公开(公告)号：EP0806416A1

公开(公告)日：1997-11-12

申请号：EP95941572.0

申请日：1995-12-26

申请人： TSUMURA & CO. ,  TSUMURA & CO. ,  Zhu, Dayuan ,  Tang, Xican ,  Lin, Jinlai ,  Zhu, Cheng ,  Shen, Jingkang ,  Wu, Guansong ,  Jiang, Shanhao ,  Yamaguchi, Takuji ,  Tanaka, Kazuhiro ,  Wakanatsu, Takeshi ,  Nishimura, Hiroaki

发明人： ZHU, Dayuan ,  TANG, Xican ,  LIN, Jinlai ,  ZHU, Cheng ,  SHEN, Jingkang ,  WU, Guansong ,  JIANG, Shanhao ,  YAMAGUCHI, Takuji c/o Tsumura & Co. ,  TANAKA, Kazuhiro ,  WAKANATSU, Takeshi c/o Tsumura & Co. ,  NISHIMURA, Hiroaki Tsumura & Co.

IPC分类号： C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D221/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is
or R'' and Y together form =CH; R is (C 1 -C 5 ) alkyl,
wherein n is 0 or 1, X is H, (C 1 -C 5 ) alkyl; (C 1 -C 5 ) alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis-(C 1 -C 5 ) alkyl; -(CH 2 ) m COOZ, wherein m=0-5, Z is H or (C 1 -C 5 ) alkyl; -CH=CH-G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl substituted by (C 1 -C 5 ) alkyl at the nitrogen atom; R' is H, (C 1 -C 5 ) alkyl, pyridoyl, benzoyl substituted by (C 1 -C 5 ) alkyloxy; R'' is H or (C 1 -C 5 ) alkyl; processes for their use as acetylcholinesterase inhibitor.

摘要翻译： 本发明涉及式（II）的新颖的石杉碱甲基衍生物，其中Y是或R“，Y一起形成= CH; R是（C1-C5）烷基，其中n是0或1，X是H，（C1-C5）烷基; （C1-C5）烷氧基; 硝基，卤素，羧基，烷氧基羰基，羟甲基，羟基，被双 - （C 1 -C 5）烷基取代的氨基; - （CH 2）m COOZ，其中m = 0-5，Z是H或（C1-C5）烷基; -CH = CH-G，其中G是苯基，呋喃基，羧基，烷氧基羰基; 和由（C1-C5）烷基在氮原子上取代的二氢或四氢吡啶基; R'是H，（C1-C5）烷基，吡啶基，（C1-C5）烷氧基取代的苯甲酰基; R“是H或（C 1 -C 5）烷基; 其用作乙酰胆碱酯酶抑制剂的方法。

公开(公告)号：EP0806416A4

公开(公告)日：1998-04-15

申请号：EP95941572

申请日：1995-12-26

申请人： TSUMURA & CO ,  ZHU DAYUAN ,  TANG XICAN ,  LIN JINLAI ,  ZHU CHENG ,  SHEN JINGKANG ,  WU GUANSONG ,  JIANG SHANHAO ,  YAMAGUCHI TAKUJI ,  TANAKA KAZUHIRO ,  WAKANATSU TAKESHI ,  NISHIMURA HIROAKI

发明人： ZHU DAYUAN ,  TANG XICAN ,  LIN JINLAI ,  ZHU CHENG ,  SHEN JINGKANG ,  WU GUANSONG ,  JIANG SHANHAO ,  YAMAGUCHI TAKUJI ,  TANAKA KAZUHIRO ,  WAKANATSU TAKESHI ,  NISHIMURA HIROAKI

IPC分类号： A61K31/435 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4748 ,  A61K36/18 ,  A61P21/00 ,  A61P25/28 ,  C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

CPC分类号： C07D401/06 ,  C07D221/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is (a), or R' and Y together form =CH; R is (C1-C5)alkyl, (b), (c), (d), wherein n is 0 or 1, X is H, (C1-C5)alkyl; (C1-C5)alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis -(C1-C5)alkyl; -(CH2mCOOZ, wherein m=0∩5, Z is H or (C1-C5)alkyl; -CH=CH-G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl1 substituted by (C1-C5)alkyl at the nitrogen atom; R' is H, (C1-C5)alkyl, pyridoyl, benzoyl substituted by (C1-C5)alkyloxy; R' is H or (C1-C5)alkyl; processes for their manufacture and their use as acetyl cholinesterase inhibitor.