MEDICAL COMPOSITION CONTAINING NITROETHENEAMINE DERIVATIVE OR SALT THEREOF AS ACTIVE CONSTITUENT
申请人:ISHIHARA SANGYO KAISHA, LTD.
公开号:EP1116486A1
公开(公告)日:2001-07-18
The present invention provides a medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I):
wherein R1 is hydrogen, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, or cyano; each of R2 and R3 is hydrogen, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group, or -A-R7 (A is S, SO, SO2, SO3, CO or CO2, and R7 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic group) ; or R2 and R3 may form N=CR8R9 (each of R8 and R9 is hydrogen, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclic, alkoxy or aryloxy group, cyano, nitro, or -A-R7 (A and R7 are as defined above); each of R4 and R5 is hydrogen, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclic, alkoxy, amino or aryloxy group, -A-R7 (A and R7 are as defined above), cyano, ester, or a hydroxyl group; or R4 and R5 may form N=CR8R9 (R8 and R9 are as defined above); R6 is hydrogen, nitro, cyano, -A-R7 (A and R7 are as defined above), an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclic, alkoxy or amino group, or halogen; and further R1, R2, R3, R4 and R5 may form a ring containing or not containing a hetero atom; or a salt thereof.
本发明提供了一种医疗组合物,其活性成分含有由式(I)表示的硝基乙烯胺衍生物:
其中 R1 是氢、任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基或杂环基团或氰基;R2 和 R3 各为氢、任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基或杂环基团,或 -A-R7 (A 为 S、SO、SO2、SO3、CO 或 CO2,R7 为氢或任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基或杂环基团);或 R2 和 R3 可形成 N=CR8R9 (R8 和 R9 各为氢、任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基、杂环基、烷氧基或芳氧基、氰基、硝基或-A-R7(A 和 R7 如上定义);R4 和 R5 各自为氢、任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基、杂环基、烷氧基、氨基或芳氧基、-A-R7(A 和 R7 如上定义)、氰基、酯或羟基;或 R4 和 R5 可形成 N=CR8R9 (R8 和 R9 如上定义);R6 是氢、硝基、氰基、-A-R7(A 和 R7 如上定义)、任选取代的烷基、烯基、炔基、环烷基、环烯基、芳基、杂环基、烷氧基或氨基,或卤素;此外,R1、R2、R3、R4 和 R5 可形成含有或不含有杂原子的环;或其盐。