公开(公告)号：EP0696586A1

公开(公告)日：1996-02-14

申请号：EP94913822.6

申请日：1994-04-26

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： NODA, Ichio ,  IWATA, Masahiro ,  SAKAMOTO, Shuichi ,  KOSHIYA, Kazuo ,  MORITA, Takuma ,  KOHARA, Atsuyuki

IPC分类号： C07D307/52 ,  C07D333/20 ,  C07D333/24 ,  C07D409/06 ,  C07D413/06 ,  C07D407/06 ,  A61K31/34 ,  A61K31/40 ,  A61K31/445 ,  A61K31/55

CPC分类号： C07D409/06 ,  C07D307/52 ,  C07D307/54 ,  C07D333/20 ,  C07D333/24 ,  Y02P20/55

摘要： A serine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having an anti-PCP(phencyclidine) activity and being useful as a psychotropic, wherein X represents sulfur or oxygen; Y represents nitrogen or CH; R¹ and R² represent each independently hydrogen, lower alkyl or an amino-protecting group, or R¹ and R² may be combined together to form 4- to 9-membered nitrogenous cycloalkyl; R³ represents hydrogen, carboxy, protected carboxy, aralkyl, or lower alkyl which may be hydroxylated; R⁴ represents hydrogen or hydroxy; R⁵ represents hydrogen or lower alkyl; A represents lower alkylene; B represents (1) an (un)saturated 4-to 10-membered nitrogenous cycloalkyl group which may be substituted by lower alkyl or aralkyl, or (2) a bicyclic nitrogenous hydrocarbon ring group comprising a 4- to 8-membered nitrogenous cycloalkyl group and a benzene ring fused together; and ... represents a single or a double bond.

摘要翻译： 由通式（I）表示的丝氨酸衍生物或其药学上可接受的盐，具有抗PCP（苯环利定）活性，可用作精神药物，其中X表示硫或氧; Y表示氮或CH; R 1和R 2各自独立地表示氢，低级烷基或氨基保护基，或者R 1和R 2可以组合在一起形成4-至9-元含氮环烷基; R 3表示氢，羧基，保护的羧基，芳烷基或可被羟基化的低级烷基; R 4表示氢或羟基; R 5表示氢或低级烷基; A表示低级亚烷基; B表示（1）可被低级烷基或芳烷基取代的（未）饱和的4至10元含氮环烷基，或（2）包含4-至8-元含氮环烷基的双环含氮环烃基 和苯环稠合在一起; 和...表示单键或双键。