公开(公告)号：EP0285085A3

公开(公告)日：1990-05-16

申请号：EP88105058.7

申请日：1988-03-29

申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： Okuhara, Masakuni ,  Goto, Toshio ,  Ezaki, Masami ,  Tanaka, Miho ,  Takase, Shigehiro ,  Nakajima, Hidenori ,  Hirai, Hideo ,  Katayama, Akira

IPC分类号： C07C113/00 ,  C12P13/00 ,  A61K31/215

CPC分类号： C12P13/04 ,  C07C245/18 ,  C12P13/00 ,  Y10S435/886

摘要： 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.

公开(公告)号：EP0285085A2

公开(公告)日：1988-10-05

申请号：EP88105058.7

申请日：1988-03-29

申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： Okuhara, Masakuni ,  Goto, Toshio ,  Ezaki, Masami ,  Tanaka, Miho ,  Takase, Shigehiro ,  Nakajima, Hidenori ,  Hirai, Hideo ,  Katayama, Akira

IPC分类号： C07C113/00 ,  C12P13/00 ,  A61K31/215

CPC分类号： C12P13/04 ,  C07C245/18 ,  C12P13/00 ,  Y10S435/886

摘要： 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.

摘要翻译： 氢其中R <1>是，低级烷基，卤代（低级）烷基或芳基 - [R <2>为氢，羟基或保护的羟基，R <3>是氢，R：下式的氨基酸衍生物 <4>被低级烷基，氨基（低级）烷基，羧基（低级）烷基，氨基羧基（低级）烷基，保护的氨基（低级）烷基或保护的氨基羧基（低级）烷基，R <5>是氢或低级烷基 和R <2>和R <3>可以组合成氧代基，和其药学上可接受的盐，其具有抗肿瘤活性的其制备和药物组合物包含相同的处理。