申请人:ISF SOCIETA PER AZIONI
公开号:EP0207680A2
公开(公告)日:1987-01-07
Compounds of Structure (1):
in which
R' is H, C1-5 alkyl (straight or branched), or phenyl;
W is a bond, -NHC.HR6CO- or -NHCHR6CONH-CHR7CO-, where R6 and R7, which can be the same or different are H or C1-6 alkyl (straight or branched);
R2 is H, C1-5 alkyl (straight or branched), aryl or a benzyl group optionally substituted by C1-5 alkyl (straight or branched), C1-4, alkoxy (straight or branched) or hydroxy;
R3 and R4, which can be the same or different, are H, C1-5 alkyl (straight or branched) or phenyl, or R3 and R4 can together form a 1,4-butylene or 1,5-pentylene group;
R6 is H or -CHR8CONR9R10, where R8, R9 and R'°, which can be the same or different, are H or C1-5 alkyl (straight or branched);
R" and R12, which can be the same or different, are H, C1-5 alkyl (straight or branched), or acyl or together with the nitrogen atom shown form a 2-oxo-pyrrolidino group optionally substituted in the 4-position by a hydroxy or C1-5 (straight or branched) alkoxy group, or a 5-oxo-1-imidazolidine group optionally substituted at the 2- position by one or two C1-5 alkyl groups or a 1,4-butylene or 1,5-pentylene group, or optionally substituted at the 4-position by C1-5 alkyl, or a pharmaceutically acceptable salt thereof, processes and intermediates for making them, pharmaceutical compositions containing them and their use as nootropic agents.
结构 (1) 的化合物:
其中
R' 是 H、C1-5 烷基(直链或支链)或苯基;
W 是键、-NHC.HR6CO- 或 -NHCHR6CONH-CHR7CO-,其中 R6 和 R7(可以相同或不同)是 H 或 C1-6 烷基(直链或支链);
R2 是 H、C1-5 烷基(直链或支链)、芳基或任选被 C1-5 烷基(直链或支链)、C1-4、烷氧基(直链或支链)或羟基取代的苄基;
R3 和 R4(可以相同或不同)是 H、C1-5 烷基(直链或支链)或苯基,或 R3 和 R4 可共同形成 1,4-丁烯或 1,5-戊烯基团;
R6 是 H 或 -CHR8CONR9R10,其中 R8、R9 和 R'° 可以相同或不同,是 H 或 C1-5 烷基(直链或支链);
R "和 R12(可以相同或不同)是 H、C1-5 烷基(直链或支链)或酰基,或与所示的氮原子一起形成 2-氧代吡咯烷基,可选择在 4 位被羟基或 C1-5(直链或支链)烷氧基取代、或 5-氧代-1-咪唑烷基,可选择在 2-位被一个或两个 C1-5 烷基或 1,4-丁烯或 1,5-戊烯基取代,或可选择在 4-位被 C1-5 烷基取代,或其药学上可接受的盐、制造它们的工艺和中间体、含有它们的药物组合物,以及它们作为促智剂的用途。