it has preferable characteristics as a pharmaceutical used for the diseases.