Bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them
申请人:ZENYAKU KOGYO KABUSHIKI KAISHA
公开号:EP0140327A2
公开(公告)日:1985-05-08
Disclosed are novel bis-dioxopiperazine derivatives and non-toxic salts thereof, process for their preparation, antitumor agents comprising them and compositions containing them.
The bis-dioxopiperazine derivatives are represented by the following general formula (I):
wherein R represents an alkyl radical having 1 to 17 carbon atoms, a cycloalkyl radical having 3 to 7 carbon atoms, a lower alkyl radical having a substituent or substituents selected from the group consisting of halogeno, carboxy, alkoxycarbonyl having 2 to 5 carbon atoms, lower alkoxy, substituted or unsubstituted phenoxy, naphthyloxy, substituted or unsubstituted phenylthio, substituted or unsubstituted phenyl and naphthyl, a substituted or unsubstituted phenyl lower alkenyl radical, a substituted or unsubstituted phenyl radical, a naphthyl radical, a heterocyclic radical selected from the group consisting of pyridyl, furyl and thienyl, an alkoxy radical having 1 to 8 carbon atoms, a substituted or unsubstituted phenyl lower alkoxy radical, or a substituted or unsubstituted phenoxy radical. A substituent or substituents on R may be selected from the group consisting of lower alkyl, halogeno, lower alkoxy, acyloxy having 2 to 5 carbon atoms, methylenedioxy, carboxy, amino, methanesulfonylamino and nitro. The above- mentioned "lower alkyl", "lower alkoxy" and "lower alkenyl" respectively refer to alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and alkenyl having 2 to 4 carbon atoms.
本发明公开了新型双-二氧代哌嗪衍生物及其无毒盐、制备工艺、包含它们的抗肿瘤药物和含有它们的组合物。
双-二氧代哌嗪衍生物由以下通式(I)表示:
其中 R 代表具有 1 至 17 个碳原子的烷基、具有 3 至 7 个碳原子的环烷基、具有一个或 多个取代基的低级烷基,取代基选自由卤素、羧基、具有 2 至 5 个碳原子的烷氧羰基、低 级烷氧基、取代或未取代的苯氧基、萘氧基、取代或未取代的苯硫基、取代或未取代的苯基硫 基、取代或未取代的苯基硫醚、取代或未取代的苯基硫醚、取代或未取代的苯基硫醚、取代或未 取代的苯基硫醚、取代或未取代的苯基硫醚、取代或未取代的苯基硫醚、取代或未取代的苯基和萘基、取代或未取代的苯基低级烯基、取代或未取代的苯基、萘基、选自吡啶基、呋喃基和噻吩基组成的杂环基、具有 1 至 8 个碳原子的烷氧基、取代或未取代的苯基低级烷氧基或取代或未取代的苯氧基。R 上的一个或多个取代基可选自由低级烷基、卤素、低级烷氧基、具有 2 至 5 个碳原子的酰氧基、亚甲基二氧基、羧基、氨基、甲磺酰氨基和硝基组成的组。上述 "低级烷基"、"低级烷氧基 "和 "低级烯基 "分别指具有 1 至 4 个碳原子的烷基、具有 1 至 4 个碳原子的烷氧基和具有 2 至 4 个碳原子的烯基。