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    • 2. 发明公开
    • CYANOPYRROLIDINE DERIVATIVES
    • CYANOPYRROLIDINDERIVATE
    • EP1333025A4
    • 2004-03-24
    • EP01981047
    • 2001-11-09
    • TAISHO PHARMA CO LTD
    • FUKUSHIMA HIROSHIHIRATATE AKIRATAKAHASHI MASATOKAMEO KAZUYA
    • A61P3/10A61P29/00A61P31/18A61P35/04A61P37/02A61P43/00C07D207/16C07D401/06A61K31/40C07D401/12
    • C07D401/06C07D207/16Y02P20/55
    • Cyanopyrrolidine derivatives represented by the general formula (1) or pharmaceutically acceptable salts thereof: (1) wherein R1 is halogeno, hydroxyl, or the like, and R2 is hydrogen, halogeno, or the like, or alternatively R?1 and R2¿ are united to form oxo, hydroxyimino, or the like; R?3 and R4¿ are each hydrogen, halogeno, or the like, or alternatively R?3 and R4¿ are united to form oxo, hydroxyimino, or the like; X is oxygen or sulfur; Y is CR5R6- (wherein R?5 and R6¿ are each independently hydrogen, halogeno, or the like) or CR?7R8-CR9R10¿- (wherein R?7, R8, R9, and R10¿ are each independently hydrogen, halogeno, or the like, or alternatively R?7 and R9¿ together with the carbon atoms adjacent thereto form C¿3-8? cycloalkyl or the like); and Z is hydrogen, C1-10 alkyl, or the like, or alternatively Y and Z together with the nitrogen atom adjacent thereto form cyclic C2-10 amino or the like.
    • (1)代表的氰基吡咯烷衍生物或其药学上可接受的盐:(1)其中R1是卤代,羟基等,R2是氢,卤素等,或者R1和R2是 结合形成氧代,羟基亚氨基等; R 3和R 4各自为氢,卤素等,或者R 3和R 4结合形成氧代,羟基亚氨基等; X是氧或硫; Y是CR 5 R 6 - (其中R 5和R 6各自独立地是氢,卤素等)或CR 7 R 8 -CR 9 R 10 - (其中R 7,R 8,R 9和R 10各自独立地是氢,卤素 或者类似的,或者R7和R9与其相邻的碳原子一起形成C8-8环烷基等)。 并且Z是氢,C1-10烷基等,或者Y和Z与其相邻的氮原子一起形成环状的C2-10氨基或类似基团。