申请人:MITSUBISHI CHEMICAL CORPORATION
公开号:EP0721930A1
公开(公告)日:1996-07-17
Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof.
R1 to R5: a hydrogen atom, -OR9 (R9: a hydrogen atom, a C1-C5 alkyl group, etc.), etc.,
R6: a hydrogen atom, a C1-C5 alkyl group, etc.,
R7: a hydrogen atom, a cyano group, a C1-C5 alkyl group, -SOqR15 (q: 0, 1, 2, R15: a thienyl group, a phenyl group, etc.) etc.,
R8: a cyano group, -CR22R23X (R22, R23: a hydrogen atom, a C1-C5 alkyl group, etc., X: -NR24R25 (R24, R25: a C1-C5 alkyl group, etc., an alkylene group by combining, etc.)), etc.
The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.
本发明公开了由下式(I)代表的苯甲酰
乙烯衍
生物或其盐。
R1 至 R5:氢原子、-OR9(R9:氢原子、C1-C5 烷基等)等、
R6:氢原子、C1-C5 烷基等、
R7:氢原子、
氰基、C1-C5 烷基、-SOqR15(q:0、1、2,R15:
噻吩基、苯基等)等、
R8:
氰基,-C
R22R23X(
R22、R23:氢原子、C1-C5 烷基等,X:-NR24R25(R24、R25:C1-C5 烷基等,通过组合为亚烷基等))等。
本发明的苯甲酰
乙烯衍
生物具有强效的
酪氨酸激酶抑制活性和癌细胞生长抑制活性。本发明的
酪氨酸激酶
抑制剂可用作抗癌剂。