公开(公告)号：EP1157989B1

公开(公告)日：2004-09-22

申请号：EP00906631.7

申请日：2000-03-02

申请人： Eisai Co., Ltd.

发明人： IIMURA, Yoichi ,  KOSASA, Takashi ,  YAMANISHI, Yoshiharu ,  SUGIMOTO, Hachiro ,  TAKEUCHI, Yoshio ,  SHIBATA, Tetsuo, Iyakudaishukusha 5-104 ,  SUZUKI, Emiko

IPC分类号： C07D211/32 ,  C07D401/06 ,  C07D405/06 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/4545 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D401/06 ,  C07D211/32

摘要： Novel compounds exhibiting an excellent acetylcholinesterase inhibiting effect, i.e., fluorides of 4-substituted piperidine derivatives as represented by general formula (I), pharmacologically acceptable salts of the same, and hydrates of both (exclusive of 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, pharmacologically acceptable salts of the same, and hydrates of both). In formula (I), wherein R1 is (II) or the like; and R2 is (III) (wherein A is a benzene ring or a heterocycle), or the like.

公开(公告)号：EP1316549A1

公开(公告)日：2003-06-04

申请号：EP00956886.6

申请日：2000-09-01

申请人： Eisai Co., Ltd.

发明人： TAKEUCHI, Yoshio ,  SHIBATA, Tetsuo ,  SUZUKI, Emiko ,  IIMURA, Yoichi ,  KOSASA, Takashi ,  YAMANISHI, Yoshiharu ,  SUGIMOTO, Hachiro

IPC分类号： C07D211/32 ,  A61K31/445 ,  A61P25/28 ,  A61P25/14 ,  A61P43/00

CPC分类号： A61K31/445

摘要： The present invention provides a novel compound which shows the excellent acetylcholinesterase inihibitory action and is useful as a medicament, especially as an agent for preventing, treating or improving various kinds of senile dementia, Alzheimer-type senile dementia, cerebrovascular dementia, attention deficit hyperactivity disorder etc., and a process for producing it.
Namely, it provides 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl] methylpiperidine represented by the formula:
or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供一种显示出优异的乙酰胆碱酯酶抑制作用的新化合物，可用作药物，特别是作为预防，治疗或改善各种老年性痴呆，阿尔茨海默氏老年性痴呆，脑血管性痴呆，注意缺陷多动障碍 等等，以及其生产方法。 即，它提供由下式表示的1-苄基-4-Ä（5,6-二甲氧基-2-茚基）-2-基甲基哌啶或其药学上可接受的盐，