申请人:FISONS CORPORATION
公开号:EP0540318A1
公开(公告)日:1993-05-05
Compounds of formula I,
wherein
A represents C=C, S or O;
Q represents a 5- or 6-membered unsaturated heterocyclic ring having a nitrogen atom in the position adjacent to the point of attachment, 0-3 further heteroatoms selected from N, O and S, and substituents R⁶ and R⁷;
R¹ represents H or C₁₋₆ alkyl;
R² represents H, C₁₋₆ alkyl, C₃₋₆ alkenyl, C₃₋₆ alkynyl, C₃₋₆ cycloalkyl or NH₂CH₂CO-; in addition, R¹ and R² taken together may form a C₃₋₅ alkylene chain;
R³ represents H, C₁₋₆ alkyl, C₃₋₆ alkenyl, C₃₋₆ alkynyl;
R⁴ and R⁵ independently represent H, OH, C₁₋₆ alkoxy, C₁₋₆ alkyl, halogen, trifluoromethyl or NR⁸R⁹;
R⁶ and R⁷ independently represent H, OH, C₁₋₆ alkoxy, C₁₋₆ alkyl, halogen, trifluoromethyl, C₁₋₆ hydroxyalkyl, amidino, CONH₂ or NR⁸R⁹;
in addition, R⁶ and R⁷ may independently represent O when substituted on N;
R⁸ and R⁹ independently represent H or C₁₋₆ alkyl;
with various provisos;
and pharmaceutically acceptable derivatives thereof;
are useful as pharmaceuticals, in particular in the treatment of neurological disorders.
式 I 的化合物、
其中
A 代表 C=C、S 或 O;
Q 代表 5 或 6 元不饱和杂环,该杂环在邻近连接点的位置有一个氮原子,0-3 个选自 N、O 和 S 的杂原子,以及取代基 R⁶ 和 R⁷;
R¹ 代表 H 或 C₁₋₆ 烷基;
R² 代表 H、C₁₋₆ 烷基、C₃₋₆ 烯基、C₃₋₆ 炔基、C₃₋₆ 环烷基或 NH₂CH₂CO-;此外,R¹ 和 R² 合在一起可形成 C₃₋₅亚烷基链;
R³ 代表 H、C₁₋₆ 烷基、C₃₋₆ 烯基、C₃₋₆ 炔基;
R⁴ 和 R⁵ 各自代表 H、OH、C₁₋₆ 烷氧基、C₁₋₆ 烷基、卤素、三氟甲基或 NR⁸R⁹;
R⁶ 和 R⁷ 独立地代表 H、OH、C₁₋₆ 烷氧基、C₁₋₆ 烷基、卤素、三氟甲基、C₁₋₆ 羟烷基、脒基、CONH₂ 或 NR⁸R⁹;
此外,当 R⁶ 和 R⁷ 被 N 取代时,可独立地代表 O;
R⁸ 和 R⁹ 独立地代表 H 或 C₁₋₆ 烷基;
具有各种但书;
及其药学上可接受的衍生物;
可用作药物,特别是用于治疗神经系统疾病。