Amino acid derivatives, process for the preparation thereof and pharmaceutical composition comprising the same
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0285085A2
公开(公告)日:1988-10-05
An amino acid derivative of the formula:
in which
R¹ is hydrogen, lower alkyl, halo(lower)alkyl or aryl
R² is hydrogen, hydroxy or protected hydroxy,
R³ is hydrogen,
R⁴ is lower alkyl, amino(lower)alkyl, carboxy(lower)alkyl, aminocarboxy(lower)alkyl, protected amino(lower)alkyl or protected amino-carboxy(lower)alkyl,
R⁵ is hydrogen or lower alkyl, and
R² and R³ may combine to be oxo, and its pharmaceutical acceptable salt, having anti-tumor activity a process for preparation thereof and pharmaceutical compositions comprising the same.
一种氨基酸衍生物,其式如下
其中
R¹ 是氢、低级烷基、卤代(低级)烷基或芳基
R² 是氢、羟基或受保护的羟基、
R³ 是氢
R⁴ 是低级烷基、氨基(低级)烷基、羧基(低级)烷基、氨基羧基(低级)烷基、受保护氨基(低级)烷基或受保护氨基羧基(低级)烷基、
R⁵ 是氢或低级烷基,以及
R² 和 R³ 可结合为氧代,以及具有抗肿瘤活性的其药用可接受盐及其制备工艺和由其组成的药物组合物。